At 4- Or 6-position Patents (Class 544/326)
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Patent number: 6936600Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, wherein R1, R2 and R3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith.Type: GrantFiled: August 12, 2004Date of Patent: August 30, 2005Assignee: Pfizer IncInventors: Margaret Y. Chu-Moyer, Banavara L. Mylari, William J. Zembrowski
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Patent number: 6919347Abstract: Bradykinin B1-receptor antagonists of formula are disclosed. The compounds are useful for treating diseases associated with inappropriate bradykinin receptor activity, such as diabetic vasculopathy, inflammation, pain, hyperalgesia, asthma, rhinitis, septic shock, atherosclerosis and multiple sclerosis. Pyrimidines, triazines, and anilines in which Q is imidazolyl or pyrrolyl are particularly preferred.Type: GrantFiled: January 14, 2002Date of Patent: July 19, 2005Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: Michael H. J. Ohlmeyer, John J. Baldwin, Roland E. Dolle, III, Vidyadhar Paradkar, Jorge Gabriel Quintero, Gonghua Pan
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Patent number: 6906076Abstract: The present invention concerns alkyl aryl carbonyl compounds that possess anti-infective activity. The compounds of the invention can be used to target specific nuclear localization signal, thereby blocking importation of specific proteins or molecular complex into the nucleus of a cell. The invention encompasses methods of use of such compounds for treatment or prevention of infectious diseases, such as parasitic and viral diseases, including, for example, malaria and acquired immunodeficiency syndrome. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.Type: GrantFiled: September 12, 2003Date of Patent: June 14, 2005Assignee: Cytokine Pharmasciences, Inc.Inventors: Michael I. Bukrinsky, Anthony Cerami, Peter Ulrich, Bradley Berger
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Patent number: 6894067Abstract: The present invention relates to 5-heteroatom-substituted pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.Type: GrantFiled: November 1, 2002Date of Patent: May 17, 2005Assignee: Pfizer, Inc.Inventors: Martha L. Minich, Subas M. Sakya, Andrei Shavnya, Kristin Lundy DeMello
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Patent number: 6869943Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, wherein R1, R2 and R3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith.Type: GrantFiled: August 21, 2003Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Margaret Y. Chu-Moyer, Jerry A. Murry, Banavara L. Mylari, William J. Zembrowski
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Patent number: 6867205Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: February 10, 2003Date of Patent: March 15, 2005Assignee: Hoffman-La Roche Inc.Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Matthias Steger, Peter Weiss
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Patent number: 6867212Abstract: The present invention relates to a 6-(1-fluoroethyl)-5-iodo-4-aminopyrimidine compound represented by the following formula (1): wherein Ar represents a phenyl group, a naphthyl group, a thienyl group, an indanyl group or a 1,4-benzodioxan-6-yl group, which is unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, a haloalkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a haloalkoxy group having 1 to 4 carbon atoms and a phenoxy group; R represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; *1 represents an asymmetric carbon atom; *2 represents an asymmetric carbon atom when R represents an alkyl group having 1 to 4 carbon atoms, a process for preparing the same, and agricultural and horticultural chemicals for controlling noxious organisms.Type: GrantFiled: January 10, 2002Date of Patent: March 15, 2005Assignee: Ube Industries, Ltd.Inventors: Katsutoshi Fujii, Shoji Shikita
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Patent number: 6858606Abstract: This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl optionally substituted with Rd and Rem; each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; Rd is halogen, CN, alkyl alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; Re is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g.Type: GrantFiled: November 26, 2002Date of Patent: February 22, 2005Assignee: Synta Pharmaceutical Corp.Inventors: Lijun Sun, Mitsunori Ono, Elena Kostik, Yumiko Wada
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Patent number: 6846827Abstract: The invention concerns pyrimidine derivatives of Formula (I) wherein m is 0-3 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R3 is hydrogen, halogeno or (1-6C)alkyl; n is 0-2 and each R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; p is 0-4; and Q1 is aryl or heteroaryl; 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: GrantFiled: October 10, 2000Date of Patent: January 25, 2005Assignee: AstraZeneca ABInventor: John Graham Cumming
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Patent number: 6846828Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.Type: GrantFiled: November 6, 2002Date of Patent: January 25, 2005Assignee: Roche Palo Alto LLCInventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
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Patent number: 6844347Abstract: The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the treatment and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis or atherosclerosis. The compounds of the formula I are able to modulate the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis of disorders associated with impaired cGMP balance. The invention furthermore relates to methods for producing compounds of the formula I, their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and pharmaceutical preparations containing the compounds of formula I.Type: GrantFiled: August 4, 1999Date of Patent: January 18, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schnidler, Karl Schoenafinger, Hartmut Strobel
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Patent number: 6838464Abstract: Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.Type: GrantFiled: February 26, 2001Date of Patent: January 4, 2005Assignee: AstraZeneca ABInventors: Elizabeth Janet Pease, Emma Jane Williams, Robert Hugh Bradbury, Stuart Eric Pearson
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Patent number: 6833364Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R1, R2, R3, A, X and Y are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.Type: GrantFiled: March 26, 2001Date of Patent: December 21, 2004Assignee: Bayer HealthCare AGInventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Elke Stahl, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky
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Publication number: 20040249153Abstract: The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof (I), wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.Type: ApplicationFiled: February 24, 2004Publication date: December 9, 2004Inventors: Eva Altmann, Kenji Hayakawa, Genji Iwasaki
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Patent number: 6821980Abstract: The invention relates to substituted 5-benzyl-2,4-diaminopyrimidines of general formula (A) wherein R1 is C2-C3 alkyl an R2 is heterocyclyl, phenyl or naphthyl, bonded by one of its C-atoms and R3 is C2-C6 alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfamoyl, heterocyclysylfonyl, heterocyclylalkylsulfonyl or dialkylsulfamoyl; wherein alkyl, cycloalkyl and alyenyl can carry up to 6 carbon atoms alone or in compositions and can carry up to 6 ring members heterocyclically, alone, or in compositions and the groups R2 and R3 can be substituted; and to acid addition salts of compounds. The invention also relates to a method for producing the above 5-benzyl-2,4-diaminopyrimidines, to the intermediate. products that are produced, to corresponding medicaments and to the use of 5-benzyl-2,4-diaminopyrimidines as medicinal preparations.Type: GrantFiled: July 18, 2002Date of Patent: November 23, 2004Assignee: Basilea Pharmaceutica AGInventors: Philippe Guerry, Peter Mohr, Marc Muller, Werner Mueller, Philippe Pflieger
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Patent number: 6797714Abstract: This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.Type: GrantFiled: August 21, 2002Date of Patent: September 28, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Richard D. Connell, Timothy G. Lease, Jeremy L. Baryza
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Patent number: 6787551Abstract: The present invention relates to a thiazolidinedione derivative, represented in formula (1) below, pharmaceutically acceptable salts thereof, and/or pharmaceutically acceptable solvates thereof. Further, the present invention provides a pharmaceutical composition comprising the compound represented in formula (1) below, wherein: X represents a carbon or nitrogen atom, Y represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen, or an aryl group, Z represents an oxygen, nitrogen, or sulfur atom, and R1 and R2 each represent a hydrogen atom; or R1 and R2 together form a bond.Type: GrantFiled: July 3, 2003Date of Patent: September 7, 2004Assignee: Chong Kun Dang Pharmaceutical CorporationInventors: Chung-Il Hong, Soon-Kil Ahn, Bok-Young Kim, Joong-Bok Ahn, Do-Young Lee, Hong-Woo Lee, Jae-Soo Shin
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Patent number: 6756367Abstract: The invention provides a compound of formula I wherein X, R1, R2 and Het are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.Type: GrantFiled: February 15, 2002Date of Patent: June 29, 2004Assignee: Novartis AGInventor: Bernhard Peter Neumann
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Publication number: 20040116424Abstract: The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula 1Type: ApplicationFiled: March 28, 2003Publication date: June 17, 2004Applicant: Neurogen CorporationInventors: George P. Luke, George D. Maynard, Scott Mitchell, Andrew Thurkauf, Linghong Xie, LuYan Zhang, Suoming Zhang, He Zhao, Bertrand L. Chenard, Yang Gao, Bingsong Han, Xiao Shu He
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Publication number: 20040102630Abstract: This invention relates to pyrimidine derivatives of general formula I 1Type: ApplicationFiled: November 7, 2002Publication date: May 27, 2004Applicant: Schering AGInventors: Thomas Brumby, Rolf Jautelat, Olaf Prien, Martina Schafer, Gerhard Siemeister, Ulrich Lucking, Christoph Huwe
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Patent number: 6734187Abstract: Purine derivatives represented by the following formula and salts thereof: wherein R1 represents a C1-C4 alkyl group or difluoromethyl group; R2 represents tetrahydrofuranyl group, a C1-C7 alkyl group and the like; X represents hydrogen atom, a halogen atom or nitro group; and A represents a group represented by the following formula: wherein R3 represents hydrogen atom, a halogen atom and the like; R4 and R5 represent hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxyl group and the like, which are useful as active ingredients of medicaments such as antiasthmatic agents.Type: GrantFiled: July 23, 2002Date of Patent: May 11, 2004Assignee: Mitsubishi Chemical CorporationInventors: Toshihiko Tanaka, Eiichirou Iwashita, Akiko Tarao, Akira Amenomori, Yuya Ono
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Publication number: 20040063945Abstract: The present invention relates to a 6-(1-fluoroethyl)-5-iodo-4-aminopyrimidine compound represented by the following formula (1): 1Type: ApplicationFiled: July 10, 2003Publication date: April 1, 2004Inventors: Katsutoshi Fujii, Shoji Shikita
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Publication number: 20040038969Abstract: Compounds having the general structure 1Type: ApplicationFiled: May 20, 2003Publication date: February 26, 2004Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Vassil I. Ognyanov, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Liping H. Pettus, Hui-Ling Wang, Xianghong Wang, Premilla Arasasingham
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Publication number: 20040029886Abstract: Dihalopropene compounds, process for their preparation, compositions comprising them and their use as pesticidesType: ApplicationFiled: November 7, 2002Publication date: February 12, 2004Inventors: Jorg Tiebes, Ralf Braun, Joachim Dickhaut, Harald Jakobi, Stephen Lindell, Vincent L. Salgado, Eva Wojtech, Daniela Jans, Jutta Maria Waibel, Waltraud Hempel, Ronald Wilhelm
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Patent number: 6686469Abstract: The invention relates to compounds of the general formula wherein R1 is unsubstituted or mono- to penta-substituted aryl, whereby the substituents are selected from the group consisting for instance of OH, Halogen, CN, C1-C6-alkyl, optionally substituted C3-C8-cycloalkyl and optionally substituted C3-C8-cycloalkenyl; A is for instance a single bond, C1-C12-alkylene or O; X1 and X2, independently of one another, are R10; X3 is H or R10; R10 is for instance halogen, CN, NO2, C1-C6-alkyl, C3-C8-cycloalkyl or C1-C6-haloalkyl; R21 and R22, independently of one another are for instance H, halogen, CN, NO2, OH, SH, C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-alkyl-C3-C8-cycloalkyl or C3-C8-cycloalkyl-C1-C6-alkyl; R23 and R24, independently of one another, are for instance H, C1-C6-alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C1-C6-haloalkyl or C3-C8-halocycloalkyl; m is 1, 2, 3 or 4; and n is 0, 1 or 2; as well as the physiologically acceptable addition compounds, a method of producingType: GrantFiled: November 5, 2001Date of Patent: February 3, 2004Assignee: Novartis Animal Health US, Inc.Inventors: Martin Eberle, André Jeanguenat, Werner Zambach, Arthur Steiger, Saleem Farooq
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Patent number: 6677353Abstract: 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. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: 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: 20040006068Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.Type: ApplicationFiled: January 24, 2003Publication date: January 8, 2004Applicant: Tularik Inc.Inventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
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Publication number: 20040006094Abstract: This invention provides novel neuroprotective 4-pyrimidineamine derivatives and neuroprotective pharmaceutical compositions comprising 4-pyrimidinamines. This invention also provides methods of using these compositions to prevent ischemic cell death, particularly neuronal cell death, and reduce the likelihood of neuronal cell death in a subject due to a traumatic event. Finally, this invention provides an apparatus for administering to a subject the instant pharmaceutical compositions.Type: ApplicationFiled: March 25, 2003Publication date: January 8, 2004Inventors: Elfrida R. Grant, Frank K. Brown, Robert Allan Zivin, Michael McMillian, Zhong Zhong, Malcolm Scott, Allen B. Reitz, Tina Morgan Ross
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Patent number: 6673795Abstract: The present invention is a pyrimidine, triazine or pyrazine derivative of the formula or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, X, Y and Z are as defined in the specification. The invention is a pharmaceutical composition containing an effective amount of the compound of formula 1, its preparation and to a method of treatment, control or prevention of acute and/or chronic neurological disorders by administering a therapeutically effective amount of a compound of formula 1.Type: GrantFiled: May 29, 2002Date of Patent: January 6, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Hans-Peter Maerki, Thierry Masquelin, Vincent Mutel, Maurice Wilhelm, Wolfgang Wostl
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Patent number: 6667342Abstract: Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a halocycloalkyl ring; R5 is a substituent as defined within; Y—Z is a linking group as defined within; are useful in the production of a elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.Type: GrantFiled: August 22, 2000Date of Patent: December 23, 2003Assignee: Astrazeneca ABInventors: David S Clarke, Jeremy N Burrows, Paul Ro Whittamore, Roger J Butlin, Thorsten Nowak
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Patent number: 6664247Abstract: This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ 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: December 19, 2001Date of Patent: December 16, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
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Patent number: 6657060Abstract: Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.Type: GrantFiled: November 8, 2001Date of Patent: December 2, 2003Assignee: Hoffman-La Roche Inc.Inventors: Volker Breu, Frank Dautzenberg, Patrizio Mattei, Werner Neidhart, Philippe Pflieger
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Patent number: 6653300Abstract: This invention describes novel pyrazole compounds of formula I′: wherein Q′ is —O—, —C(R6′)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclopropanediyl, and R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3 or L—Z—R3, or Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ 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: December 19, 2001Date of Patent: November 25, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Jeremy Green, David Kay, Ronald Knegtel, Andrew Miller, Ronald Tomlison, Pan Li
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Patent number: 6653301Abstract: This invention describes novel pyrazole compounds of formula IIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2 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: December 19, 2001Date of Patent: November 25, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Robert Davies, Julian M. C. Golec, David Kay, Ronald Knegtel, Sanjay Patel
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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: 20030203894Abstract: A compound represented by the formula (I): 1Type: ApplicationFiled: July 12, 2002Publication date: October 30, 2003Inventors: Hidekazu Tanaka, Kazuo Ueda, Shinji Suzuki, Hideyuki Takenaka
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Publication number: 20030195222Abstract: This invention relates to substituted pyrimidinone and pyrimidithione derivatives that bind with high affifnity to CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety disorders, and depression and stress related disorders.Type: ApplicationFiled: February 20, 2003Publication date: October 16, 2003Inventors: Jian-Min Fu, Jeffrey W. Corbett, Michael Dalton Ennis, Kristine E. Frank, Robert Louis Hoffman, Patrick R. Verhoest
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Patent number: 6632820Abstract: A pyrimidine derivative of formula (I) wherein, for example, R1 is-(1-6C)alkyl or (3-5C)alkenyl [optionally substituted by a phenyl substituent]; Q1 and Q2 are independently selected from phenyl, naphthyl, indanyl and 1,2,3,4-tetrahydronaphthyl; and one or both of Q1 and Q2 bears one substituent of formula (Ia) [provided that when present in Q1 the substituent of formula (Ia) is not adjacent to the —NH-link]; wherein, for example, X is CH2, O, S or NH; Y is H or as defined for Z; Z is OH, SH, NH2, (1-4C)alkoxy, (1-4C)alkylthio, —NH(1-4C)alkyl, —N[(1-4C)alkyl]2 or —NH-(3-8C)cycloalkyl; n is 1, 2 or 3; m is 1, 2 or 3; and Q1 and Q2 may each optionally bear other substituents selected from halogeno, (1-6C)alkyl, cyano and (2-4C)alkenyl, or a pharmaceutically-acceptable salt, or in-vivo-hydrolysable ester thereof; are useful as anti-cancer agents; and processes for their manufacture and pharmaceutical compositions containing them are describeType: GrantFiled: February 26, 2001Date of Patent: October 14, 2003Assignee: AstraZeneca ABInventors: Gloria Anne Breault, Philip John Jewsbury, Janet Elizabeth Pease
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Patent number: 6620963Abstract: Compounds of the formula where the variables have the meaning defined in the specification, which bind specifically or selectively to to RAR&agr; retinoid receptors.Type: GrantFiled: September 19, 2002Date of Patent: September 16, 2003Assignee: Allergan, Inc.Inventors: Tien T. Duong, Richard Beard, Roshantha A. Chandraratna
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Patent number: 6610678Abstract: This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R6 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R7 is hydrogen, C1-8alkyl, mono- or di(C3-6cyclo-alkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached maType: GrantFiled: October 8, 2002Date of Patent: August 26, 2003Inventors: Charles Huang, Keith M. Wilcoxen, Chen Chen, Mustapha Haddach, James R. McCarthy
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Patent number: 6608071Abstract: The invention relates to compounds of formula I wherein r is from 0 to 2; n is from 0 to 2; m is from 0 to 4; A, B, D and E are each independently of the others N or CH, with the proviso that not more than two of those radicals are N; G is lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa (—O—), thia (—S—) or imino (—NH—), or is lower alkylene substituted by acyloxy or by hydroxy; Q is lower alkyl, especially methyl; R is H or lower alkyl; X is imino, oxa or thia; Y is lower alkyl or, especially, aryl, heteroaryl or unsubstituted or substituted cycloalkyl; and Z is amino, mono- or di-substituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-di-substituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-loweType: GrantFiled: February 9, 2001Date of Patent: August 19, 2003Assignee: Novartis AGInventors: Karl-Heinz Altmann, Guido Bold, Paul William Manley
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Publication number: 20030144300Abstract: Compounds of formula (1.0.0) are described, as well as the usefulness of a pharmaceutical composition for treating inflammatory, respiratory and allergic diseases and conditions, especially asthma; chronic obstructive pulmonary disease (COPD) including chronic bronchitis, emphysema, and bronchiectasis; chronic rhinitis; and chronic sinusitis.Type: ApplicationFiled: July 24, 2002Publication date: July 31, 2003Inventors: Thomas Victor Magee, Anthony Marfat, Robert James Chambers
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Publication number: 20030139404Abstract: New compounds represented by the formula 1Type: ApplicationFiled: August 6, 2002Publication date: July 24, 2003Inventors: Rainer Haag, Ulrike Leser-Reiff, Anja Limberg, Michael Weidner, Gerd Zimmermann
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Patent number: 6596863Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formulaType: GrantFiled: April 29, 2002Date of Patent: July 22, 2003Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Substituted pyrimidines, processes for their preparation, and their use as pesticides and fungicides
Patent number: 6596727Abstract: Substituted 4-amino- and 4-alkoxy-cycloalkylpyrimidines, processes for their preparation, and their use as pesticides and fungicides The invention relates to compounds of the formula in which R1, R2, R3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.Type: GrantFiled: March 15, 1996Date of Patent: July 22, 2003Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lümmen, Werner Bonin -
Publication number: 20030130271Abstract: The invention provides compounds of formula 1Type: ApplicationFiled: August 27, 2002Publication date: July 10, 2003Applicant: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
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Patent number: 6589947Abstract: The present invention relates to compositions and methods of achieving a therapeutic effect including, the treatment or prevention of Syndrome X in an animal, preferably a mammal including a human subject or a companion animal, using a corticotropin releasing factor (CRF) antagonist alone or together with a glucocorticoid receptor antagonist.Type: GrantFiled: October 26, 2000Date of Patent: July 8, 2003Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Ernest S. Hamanaka, Yuhpyng Liang Chen
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Patent number: 6586433Abstract: 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. Preferred tertiary-heteroalkylamine compounds are substituted N-heteroaryl-N-phenyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: July 1, 2003Assignee: Pharmacia CorporationInventors: 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: 6583148Abstract: The present invention relates to novel derivatives of a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral systems.Type: GrantFiled: April 8, 1999Date of Patent: June 24, 2003Assignee: Krenitsky Pharmaceuticals, Inc.Inventors: James L. Kelley, Thomas A. Krenitsky, Lilia M. Beauchamp
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Publication number: 20030055062Abstract: The present invention relates to compounds represented by the structural Formula I: 1Type: ApplicationFiled: December 18, 2001Publication date: March 20, 2003Applicant: Schering CorporationInventors: Andrew Stamford, Youhao Dong, Stuart W. McCombie, Yusheng Wu