Polycyclo Ring System Patents (Class 562/427)
  • Patent number: 7250529
    Abstract: 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: Grant
    Filed: September 16, 2005
    Date of Patent: July 31, 2007
    Assignee: Albemarle Corporation
    Inventor: Eric L. Williams
  • Patent number: 7199265
    Abstract: 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: Grant
    Filed: June 15, 2001
    Date of Patent: April 3, 2007
    Assignee: Karo Bio AB
    Inventors: Li Yi-Lin, Johan Malm, Chris Litten, Ana Maria Garcia Collazo, Neeraj Garg
  • Patent number: 7157454
    Abstract: 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: Grant
    Filed: March 27, 2002
    Date of Patent: January 2, 2007
    Assignee: Sanofi-Aventis
    Inventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
  • Patent number: 7129374
    Abstract: 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: Grant
    Filed: November 26, 2003
    Date of Patent: October 31, 2006
    Assignees: Florida Atlantic University, Hospital for Special Surgery
    Inventors: Herbert Weissbach, Nathan Brot
  • Patent number: 7091245
    Abstract: 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: Grant
    Filed: September 4, 2003
    Date of Patent: August 15, 2006
    Assignee: Novo Novdisk A/S
    Inventors: Lone Jeppesen, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
  • Patent number: 6960683
    Abstract: Organic amine salts of compounds of the formula: and their pharmaceutically acceptable salts, and uses in medical therapy are provided.
    Type: Grant
    Filed: July 14, 2003
    Date of Patent: November 1, 2005
    Assignee: Atherogenics, Inc.
    Inventor: Charles Q. Meng
  • Patent number: 6946474
    Abstract: 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: Grant
    Filed: September 13, 2001
    Date of Patent: September 20, 2005
    Assignee: Merck & Co., Inc.
    Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
  • Patent number: 6936636
    Abstract: 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: Grant
    Filed: June 26, 2003
    Date of Patent: August 30, 2005
    Assignee: Allergan, Inc.
    Inventors: Santosh Sinha, Kwok Yin Tsang, Smita Bhat, Roshantha A. Chandraratna
  • Patent number: 6916837
    Abstract: 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: Grant
    Filed: November 14, 2002
    Date of Patent: July 12, 2005
    Assignee: Eisai Co., Ltd.
    Inventors: Takashi Satoh, Yasushi Okamoto, Osamu Asano, Nobuhisa Watanabe, Tadashi Nagakura, Takao Saeki, Atsushi Inoue, Masahiro Sakurai
  • Patent number: 6897237
    Abstract: 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: Grant
    Filed: April 23, 2001
    Date of Patent: May 24, 2005
    Assignee: Shionogi & Co. Ltd.
    Inventors: Yozo Hori, Fumihiko Watanabe, Hiroshige Tsuzuki, Shingo Furue, Yoshinori Tamura
  • Patent number: 6884907
    Abstract: 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: Grant
    Filed: May 10, 2002
    Date of Patent: April 26, 2005
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Takashi Tsukamoto, Pavel Majer, Bunda Hin, Weizheng Xu, Qun Liu, Doris Stoermer
  • Patent number: 6869975
    Abstract: 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: Grant
    Filed: September 13, 2002
    Date of Patent: March 22, 2005
    Assignees: Tularik Inc., Japan Tobacco, Inc.
    Inventors: Hiroyuki Abe, Jonathan Houze, Hisashi Kawasaki, Frank Kayser, Rajiv Sharma, Samuel Sperry
  • Patent number: 6777418
    Abstract: 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: Grant
    Filed: October 1, 2001
    Date of Patent: August 17, 2004
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
  • Patent number: 6767920
    Abstract: 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 may
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: July 27, 2004
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
  • Publication number: 20040110951
    Abstract: The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands.
    Type: Application
    Filed: July 11, 2003
    Publication date: June 10, 2004
    Inventor: Yuan-Ching P. Chiang
  • Patent number: 6747148
    Abstract: 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: Grant
    Filed: October 9, 2001
    Date of Patent: June 8, 2004
    Assignees: 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
  • Publication number: 20040034237
    Abstract: 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: Application
    Filed: August 18, 2003
    Publication date: February 19, 2004
    Inventors: Pascal Druzgala, Peter G. Milner, Jurg Pfister, Xiaoming Zhang
  • Patent number: 6693136
    Abstract: 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: Grant
    Filed: July 26, 2002
    Date of Patent: February 17, 2004
    Assignee: Abbott Laboratories
    Inventors: Chih-Hung Lee, Meiqun Jiang, Richard A. Perner, Arthur Gomtsyan, Erol K. Bayburt, Guo Zhu Zheng
  • Patent number: 6653483
    Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: November 25, 2003
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 6632816
    Abstract: 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: Grant
    Filed: December 23, 2002
    Date of Patent: October 14, 2003
    Assignee: Pharmacor Inc.
    Inventors: Brent Richard Stranix, Jean-François Lavallée, Nicolas LeBerre, Valérie Perron
  • Patent number: 6613782
    Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.
    Type: Grant
    Filed: February 21, 2002
    Date of Patent: September 2, 2003
    Assignee: Novartis AG
    Inventors: Stéphane De Lombaert, Cynthia Anne Fink, Fariborz Firooznia, Denton Wade Hoyer, Arco Yingcheu Jeng
  • Patent number: 6610882
    Abstract: 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: Grant
    Filed: June 7, 2002
    Date of Patent: August 26, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Bernard Ferrari, Jean Gougat, Claude Muneaux, Yvette Muneaux, Pierre Perreaut, Claudine Planchenault
  • Patent number: 6603041
    Abstract: 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: Grant
    Filed: September 5, 2001
    Date of Patent: August 5, 2003
    Assignee: Celltech R & D Limited
    Inventors: Timothy John Norman, John Robert Porter, John Clifford Head, Andrew James Ratcliffe
  • Patent number: 6603012
    Abstract: 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: Grant
    Filed: April 23, 2001
    Date of Patent: August 5, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paula Nanette Belloni, Synese Jolidon, Michael Klaus, Jean-Marc Lapierre
  • Patent number: 6495546
    Abstract: 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: Grant
    Filed: November 22, 2000
    Date of Patent: December 17, 2002
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
  • Patent number: 6492422
    Abstract: 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: Grant
    Filed: March 27, 2002
    Date of Patent: December 10, 2002
    Assignee: Warner-Lambert Company
    Inventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic
  • Patent number: 6448254
    Abstract: 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 an
    Type: Grant
    Filed: October 3, 2000
    Date of Patent: September 10, 2002
    Assignee: Abbott Laboratories
    Inventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
  • Patent number: 6433021
    Abstract: 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: Grant
    Filed: December 3, 1999
    Date of Patent: August 13, 2002
    Assignee: Venantius Limited
    Inventors: Neil Frankish, Helen Sheridan, John Walsh, Michael Jordan
  • Patent number: 6423727
    Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.
    Type: Grant
    Filed: October 16, 2000
    Date of Patent: July 23, 2002
    Assignee: Novartis AG
    Inventors: Stéphane De Lombaert, Cynthia Anne Fink, Fariborz Firooznia, Denton Wade Hoyer, Arco Yingcheu Jeng
  • Patent number: 6387951
    Abstract: 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: Grant
    Filed: August 29, 2000
    Date of Patent: May 14, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
  • Publication number: 20020019543
    Abstract: 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: 1
    Type: Application
    Filed: December 20, 2000
    Publication date: February 14, 2002
    Inventors: James M. Balkovec, Mark L. Greenlee, Milton L. Hammond, James V. Heck
  • Patent number: 6313119
    Abstract: 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: Grant
    Filed: May 5, 2000
    Date of Patent: November 6, 2001
    Assignees: 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
  • Patent number: 6291702
    Abstract: 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: Grant
    Filed: February 8, 2000
    Date of Patent: September 18, 2001
    Assignee: Florida International University
    Inventor: David Alan Becker
  • Patent number: 6265603
    Abstract: 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: Grant
    Filed: April 1, 1999
    Date of Patent: July 24, 2001
    Assignee: Eisai Co., Ltd.
    Inventors: Michael D. Lewis, Ana Maria Garcia, James J. Kowalczyk, Hu Yang, Eric Schwartz
  • Patent number: 6248781
    Abstract: 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: Grant
    Filed: October 19, 1999
    Date of Patent: June 19, 2001
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6235779
    Abstract: Cis-&Dgr;4 analogs of prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.
    Type: Grant
    Filed: June 2, 1999
    Date of Patent: May 22, 2001
    Assignee: Alcon Laboratories, Inc.
    Inventors: Peter G. Klimko, Paul W. Zinke
  • Patent number: 6235777
    Abstract: 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: Grant
    Filed: May 14, 1998
    Date of Patent: May 22, 2001
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Shuichi Ohuchida, Yuuki Nagao, Takayuki Maruyama
  • Patent number: 6201019
    Abstract: 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: Grant
    Filed: April 8, 1999
    Date of Patent: March 13, 2001
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Philippe Diaz
  • Patent number: 6187933
    Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: February 13, 2001
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
  • Patent number: 6172115
    Abstract: 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: Grant
    Filed: January 12, 1998
    Date of Patent: January 9, 2001
    Assignee: Allergan Sales, Inc.
    Inventor: Roshantha A. Chandraratna
  • Patent number: 6166072
    Abstract: 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: Grant
    Filed: June 29, 1999
    Date of Patent: December 26, 2000
    Assignee: Allelix Neuroscience, Inc.
    Inventors: Stanley Charles Bell, Michael De Vivo, Allen Hopper, Methvin Isaac, Anne O'Brien, Vassil Ilya Ognyanov, Richard Schumacher
  • Patent number: 6156798
    Abstract: 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: Grant
    Filed: April 9, 1999
    Date of Patent: December 5, 2000
    Assignee: Pfizer Inc
    Inventor: Lawrence A. Reiter
  • Patent number: 6117869
    Abstract: 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: Grant
    Filed: July 26, 1999
    Date of Patent: September 12, 2000
    Assignee: Warner-Lambert Company
    Inventors: Joseph Armand Picard, Bruce David Roth, Drago Robert Sliskovic
  • Patent number: 6114568
    Abstract: The present invention relates to a process for alkylating hindered sulfonamides useful as intermediates in the preparation of matrix metalloproteinase inhibitors.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: September 5, 2000
    Assignee: Pfizer Inc.
    Inventors: Brian Michael Andresen, Phillip Dietrich Hammen, Joel Michael Hawkins
  • Patent number: 6087389
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: June 18, 1998
    Date of Patent: July 11, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 6018068
    Abstract: 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: Grant
    Filed: January 26, 1998
    Date of Patent: January 25, 2000
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Yuuki Nagao, Kazuhiko Torisu, Nobuyuki Hamanaka
  • Patent number: 6017925
    Abstract: 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: Grant
    Filed: January 13, 1998
    Date of Patent: January 25, 2000
    Assignee: Merck & Co., Inc.
    Inventor: Mark E. Duggan
  • Patent number: 5998471
    Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification.
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: December 7, 1999
    Assignee: Allergan Sales, Inc.
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5985928
    Abstract: 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: Grant
    Filed: January 9, 1998
    Date of Patent: November 16, 1999
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5945450
    Abstract: Naphthalene derivatives represented by formula ?I!: ##STR1## (wherein A is a hydrogen atom, a hydroxy group, a C.sub.7 -C.sub.11 aralkyloxy group, or an alkoxy group composed of an oxy group and a C.sub.1 -C.sub.12 aliphatic or alicyclic, saturated or unsaturated hydrocarbon group where the allyl may be substituted with a C.sub.6 -C.sub.10 allyloxy group; Q represents O, S, CH.sub.2, O--CH.sub.2, S--CH.sub.2, CO, or CHOR.sup.1 ; L represents CO, CR.sup.2 R.sup.3 CO, CH.sub.2 CH.sub.2 CO, or CH.dbd.CHCO; D represents a hydrogen atom, NO.sub.2, NH.sub.2, CO.sub.2 R.sup.4, or a group having the following formula ?II!: ##STR2## (wherein G represents. a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.6, CN, or a tetrazol-5-yl group); E represents a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.5, CN, or a tetrazol-5-yl group; M represents a hydrogen atom, a C.sub.1 -C.sub.4 lower alkyl group, a nitro group, or a halogen atom; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.
    Type: Grant
    Filed: November 22, 1996
    Date of Patent: August 31, 1999
    Assignee: Teijin Limited
    Inventors: Kazuya Takenouchi, Katsushi Takahashi, Masaichi Hasegawa, Takahiro Takeuchi, Keiji Komoriya