Patents & Patent Applications In The Public Domain
Mark Brian Anderson, PhD, RAC
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Dr. Mark Anderson brings over 20 years of experience in basic research
as a scientist, leader and mentor driving drugs, medical devices, biological and combination
products in multiple therapeutic areas. He is RAC Certified and brings his experience in the
sciences to the front line, currently working in regulatory affairs as a consultant. His contract consulting
expertise includes clinical development, formulations, and research in drug discovery and innovations in start-up,
mid-sized and large pharmaceutical companies. He has introduced "From Principle to Practice" the business
of science; bringing the principles of science methodology of drugs, biologic, medical devices from idea to clinical
practice. Contract consulting areas include the following;
AREAS Of EXPERTISE: cancer/oncology;
infectious diseases; neurology; adverse drug reactions; neurodegeneration; multiple kinase targets; antivirals, HIV, genetic,
epigenetic and metabolic targets; bacterial and fungal targets; thrombosis; endocrine; cardiovascular; inflammation, cell
adhesion, pulmonary, chemical biology, chemical proteomics, vascular disrupting and vascular targeting agents, tubulin agents,
Alzheimer's disease, and ischemia-reperfusion inhibitors.
OVERVIEW
OF INTELLECTUAL PROPERTIES: 100+ US &
international issued and pending patent applications covering novel therapeutic agents, HIV maturation inhibitors, novel agents
for treating HIV, novel antiviral (HIV) agents, blood brain barrier permeable anti-cancer agents, methods for treating brain
cancer, novel anti-tumor agents, caspase activators and inducers of apoptosis, Anti-infectives, Cardiovascular, Alzheimer's
disease (neurodegeneration), non-peptide GnRH agents, kinases, etc., additional IP pending.
Patents
2011 - Application number: 13/004,311;
Publication number: US 2011/0200619 A1; Filing date: Jan 11, 2011. Inventors: Mark B. Anderson, In Chul Kim. Pharmaceutical
Compounds as Cytotoxic Agents and Uses Thereof. Abstract: Disclosed are compounds effective as cytotoxic agents.
The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth
and spread of abnormal cells occurs.
2011 - Application number: 11/773,303; Publication number: US 2008/0004297
A1; Filing date: Jul 3, 2007; Issued patent: US 7,989,462 (Issue date Aug 2, 2011). Inventors: Sui Xiong Cai, Mark
B. Anderson, Adam Willardsen, Nilantha Sudath Sirisoma, Hong Zhang, Kazuyuki Suzuki. Compounds and Therapeutic Use
Thereof. Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases
and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions
in which uncontrolled growth and spread of abnormal cells occurs.
2010 - Application number: 12/780,828;
Publication number: US 2010/0292255 A1; Filing date: May 14, 2010. Inventors: Ashok C. Bajji, Se-Ho Kim, Rajendra
Tangallapally, Benjamin J. Markovitz, Richard Trovato, Mark B. Anderson, Daniel A. Wettstein, Mark D. Shenderovich.
Therapeutic Compounds and Their Use in Treating Diseases and Disorders. Abstract: The invention provides novel therapeutic
compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions
to treat diseases and disorders, such as cancer.
2010 - Application number: 12/794,300. Publication number:
US 2010/0240630 A1. Filing date: Jun 4, 2010. Inventors: Dange Vijay KUMAR, Kraig M. Yager, David A. Gerrish, Christophe
Hoarau, Mark B. Anderson. Compounds and Therapeutic Uses Thereof. Abstract: The invention relates to compounds,
pharmaceutical compositions and methods useful for treating viral infection.
2010 - Application number:
12/775,253; Publication number: US 2010/0216862 A1; Filing date: May 6, 2010. Inventors: Warren S. Weiner, Rachel
M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson. Novel pyrrole derivatives
are disclosed as Aβ42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by
the formation or accumulation of amyloid plaques comprising the Aβ42 peptide.
2010 - Application number: 12/719,672;
Publication number: US 2010/0184975 A1; Filing date: Mar 8, 2010. Inventors: Rachel Slade, Yevgeniya Klimova, Robert
J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz. Compounds for Alzheimer’s Disease. The invention provides novel compounds useful for the treatment
of neurodegenerative disorders including Alzheimer's disease and dementia.
2010 - Application number: 12/574,632;
Publication number: US 2010/0093773 A1; Filing date: Oct 6, 2009.
Inventors: Mark Laughlin, Mark B. Anderson,
Adam Willardsen, Chris Pleiman. Methods of Treating Cancer. Abstract: Disclosed is (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine
hydrochloride effective as a vascular disrupting agent. (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride
is useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs,
and in particular to its use in treating cancer.
2010 - Application number: 12/500,863; Publication number:
US 2010/0069383 A1; Filing date: Jul 10, 2009. Inventors: Mark B. Anderson, J. Adam Willardsen, Warren S. Weiner,
Ashantai Yungai, Robert J. Halter, Yevgeniya Klimova, Kazuyuki Suzuki, Matthew Reeder. Compounds and Therapeutical
Use Thereof. Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators
of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical
conditions in which uncontrolled growth and spread of abnormal cells occurs.
2010 - Application number:
12/500,449; Publication number: US 2010/0068197 A1; Filing date: Jul 9, 2009. Inventors: Mark B. Anderson, J. Adam
Willardsen, Warren S. Weiner, Kazuyuki Suzuki, Robert J. Halter, In Chul Kim, Matthew Reeder, Ashantai Yungai. Pharmaceutical
Compounds as Inhibitors of Cell Proliferation and The Use Thereof. Abstract: Disclosed are compounds of Formula I
effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions
in which uncontrolled growth and spread of abnormal cells occurs.
2010 - Application number: 12/057,140;
Patent number: 7714022; Filing date: Mar 27, 2008; Issue date: May 11, 2010. Inventors: Warren S. Weiner, Rachel
M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson. Novel pyrrole derivatives
are disclosed as Aβ42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by
the formation or accumulation of amyloid plaques comprising the Aβ42 peptide.
2010 - Application number: 11/773,293;
Publication number: US 2008/0020985 A1; Filing date: Jul 3, 2007; Issued patent: US 7,842,805 (Issue date Nov 30, 2010). Inventors:
Sui Xiong Cai, Mark B. Anderson, Adam Willardsen, Songchun Jiang, Robert J. Halter, Rachel Slade, Yevgeniya Klimova.
Pharmaceutical Compounds as Activators of Caspases and Inducers of Apoptosis. Abstract: Disclosed are 1-arylamino-phthalazines,
4-arylamino-benzo[d][1,2,3]triazines, and analogs thereof effective as activators of caspases and inducers of apoptosis. The
compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and
spread of abnormal cells occurs.
2010 - Application number: 11/696,526; Publication number: US 2008/0249135
A1; Filing date: Apr 4, 2007; Issued patent: US7678823 (Issue date Mar 16, 2010). Inventors: Rachel Slade, Yevgeniya
Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton
Zavitz. Compounds for Alzheimer’s Disease. Abstract: The invention provides novel compounds useful
for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia.
2009 - Application
number: 12/422,767; Publication number: US 2009/0275583 A1; Filing date: Apr 13, 2009. Inventors; Kraig Yager, In Chul Kim, Michael Saunders, David Gerrish,
Dange Vijay Kumar, Mark B. Anderson. Antiviral Compounds and Use Thereof. Abstract: The invention relates
ot compounds, pharmaceutical compositions and methods useful for treating viral infections.
2009 - Application
number: 11/993,519; Publication number: US 2009/0149429 A1; Filing date: Jun 22, 2006. Inventors: Esther Arranz Plaza, Kraig M. Yager, David Allen
Gerrish, Mark B. Anderson, In Chul Kim, Dange Vijay Kumar. Antiviral Compounds. Abstract: The invention relates
to compounds, pharmaceutical compositions and methods useful for treating viral infection.
2009 - Application number: 11/748,362; Patent number: 7595401; Filing date: May 14, 2007; Issue date: Sep 29, 2009. Inventors: Ashok C. Bajji, Se-Ho Kim,
Benjamin Markovitz, Richard Trovato, Rajendra Tangallapally, Mark B. Anderson, Daniel Wettstein, Mark Shenderovich, John A.
Vanecko. Therapeutic compounds and their use in cancer. Abstract: The invention relates to compounds of Formula
I for use in cancer.
2009 - WO/2009/065035
BAJJI, Ashok
C.; KIM, Se-Ho; TANGALLAPALLY, Rajendra; MARKOVITZ, Benjamin; TROVATO, Richard; ANDERSON, Mark B.; WETTSTEIN, Daniel; SHENDEROVICH,
Mark. Therapeutic Compounds And Their Use In Treating Diseases And Disorders. The invention provides novel
therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions
to treat diseases and disorders, such as cancer.
2008 - Patent Number: 2008097341 (application serial number US2007/074478)
Kraig
M. Yager, In Chul Kim, David Gerrish, Mark B. Anderson. ANTIVIRAL COMPOUNDS AND USE THEREOF. / COMPOSÉS ANTIVIRAUX
ET LEUR UTILISATION. The invention relates to compounds, pharmaceutical compositions and methods useful for treating
viral infection. L'invention concerne des composés, des compositions pharmaceutiques et des procédés
qui s'utilisent pour traiter une infection virale.
2008 - CIP of PCT/US06/000056
Cai, Sui Xiong; Anderson,
Mark B.; Willardsen, Adam; Sirisoma, Nilantha Sudath; Zhang, Hong; Suzuki, Kazuyuki. PREPARATION OF SUBSTITUTED QUINAZOLINAMINES
AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS. U.S. Pat. Appl. Publ. (2008), 50pp., Cont.-in-part of Appl.
No. PCT/US06/000056. CODEN: USXXCO US 2008004297 A1 20080103 CAN 148:121727 AN 2008:12280. (drug design, drug discovery, blood
brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics).
2007 - WO 2007095383
Walton, Ruth J.; Slade, Rachel M.; Willardsen, J. Adam; Weiner, Warren S.; Anderson,
Mark B.. PRODRUGS OF PH ALKANOIC ACIDS WITH ENHANCED DELIVERY TO THE BRAIN OR ACROSS THE BLOOD-BRAIN-BARRIER FOR TREATMENT
OF DEMENTIA. PCT Int. Appl. (2007), 56pp. CODEN: PIXXD2 WO 2007095383 A2 20070823 CAN 147:285038 AN 2007:941178.
PCT/US2007/004189. Abstract: The invention relates prodrugs of phenyl alkanoic acids. The prodrugs of the invention can enhance
and/or improve delivery of the phenyl alkanoic acid moiety to a desired target tissue. (drug design, drug discovery, blood
brain barrier, SAR, SXR, Alzheimer's, synthesis, bioavailable, drug delivery, pharmacokinetics).
2007 - WO 2007076161
Bajji, Ashok C.; Kim, Se-Ho; Trovato, Richard; Mchugh, Robert J.; Markovitz, Benjamin; Anderson,
Mark B.. PREPARATION OF OXAZOLE DERIVATIVES AS ANTIVIRAL AGENTS. PCT Int. Appl. (2007), 116pp. CODEN: PIXXD2
WO 2007076161 A2 20070705 CAN 147:143467 AN 2007:729694. PCT/US2006/049558. Abstract: Methods and pharmaceutical compositions
for treating and/or delaying the onset of viral infection are provided. The pharmaceutical compositions include compounds
having an oxazole core. Additionally, the compositions can be used to treat cardiovascular disorders and cancer. (drug design,
drug discovery, SAR, SXR, HIV, antiviral, synthesis).
2007 - WO 2007002411, CA 2609280
Arranz
Plaza, Esther; Yager, Kraig M.; Gerrish, David Allen; Anderson, Mark B.; Kim, In Chul; Kumar, Dange Vijay. ANTIVIRAL
COMPOUNDS. . International Application Number: PCT/US2006/024493. PCT Int. Appl. (2007), 91pp. CODEN:
PIXXD2 WO 2007002411 A1 20070104 CAN 146:100898 AN 2007:14669. 04.01.2007 C07J 53/00 PCT/US2006/024493 MYRIAD GENETICS, INC.
The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection. (drug design,
drug discovery, SAR, SXR, HIV, antiviral, synthesis).
2007 - US 20070299258, WO 2007134298
Bajji, Ashok C.; Kim, Se-Ho; Markovitz, Benjamin; Trovato, Richard; Tangallapally, Rajendra; Anderson, Mark
B.; Wettstein, Daniel; Shenderovich, Mark; Vanecko, John A. PREPARATION OF SUBSTITUTED
PURINAMINES AS ANTITUMOR AGENTS. PCT Int. Appl. (2007), 477pp. CODEN: PIXXD2 WO 2007134298 A2 20071122 CAN 148:11252
AN 2007:1332992. PCT/US2007/068899. Abstract: Compounds of the formula (I) (II) (III) in which A is chosen from a substituted
or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group. B is chosen from a substituted or unsubstituted aryl,
heteroaryl, heterocyclic, or carbocyclic group Rl is chosen from hydro, alkyl, aryl, heteroaryl, amino, halo, sulfur, and
thioalkyl. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, purine, pharmacokinetics,
ADME).
2007 - WO 2007038684, CA 2623558,
PCT/US2006/037903
Weiner, Warren S.; Slade,
Rachel M.; Klimova, Yevgeniya I.; Walton, Ruth J.; Anderson, Mark B.. PYRROLE DERIVATIVES AS THERAPEUTIC COMPOUNDS.
PYRROLE DERIVATIVES AS AMYLOID BETA 42-LOWERING AGENTS, THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS, AND USE IN THERAPY.
PCT Int. Appl. (2007), 84pp. CODEN: PIXXD2 WO 2007038684 A2 20070405 CAN 146:379817 AN 2007:384648. PCT/US2006/037903. Abstract:
Novel pyrrole derivatives are disclosed as Aβ42-lowering agents for the treatment and prevention of neurodegenerative
disorders characterized by the formation or accumulation of amyloid plaques comprising the Aβ42 peptide. (drug design,
drug discovery, blood brain barrier, SAR, SXR, Alzheimer's, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics,
ADME).
2006 - WO 2006135383
Bajji, Ashok; Morham, Scott; Anderson, Mark B.; McHugh, Robert J.; Trovato,
Richard; Weiner, Warren S.; Kim, Se-Ho. INDAZOLES: PREPARATION OF INDAZOLES FOR TREATING VIRAL INFECTION
AND OTHER DISEASES MEDIATED BY RHO KINASE. PCT Int. Appl. (2006), 221pp. CODEN: PIXXD2 WO 2006135383 A2 20061221
CAN 146:62713 AN 2006:1338316. PCT/US2005/027730. Abstract: Methods and pharmaceutical compositions for treating and/or delaying
the onset of viral infection are provided. The pharmaceutical compositions include compounds having an indazole core. Additionally,
the compositions can be used to treat cardiovascular disorders and cancer. (drug design, drug discovery, SAR, SXR, cancer,
tumor, synthesis, pharmacokinetics, pharmacodynamics, ADME).
2006 - WO 2006074223, CA 2593005
Cai, Sui Xiong; Anderson, Mark B.; Willardsen, Adam; Jiang, Songchun; Halter, Robert J.; Slade, Rachel; Klimova,
Yevgeniya. PHARMACEUTICAL COMPOUNDS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF.
International Application Number: PCT/US2006/000176. PCT Int. Appl. (2006), 97 pp. CODEN: PIXXD2 WO 2006074223 A2 20060713
CAN 145:145755 AN 2006:676927. Disclosed are 1-arylamino-phthalazines, 4-arylamino-benzo[d][1,2,3]triazines, and analogs thereof
effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment
of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. (drug design, drug discovery,
blood brain barrier, SAR, SXR, cancer, tumor, synthesis, pharmacokinetics, ADME).
2006 - US 20080051398, WO 2006074187, CA 2592971
Cai, Sui Xiong; Anderson, Mark B.; Willardsen, Adam; Sirisoma, Nilantha Sudath.
METHOD OF TREATING BRAIN CANCER. International Application Number: PCT/US2006/000122. PCT Int. Appl. (2006),
90 pp. CODEN: PIXXD2 WO 2006074187 A2 20060713 CAN 145:145733 AN 2006:675266. 13.07.2006 A61K 39/395 PCT/US2006/000122 MYRIAD
GENETICS, INC. Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers
of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled
growth and spread of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer. http://www.freepatentsonline.com/y2008/0051398.html (drug design, drug discovery, blood brain barrier, SAR, SXR,
cancer, tumor, pharmacokinetics, pharmacodynamics, ADME).
2006 - WO 2006074147, CA 2592900
Cai,
Sui Xiong; Anderson, Mark B.; Willardsen, Adam; Sirisoma, Nilantha Sudath; Zhang, Hong; Suzuki, Kazuyuki. NITROGEN
CONTAINING BICYCLIC COMPOUNDS AND THERAPEUTICAL USE THEREOF. International Application Number: PCT/US2006/000056.
13.07.2006 C07D 401/00 MYRIAD GENETICS, INC. Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators
of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical
conditions in which uncontrolled growth and spread of abnormal cells occurs. (drug design, drug discovery, SAR, SXR, cancer,
tumor, synthesis, pharmacokinetics).
2006
- WO 2006074147
Cai, Sui Xiong; Anderson,
Mark B.; Willardsen, Adam; Sirisoma, Nilantha Sudath; Zhang, Hong; Suzuki, Kazuyuki. PREPARATION OF 4-ARYLAMINO-QUINAZOLINES
AND THEIR ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS. PCT Int. Appl. (2006), 133 pp. CODEN: PIXXD2
WO 2006074147 A2 20060713 CAN 145:145736 AN 2006:678591. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis,
oral, bioavailable, pharmacokinetics).
2006
- WO 2006041874, CA 2582674, PCT/US2005/035747
Slade,
Rachel; Klimova, Yevgeniya; Halter, Robert J.; Yungai, Ashantai J.; Weiner, Warren S.; Walton, Ruth J.; Willardsen, Jon Adam;
Anderson, Mark B.; Zavitz, Kenton. COMPOUNDS FOR ALZHEIMER'S DISEASE. International Application Number: PCT/US2005/035747.
PCT Int. Appl. (2006), 300 pp. CODEN: PIXXD2 WO 2006041874 A2 20060420 CAN 144:412361 AN 2006:361235. 20.04.2006 C07D 209/04
MYRIAD GENETICS, INC. (drug design, drug discovery, blood brain barrier, SAR, SXR, Alzheimer's, synthesis, pharmacokinetics,
pharmacodynamics, ADME).
2006 - US 7101878,
WO 20040010033 (2004), WO00/20358
Anderson,
Mark Brian; Vazir, Haresh N.; Luthin, David Robert; Paderes, Genevieve Deguzman; Pathak, Ved P.; Christie, Lance Christopher;
Hong, Yufeng; Tompkins, Eileen Valenzuela; Li, Haitao; Faust, James. NON-PEPTIDE GNRH AGENTS, METHODS AND INTERMEDIATES
FOR THEIR PREPARATION. PCT/US2007/068899. Also see Appl. No. 9/763,216. PCT Filed Aug. 20, 1999, PCT No. PCT/US99/18790
§ 371(c)(1), (2), (4) Date Feb. 20, 2001, PCT Pub. No. WO00/20358, PCT Pub. Date Apr. 13, 2000. Abstract: Non-peptide
GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically
acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and
steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated.
Methods for synthesizing the compounds and intermediates useful in their preparation are also described. (drug design, drug
discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, bioavailable, pharmacokinetics, pharmacodynamics, ADME).
2006 - WO 2006074187
Cai, Sui Xiong; Anderson, Mark B.; Willardsen, Adam; Sirisoma, Nilantha Sudath.
PREPARATION OF 4-ARYLAMINO-QUINAZOLINES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS.
PCT Int. Appl. (2006), 90 pp. CODEN: PIXXD2 WO 2006074187 A2 20060713 CAN 145:145733 AN 2006:675266. (drug design, drug discovery,
blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics, ADME).
2005 - WO 20050250846, USPTO Application: 20050250846
Mark B. Anderson, Lance Christopher Christie,
Quyen-Quyen Thuy Do, Yufeng Hong, Haitao Li, Ranjan Jagath Rajapakse, Eric T. Sun, Eileen Valenzuela Tompkins, Jun Feng, Ved
P. Pathak. USPTO Application #: 20050250846. NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR
THEIR USE. Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are
described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating
mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression
of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation
are also described. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable,
pharmacokinetics, pharmacodynamics, ADME).
2005
- US 6903132
Anderson, Mark B.; Christie, Lance Christopher; Do, Quyen-Quyen Thuy; Feng, Jun; Hong, Yufeng;
Li, Haitao; Pathak, Ved P.; Rajapakse, Ranjan Jagath; Sun, Eric T.; Tompkins, Eileen Valenzuela. NON-PEPTIDE GNRH
AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE. Non-peptide GnRH agents capable of inhibiting the
effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs,
and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as
well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods
for synthesizing the compounds and intermediates useful in their preparation are also described. (drug design, drug discovery,
blood brain barrier, SAR, SXR, prodrugs, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics,
ADME).
2004 - US 20040053951
Christie, Lance C.; Anderson, Mark B.; Feng, Jun; Hong, Yufeng; Pathak, Ved P.; Rajapakse, Ranjan J.; Tompkins,
Eileen V.; Vazir, Haresh; Li, Haitao. NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR THEIR
USE. Pfizer Inc. No. 10364193 filed on 02/11/2003. Abstract: Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing
hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent
tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. United States Application
20040053951 A1. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis, pharmacokinetics, pharmacodynamics, ADME).
2004 - US 20040014787
Mark B. Anderson; Lance Christopher Christie, Ballwin; Quyen-Quyen Thuy Do; Jun Feng; Yufeng Hong, San; Haitao
Li, San Diego; Ved P. Pathak, San Diego; Ranjan Jagath Rajapakse; Eric T. Sun, San; Eileen Valenzuela Tompkins. US 20040014787A1.
2004/0014787 Al. NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE. Agouron
Pharmaceuticals, Inc. Appl. No.: 10/459,364. Filed: Jun. 11, 2003 Related U.S. Application Data. Provisional application No.
60/388,788, filed on Jun. 13, 2002. Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing
hormone are described. Such compounds and their pharmaceutically acceptable salts, pro- drugs, and active metabolites are
suitable for treating mammalian reproductive disorders and steroid hormone- dependent tumors as well as for regulating fertility,
where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in
their preparation are also described. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable,
pharmacokinetics, pharmacodynamics, ADME).
2004 - US 6833372
Christie, Lance C.; Anderson, Mark B.; Feng, Jun; Hong, Yufeng; Pathak,
Ved P.; Rajapakse, Ranjan J.; Tompkins, Eileen V.; Vazir, Haresh; Li, Haitao. NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL
COMPOSITIONS, AND METHODS FOR THEIR USE. Pfizer Inc. No. 10364193 filed on 02/11/2003 Non-peptide GnRH agents that
inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive
disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release
is indicated. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis, pharmacokinetics, ADME).
2003 - WO 2003106446, CA 2489252
Anderson, Mark Brian; Christie, Lance Christopher; Do, Quyen-Quyen Thuy;
Feng, Jun; Hong, Yufeng; Li, Haitao; Pathak, Ved Prakash; Rajapakse, Ranjan Jagath; Sun, Eric Tak On; Tompkins, Eileen Valenzuela.
NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE. (PREPARATION OF FURANCARBONYLHYDRAZINES
AS INHIBITORS OF GONADOTROPIN-RELEASING HORMONE.) 24.12.2003 A61K 31/341 PCT/IB2003/002379 PFIZER INC. PCT Int. Appl.
(2003), 115 pp. CODEN: PIXXD2 WO 2003106446 A1 20031224 CAN 140:42021 AN 2003:1006973. Methods for synthesizing the compounds
and intermediates useful in their preparation are also described. (drug design, drug discovery, blood brain barrier, SAR,
SXR, cancer, tumor, synthesis, prodrugs, pharmacokinetics, pharmacodynamics, active metabolites, ADME).
2003 - WO 2003068769, CA 2418712
Christie, Lance; Anderson, Mark, Brian; Feng, Jun; Hong, Yufeng; Pathak,
Ved, Prakash; Rajapakse, Ranjan, Jagath; Tompkins, Eileen, Valenzuela; Vazir, Haresh; Li, Haitao. NON-PEPTIDE COMPOUNDS
AFFECTING THE ACTION OF GONADOTROPIN-RELEASING HORMONE (GNRH). International Application Number: 21.08.2003 C07D
405/12 PCT/IB2003/000316 PFIZER INC. Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are
described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well
as for regulating fertility, where suppression of gonadotropin release is indicated. The compound have the following structure:
(Formula I). Canadian Patent (CA) of US 6833372. (CA 2418712) Non-peptide gnrh agents, pharmaceutical compositions, and methods
for their use|Agents et compositions pharmaceutiques non peptidiques anti-gnrh et methodes d'utilisation. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis,
pharmacokinetics, pharmacodynamics, ADME).
2003
- US 6670167, US 20030235899 (2003) EP 1096014 (2001)
Chen, Ping; Anderson, Mark; Deng, Ya-Li; Gaur, Smita;
Kan, Chen Chen; Luo, Chun; Lundgren, Karen; Margosiak, Stephen; Nguyen, Binh; O'Connor, Patrick; Register, James; Russell,
Anna Tempczyk; Sarup, Jay. CATALYTIC DOMAIN OF THE HUMAN EFFECTOR CELL CYCLE CHECKPOINT
PROTEIN KINASE CHK1 MATERIALS AND METHODS FOR IDENTIFICATION OF INHIBITORS THEREOF The present invention relates to the identification, isolation
and purification of the catalytic domain of the human effector checkpoint protein kinase (hChk1). A 1.7Å crystal structure
of the hChk1 kinase domain in the active conformation is reported herein. The kinase domain of hChk1 and its associated crystal
structure is described for use in the discovery, identification and characterization of inhibitors of hChk1. This structure
provides a three-dimensional description of the binding site of the hChk1 for structure-based design of small molecule inhibitors
thereof as therapeutic agents. Inhibitors of hChk1 find utility in the treatment of hyperproliferative disorders such as HIV
and cancer. http://www.wikipatents.com/6670167.html (drug design, drug discovery, SAR, SXR, cancer, tumor, crystal structure,
kinase).
2003 - US 6646137
Anderson, Mark Brian; Polinsky, Alexander; Hong, Yufeng; Gregor, Vlad Edward. NON-PEPTIDE GNRH AGENTS.
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general
formula, where X1, X2, Y, and Z are defined variables: STR1 Such compounds and their pharmaceutically acceptable salts, multimers,
prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent
tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing
the compounds and intermediates useful in their preparation are also described. (drug design, drug discovery, SAR, SXR, prodrugs,
cancer, tumor, synthesis, pharmacokinetics, pharmacodynamics, ADME).
2003 - EP 1334972
Anderson, Mark B.; Christie, Lance C.; Feng, Jun; Hong, Yufeng; Li, Haitao; Pathak, Ved P.; Rajapakse, Ranjan;
Tompkins, Eileen; Vazir, Haresh N. PREPARATION OF NON-PEPTIDE COMPOUNDS AFFECTING THE ACTION OF GONADOTROPIN-RELEASING
HORMONE (GNRH). International Application Number: Eur. Pat. Appl. (2003), 1 p. CODEN: EPXXDW EP 1334972 A1 20030813
CAN 139:179968 AN 2003:626431. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis).
2002 - WO 2002098363, CA 2449843
Sun, Eric T.; Anderson, Mark B.; Anderes, Kenna L.; Christie, Lance
C.; Do, Quyen-Quyen T.; Feng, Jun; Goetzen, Thomas; Hong, Yufeng; Iatsimirskaia, Eugenia A.; Li, Haitao; Luthin, David R.;
Paderes, Genevieve D.; Pathak, Ved P.; Rajapakse, Ranjan Jagath; Shackelford, Scott; Tompkins, Eileen Valenzuela; Truesdale,
Larry K.; Vazir, Haresh. NON-PEPTIDE FURANYL GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE, AND
PROCESSES FOR PREPARING THEM AND THEIR INTERMEDIATES. PCT Int. Appl. (2002), 243 pp. CODEN: PIXXD2 WO 2002098363
A2 20021212 CAN 138:24635 AN 2002:946059. PCT/US2002/017846. Abstract: Non-peptide GnRH agents capable of inhibiting the effect
of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and
active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well
as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds
and intermediates useful in their preparation are also described. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis,
pharmacokinetics, pharmacodynamics, ADME).
2001
- US 6218426 (2001), WO 1999/044987 (1999)
Anderson,
Mark; Polinsky, Alexander; Hong, Yufeng; Gregor, Vlad. NON-PEPTIDE GnRH AGENTS 10.09.1999 C07C 279/12 PCT/US1999/004457.
PCT Int. Appl. (1999), 90 pp. CODEN: PIXXD2 WO 9944987 A1 19990910 EP1068178, WO09944987. CA2322444 CAN 131:214183
AN 1999:576906 AGOURON PHARMACEUTICALS, INC. Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing
hormone are of general formula (I), where X1, X2, Y, and Z are defined variables. Such compounds and their pharmaceutically
acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and
steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated.
Methods for synthesizing the compounds and intermediates useful in their preparation are also described. (SAR, SXR, synthesis).
2000 - US 7101878, WO
2000020358, EP1105120 (2000), WO 0020358 (2000)
Anderson,
Mark Brian; Vazir, Haresh N.; Luthin, David Robert; Paderes, Genevieve Deguzman; Pathak, Ved P.; Christie, Lance Christopher;
Hong, Yufeng; Tompkins, Eileen Valenzuela; Li, Haitao; Faust, James. NON-PEPTIDE GNRH AGENTS, METHODS AND INTERMEDIATES
FOR THEIR PREPARATION. PCT Int. Appl. (2000), 444 pp. CODEN: PIXXD2 WO 2000020358 A2 20000413 CAN 132:279106 AN 2000:241135.
(drug design, drug discovery, synthesis, SAR, SXR).
1999 - WO 9929705
Anderson,
Mark B.; Kobayashi, Yoshiyuki; Itoh, Kazuhiro; Holme, Kevin R.; Cui, Jingrong; Fugedi, Peter; Peto, Csaba F.; Wang, Li; Vazir,
Harish. PREPARATION OF SIALYL LEWISX AND SIALYL LEWISA GLYCO-MIMETICS AS SELECTIN INHIBITORS. PCT Int. Appl.
(1999), 184 pp. CODEN: PIXXD2 WO 9929705 A2 19990617 CAN 131:45047 AN 1999:390408. (drug design, drug discovery, synthesis,
SAR, SXR).
1999 - WO 9944987
Anderson, Mark; Polinsky, Alexander; Hong, Yufeng; Gregor, Vlad. PREPARATION
OF N-(HETERO)AROYL-N-(GUANIDINOMETHYLARYLMETHYL)-N-[(POLY)CYCLYLMETHYL)]AMINES AS NON-PEPTIDE GONADOTROPIN RELEASING HORMONE
INHIBITORS. PCT Int. Appl. (1999), 90 pp. CODEN: PIXXD2 WO 9944987 A1 19990910 CAN 131:214183 AN 1999:576906. (drug
design, drug discovery, synthesis, SAR, SXR).
1999
- WO 9929706
Anderson, Mark B.; Levy, Daniel
E.; Holme, Kevin R. PREPARATION OF DISALICYLATE ANALOG BASED SIALYL LEWISX MIMETICS AS ANTIINFLAMMATORY AGENTS AND
SELECTIN RECEPTORS. PCT Int. Appl. (1999), 104 pp. CODEN: PIXXD2 WO 9929706 A2 19990617 CAN 131:45048 AN 1999:390409.
(drug design, drug discovery, synthesis, SAR, SXR).
1999 - US 6218426, EP1068178, WO09944987, CA2322444
US Patent 6,218,426 M. B. Anderson, A. Polinsky, Y. Hong, Vlad. E. Gregor. NON-PEPTIDE GNRH
AGENTS. EP1068178, WO09944987. CA2322444. (drug design, drug discovery, synthesis, SAR, SXR).
1998 - US CIP of US 5837689
Anderson, Mark B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.;
Rao, Narasinga. PREPARATION OF SIALYL LEWIS-X MIMETICS CONTAINING NAPHTHYL BACKBONES AS SELECTIN INHIBITORS.
U.S. (1998), 48 pp., Cont.-in-part of U. S. Ser. No. 446,185. CODEN: USXXAM US 5837689 A 19981117 CAN 130:14166 AN 1998:752223.
(drug design, drug discovery, synthesis, SAR, SXR).
1998 - US CIP of US 5789385
Anderson,
Mark B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga; Cui, Jing Rong. PREPARATION OF SIALYL LEWIS
X MIMETICS CONTAINING PHENYL BACKBONES AS SELECTIN INHIBITORS. U.S. (1998), 55 pp. Cont.-in-part of U.S. Ser. No.
446,185. US 5789385 A 19980804 CAN 129:161815 AN 1998:534879. (drug design, drug discovery, synthesis, SAR, SXR).
1998 - US 5837690B. N. Narasinga Rao, M.B. Anderson, and J. H.
Musser. DERIVATIVES OF TRITERPENOID ACIDS AND USES THEREOF. International Patents: AU6529194. Abstract:
Derivatives of triterpenoid acids and uses thereof.: United States Patent 5837690 Abstract: Triterpenoid acid derivatives
are described that exhibit dual pharmacophobic activities, specifically selectin ligand and leukotriene biosynthetic inhibitory
activities, and that thus have significant applications for the treatment or prevention of certain diseases including cancer
and diseases associated with the inflammatory process as well as applications for the diagnosis of disease. (drug design,
drug discovery, synthesis, SAR, SXR).
1998 - US 5837689
M. B. Anderson, D. Levy, P. Tang, J. H. Musser, B. N. N.
Rao, SIALYL LEWIS-X MIMETICS CONTAINING NAPHTHYL BACKBONES. International Patents: AU2137297, WO9731006.
Abstract: Sialyl lewis-x mimetics containing naphthyl backbones: United States Patent 5837689 (drug design, drug discovery,
synthesis, SAR, SXR).
1998 - US 5789385, WO 9730984 (1997)
M. B. Anderson,
D. Levy, P. Tang, J. H. Musser, B. N. N. Rao, J. Cui, SIALYL LEWISX MIMETICS CONTAINING PHENYL BACKBONES.
AU2136597, WO9730984. (drug design, drug discovery, synthesis, SAR, SXR). 1997 - WO 9730984 (drug design, drug discovery,
synthesis, SAR, SXR).
1998
- US 5763582B. N. Narasinga Rao, M.B. Anderson, and J. H. Musser. DERIVATIVES
OF TRITERPENE ACIDS AND USES THEREOF. Abstract: Triterpenoid acid derivatives are
described that exhibit dual pharmacophobic activities, specifically selectin ligand and leukotriene biosynthetic inhibitory
activities, and that thus have significant applications for the treatment or prevention of certain diseases including cancer
and diseases associated with the inflammatory process as well as applications for the diagnosis of disease. (drug design,
drug discovery, synthesis, SAR, SXR).
1998
- U.S. (1998), 48 pp., Cont.-in-part of U. S. Ser. No. 446,185. US 5837689
Anderson, Mark B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga. PREPARATION
OF SIALYL LEWISX MIMETICS CONTAINING NAPHTHYL BACKBONES AS SELECTIN INHIBITORS. U.S. (1998), 48 pp., Cont.-in-part
of U. S. Ser. No. 446,185. US 5837689 A 19981117 CAN 130:14166 AN 1998:752223. (drug design, drug discovery, synthesis, SAR,
SXR).
1998 - CIP of US 5837689
Anderson, Mark B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.;
Rao, Narasinga. PREPARATION OF SIALYL LEWIS-X MIMETICS CONTAINING NAPHTHYL BACKBONES AS SELECTIN INHIBITORS.
U.S. (1998), 48 pp., Cont.-in-part of U. S. Ser. No. 446,185. CODEN: USXXAM US 5837689 A 19981117 CAN 130:14166 AN 1998:752223.
(drug design, drug discovery, synthesis, SAR, SXR).
1998 - CIP of US 5789385
Anderson,
Mark B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga; Cui, Jing Rong. PREPARATION OF SIALYL LEWISX
MIMETICS CONTAINING PHENYL BACKBONES AS SELECTIN INHIBITORS. U.S. (1998), 55 pp., Cont.-in-part of U.S. Ser. No.
446,185. CODEN: USXXAM US 5789385 A 19980804 CAN 129:161815 AN 1998:534879. (drug design, drug discovery, synthesis, SAR,
SXR).
1997 - WO 9731007, AU1975297
Anderson, Mark B.; Levy, Daniel E.; Tang, Peng
Cho; Musser, John H.; Rao, Narasinga. PREPARATION OF SIALYL LEWISX MIMETICS CONTAINING FLAVANOID BACKBONES AS SELECTIN
INHIBITORS. PCT Int. Appl. (1997), 160 pp. CODEN: PIXXD2 WO 9731007 A1 19970828 CAN 127:248358 AN 1997:579729. (drug
design, drug discovery, synthesis, SAR, SXR).
1997
- WO 9731006
Anderson, Mark B.; Levy, Daniel
E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga. PREPARATION OF SIALYL LEWISX MIMETICS CONTAINING NAPHTHYL BACKBONES
AS SELECTIN INHIBITORS. PCT Int. Appl. (1997), 178 pp. CODEN: PIXXD2 WO 9731006 A1 19970828 CAN 127:248357 AN 1997:579728.
(drug design, drug discovery, synthesis, SAR, SXR).
1997 - WO 9731007
Anderson,
Mark B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga. PREPARATION OF SIALYL LEWISX MIMETICS CONTAINING
FLAVANOID BACKBONES AS SELECTIN INHIBITORS. PCT Int. Appl. (1997), 160 pp. CODEN: PIXXD2 WO 9731007 A1 19970828 CAN
127:248358 AN 1997:579729. (drug design, drug discovery, synthesis, SAR, SXR).
1997 - US 5695738
M.B. Anderson and J. H. Musser, STEROIDAL C-GLYCOSIDES. Glycomed Incorporated U.S. (1997),
20 pp. US 5695738 A 19971209 CAN 128:75635 AN 1997:803505. Abstract: Compositions of sterodial glycosides are described wherein
the glycoside is linked directly, or indirectly to a desired steroidal compound via a carbon, or similar stable linkage, and
methods of using the compositions to treat patients by binding to and/or blocking cellular receptors for a variety of diseases
including cancer, inflammation, and autoimmune diseases. (drug design, drug discovery, synthesis, SAR, SXR).
1997 - US 5688922
B.N. Narasinga Rao, M. B. Anderson, and
J. H. Musser. Substituted Fucopyranosides. SUBSTITUTED FUCOPYRANOSIDES 2-Chloromethyl-3-(tri-O-benzyl-α-L-C-fucopyranoside)-1-propene
and methods of making the same are described. Methods of combining this substituted fucopyranose with triterpenoid acid also
are described. (drug design, drug discovery, synthesis, SAR, SXR).
1997 - US 5679644
B.N. Narasinga Rao, M. B. Anderson, and J. H. Musser.
METHODS OF TREATING DISEASES USING TRITERPENOID ACID DERIVATIVES. (Triterpenoid acid derivatives, dual pharmacophobic
activities, selectin ligand and leukotriene biosynthetic inhibitory activities, cancer, diseases associated with the inflammatory
process, diagnosis of disease, drug design, drug discovery, synthesis, SAR, SXR, inflammation).
1997 - US 5643884
Anderson, Mark Brian; Musser, John Henry.
LUPANE TRITERPENOID DERIVATIVES. PCT Int. Appl. (1995), 42 pp. CODEN: PIXXD2 WO 9504526 A1 19950216 CAN 122:256432
AN 1995:516374, AU7520594, CA2169291, EP0714291, WO9504526.US Patent Issued on July 1, 1997, United States Patent 5643884 (drug design, drug
discovery, synthesis, SAR, SXR, HIV, antiviral, cancer, tumor).
1997 - US 5624909
B.N. Narasinga Rao, M. B. Anderson, J. J. Nalway, and
J. H. Musser. DERIVATIVES OF TRITERPENE ACIDS AS INHIBITORS OF CELL ADHESION MOLECULES ELAM-1 (E-SELECTIN) AND LECAM-1
(L-SELECTIN). Abstract: Derivatives of triterpenoid acids as inhibitors of cell-adhesion molecules ELAM-1 (e-selectin)
and LECAM-1 (l-selectin): United States Patent 5624909 (Triterpenoid acid derivatives, dual pharmacophobic activities, selectin
ligand and leukotriene biosynthetic inhibitory activities, cancer, diseases associated with the inflammatory process, diagnosis
of disease, drug design, drug discovery, synthesis, SAR, SXR, inflammation).
1996 - WO 9636627
Anderson, Mark Brian; Musser, John H. PROCESS FOR THE PREPARATION OF ACTIVATED GLYCOMIMETIC C-GLYCOSIDES
AS SELECTIN INHIBITORS. PCT Int. Appl. (1996), 132 pp. CODEN: PIXXD2 WO 9636627 A1 19961121 CAN 126:89699 AN 1997:51546.
(drug design, drug discovery, synthesis, SAR).
1996 - US 5527890, CA 2160370, EP 0693079, AU 6529194, WO 9424145
M.B. Anderson, B. N. Narasinga Rao, and J. H. Musser. DERIVATIVES OF TRITERPENE ACIDS AND USES THEREOF.
International Patents: CA2160370, EP0693079, AU6529194, WO9424145. United States Patent 5527890 (Triterpenoid
acid derivatives, dual pharmacophobic activities, selectin ligand and leukotriene biosynthetic inhibitory activities, cancer,
diseases associated with the inflammatory process, diagnosis of disease, drug design, drug discovery, synthesis, SAR, SXR,
inflammation).
1996 - US 5519008, AU 5160093, AU 675085, EP 0691813, AU 675085, WO 9405152
B.N.
Narasinga Rao, M. B. Anderson, J. J. Nalway, and J. H. Musser. DERIVATIVES OF TRITERPENE ACIDS AS INHIBITORS OF CELL
ADHESION MOLECULES ELAM-1 (E-SELECTIN) AND LECAM-1 (L-SELECTIN). International Patents: AU5160093, AU675085,
EP0691813, AU675085, WO9405152. United States Patent 5519008 Abstract: Triterpenoid acid derivatives have been found to have
structures similar to natural ligands to the extent that these derivatives bind to natural selectin receptors including endothelial
leukocyte adhesion molecule-1 (ELAM-1) and leukocyte/endothelial cell adhesion molecule-1 (LECAM-1). The molecules can be
administered to the patients by themselves or in pharmaceutical formulations; in order to alleviate inflammation and/or treat
other abnormalities associated with the excessive binding of leukocytes to endothelial receptors. (drug design, drug discovery,
synthesis, SAR, SXR).
1996
- CA 2221589, AU 5855296, EP 0828729, WO 9636627
CA2221589,
AU5855296, EP0828729, WO9636627: COLLECTION OF ACTIVATED GLYCOSIDE COMPOUNDS AND THEIR BIOLOGICAL USE. Anderson,
Mark Brian and Musser, John H. US patent pending. (drug design, drug discovery).
1995 - WO 9504526
Anderson, Mark Brian; Musser, John Henry. LUPANE TRITERPENOID DERIVATIVES. PCT Int. Appl.
(1995), 42 pp. CODEN: PIXXD2 WO 9504526 A1 19950216 CAN 122:256432 AN 1995:516374. (drug design, drug discovery, synthesis,
SAR).
1994 - WO 9424145
Rao, Narasinga; Anderson, Mark Brian; Musser, John Henry. PREPARATION
OF GLYCYRRHETINIC ACID DERIVATIVES AS SELECTIN LIGANDS AND LEUKOTRIENE BIOSYNTHESIS INHIBITORS. PCT Int. Appl. (1994),
49 pp. CODEN: PIXXD2 WO 9424145 A1 19941027 CAN 122:240077 AN 1995:468527. (drug design, drug discovery, synthesis, SAR, SXR).
1994 - WO 9405152
Rao, Narasinga; Anderson, Mark Brian; Naleway, John J.; Musser, John Henry. DERIVATIVES
OF TRITERPENOID ACIDS AS INHIBITORS OF CELL-ADHESION MOLECULES ELAM-1 (E-SELECTIN) AND LECAM-1 (L-SELECTIN). PCT
Int. Appl. (1994), 77 pp. WO 9405152 A1 19940317 CAN 120:315817 AN 1994:315817. (drug design, drug discovery, synthesis, SAR,
SXR).
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