The Additional Hetero Ring Is A Diazine Patents (Class 514/252.02)
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Publication number: 20030225098Abstract: The present application is directed to pyrazolopyrirnidine and furopyrimidine analogs of the formula (I) 1Type: ApplicationFiled: March 21, 2003Publication date: December 4, 2003Inventors: Gavin C. Hirst, Lee D. Arnold, Andrew Burchat, Neil Wishart, David Calderwood, Carol K. Wada, Michael R. Michaelides, Zhiqin Ji, Melanie Muckey
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Publication number: 20030225273Abstract: Compounds having the formula 1Type: ApplicationFiled: March 3, 2003Publication date: December 4, 2003Inventors: Michael R. Michaelides, Michael L. Curtin, Yujia Dai, Steven K. Davidsen, Robin R. Frey, Yan Guo, Zhiqin Ji
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Publication number: 20030225081Abstract: The present invention provides a novel compound exhibiting an excellent inhibitory action on AMPA receptor and/or kainate receptor. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.Type: ApplicationFiled: March 18, 2003Publication date: December 4, 2003Inventors: Satoshi Nagato, Koki Kawano, Koichi Ito, Yoshihiko Norimine, Koshi Ueno, Takahisa Hanada, Hiroyuki Amino, Makoto Ogo, Shinji Hatakeyama, Masataka Ueno, Anthony John Groom, Leanne Rivers, Terence Smith
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Publication number: 20030220338Abstract: This invention relates to compounds that are efflux pump inhibitors and therefore are useful as potentiators of anti-fungal agents for the treatment of infections caused by fungi that employ an efflux pump resistance mechanism.Type: ApplicationFiled: September 12, 2002Publication date: November 27, 2003Inventors: Will J. Watkins, Remy Lemoine, Aesop Cho, Monica Palme
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Publication number: 20030220227Abstract: Novel quinazoline derivatives possessing activity as estrogen receptor beta (ER&bgr;) modulators are provided which have the general formula I 1Type: ApplicationFiled: March 13, 2003Publication date: November 27, 2003Inventors: Timur Gungor, James R. Corte
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Patent number: 6653316Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: November 20, 2000Date of Patent: November 25, 2003Assignee: Pharmacia CorporationInventors: Michael S. South, Ashton T. Hamme, II, William L. Neumann, Darin E. Jones, Melvin L. Rueppel
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Publication number: 20030216394Abstract: Ethylene derivatives of formula (I): 1Type: ApplicationFiled: August 8, 2002Publication date: November 20, 2003Applicant: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
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Publication number: 20030216404Abstract: The invention encompasses novel compounds which are inhibitors of matrix metalloproteinase, ADAM or ADAM-TS enzymes, and which are useful for the treatment of diseases mediated by those enzymes, including degenerative diseases and certain cancers.Type: ApplicationFiled: June 12, 2003Publication date: November 20, 2003Inventors: Duncan Robert Hannah, Hazel Joan Dyke, Andrew Sharpe, Andrew Douglas Baxter
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Publication number: 20030216382Abstract: The present invention provides compounds of formula (I) 1Type: ApplicationFiled: February 10, 2003Publication date: November 20, 2003Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Matthias Steger, Peter Weiss
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Publication number: 20030212071Abstract: Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: ApplicationFiled: August 19, 2002Publication date: November 13, 2003Applicant: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
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Publication number: 20030212075Abstract: The present invention relates to novel pharmaceutical compositions based on anticholinergics and NK1-receptor antagonists, processes for preparing them and their use in the treatment of respiratory tract diseases.Type: ApplicationFiled: April 21, 2003Publication date: November 13, 2003Applicant: Boehringer Ingelheim Pharma KGInventors: Michel Pairet, Michael P. Pieper, Christopher J. M. Meade
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Patent number: 6645992Abstract: Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: October 1, 2001Date of Patent: November 11, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Manfred Schudok, Otmar Klingler, Hans-Peter Nestler, Hans Matter, Herman Schreuder
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Publication number: 20030207882Abstract: Compounds of formula (I), wherein G1 is CH or N; G2 is CH or N; R1 is a variety of optional substituents, L1 is (1-4C)alkylene; T1 is CH or N; R2 and R3 are independently hydrogen or (1-4C)alkyl or are joined to form a ring; X1 and X2 represent various linking groups; Ar is phenylene or certain heteroaryl rings and Q represents a variety of aromatic or heterocyclic rings systems, and pharmaceutically acceptable salts thereof are described as useful antithrombotic and anticoagulant agents, and are selective Factor Xa inhibitors. Processes for their preparation and pharmaceutical compositions containing them are also described.Type: ApplicationFiled: May 2, 2003Publication date: November 6, 2003Applicant: ZENECA LIMITEDInventors: Andrew Stocker, John Preston, Michael James Smithers
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Patent number: 6642237Abstract: &ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.Type: GrantFiled: November 21, 2000Date of Patent: November 4, 2003Assignee: Merck & Co., Inc.Inventors: James R. Tata, Kevin T. Chapman, Joseph Leslie Duffy, Nancy J. Kevin, Yuan Cheng, Thomas A. Rano, Fengqi Zhang, Tracy Huening, Brian Anthony Kirk, Zhijian Lu, Subharekha Raghavan, Fred J. Fleitz, Daniel E. Petrillo, Joseph D. Armstrong, III, Richard J. Varsolona, David Askin, R. Scott Hoerrner, Robert Purick
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Publication number: 20030199516Abstract: Methods are provided for treating an infection by Gram-positive bacteria in a mammal, by administering to the mammal an effective amount of a compound that binds noncovalently in the minor groove of duplex DNA, the compound being identified by a number of DNA binding parameters and, in many instances, being a polyaromatic compound.Type: ApplicationFiled: September 12, 2002Publication date: October 23, 2003Applicant: Genesoft, Inc.Inventors: Heinz E. Moser, Eldon E. Baird, Roland W. Burli, Yigong Ge, Sarah White
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Publication number: 20030191129Abstract: The invention relates to compounds of formula I, 1Type: ApplicationFiled: January 7, 2003Publication date: October 9, 2003Inventors: Guido Bold, Jorg Frei, Peter Traxler, Karl-Heinz Altmann, Helmut Mett, David Raymond Stover, Jeanette Marjorie Wood
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Publication number: 20030191110Abstract: The present invention relates to methods for modulating the cholesterol biosynthetic pathway. The level of cholesterol in the body is linked to numerous pathological states. The methods of the present invention alter the transcription levels of genes involved in the cholesterol biosynthesis. The methods of the present invention can used for treating diseases mediated by the cholesterol biosynthetic pathway.Type: ApplicationFiled: November 1, 2002Publication date: October 9, 2003Inventors: Martyn Botfield, Fiona McDonald, Joern Kraetzschmar, Bernhard Lindenthal, Bertold Kreft
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Patent number: 6630475Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of ParkinsoType: GrantFiled: May 24, 2001Date of Patent: October 7, 2003Assignee: Schering CorporationInventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil
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Publication number: 20030186989Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of Formula (1.0.Type: ApplicationFiled: July 24, 2002Publication date: October 2, 2003Inventors: Anthony Marfat, Robert James Chambers
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Publication number: 20030186990Abstract: The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(═O)—R8; —S(═O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula 1Type: ApplicationFiled: November 7, 2002Publication date: October 2, 2003Inventors: Michael Joseph Kukla, Donald William Ludovici, Robert William Kavash, Bart Lieven Daniel De Corte, Jan Heeres, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Marc Rene de Jonge, Koen Jeanne Alfons Van Aken, Alain Krief
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Publication number: 20030186966Abstract: This invention concerns amide derivatives of Formula (I) wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: January 29, 2003Publication date: October 2, 2003Applicant: ASTRAZENECA ABInventor: Dearg S. Brown
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Patent number: 6624166Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(═O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(═O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, sybstituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1&bgr; protease activity in a mammal utilizing the compounds and compositions.Type: GrantFiled: April 3, 1996Date of Patent: September 23, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roland E. Dolle, Denton W. Hoyer, Tina Morgan Ross, James M. Rinker, Stanley J. Schmidt, Mark A. Ator
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Publication number: 20030176437Abstract: A novel class of pyridazine compositions and related methods of use.Type: ApplicationFiled: September 3, 2002Publication date: September 18, 2003Inventors: D.M. Watterson, Anu R. Sawkar, Thomas J. Lukas, Salida Mirzoeva, Linda J. Van Eldik, Marcel Hibert, Anastasia Velentza, Magdalena Zasadzki, Jacques Haiech, Jean-Jacques Bourguignon
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Publication number: 20030171374Abstract: This invention concerns HIV replication inhibitors of formula 1Type: ApplicationFiled: November 8, 2002Publication date: September 11, 2003Inventors: Michael Joseph Kukla, Donald William Ludovici, Robert William Kavash, Bart Lieven Daniel De Corte, Jan Heeres, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Marc Rene de Jonge, Koen Jeanne Alfons Van Aken, Alain Krief, Ruben Gerardus George Leenders
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Publication number: 20030166637Abstract: The present invention relates to substituted piperazine derivatives of general formula 1Type: ApplicationFiled: October 9, 2002Publication date: September 4, 2003Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
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Publication number: 20030166644Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.Type: ApplicationFiled: December 13, 2002Publication date: September 4, 2003Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
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Patent number: 6613773Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocyclyl group.Type: GrantFiled: March 5, 2002Date of Patent: September 2, 2003Assignee: Syngenta LimitedInventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
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Patent number: 6613772Abstract: Compounds of the formula I in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular diseases such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance.Type: GrantFiled: June 16, 2000Date of Patent: September 2, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel, Peter Schindler
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Publication number: 20030162784Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.Type: ApplicationFiled: February 20, 2003Publication date: August 28, 2003Inventor: Banavara L. Mylari
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Patent number: 6610677Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII: wherein Z1 is N or C—R9, Z2 is N or CH, and Z3 is N or C—Rx, provided that one of Z1 and Z3 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and Rx, R1, R2, R2′, R3, and R9 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: August 26, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Davies, Pan Li, Julian M. C. Golec, Jean-Damien Charrier, Ronald Knegtel, David Bebbington
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Publication number: 20030158184Abstract: The invention provides methods for treating female sexual dysfunctions by administering to a female individual a therapeutically effective amount of at least one compound that donates, transfers or release nitrogen monoxide, that induces the production of endogenous endothelium-derived relaxing factor, that stimulates endogenous synthesis of nitrogen monoxide, or that is a substrate for nitric oxide synthase. The methods may further comprise administering a therapeutically effective amount of a phosphodiesterase inhibitor and/or a nitrosated and/or nitrosylated phosphodiesterase inhibitor.Type: ApplicationFiled: December 21, 2001Publication date: August 21, 2003Inventors: David S. Garvey, Inigo Saenz de Tejada
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Publication number: 20030149038Abstract: The present invention provides methods for making compounds and methods for using the compounds to disrupt or inhibit protein-protein interactions. Also provided are pharmaceutical compositions comprising the compounds of the current invention.Type: ApplicationFiled: November 12, 2002Publication date: August 7, 2003Applicant: The Regents of the University of CaliforniaInventors: Rodney K. Guy, Irwin D. Kuntz, Felice Lu
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Patent number: 6602872Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.Type: GrantFiled: November 21, 2000Date of Patent: August 5, 2003Assignee: Merck & Co., Inc.Inventors: Charles J. McIntyre, Nigel J. Liverton, David A. Claremon
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Publication number: 20030125329Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: May 23, 2002Publication date: July 3, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030125328Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: May 23, 2002Publication date: July 3, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030119876Abstract: The invention relates to new diphenylurea having the formula (I) 1Type: ApplicationFiled: February 26, 2002Publication date: June 26, 2003Inventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jurgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
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Publication number: 20030119833Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: May 23, 2002Publication date: June 26, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030119838Abstract: Compounds having the formula (1): 1Type: ApplicationFiled: September 25, 2002Publication date: June 26, 2003Applicant: KOWA CO., LTD.Inventors: Yoshinori Kyotani, Tomoyuki Koshi, Hiromichi Shigyo, Hideo Yoshizaki, Takahiro Kitamura, Shunji Takemura, Kyoko Yasuoka, Junko Totsuka, Seiichi Sato
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Publication number: 20030119834Abstract: The present invention generally relates to compositions useful in the treatment or prevention of cancer, in some cases by limiting or preventing angiogenesis. Other compositions useful for the treatment or prevention of cancer or angiogenesis include homologs, analogs, derivatives, enantiomers or functionally equivalent compositions of the present invention. The present compositions can be packaged in kits. The present invention also relates to the use of compositions useful for the treatment of patients susceptible to or exhibiting symptoms characteristic of cancer, for example, patients with solid tumors.Type: ApplicationFiled: September 5, 2002Publication date: June 26, 2003Inventor: Cynthia C. Bamdad
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Publication number: 20030119829Abstract: The invention relates to 4-amino-5,6-substituted thiopheno [2,3-d] pyrimidines, pharmaceutical compositions containing the same and their use to treat or prevent diseases and conditions mediated by the phosphodiesterase enzyme 7B (PDE7B). Diseases and conditions mediated by PDE7B include osteoporosis, osteopenia and asthma.Type: ApplicationFiled: April 29, 2002Publication date: June 26, 2003Inventors: Andreas Stolle, Donald E. Bierer, Yuanwei Chen, Dongping Fan Can, Barry Hart, Mary Katherine Monahan, William J. Scott
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Patent number: 6583146Abstract: Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A3 receptor antagonism: wherein A is an optionally substituted benzene ring; B may be further substituted; and R1 is an optionally substituted cyclic group.Type: GrantFiled: July 12, 2001Date of Patent: June 24, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Naoyuki Kanzaki, Seiji Miwatashi
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Publication number: 20030114454Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: May 23, 2002Publication date: June 19, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6579879Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.Type: GrantFiled: March 21, 2002Date of Patent: June 17, 2003Assignee: Pfizer IncInventor: Banavara L. Mylari
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Publication number: 20030109528Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: May 23, 2002Publication date: June 12, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030105094Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: ApplicationFiled: March 19, 2002Publication date: June 5, 2003Applicant: Schering CorporationInventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
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Publication number: 20030105100Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: May 23, 2002Publication date: June 5, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6573262Abstract: The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I, compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.Type: GrantFiled: December 19, 2001Date of Patent: June 3, 2003Assignee: Bristol-Myers Sqibb CompanyInventors: Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin
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Publication number: 20030100559Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: May 23, 2002Publication date: May 29, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6569860Abstract: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I): wherein G2 is a heteroaryl group containing one or two nitrogen atoms substituted with a carboxylic acid group, said heteroaryl ring containing one or two nitrogen atoms, and G1 is as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: March 1, 2002Date of Patent: May 27, 2003Assignee: Roćhe Palo Alto LLCInventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
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Publication number: 20030096818Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: May 23, 2002Publication date: May 22, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel