The Additional Hetero Ring Consists Of One Sulfur And Four Carbons Patents (Class 546/212)
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Patent number: 6180787Abstract: The present invention relates to a novel process for preparing O-(3-amino-2-hydroxy-propyl)-hydroxymic acid halides of formula (I) by reacting a carboxamide oxime of formula (II) wherein R1 is as specified above with reactive 3-amino-2-hydroxy-propane derivative diazotizing the O-substituted carboxamide oxime thus obtained with sodium nitrite in the presence of hydrogen halide, decomposing the diazonium salt and if desired, separating the optically active enantiomers and/or reacting the resulting base with an organic or mineral acid wherein the carboxamide oxime of formula (II) is reacted with a 3-hydroxy azetidinium salt of formula (III) wherein R2 and R3 are a defined above and Y− is a salt forming anion, in a lower alcoholic, preferably ethanolic medium optionally containing water and made alkaline with an alkali hydroxide, and before diazotizing the O-substituted carboxamide oxime intermediate obtained, the reaction mixture is neutralised and the organic solvent is removed.Type: GrantFiled: December 15, 1999Date of Patent: January 30, 2001Assignee: Biorex Kutato es Fejleszto Rt.Inventors: L{acute over (a)}szl{acute over (o)} {umlaut over (U)}rögdi, Mih{acute over (a)}ly Barab{acute over (a)}s, Ede M{acute over (a)}rv{acute over (a)}nyos, Magdolna Török, Zita Cs{acute over (a)}kai
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Patent number: 6143744Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 5, 1999Date of Patent: November 7, 2000Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker
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Patent number: 6140349Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: February 1, 1999Date of Patent: October 31, 2000Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Malcolm Maccoss, Paul E. Finke, Sander G. Mills, Bryan Oates, Shankaran Kothandaraman, Dooseop Kim, Liping Wang
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Patent number: 6110943Abstract: This invention provides compounds having the structure ##STR1## that are useful as antipsychotic, antidepressant and anxiolytic agents useful in the treatment and relief of the symptoms of these disease states.Type: GrantFiled: April 6, 1999Date of Patent: August 29, 2000Assignee: American Home Products CorporationInventors: Reinhartd B. Baudy, Wayne E. Childers, Jr., Michael G. Kelly
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Patent number: 6066636Abstract: Heterocyclic derivatives of di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts and solvates) ##STR1## wherein wherein one of Y and Z is --N-- and the other is --N-- or --CH--;X is --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --;Q is ##STR2## R is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R.sup.1, R.sup.2 and R.sup.3 are H or alkyl;R.sup.4 is alkyl, cycloalkyl or ##STR3## R.sup.5 is H, alkyl, --C(O)alkyl, arylcarbonyl, --SO.sub.2 alkyl, aryl-sulfonyl --C(O)Oalkyl, aryloxycarbonyl, --C(O)NH-alkyl or aryl-aminocarbonyl, wherein the aryl portion is optionally substituted;R.sup.6 is H or alkyl; andR.sup.7 is H, alkyl, hydroxyalkyl or alkoxyalkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease.Type: GrantFiled: June 28, 1999Date of Patent: May 23, 2000Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice
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Patent number: 6022971Abstract: The present invention provides compounds of the formula (I): ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is C.sub.3 -C.sub.7 cycloalkyl, aryl or C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl being optionally substituted by fluoro, --COOH, --COO(C.sub.1 -C.sub.4) alkyl, C.sub.3 -C.sub.7 cycloalkyl, adamantyl, aryl or het.sup.1, and said C.sub.3 -C.sub.7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, fluoro, fluoro(C.sub.1 -C.sub.4) alkyl and fluoro(C.sub.1 -C.sub.4)alkoxy;R.sup.1 is phenyl, benzyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo and trifluoromethyl;R.sup.2 represents various groups;X is C.sub.1 -C.sub.4 alkylene; andX.sup.1 is a direct link or C.sub.1 -C.sub.6 alkylene.Type: GrantFiled: January 26, 1998Date of Patent: February 8, 2000Assignee: Pfizer IncInventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Donald Stuart Middleton, Sandra Dora Meadows
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Patent number: 6022868Abstract: Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.Type: GrantFiled: December 19, 1997Date of Patent: February 8, 2000Assignee: Novo Nordisk AlsInventors: Preben Houlberg Olesen, John Bondo Hansen
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Patent number: 6017947Abstract: R.sup.6 is H, halogen, alkyl, alkoxy, alkylthio, cyano, or nitro;R.sup.10 is phenylthio, dialkylamino, alkylthio, alkoxycarbonyl, N-morpholinyl, or N-piperidinyl;R.sup.11 is hydrogen or alkyl;Q is alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, alkoxycarbonyl, alkoxyiminomethyl, or Y--Ar;Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, or --CH.sub.2 SO.sub.2 --;Ar is a substituted or unsubstituted phenyl or aromatic heterocyclic group,useful for the inhibition of the replication of HIV-1, in vitro and in vivo.Type: GrantFiled: September 17, 1999Date of Patent: January 25, 2000Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5969136Abstract: This invention provides a process for preparing a compound of formula III ##STR1## wherein R.sup.1 is bromo, iodo or COOR.sup.2 ;R.sup.2 is H, C.sub.1 -C.sub.4 alkyl, phenyl which may be substituted or benzyl; andA is a 5- or 6-membered aromatic residue which may contain up to three hetero atoms and which may optionally be substituted with one or two groups selected from the group consisting of halo, hydroxy, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy; or a salt thereof, which comprises(a) reacting a compound of formula I ##STR2## wherein R is C.sub.1 -C.sub.4 alkyl or phenyl which may be substituted; andR.sup.1, R.sup.2, and A are as defined above;or a salt thereof, with a sulfurization agent;(b) cyclizing the reaction product from step (a) with guanidine; and(c) optionally salifying the reaction product from step (b).Type: GrantFiled: July 23, 1993Date of Patent: October 19, 1999Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Thomas M. Wilson
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Patent number: 5968923Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C.sub.3 -C.sub.7 cycloalkyl, aryl or C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl being optionally substituted by fluoro, COOH, --COO(C.sub.1 -C.sub.4 alkyl), C.sub.3 -C.sub.7 cycloalkyl, adamantyl, aryl or het.sup.1, and said C.sub.3 -C.sub.7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, fluoro, fluoro (C.sub.1 -C.sub.4) alkyl and fluoro (C.sub.1 -C.sub.4) Alkoxy; R.sub.1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo and trifluormethyl; R.sup.2 is --CO.sub.2 H, --CONR.sup.3 R.sup.4, --CONR.sup.5 (C.sub.3 -C.sub.7 cycloalkyl), --NR.sup.5 (C.sub.2 -C.sub.5 alkanoyl), --NR.sup.Type: GrantFiled: February 10, 1997Date of Patent: October 19, 1999Assignee: Pfizer Inc.Inventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Sandra Dora Meadows, Donald Stuart Middleton
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Patent number: 5958951Abstract: The present invention provides R(-)-N-(4,4-di(3-methylthien-2-yl)but-3-enyl)-nipecotic acid hydrochloride in its pure and stable anhydrous form.Type: GrantFiled: June 10, 1997Date of Patent: September 28, 1999Assignee: Novo NordiskialsInventors: Preben Ahrndt, Henning B.o slashed.rge Petersen, Vincent H. Chang, Kimberly Ann Allen, Michael H. Cain
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Patent number: 5952354Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.Type: GrantFiled: July 21, 1993Date of Patent: September 14, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
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Patent number: 5935951Abstract: The invention relates to novel 1-acyl-4-aliphatylaminopiperidine compounds of ##STR1## formula (I), in which R.sub.1 is a benzoyl, naphthoyl or cycloalkanoyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl; R.sub.2 is cycloalkyl or a phenyl or naphthyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen, nitro, cyano and/or trifluoromethyl; R.sub.3 and R.sub.4 together are lower alkylene or aza-, oxa- or thia-lower alkylene; or R.sub.3 is lower alkyl, lower alkoxy-lower alky, di-lower alkylamino-lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); and R.sub.4 is hydrogen, lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); R.sub.Type: GrantFiled: March 5, 1997Date of Patent: August 10, 1999Assignee: Novartis Finance CorporationInventors: Silvio Ofner, Siem Jacob Veenstra
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Patent number: 5922738Abstract: The novel heteroaryloxypyridines of formula I: ##STR1## (A, B, R.sub.1 and R.sub.2 are defined in the specification) show excellent selective herbicidal activity.The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.Type: GrantFiled: July 8, 1997Date of Patent: July 13, 1999Assignee: American Cyanamid CompanyInventors: Thomas Maier, Stefan Scheiblich, Helmut Siegfried Baltruschat, Joseph Luke Pont
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Patent number: 5914333Abstract: The present invention relates to a method for the treatment of psychotic disorders.Type: GrantFiled: July 24, 1997Date of Patent: June 22, 1999Assignee: Novo Nordisk A/SInventor: Anders Fink-Jensen
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Patent number: 5834401Abstract: The present invention provides a nitrogen-containing cyclic compound represented by the formula (1): ##STR1## (wherein R.sup.1 represents an alkyl group; R represents a hydrogen atom or an alkyl group; X represents an oxygen or sulfur atom or NR.sup.3 ; Q.sup.1 represents a hydrogen atom, or an alkyl, cycloalkyl, alkenyl or alkynyl group, or a phenyl, naphthyl or heterocyclic group etc.; Q.sup.2 represents an alkyl, cycloalkyl or alkenyl group, or a phenyl or thienyl group etc.; A.sup.1 represents a carbon or nitrogen atom; A.sup.2 represents CR.sup.2 or NR.sup.2, or an oxygen or sulfur atom, or SO or SO.sub.2 ; A.sup.3 represents a single bond, or an oxygen or sulfur atom, or CR.sup.5 or NR.sup.5) and a herbicide comprising the same , which herbicide exhibits very high herbicidal activity at very low application rate and has selectivity against crops.Type: GrantFiled: December 16, 1996Date of Patent: November 10, 1998Assignee: Nissan Chemical Industries, Ltd.Inventors: Yasuo Kawamura, Eiichi Oya, Kaoru Itoh, deceased, Hiroshi Kita, Hisashi Nakata, Kanji Sawada, Yoshitake Tamada, Tsutomu Nawamaki, Kimihiro Ishikawa, Kenichi Shiojima, Chiaki Kawaguchi, Kunimitsu Nakahira
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Patent number: 5834460Abstract: A serine derivative represented by the general formula (I) ##STR1## (symbols in the formula represent the following meanings; X: a sulfur atom or an oxygen atom,Y: a nitrogen atom or CH,R.sup.1 and R.sup.2 : the same or different from each other and each represents a hydrogen atom, a lower alkyl group or a protecting group for the amino group, or R.sup.1 and R.sup.2 may be combined together to form a four- to nine-membered nitrogen-containing cycloalkyl group,R.sup.3 : a hydrogen atom, a carboxyl group, a protected carboxyl group, an aralkyl group, or a lower alkyl group unsubstituted or substituted with a hydroxyl group,R.sup.4 : a hydrogen atom or a hydroxyl group,R.sup.Type: GrantFiled: October 12, 1995Date of Patent: November 10, 1998Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Ichio Noda, Masahiro Iwata, Shuichi Sakamoto, Kazuo Koshiya, Takuma Morita, Atsuyuki Kohara
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Patent number: 5807870Abstract: Disclosed herein are compounds of formula 1 ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an optionally mono- or disubstituted carbamoyl; B is absent or an amino acid residue, for example, Val or Asn; R.sup.1 is hydrogen or a ring substituent, for example, fluoro or methyl; R.sup.2 is alkyl; and Y is a ring substituent, for example, phenoxy, 2-pyridinylmethoxy, phenylthio or 2-pyridinylthio. The compounds inhibit the activity of human immunodeficiency virus (HIV) protease and interfere with HIV induced cytopathogenic effects in human cells. These properties render the compounds useful for combating HIV infections.Type: GrantFiled: December 11, 1996Date of Patent: September 15, 1998Assignee: BioMega Boehringer Ingelheim Research Ltd.Inventors: Paul Cates Anderson, Fran.cedilla.ois Soucy, Christiane Yoakim, Pierre Lavallee, Pierre Louis Beaulieu
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Patent number: 5786373Abstract: Novel fibrinogen receptor antagonists of the formula: X--Y--Z-Aryl-A--B and the pharmaceutically acceptable salts thereof, wherein Aryl is a 5-membered aromatic ring system containing 1 or 2 heteroatoms chosen from N, O or S wherein ring atoms may be unsubstituted or substituted with R.sup.5 and wherein S may be substituted with 0, 1 or 2 oxygen atoms; and X comprises various Nitrogen substituents including aromatic or nonaromatic systems; Y comprises, for example, alkyl or alkylaminocarbonylalkyl groups and Z and A are substituents which when present are independently chosen from alkyl or alkyloxyalkyl or other groups as defined herein; B is (a) or (b). The claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating or preventing thrombus formation.Type: GrantFiled: May 31, 1995Date of Patent: July 28, 1998Assignee: Merck & Co., Inc.Inventors: George D. Hartman, John D. Prugh, Melissa S. Egbertson, Mark E. Duggan, William Hoffman
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Patent number: 5773459Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.Type: GrantFiled: June 7, 1995Date of Patent: June 30, 1998Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Gerald McMahon
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Patent number: 5767118Abstract: The present invention is directed to certain novel compounds identified as 4-heterocycle substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.4, R.sup.5, A, R.sup.3 and the dashed line are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: October 26, 1994Date of Patent: June 16, 1998Assignee: Merck & Co., Inc.Inventors: Ravi Nargund, Arthur A. Patchett, Lihu Yang
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Patent number: 5760018Abstract: The present invention is directed to certain compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, A.sup.1, A.sup.2, X, m and n are defined herein. The compounds of this invention are tachykinin receptor antagonists and are of particular use in the treatment of pain, inflammation, migraine and emesis.Type: GrantFiled: July 11, 1996Date of Patent: June 2, 1998Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Richard Thomas Lewis, Angus Murray MacLeod, Graeme Irvine Stevenson
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Patent number: 5741799Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.Type: GrantFiled: November 8, 1995Date of Patent: April 21, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau, Steven E. Hall, Wen-Ching Han
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Patent number: 5739150Abstract: Piperidinyl thiacyclic derivatives useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT.sub.2 receptors, pharmaceutical compositions and a methods of treatment using these compounds.Type: GrantFiled: June 1, 1995Date of Patent: April 14, 1998Assignee: Merrell Pharmaceuticals Inc.Inventors: Albert A. Carr, John M. Kane, George D. Maynard, Hsien C. Cheng, Mark W. Dudley
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Patent number: 5739135Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.Type: GrantFiled: June 6, 1995Date of Patent: April 14, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Richard B. Sulsky, Joseph A. Tino
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Patent number: 5721243Abstract: Novel anticholinergics which are related to vesamicol are particularly useful when radiolabeled for evaluating cholinergic innervation in the living human brain. The cholinergic deficit in the Alzheimer's brain should be identifiable with these radioligands.Type: GrantFiled: June 13, 1994Date of Patent: February 24, 1998Assignee: Regents of the University of MinnesotaInventors: Simon Mbua Ngale Efange, Stanley M. Parsons
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Patent number: 5712279Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein Z, X.sup.1, X.sup.2, x and R.sup.5 are as defined herein.Type: GrantFiled: January 11, 1996Date of Patent: January 27, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, Richard B. Sulsky, Joseph A. Tino
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Patent number: 5698581Abstract: The invention relates to heteroaroylguanidines of the formula I ##STR1## in which the substituents HA and R(1) to R(5) have the meanings given in the specification. These compounds exhibit very good antiarrhythmic properties and are outstandingly suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventative manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: April 7, 1995Date of Patent: December 16, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5691356Abstract: Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are as defined herein.Type: GrantFiled: September 4, 1996Date of Patent: November 25, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Spencer D. Kimball, Wan Fang Lau
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Patent number: 5676884Abstract: Nonlinear optical (NLO) compositions are disclosed which contain polar disulfone-functionalized molecules (PDFMs) incorporated in a polymeric material. when aligned noncentrosymmetrically in the polymeric material, the PDFMs generate a second-order NLO response. There is also disclosed: a method of preparing a NLO composition; novel PDFMs and novel polymers; and a new process for preparing PDFMs.Type: GrantFiled: November 20, 1996Date of Patent: October 14, 1997Assignee: Minnesota Mining and Manufacturing CompanyInventors: George V. Tiers, Robert J. Koshar, Louis M. Leichter
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Patent number: 5663349Abstract: Novel processes are disclosed for the preparation and resolution of substituted piperidines of the formula ##STR1## wherein R.sup.1 and R.sup.2 are defined as below, and related compounds, as well as novel intermediates used in such processes.Type: GrantFiled: July 12, 1994Date of Patent: September 2, 1997Assignee: Pfizer IncInventors: Terry J. Rosen, Dennis M. Godek, Sally Gut, Lewin Wint
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Patent number: 5663375Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.Type: GrantFiled: August 22, 1994Date of Patent: September 2, 1997Assignees: Eli Lilly and Company, Lilly Industries LimitedInventors: Michael Brunavs, Colin Peter Dell, Peter Thaddeus Gallagher, William Martin Owton, Colin William Smith
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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: 5646144Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalized carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Ciba-Geigy CorporationInventors: Walter Schilling, Silvio Ofner, Siem J. Veenstra
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Patent number: 5635510Abstract: The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.Type: GrantFiled: October 31, 1994Date of Patent: June 3, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Timothy P. Burkholder, Elizabeth M. Kudlacz, George D. Maynard
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Patent number: 5635537Abstract: A compound of the formula ##STR1## Z is hydrogen or halogen, Q is COR.sup.1 or 5-or 6-membered aryl which may contain 1 or 2 heteroatoms selected from N, 0 or S and may be substituted or fused wherein R is hydrogen or C.sub.1 -methyl (cis-configuration), R.sup.1 is C.sub.1 -C.sub.6 alkyl or an aromatic ring which may contain heteroatoms selected from O and S and may be substituted or fused to an optionally substituted benzene ring, R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.3 may be different groups defined in claim 1, and enantiomers/salts thereof, processes for preparation of said compounds, pharmaceutical preparations containing said compounds, use of and method of treatment of disorders in CNS by using said compounds.Type: GrantFiled: March 18, 1993Date of Patent: June 3, 1997Assignee: Astra AktiebolagInventors: Nils-Erik Anden, Berit C. E. Backlund Hook, Anna L. Bjork, Uli A. Hacksell, Sven-Erik Hillver, Ye Liu, Eva C. Mellin, Eva M. Persson, Karl J. Vallg.ang.rda, Hong Yu
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Patent number: 5620971Abstract: The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.Type: GrantFiled: March 25, 1994Date of Patent: April 15, 1997Assignee: Vertex Pharmaceuticals IncorporatedInventors: David M. Armistead, Jeffrey O. Saunders, Joshua S. Boger
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Patent number: 5618938Abstract: Compounds of the formula ##STR1## and their salts with mineral or organic acids are useful as neurokinin receptor antagonists. Methods of preparing the compounds, especially pure STEREO ISOMERS thereof, are provided.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5616711Abstract: A method of producing an aminobutene derivative of formula (I) by allowing a butenol derivative of formula (II) to react with an amide derivative of formula (III) is disclosed. The aminobutene derivative of formula (I) can be deprotected to produce an aminobutene derivative of formula (I-1) or an aminobutene derivative of formula (I-2): ##STR1## The aminobutene derivative of formula (I-A) can also be deprotected to produce the aminobutene derivative of formula (I-B). Any or all of the above aminobutene derivatives are useful as intermediates for producing anti-ulcer drugs, and anti-ulcer drugs having an inhibitory effect on gastric acid secretion based on the antagonism against histamine H.sub.2 receptor.Type: GrantFiled: August 6, 1993Date of Patent: April 1, 1997Assignee: Fujirebio Inc.Inventors: Hiroshi Ikawa, Hajime Matsumoto, Masakatsu Matsumoto, Yasuo Sekine, Masato Nishimura, Akihiko Hosoda
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Patent number: 5602147Abstract: Piperidinyl thiacyclic derivatives useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT.sub.2 receptors, pharmaceutical compositions and a methods of treatment using these compounds.Type: GrantFiled: June 1, 1995Date of Patent: February 11, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Albert A. Carr, John M. Kane, George D. Maynard, Hsien C. Cheng, Mark W. Dudley
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Patent number: 5596003Abstract: Piperidinyl thiacyclic derivatives useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT.sub.2 receptors, pharmaceutical compositions and a methods of treatment using these compounds.Type: GrantFiled: June 1, 1995Date of Patent: January 21, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Albert A. Carr, John M. Kane, George D. Maynard, Hsien C. Cheng, Mark W. Dudley
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Patent number: 5583146Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.Type: GrantFiled: January 17, 1995Date of Patent: December 10, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan F. Lau, Steven E. Hall, Wen-Ching Han
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Patent number: 5576313Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.Type: GrantFiled: August 29, 1994Date of Patent: November 19, 1996Assignee: Merck & Co., Inc.Inventors: Thorsten E. Fisher, John S. Wai, J. Christopher Culberson, Walfred S. Saari
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Patent number: 5569664Abstract: Compounds of the following structure, the corresponding N-oxides and agriculturally acceptable salts, are disclosed as effective insecticides: ##STR1## in which U is selected from ##STR2## Q is selected from hydrogen, hydroxy, sulfhydryl, and fluorine; R is selected from a heterocycle having 5 or 6 ring atoms, optionally fused to a benzene ring, and ##STR3## wherein V, W, X, Y, Z are as defined in the specification.Type: GrantFiled: May 19, 1995Date of Patent: October 29, 1996Assignee: FMC CorporationInventors: Ian R. Silverman, Daniel H. Cohen, John W. Lyga, Steven W. Szczepanski, Syed F. Ali
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Patent number: 5567820Abstract: A compound of the formula ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also provided by the invention are methods of use of the above compounds, and processes for the preparation thereof.Type: GrantFiled: March 15, 1995Date of Patent: October 22, 1996Assignee: Eli Lilly and CompanyInventors: Jeffrey A. Dodge, Terry D. Lindstrom, Charles W. Lugar, III, Gilbert S. Staten
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Patent number: 5561146Abstract: Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; andR.sup.1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.Type: GrantFiled: October 14, 1994Date of Patent: October 1, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Kyoung S. Kim, Spencer D. Kimball, Jagabandhu Das, Edwin J. Iwanowicz, Wen-Ching Han
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Patent number: 5534626Abstract: Synthetic intermediates of 1-arylethyl-3-substituted piperidines.Type: GrantFiled: January 4, 1995Date of Patent: July 9, 1996Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross, Robert M. Wallis
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Patent number: 5532232Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.Type: GrantFiled: November 22, 1994Date of Patent: July 2, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Paul Hadvary, Kurt Hilpert, Klaus Muller, Ludvik Labler, Gerard Schmid, Thomas B. Tschopp, Hans P. Wessel, Beat Wirz
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Patent number: 5512584Abstract: Compounds of the formula ##STR1## where A-B-D, R.sup.1, R.sup.2 and R.sup.3 have the meanings stated in the description, and their preparation are described. The compounds are suitable for controlling diseases.Type: GrantFiled: November 1, 1994Date of Patent: April 30, 1996Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Liliane Unger, Hans P. Hofmann, Hans-Juergen Teschendorf, Berthold Behl, Rudolf Binder
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Patent number: 5486614Abstract: This invention relates to intermediates, and processes thereto, for the preparation of tetrahydropyrido[2,3-d]pyrimidines which are useful for the treatment of susceptable neoplasms. The intermediates have the following formula II; ##STR1## wherein the R, R.sup.1 and A groups are as defined in the specification.Type: GrantFiled: May 30, 1995Date of Patent: January 23, 1996Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Thomas M. Wilson