Chalcogen Attached Indirectly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/252)
-
Patent number: 6495580Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infections.Type: GrantFiled: October 18, 1999Date of Patent: December 17, 2002Assignee: ViroPharma IncorporatedInventors: Theodore J. Nitz, Daniel C. Pevear
-
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
-
Publication number: 20020187982Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.Type: ApplicationFiled: November 16, 2001Publication date: December 12, 2002Inventors: Carsten Behrens, Jesper Lau, Peter Madsen
-
Patent number: 6492363Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.Type: GrantFiled: August 16, 2001Date of Patent: December 10, 2002Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
-
Publication number: 20020173665Abstract: Compounds of formula (I) 1Type: ApplicationFiled: May 18, 2001Publication date: November 21, 2002Inventors: Chih-Hung Lee, Richard J. Perner, Daniel P. Larson, John R. Koenig, Arthur R. Gomtsyan, Guo Zhu Zheng, Stanley DiDomenico, Andrew O. Stewart, Erol K. Bayburt
-
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
-
Patent number: 6479518Abstract: The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.Type: GrantFiled: September 21, 2001Date of Patent: November 12, 2002Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Laura C. Meurer, Sander G. Mills, Malcolm MacCoss, Hongbo Qi
-
Patent number: 6479527Abstract: A pharmaceutical composition comprising a compound of formula (I): or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1 and wherein A and B together form an optionally substituted 5-member aromatic ring which includes at least one heteroatom; R1 is an optionally substituted aryl or heteroaryl ring; R2 is selected from a range of organic groups including carboxy, and R3 is hydrogen, or a range of organic groups; in combination with a pharmaceutically acceptable carrier. Certain compounds of formula (I) are novel and these form a further aspect of the invention.Type: GrantFiled: July 26, 2000Date of Patent: November 12, 2002Assignee: AstraZeneca UK LimitedInventors: Andrew J. Barker, Alan W Faull, Jason G. Kettle
-
Publication number: 20020165255Abstract: 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: October 19, 2001Publication date: November 7, 2002Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
-
Publication number: 20020165235Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: March 1, 2002Publication date: November 7, 2002Inventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
-
Publication number: 20020165398Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like.Type: ApplicationFiled: April 19, 2002Publication date: November 7, 2002Inventors: Lone Jeppesen, Henrik Sune Andersen, Ole Hvilsted Olsen, Luke Milburn Judge, Daniel Dale Holsworth, Farid Bakir, Frank Urban Axe, Yu Ge
-
Publication number: 20020151723Abstract: A method for producing a compound represented by the formula: 1Type: ApplicationFiled: January 16, 2002Publication date: October 17, 2002Applicant: TAKEDA CHEMICAL INDUSTRIES, LTD.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
-
Patent number: 6465503Abstract: The present invention provides novel compounds of Formula I: its prodrug forms, or pharmaceutically acceptable salts thereof. The compounds of this invention are inhibitors of uPA, and have utility as cancer treating agents.Type: GrantFiled: August 10, 2001Date of Patent: October 15, 2002Assignee: Axys Pharmaceuticals, Inc.Inventor: Richard Laurence Mackman
-
Patent number: 6458580Abstract: A method for promoting the growth of at least one anaerobic fungus in the rumen of a ruminant animal, the method comprising the step of administering to the rumen an effective amount of a degradation resistant sulphur source.Type: GrantFiled: September 27, 2000Date of Patent: October 1, 2002Assignees: Commonwealth Scientific and Industrial Research Organisation, Australian Wool Research and Promotion OrganizationInventors: Geoffrey Leslie Raymond Gordon, Michael William Phillips
-
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
-
Patent number: 6444840Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.Type: GrantFiled: September 28, 2000Date of Patent: September 3, 2002Assignee: The Procter & Gamble Co.Inventors: Mitchell Anthony deLong, Jack Snyder Amburgey, Jr., John August Wos, Biswanath De, David Lindsey Soper
-
Patent number: 6444701Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.Type: GrantFiled: November 8, 2001Date of Patent: September 3, 2002Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Fabio Giannessi, Mauro Marzi, Patrizia Minetti, Francesco De Angelis, Maria Ornella Tinti, Piero Chiodi, Arduino Arduini
-
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
-
Patent number: 6426359Abstract: This invention relates to the use of EP2 receptor subtype selective prostaglandin E2 agonists to augment bone mass including the prevention and treatment of skeletal disorders in mammals, including humans.Type: GrantFiled: June 11, 1999Date of Patent: July 30, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L Rosati, David D. Thompson
-
Patent number: 6417178Abstract: Amyloid binding compounds which are derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing Chrysamine G and derivatives thereof and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: November 6, 1997Date of Patent: July 9, 2002Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
-
Patent number: 6410582Abstract: The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.Type: GrantFiled: October 12, 2000Date of Patent: June 25, 2002Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
-
Patent number: 6410780Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.Type: GrantFiled: September 28, 2000Date of Patent: June 25, 2002Assignee: The Procter & Gamble Co.Inventors: Mitchell Anthony deLong, Jack Snyder Amburgey, Jr., John August Wos, Biswanath De, David Lindsey Soper
-
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
-
Patent number: 6410736Abstract: The present invention relates to compounds of formula I, and to their pharmaceutically acceptable salts. Compounds of formula I exhibit activity as serotonin, norepinephrine, and dopamine reuptake inhibitors and can be used in the treatment of central nervous system and other disorders.Type: GrantFiled: October 19, 2000Date of Patent: June 25, 2002Assignee: Pfizer Inc.Inventors: Harry R. Howard, Jr., Mavis D. Adam
-
Publication number: 20020077316Abstract: The present invention relates to novel sulfide and disulfide compounds, compositions comprising sulfide and disulfide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: ApplicationFiled: October 11, 2001Publication date: June 20, 2002Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
-
Patent number: 6407250Abstract: The present invention provides novel compounds represented by the general formula I. wherein m is an integer of from 1 to 3; n is 0 or an integer of from 1 to 4; R is selected from the group consisting of CO2H, CO2 R6, CH2OH, CH2O R6 and CONR3R4; R1 and R2 are independently selected from the group consisting of H, R6, C1-C6 alkenyl, C1-C6 alkynyl, C3-C7 cycloalkyl, C4-C12 alkylcycloalkyl, C6-C10 aryl, C7-C12 alkyl aryl radicals and heteroatom-substituted derivatives thereof, wherein one or more of the hydrogen or carbon atoms in said radicals is replaced with a halogen, nitrogen or sulfur-containing radical; R3 and R4 are selected from the group consisting of H and R6; and X is selected from the group consisting of R6, hydroxy, N(R6)2, CON(R6)2, SR6, sulfoxy, sulfone, halogen, COOR6, NO2, CN and OR6, wherein R6 is C1-C6 alkyl, and pharmaceutically acceptable salts thereof.Type: GrantFiled: September 14, 2000Date of Patent: June 18, 2002Assignee: Allergan Sales, Inc.Inventors: Robert M. Burk, Yariv Donde, Michael E. Garst
-
Publication number: 20020062031Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds.Type: ApplicationFiled: November 21, 2001Publication date: May 23, 2002Inventors: William C. Shakespeare, Michael G. Yang, Rajeswari Sundaramoorthi, Regine Bohacek, Charles Joseph Eyermann, Tomi K. Sawyer
-
Patent number: 6391902Abstract: Compounds of the Formulae (I) and (II): wherein R1, R2, R3, X, Y and Z are as defined in the specification which compounds are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel modulation.Type: GrantFiled: June 25, 2001Date of Patent: May 21, 2002Assignee: American Home Products CorporationInventors: Schuyler A. Antane, John A. Butera, Joseph R. Lennox
-
Publication number: 20020052512Abstract: A compound of formula 1a 1Type: ApplicationFiled: June 12, 2001Publication date: May 2, 2002Inventors: Nader Fotouhi, Paul Gillespie, Robert W. Guthrie, Sherrie L. Pietranico-Cole, Weiya Yun
-
Publication number: 20020049243Abstract: The present invention relates to pyrrolidine derivatives and dimeric forms and/or pharmaceutically acceptable esters, and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.Type: ApplicationFiled: July 17, 2001Publication date: April 25, 2002Inventors: Johannes Aebi, Denise Blum, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow, Eric Argirios Kitas, Bernd Michael Loeffler, Ulrike Obst, Sabine Wallbaum
-
Patent number: 6376524Abstract: Triphenyl compounds of the formulae I, II, and VI: methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are compounds are interleukin-4 antagonists; and are useful for the treatment of asthma and allergies.Type: GrantFiled: June 21, 2000Date of Patent: April 23, 2002Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Kenneth J. Barr, Brian C. Cunningham, William Michael Flanagan, Wanli Lu, Brian C. Raimundo, Nathan D. Waal, Jennifer Wilkinson, Jiang Zhu, Wenjin Yang
-
Patent number: 6376533Abstract: 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, R3 is heteroaryl or a substituted heteroaryl radical, R1 and R2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) and wherein R4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.Type: GrantFiled: October 20, 2000Date of Patent: April 23, 2002Assignee: Allergan Sales, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
-
Patent number: 6376532Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.Type: GrantFiled: January 25, 2001Date of Patent: April 23, 2002Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
-
Patent number: 6369084Abstract: This invention encompasses the novel compounds of formula A, which are useful in the treatment of prostaglandin mediated diseases, or a pharmaceutically acceptable salt, hydrate or ester thereof. The invention also encompasses certain pharmaceutical compositions and methods for treatment of prostaglandin mediated diseases comprising the use of compounds of formula A.Type: GrantFiled: September 14, 2000Date of Patent: April 9, 2002Assignee: Merck Frosst Canada & Co.Inventors: Patrick Lacombe, Marc Labelle, Rejean Ruel
-
Patent number: 6369073Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.Type: GrantFiled: October 2, 2000Date of Patent: April 9, 2002Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Fabio Giannessi, Mauro Marzi, Patrizia Minetti, Francesco De Angelis, Maria Ornella Tinti, Piero Chiodi, Arduino Arduini
-
Publication number: 20020035272Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: April 23, 2001Publication date: March 21, 2002Applicant: American Home Products CorporationInventors: Paul J. Dollings, Robert E. McDevitt, Folake O. Adebayo
-
Publication number: 20020032330Abstract: A propionic acid derivative having the following formula (II) and its salt: 1Type: ApplicationFiled: March 28, 2001Publication date: March 14, 2002Inventors: Yutaka Nomura, Shogo Sakuma, Seiichiro Masui
-
Patent number: 6355808Abstract: Benzimidazole derivatives of the formula (I): wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; R2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is —O—, —S(O)m— or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin Π antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g.Type: GrantFiled: March 27, 2001Date of Patent: March 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
-
Publication number: 20020028936Abstract: 1,3-Disubstituted Indolin-2-Ones compounds are useful in the treatment of neoplasia.Type: ApplicationFiled: September 28, 2001Publication date: March 7, 2002Inventors: Gerhard Sperl, Xiaojing Wang, Gary A. Piazza, Rifat Pamukcu
-
Patent number: 6350880Abstract: The present invention provides a crystalline or crystallized acid addition salt of Losartan useful for obtaining highly pure 2-n-butyl-4-chloro-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol (Losartan), and a purification method of Losartan that includes production of the crystalline or crystallized acid addition salt.Type: GrantFiled: November 16, 2000Date of Patent: February 26, 2002Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Tadashi Katsura, Hiroshi Shiratani, Nobushige Itaya
-
Patent number: 6346532Abstract: Amide derivatives represented by general formula (I) or salts thereof wherein each symbol has the following meaning: ring B: an optionally substituted heteroaryl optionally fused with a benzene ring; X: a bond, lower alkylene or lower alkenylene optionally substituted by hydroxy or lower alkyl, carbonyl, or a group represented by —NH— (when X is lower alkylene optionally substituted by lower alkyl which may be bonded to the hydrogen atom bonded to a constituent carbon atom of ring B to form lower alkylene to thereby form a ring); A: a lower alkylene or a group represented by -(lower alkylene)—O—; R1a and R1b: the same or different and each hydrogen or lower alkyl; R2: hydrogen or halogeno; and Z: nitrogen or a group represented by ═CH—.Type: GrantFiled: April 7, 2000Date of Patent: February 12, 2002Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Tatsuya Maruyama, Takayuki Suzuki, Kenichi Onda, Masahiko Hayakawa, Hiroyuki Moritomo, Tetsuya Kimizuka, Tetsuo Matsui
-
Publication number: 20020002177Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: ApplicationFiled: July 10, 2001Publication date: January 3, 2002Applicant: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
-
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
-
Patent number: 6326499Abstract: Omega chain modified 15-HETE derivatives and methods of their use for treating dry eye are disclosed.Type: GrantFiled: October 23, 2000Date of Patent: December 4, 2001Assignee: Alcon Universal Ltd.Inventor: David B. Belanger
-
Patent number: 6323190Abstract: A method for treating symptoms, diseases and conditions in extra-reproductive tract tissues that are responsive to treatment with estrogen, using triarylethanes of formula (I) wherein R1 is —O(CH2)mR3 or —(CH2)nR3; wherein R3 is an anionic substituent; m is an integer from 1 to 4; and n is an integer from 0 to 4; and wherein R2 is either H or —OH. Each of R1 and R2 can be either meta or para to its respective phenyl ethyl linkage. Compounds having the formula (I) wherein R1 is —O(CH2)mR3 or —(CH2)nR3; R3 is an anionic substituent; m is 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; R2 is H or —OH; and wherein each of R1 and R2 is independently meta or para to its respective phenyl ethyl linkage are also provided, with the proviso that R2 is not para —OH when m is 1 and R3 is —COOH.Type: GrantFiled: July 28, 1999Date of Patent: November 27, 2001Assignee: The Univeristy of Georgia Research Foundation, Inc.Inventor: Peter C. Ruenitz
-
Patent number: 6306887Abstract: Compounds of Formula (1.0.0): are described wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably —C(═O)—; B is independently selected from a group of moieties, the most preferred of which are those of partial Formulas (1.1.2) and (1.1.6): and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial Formula (1.9.0): where R1a is hydrogen when R1 has the meaning of a mono-valent substituent; and R1a is a single bond when R1 has the meaning of a di-valent substituent. Said compounds are useful in methods of treating or preventing an inflammatory, autoimmune or respiratory diseases by inhibiting cell adhesion and consequent or associated pathogenic processes subsequently mediated by VLA-4.Type: GrantFiled: June 23, 1999Date of Patent: October 23, 2001Assignee: Pfizer IncInventors: Louis S. Chupak, Allen J. Duplantier, Anthony J. Milici
-
Patent number: 6300364Abstract: Pharmaceutical compositions having a cholesterol-lowering effect which comprises as the active ingredient a compound having a PPAR (peroxisome proliferator-activated receptor)&dgr; activating effect or a PPAR&dgr;- and PPAR&ggr;-activating effect or a pharmaceutically acceptable salt thereof; pharmaceutical compositions wherein the cholesterol-lowering effect is an LDL-cholesterol-lowering effect; and a method for identifying a compound having a cholesterol-lowering effect characterized by measuring the PPAR&dgr;-activating effect or the PPAR&dgr;- and PPAR&ggr;-activating effect thereof. Means for Solution: It is found out that a compound exerting an excellent cholesterol-lowering effect on higher animals such as humans and ape has an effect of activating PPAR&dgr; or PPAR&dgr; and PPAR&ggr;.Type: GrantFiled: January 24, 2000Date of Patent: October 9, 2001Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Teruhiko Shimokawa, Satomi Nishijima, Koyo Matsuda, Yuichi Iizumi, Seiichi Hashimoto
-
Patent number: 6294561Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: November 14, 2000Date of Patent: September 25, 2001Assignee: ICOS CorporationInventors: Kerry W. Fowler, Joshua Odingo
-
Patent number: 6291682Abstract: Pyrazol-4-ylbenzoyl derivatives where the substituents L, M, X, Y and n have the meanings given in claim 1 and Q is a pyrazole ring, linked in the 4-position, of the formula II where R15 is C1-C4-alkyl, R16 is hydrogen, C1-C4-alkyl or C1-C4-haloalkyl and R17 is hydrogen, C1-C4-alkylsulfonyl, phenylsulfonyl or alkylphenylsulfonyl, where, in the event that Y=C═O, X is other than NR23, agriculturally useful salts, a process for their preparation, and their use as herbicides.Type: GrantFiled: February 24, 1998Date of Patent: September 18, 2001Assignee: BASF AktiengesellschaftInventors: Martina Otten, Wolfgang von Deyn, Stefan Engel, Regina Luise Hill, Uwe Kardorff, Marcus Vossen, Peter Plath, Norbert Götz, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
-
Patent number: 6288099Abstract: Compounds of the Formulae (I) and (II): wherein R1, R2, R3, X, Y and Z are as defined in the specification which compounds are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel modulation.Type: GrantFiled: December 3, 1999Date of Patent: September 11, 2001Assignee: American Home Products CorporationInventors: Schuyler A. Antane, John A. Butera, Joseph R. Lennox