Plural Isoquinoline Ring Systems Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 514/308)
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Patent number: 6048860Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.Type: GrantFiled: October 4, 1999Date of Patent: April 11, 2000Assignee: Adolor CorporationInventors: John J. Farrar, An-Chih Chang, Virendra Kumar, Wei Yuan Zhang, Alan Cowan
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Patent number: 6034097Abstract: The present invention is directed to compounds that act as analgesics and that have the structure of formula (I): ##STR1## wherein; Z is ##STR2## wherein, n is 1 or 2, and R.sub.0 is C.sub.6-12 aryl or C.sub.7-8 aralkyl; orR.sub.1 is selected from the group consisting of hydrogen; --NH--C.sub.1-6 alkyl; C.sub.1-6 alkyl; C.sub.6-12 aryl; C.sub.7-18 aralkyl; arginyl; and R.sub.30 NHC(.dbd.NH)--, wherein R.sub.30 is hydrogen, C.sub.6-12 aryl, C.sub.7-18 aralkyl, or C.sub.1-6 alkyl;R.sub.2 is hydrogen; C.sub.1-6 alkyl; or OH;R.sub.3 is C.sub.6-12 aryl; C.sub.7-18 aralkyl; --CH.sub.2 --C.sub.6 H.sub.2 R.sub.8 R.sub.9 ;or --CH.sub.2 --OHC.sub.6 HR.sub.8 R.sub.9, wherein each of R.sub.8 and R.sub.9 is independently, or hydrogen;R.sub.4 C.sub.6-12 aryl; C.sub.7-18 aralkyl; C.sub.1-12 alkyl; or a substituted or unsubstituted cyclohexyl;R.sub.5 is C.sub.1-6 alkyl; hydrogen; OH; halogen; SH; NO.sub.2 ; NH.sub.2 ; --NH--C.sub.1-6 alkyl; NH.sub.2 C (.dbd.NH--; NH.sub.2 C (.dbd.NH)--NH--; COOR.sub.31, wherein, R.sub.Type: GrantFiled: October 6, 1997Date of Patent: March 7, 2000Assignee: Astra ABInventors: John DiMaio, Wuyi Wang
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Patent number: 5994323Abstract: A pharmaceutical composition is disclosed that comprises clioquinol, vitamin B.sub.12, and, optionally, pharmaceutical acceptable carriers and/or excipients. The use of the pharmaceutical composition removes or alleviates the side effects of clioquinol.Type: GrantFiled: February 13, 1998Date of Patent: November 30, 1999Assignee: P.N. Gerolymatos S.A.Inventor: Panayotis N. Gerolymatos
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Patent number: 5965730Abstract: A pyridine derivative of the formula (I): ##STR1## wherein A is group of the following formulae: ##STR2## (R.sup.1 and R.sup.2 are each H, or protected or unprotected OH, R.sup.31, R.sup.41 and R.sup.42 are protected or unprotected hydroxymethyl, R.sup.32 is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.33 is substituted or unsubstituted lower alkyl, and the dotted line means the presence or absence of a double bond), R.sup.5 and R.sup.6 are H, or protected or unprotected amino, or both combine together with the adjacent nitrogen to form substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof, these compounds showing excellent bronchoconstriction inhibitory activity and/or anti-inflammatory activity of airway, and being useful in the prophylaxis or treatment of asthma.Type: GrantFiled: December 4, 1997Date of Patent: October 12, 1999Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tatsuzo Ukita, Masakatsu Sugahara, Katsuo Ikezawa, Hideo Kikkawa, Kazuaki Naito
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Patent number: 5905086Abstract: N-(2-Hydroxyethyl)nicotinamide nitrate or its salt prevents or ameliorates anxiety neurosis or panic disorder, or the following anxiety. This compound or its salt has few side effects and exhibits immediate action.Type: GrantFiled: February 13, 1998Date of Patent: May 18, 1999Assignee: Chugai Seiyaku Kabushiki KaishaInventor: Toshiro Miura
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Patent number: 5863929Abstract: This invention relates to a compound of the Formula IX--C(O)--Y--G--R I(wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, processes and intermediates for the preparation of such a compound or salt, pharmaceutical compositions comprising such a compound or salt and methods of their use as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.Type: GrantFiled: June 20, 1997Date of Patent: January 26, 1999Assignee: Eli Lilly and CompanyInventors: Valentine Joseph Klimkowski, Aaron Leigh Schacht, Michael Robert Wiley
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Patent number: 5744472Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.Type: GrantFiled: June 5, 1995Date of Patent: April 28, 1998Assignee: Neurogen CorporationInventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
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Patent number: 5733931Abstract: The present invention provides a cyclohexanediurea derivative, inclusive of its salt, represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and they each represent a straight-chain or branched alkyl group having at least 3 carbons, a cycloalkyl group, a cycloalkyl group having a bridge head, a furyl group, a furyl lower alkyl group or an aralkyl group, A.sub.1 and A.sub.2 are the same or different and they each represent a phenyl, pyridyl, quinolyl, isoquinolyl or indolyl group which may have substituents; a process for production thereof; an intermediate thereof; pharmaceutical use, a method for treatment and use thereof.Type: GrantFiled: March 8, 1996Date of Patent: March 31, 1998Assignee: Nissin Food Products Co., Ltd.Inventors: Toshihiro Yamada, Yoichi Nobuhara, Ichinari Takagi, Shiho Furumoto, Kazuhiro Kobayashi, Kiyohito Ikemoto
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Patent number: 5656632Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.Type: GrantFiled: June 5, 1995Date of Patent: August 12, 1997Assignee: Neurogen CorporationInventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
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Patent number: 5607693Abstract: The invention relates to a cosmetic or pharmaceutical composition which comprises oxyacanthine, one of its derivatives, one of their cosmetically or pharmaceutically acceptable acid addition salts or an extract of a plant in which it is present, such as Berberis vulgaris or barberry. One particular association is that of oxyacanthine with a saponin. This composition can be intended in particular for stimulating hair growth, retarding hair loss or combating pruritus.Type: GrantFiled: June 1, 1995Date of Patent: March 4, 1997Assignee: LVMH RechercheInventors: Frederic Bonte, Alain Meybeck
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Patent number: 5604224Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: May 30, 1995Date of Patent: February 18, 1997Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5602168Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.Type: GrantFiled: June 5, 1995Date of Patent: February 11, 1997Assignee: Neurogen CorporationInventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
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Patent number: 5569655Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: July 29, 1994Date of Patent: October 29, 1996Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5534523Abstract: An anti-AIDS virus composition comprising a therapeutically effective amount of cepharanthine or a pharmaceutically acceptable salt thereof and a method for treating AIDS which comprises administering a therapeutically effective amount of cepharanthine or a pharmaceutically acceptable salt thereof are disclosed.Type: GrantFiled: December 2, 1994Date of Patent: July 9, 1996Assignee: Kaken Shoyaku Co., Ltd.Inventors: Minoru Ono, Yuka Tamura, Michinori Akasu
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Patent number: 5527811Abstract: Compounds represented by the formula: ##STR1## wherein the ring A and the ring B each stand for an optionally substituted benzene ring; Ar stands for an optionally substituted aryl group or an optionally substituted heterocyclic group; Q stands for an oxygen atom or a sulfur atom; R stands for a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted hydroxyl group or an optionally substituted amino group; X stands for --O-- or --NR.sup.1 -- wherein R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon group; Y stands for --O--, --NR.sup.2 -- wherein R.sup.2 stands for a hydrogen atom or an optionally substituted hydrocarbon group, or a bond; m denotes 1, 2 or 3, and n denotes 0, 1 or 2, and salts thereof which have excellent calcium- or substance P receptor-antagonistic activity, being useful for treating a cerebralvascular disorder in mammals such as cerebralischemia, cerebral edema and neuronal damage, their production and use.Type: GrantFiled: July 13, 1994Date of Patent: June 18, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Tetsuji Imamoto, Yuzo Ichimori
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Patent number: 5519033Abstract: The present invention relates to a method of treating urinary incontinence in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives of azabiaglo and related compounds.Type: GrantFiled: May 31, 1994Date of Patent: May 21, 1996Assignee: Pfizer Inc.Inventors: Terry J. Rosen, Manoj C. Desai, John A. Lowe, III
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Patent number: 5506243Abstract: Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infarction, stroke, Alzheimer's disease, amyotrophia, osteoporosis, hypercalcemia or the like.Type: GrantFiled: April 28, 1994Date of Patent: April 9, 1996Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Toshiro Sakaki, Chizuko Takahashi, Yoshiyuki Fujimura
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Patent number: 5462963Abstract: The present invention involves photoprotective compositions which are useful for topical application to prevent damage to skin caused by acute or chronic exposure to ultraviolet light comprising chelating agents having the structure: ##STR1## wherein each --R.sup.1 is independently selected from the group consisting of alkyl, aryl, heteroaryl and heterocycle, or the --R.sup.1 's are covalently bonded together to form a cyclic alkyl or heterocyclic ring; --R.sup.2 and --R.sup.3 are --OR.sup.4, in which case there is no bond or a polar bond between --R.sup.2 and the nitrogen covalently bonded to --R.sup.3, each --R.sup.4 being independently selected from the group consisting of hydrogen, alkyl and aryl, except that both --R.sup.4 's are not methyl when both --R.sup.1 's are furyl; or --R.sup.2 is --O-- and is covalently bonded to the nitrogen which is covalently bonded to --R.sup.3, and --R.sup.3 is --O-- (there being a + charge on the nitrogen to which it is bonded) or nil;wherein the .alpha.Type: GrantFiled: August 2, 1991Date of Patent: October 31, 1995Assignee: The Procter & Gamble CompanyInventors: Rodney D. Bush, Donald L. Bissett
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Patent number: 5455251Abstract: The present invention provides new antiviral compounds, i.e., michellamines and derivatives and pharmacologically acceptable salts thereof, methods for isolating such antiviral compounds from a plant species of the genus Ancistrocladus, antiviral compositions containing such antiviral compounds, and methods of using such antiviral compounds for treating patients with viral infections. The antiviral compounds of the present invention inhibit the reproduction and cytopathicity of human acquired immunodeficiency viruses.Type: GrantFiled: April 19, 1993Date of Patent: October 3, 1995Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Michael R. Boyd, John H. Cardellina, II, Kirk P. Manfredi, John W. Blunt, Lewis K. Pannell, James B. McMahon, Robert J. Gulakowski, Gordon M. Cragg, Gerhard Bringmann, Duncan Thomas, Johnson Jato
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Patent number: 5430041Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aralkanoyl, heterocyclylcarbonyl or a group of the formula: ##STR2## R.sup.2 is alkyl, cycloalkylalkyl or aralkyl; R.sup.3 is hydrogen and R.sup.4 is hydroxy or R.sup.3 and R.sup.4 together are oxo; R.sup.5 is alkoxycarbonyl or alkylcarbamoyl; R.sup.6 and R.sup.7 together are trimethylene or tetramethylene optionally substituted by alkyl or on adjacent carbon atoms by tetramethylene; R.sup.8 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aroyl, aralkanoyl or heterocyclylcarbonyl; and R.sup.9 is alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, cyanoalkyl, carbamoyl-alkyl, alkylthioalkyl, alkoxyalkyl or alkoxycarbonylalkyl: and pharmaceutically acceptable acid addition salts of those compounds of formula I which are basic, inhibit aspartyl proteases of viral origin and can be used in the form of medicaments for the prophylaxis or treatment of viral infections.Type: GrantFiled: April 21, 1992Date of Patent: July 4, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Joseph A. Martin, Gareth J. Thomas
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Patent number: 5416094Abstract: Described are guanidinocarbonyl isoquinolines of the formula I, ##STR1## wherein R(1) is hydrogen, (amino) (cyclo) (aryl)alk(en)yl (heteroaryl); R(2) is hydrogen, halogen, alkyl, or aryl; G is a radical of the formula VII: ##STR2## X(2), X(3) and X(4) are hydrogen, halogen, nitro, amino, alkyl, sulfonamide, (mono) (di) (lower alkyl) (amino), benzyloxy, hydroxy; X(1) hydrogen, oxygen, sulfur and NR(7)R(8), and their pharmaceutically acceptable salts; described is also a process for their preparation, their use as medicaments, and medicaments containing them for treating congestive heart failure, and arrhythmic conditions as well as cardioprotective agents in mammals.Type: GrantFiled: September 24, 1993Date of Patent: May 16, 1995Assignee: Hoechst AktiengesellschaftInventors: Bansi Lal, Ramesh Gidwani, Ramanujam Rajagopalan, Radha Panicker, Chinnakulandai Sankar, Hans-Jochen Lang, Heinrich Englert, Wolfgang Scholz
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Patent number: 5321032Abstract: A tachykinin-antagonistic compound of the following general formula:R.sup.1 --A.sup.1 --D--Trp(R.sup.2)--A.sup.2 --R.sup.3[whereinR.sup.1 is hydrogen or amino-protective groupR.sup.2 is amino-protective groupR.sup.3 is ar(lower)alkoxy or N-(lower)alkyl or N-ar(lower)alkylaminoA.sup.1 is single bond or one amino acid residueA.sup.2 is one amino acid residue other than Phe.]or the salt thereof.Type: GrantFiled: August 12, 1992Date of Patent: June 14, 1994Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Daijiro Hagiwara, Hiroshi Miyake
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Patent number: 5283245Abstract: The invention concerns a thiazole of the formula I, ##STR1## wherein Q.sup.1 is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents, or Ar is an optionally substituted 6-membered heterocyclene moiety contining up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;R.sup.2 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl or substituted (1-4C)alkyl or R.sup.2 is optionally substituted benzoyl; andQ.sup.2 is optionally substituted thiazolyl;or a pharmaceutically-acceptable salt thereof.The invention also concerns processes for the manufacture of a thiazole of the formula I and pharmaceutical compositions containing said thiazole.Type: GrantFiled: November 18, 1991Date of Patent: February 1, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Martin P. Edwards
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Patent number: 5244895Abstract: An anti-ulcer agent contains a compound expressed by the following general formula 1: ##STR1## where, R.sub.1 is hydrogen atom or an alkyl group having 1 or 2 carbon atoms with or without substitution, R.sub.2 and R.sub.3 are resp. hydrogen atom or form oxo group together, R.sub.4 is hydrogen atom or methyl group or isoquinoline sulfonyl group, n is 2 or 3, A is N--R.sub.5 or CH--R.sub.5, R.sub.5 is phenyl group with or without substitution or benzyloxycarbonyl group with or without substitution, or a physiologically allowable acid added salt thereof as the active component.Type: GrantFiled: May 15, 1992Date of Patent: September 14, 1993Assignee: Hiroyoshi HidakaInventors: Hiroyoshi Hidaka, Tomohiko Ishikawa
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Patent number: 5240939Abstract: Muscle relaxant nitrogen bridge tetrahydroisoquinolines are disclosed. The novel compounds are represented by the formula ##STR1## wherein A is ##STR2## M represents --(CH.sub.2).sub.n --Z--(CH.sub.2).sub.n or ##STR3## R is a C.sub.1-3 alkoxy group, or adjacent Rs are a methylenedioxy group, R.sub.1 is lower alkyl; n is 1-6;m is 2 or 3; p is 1-3; Z is --N.sup.+ (R.sub.2 R.sub.3)--, --N(R.sub.4)--, ##STR4## and --N[(CH.sub.2).sub.n --A--R.sub.5 ]--; R.sub.2 and R.sub.3 are independently lower alkyl groups wherein a carbon atom within the chain may be replaced by a heteroatom, lower cycloalkyl, lower cycloalkyl lower alkyl, aryl, aryl lower alkyl, a 4- to 6-member heteroring or may be combined with the nitrogen to form a heteroring; R.sub.4 is a straight- or branched- chain C.sub.1-10 alkyl wherein a carbon atom within the chain may be replaced by a heteroatom, lower cycloalkyl, lower cycloalkyl lower alkyl, aryl, or a heteroring, which groups may be substituted or unsubstituted; or ##STR5## R.sub.Type: GrantFiled: November 16, 1992Date of Patent: August 31, 1993Assignee: Anaquest, Inc.Inventor: Donald M. Demko
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Patent number: 5212179Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: October 25, 1990Date of Patent: May 18, 1993Assignee: John Wyeth and Brother LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 5190961Abstract: Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof.The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.Type: GrantFiled: August 2, 1991Date of Patent: March 2, 1993Assignee: Terumo Kabushiki KaishaInventors: Hirokazu Hasegawa, Isamu Endo, Shingo Koyama, Masashi Isozaki, Yukari Yoshiyama, Shigenori Nozawa, Norio Arakawa
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Patent number: 5158959Abstract: What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.Type: GrantFiled: December 27, 1983Date of Patent: October 27, 1992Assignee: Hoechst AktiengesellschaftInventors: Rolf Geiger, Volker Teetz, Hansjorg Urbach, Bernward Scholkens, Rainer Henning
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Patent number: 5068337Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein Ar is an optionally substituted aryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optionally substituted aryl;A represents a group of formula --XR.sup.3 whereinX is (i) a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q --or (ii) a group of formula --(CHR.sup.6).sub.r --O--(CHR.sup.7).sub.qin which formulae: Y represents --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 providing that p and q do not both represent 0, 1 or 2 and the other is zero; R.sup.6, R.sup.7 and R.sup.8 independently represent hydrogen or lower alkyl, and R.sup.Type: GrantFiled: November 13, 1986Date of Patent: November 26, 1991Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 5032591Abstract: A pharmaceutical product comprising a potassium channel activator antihypertensive agent and a .beta.-blocker antihypertensive agent as a combined preparation for simultaneous, separate or sequential use in therapy of hypertension.Type: GrantFiled: January 4, 1989Date of Patent: July 16, 1991Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Robin E. Buckingham
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Patent number: 5032590Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: March 8, 1990Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 4975438Abstract: Compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, Aryl, R.sub.3, R.sub.4 and R.sub.8, independently, are hydrogen, lower alkyl, aryl, R.sub.5 and R.sub.6, independently, are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.Type: GrantFiled: September 6, 1988Date of Patent: December 4, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
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Patent number: 4968681Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: November 15, 1988Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 4954518Abstract: This invention relates to a 4H-1-benzopyran-4-one derivative represented by the formula: ##STR1## or a salt thereof, a process for producing the same and a pharmaceutical composition comprising the same as active ingredient.Type: GrantFiled: October 7, 1988Date of Patent: September 4, 1990Assignee: Toyama Chemical Company, Ltd.Inventors: Shuntaro Takano, Chosaku Yoshida, Takihiro Inaba, Keiichi Tanaka, Ryuko Takeno, Hideyoshi Nagaki, Tomoya Shimotori, Shinji Makino
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Patent number: 4937255Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.Type: GrantFiled: March 16, 1989Date of Patent: June 26, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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Patent number: 4833152Abstract: Novel inhibitors of angiotensin coverting enzyme having the general formula R - A - S - Z are disclosed as potent inhibitors of angiotensin converting enzyme and are useful anti-hypertensive agents.Type: GrantFiled: November 20, 1987Date of Patent: May 23, 1989Assignee: University of MiamiInventors: James W. Ryan, Alfred Chung
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Patent number: 4808627Abstract: A method is provided for preventing or treating toxemia during pregnancy by administering a thromboxane A.sub.2 receptor antagonist before or during toxemia.Type: GrantFiled: December 16, 1987Date of Patent: February 28, 1989Assignee: E. R. Squibb & Sons, Inc.Inventor: Martin L. Ogletree
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Patent number: 4761418Abstract: Neuromuscular blocking agents of formula (1) which are useful as skeletal muscle relaxants during surgery are disclosed. ##STR1## and X is an anion, preferably pharmaceutically acceptable.Type: GrantFiled: July 17, 1985Date of Patent: August 2, 1988Assignees: Burroughs Wellcome Co., General Hospital CorporationInventors: Roy A. Swaringen, Jr., Hassan A. El-Sayad, David A. Yeowell, John J. Savarese
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Patent number: 4749698Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.Type: GrantFiled: July 8, 1985Date of Patent: June 7, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Edward S. Neiss, John T. Suh, John R. Regan, Jerry W. Skiles, Jeffrey N. Barton, James J. Mencel, Paul Menard
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Patent number: 4745124Abstract: Novel thiolester compounds are disclosed which are orally effective angiotensin converting enzyme inhibitors useful in the treatment of mammalian hypertension. They have the formula,R.sub.1 -A.sub.1 -S-Z,wherein Z denotes -B-A.sub.2, R.sub.1 is H or an acyl group, A.sub.1 is a carboxylic acid containing at least one amino or imino -N-, A.sub.2 is a carboxylic acid containing at least one amino or imino -N- or a lower alkyl ester or amide thereof, B is a 2-4 carbon backbone chain in mercapto linkage to S which includes a carbonyl or sulfonyl group joined in carboxamido or sulfonamido linkage, respectively, to A.sub.2.Preferably A.sub.2 includes a 4-6 membered C-N ring or a 5 membered ring of one N, one S and 3 C atoms.Type: GrantFiled: July 20, 1983Date of Patent: May 17, 1988Assignee: University of MiamiInventors: James W. Ryan, Alfred Chung
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Patent number: 4734420Abstract: Novel inhibitors of angiotensin converting enzyme having the general formula R - A - S - Z are disclosed as potent inhibitors of angiotensin converting enzyme and are useful anti-hypertensive agents.Type: GrantFiled: May 2, 1980Date of Patent: March 29, 1988Assignee: University of MiamiInventors: James W. Ryan, Alfred Chung
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Patent number: 4701460Abstract: Long duration muscle relaxant compound of formula (I) ##STR1## and its use in producing muscle relaxation in mammals including man.Type: GrantFiled: January 25, 1985Date of Patent: October 20, 1987Assignee: Burroughs Wellcome Co.Inventors: Hassan A. El-Sayad, Roy A. Swaringen, Jr., David A. Yeowell
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Patent number: 4698352Abstract: This invention relates to a novel 4-oxo-1,4-dihydronicotinic acid derivative ##STR1## or a salt thereof, wherein R.sup.1 is hydrogen or carboxyl-protecting group;R.sup.2 is substituted phenyl and naphthyl, or a substituted or unsubstituted heterocyclic group; andR.sup.3 is haloalkyl, aminoalkyl, or substituted or unsubstituted alkenyl, phenylalkenyl, naphthylalkenyl, phenylalkyl, naphthylalkyl, phenylalkynyl, naphthylalkynyl, heterocyclic alkyl, heterocyclic alkenyl, phenyl, naphthyl, cycloalkyl, cycloalkenyl, carboxylic acyl, iminoalkyl, heterocyclic or bridged hydrocarbon, which has a broad antibacterial spectrum and a low toxicity, and are useful for treatment of diseases of human beings and animals, to a process for producing the same and to an antibacterial agent containing the same.Type: GrantFiled: October 27, 1983Date of Patent: October 6, 1987Assignee: Toyama Chemical Co., Ltd.Inventors: Hirokazu Narita, Yoshinori Konishi, Jun Nitta, Shunjiro Misumi, Hideyoshi Nagaki, Isao Kitayama, Yoriko Nagai, Yasuo Watanabe, Nobuyuki Matsubara, Shinzaburo Minami, Isamu Saikawa
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Patent number: 4698356Abstract: Novel compounds are disclosed as potent inhibitors of angiotensin converting enzyme and as orally effective antihypertensive agents.Type: GrantFiled: August 14, 1979Date of Patent: October 6, 1987Assignee: University of MiamiInventors: James W. Ryan, Alfred Chung
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Patent number: 4698355Abstract: Novel compounds are disclosed as potent inhibitors of angiotensin converting enzyme and as orally effective antihypertensive agents.Type: GrantFiled: August 14, 1979Date of Patent: October 6, 1987Assignee: University of MiamiInventors: James W. Ryan, Alfred Chung
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Patent number: 4695577Abstract: Novel compounds are disclosed as potent inhibitors of angiotensin converting enzyme and as orally effective antihypertensive agents.Type: GrantFiled: August 14, 1979Date of Patent: September 22, 1987Assignee: University of MiamiInventors: James W. Ryan, Alfred Chung
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Patent number: 4692459Abstract: Inhibitors of angiotensin converting enzyme which have the formula: ##STR1## wherein R is hydrogen, formyl, acetyl propanoyl, butanoyl, phenylacetyl, phenylpropanoyl, benzoyl, cyclopentanecarbonyl, tert-butyloxycarbonyl, cyclopentanecarbonyl-L-lysyl, pyro-L-glutamyl-L-lysyl, L-lysyl, L-arginyl or pyro-L-glutamyl;A is L-phenylalanyl, D-phenylalanyl, D,L-alanyl, D-alanyl, D,L-tryptophyl, D-tryptophyl, D,L-tyrosyl, D-tyrosyl, D,L-isoleucyl, D-isoleucyl, D,L-leucyl, D-leucyl, D,L-histidyl, D-histidyl, D,L-valyl, or D-valyl, the .alpha.-amino group thereof being in amide linkage with R;R.sub.1 is hydrogen or methyl;R.sub.2 is L-proline, L-3,4-dehydroproline, D,L-3,4-dehydroproline, L-3-hydroxyproline, L-4-hydroxyproline, L-thiazolidine-4-carboxylic acid, or L-5-oxo-proline, the imino group thereof being in imide linkage with the adjacent ##STR2## and, n is 0 or 1, such that when n is 0, R.sub.1 is methyl are disclosed as useful anti-hypertensive agents.Type: GrantFiled: March 3, 1980Date of Patent: September 15, 1987Assignee: University of MiamiInventors: James W. Ryan, Alfred Chung
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Patent number: 4692458Abstract: Novel inhibitors of angiotensin converting enzyme having the general formula R--A--S--Z are disclosed as potent inhibitors of angiotensin converting enzyme and are useful anti-hypertensive agents.Type: GrantFiled: March 5, 1980Date of Patent: September 8, 1987Assignee: University of MiamiInventors: James W. Ryan, Alfred Chung
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Patent number: 4690940Abstract: Novel Compounds are disclosed as potent inhibitors of angiotensin converting enzyme and as orally effective antihypertensive agents.Type: GrantFiled: August 14, 1979Date of Patent: September 1, 1987Assignee: University of MiamiInventors: James W. Ryan, Alfred Chung
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Patent number: 4690939Abstract: Novel compounds are disclosed as potent inhibitors of angiotensin converting enzyme and as orally effective anti-hypertensive agents.Type: GrantFiled: August 14, 1979Date of Patent: September 1, 1987Assignee: University of MiamiInventors: James W. Ryan, Alfred Chung