Q Contains Benzene Ring Patents (Class 514/602)
  • Patent number: 5929118
    Abstract: The present invention relates to novel fluorobutenic acid hydrazides of the formula (I) ##STR1## in which Y represents C.dbd.O, C.dbd.S or SO.sub.2,R.sup.1 represents hydrogen or halogen andR.sup.2 represents alkyl, halogenoalkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkenyloxy, alkoxy, cycloalkyloxy, alkylthio or respectively optionally substituted aryl, aralkyl, aralkyloxy or hetaryl,to processes for their preparation and to their use for controlling animal pests.
    Type: Grant
    Filed: February 9, 1998
    Date of Patent: July 27, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Kraatz, Wolfgang Kramer, Wolfram Andersch, Andreas Turberg, Norbert Mencke
  • Patent number: 5929097
    Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha.
    Type: Grant
    Filed: October 6, 1997
    Date of Patent: July 27, 1999
    Assignee: American Cyanamid Company
    Inventors: Jeremy Ian Levin, Mila T. Du, Aranapakam Mudumbai Venkatesan, Frances Christy Nelson, Arie Zask, Yansong Gu
  • Patent number: 5880151
    Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: July 18, 1997
    Date of Patent: March 9, 1999
    Assignee: Tularik Inc.
    Inventors: Julio Cesar Medina, David Louis Clark, John A. Flygare, Terry J. Rosen, Bei Shan
  • Patent number: 5843999
    Abstract: A series of new azulene derivatives are disclosed, which are represented by the following formula; ##STR1## wherein: R.sub.1 is hydrogen atom, lower alkoxycarbonyl group, carboxy group, halogen atom, lower alkyl group, phenyl group or lower alkanoyl group; R.sub.2, R.sub.3 and R.sub.4 are hydrogen atom, lower alkyl group, lower alkoxy group or halogen atom; X is lower alkyl group or amino group.The compounds of the present invention are useful for treatment of inflammation.
    Type: Grant
    Filed: December 2, 1997
    Date of Patent: December 1, 1998
    Assignee: Kotobuki Seiyaku Co., Ltd.
    Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Masayuki Yokota, Satoko Uchibori
  • Patent number: 5760064
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: June 2, 1998
    Assignee: G.D. Searle
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5747535
    Abstract: The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R.sup.1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group,X represents a group of formula ##STR2## R.sup.2 and R.sup.3 independently of one another represent hydrogen; cycloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substituted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, orR.sup.2 and R.sup.3 together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl,R.sup.4 represents hydrogen, lower alkyl or lower alkoxy,R.sup.
    Type: Grant
    Filed: January 16, 1996
    Date of Patent: May 5, 1998
    Assignee: LG Chemical Ltd.
    Inventors: Yeong Soo Oh, Sang Soo Kim, Sang Yeul Hwang, Mi Kyung Yun, Seong Ryul Hwang, Seong Won Hong, Yong Hee Lee, Yi Na Jeong, Koo Lee, You Seung Shin
  • Patent number: 5744481
    Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: April 25, 1997
    Date of Patent: April 28, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5741819
    Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: ##STR1## or pharmaceutically acceptable salts thereof; whereinR.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R.sup.2 is one of hydrogen, alkyl, cycloalkyl or aryl; R.sup.3 is one of hydrogen, hydroxy or alkoxy; R.sup.4 is one of --NH.sub.2, phenyl or pyridyl, wherein said phenyl and said pyridyl are optionally substituted with one or two of halogen, hydroxy, hydroxyalkyl, alkoxy, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and/or dialkylaminoalkyl; X is one of --CH.sub.2 -- or --C(O)--; and n is from zero to eleven; provided that when R.sup.4 is --NH.sub.2, then R.sup.3 is hydrogen and n is other than zero; and also provided that when R.sup.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 21, 1998
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Carl R. Illig, Richard M. Soll, Joseph M. Salvino, Bruce E. Tomczuk, Tianbao Lu, Nalin L. Subasinghe
  • Patent number: 5741794
    Abstract: Compounds of formula (I), wherein: A represents: a) a --VR.sup.6 group wherein v is --C(.dbd.O), --C(.dbd.O)O--, --CH.sub.2 O--, --CH.sub.2 OC(.dbd.O)--, --C(.dbd.S)--, --CH.sub.2 OC(.dbd.O)NH--, --C(.dbd.S)O--, --CH.sub.2 S--, --C(.dbd.O)NHSO.sub.2 --, --SO.sub.2 NHC(.dbd.O)-- or --CH.sub.2 OSiPh.sub.2 --; b) a --CH.sub.2 NR.sup.9 R.sup.10 group or a --CONR.sup.9 R.sup.10 group wherein each of R.sup.9 and R.sup.10 is independently hydrogen, -alkyl-, -alkenyl-, -alkynyl, -cycloalkyl, -cycloalkenyl, pyridyl (any of which may optionally be substituted) or a group --D as defined above or R.sup.9 and R.sup.10 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring; c) a group Y where Y is a 5- or 6-membered optionally substituted heterocyclic ring containing one or more heteroatoms selected from nitrogen, oxygen and sulphur; or d) a group --CH.sub.2 Y or --C(.dbd.
    Type: Grant
    Filed: September 1, 1994
    Date of Patent: April 21, 1998
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Stephen Arthur Bowles, Christopher David Floyd, Andrew Miller, Mark Whittaker, Lars Michael Wood
  • Patent number: 5739166
    Abstract: A class of terphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and halo; or wherein R.sup.2 and R.sup.3 together form --OCH.sub.2 O--; wherein each of R.sup.6 through R.sup.8 is independently selected from hydrido, lower alkyl, halo, lower alkoxy, lower haloalkyl, and lower dialkylamino; or wherein R.sup.6 and R.sup.7 together form --OCH.sub.2 O; and wherein R.sup.12 is selected from lower alkylsulfonyl and aminosulfonyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: November 29, 1994
    Date of Patent: April 14, 1998
    Assignee: G.D. Searle & Co.
    Inventors: David B. Reitz, Jinglin Li, Monica B. Norton
  • Patent number: 5736579
    Abstract: A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein n is a number selected from 0, 1 and 2; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: November 18, 1994
    Date of Patent: April 7, 1998
    Assignee: G.D. Searle & Co.
    Inventors: David B. Reitz, Robert E. Manning, Horng-Chi Huang, Jinglin Li
  • Patent number: 5733935
    Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.
    Type: Grant
    Filed: June 17, 1996
    Date of Patent: March 31, 1998
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
  • Patent number: 5716980
    Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.
    Type: Grant
    Filed: June 27, 1995
    Date of Patent: February 10, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
  • Patent number: 5705528
    Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein thyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: ##STR1## wherein R.sup.1 represents farnesyl, geranyl or geranyl-geranyl;Z represents C--R.sup.6 or N;R.sup.2 represents H, CN, the groups COOR.sup.7, SO.sub.3 R.sup.7, CONR.sup.7 R.sup.8 and SO.sub.2 NR.sup.7 R.sup.7, wherein R.sup.7 and R.sup.8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO.sub.3 M, wherein M is a cation;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato;X represents O, S, SO, SO.sub.2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: January 6, 1998
    Assignee: Ramot University Authority for Applied Research & Industrial Development
    Inventor: Yoel Kloog
  • Patent number: 5700816
    Abstract: Combinations of a cyclooxygenase-2 inhibitor and a leukotriene A.sub.4 hydrolase inhibitor are described for treatment of inflammation and inflammation-related disorders.
    Type: Grant
    Filed: June 12, 1995
    Date of Patent: December 23, 1997
    Inventors: Peter C. Isakson, Gary D. Anderson, Susan A. Gregory
  • Patent number: 5686429
    Abstract: The present invention provides a method for providing nutrition to elderly patients. Pursuant to the present invention, the enteral composition includes a protein source, a lipid source, and a carbohydrate source. Preferably, the protein source includes at least 18% of the total calories. In an embodiment, the carbohydrate source includes a source of dietary fiber including a balance of soluble to insoluble fiber ratio of approximately 1:3. Still further, the composition of the present invention also includes increased levels of certain vitamins and minerals.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: November 11, 1997
    Assignee: Nestec Ltd
    Inventors: Paul M. Lin, Shen-Youn Chang, Chris Kruzel
  • Patent number: 5672615
    Abstract: Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 together with the chain to which they are attached or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a ring; pharmaceutically acceptable prodrug derivatives and pharmaceutically salts thereof; methods of preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.
    Type: Grant
    Filed: March 11, 1996
    Date of Patent: September 30, 1997
    Assignee: Novartis Corporation
    Inventors: Lawrence J. MacPherson, David Thomas Parker
  • Patent number: 5663174
    Abstract: Aromatic sulfonamide derivatives, particularly benzenesulfonamide, 4-fluorobenzenesulfonamide, 5-chloro-1-naphthalenesulfonamide and 5-isoquinolinesulfonamide derivatives are provided that inhibit Ca.sup.2+ -dependent enzymes and proteins such as Phospholipase A.sub.2, protein kinases such as Protein Kinase C, and inhibit membrane fusion, thereby being a valuable drug for the treatment of inflammation, arthritis, infarction, nephritis and many other types of tissue injury.
    Type: Grant
    Filed: January 17, 1997
    Date of Patent: September 2, 1997
    Assignee: Pharno-Wedropharm GmbH
    Inventor: Raymond Dumont
  • Patent number: 5663180
    Abstract: A class of 1,2-diarylcyclopentenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from alkyl, hydrido, hydroxyalkyl, halo, haloalkyl, alkoxycarbonyl and carboxyl; wherein R.sup.5 is selected from alkylsulfonyl, haloalkylsulfonyl and sulfamyl; and wherein B is phenyl or pyridyl, wherein B is optionally substituted at a substitutable position with alkyl, halo, alkylthio, cyano, haloalkyl, alkoxy, hydroxyalkyl and alkoxyalkyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 15, 1994
    Date of Patent: September 2, 1997
    Assignee: G.D. Searle & Co.
    Inventors: David B. Reitz, Jinglin Li
  • Patent number: 5663205
    Abstract: A pharmaceutical composition for use in glaucoma treatment which contains as an active ingredient 5-[1-hydroxy-2-[2-(2-methoxyphenoxyl)ethylamino]ethyl]-2-methylbenzenesulf onamide of the formula: ##STR1## or its acid salt. This agent is free from side effects and stable and has an excellent intraocular pressure reducing activity at its low concentrations, thus being useful as a pharmaceutical composition for use in glaucoma treatment.
    Type: Grant
    Filed: November 15, 1994
    Date of Patent: September 2, 1997
    Assignee: Senju Pharmaceutical Co. Ltd.
    Inventors: Takahiro Ogawa, Takaaki Deguchi, Yoshifumi Ikejiri, Katsuhiro Inada
  • Patent number: 5663414
    Abstract: A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.
    Type: Grant
    Filed: December 29, 1995
    Date of Patent: September 2, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Hitoshi Oinuma, Takashi Hasegawa, Tadanobu Takamura, Kenichi Nomoto, Yoshiharu Daiku, Toshihiko Naito, Sachiyuki Hamano
  • Patent number: 5650405
    Abstract: A method of reducing the severity of toxoplasmosis resulting from infection of a patient with Toxoplasma gondii by administering to a patient in need of such treatment, either after infection or before exposure to infection, a therapeutically effective amount of a compound that is a spiropiperidyl derivative of rifamycin S, wherein the derivative comprises an imidazole ring that includes carbons at positions 3 and 4 of the rifamycin ring, the carbon at position 2 of the imidazole ring also being a ring carbon at position 4 of a piperidine ring system, thereby forming a spiropiperidyl ring system, the spiropiperidyl ring system optionally comprising a lower hydrocarbon substituent on the nitrogen of the piperidine.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 22, 1997
    Assignee: Palo Alto Medical Foundation
    Inventors: Jack S. Remington, Fausto G. Araujo
  • Patent number: 5639769
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: January 17, 1996
    Date of Patent: June 17, 1997
    Assignee: G.D. Searle and Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5633287
    Abstract: The present invention is directed to compounds useful for the regulation of cholesterol of Formula I, methods for using them and pharmaceutical compositions thereof, ##STR1## wherein X and Y are oxygen, sulfur, or (CR'R").sub.n wherein n is 1 to 4; R is hydrogen, alkyl, or benzyl; R.sub.1 and R.sub.2 are phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, an alkyl chain, adamantyl, or a cycloalkyl group.
    Type: Grant
    Filed: October 23, 1995
    Date of Patent: May 27, 1997
    Assignee: Warner-Lambert Company
    Inventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic, Wendell Wierenga
  • Patent number: 5612378
    Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: ##STR1## wherein each R.sup.1 is independently one of alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl;each R.sup.2 and R.sup.3 is independently one of hydrogen, alkyl, aryl or arylalkyl;Y is a bond, or is one of --(CH.sub.2).sub.p --, cycloalkyl, aryl or C.sub.2-10 heterocycle; andm, n and p are each independently 1 to 10.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 18, 1997
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Lu Tianbao, Richard M. Soll
  • Patent number: 5597809
    Abstract: Methods of treating optic neuritis comprising administering a protective agent which inhibits glutamate-mediated retinal cell damage to a mammal at risk of developing optic neuritis.
    Type: Grant
    Filed: June 23, 1994
    Date of Patent: January 28, 1997
    Assignee: Massachusetts Eye & Ear Infirmary
    Inventor: Evan B. Dreyer
  • Patent number: 5589468
    Abstract: The present invention provides a method for providing nutrition to elderly patients. Pursuant to the present invention, the enteral composition includes a protein source, a lipid source, and a carbohydrate source. Preferably, the protein source includes at least 18% of the total calories. In an embodiment, the carbohydrate source includes a source of dietary fiber including a balance of soluble to insoluble fiber ratio of approximately 1:3. Still further, the composition of the present invention also includes increased levels of certain vitamins and minerals.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: December 31, 1996
    Assignee: Clintec Nutrition Co.
    Inventors: Paul M. Lin, Shen-Youn Chang, Chris Kruzel
  • Patent number: 5573769
    Abstract: A method for coating finely divided particles with one or more hydrophobic materials, such as waxes, in order to envelope each particle with a thin layer of material that entraps air adhering to the surface of the particle. Because of the entrapped air, the apparent density of the particles is decreased and their stability in aqueous suspensions is greatly improved. When applied to pesticides, this process produces mixtures that remain substantially in suspension for several hours after agitation, thus allowing more uniform and trouble-free application.
    Type: Grant
    Filed: March 18, 1994
    Date of Patent: November 12, 1996
    Assignee: Gowan Company
    Inventors: David C. Creech, Jon S. Bach
  • Patent number: 5571844
    Abstract: The invention relates to amidinophenylalanine derivatives, to the synthesis of these compounds, to their use and to pharmaceutical compositions which contain these compounds which act as thrombin inhibitors.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: November 5, 1996
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Werner St uber, Rainer Koschinsky
  • Patent number: 5552419
    Abstract: The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.
    Type: Grant
    Filed: November 3, 1994
    Date of Patent: September 3, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker
  • Patent number: 5541197
    Abstract: Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
    Type: Grant
    Filed: March 21, 1995
    Date of Patent: July 30, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Michael H. Fisher, Elizabeth M. Naylor, Ann E. Weber
  • Patent number: 5536752
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: July 16, 1996
    Assignee: Merck Frosst Canada Inc.
    Inventors: Yves Ducharme, Jacques Y. Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
  • Patent number: 5521219
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: August 24, 1993
    Date of Patent: May 28, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5519060
    Abstract: Methods are provided for using 2-hydroxy-3-aminopropylsulfonamides to mimic peptides and to modulate the chemical and/or biological activity of enzymes, particularly proteolytic enzymes. Also provided are compositions comprising the sulfonamides in admixture with a pharmaceutically acceptable carrier, adjuvant, or vehicle.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: May 21, 1996
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Paul Sprengeler, Amos B. Smith, III, Ralph F. Hirschmann, Akihisa Yokoyama
  • Patent number: 5516784
    Abstract: Compounds of formula ##STR1## wherein Ar, W, Z, Q, R.sub.1, U, and T are as set forth herein, are described. These compounds are active as agents against retroviruses and in particular against HIV.
    Type: Grant
    Filed: February 10, 1994
    Date of Patent: May 14, 1996
    Assignee: Schering Corporation
    Inventors: Frank Bennett, Ashit Ganguly, Viyyoor Girijavallabhan, Naginbhai Patel
  • Patent number: 5510388
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: April 23, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5508294
    Abstract: Sulfonamide-containing hydroxethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: April 16, 1996
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5506242
    Abstract: The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which comprises administering to a mammal in need thereof an effective macrophage metalloelastase inhibiting amount of a compound of formula I ##STR1## wherein Ar, R, R.sub.1 and R.sub.2 have meanings as defined, or of a pharmaceutically acceptable prodrug derivative thereof, or of a pharmaceutically acceptable salt thereof, or of pharmaceutical compositions comprising a said compound.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: April 9, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker, Arco Y. Jeng
  • Patent number: 5504115
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: April 2, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
  • Patent number: 5491172
    Abstract: The present invention is directed to compounds useful for the regulation of cholesterol of Formula I, methods for using them and pharmaceutical compositions thereof, ##STR1## wherein X and Y are oxygen, sulfur, or (CR'R").sub.n wherein n is 1 to 4; R is hydrogen, alkyl, or benzyl; R.sub.1 and R.sub.2 are phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, an alkyl chain, adamantyl, or a cycloalkyl group.
    Type: Grant
    Filed: April 13, 1994
    Date of Patent: February 13, 1996
    Assignee: Warner-Lambert Company
    Inventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic, Wendell Wierenga
  • Patent number: 5476846
    Abstract: The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts, complexes, esters and amides thereof, represented by the formula ##STR1## which is defined herein. Said compounds find application as anti-thrombotic and anti-asthmatic medicines.
    Type: Grant
    Filed: November 17, 1994
    Date of Patent: December 19, 1995
    Assignee: Lipha, Lyonnaise Industrielle Pharmaceutique
    Inventors: Claude Lardy, Daniel Guerrier, Gilles Chavernac, Francois Collonges
  • Patent number: 5466712
    Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: November 14, 1995
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth
  • Patent number: 5464867
    Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: November 16, 1994
    Date of Patent: November 7, 1995
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
  • Patent number: 5461076
    Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: October 24, 1995
    Inventors: Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
  • Patent number: 5455273
    Abstract: The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: October 3, 1995
    Assignee: Karl Thomae GmbH
    Inventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
  • Patent number: 5455258
    Abstract: Particularly the invention relates to the compounds of formula I ##STR1## (a) wherein Ar is carbocyclic or heterocyclic aryl;R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl;R.sub.1 is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: January 6, 1993
    Date of Patent: October 3, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker
  • Patent number: 5455262
    Abstract: Novel mercaptosulfide matrix metalloproteinase inhibitors of the Formula I, ##STR1## wherein: n is 0 or 1;R.sup.1 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH(lower alkyl); andR.sup.2 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH (lower alkyl); orR.sup.1 and R.sup.2 together are --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sup.3 is selected from the group consisting of hydrogen, lower alkyl, aralkyl and heteroaralkyl; andR.sup.4 is selected from the group consisting of hydrogen, lower alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, aralkyl and 2-indolylmethyl; andR.sup.5 is selected from the group consisting of lower alkyl, aralkyl and --CH(R.sup.6)--C(O)NH.sub.2,whereinR.sup.
    Type: Grant
    Filed: October 6, 1993
    Date of Patent: October 3, 1995
    Assignee: Florida State University
    Inventors: Martin A. Schwartz, Harold Van Wart
  • Patent number: 5446065
    Abstract: Compounds of the formula I ##STR1## in which R.sub.1 signifies an aryl, aralkyl or an aralkenyl group, the aryl radical of which can, in each case, be substituted one or more times by halogen, cyano, alkyl, trifluoromethyl, alkoxy, alkylthio, trifluoromethoxy, hydroxyl or carboxyl, m a whole number from 1 to 3, n a whole number from 1 to 5, R.sub.2 hydrogen, an alkyl, aralkyl or acyl group, Q a bond or an oxygen atom, R.sub.3 hydrogen or a lower alkyl radical which is possibly terminally substituted by carboxyl or by a hydroxyl group and R.sub.4 hydrogen, a lower alkyl group with 1-4 C-atoms, which is possibly terminally substituted by carboxyl or hydroxyl, a possibly substituted phenyl, heteroaryl, cycloalkyl or acyl group or a group ##STR2## in which R.sub.
    Type: Grant
    Filed: June 21, 1993
    Date of Patent: August 29, 1995
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ernst-Christian Witte, Hansjorg Beckh, Karlheinz Stegmeier, Liesel Doerge
  • Patent number: 5441983
    Abstract: A method for inhibiting cell infection by an enveloped virus, by administering to an infection site, a therapeutically effective amount of a calix(n)arene compound derivatized, at its ring positions meta to the bridge attachements to the ring, with polar substitutent having a terminal carboxylate, phosphate, or sulfonate groups, including esters and amides which are cleavable in vivo. The compound may be administered orally, or topically, e.g., for treatment of herpes virus.
    Type: Grant
    Filed: August 6, 1992
    Date of Patent: August 15, 1995
    Assignee: Genelabs Incorporated
    Inventors: Kou M. Hwang, You M. Qi, Su-Ying Liu, William Choy, Jen Chen
  • Patent number: 5434186
    Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: July 18, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff