The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
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Publication number: 20030130325Abstract: A compound of the formula (I): 1Type: ApplicationFiled: July 10, 2002Publication date: July 10, 2003Inventor: Fumihiko Watanabe
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Publication number: 20030125565Abstract: The present invention relates to novel imidazolidine derivatives of the formula I, 1Type: ApplicationFiled: May 20, 2002Publication date: July 3, 2003Inventors: Volkmar Wehner, Hans Ulrich Stilz, Wolfgang Schmidt, Dirk Seiffge
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Patent number: 6586462Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an &agr; bonds, the solid triangle represents a &bgr; bond, the wavy segments represent &agr; or &bgr; bond, dashed lines represent a double bond or a single bond R, , R1, R2 and R3 are as defined in the specification.Type: GrantFiled: May 24, 2002Date of Patent: July 1, 2003Assignee: Allergan, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
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Patent number: 6583164Abstract: The composition of the present invention comprises a quaternized nitrogen-containing imidazole-1-yl or 1,2,4-triazole-1-yl compound wherein one of the nitrogen atoms constituting the azole ring is quaternized with a group eliminating in vivo and represented by the formula: wherein R1 represents a hydrocarbon or heterocyclic group which may be substituted, R2 represents a hydrogen atom or a lower alkyl group, and n is 0 or 1, and a saccharide, said compound being capable of being converted into an anti-fungal azole compound upon elimination of said group in vivo. The composition of the present invention is stable and usable particularly as a pharmaceutical preparation for an injection composition.Type: GrantFiled: March 19, 2001Date of Patent: June 24, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Hidetoshi Horibe, Yoko Nishida, Masao Nagao
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Patent number: 6569888Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt, in vivo hydrolysable ester, or an N—C1-6alkyl or N,N-di-(C1-6alkyl)amide thereof, where X is CH2 or SO2; R1 is an aryl optionally substituted by alkyl, alkenyl, alkynyl, halo, haloalkyl including perhaloalkyl such as trifluoromethyl, mercapto, alkoxy, haloalkoxy, alkenyloxy, alkynyloxy, hydroxyalkoxy, alkoxyalkoxy, alkanoyl, alkanoyloxy, cyano, nitro, amino, mono- or di-alkyl amino, oximino, sulphonamido, carbamoyl, mono or dialkylcarbamoyl or S(O)mR21 where m is defined above and R21 is hydrocarbyl; R4 is a group OR15 or S(O)qR15, where q is 0, 1 or 2 and R15 is a hydrogen-containing alkyl group substituted by at least one functional group as defined below, or an aryl group which is optionally substituted by one or more functional groups as defined below; and R2, R3, R5, R6 and R7 are specified organic groups.Type: GrantFiled: September 12, 2001Date of Patent: May 27, 2003Assignee: AstraZeneca ABInventors: Jason Kettle, Alan W Faull
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Patent number: 6555559Abstract: The present invention provides novel PGI2 derivatives and an anti Helicobacter agent, a platelet function potentiating agent or a cervical ripening agent containing any of the derivatives.Type: GrantFiled: August 1, 2000Date of Patent: April 29, 2003Assignee: Toray Industries, Inc.Inventors: Hisanori Wakita, Naohiro Yamada, Hitoshi Hatakeyama, Takeshi Ishigaki, Noriyuki Hirano, Takeshi Mori
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Publication number: 20030078435Abstract: The invention relates to a process for the synthesis of losartan potassium of formula (I), chemical name: 2-n-butyl-4-chloro-1-[(2′-(tetrazol-5-yl)-1,1′biphenyl-4-yl)-methyl]-imidazol-5-methanol potassium, starting from 2-n-butyl-4-chloro-1-[(2′-(2-triphenylmetyl-2H-tetrazol-5-yl)-1,1′-biphenyl-4-yl)-methyl]-1H-imidazol-4-methanol of formula (III). According to the process the compound of formula (III) is reacted in an alcohol of formula (VI),—wherein the meaning of R is C1-C4 straight chain alkyl group—with 0.1-1 equivalent of potassium hydroxide. The final product of formula (I) is isolated after crystallizing out by changing the solvent to an aprotic or weakly protic solvent (I).Type: ApplicationFiled: July 24, 2002Publication date: April 24, 2003Inventors: Janos Fischer, Ildiko Ballo, Endrene Petenyi, Janos Kreidl, Laszlo Czibula, Andras Nemes, Ida Deutschne Juhasz, Eva Werkne Papp, Judit Nagyne Bagdy, Istvan Hegeds, Jen?ouml;me Farkas
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Patent number: 6545152Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.Type: GrantFiled: July 18, 2000Date of Patent: April 8, 2003Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Venkatachalam
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Publication number: 20030064964Abstract: This invention relates to 8-aza prostanoid analogs which are generally EP4 receptor agonists and are represented by Formula I: 1Type: ApplicationFiled: July 16, 2002Publication date: April 3, 2003Inventors: Todd Richard Elworthy, Michael Garret Roepel, David Bernard Smith
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Publication number: 20030060494Abstract: The present invention relates to use of 1-carbamoylazole derivatives as medicaments and pharmaceutical compositions containing 1-carbamoylazole derivatives as the active ingredient, based on their DPPIV inhibiting effects.Type: ApplicationFiled: May 15, 2002Publication date: March 27, 2003Inventors: Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki, Seiji Yoshikawa, Toshimi Okada, Hironori Ikuta, Mika Koyanagi
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Patent number: 6531485Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: December 16, 1999Date of Patent: March 11, 2003Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Paul A. DaSilva-Jardine
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Publication number: 20030040535Abstract: The present invention relates to tetrazole compounds of Formula 1, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, and pharmaceutically acceptable salts of the prodrugs.Type: ApplicationFiled: June 21, 2002Publication date: February 27, 2003Inventors: Gary E. Aspnes, Yuan-Ching P. Chiang
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Patent number: 6525036Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.Type: GrantFiled: January 5, 2001Date of Patent: February 25, 2003Assignee: Merck & Co., Inc.Inventors: Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
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Patent number: 6518292Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably, and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.Type: GrantFiled: February 18, 2000Date of Patent: February 11, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, James J. Li, Jun Li, Stephen G. Swartz
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Publication number: 20030008895Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: ApplicationFiled: December 16, 1999Publication date: January 9, 2003Inventors: KIMBERLY O CAMERON, PAUL A. DASILVA-JARDINE
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Publication number: 20030004202Abstract: Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: ApplicationFiled: April 30, 2002Publication date: January 2, 2003Applicant: SmithKline Beecham CorporationInventors: John Duncan Elliott, Joseph Weinstock, Jia-Ning Xiang
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Patent number: 6498180Abstract: Compounds of formula (I) in which R1 is halo-C1-10 alkyl; halo-C2-10 alkenyl; or (CH2)nY in which n is 1 or 2 and Y is OH, CN, N3, OR3, SH, S(O)pR4, S(O)3H, NH2, NHR5, NR6R7, NHCOR8, NO2, CO2H, CONHR9, 1H-tetrazol-5-yl, 5-phenyltetrazol-2-yl or PO3H2; R3, R5, R6, R7, R8 and R9 are each selected independently from C1-4 alkyl, aryl and aryl-C1-4 alkyl; R4 is selected from C1-4 alkyl, aryl, aryl-C1-4 alkyl, and 1H-tetrazol-5-yl, carboxy-(1-4C)alkyl and 1H-tetrazol-5-yl-C1-4 alkyl; and p is 0, 1, 2 or 3; or a salt or ester thereof, provided that R1 is not methoxymethyl, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system.Type: GrantFiled: November 16, 2001Date of Patent: December 24, 2002Assignee: Eli Lilly and CompanyInventors: Ivan Collado Cano, Concepcion Pedregal Tercero, Alicia Marcos Llorente, Beatriz Lopez de Uralde Garmendia, Maria Rosario Gonzalez Garcia, Ana Belen Bueno Melendo
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Patent number: 6495604Abstract: The present invention provides a compound represented by the formula: wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula: wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents, and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating diseaseType: GrantFiled: August 14, 2000Date of Patent: December 17, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Yuzo Ichimori, Masayuki Ii, Katsumi Itoh, Tomoyuki Kitazaki, Junji Yamada
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Publication number: 20020188132Abstract: Compounds of the formula: 1Type: ApplicationFiled: December 4, 2000Publication date: December 12, 2002Inventors: Jeremy I. Levin, James M. Chen, Frances C. Nelson
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Publication number: 20020169192Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: ApplicationFiled: February 14, 2002Publication date: November 14, 2002Inventors: Cheryl M. Hayward, David A. Perry
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Publication number: 20020161237Abstract: Compounds of formula 1 and 1-1, 1Type: ApplicationFiled: January 5, 2001Publication date: October 31, 2002Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Patent number: 6451833Abstract: A class of N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders.Type: GrantFiled: November 1, 2000Date of Patent: September 17, 2002Assignee: Pharmacia CorporationInventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
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Patent number: 6448281Abstract: A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (CType: GrantFiled: July 3, 2001Date of Patent: September 10, 2002Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Patent number: 6441015Abstract: The present invention relates to tetrazole compounds of Formula I, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, and pharmaceutically acceptable salts of the prodrugs. The invention also relates to compositions comprising the tetrazole compounds and to methods of treating obesity, diabetes, atherosclerosis, hypertension, coronary heart disease, hypercholesterolemia, hyperlipidemia, thyroid disease, thyroid cancer, hypothyroidism, depression, glaucoma, cardiac arrhythmias, congestive heart failure, and osteoporosis using the tetrazole compounds.Type: GrantFiled: January 23, 2001Date of Patent: August 27, 2002Assignee: Pfizer Inc.Inventors: Gary E. Aspnes, Yuan-Ching P. Chiang
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Patent number: 6441177Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.Type: GrantFiled: December 16, 1999Date of Patent: August 27, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synèse Jolidon, Hans Lengsfeld, Olivier Morand, Gérard Schmid, Yu-Hua Ji
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Patent number: 6436904Abstract: Disclosed are compounds which bind VAL-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: January 21, 2000Date of Patent: August 20, 2002Assignees: Elan Pharmaceuticals, Inc., American Home Products CorporationInventors: Susan Ashwell, Reinhardt Bernhard Baudy, Michael A. Pleiss, Dimitrios Sarantakis, Eugene D. Thorsett
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Patent number: 6413996Abstract: The invention relates to compounds having the formula (I) or a pharmaceutically acceptable salt thereof. In the formula (I), X represents a group having the structural formula (II), and Y represents O or S. The compounds of the invention can be used a chloride channel blockers.Type: GrantFiled: March 8, 2001Date of Patent: July 2, 2002Assignee: Neurosearch A/SInventors: Bjarne H. Dahl, Palle Christophersen
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Patent number: 6410591Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma a therapeutically effective amount of a 3, 7 or 3 and 7 thia or oxa prostanoic acid derivative.Type: GrantFiled: May 8, 2001Date of Patent: June 25, 2002Assignee: Allergan Sales, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
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Patent number: 6407129Abstract: A quaternized nitrogen-containing imidazol-1-yl or 1,2,4-triazol-1-yl compound wherein one of the nitrogen atoms constituting an azole ring is quaternized with a substituent capable of being eliminated in vivo and the substituent can be eliminated in vivo to be converted into an antifungal azole compound, has an improved solubility in water, can advantageously be applied to injection, has an improved internal absorption and can be expected to have a good effect for the treatment or prevention of disease.Type: GrantFiled: September 20, 1999Date of Patent: June 18, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Katsumi Itoh, Tomoyuki Kitazaki, Kenji Okonogi
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Publication number: 20020065308Abstract: This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, 1Type: ApplicationFiled: November 21, 2001Publication date: May 30, 2002Inventors: Kimberly O. Cameron, Bruce A. Lefker
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Publication number: 20020065391Abstract: The present invention relates to compounds of the formula I 1Type: ApplicationFiled: November 29, 2001Publication date: May 30, 2002Inventors: Hans Ulrich Stilz, Volkmar Wehner, Christoph Huls, Dirk Seiffge
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Publication number: 20020065275Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: ApplicationFiled: January 16, 2002Publication date: May 30, 2002Inventor: Achyutharao Sidduri
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Publication number: 20020065230Abstract: The present invention provides bis-aminomethylcarbonyl compounds that are inhibitors of cysteine and serine proteases. The compounds are particularly useful for treating diseases in which excess cysteine protease activity has been implicated, including osteoporosis, periodontitis and arthritis.Type: ApplicationFiled: January 22, 2002Publication date: May 30, 2002Applicant: SmithKline Beecham CorporationInventors: William Edward Bondinell, Renee Louise Desjarlais, Daniel Frank Veber, Dennis Shinji Yamashita
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Patent number: 6388088Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: GrantFiled: October 11, 2001Date of Patent: May 14, 2002Assignee: Hoffman-La Roche Inc.Inventor: Achyutharao Sidduri
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Publication number: 20020045751Abstract: Compounds of the present invention of the formula 1Type: ApplicationFiled: September 28, 2001Publication date: April 18, 2002Inventor: Paivi Jaana Kukkola
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Patent number: 6369232Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: GrantFiled: August 8, 2001Date of Patent: April 9, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Achyutharao Sidduri
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Publication number: 20020040149Abstract: This invention is directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth comprising administering prostaglandin agonists which are EP4 receptor selective prostaglandin agonists.Type: ApplicationFiled: November 16, 2001Publication date: April 4, 2002Inventors: Kimberly O. Cameron, HuaZhu Ke, Bruce A. Lefker, David D. Thompson
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Patent number: 6365746Abstract: This invention relates to an organomercapto Au(I) complex having the formula [(M—SOL)n—A—S—Au—S—A—(SOL—M)n]M wherein M is a cationic counterion; SOL is a solubilizing group: A is a substituted or unsubstituted divalent organic linking group; and n is 1 to 4 and wherein the compound is symmetrical. It further relates to a method of manufacturing an organomercapto Au(I) complex comprising reacting an Au (I) complex with an organomercapto ligand and isolating the resulting organomercapto Au(I) complex from the reaction mixture.Type: GrantFiled: December 27, 1999Date of Patent: April 2, 2002Assignee: Eastman Kodak CompanyInventors: Roger Lok, Weimar W. White, Brian P. Cleary
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Publication number: 20020038035Abstract: A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders.Type: ApplicationFiled: April 3, 2001Publication date: March 28, 2002Applicant: G.D. Searle & Co.Inventors: David B. Reitz, Robert E. Manning
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Publication number: 20020035137Abstract: Compounds of formula (I) 1Type: ApplicationFiled: July 31, 2001Publication date: March 21, 2002Inventors: Gang Liu, Bruce G. Szczepankiewicz, Zhonghua Pei, Zhili Xin, Thorsten K. Oost, David A. Janowick
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Publication number: 20020035266Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: ApplicationFiled: August 8, 2001Publication date: March 21, 2002Inventor: Achyutharao Sidduri
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Patent number: 6358949Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: A, B, C and D are N or CH; X is a bond or (un)substituted CH2; R1 is lower alkenyl or (un)substituted lower alkyl; R3 is lower alkyl; and R2, R4, R5, and R6 are variables defined herein; which compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatroy disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility or glaucoma, or for the increase of permeability of blood-brain barrier, pain, asthma, and rhinitis.Type: GrantFiled: March 31, 2000Date of Patent: March 19, 2002Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Alan Hutchison, Kenneth Shaw, George D. Maynard, John M. Peterson, Richard Lew, Harry L. Brielmann
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Publication number: 20020032210Abstract: 1 The present invention discloses compounds having formula (I) wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.Type: ApplicationFiled: April 19, 2001Publication date: March 14, 2002Inventors: Bjarne H. Dahl, Palle Christophersen
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Patent number: 6352985Abstract: A benzimidazole compound represented by the formula (I): wherein R3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.Type: GrantFiled: January 28, 2000Date of Patent: March 5, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Noritsugu Yamasaki, Takafumi Imoto, Yoshiyuki Murai, Takahiro Hiramura, Teruo Oku, Kouzou Sawada
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Publication number: 20020016324Abstract: The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of andrographolide have the general formula (I).Type: ApplicationFiled: May 4, 2001Publication date: February 7, 2002Applicant: DR. REDDY'S RESEARCH FOUNDATIONInventors: Srinivas Nanduri, Sriram Rajagopal, Venkateswarlu Akella
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Patent number: 6335459Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor agonists, and which are represented by Formula I: wherein R1, R2, R3, R4, R5, A, and B are as defined in the specification, and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: December 7, 1999Date of Patent: January 1, 2002Assignee: Syntex (U.S.A.) LLCInventors: Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Daniel Lee Severance
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Patent number: 6333323Abstract: A compound of the formula: wherein R1 is hydrogen, lower alkyl, or optionally substituted arylsulfonyl, or the like, R2 is hydrogen, lower alkyl, or optionally substituted aralklyl, or the like, R3, R4, R5, and R6 each is independently hydrogen, halogen, trihalogenated lower alkyl, or the like, X is hydroxy or optionally substituted amino, Y is COOR R is hydrogen or an ester residue), optionally substituted aryl, or optionally substituted heteroaryl, has integrase inhibition activity, and is useful as an anti-HIV drug.Type: GrantFiled: August 18, 2000Date of Patent: December 25, 2001Assignee: Shionogi & Co., Ltd.Inventors: Toshio Fujishita, Tomokazu Yoshinaga
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Publication number: 20010047105Abstract: This invention is directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth comprising administering prostaglandin agonists which are EP4 receptor selective prostaglandin agonists.Type: ApplicationFiled: December 15, 2000Publication date: November 29, 2001Inventors: Kimberly O. Cameron, HuaZhu Ke, Bruce A. Lefker, David D. Thompson
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Patent number: 6323230Abstract: Derivatives of general chemical formula L(I) and (IV) are used in the topical treatment of diseases of the epithelial tissues, like psoriasis (epidermis) and ulcerative colitis L(lower intestine). These compounds display a high efficacy when administered for example by epicuaneous route in the case of dermatological illnesses like psoriasis, atopic dermatitis and other similar affections, or when administered by oral or rectal route in the case of diseases of the epithelia of the lower intestine like the ulcerative colitis and Crohn's disease.Type: GrantFiled: April 24, 2000Date of Patent: November 27, 2001Assignee: Geange Ltd.Inventor: Carla Rossi
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Patent number: 6319939Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkType: GrantFiled: June 1, 2000Date of Patent: November 20, 2001Assignee: Janssen Pharmaceutica N.V.Inventors: Dominique Mabire, Christophe Denis Adelinet, Imré Christian Csoka, Marc Gaston Venet