The Nitrogen Is In A Substituent Attached To The Ring Nitrogen Of The Five Membered Hetero Ring Patents (Class 548/569)
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Patent number: 6887872Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.Type: GrantFiled: March 13, 2001Date of Patent: May 3, 2005Assignee: N-Gene Research Laboratiories Inc.Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
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Patent number: 6878736Abstract: Compounds of formula (I) (and pharmaceutically acceptable salts thereof) are histamine H3 receptor ligands.Type: GrantFiled: February 15, 1999Date of Patent: April 12, 2005Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Ildiko Maria Buck, Ian Duncan Linney, Gillian Fairfull Watt, Elaine Anne Harper, Nigel Paul Shankley
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Patent number: 6818715Abstract: Bisimine compounds of the formula (I) where the symbols are defined in the specification are used to prepare bisimidinato complexes which can be used in the polymerization of unsaturated compounds.Type: GrantFiled: February 19, 2002Date of Patent: November 16, 2004Assignee: BASF AktiengesellschaftInventors: Marc Oliver Kristen, Andrei Gonioukh, Dieter Lilge, Stephan Lehmann, Benno Bildstein, Christoph Amort, Michael Malaun
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Patent number: 6624177Abstract: The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix melatoproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: March 2, 1999Date of Patent: September 23, 2003Assignee: Warner-Lambert CompanyInventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic, Andrew David White
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Patent number: 6608196Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.Type: GrantFiled: May 3, 2002Date of Patent: August 19, 2003Assignee: Galileo Pharmaceuticals, Inc.Inventors: Bing Wang, Satyanarayana Janagani, Wyeth B. Callaway, Jonathan L. Sessler
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Patent number: 6545037Abstract: A compound of formula (I): which is useful as a TXA2 and 5-HT2 receptor and pharmaceutical compositions containing the same.Type: GrantFiled: March 14, 2002Date of Patent: April 8, 2003Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Bernard Cimetiere, Tony Verbeuren, Serge Simonet, Jean-Jacques Descombes
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Patent number: 6506759Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: October 31, 2000Date of Patent: January 14, 2003Assignee: Monsanto CompanyInventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
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Patent number: 6469011Abstract: Compound of formula (I): which is useful as a TXA2 and 5-HT2 receptor antagonist and pharmaceutical compositions containing the same.Type: GrantFiled: January 18, 2001Date of Patent: October 22, 2002Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Bernard Cimetiere, Tony Verbeuren, Serge Simonet, Jean-Jacques Descombes
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Patent number: 6436235Abstract: N-substituted perfluoroalkylated pyrrolidines of the formula III where RF, B, Q and q are as defined herein are prepared from diallylamine, a perfluoroalkyl iodide and an amino-reactive compound selected from the group of carboxylic acids, anhydrides, acid chlorides, oxiranes, haloalkanes, isocyanates, ureas and (meth)acrylic compounds. These compounds are useful as specialty surfactants and as oil-proofing agents for paper and textiles. Polymers derived from the (meth)acrylamides are useful to impart water, oil and grease repellency to various substrates.Type: GrantFiled: October 18, 2000Date of Patent: August 20, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Marlon Haniff, John Jennings, Karl Friedrich Mueller, Shobha Kantamneni
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Patent number: 6413987Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.Type: GrantFiled: June 6, 2000Date of Patent: July 2, 2002Assignee: Bridge Pharma, Inc.Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
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Patent number: 6399824Abstract: Substituted cinnamic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I which may be obtained by reaction of a compound II with guanidine.Type: GrantFiled: September 18, 2001Date of Patent: June 4, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Armin Hofmeister, Max Hropot, Uwe Heinelt, Markus Bleich, Hans-Jochen Lang
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Patent number: 6395735Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.Type: GrantFiled: December 19, 2000Date of Patent: May 28, 2002Assignee: Eli Lilly and CompanyInventors: Sean Patrick Hollinshead, Philip Floyd Hughes, Jose Serafin Mendoza, Joseph Wendell Wilson, Bret Eugene Huff, Charles Howard Mitch, Michael Alexander Staszak, John Stanley Ward
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Patent number: 6362230Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: November 21, 2000Date of Patent: March 26, 2002Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Dennis Michael Zimmerman, Ana Maria Escribano
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Publication number: 20020026034Abstract: 1 The present invention ocncerns new amidinopyrroline derivatives of formula (I) with the meanings of the symbols as given in the description as well as a process for their production and their use in pharmaceutical preparations.Type: ApplicationFiled: June 8, 1998Publication date: February 28, 2002Inventors: RICHARD ENGH, SILVIA KONETSCHNY-RAPP, HANS-WILLI KRELL, MARTIN ULRICH, CHRISTOS TSAKLAKIDIS
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Patent number: 6342609Abstract: A process for industrially preparing intermediates of aromatic amidine derivatives having anticoagulant activity, i.e.Type: GrantFiled: November 26, 1999Date of Patent: January 29, 2002Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Toru Makino, Yukio Yokoyama
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Patent number: 6323223Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 14, 1998Date of Patent: November 27, 2001Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Patent number: 6294569Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.Type: GrantFiled: January 26, 2001Date of Patent: September 25, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6281211Abstract: This invention is related to substituted semicarbazides represented by Formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1 and R2 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R3, R4, R5 and R6 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R3 and R4 is defined as above, and R5 and R6 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one of O, S, NR7, CH2, C(O), NR7C(O), C(O)NR7, SO, SO2 or a covalent bond; where R7 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n isType: GrantFiled: September 21, 2000Date of Patent: August 28, 2001Assignee: Euro-Celtique S.A.Inventors: Sui Xiong Cai, Nancy C. Lan, Soo Hong-Bae
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Patent number: 6281206Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: February 11, 2000Date of Patent: August 28, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6255277Abstract: A method for preventing adverse effects associated with the use of a medical device in a patient by introducing into the patient a device of which at least a portion includes a prophylactic or therapeutic amount of a nitric oxide adduct. The nitric oxide adduct can be present in a matrix coating on a surface of the medical device; can be coated per se on a surface of the medical device; can be directly or indirectly bound to reactive sites on a surface of the medical device; or at least a portion of the medical device can be formed of a material, such as a polymer, which includes the nitric oxide adduct. Also disclosed is a method for preventing adverse effects associated with the use of a medical device in a patient by introducing the device during a medical procedure and before or during said procedure locally administering a nitric oxide adduct to the site of contact of said device with any internal tissue.Type: GrantFiled: May 10, 1995Date of Patent: July 3, 2001Assignees: Brigham and Women's Hospital, NitroMed, Inc.Inventors: Jonathan Stamler, Joseph Loscalzo, John D. Folts
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Publication number: 20010001802Abstract: A process for industrially preparing intermediates of aromatic amidine derivatives having anticoagulant activity (Japanese Patent Application Laid-Open No. 5-208946); i.e., compounds represented by formula (3) or salts thereof by the following reaction scheme including (1), (2), and (3), wherein R1 represents H, an alkanoyl group, an alkoxycarbonyl group, an aralkyl group, an aralkyloxycarbonyl group, or the like; and R3 represents H, an alkyl group, or an alkanoyl group.Type: ApplicationFiled: November 26, 1999Publication date: May 24, 2001Inventors: TORU MAKINO, YUKIO YOKOYAMA
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Patent number: 6201007Abstract: A compound of the following formula: and the salts thereof wherein A is hydrogen, halo, or hydroxy, broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.Type: GrantFiled: March 12, 1999Date of Patent: March 13, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6174922Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: February 23, 1999Date of Patent: January 16, 2001Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Dennis Michael Zimmerman, Ana Maria Escribano
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Patent number: 6110944Abstract: The present invention provides compounds having the structureAr.sub.1 --Q--Ar.sub.2 --O--(CH.sub.2).sub.n --Zand pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.Type: GrantFiled: March 12, 1997Date of Patent: August 29, 2000Assignee: G. D. Searle & Co.Inventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell
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Patent number: 6033446Abstract: A polyalklpyroroplidine compound of the formula: ##STR1## or a fuel-soluble salt thereof; wherein R.sub.1 is a polyalkyl group having an average molecular weight in the range of from about 500 to 5,000;R.sub.2 is a straight- or branched-chain alkylene group having from about 2 to 6 carbon atoms;is R.sub.3 is H or CH.sub.3 ; andx is an integer from about 0 to 4.The polyalkylpyrrolidines of the present invention are useful as fuel additives for the prevention and control of engine deposits.Type: GrantFiled: June 2, 1999Date of Patent: March 7, 2000Assignee: Chevron Chemical Company LLCInventors: Richard E. Cherpeck, James D. Kramer
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Patent number: 6017918Abstract: The present invention provides compounds having the Formula I ##STR1## The present invention also provides methods of treating atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.Type: GrantFiled: July 26, 1999Date of Patent: January 25, 2000Assignee: Warner-Lambert CompanyInventors: Helen Tsenwhei Lee, Mark Alan Massa, William Chester Patt, Bruce David Roth
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Patent number: 5998630Abstract: The present invention relates to compounds used for increasing activation of the 5-HT1F receptor.Type: GrantFiled: May 21, 1999Date of Patent: December 7, 1999Assignee: Eli Lilly and CompanyInventors: James E Fritz, Patric J Hahn, Stephen W Kaldor, Miles G Siegel, Yao-Chang Xu
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Patent number: 5998399Abstract: Method of treating or reducing the risk of human disease or condition in which the synthesis or oversynthesis of nitric oxide forms a contributory part wherein a therapeutically effective amount of the compound of formula (I) as defined in the specification is administered to a person suffering from or susceptible to such disease or condition.Type: GrantFiled: November 16, 1998Date of Patent: December 7, 1999Assignee: Astra AktiebolagInventors: James E. Macdonald, Robert Gentile, Robert J. Murray
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Patent number: 5955632Abstract: New seco-D steroid derivatives, processes for their preparation and pharmaceutical compositions are provided, which are active on the cardiovascular system.Type: GrantFiled: July 10, 1997Date of Patent: September 21, 1999Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Mauro Gobbini, Sergio De Munari, Giorgio Fedrizzi, Patrizia Ferrari, Piero Melloni, Marco Santagostino, Marco Torri
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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: 5922763Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: November 26, 1997Date of Patent: July 13, 1999Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
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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: 5885990Abstract: Substituted amidinonaphthyl ester compounds effective for treatment of thrombosis are represented by the following formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1## wherein R.sub.1 represents (4,5-dihydro-1H-imidazol-2-yl)amino group, (4,5-dihydro-1,3-thiazol-2-yl)amino group, amidino group, morpholinomethyl group, nitro group, amino group, dimethylamino group, ##STR2## R.sub.3 represents hydrogen, methoxy group, hydroxyl group, acetylamino group, morpholino group, piperidino group, 1-pyrrolidinyl group or dimethylamino group,m represents 0-4,R.sub.4 represents hydrogen or methyl group,R.sub.2 represents NH.sub.2 CO(CH.sub.2).sub.n --, 2-(carbamoyl)vinyl group or R.sub.5 OOC(CH.sub.2).sub.n --,R.sub.5 represents dimethylcarbamoylmethyl group, hydrogen or lower alkyl group, andn represents 0-2.Type: GrantFiled: June 12, 1997Date of Patent: March 23, 1999Assignee: Torii Pharmaceutical Co., Ltd.Inventors: Toyoo Nakayama, Hiroyuki Kawamura, Hiroyuki Uchiyama
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Patent number: 5856309Abstract: Compound of formula (I) are disclosed ##STR1## as well as optically active isomers or pharmacologically acceptable salts thereof. The compounds are useful active ingredients in pharmaceutical compositions, and methods of treating osteoporosis, inflammation or diseases which are due to thromboembolic events. Compounds of formula (II) are also disclosed ##STR2## which are useful as starting compounds for preparing compounds of formula (I).Type: GrantFiled: April 14, 1997Date of Patent: January 5, 1999Assignee: Boehringer Mannheim GmbHInventors: Silvia Konetschny-Rapp, Hans-Willi Krell, Ulrich Martin, Richard Engh, Christos Tsaklakidis
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Patent number: 5834508Abstract: A novel ketone 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 6, 1997Date of Patent: November 10, 1998Assignee: Mitsubishi Chemical CorporationInventors: Ryoichi Ando, Naoko Ando, Hirokazu Masuda, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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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: 5801179Abstract: The present invention is concerned with compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1--6 alkyl; R.sup.2 is hydrogen or C.sub.1- 6 alkyl; R.sup.3 is C.sub.1-6 alkyl, hydroxy, cyano, halo, C.sub.1-6 alkyloxy, aryloxy, arylmethoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkyl--S--, C.sub.1-6 alkyl(S.dbd.O)--, C.sub.1-6 alkylcarbonyl; R.sup.4 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxy; or R.sup.3 and R.sup.4 taken together form a bivalent radical; R.sup.5 and R.sup.6 each independently are hydrogen, halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.7 is hydrogen; Alk.sup.1 is C.sub.2-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## Pharmaceutical compositions, preparations and use as a medicine are described.Type: GrantFiled: June 2, 1997Date of Patent: September 1, 1998Assignee: Janssen Pharmaceutica, NVInventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Piet Tom Bert Paul Wigerinck
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Patent number: 5756765Abstract: The present invention relates to a mercaptopyrrolidinyl derivative of the following formula ##STR1## suitable for the preparation of carbapenem compounds.Type: GrantFiled: March 14, 1997Date of Patent: May 26, 1998Assignee: Chong Kun Dang Corp.Inventors: Hyo Sung Kwak, Chong Ryul Lee, Sang Choon Lee, Hong Woo Lee, Hoi Choo Son, Eung Nam Kim, Kyeong Bok Min
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Patent number: 5753715Abstract: The invention relates to cyclohexenyl antibacterial compounds of the formula I: ##STR1## and pharmaceutical compositions containing the compounds, methods for their production and use.Type: GrantFiled: June 2, 1995Date of Patent: May 19, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Robert H. Chen, Maud Urbanski, Min Xiang, John Francis Barrett
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Patent number: 5753680Abstract: Heterocyclyl-benzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Het have the meanings given herein, and physiologically unobjectionable salts thereof, display antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.Type: GrantFiled: August 30, 1995Date of Patent: May 19, 1998Assignee: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Rolf Gericke, Dieter Dorsch, Manfred Baumgarth, Klaus-Otto Minck, Norbert Beier
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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: 5736559Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: August 1, 1996Date of Patent: April 7, 1998Assignee: Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5686447Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.Type: GrantFiled: June 1, 1995Date of Patent: November 11, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
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Patent number: 5686446Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.Type: GrantFiled: June 1, 1995Date of Patent: November 11, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
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Patent number: 5686483Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.Type: GrantFiled: June 1, 1995Date of Patent: November 11, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
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Patent number: 5684021Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.Type: GrantFiled: June 1, 1995Date of Patent: November 4, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
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Patent number: 5648367Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.Type: GrantFiled: June 1, 1995Date of Patent: July 15, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
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Patent number: 5618825Abstract: Combinatorial libraries are disclosed which are represented by Formula I:(T'--L).sub.q -- S--C(O)--L'--II' Iwherein:S is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. Compounds which contain aryl sulfonamides, N-acyl derivatives, and N-substituted pyrrolidines and piperidines of the formula :Y--A--CO--R.sup.1are inhibitors of serine proteases and carbonic anhydrase isozymes. They are useful in the treatment of hyper-coagulation disease and ocular diseases such as glaucoma.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: Pharmacopeia, Inc.Inventors: John J. Baldwin, Michael H. J. Ohlmeyer, Ian Henderson
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Patent number: 5614536Abstract: Substituted N-aminoalkylmethane sulfanilide of formula (I), their solutions and pharmaceutically acceptable addition salts, their pharmaceutical compositions and their therapeutic use. In formula (I) Y represents hydrogen, cyano, nitro, amino, acetamide or halogen; n is an integer between 2 and 4, R.sup.1 and R.sup.2 equal or different are alkyl-(C1-C4) or they are connected together and with the N-atom thereby forming a 1-pyrrolidinyl, 1-piperidinyl, 1-piperazinyl, 4-methyl-1-piperazinyl, 4-ethylpiperazinyl, 4-propylpiperazinyl, 1-homopiperidinyl or 4-morpholine residue. The products of formula (I) are used as antispasmodic agents.Type: GrantFiled: January 7, 1994Date of Patent: March 25, 1997Assignee: Roemmers S.A.I.C.F.Inventors: Carlos E. A. Monti, Gustavo E. Aldom a