Q Is Acyclic And Benzene Ring In A Substituent E Patents (Class 514/605)
-
Patent number: 5763474Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 and R.sub.5 are, independently, cyano, nitro, amino, alkyl, perfluoroalkyl, fluoroalkyl, alkoxy, perfluoroalkoxy, fluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen, with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen; or a pharmaceutically acceptable salt thereof, relaxes smooth muscles.Type: GrantFiled: July 7, 1997Date of Patent: June 9, 1998Assignee: American Home Products CorporationInventors: David R. Herbst, Madelene M. Antane, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
-
Patent number: 5760064Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 6, 1997Date of Patent: June 2, 1998Assignee: G.D. SearleInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
-
Patent number: 5756546Abstract: Water-soluble nimesulide salt consisting of the product of reaction of nimesulide and of L-lysine and its preparation, aqueous solution containing it, nimesulide-based combinations with cyclodextrins and their uses.Type: GrantFiled: June 11, 1996Date of Patent: May 26, 1998Inventors: Bernard Pirotte, Geraldine Piel, Philippe Neven, Isabelle Delneuville, Joszef Geczy
-
Patent number: 5750574Abstract: A compound of the general formula (I) ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 is F, perfluoroalkyl group of 1 to 10 carbon atoms or perfluoroalkoxy of 1 to 10 carbon atoms; or a pharmaceutically acceptable salt thereof relax smooth muscles.Type: GrantFiled: July 7, 1997Date of Patent: May 12, 1998Assignee: American Home Products CorporationInventor: Adam M. Gilbert
-
Patent number: 5733935Abstract: 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: GrantFiled: June 17, 1996Date of Patent: March 31, 1998Assignee: Nihon Nohyaku Co., Ltd.Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
-
Patent number: 5728875Abstract: .alpha.-Amino acid amides of the formula I ##STR1## in which n is the number zero or one;R.sub.1 is C.sub.1 -C.sub.12 alkyl, which is unsubstituted or can be substituted by C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.3 -C.sub.8 cycloalkyl, cyano, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.3 -C.sub.6 alkenyloxycarbonyl or C.sub.3 -C.sub.6 alkynyloxycarbonyl; C.sub.3 -C.sub.8 cycloalkyl; C.sub.2 -C.sub.12 alkenyl;C.sub.2 -C.sub.12 alkynyl; C.sub.1 -C.sub.12 halogenoalkyl or a group NR.sub.13 R.sub.14 ; in which R.sub.13 and R.sub.14 independently of one another are hydrogen or C.sub.1 -C.sub.6 alkyl or together are tetra- or pentamethylene;R.sub.2 and R.sub.3 independently of one another are hydrogen; C.sub.1 -C.sub.8 alkyl; C.sub.1 -C.sub.8 alkyl which is substituted by hydroxyl, C.sub.1 -C.sub.4 alkoxy, mercapto or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.8 alkenyl;C.sub.3 -C.sub.8 alkynyl; C.sub.3 -C.sub.8 cycloalkyl or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.Type: GrantFiled: August 26, 1996Date of Patent: March 17, 1998Assignee: Novartis CorporationInventor: Martin Zeller
-
Patent number: 5723489Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1.These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.Type: GrantFiled: May 7, 1996Date of Patent: March 3, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, William N. Washburn, Kathleen M. Poss
-
Patent number: 5716980Abstract: 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: GrantFiled: June 27, 1995Date of Patent: February 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
-
Patent number: 5688829Abstract: Therapeutic injectable analgesic pharmaceutical compositions for intramuscular administration containing nimesulide. The pharmaceutical compositions comprise nimesulide, dimethylacetamide, benzyl benzoate and ethyl oleate.Type: GrantFiled: June 13, 1996Date of Patent: November 18, 1997Assignee: Panacea Biotec LimitedInventors: Rajesh Jain, Amarjit Singh
-
Patent number: 5672608Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.Type: GrantFiled: November 22, 1994Date of Patent: September 30, 1997Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
-
Patent number: 5670519Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.Type: GrantFiled: June 5, 1995Date of Patent: September 23, 1997Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
-
Patent number: 5639768Abstract: The invention relates to the compounds of formula (I) wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which: R.sub.1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy; R.sub.3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); and X.sub.2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical.Type: GrantFiled: July 25, 1995Date of Patent: June 17, 1997Assignee: Ciba-Geigy CorporationInventors: Michael M. Morrissey, Hongsuk Suh
-
Patent number: 5639769Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: January 17, 1996Date of Patent: June 17, 1997Assignee: 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: 5633287Abstract: 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: GrantFiled: October 23, 1995Date of Patent: May 27, 1997Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic, Wendell Wierenga
-
Patent number: 5622968Abstract: Modulators of neurotransmitter release including substituted guanidines, and N"-aminoguanidines, and N,N'N", N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.Type: GrantFiled: June 5, 1995Date of Patent: April 22, 1997Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew G. Knapp, Lee D. Margolin
-
Patent number: 5610174Abstract: The present invention provides a method of treating urinary incontinence in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the following structure: ##STR1## wherein each of the substiutents for the compound is as defined in the specification.Type: GrantFiled: June 2, 1995Date of Patent: March 11, 1997Assignee: Synaptic Pharmaceutical CorporationInventors: Douglas A. Craig, Carlos C. Forray, Charles Gluchowski, Theresa A. Branchek
-
Patent number: 5604260Abstract: The Compound of Formula I and pharmaceutically acceptable salts thereof in the treatment of cyclooxygenase-2 mediated diseases are disclosed.Type: GrantFiled: November 4, 1993Date of Patent: February 18, 1997Assignee: Merck Frosst Canada Inc.Inventors: Daniel Guay, Chun-Sing Li
-
Patent number: 5559150Abstract: The present invention is directed to novel compounds that are non-peptidic thrombin inhibitors. The compounds have the structure: ##STR1## and pharmaceutically acceptable salts thereof; wherein R.sup.1 is one of alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; and n is from zero to five. The compounds of the invention are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventor: Richard M. Soll
-
Patent number: 5554653Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.Type: GrantFiled: December 22, 1992Date of Patent: September 10, 1996Assignee: Eli Lilly and CompanyInventors: Kwan Hui, Charles D. Jones, Louis N. Jungheim, Timothy A. Shepherd
-
Patent number: 5545669Abstract: This invention relates to the novel compounds and pharmaceutical compositions of Formula (I).This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound or composition of Formula (I).Type: GrantFiled: June 2, 1994Date of Patent: August 13, 1996Inventors: Jerry L. Adams, Ralph F. Hall, Dennis Lee, Ruth J. Mayer, George L. Seibel
-
Patent number: 5527824Abstract: Substituted Di-T-Butylphenols useful for inhibiting the synthesis of leukotrienes are disclosed.Type: GrantFiled: May 5, 1995Date of Patent: June 18, 1996Assignee: Riker Laboratories, Inc.Inventor: Robert A. Scherrer
-
Patent number: 5527829Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: May 23, 1994Date of Patent: June 18, 1996Assignee: Agouron Pharmaceuticals, Inc.Inventor: Vincent J. Kalish
-
Patent number: 5527830Abstract: The invention relates to new drugs for augmenting perfusion pressure administered during cardiopulmonary resuscitation and other shock states. The compounds include phenylethanolamines and imidazolines, and fluorinated derivatives thereof, which act on adrenergic receptors in patients. The compounds of the invention enhance neurologic outcome and survival, and decrease ventricular dysrhythmias in patients suffering cardiac arrest and other shock states, relative to the outcomes, survival, and post defibrillation ventricular dysrhythmias in conventional therapy for use in resuscitation.Type: GrantFiled: September 26, 1994Date of Patent: June 18, 1996Assignee: The Ohio State UniversityInventors: Charles G. Brown, Duane D. Miller
-
Patent number: 5521219Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: August 24, 1993Date of Patent: May 28, 1996Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
-
Patent number: 5521311Abstract: The present compounds represented by the formula: ##STR1## (wherein R.sup.1 is a phenyl group, a halophenyl group or a cycloalkyl group having 3 to 8 carbon atoms, R.sup.2 is a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, R.sup.3 is a hydrogen atom, an alkyl group having 1 to 7 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 5 carbon atoms or a benzyl group, or R.sup.2 and R.sup.3 are bonded together to form a 5- to 7-membered heterocycle) and salts thereof have potent anti-inflammatory, antipyretic, analgesic and anti-allergic actions with less side effects such as gastrointestinal disorders and with such a high safety as to permit long-term administration.Type: GrantFiled: August 14, 1995Date of Patent: May 28, 1996Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Kensei Yoshikawa, Shiuji Saito, Yohichi Shimazaki, Mariko Kashiwa, Katsuo Hatayama
-
Patent number: 5519060Abstract: 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: GrantFiled: January 17, 1995Date of Patent: May 21, 1996Assignee: The Trustees of the University of PennsylvaniaInventors: Paul Sprengeler, Amos B. Smith, III, Ralph F. Hirschmann, Akihisa Yokoyama
-
Patent number: 5510388Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 31, 1995Date of Patent: April 23, 1996Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
-
Patent number: 5508294Abstract: Sulfonamide-containing hydroxethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 31, 1995Date of Patent: April 16, 1996Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
-
Patent number: 5504115Abstract: 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: GrantFiled: June 28, 1994Date of Patent: April 2, 1996Assignee: Merck & Co., Inc.Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
-
Patent number: 5491172Abstract: 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: GrantFiled: April 13, 1994Date of Patent: February 13, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic, Wendell Wierenga
-
Patent number: 5491170Abstract: .beta.-Carboxy sulfonyl compounds of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 is hydrogen or alkyl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is --O--, --S--, or --NR.sub.2 --, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.Type: GrantFiled: December 19, 1994Date of Patent: February 13, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
-
Patent number: 5466712Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##Type: GrantFiled: November 4, 1994Date of Patent: November 14, 1995Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth
-
Patent number: 5464867Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: November 16, 1994Date of Patent: November 7, 1995Assignee: American Home Products CorporationInventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
-
Patent number: 5457131Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: August 18, 1994Date of Patent: October 10, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
-
Patent number: 5455273Abstract: 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: GrantFiled: November 19, 1993Date of Patent: October 3, 1995Assignee: Karl Thomae GmbHInventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
-
Patent number: 5449691Abstract: A method for inducing the production of interleukin 2 in a warm blooded animal by administering an effective amount of a compound of the formula (I) ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.Type: GrantFiled: June 24, 1993Date of Patent: September 12, 1995Assignee: Sterling Winthrop Inc.Inventors: William N. Washburn, Lee H. Latimer, Barbara B. Lussier, Carl R. Illig, Alexander L. Weis
-
Patent number: 5416113Abstract: Novel compounds which are 2,6-di-t-butylphenols substituted on the 4 position by an anilino group, which anilino group is substituted by a carboxyl substituent, a tetrazolyl substituent or an N-methyltetrazolyl substituent, are useful antiallergic agents. Pharmaceutical compositions containing and pharmacological methods of using such compounds are also disclosed, as are synthetic intermediates for preparing such compounds. Certain of the synthetic intermediates also exhibit useful antiallergic activity.Type: GrantFiled: June 22, 1994Date of Patent: May 16, 1995Assignee: Riker Laboratories, Inc.Inventor: Robert A. Scherrer
-
Patent number: 5416117Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 28, 1994Date of Patent: May 16, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
-
Patent number: 5409956Abstract: The present invention relates to indan derivatives represented by the formula (1) or pharmaceutically acceptable salts thereof: ##STR1## [wherein R.sup.1 represents C1 to C12 alkyl, benzyl, styryl, naphthyl, optionally substituted phenyl or optionally substituted thienyl; R.sup.2 represents carboxyl, C1 to C4 alkoxycarbonyl, ##STR2## Y represents --(CH.sub.2).sub.p -- (wherein p represents an integer of 0 to 5), --CO--(CH.sub.2).sub.q .about., --CH(OH)--(CH.sub.2).sub.q .about., (wherein q represents an integer of 1 to 4, and the symbol .about. represents a linkage to R.sup.2), oxymethylene or ethylene; and n represents an integer of 1 to 4]. The compounds according to the present invention potently antagonize the action of thromboxane A.sub.2, and therefore useful for the treatment and prevention of diseases caused by thromboxane A.sub.2 such as angiosis, vasospasm, asthma and the like.Type: GrantFiled: August 30, 1993Date of Patent: April 25, 1995Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Kiyoshi Yoshida, Yoshiaki Yamaji, Tadashi Kurimoto, Ryuichi Sato, Motoki Torizuka
-
Patent number: 5405872Abstract: This invention relates to tetralin derivatives useful in medicine for the treatment of hypertension, to the synthesis of the compounds, to the pharmaceutical formulations containing the compounds and the use of the compounds in medical practice.Type: GrantFiled: March 22, 1993Date of Patent: April 11, 1995Assignee: Burroughs Wellcome Co.Inventors: John D. McDermed, Kevin P. Hurley, Vincent H. Chang, Anjaneyulu S. Tadepalli
-
Patent number: 5393776Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.Type: GrantFiled: May 13, 1994Date of Patent: February 28, 1995Assignee: Bristol-Myers Squibb CompanyInventor: Bradley C. Pearce
-
Patent number: 5382595Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: October 13, 1992Date of Patent: January 17, 1995Assignee: Eisai Co., Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
-
Patent number: 5360822Abstract: An object of the present invention is to offer an agent for curing urinary incontinence with high selectivity for the urethra.One of the compounds of the present invention is a sulfonanilide derivative having the following formula (I). ##STR1## The compounds of the present invention exhibit selective contracting action to smooth muscle of the urethra tract whereupon they have useful effect as remedies for urinary incontinence.Type: GrantFiled: December 21, 1993Date of Patent: November 1, 1994Assignee: Nippon Shinyaku Co. Ltd.Inventors: Akira Morino, Iwao Morita, Shin-ichi Tada
-
Patent number: 5352705Abstract: 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: GrantFiled: June 26, 1992Date of Patent: October 4, 1994Assignee: Merck & Co., Inc.Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
-
Patent number: 5346887Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, (alpha, alpha) -dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is substituted hydroxyalkylamino.Type: GrantFiled: April 23, 1991Date of Patent: September 13, 1994Assignee: Abbott LaboratoriesInventors: Herman H. Stein, Jacob J. Plattner, Steven R. Crowley
-
Patent number: 5340837Abstract: Compounds of the formula ##STR1## wherein each of o and p, independently of the other, is 0, 1, 2, 3, 4 or 5, the radicals R.sub.1 being the same or different when o is greater than 1 and the radicals R.sub.2 being the same or different when p is greater than 1;each of R.sub.1 and R.sub.2, independently of the other, is C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkyl, halogen, --NO.sub.2, --OH, C.sub.1 -C.sub.4 alkoxy, halo-C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, halo-C.sub.1 -C.sub.4 alkylthio, --O--S(.dbd.O)--R.sub.6, --O--S(.dbd.O).sub.2 --R.sub.6, phenoxy or --N(R.sub.11)SO.sub.2 R.sub.12 and/or two substituents R.sub.1 and/or two substituents R.sub.2 are, independently of one another, together --Y--Z--Y--;R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl or halo-C.sub.1 -C.sub.4 alkyl;R.sub.4 is hydrogen, C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkyl, unsubstituted phenyl or naphthyl or mono- or di-substituted phenyl or naphthyl;R.sub.5 is --S--R.sub.7, --S(.dbd.O)--R.sub.7, --S(.dbd.O).Type: GrantFiled: June 25, 1993Date of Patent: August 23, 1994Assignee: Ciba-Geigy CorporationInventors: Roger G. Hall, Alfons Pascual, Odd Kristiansen
-
Patent number: 5336690Abstract: A compound of the following general formula which is useful in treating hypercholesterolemia and atherosclerosis: ##STR1## wherein X is oxygen or sulfur; R is hydrogen, alkyl having from 1 to 8 carbon atoms, or benzyl; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, a heterocyclic group, or a hydrocarbon chain of from 1 to 20 carbon atoms which is saturated or contains 1 to 3 double bonds and each of R.sub.2 and R.sub.3 is selected from hydrogen, provided both are not hydrogen, an aralkyl group, a hydrocarbon chain of from 1 to 20 carbon atoms which is saturated or contains 1 to 3 double bonds, an w-substituted alkylC.sub.1-6, a heterocyclic group, phenyl, substituted phenyl or NR.sub.2 R.sub.3 taken together form a monocyclic heterocyclic group.Type: GrantFiled: June 10, 1993Date of Patent: August 9, 1994Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, Drago R. Sliskovic
-
Patent number: 5328909Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
-
Patent number: 5283261Abstract: Nimesulide is effective in the treatment of cataracts.Type: GrantFiled: September 25, 1992Date of Patent: February 1, 1994Assignee: LPB Istituto FarmaceuticoInventor: Filippo Drago
-
Patent number: 5246965Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which:R is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid;R.sub.1 is a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical and a cycloaliphatic hydrocarbon radical;X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); andX.sub.Type: GrantFiled: September 17, 1992Date of Patent: September 21, 1993Assignee: Ciba-GeigyInventor: Alan J. Main