Nitrogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/566)
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Patent number: 5932595Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.Type: GrantFiled: December 18, 1996Date of Patent: August 3, 1999Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Lawrence Emerson Fisher, Robert Than Hendricks, Keshab Sarma
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Patent number: 5925667Abstract: A pyrrolidine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein R.sub.1 is an alkenyl group; R.sub.2 is a lower alkoxy group or a halogen atom;R.sub.3 is a lower alkyl group;X is a group expressed by --O-- or --S--;Y is carbon or nitrogen atom;m is an integer of 1 to 3; andn is an integer of 0 to 2.The pyrrolidine derivative has an anti-ulcer effect or an antibacterial activity against Helicobacter pyroli, and has also high safety to be available for prevention or cure of ulcers.Type: GrantFiled: April 2, 1998Date of Patent: July 20, 1999Assignee: Shiseido Co., Ltd.Inventors: Chikao Nishino, Tomohiro Uetake
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Patent number: 5922887Abstract: A compound, or solvate or salt thereof, of formula (I) ##STR1## in which, R.sub.1 and R.sub.2, are, independently hydrogen, linear or branched C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkenyl, or C.sub.3-6 alkenyl, or together form a C.sub.3-7 alkyl;R.sub.3 and R.sub.4 are, independently, hydrogen, linear or branched C.sub.1-6 alkyl, or R.sub.4 is oxygen forming with the carbon atom to which is attached a C.dbd.O group;R.sub.5 is hydrogen, hydroxy, or C.sub.1-3 alkoxy;R.sub.6 is halogen, NH.sub.2 or a para or meta --COR-8 group, in which R.sub.8 is C.sub.1-8 -alkyl, C.sub.1-8 -alkoxy or NR.sub.9 R.sub.10, wherein R.sub.9 and R.sub.10, are, independently, hydrogen, straight or branched C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl or phenyl; or R.sub.6 is a para or meta group ##STR2## in which R.sub.11 and R .sub.12 are, independently, hydrogen or straight or branched C .sub.1-6 and,R.sub.7 is hydrogen, or straight or branched C.sub.1-8 alkyl; is provided.Type: GrantFiled: November 18, 1997Date of Patent: July 13, 1999Assignee: SmithKline Beecham SpAInventors: Giulio Dondio, Silvano Ronzoni
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Patent number: 5914319Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: June 22, 1999Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5907039Abstract: Amino alcohol derivatives with a primary amino group or a substituted amino group influence the synthesis of glycolipids and have antiviral, antitumor, metastasis inhibiting and neural cell growth enhancing functions. The amino alcohol derivatives are useful in preparing 2-acylamino alcohol derivatives.Type: GrantFiled: December 9, 1996Date of Patent: May 25, 1999Assignee: Seikagaku Kogyo Kabushiki KaishaInventors: Masayuki Jinbo, Hidekazu Oyamada, Jinichi Inokuchi
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Patent number: 5907043Abstract: The present invention relates to pyrrolidine derivatives, and more particularly to the compound (S)-1-?(S)-2-(4-methoxybenzamido)-3-methylbutyryl!-N-?(S)-2-methyl-1-(trif luoroacetyl)propyl!pyrrolidine-2-carboxamide, shown by formula I, and solvates thereof. The present invention also provides pharmaceutical compositions, intermediates and methods of preparation of the compound. The compound of formula I is an inhibitor of human neutrophil elastase and is useful in the treatment of diseases in which the enzyme is implicated, such as, for example, emphysema and acute respiratory distress syndrome (ARDS).Type: GrantFiled: January 27, 1998Date of Patent: May 25, 1999Assignee: Zeneca LimitedInventors: Stephen John Pegg, George Joseph Sependa, Elwyn Peter Davies, Chris Allan Veale
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Patent number: 5856560Abstract: A process and intermediates for preparing .alpha.Type: GrantFiled: December 10, 1996Date of Patent: January 5, 1999Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Heinz Isak, Horst Wingert, Hubert Sauter, Michael Keil, Markus Nett, Remy Benoit, Ruth Muller
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Patent number: 5804595Abstract: The invention provides certain amino acid conjugates of substituted 2-phenyl-N-?1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.Type: GrantFiled: December 5, 1995Date of Patent: September 8, 1998Assignee: Regents of the University of MinnesotaInventors: Philip S. Portoghese, An-Chih Chang
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Patent number: 5739157Abstract: The present invention relates to pyrrolidine derivatives, and more particularly to the compound (S)-1-?(S)-2-(4-methoxybenzamido)-3-methylbutyryl!-N-?(S)-2-methyl-1-(trif luoroacetyl)propyl!pyrrolidine-2-carboxamide, shown by formula I, and solvates thereof. The present invention also provides pharmaceutical compositions, intermediates and methods of preparation of the compound. The compound of formula I is an inhibitor of human neutrophil elastase and is useful in the treatment of diseases in which the enzyme is implicated, such as, for example, emphysema and acute respiratory distress syndrome (ARDS).Type: GrantFiled: July 25, 1996Date of Patent: April 14, 1998Assignee: Zeneca LimitedInventors: Stephen John Pegg, George Joseph Sependa, Elwyn Peter Davies, Chris Allan Veale
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Patent number: 5731434Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: June 1, 1995Date of Patent: March 24, 1998Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen
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Patent number: 5726159Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
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Patent number: 5714491Abstract: Peptidyl derivatives are disclosed that are orally active metalloproteinase inhibitors. The peptidyl derivatives have a selective gelatinase action, have a long duration of action, and are useful in the prophylaxis or treatment of diseases or disorders in which stromelysis, collagenase or gelatinase have a role, for example, in the treatment of cancer to control the development of tumor metastases.Type: GrantFiled: February 6, 1995Date of Patent: February 3, 1998Assignee: Celltech Therapeutics LimitedInventors: John Richard Morphy, Thomas Andrew Millican
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Patent number: 5709867Abstract: Novel pharmaceutically/cosmetically-active polyaromatic amides have the structural formula (I): ##STR1## wherein Z is a radical --CO--NH-- or --NH--CO--, and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: December 15, 1994Date of Patent: January 20, 1998Assignee: Centre International De Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5710130Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 20, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5707966Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 13, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5705487Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 6, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5688945Abstract: The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R.sup.3, R.sup.4 are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z--R.sup.5 wherein Z is selected from CH.sub.n, NH.sub.m, O, S, SO.sub.2 and CO wherein n=1 or 2; m=0 or 1 and R.sup.5 is selected from alkyl, aryl and fluoroalkyl; or R.sup.3 and R.sup.4 together form a saturated or unsaturated ring system Y--V--Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C.sub.1 -C.sub.3 alkylene or alkenylene, --N.dbd., --N.dbd.N-- and ##STR2## wherein R.sub.Type: GrantFiled: December 20, 1996Date of Patent: November 18, 1997Assignees: Astra Aktiebolag, The University of Maryland at BaltimoreInventors: Susanna Karin Maria Bjork, Birgitta Kristina Gotthammar, Mats Torbjorn Linderberg, Johan Per Luthman, Kerstin Margareta Irma Persson, Robert Schwarcz
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Patent number: 5677466Abstract: The invention relates to new labelled fibrinogen receptor antagonists which have an affinity for the receptor which is comparable to or greater than that of .sup.125 I-fibrinogen and whose binding is not disrupted by foreign proteins.Type: GrantFiled: May 23, 1995Date of Patent: October 14, 1997Assignee: Dr. Karl Thomae, GmbHInventors: Johannes Weisenberger, Hans-Dieter Schubert, Gunter Linz, Karl-Heinz Switek, Frank Himmelsbach
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Patent number: 5659065Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or heteroaromatic radical, a hydroxy group that is aliphatically, araliphatically or heteroarylaliphatically etherified or protected by a hydroxy-protecting group, or an aliphatically etherified mercapto group, andR.sub.2 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical, orR.sub.1 and R.sub.2 together form a divalent aliphatic radical,R.sub.3 is free or aliphatically, araliphatically or aromatically esterified carboxy, formyl or hydroxymethyl,R.sub.4 is hydrogen, an aliphatic or araliphatic radical or an amino-protecting group, andR.sub.5 is hydrogen or an aliphatic radical,and the salts thereof can be used as intermediates in the preparation of medicinal active ingredients.Type: GrantFiled: April 4, 1995Date of Patent: August 19, 1997Assignee: Novartis CorporationInventor: Richard Goschke
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Patent number: 5646147Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.Type: GrantFiled: April 20, 1994Date of Patent: July 8, 1997Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5607950Abstract: The invetion is a method of treating irritable bowel syndrome with a compound selected from the formula ##STR1## wherein R, R.sup.1, m, n p are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 10, 1994Date of Patent: March 4, 1997Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross, Alexander R. Mackenzie
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Patent number: 5571832Abstract: Compounds comprising a pyrrolidinyl ring are disclosed for use in the treatment of cerebral ischemia.Type: GrantFiled: June 20, 1994Date of Patent: November 5, 1996Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Brian R. de Costa, Wayne D. Bowen, Xiao-Shu He, Lilian Radesca, Kenner C. Rice
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Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5552412Abstract: Compounds of this formula ##STR1## are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.Type: GrantFiled: January 9, 1995Date of Patent: September 3, 1996Assignee: Pfizer IncInventors: Kimberly O. Cameron, Paul A. Dasilva Jardine, Robert L. Rosati
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Patent number: 5535048Abstract: Novel nonlinearly optically active compound's, well suited for electrooptical applications, have the following general formulae: ##STR1## wherein D is an electron donor group; A and A.sub.1, which may be identical or different, are each an electron acceptor group; and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each a lower alkyl radical or a hydrogen atom.Type: GrantFiled: March 21, 1994Date of Patent: July 9, 1996Assignee: Flamel TechnologiesInventors: Gerard Mignani, Gerard Soula, Remi Meyrueix
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Patent number: 5525735Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds and derivatives thereof on solid supports and synthetic compound libraries comprising pyrrolidine groups and derivatives thereof prepared by such methods.Type: GrantFiled: December 12, 1994Date of Patent: June 11, 1996Assignee: AFFYMAX Technologies NVInventors: Mark A. Gallop, Martin A. Murphy
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Patent number: 5525734Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds on solid supports and synthetic compound libraries comprising pyrrolidine groups prepared by such methods.Type: GrantFiled: June 22, 1994Date of Patent: June 11, 1996Assignee: Affymax Technologies N.V.Inventors: Mark A. Gallop, Martin A. Murphy
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Patent number: 5514683Abstract: The compounds of the formula I ##STR1## and their pharmaceutical acceptable salts, which are defined herein, are ligands for cholecystokinin and/or gastrin receptors.Type: GrantFiled: August 9, 1994Date of Patent: May 7, 1996Assignee: James Black Foundation LimitedInventors: Sarkis B. Kalindjian, Caroline M. R. Low, Iain M. McDonald, Robert A. D. Hull, Nigel P. Shankley, Ildiko M. Buck, Katherine I. M. Steel, Jonathan M. R. Davies, David J. Dunstone, Elaine A. Harper, Michael J. Pether, Michael J. Bodkin, Matthew J. Tozer, Martin L. Hudson
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Patent number: 5508418Abstract: Novel compounds useful in the preparation of enantiomerically-pure 3-methyl-5-(1-(C.sub.1 -C.sub.3 -alkyl)-2-pyrrolidinyl)isoxazole in high yield, namely 5(S)-(3-methyl-5-isoxazolyl)-2-pyrrolidinone, 3-methyl-5-(1-methyl-2-pyrrolidinyl)-5-hydroxy-4,5-dihydro-isoxazole, and 1-(1-methyl-2(S)-pyrrolidinyl)-1,3-butanedione-3-oxime.Type: GrantFiled: June 7, 1995Date of Patent: April 16, 1996Assignee: Abbott LaboratoriesInventors: Nan-Horng Lin, Yun He, William H. Bunnelle
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Patent number: 5489562Abstract: A herbicidal composition having acivicin, its derivatives or salts or combinations thereof as its active component.A process for controlling unwanted plants comprising applying a herbicidally effective amount of acivicin, its derivatives or salts or combinations thereof to the unwanted plant.Type: GrantFiled: July 13, 1994Date of Patent: February 6, 1996Assignee: Rohm and Haas CompanyInventors: Ernest L. Burdge, Lori A. Spangler
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Patent number: 5489603Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.Type: GrantFiled: July 15, 1993Date of Patent: February 6, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
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Patent number: 5486528Abstract: Novel basic ether of general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen or C.sub.1-4 alkoxy, or together they represent a 3,4-methylenedioxy group,R stands for C.sub.1-8 alkyl,R.sup.3 represents hydrogen, C.sub.1-4 alkyl or hydroxy,A is a valency bond or methylene group,R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-12 alkyl or C.sub.1-12 alkenyl, orR.sup.4 and R.sup.5 form together with the adjacent nitrogen atom 1-pyrrolidinyl, 1-piperidinyl, morpholino or 1-piperazinyl groups, stereo and optically active isomers and their possible mixtures, acid-addition salts and quaternary ammonium derivatives thereof. The basic ethers have antiulceric and anxiolytic activities.Type: GrantFiled: April 11, 1994Date of Patent: January 23, 1996Assignee: Egis Gyogyszergyar Rt.Inventors: Judit Bajnogel, Gabor Blasko, Zoltan Budai, Eva Schmidt, Andras Egyed, Marton Fekete, Istvan Gacsalyi, Istvan Gyertyan, Tibor Mezei, Kalara Reiter nee Esses, Gyula Simig, Katalin Szemeredi, Enik Szirt nee Kiszelly
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Patent number: 5476950Abstract: This invention provides novel pyridonecarboxylic acid derivatives having a quite high antimicrobial activity. The derivatives have the following formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 represent each a hydrogen or C.sub.1-C.sub.6 alkyl group; R.sup.4 represents an ethyl, 2-fluoroethyl, vinyl, isopropyl, isopropenyl or cyclopropyl group; and X represents CH, C--F, C--Cl or Ncharacterized in that R.sup.2 and R.sup.3 are not hydrogen at the same time.Type: GrantFiled: March 20, 1995Date of Patent: December 19, 1995Assignee: Daiichi Seiyaku Co., Ltd.Inventors: Isao Hayakawa, Shohgo Atarashi
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5472984Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: December 29, 1993Date of Patent: December 5, 1995Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5470921Abstract: A synthetic polyamide of formula I and its salts ##STR1## in which each R.sub.1 independently is selected from hydrogen, carboxyl, amino or a group of formula .alpha.-A.sub.1 -R.sub.10 (.alpha.)where A, is a bridging group and R.sub.10 is a sterically hindered amine group;each R.sub.2 independently is hydrogen or a group of formula .alpha.A is a bridging group of the formula ##STR2## is 0 or 1; R.sub.3 is hydrogen, C.sub.1-12 alkyl or is a significance of R.sub.10 ;R.sub.5 is hydrogen or C.sub.1-12 alkylR.sub.4 is a significance of R.sub.10 or a group of formula .alpha.; andp is an integer from 5 to 200;with the proviso that the compound of formula I contains 1-400 sterically hindered amine groups.Type: GrantFiled: May 20, 1994Date of Patent: November 28, 1995Assignee: Sandoz Ltd.Inventors: Bansi L. Kaul, Angelos-Elie Vougioukas, Jurgen Goldmann
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Patent number: 5466828Abstract: Chiral 3-cyanopyrrolidines of the following formula are disclosed, wherein R' is as defined herein. The compounds are useful as intermediates for naphthyridine and quinoline antibiotics.Type: GrantFiled: May 5, 1994Date of Patent: November 14, 1995Assignee: Warner-Lambert CompanyInventors: Victor Fedij, Mark J. Suto, James N. Wemple, James R. Zeller
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Patent number: 5461165Abstract: Individual stereoisomers of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones are described, their therapeutic advantages as antibacterial agents, as well as a novel method for the preparation and isolation of such stereoisomers.Type: GrantFiled: March 30, 1994Date of Patent: October 24, 1995Assignee: Warner-Lambert CompanyInventors: John M. Domagala, John S. Kiely, Mel C. Schroeder
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Patent number: 5457122Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 13, 1993Date of Patent: October 10, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5457202Abstract: A process for preparing (6S)-5-methyltetrahydrofolic acid by resolution of racemic (6R,S)-5-methyltetrahydrofolic acid using a base, wherein the base is N-ethyl-2-aminomethylpyrrolidine or its optical isomers.Type: GrantFiled: May 6, 1994Date of Patent: October 10, 1995Assignee: Knoll AktiengesellschaftInventors: Klaus Scheib, Peter Klein, Robert Carter
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Patent number: 5439888Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.Type: GrantFiled: March 4, 1994Date of Patent: August 8, 1995Assignee: Eli Lilly and CompanyInventors: Robert T. Shuman, Gerald F. Smith
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Patent number: 5432178Abstract: Amidinophenol derivatives of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are (i) H, (ii) C1-4 alkyl, (iii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO.sub.2, (vii) benzoyl, (viii) COOR.sup.4 (in which R.sup.4 is C1-3 alkyl); A is bond, C1-4 alkylene, --C(R.sup.5).dbd.C(R.sup.6)-- (in which R.sup.5 and R.sup.6 are H or C1-4 alkyl; R.sup.3 is (i) CON(R.sup.7)(R.sup.8), (ii) CON(R.sup.9)--CH(R.sup.7)(R.sup.8) or (iii) ##STR2## in which ##STR3## is 4-7 membered, mono-cyclic hetero ring containing 1 or 2 N atom; R.sup.10 is H, C7-10 phenylalkyl or COOR.sup.13 (in which R.sup.13 is H, C1-4 alkyl or C7-10 phenylalkyl)); with the proviso that (i) both R.sup.7 and R.sup.8 do not represent hydrogen at the same time, and (ii) when at least one group in R.sup.7, R.sup.8 and R.sup.9 represents the group containing t-butyl ester, the other groups do not represent tile group containing carboxy; or an acid-addition salt thereof, have inhibitory activities on PLA.sub.Type: GrantFiled: September 16, 1993Date of Patent: July 11, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Masanori Kawamura, Tsumoru Miyamoto
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Patent number: 5401869Abstract: Aminomethylene compounds of the formula ##STR1## may advantageously be prepared by reacting C--H-acidic compounds of the formula ##STR2## with formamide acetals of the formula ##STR3## in which the radicals R.sup.1 to R.sup.6 have the meaning given in the description,if the process is carried out in the presence of a secondary amine of the formula ##STR4## in which R.sup.7 and R.sup.8 have the meaning given in the description.Type: GrantFiled: January 21, 1994Date of Patent: March 28, 1995Assignee: Bayer AktiengesellschaftInventors: Helmut Kraus, Nikolaus Muller, Gerhard Marzolph, Bernhard Beitzke
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Patent number: 5399570Abstract: Aspartic acid derivatives of the formula ##STR1## in which X denotes, for example, ##STR2## and R denotes, for example, cyclohexylamino, have useful pharmacological properties.Type: GrantFiled: March 25, 1993Date of Patent: March 21, 1995Assignee: Cassella AktiengesellschaftInventors: Otmar Klingler, Gerhard Zoller, Melitta Just, Bernd Jablonka
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Patent number: 5389616Abstract: The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth above, are described.The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.Type: GrantFiled: July 29, 1993Date of Patent: February 14, 1995Assignee: Hoffman-LaRoche Inc.Inventors: Quirico Branca, Werner Neidhart, Jenri Ramuz, Henri Ramuz, Heinz Stadler, Wolfgang Wostl
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Patent number: 5359072Abstract: Novel nonlinearly optically active compounds, well suited for electrooptical applications, have the following general formulae: ##STR1## wherein D is an electron donor group; A and A.sub.1, which may be identical or different, are each an electron acceptor group; and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each a lower alkyl radical or a hydrogen atom.Type: GrantFiled: June 13, 1991Date of Patent: October 25, 1994Assignee: Rhone-Poulenc ChimieInventors: Gerard Mignani, Gerard Soula, Remi Meyrueix
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Patent number: 5354904Abstract: The sulfonamides have the formula ##STR1## where R.sup.1 is C.sub.1 -C.sub.13 -lkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.8 -alkanoyl or substituted or unsubstituted benzoyl, andR.sup.2 and R.sup.3 are each independently of one another substituted or unsubstituted C.sub.1 -C.sub.13 -alkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkyl or substituted or unsubstituted piperidinyt, or R.sup.2 may also be hydrogen.Type: GrantFiled: October 8, 1992Date of Patent: October 11, 1994Assignee: BASF AktiengesellschaftInventors: Udo Mayer, Ulrike Schloesser
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Patent number: 5347017Abstract: The process for the preparation of chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines used as key intermediates for the preparation of naphthyridine and quinolone antibacterial agents which comprises reacting readily available chiral 1-substituted-3-pyrrolidinols to their corresponding chiral sulfonate esters; converting the sulfonate esters to chiral 1-substituted-3-cyanopyrrolidines having an inverse configuration, and then dialkylating the chiral cyanopyrrolidines with alkyl lithium in the presence of a Lewis acid without racemization at the asymmetric carbon atom is described.Type: GrantFiled: July 7, 1993Date of Patent: September 13, 1994Assignee: Warner-Lambert CompanyInventors: Victor Fedij, Mark J. Suto, James N. Wemple, James R. Zeller
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Patent number: 5340831Abstract: Muscarinic receptor antagonists of formula (I), and their pharmaceutically acceptable salts, wherein Y is --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.sub.2 O--, --(CH.sub.2).sub.2 O-- or --CH.sub.2 S--; R is --CH or --CONH.sub.2 ; and R.sup.1 is a group of formula (a), where R.sup.2 and R.sup.3 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.n OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.n NR.sup.4 R.sup.5, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), --CH(OH)(C.sub.1 -C.sub.4 alkyl), --C(OH)(C.sub.1 -C.sub.4 alkyl.sub.2, --SO.sub.2 NH.sub.2, --(CH.sub.2).sub.n CONR.sup.6 R.sup.7 or --(CH.sub.2).sub.n COO(C.sub.1 -C.sub.4 alkyl); R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; R.sup.5 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkysulphonyl; R.sup.6 and R.sup.7 are each independently H or C.sub.1 -C.sub.4 alkyl; and n is 0, 1 or 2. The compounds are particularly useful in treating irritable bowel syndrome.Type: GrantFiled: June 12, 1990Date of Patent: August 23, 1994Assignee: Pfizer Inc.Inventors: Peter E. Cross, Alexander R. MacKenzie
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Patent number: 5322858Abstract: There are provided compounds of the formula ##STR1## wherein R.sup.1 is a substituted or unsubstituted divalent aliphatic group of 1 to 16 carbon atoms; wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, aryl and arlkyl, R.sup.3 is selected from the group consisting of same group of values as R.sup.5, R.sup.5 is selected from the group consisting of substituted and unsubstituted alkyl of 1-10 carbon atoms, aryl, cycloalkyl and heterocycloalkyl of 3-8 carbon atoms, wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, cycloalkyl of 3-8 carbon atoms, lower alkenyl, lower alkynyl, nitro, lower alkoxy, lower alkoxycarbonyl, phenyl loweralkyl, phenyl, mono and polyhalophenyl, phenoxy, mono and polyhalophenoxy, R.sup.6 and R.sup.7 may be the same or different and are hydrogen, alkanoyl or alkoxyalkanoyl, R.sup.7 may also have the same value as R.sup.Type: GrantFiled: February 14, 1992Date of Patent: June 21, 1994Assignee: Jacobus Pharmaceutical Co. Inc.Inventors: Craig Canfield, David P. Jacobus, Neil J. Lewis
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Patent number: 5300660Abstract: Stereoconservative method for preparation of an (R)- or (S)-isomer of the compound of the formula I with at least 95% optical purity ##STR1## wherein R.sup.1 is a hydrogen atom, a saturated or unsaturated lower alkyl group, a cycloalkyl group, or a group (CH.sub.2).sub.m Ph wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group including1) O,N-dialkylation, directly or stepwise of (R)- or (S)-proline2) aminolysis3) reduction to formation of the (R)- or (S)-isomer of the compound of the formula I, and new intermediates II and III in optical active form obtained by the reaction steps above and wherein R.sup.2 is defined as R.sup.1 above.Type: GrantFiled: November 12, 1992Date of Patent: April 5, 1994Assignee: Astra Lakemedel AktiebolagInventors: Hans-Jurgen Federsel, Thomas Hogberg, Sten I. Ramsby, Hans E. P. Strom