Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Pyridine Or Partially Hydrogenated Pyridine Ring Patents (Class 546/262)
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Patent number: 6458813Abstract: Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: August 17, 2001Date of Patent: October 1, 2002Assignee: Amgen Inc.Inventors: Nathan B. Mantlo, Stephen T. Schlachter, John A. Josey
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Patent number: 6458957Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.Type: GrantFiled: July 12, 2000Date of Patent: October 1, 2002Assignee: Geneva Pharmaceuticals, Inc.Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
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Publication number: 20020111494Abstract: Dihydropyridine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel. They are used as remedies for various diseases relating to the N-type calcium channel such as encephalopathies caused by the ischemia in the acute phase after the onset of cerebral infarction, cerebral hemorrhage or the like, Alzheimer's disease, etc.Type: ApplicationFiled: December 13, 2001Publication date: August 15, 2002Applicant: AJINOMOTO CO., INC.Inventors: Hisayuki Uneyama, Seiji Niwa, Tomoyuki Onishi
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3-Substituted tetrahydropyridopyrimidinone derivatives, method for producing the same, and their use
Patent number: 6414157Abstract: 3-substituted tetrahydropyridopyrimidinone derivatives of the formula (I) wherein the radicals have the meanings given in the Description, to a method for producing said derivatives and, to their use for producing active ingredients for drugs.Type: GrantFiled: April 10, 2000Date of Patent: July 2, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Uta Dullweber, Dorothea Starck, Gerd Steiner, Alfred Bach, Franz Emling, Xavier Garcia-Ladona, Hans-Jürgen Teschendorf, Karsten Wicke -
Patent number: 6399606Abstract: Neuroprotective agents are disclosed having the following structure: wherein R1, R2, R3, R4 and R5 are as defined herein. Such compounds have utility in the treatment of conditions which benefit from administration of neuroprotective agents generally, including treatment of central and peripheral nervous condition as well as for promoting nerve cell differentiation. Methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more of the compounds of this invention.Type: GrantFiled: November 27, 2000Date of Patent: June 4, 2002Assignee: Nippon Kayaku Co., Ltd.Inventors: Moorthy S. S. Palanki, Shripad S. Bhagwat, Hiroshi Sato, Paul E. Erdman, Mary Doubleday
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Publication number: 20020026055Abstract: Compounds of the formula 1Type: ApplicationFiled: March 12, 2001Publication date: February 28, 2002Applicant: American Home Products CorporationInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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Patent number: 6329362Abstract: Compounds of formula (1) are described: wherein L1 is a covalent bond or a linker atom or group; R is a carboxylic acid (—CO2H) or a derivative threof; R6 and R7 which may be the same or different is each an atom or group —L2(Alk2)tL3R12 in which L2, L3, Alk2 and t are as previously defined and R12 is a hydrogen or halogen atom or an —OR9, —NR9R10, —NO2, —CN, —CO2R9, —CONR9R10, —COR9, —N(R9)COR10, —N(R9)CSR10, —SO2N(R9)(R10), —N(R9)SO2R9, —N(R9)CON(R10)(R11), —N(R9)CSN(R10)(R11), —N(R9)SO2N(R10)(R11), or an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group provided that R6 and R7 are not both hydrogen atoms and when R7 is a hydrogen atom then R4 and R5 is each a hydrogen or halogen atom or an alkyl, alkoxy or nitro group; and the salts, solvates, hydrates and N-oxides thereof, for use in modulating cell adhesion.Type: GrantFiled: March 16, 1999Date of Patent: December 11, 2001Assignee: Celltech Therapeutics LimitedInventors: Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
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Patent number: 6313148Abstract: Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a —CH(R3)N(R2)B—R1 and —OD groups positioned in a 1,2 relationship to one another on ring carbon atoms. The 3-position ring-atom is not substituted. B is an optionally-substituted pyridyl ring and the group R1 is positioned on B in a 1,3 or 1,4 relationship with the —CH(R3)N(R2)B- linking group. R1, R2 and R3 and D can be a number of different organic or halogen moieties. N-oxides of —NR2 and S-oxides of sulphur containing rings are disclosed as are processes for the preparation of the compounds, intermediates in their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents.Type: GrantFiled: April 3, 2000Date of Patent: November 6, 2001Assignee: Zeneca LimitedInventor: Gloria Anne Breault
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Patent number: 6225316Abstract: The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 may be together —CH═CH—CH═CH—; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, —N(R5)2, —N(R5)S(O)2-lower alkyl, —N(R5)C(O)R5 or a cyclic tertiary amine of the group R5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, —N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, —CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is —C(O)N(R5)—, —(CH2)mO—, —(CH2)mN(R5)—, —N(R5)C(O)—, or —N(R5)(CH2)m—; n is 0-4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: February 16, 2000Date of Patent: May 1, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
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Patent number: 6197793Abstract: Novel compounds of general formula (I) which have homoregulatory activities and can be used to stimulate haematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.Type: GrantFiled: December 4, 1998Date of Patent: March 6, 2001Assignees: SmithKline Beecham Corporation, Nycomed Austria GmbHInventors: Pradip Kumar Bhatnagar, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
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Patent number: 6197792Abstract: Compounds of the general formula (1) wherein: ═W— is ═N—; Y is halogen or an alkyl or —XRa group; X is —O—, —S(O)m— or —N(Ra)—, where m is zero or an integer 1 or 2; Ra is hydrogen or an optionally substituted alkyl group; R2 is an optionally substituted cycloalkyl or cycloalkenyl group; R3 is R13 or —L1R13, where R13 is a halogen atom, an optionally substituted straight or branched chain C2-6alkenyl group or an optionally substituted C6-12 monocyclic or bicyclic aryl group and L1 is an optionally substituted straight or branched chain C1-6alkylene, C2-6alkenylene or C2-6alkynylene group; R4 is a hydrogen atom or a group —(CH2)nAr where Ar is an optionally substituted monocyclic aryl group and n is zero or an integer 1, 2 or 3; R5 is hydrogen; R6 is an optionally substituted 2-, 3- or 4-pyridyl group; and each of R7 and R8 is independently hydrogen or an optionally substituted straight or branched alkyl group.Type: GrantFiled: March 26, 1998Date of Patent: March 6, 2001Assignee: Celltech Therapeutics LimitedInventors: Rikki Peter Alexander, Graham John Warrellow
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Patent number: 6191146Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.Type: GrantFiled: April 1, 1999Date of Patent: February 20, 2001Assignees: SmithKline Beecham Corporation, Nycomed Austria GmbHInventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding, James Francis Callahan, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
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Patent number: 6187926Abstract: The present invention relates to a process for producing a 4-quinolone derivative, comprising allowing an o-aminoacetophenone derivative to react with a formic acid in an aprotic solvent in the presence of a suitable base, and adding a protic solvent to the reaction mixture. This is a simple process for producing 4-quinolone derivatives, applicable to large-scale commercial production.Type: GrantFiled: October 18, 1999Date of Patent: February 13, 2001Assignee: Kirin Beer Kabushiki KaishaInventors: Tatsushi Osawa, Kazuo Kubo, Hideko Murooka, Tatsuo Nakajima
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Patent number: 6184237Abstract: Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, suchas pain and diabetes. The inventin encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermedates useful in such processes.Type: GrantFiled: November 1, 1999Date of Patent: February 6, 2001Assignee: Amgen Inc.Inventors: Nathan B. Mantlo, Stephen T. Schlachter, John A. Josey
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Patent number: 6114357Abstract: Novel compounds of general formula (1), which have hemoregulatory activities and can be used to stimulate haematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.Type: GrantFiled: February 9, 1999Date of Patent: September 5, 2000Assignees: SmithKline Beecham Corporation, Nycomed Austria GmbHInventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
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Patent number: 6107309Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.Type: GrantFiled: December 4, 1998Date of Patent: August 22, 2000Assignees: SmithKline Beecham Corporation, Nycomed Austria GmbHInventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding, James Francis Callahan, Johann Hiebl, Michael Hartmann, Peter Kremminger, Franz Rovenszky
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Patent number: 6051584Abstract: Novel compounds of the general formula (I) which have hemoregulatory activities and can be used to stimulate haematopolesis and for the treatment of viral, fungal and bacterial infectious diseases ##STR1##Type: GrantFiled: November 23, 1998Date of Patent: April 18, 2000Assignees: SmithKline Beecham Corporation, Nycomed Austria GmbHInventors: Pradip Kumar Bhatnagar, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
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Patent number: 6051713Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.Type: GrantFiled: December 17, 1998Date of Patent: April 18, 2000Assignee: Allergan Sales, Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6030989Abstract: Novel compounds of general formula (I) which have hemoregulatory activities and can be used to stimulate haematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.Type: GrantFiled: November 23, 1998Date of Patent: February 29, 2000Assignee: SmithKline Beecham CorporationInventors: Pradip Kumar Bhatnagar, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
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Patent number: 6020335Abstract: An (N-(pyridinylmethyl)-heterocyclic)ylideneamine compound of the formula ##STR1## wherein R.sup.3, A, and B are as described below, and its pharmaceutically acceptable salts and prodrugs. Compounds of the formula I and their pharmaceutically acceptable salts and prodrugs are useful in the treatment of addictive disorders, such as the use of tobacco or other nicotine containing products, neurological and mental disorders such as senile dementia of the Alzheimer's type, Parkinson's disease, attentional hyperactivity disorder, anxiety, obesity, Tourette's Syndrome and ulcerative colitis.Type: GrantFiled: November 4, 1997Date of Patent: February 1, 2000Assignee: Pfizer IncInventors: Arthur A. Nagel, Steven W. Goldstein, Stanley Jung, Peter H. Dorff
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Patent number: 6005113Abstract: The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.Type: GrantFiled: May 14, 1997Date of Patent: December 21, 1999Assignee: Molecular Probes, Inc.Inventors: Yexin Wu, Dieter H. Klaubert, Hee Chol Kang, Yu-Zhong Zhang
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Patent number: 6002010Abstract: A process for preparing carboxylic acid derivatives of the formula I ##STR1## where X is OR.sup.2 or NH.sub.2,R.sup.1 is C.sub.1 -C.sub.20 -alkyl, C.sub.l -C.sub.20 -hydroxyalkyl, C.sub.3 -C.sub.12 -cycloalkyl, C.sub.4 -C.sub.12 -alkylcycloalkyl, C.sub.4 -C.sub.12 -cycloalkylalkyl, C.sub.5 -C.sub.20 -alkylcycloalkylalkyl, aryl, C.sub.7 -C.sub.20 -aralkyl, C.sub.7 -C.sub.20 -alkylaryl, a heteroaliphatic or heteroaromatic ring with 5 to 8 carbon atoms andR.sup.2 is C.sub.1 -C.sub.20 -alkyl,from carbonitriles of the formula IIR.sup.1 --C.tbd.N (II),where R.sup.1 has the abovementioned meanings, and alcohols of the formula IIIR.sup.2 --OH (III),where R.sup.2 has the abovementioned meanings, at from 50 to 300.degree. C. under from 0.1 to 350 bar in the presence of a heterogeneous catalyst, wherein the reaction is carried out in liquid phase.Type: GrantFiled: November 10, 1997Date of Patent: December 14, 1999Assignee: BASF AktiengesellschaftInventor: Eberhard Fuchs
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Patent number: 5962479Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.Type: GrantFiled: December 6, 1996Date of Patent: October 5, 1999Assignee: Pfizer Inc.Inventor: Yuhpyng Liang Chen
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Patent number: 5880140Abstract: The present invention is directed to compounds of the formula A which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras: ##STR1## The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: April 1, 1997Date of Patent: March 9, 1999Assignee: Merck & Co., Inc.Inventor: Neville J. Anthony
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Patent number: 5872257Abstract: The present invention provides a chelating agent suitable for forming coordinated complexes with a metal in liquid and supercritical carbon dioxide of covalently bonded (i) a chelating group selected from the group consisting of a dithio carbamate, a thiol group, and a picolyl amine group, (ii) a non-electron withdrawing spacer group selected from (CH.sub.2).sub.x ; and (iii) a CO.sub.2 -soluble functional group selected from (CF.sub.2 CF.sub.2 O).sub.X, (CF.sub.2 O).sub.X, (CF.sub.2).sub.X, and ?CF.sub.2 (CF.sub.3 FO)!.sub.x. X is selected to be greater or equal to 3 and to minimize the electron withdrawing effect of the CO.sub.2 -soluble functional group and to achieve a chelating agent solubility of at least a 10.sup.-3 gm/gm CO.sub.2. A solubility of at least 10.sup.-2 gm/gm CO.sub.2 is attained at a temperature in the range of approximately 0.degree. to 100.degree. C. and a pressure of approximately 500 to 5000 psi.Type: GrantFiled: April 1, 1997Date of Patent: February 16, 1999Assignee: University of PittsburghInventors: Eric J. Beckman, Alan J. Russell
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Patent number: 5814645Abstract: The present invention pertains to new substituted nitrogen heterocycles of general formula (I) ##STR1## in which R.sup.1 and R.sup.2 independently of each other, stand for hydrogen or alkyl,X stands for oxygen, sulfur or an NR.sup.3 group,Y stands for carbon (C or CH) or nitrogen,Z stands for an electron-attracting group,T stands for the remainder of an unsaturated ring system broken possibly by other heteroatoms or heteroatom groups,Q stands for possibly substituted aryl or possibly substituted hetaryl, wherein R.sup.3 stands for hydrogen, alkyl or alkenyl, method for preparing them and their use as pesticides.Type: GrantFiled: August 18, 1997Date of Patent: September 29, 1998Assignee: Bayer AktiengesellschaftInventors: Johannes Kanellakopulos, Rainer Fuchs, Johannes Rudolf Jansen, Michael Schindler, Christoph Erdelen, Wolfgang Leicht, Ulrike Wachendorff-Neumann, Andreas Turberg
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Patent number: 5801175Abstract: Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.Type: GrantFiled: September 13, 1996Date of Patent: September 1, 1998Assignees: Schering Corporation, Pharmacopeia, Inc.Inventors: Adriano Afonso, John J. Baldwin, Ronald J. Doll, Ge Li, Alan K. Mallams, F. George Njoroge, Dinanath F. Rane, John C. Reader, Randall R. Rossman
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Patent number: 5714503Abstract: Treatment of AIDS, inhibition of the replication of HIV and related viruses thereof, and formulations using thiourea derivative compounds or salts thereof is disclosed. Also disclosed are novel thiourea derivative compounds.Type: GrantFiled: May 31, 1995Date of Patent: February 3, 1998Assignee: Medivir ABInventors: John M. Morin, Jr., Robert J. Ternansky, Rolf Noreen, Peter Tomas Lind
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Patent number: 5712294Abstract: A compound selected from those of formula (I): ##STR1## where m is equal to 0 or 1andHet, A, X, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and the ring ##STR2## are defined in the description, and a medicinal product comprising the same for treating an inflammatory disorder.Type: GrantFiled: May 25, 1995Date of Patent: January 27, 1998Assignee: Adir Et CompagnieInventors: Jean-Michel Robert, Odile Rideau, Sylvie Robert-Piessard, Jacqueline Courant, Guillaume Le Baut, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
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Patent number: 5700811Abstract: This invention is directed to compounds having the structure: ##STR1## wherein R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine or thiazoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, and n is an integer from about 4 to about 8. This invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of the compounds of the present invention and a pharmaceutically acceptable carrier.Type: GrantFiled: May 19, 1994Date of Patent: December 23, 1997Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind
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Patent number: 5684198Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.Type: GrantFiled: August 23, 1996Date of Patent: November 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Keith Russell, Cyrus John Ohnmacht, Keith Hopkinson Gibson
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Patent number: 5672708Abstract: N-arylaminoacrylic acid derivatives are obtained in good yields and in high purities when benzoylacetic acid derivatives are reacted with N-arylimino ethers. The products thus prepared are used, in particular, for the preparation of 4-quinolone-3-carboxylic acid derivatives, which have an outstanding bactericidal action.Type: GrantFiled: August 31, 1995Date of Patent: September 30, 1997Assignee: Bayer AktiengesellschaftInventors: Gunter Rauchschwalbe, Bernhard Beitzke, Wolfgang Eymann, Helmut Fiege
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Patent number: 5641887Abstract: The present invention provides a chelating agent suitable for chelating metals metals in liquid or supercritical carbon dioxide. The chelating agent comprises generally a conventional chelating group and a CO.sub.2 -soluble functional group covalently attached to the chelating group. Examples of suitable CO.sub.2 -soluble functional groups include fluorinated polyether groups, silicone groups, fluorinated polyalkyl groups, phosphazene groups and fluorinated polyacrylate groups. The present invention also provides a method of extracting a metal from a matrix containing at least one other material and the metal using such CO.sub.2 -soluble chelating agents.Type: GrantFiled: April 1, 1994Date of Patent: June 24, 1997Assignee: University of PittsburghInventors: Eric J. Beckman, Alan J. Russell
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Patent number: 5631401Abstract: The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful in inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.Type: GrantFiled: January 24, 1995Date of Patent: May 20, 1997Assignee: Abbott LaboratoriesInventors: Herman H. Stein, William R. Baker, Anthony K. L. Fung, Saul H. Rosenberg, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, William J. McClellan, Stephen J. O'Connor, Rajnandan Prasad, Wang Shen, Gerard M. Sullivan
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Patent number: 5614634Abstract: Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,B means an alkylene group with 1-3 C atoms in the chain, a radical ##STR2## or a radical ##STR3## with R.sup.3 meaning a hydrogen atom, a carboxy or methoxycarbonyl group, A means groups ##STR4## --NH--CO--, --CO--NH--, --OCH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --COCH.sub.2 -- or --CHOH--CH.sub.2 --,X means N or CH,D means groups or ##STR5## and . . . . . means a single or double bond, as well as optionally their salts with physiologically harmless bases, process for their production and their pharmaceutical use.Type: GrantFiled: June 5, 1995Date of Patent: March 25, 1997Assignee: Schering AktiengesellschaftInventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
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Patent number: 5580983Abstract: 2-Chloro-5-(N-acyl-aminomethyl)pyridines can be prepared by hydrogenation of 2-chloro-5-cyanopyridine with hydrogen in an acylating agent using a hydrogenation catalyst.Type: GrantFiled: June 27, 1995Date of Patent: December 3, 1996Assignee: Bayer AktiengesellschaftInventor: Helmut Kraus
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Patent number: 5556990Abstract: This invention relates to a class of novel dicarboxy amide derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis-aryl and/or heteroaryl alkyl or cycloalkylamino dicarboxy amides. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.Type: GrantFiled: December 16, 1994Date of Patent: September 17, 1996Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Henry W. Pauls, Yong-Mi Choi, Robert W. Studt, Martin P. Maguire, Alfred P. Spada, Don D. Cha
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Patent number: 5545835Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pylidinedicarboxylic acids.Type: GrantFiled: November 4, 1994Date of Patent: August 13, 1996Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Propenoic acid derivatives diazole propenoic acid compounds which have useful pharmaceutical utility
Patent number: 5541213Abstract: A novel propenoic acid derivative which exhibits adenosine A1 antagonism is defined by the general formula (I): ##STR1## (wherein A represents an aromatic ring; R.sup.1 represents aryl or the like; R.sup.2, R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like; and R.sup.7 and R.sup.8 each represent lower alkyl or the like) or a pharmacologically acceptable salt thereof.Type: GrantFiled: June 10, 1994Date of Patent: July 30, 1996Assignee: Eisai Co., Ltd.Inventors: Masayuki Matsukura, Keizoh Satoh, Naoki Yoneda, Makoto Kaino, Kazutoshi Miyake, Yoshiharu Daiku, Naoya Kishi, Fusayo Yoshida, Kenichi Nomoto, Toshiaki Ogawa, Tadanobu Takamura, Koichi Nose, Mikio Tomimatsu, Masanori Mizuno, Shigeto Negi, Shigeru Souda -
Patent number: 5493063Abstract: This invention provides a process for producing an optically active 1,2-diol derivative by optical resolution. The optically active 1,2-diol derivative of the formula (I) which is capable of utilizing as an intermediate of fungicidal optically-active azole derivatives can be produced by esterifying a 1,2-diol derivative of the formula (I) as a substrate with a carboxylic acid derivative of the formula (II) as a reagent in the presence of a lipase as a catalyst. ##STR1## wherein R.sup.1 is C1-C5 alkyl group, C3-C7 cycloalkyl group or C1-C5 haloalkyl group, R.sup.2 is C1-C3 alkyl group substituted by a phenyl group which may have one or two halogen atoms and/or C1-C4 alkyl groups, C2-C3 alkenyl group substituted by a phenyl group which may have one or two halogen atoms and/or C1-C4 alkyl groups, or C1-C3 alkyl group substituted by a phenoxy group which may have one or two halogen atoms and/or C1-C4 alkyl groups, R.sup.3 is C1-C10 alkyl group or aryl group, and R.sup.Type: GrantFiled: November 21, 1994Date of Patent: February 20, 1996Assignee: Kureha Kagaku Kogyo K.K.Inventors: Eisaku Takahashi, Takashi Kimura, Satoru Kumazawa
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Patent number: 5474999Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.Type: GrantFiled: October 26, 1994Date of Patent: December 12, 1995Assignee: Imperial Chemical Industries PLCInventors: Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
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Patent number: 5439922Abstract: A method for treating anxiety in mammals comprising administering in an effective amount to said mammal an 1-aryl-3-(4-piperidyl)-indole derivative having the general formula: ##STR1## wherein R.sup.1 is H, F, Cl, Br, methyl, methoxy or cyano; and R.sup.3 is H or methyl; or a pharmaceutical acceptable acid addition salt thereof.Type: GrantFiled: December 17, 1992Date of Patent: August 8, 1995Assignee: H. Lundbeck A/SInventors: Jens K. Perregaard, Brenda Costall
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Patent number: 5416117Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 28, 1994Date of Patent: May 16, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5414003Abstract: Pyridinylmethyl-substituted pyridines and pyridones are prepared by reacting pyridine- or pyridone-substituted halogenopyridines with tetrazolylphenylboronic acids. The substances according to the invention can be used as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.Type: GrantFiled: April 29, 1994Date of Patent: May 9, 1995Assignee: Bayer AktiengesellschaftInventors: Peter Fey, Jurgen Dressel, Rudolf Hanko, Walter Hubsch, Thomas Kramer, Ulrich Muller, Matthias Muller-Gliemann, Martin Beuck, Hilmar Bischoff, Stefan Wohlfeil, Dirk Denzer, Stanislav Kazda, Johannes-Peter Stasch, Andreas Knorr, Siegfried Zaiss
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Patent number: 5413997Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5411972Abstract: An arylamide derivative of formula (1), a salt thereof and a therapeutic agent for hyperlipemia which comprises the derivative or salt: ##STR1## wherein Ar represents a group ##STR2## a naphthyl group, a pyridinyl group, a furyl group, a thienyl group, a quinolyl group or an indolyl group; Y represents a group ##STR3## and Q represents --O-- or a single bond, Z represents an alkylene group, and R.sup.4 represents a hydroxyl group, an alkoxy group or a group --NH(CH.sub.2).sub.m COOH, useful for the treatment and prevention of hyperlipemia due to their excellent cholesterol reducing action, triglyceride reducing action and high safety.Type: GrantFiled: November 29, 1993Date of Patent: May 2, 1995Assignee: SS Pharmaceutical Co., Ltd.Inventors: Teruo Komoto, Hiroyuki Hirota, Susumu Sato, Mari Ohtsuka, Hidehiko Koya, Hiroyuki Mizuno, Tadayuki Kuraishi
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Patent number: 5393730Abstract: The invention relates to nicotinic acid hydrazone derivatives of formula I: ##STR1## in which the various symbols are as defined in the description, and their use as herbicides or as intermediates in the synthesis of herbicides.Type: GrantFiled: January 12, 1994Date of Patent: February 28, 1995Assignee: Rhone-Poulenc Agriculture Ltd.Inventor: Philip H. G. Smith
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Patent number: 5378843Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pyridinedicarboxylic acids.Type: GrantFiled: November 22, 1993Date of Patent: January 3, 1995Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Patent number: 5369108Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.Type: GrantFiled: October 4, 1991Date of Patent: November 29, 1994Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of ColumbiaInventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic
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Patent number: 5364873Abstract: The invention relates to pyridine-2,4- and -2,5-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2 and X have the meanings given, a process for the preparation of these compounds and their use, in particular in medicaments for influencing the metabolism of collagen and collagen-like substances or the biosynthesis of C1.sub.q.Type: GrantFiled: April 1, 1993Date of Patent: November 15, 1994Assignee: Hoechst AktiengesellschaftInventors: Martin Bickel, Dietrich Brocks, Harald Burghard, Volkmar Gunzier, Stephan Henke