The Other Ring Is A Benzene Ring Patents (Class 548/361.1)
  • Patent number: 6841563
    Abstract: Disclosed is a compound represented by structural formula (I): R1 is a substituted or unsubstituted aryl group. R2 and R3 are independently —H, a C1-C4 straight chained or branched alkyl group. R4 and R5 are independently —H, a C1-C4 straight chained or branched alkyl group or, taken together with the nitrogen atom to which each is bonded, a non-aromatic heterocyclic ring. Ring A and Ring B are independently further substituted with zero, one or two substituents. Physiologically acceptable salts of structural formula shown above are also included. Also disclosed is a method promoting growth, efficiency of feed utilization and/or production of lean body mass in a livestock animal. The method comprises administering to the animal an effective amount of one or more compounds represented by the structural formula as shown or a physiologically acceptable salt thereof.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: January 11, 2005
    Assignee: Eli Lilly and Company
    Inventors: Randall Bruce Hopkins, Deana Lori Hancock, Michael Eugene Quimby
  • Publication number: 20040259928
    Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): 1
    Type: Application
    Filed: July 6, 2004
    Publication date: December 23, 2004
    Inventors: Han-Cheng Zhang, Bruce Maryanoff, Bruce Conway, Kimberly White, Hong Ye, Leonard Robert Hecker, David F. McComsey
  • Publication number: 20040242886
    Abstract: Compounds and compositions containing compounds given by the structural Formula 8, for tumor therapeutic applications are disclosed.
    Type: Application
    Filed: April 30, 2004
    Publication date: December 2, 2004
    Inventors: Sandeep Gupta, David Michael Carrig, Prabhavathi Fernandes
  • Publication number: 20040235892
    Abstract: Compounds having the formula 1
    Type: Application
    Filed: May 22, 2003
    Publication date: November 25, 2004
    Inventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
  • Publication number: 20040236101
    Abstract: One aspect of the invention is concerned with cannabimimetic heteroindane analogs having affinities and/or selectivities for a cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.
    Type: Application
    Filed: July 2, 2004
    Publication date: November 25, 2004
    Inventors: Alexandros Makriyannis, Qian Liu
  • Publication number: 20040220248
    Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
    Type: Application
    Filed: February 15, 2003
    Publication date: November 4, 2004
    Inventors: Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Ye Hua, Michael David Johnson, Theodore Otto Johnson, Hiep The Luu, Cynthia Louise Palmer, Siegfried Heinz Reich, Anna Marie Tempczyk-Russell, Min Teng, Christine Thomas, Michael David Varney, Michael Brennan Wallace, Michael Raymond Collins
  • Publication number: 20040214808
    Abstract: The present application describes linear chain substituted monocyclic and bicyclic compounds and derivatives thereof of Formula I:
    Type: Application
    Filed: March 16, 2004
    Publication date: October 28, 2004
    Inventor: Donald J. Pinto
  • Publication number: 20040186129
    Abstract: Disclosed is a compound represented by Structural Formula (I): 1
    Type: Application
    Filed: March 16, 2004
    Publication date: September 23, 2004
    Inventors: Keizo Koya, Lijun Sun, Mitsunori Ono, David James, Weiwen Ying, Shoujun Chen
  • Patent number: 6794518
    Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: September 21, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
  • Publication number: 20040171634
    Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
    Type: Application
    Filed: February 13, 2003
    Publication date: September 2, 2004
    Inventors: Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Ye Hua, Michael David Johnson, Theodore Otto Johnson, Hiep The Luu, Cynthia Louise Palmer, Siegfried Heinz Reich, Anna Maria Tempczyk-Russell, Min Teng, Christine Thomas, Michael David Varney, Michael Brennan Wallace, Michael Raymond Collins
  • Publication number: 20040167127
    Abstract: This invention provides compound of formulae I or II having the structure 1
    Type: Application
    Filed: September 24, 2003
    Publication date: August 26, 2004
    Applicant: Wyeth
    Inventors: Robert J. Steffan, Edward M. Matelan, Mark A. Ashwell, William R. Solvibile
  • Patent number: 6767912
    Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: July 27, 2004
    Assignee: Wyeth
    Inventors: Ping Zhou, Derek Cecil Cole, Michael Gerard Kelly, William Joseph Lennox
  • Publication number: 20040142998
    Abstract: Methods of making indazoles are described. The methods involved reacting an aromatic aldehyde with a nitrogen source to form a nitroso aromatic aldehyde. The nitroso aromatic aldehyde is reacted with a reducing agent to form an indazole which ultimately can be used to form desired indazoles which are preferably pharmaceutically active products. The process of the present invention further permits the formation of enantiomerically enriched or pure indazoles such as aminoalkyl indazoles.
    Type: Application
    Filed: November 26, 2003
    Publication date: July 22, 2004
    Inventors: Raymond E. Conrow, Pete Delgado, William D. Dean, David R. Pierce, Michael S. Gaines
  • Publication number: 20040138141
    Abstract: The invention is directed to novel heteroaryl peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, angiogenesis and related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted heteroaryl peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
    Type: Application
    Filed: December 10, 2003
    Publication date: July 15, 2004
    Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, William J. Hoekstra, Kimberly White
  • Publication number: 20040132741
    Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: December 4, 2003
    Publication date: July 8, 2004
    Applicant: Wyeth
    Inventors: Michael Gerard Kelly, Derek Cecil Cole
  • Publication number: 20040132790
    Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the &agr;7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Application
    Filed: September 25, 2003
    Publication date: July 8, 2004
    Inventors: Wenge Xie, Brian Herbert, Truc Nguyen, Carla Gauss, Ashok Tehim
  • Patent number: 6759428
    Abstract: Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
    Type: Grant
    Filed: June 2, 2003
    Date of Patent: July 6, 2004
    Assignee: Roche Palo Alto LLC
    Inventors: Joe Timothy Bamberg, Tobias Gabriel, Nancy Elisabeth Krauss, Taraneh Mirzadegan, Wylie Solang Palmer, David Bernard Smith
  • Publication number: 20040127538
    Abstract: The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.
    Type: Application
    Filed: August 28, 2003
    Publication date: July 1, 2004
    Inventors: Hitoshi Oinuma, Norihito Ohi, Nobuaki Sato, Motohiro Soejima, Hidenori Seshimo, Taro Terauchi, Takashi Doko, Naohiro Kohmura
  • Publication number: 20040110951
    Abstract: The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands.
    Type: Application
    Filed: July 11, 2003
    Publication date: June 10, 2004
    Inventor: Yuan-Ching P. Chiang
  • Publication number: 20040097575
    Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
    Type: Application
    Filed: October 14, 2003
    Publication date: May 20, 2004
    Inventors: James B. Doherty, Meng-Hsin Chen, Luping Liu, Swaminathan R. Natarajan, Robert M. Tynebor
  • Publication number: 20040092564
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: October 28, 2003
    Publication date: May 13, 2004
    Applicant: Wyeth
    Inventors: Ping Zhou, Michael Gerard Kelly
  • Publication number: 20040092546
    Abstract: Compounds of Formula I are useful as mediators of protein kinases and have activity as cell proliferation inhibitors: 1
    Type: Application
    Filed: August 12, 2003
    Publication date: May 13, 2004
    Applicant: Sugen, Inc.
    Inventors: Chung Chen Wei, Ping Huang, Yi Xia
  • Publication number: 20040087637
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: October 29, 2003
    Publication date: May 6, 2004
    Applicant: Wyeth
    Inventors: Ping Zhou, Michael Gerard Kelly
  • Publication number: 20040087584
    Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs.
    Type: Application
    Filed: July 18, 2003
    Publication date: May 6, 2004
    Applicant: MEMORY PHARMACEUTICALS CORP.
    Inventors: Richard A. Schumacher, Allen T. Hopper, Ashok Tehim
  • Publication number: 20040077680
    Abstract: The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.
    Type: Application
    Filed: November 17, 2003
    Publication date: April 22, 2004
    Applicants: Telik, Inc., Sanwa Kagaku Kenkyusho Co., Ltd.
    Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
  • Patent number: 6716978
    Abstract: This application is directed to therapeutically active compositions of matter are useful for treating or preventing inflammatory bowel disease and conditions including joint inflammation, Crohn's disease and inflammatory bowel disease; respiratory diseases such as chronic obstructive pulmonary disease (COPD) including asthma, chronic bronchitis, and pulmonary emphysema; infectious diseases including endotoxic shock and toxic shock syndrome; immune diseases including systemic lupus erythematosis and psoriasis; and other diseases including bone resorption diseases and reperfusion injury; wherein said composition of matter comprises a compound which is an inhibitor of phosphodiesterase isozyme 4 (PDE4) and wherein an indazole is one essential component of said compound's overall chemical structure, and wherein said indazole constitutes a bioisosteric replacement of a catechol component or functional derivative thereof in a known compound having the same said therapeutic activity and the same remaining
    Type: Grant
    Filed: September 20, 1999
    Date of Patent: April 6, 2004
    Assignee: Pfizer Inc
    Inventor: Anthony Marfat
  • Patent number: 6716837
    Abstract: Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c a
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: April 6, 2004
    Assignee: NPS Allelix Biopharmaceuticals, Inc.
    Inventors: Louise Edwards, Methvin Isaac, Shawn Maddaford, Abdelmalik Slassi, Tao Xin
  • Publication number: 20040063768
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds 1
    Type: Application
    Filed: September 15, 2003
    Publication date: April 1, 2004
    Inventors: Derek John Denhart, Jonathan L. Ditta, Dalton King, John E. Macor, Lawrence R. Marcin, Ronald J. Mattson, Zhaoxing Meng
  • Publication number: 20040048866
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: February 26, 2003
    Publication date: March 11, 2004
    Inventors: Teodozyj Kolasa, Jorge D. Brioni, Vijaya Gracias, Masaki Nakane, Meena V. Patel, Jeffrey Rohde
  • Patent number: 6677365
    Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.
    Type: Grant
    Filed: March 25, 2002
    Date of Patent: January 13, 2004
    Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co., Ltd.
    Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
  • Publication number: 20040006236
    Abstract: A compound of formula 1a 1
    Type: Application
    Filed: January 22, 2003
    Publication date: January 8, 2004
    Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
  • Publication number: 20030236252
    Abstract: Described are bicycle-substituted cyclohexylamines of Formula (I) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's specification. disease. The substituents are defined in the specification.
    Type: Application
    Filed: November 12, 2002
    Publication date: December 25, 2003
    Inventors: Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • Publication number: 20030232810
    Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.
    Type: Application
    Filed: December 3, 2002
    Publication date: December 18, 2003
    Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • Publication number: 20030207927
    Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1
    Type: Application
    Filed: December 11, 2002
    Publication date: November 6, 2003
    Applicant: Wyeth
    Inventors: Michael S. Malamas, Tam Q. Dinh, Iwan Gunawan, Michael D. Collini, Heather A. Harris, James C. Keith, Leo M. Albert
  • Publication number: 20030199455
    Abstract: The invention is directed to novel indazole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indazole peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
    Type: Application
    Filed: March 31, 2003
    Publication date: October 23, 2003
    Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, Anjali Pandey, Robert M. Scarborough
  • Patent number: 6635639
    Abstract: Described are compounds having formula I or II: wherein: X is N, and Ak represents a C1-3 alkylene chain; and a salt, solvate or prodrug thereof.
    Type: Grant
    Filed: February 13, 2002
    Date of Patent: October 21, 2003
    Assignee: NPS Allelix Corp.
    Inventors: Jalaj Arora, Louise Edwards, Methvin Issac, Anne O'Brien, Abdelmalik Slassi, Ashok Tehim, Tao Xin
  • Publication number: 20030171412
    Abstract: This invention provides estrogen receptor modulators of formula 1, having the structure 1
    Type: Application
    Filed: December 11, 2002
    Publication date: September 11, 2003
    Applicant: Wyeth
    Inventors: Michael S. Malamas, Iwan Gunawan, Heather A. Harris, James C. Keith, Leo M. Albert
  • Publication number: 20030166654
    Abstract: The invention provides compounds of formula (I) wherein n, A, R1, R2 and R3 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.
    Type: Application
    Filed: October 31, 2002
    Publication date: September 4, 2003
    Inventor: Joachim Nozulak
  • Publication number: 20030153576
    Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I):
    Type: Application
    Filed: December 19, 2001
    Publication date: August 14, 2003
    Inventors: Albert J. Robichaud, Ian S. Mitchell
  • Publication number: 20030130329
    Abstract: Compounds characterized generally as imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension.
    Type: Application
    Filed: November 8, 2002
    Publication date: July 10, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Publication number: 20030109550
    Abstract: The present invention relates to substituted indazole derivatives, compositions comprising such, intermediates, methods of making substituted indazolel derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
    Type: Application
    Filed: September 19, 2002
    Publication date: June 12, 2003
    Inventors: Michael Clare, Joyce Z. Crich, Francis J. Koszyk, Richard A. Partis, Michael A. Stealey, Richard M. Weier, Xiangdong Xu, Cathleen E. Hanau
  • Publication number: 20030096705
    Abstract: The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.
    Type: Application
    Filed: January 29, 2002
    Publication date: May 22, 2003
    Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
  • Publication number: 20030073720
    Abstract: Compounds of formula (I), in which M, A1, A2, K1 and K2 have the meanings as indicated in the description are novel active tryptase inhibitors.
    Type: Application
    Filed: September 9, 2002
    Publication date: April 17, 2003
    Inventor: Thomas Martin
  • Publication number: 20030073127
    Abstract: Novel multibinding compounds are disclosed. The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel , thereby modulating the biological activities thereof.
    Type: Application
    Filed: December 8, 1999
    Publication date: April 17, 2003
    Inventors: YU-HUA JI, MAYA NATARAJAN, JOHN H. GRIFFIN, THOMAS E. JENKINS
  • Patent number: 6534504
    Abstract: Disclosed is compound represented by Structural Formula (I), wherein Ring A, Ring B and Ring C are independently substituted or unsubstituted. R1 and R2 are independently a C1-C4 straight chained or branched alkyl group. Also disclosed is a method of increasing the quantity and improving quality of meat obtained from a livestock animal. The method comprises administering to the animal an effective amount of one or more compounds represented by Structural Formula (I).
    Type: Grant
    Filed: April 16, 2002
    Date of Patent: March 18, 2003
    Assignee: Eli Lilly and Company
    Inventors: Deana Lori Hancock, Randall Bruce Hopkins, Michael Eugene Quimby, Andrew Jason Wuethrich
  • Patent number: 6531491
    Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
    Type: Grant
    Filed: October 25, 2001
    Date of Patent: March 11, 2003
    Assignee: Agouron Pharamaceuticals, Inc.
    Inventors: Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Cynthia Louise Palmer, Anna Maria Tempczyk-Russell, Michael David Varney, Michael Raymond Collins
  • Publication number: 20030004351
    Abstract: Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-Cl1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydmogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by c
    Type: Application
    Filed: August 8, 2001
    Publication date: January 2, 2003
    Inventors: Stephen Thomas Davis, Scott Howard Dickerson, Stephen Vernon Frye, Philip Anthony Harris, Robert Neil Hunter, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
  • Publication number: 20020193610
    Abstract: The invention relates to new indazole derivatives, processes for their preparation, and their use in medicaments.
    Type: Application
    Filed: September 18, 2001
    Publication date: December 19, 2002
    Inventors: Michael Woltering, Helmut Haning, Gunter Schmidt, Josef Pernerstorfer, Hilmar Bischoff, Axel Kretschmer, Verena Vohringer, Christiane Faeste
  • Publication number: 20020173663
    Abstract: A class of aryloxyacetic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.
    Type: Application
    Filed: August 17, 2001
    Publication date: November 21, 2002
    Inventors: Kun Liu, Libo Xu, A. Brian Jones
  • Patent number: 6469036
    Abstract: The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.
    Type: Grant
    Filed: January 13, 2000
    Date of Patent: October 22, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael J. Costanzo, Bruce E. Maryanoff, Stephen C. Yabut