Polycyclo Ring System Patents (Class 562/427)
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Patent number: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
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Patent number: 7250529Abstract: A highly advantageous process for the preparation of 2-(3-hydroxy-1-adamantyl)-2-oxoacetic acid or a salt thereof is described. The process comprises subjecting 1-acetyl 3-hydroxyadamantane to liquid phase oxidation with permanganate to produce 2-(3-hydroxy-1-adamantyl)-2-oxoacetic acid or a salt thereof, with acidification to form the free acid when appropriate.Type: GrantFiled: September 16, 2005Date of Patent: July 31, 2007Assignee: Albemarle CorporationInventor: Eric L. Williams
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Patent number: 7199265Abstract: This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor ?, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.Type: GrantFiled: June 15, 2001Date of Patent: April 3, 2007Assignee: Karo Bio ABInventors: Li Yi-Lin, Johan Malm, Chris Litten, Ana Maria Garcia Collazo, Neeraj Garg
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Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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Patent number: 7129374Abstract: The invention provides small molecules that act as catalytic antioxidants and methods of use thereof. The compounds can repeatedly bind and destroy reactive oxygen species by serving as substates for enzymes of the methionine sulfoxide reductase (Msr) class. Some embodiments of the catalytic antioxidant compounds are derived from drugs with anti-inflammatory activity due to inhibition of cyclooxygenase enzymes.Type: GrantFiled: November 26, 2003Date of Patent: October 31, 2006Assignees: Florida Atlantic University, Hospital for Special SurgeryInventors: Herbert Weissbach, Nathan Brot
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Patent number: 7091245Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? suptype.Type: GrantFiled: September 4, 2003Date of Patent: August 15, 2006Assignee: Novo Novdisk A/SInventors: Lone Jeppesen, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
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Patent number: 6960683Abstract: Organic amine salts of compounds of the formula: and their pharmaceutically acceptable salts, and uses in medical therapy are provided.Type: GrantFiled: July 14, 2003Date of Patent: November 1, 2005Assignee: Atherogenics, Inc.Inventor: Charles Q. Meng
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Patent number: 6946474Abstract: The present invention provides trichloroethyl-sulfonylurea-containing compounds that inhibit glycing transporters, pharmaceutical compositions comprising such compounds, methods for using such compounds for inhibiting glycine transporters and methods for using such compounds for the treatment of disease states in which glycine is involved.Type: GrantFiled: September 13, 2001Date of Patent: September 20, 2005Assignee: Merck & Co., Inc.Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
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Patent number: 6936636Abstract: Compounds of the formula: where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.Type: GrantFiled: June 26, 2003Date of Patent: August 30, 2005Assignee: Allergan, Inc.Inventors: Santosh Sinha, Kwok Yin Tsang, Smita Bhat, Roshantha A. Chandraratna
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Patent number: 6916837Abstract: Amidino derivatives represented by the following general formula (I): {where X is a group represented by R1SO2NR2— (wherein R1 represents optionally substituted C6-14 aryl, etc. and R2 represents hydrogen atom, etc.), etc., Ar1 represents 2,6-naphthylene, etc., R3 represents hydrogen atom, etc. and Y represents carboxyphenyl, etc.} and their pharmacologically acceptable salts or solvates.Type: GrantFiled: November 14, 2002Date of Patent: July 12, 2005Assignee: Eisai Co., Ltd.Inventors: Takashi Satoh, Yasushi Okamoto, Osamu Asano, Nobuhisa Watanabe, Tadashi Nagakura, Takao Saeki, Atsushi Inoue, Masahiro Sakurai
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Patent number: 6897237Abstract: A compound of the formula (I): wherein R1 is hydroxy and the like; R2 is optionally substituted lower alkyl and the like; R3 is hydrogen atom and the like; R4 is optionally substituted arylene and the like; R5 is —C?C— and the like; R6 is optionally substituted naphtyl and the like its optically active substance, its prodrug, their pharmaceutically acceptable salt, or solvate thereof.Type: GrantFiled: April 23, 2001Date of Patent: May 24, 2005Assignee: Shionogi & Co. Ltd.Inventors: Yozo Hori, Fumihiko Watanabe, Hiroshige Tsuzuki, Shingo Furue, Yoshinori Tamura
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Patent number: 6884907Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: GrantFiled: May 10, 2002Date of Patent: April 26, 2005Assignee: Guilford Pharmaceuticals Inc.Inventors: Takashi Tsukamoto, Pavel Majer, Bunda Hin, Weizheng Xu, Qun Liu, Doris Stoermer
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Patent number: 6869975Abstract: Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.Type: GrantFiled: September 13, 2002Date of Patent: March 22, 2005Assignees: Tularik Inc., Japan Tobacco, Inc.Inventors: Hiroyuki Abe, Jonathan Houze, Hisashi Kawasaki, Frank Kayser, Rajiv Sharma, Samuel Sperry
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Patent number: 6777418Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.Type: GrantFiled: October 1, 2001Date of Patent: August 17, 2004Assignee: Syntex (U.S.A.) LLCInventors: Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
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Patent number: 6767920Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein hatched lines represent the &agr; configuration, a triangle represents the &bgr; configuration, a wavy line represents the &agr; configuration or the &bgr; configuration and a dotted line represents the presence or absence of a double bond; A and B are independently selected from the group consisting of O, S and CH2; provided that at least one of A or B is S; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents mayType: GrantFiled: January 16, 2003Date of Patent: July 27, 2004Assignee: Allergan, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
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Publication number: 20040110951Abstract: The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands.Type: ApplicationFiled: July 11, 2003Publication date: June 10, 2004Inventor: Yuan-Ching P. Chiang
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Patent number: 6747148Abstract: Sulfonamide derivatives, their physiologically tolerable salts and their prodrugs according to the present invention are vitronectin receptor antagonists and inhibitors of cell adhesion, as well as inhibit bone resorption by osteoclasts. These derivatives, salts and prodrugs are pharmaceutically active compounds useful in the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. Processes for the preparation of the sulfonamide derivatives according to the present invention, the use of these derivatives as pharmaceutically active ingredients, and pharmaceutical preparations comprising these derivatives also are disclosed.Type: GrantFiled: October 9, 2001Date of Patent: June 8, 2004Assignees: Hoechst Marion Roussel Deutschland GmbH, Genentech, Inc.Inventors: Anuschirwan Peyman, David William Will, Jochen Knolle, Karlheinz Scheunemann, Denis Carniato, Jean-Francois Gourvest, Thomas R. Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
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Publication number: 20040034237Abstract: The subject invention provides useful and novel calcium channel blockers based upon mibefradil. The subject invention also provides methods for synthesizing the compounds of the invention. The invention also provides methods for the control or prevention of hypertension, angina pectoris, ischemia, arrhythmias, and cardiac insufficiency in a patient by administering a compound, or composition, of the invention to an individual in need of such treatment.Type: ApplicationFiled: August 18, 2003Publication date: February 19, 2004Inventors: Pascal Druzgala, Peter G. Milner, Jurg Pfister, Xiaoming Zhang
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Patent number: 6693136Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 containing receptor antagonists and are useful in treating pain, urinary incontinence, and bladder overactivity.Type: GrantFiled: July 26, 2002Date of Patent: February 17, 2004Assignee: Abbott LaboratoriesInventors: Chih-Hung Lee, Meiqun Jiang, Richard A. Perner, Arthur Gomtsyan, Erol K. Bayburt, Guo Zhu Zheng
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Patent number: 6653483Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: April 17, 2000Date of Patent: November 25, 2003Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6632816Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1 may be, for example, iso-butyl, wherein X and Y, same or different, may be, for example, NH2 and F, and wherein R2 and R3 are as defined herein.Type: GrantFiled: December 23, 2002Date of Patent: October 14, 2003Assignee: Pharmacor Inc.Inventors: Brent Richard Stranix, Jean-François Lavallée, Nicolas LeBerre, Valérie Perron
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Patent number: 6613782Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.Type: GrantFiled: February 21, 2002Date of Patent: September 2, 2003Assignee: Novartis AGInventors: Stéphane De Lombaert, Cynthia Anne Fink, Fariborz Firooznia, Denton Wade Hoyer, Arco Yingcheu Jeng
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Patent number: 6610882Abstract: The invention relates to compounds of formula in which R1 to R9, R16 and R17 are as defined in claim 1. These compounds are pharmacologically active.Type: GrantFiled: June 7, 2002Date of Patent: August 26, 2003Assignee: Sanofi-SynthelaboInventors: Bernard Ferrari, Jean Gougat, Claude Muneaux, Yvette Muneaux, Pierre Perreaut, Claudine Planchenault
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Patent number: 6603012Abstract: New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.Type: GrantFiled: April 23, 2001Date of Patent: August 5, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Paula Nanette Belloni, Synese Jolidon, Michael Klaus, Jean-Marc Lapierre
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Patent number: 6603041Abstract: Enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an optionally substituted arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; X is an O or S atom or the group NR30 group; j and k is each zero or the integer 1 or 2 provided that the sum of j and k is zero or the integer 1 or 2; Cy1 is an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof.Type: GrantFiled: September 5, 2001Date of Patent: August 5, 2003Assignee: Celltech R & D LimitedInventors: Timothy John Norman, John Robert Porter, John Clifford Head, Andrew James Ratcliffe
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6492422Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: March 27, 2002Date of Patent: December 10, 2002Assignee: Warner-Lambert CompanyInventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic
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Patent number: 6448254Abstract: Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the following meanings: R1 [sic] can be C1-C6-alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, where the rings can additionally be substituted by up to 2 radicals R4 [sic], and R2 [sic] is —(CH2)m—R8 [sic], where R8 [sic] can be phenyl, cyclohexyl- or indolyl and m=1 to 6, and X is a bond, —CH2—, —CH2CH2—, —CH═CH—, —C≡C—, —CONH—, —SO2NH— [sic], and and [sic] R1—X [sic] together are also and R3 [sic] is hydrogen and CO—NR6R7 [sic], R4 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched anType: GrantFiled: October 3, 2000Date of Patent: September 10, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Patent number: 6433021Abstract: Indane compounds of general formulae (1) to (4) and their pharmaceutical use, particularly to achieve mast cell stabilising activity and/or anti-inflammatory activity are described.Type: GrantFiled: December 3, 1999Date of Patent: August 13, 2002Assignee: Venantius LimitedInventors: Neil Frankish, Helen Sheridan, John Walsh, Michael Jordan
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Patent number: 6423727Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.Type: GrantFiled: October 16, 2000Date of Patent: July 23, 2002Assignee: Novartis AGInventors: Stéphane De Lombaert, Cynthia Anne Fink, Fariborz Firooznia, Denton Wade Hoyer, Arco Yingcheu Jeng
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Patent number: 6387951Abstract: Compounds having Formulas 5 and 6 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: May 14, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
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Publication number: 20020019543Abstract: Ar is optionally substituted with 1 to 3 RX groups, and where n is 0, 1, 2 or 3; and a group of formula III: 1Type: ApplicationFiled: December 20, 2000Publication date: February 14, 2002Inventors: James M. Balkovec, Mark L. Greenlee, Milton L. Hammond, James V. Heck
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Patent number: 6313119Abstract: Sulfonamide derivatives, their physiologically tolerable salts and their prodrugs according to the present invention are vitronectin receptor antagonists and inhibitors of cell adhesion, as well as inhibit bone resorption by osteoclasts. These derivatives, salts and prodrugs are pharmaceutically active compounds useful in the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. Processes for the preparation of the sulfonamide derivatives according to the present invention, the use of these derivatives as pharmaceutically active ingredients, and pharmaceutical preparations comprising these derivatives also are disclosed.Type: GrantFiled: May 5, 2000Date of Patent: November 6, 2001Assignees: Adventis Pharma Deutschland GmbH, Genentech, Inc.Inventors: Anuschirwan Peyman, David William Will, Jochen Knolle, Karlheinz Scheunemann, Denis Carniato, Jean-Francois Gourvest, Thomas R. Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
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Patent number: 6291702Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be colorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.Type: GrantFiled: February 8, 2000Date of Patent: September 18, 2001Assignee: Florida International UniversityInventor: David Alan Becker
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Patent number: 6265603Abstract: Peptidomimetic isoprenyl transferase inhibitors R6SCHR1′CHR1WCHR2YC(:X)NR3CHR5COR4 wherein R1=OH, H, alkyl, amino group or R1 and R6 together form a heterocyclic ring; R1′=H, alkyl, aryl; R2=H, alkyl, arylalkyl, heteroarylalkyl; R3=H, alkyl, arylalkyl; R4=OH, alkoxy, amino group; R5=natural amino acid residue or D—E—F, where D is alkyl or alkenyl, E is O, S, N, or null, F is H, alkyl, aryl, carboxy amino, etc.; R6=H, alkyl, acyl, etc.; W=alkyl, alkenyl; X=O, S, Y is M—O—P, where M is C0-6 alkyl, O is oxygen-C0-4 alkyl, P is(un)substituted C6-20 aryl are disclosed.Type: GrantFiled: April 1, 1999Date of Patent: July 24, 2001Assignee: Eisai Co., Ltd.Inventors: Michael D. Lewis, Ana Maria Garcia, James J. Kowalczyk, Hu Yang, Eric Schwartz
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Patent number: 6248781Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 19, 1999Date of Patent: June 19, 2001Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6235777Abstract: A benzenesulfonamide compound of the formula (I) (R1 is hydroxy, C1˜4 alkoxy, NR6R7 (each R6 and R7 is, independently, H or C1˜4 alkyl.); R2 is H, C1˜4 alkyl; R3, R4 are C1˜4 alkyl, halogen trifluoromethyl; R5 is H, C1˜4 alkyl, halogen, trifluoromethyl; Y is cis-vinylene, trans-vinylene; and the symbol (i) is single bond, double bond.), non-toxic salt thereof or cyclodextrin clathrate thereof and an antagonist of EP1 receptor which is a prostaglandin E2 receptor subtype comprising it as an active ingredient. The present invention compounds of the of the formula (I) can bind strongly to EP1 receptor which is a prostaglandin E2 receptor subtype and scarcely bind to the other receptor subtypes. Therefore, they are considered to be useful as antipyretic agents, as analgesics or as treating agent for pollakiuria having little side effect.Type: GrantFiled: May 14, 1998Date of Patent: May 22, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Yuuki Nagao, Takayuki Maruyama
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Patent number: 6235779Abstract: Cis-&Dgr;4 analogs of prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: June 2, 1999Date of Patent: May 22, 2001Assignee: Alcon Laboratories, Inc.Inventors: Peter G. Klimko, Paul W. Zinke
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Patent number: 6201019Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.Type: GrantFiled: April 8, 1999Date of Patent: March 13, 2001Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Philippe Diaz
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Patent number: 6187933Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: January 27, 2000Date of Patent: February 13, 2001Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 6172115Abstract: A method is provided for preventing or reducing the risk of restenosis following angioplasty by administering a retinoid, such as an RXR-selective retinoid, e.g. the compound of the formula: and pharmaceutically acceptable salts and esters and amides thereof.Type: GrantFiled: January 12, 1998Date of Patent: January 9, 2001Assignee: Allergan Sales, Inc.Inventor: Roshantha A. Chandraratna
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Patent number: 6166072Abstract: Described herein are compounds having the general formula: ##STR1## wherein: Ar.sup.1 and Ar.sup.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sup.1 or Ar.sup.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sup.1 and Ar.sup.Type: GrantFiled: June 29, 1999Date of Patent: December 26, 2000Assignee: Allelix Neuroscience, Inc.Inventors: Stanley Charles Bell, Michael De Vivo, Allen Hopper, Methvin Isaac, Anne O'Brien, Vassil Ilya Ognyanov, Richard Schumacher
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Patent number: 6156798Abstract: A compound of the formula ##STR1## wherein Y and R.sup.1 are defined in the specification, useful in the treatment of arthritis or cancer and other diseases involving selective inhibition of matrix metalloproteinase-13.Type: GrantFiled: April 9, 1999Date of Patent: December 5, 2000Assignee: Pfizer IncInventor: Lawrence A. Reiter
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Patent number: 6117869Abstract: The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds ##STR1## More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilatation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: July 26, 1999Date of Patent: September 12, 2000Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Bruce David Roth, Drago Robert Sliskovic
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Patent number: 6114568Abstract: The present invention relates to a process for alkylating hindered sulfonamides useful as intermediates in the preparation of matrix metalloproteinase inhibitors.Type: GrantFiled: April 9, 1999Date of Patent: September 5, 2000Assignee: Pfizer Inc.Inventors: Brian Michael Andresen, Phillip Dietrich Hammen, Joel Michael Hawkins
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Patent number: 6087389Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: June 18, 1998Date of Patent: July 11, 2000Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 6017925Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, viral disease, and tumor growth.Type: GrantFiled: January 13, 1998Date of Patent: January 25, 2000Assignee: Merck & Co., Inc.Inventor: Mark E. Duggan
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Patent number: 6018068Abstract: The naphthyloxyacetic acid derivatives of the formula (I) ##STR1## wherein A is H, --(alkylene)COOR.sup.1, --(alkylene)CONR.sup.2 R.sup., --(alkylene)OH, --(alkylene)tetrazole, --(alkylene)CN; E is single bond or alkylene; G is --S--, --SO--, --SO.sub.2 --, --O-- or --NR.sup.4 --; L is alkylene, --(CH.sub.2).sub.m --CH=CH--(CH.sub.2).sub.n -- or --(CH.sub.2).sub.x --CH(OH)--(CH.sub.2).sub.y --; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE.sub.2 receptor and exhibit the activity to antagonize or agonize for PGE.sub.2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.Type: GrantFiled: January 26, 1998Date of Patent: January 25, 2000Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Yuuki Nagao, Kazuhiko Torisu, Nobuyuki Hamanaka
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Patent number: 5998471Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification.Type: GrantFiled: August 11, 1998Date of Patent: December 7, 1999Assignee: Allergan Sales, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5985928Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: January 9, 1998Date of Patent: November 16, 1999Assignee: Centre International De Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon