Plural -c(=x)- Groups Bonded Directly To The Piperazine Ring Patents (Class 544/387)
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Patent number: 7094895Abstract: The present invention relates to compounds of the formula wherein R1 and R2 are independently hydrogen, C1–C4 alkyl, C1–C4 substituted alkyl, C1–C4 alkoxy, C1–C4 substituted alkoxy, C1–C4 acyl, halogen, cyano, nitro, amino, alkylamino, or dialkylamino; R3, R4, R5, R6, R7, and R8 are independently CH or nitrogen; R9 is hydrogen or methyl; R10 is C?O or (CH2)n; where n is 0, 1, 2, 3, or 4; R11 and R12 are independently nitrogen or CH; X1 and X2 are independently hydrogen, deuterium, tritium or halogen; and X3 is N; and their pharmaceutically acceptable salts; compositions thereof. Methods of preparing the compounds are also described. The compounds are useful in the treatment of diseases in mammals that are mediated by the action of the P2X7 receptor.Type: GrantFiled: December 23, 2002Date of Patent: August 22, 2006Assignee: King Pharmaceuticals Research & Development, Inc.Inventors: Pier Giovanni Baraldi, Pier A. Borea
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Patent number: 7026323Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: September 22, 2004Date of Patent: April 11, 2006Assignee: Schering AktiengesellschaftInventors: Judi A. Bryant, Brad O. Buckman, Imadul Islam, Raju Mohan, Michael M. Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan
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Patent number: 6872825Abstract: The subject invention involves compounds having structure (I), wherein: (a) R1 is hydrogen or alkyl; and R2 is selected from hydrogen, alkyl, aryl, heterocyclyl, carboxy and its esters and amides; or R1 and R2 are attached and are together alkylene or heteroalkylene; (b) R4 is selected from aryl, heteroaryl, and ?,?-unsaturated conjugated aryl or heteroaryl; and (c) R5 is selected from hydrogen, alkyl, aryl, and heterocyclyl; and an optical isomer, diesteriomer, or enantiomer thereof; a salt, hydrate, ester, amide or imide thereof. The subject invention also includes libraries of such compounds, and processes for making the subject compounds and libraries.Type: GrantFiled: December 20, 2000Date of Patent: March 29, 2005Assignee: The Procter & Gamble CompanyInventors: Adam Golebiowski, Sean Rees Klopfenstein
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Patent number: 6858599Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.Type: GrantFiled: December 27, 2001Date of Patent: February 22, 2005Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
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Publication number: 20040259804Abstract: This invention is directed to novel (substituted) acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: ApplicationFiled: July 20, 2001Publication date: December 23, 2004Inventor: Donald S. Karanewsky
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Patent number: 6818637Abstract: The invention concerns novel derivatives of formula (I) wherein: R1 represents the stereoisomeric forms of the chain —(CHOH)3—CH2—O—COR (II) and either R2 represents a hydrogen atom and R3 represents the stereoisomeric forms of the chain —CH2—(CHOH)2—CH2—O—COR (III) or R2 represents the stereoisomeric forms of the chains —(CHOH)3—CH2—O—COR (II) or —CH2—(CHOH)2—CH2—O—COR (III) and R3 represents a hydrogen atom and R represents —(Alk)1—(Cycloalk) radical; i is equal to 0 or 1; Alk represents and alkyl radical, Cycloalk represents a cycloalkyl radical, and their salts with a inorganic or organic acid, their preparation and the medicines containing as active principle at least a product of general formula (I) or its salts with a inorganic or organic acid.Type: GrantFiled: July 11, 2001Date of Patent: November 16, 2004Assignee: Aventis Pharma SAInventors: Herve Bouchard, Alain Commercon
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Patent number: 6809202Abstract: The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl gorup and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.Type: GrantFiled: June 6, 2002Date of Patent: October 26, 2004Assignee: Torrey Pines Institute for Molecular StudiesInventors: Adel Nefzi, John M. Ostresh, Richard A. Houghten
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Publication number: 20040157836Abstract: Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.Type: ApplicationFiled: September 23, 2003Publication date: August 12, 2004Inventors: Kenneth M. Comess, Scott A. Erickson, Jack Henkin, Douglas M. Kalvin, Megumi Kawai, Ki H. Kim, Nwe Y. BaMaung, Chang Hoon Park, George S. Sheppard, Anil Vasudevan, Jieyi Wang, David M. Barnes, Steve D. Fidanze, Lawrence Kolaczkowski, Robert A. Mantei, David C. Park, William J. Sanders, Jason S. Tedrow, Gary T. Wang
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Publication number: 20040106794Abstract: There are disclosed compounds of the formula 1Type: ApplicationFiled: September 11, 2002Publication date: June 3, 2004Applicant: Schering CorporationInventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, Laura L. Rokosz
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Patent number: 6635786Abstract: Symmetrically disubstituted aromatic compounds and pharmaceutical compositions containing such compounds that inhibit and/or modulate the activity of poly(ADP-ribose) glycohydrolase, also known as PARG, are described. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.Type: GrantFiled: April 10, 2001Date of Patent: October 21, 2003Assignee: Guilford Pharmaceuticals, Inc.Inventors: Jia-He Li, Dana Victor Ferraris, Paul W. Kletzly, Weixing Li, Eric Yanjun Wang, Amy D. Xing, Weizheng Xu, Jie Zhang
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Patent number: 6608061Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.Type: GrantFiled: February 14, 2000Date of Patent: August 19, 2003Assignees: Kyoma Hakko Kogyo Co., Ltd., Fuji Photo Film Co., Ltd.Inventors: Yoshiyuki Yonetani, Takeshi Takahashi, Yuko Kanda, Tamio Mizukami, Tatsuya Tamaoki, Shun-ichi Ikeda, Masanobu Takashima, Naoki Asanuma, Tadashi Inaba, Hiroshi Takeuchi, Hiroshi Kawamoto, Yoshihisa Tsukada, Masato Satomura, Hiroshi Kitaguchi
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Publication number: 20030055052Abstract: The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP&agr;), said prodrug having a cleavage site which is recognised by FAP&agr;, and said drug being cytotoxic or cytostatic under physiological conditions.Type: ApplicationFiled: November 9, 2001Publication date: March 20, 2003Inventors: Stefan Peters, Dietmar Leipert, John Edward Park, Martin Lenter, Pilar Garin-Chesa
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Patent number: 6534509Abstract: This invention is directed to acyl piperazine derivatives, for example, of the following formula (1a): wherein R1a, R2, R3, R4, R5, and R6are descried herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmacetutical compostions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.Type: GrantFiled: November 15, 2000Date of Patent: March 18, 2003Assignee: Schering AktiengesellschaftInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
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Patent number: 6531476Abstract: The invention concerns the use of a piperazine derivative of formula (I) wherein: A and B=C═O, C═S or CR7R8 with R7=H, methyl, cyano, cyanomethyl, CO2CH3 or (C═O)CH3 and R8=H or phenyl; R1 to R6=H, OH, or C1-C5 alkoxy; X represents: either C═O, O(C═O), O(C═S), O(SO2), NH(C═O), NH(C═S), NH(SO2), S(C═O) or S(C═S), then Y=NR9R10, CR9R10R11 in which R9, R10 and R11=H, C1-C5 alkyl, C2-C5 alkenyl, or C2-C5 alkynyl or Y=nitrogenous heterocycle comprising 5 to 10 atoms; or X represents O, S, O(C═O)O, NH(C═O)O, or S(C═O)O, then Y=CR9R10R11 with R9, R10, R11 as above; or one of its pharmaceutically acceptable salts for preparing a medicine inhibiting HIV. The invention is useful for treating HIV infection.Type: GrantFiled: March 20, 2001Date of Patent: March 11, 2003Assignees: Universite Paris 7 - Denis Diderot, Commissariat a l'Energie AtomiqueInventors: Francoise Heymans, Nathalie Dereuddre-Bosquet, Jean-Jacques Godfroid, Aazdine Lamouri, Pascal Clayette, Marc Martin
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Patent number: 6521619Abstract: The present invention relates to novel cyclopropane-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: GrantFiled: June 25, 2001Date of Patent: February 18, 2003Assignees: Icos Corporation, Abbott LaboratoriesInventors: James T. Link, Bryan K. Sorensen
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Patent number: 6492368Abstract: Novel compounds of the formula I in which X, Y, R1, R2 and R3 are as defined in Patent Claim 1 are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.Type: GrantFiled: March 31, 2000Date of Patent: December 10, 2002Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Hanns Wurziger, Guido Melzer, Horst Juraszyk, Sabine Bernotat-Danielowski
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Patent number: 6441172Abstract: The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl group and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.Type: GrantFiled: May 12, 1999Date of Patent: August 27, 2002Assignee: Torrey Pines Institute for Molecular StudiesInventors: Adel Nefzi, John M. Ostresh, Richard A. Houghten
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Publication number: 20020107253Abstract: The present invention relates to a novel 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 and D4 receptors represented by the following Formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent, 1Type: ApplicationFiled: April 20, 2001Publication date: August 8, 2002Inventors: Hun Yeong Koh, Kyung IL Choi, Yong Seo Cho, Ae Nim Pae, Jae Yang Kong, Dae Young Jeong, Sun Ho Jung, Ji Young Jung, Hee-Yoon Lee
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Patent number: 6399613Abstract: The invention concerns pyrazine derivatives of formula (1) in which a pharmaceutical composition comprising at least one compound of formula: in which R represents a nitrogen atom, R1 and R3 each represent the same radical selected from the group consisting of —CO—NR5R6, —CO—N(CH(CH2OH)2)2, —CO—N(CH2OH)2, —CO—N(CH2—CH(CH2OH)2)2, —CO—N(CH2—(CHOH)n—CH2OH)2 in which n is equal to 0, 1, 2, 3 or 4, —CH2—O—R6, —NR5—CO—R6, —CH2—NR5R6, —CH2—N(CH2OH)2, —CH2—N(CH2—(CHOH)y—CH2OH)2 in which y is equal to 0, 1, 2, 3 or 4, —CH2—N(CH(CH2OH)2)2 and —CH2—N(CH2—CH(CH2OH)2)2 and R2 and R4 each represents a hydrogen atom, R5 represents a hydrogen atom or an alkyl radical, R6 represents a radical —CH2—(CHOH)m—CH2OH in which m is equal to 0, 1, 2, 3 or 4, -alk-O-alk-CH2OH, -alk-O-alk, —CH(CH2OH)2,Type: GrantFiled: January 14, 2000Date of Patent: June 4, 2002Assignee: Aventis Pharma S.A.Inventors: Georges Bashiardes, Jean-Christophe Carry, Michel Evers, Bruno Filoche, Serge Mignani
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Publication number: 20020049316Abstract: The present invention provides compounds of formula (I) which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia or malignancy; and metabolic bone disease therewith.Type: ApplicationFiled: December 17, 2001Publication date: April 25, 2002Inventors: Stacie Marie Halbert, Evelyne Michaud, Scott Kevin Thompson, Daniel Frank Veber
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Patent number: 6344466Abstract: The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NH, L is —O— or —SO2—, and R1-R4, R9-R19, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal.Type: GrantFiled: February 28, 2001Date of Patent: February 5, 2002Assignee: 3-Dimensional Pharmaceuticals Inc.Inventors: Richard M. Soll, Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Patent number: 6340682Abstract: The present invention provides diamide derivatives represented by the following general formula (1): wherein A is a phenyl group or the like, which may be substituted, B is —CH═CH—, —C═C—, —(CH═CH)2—, —C≡C—CH═CH—, —CH═CH—C≡C—, phenylene or the like, and W is or and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.Type: GrantFiled: February 23, 1999Date of Patent: January 22, 2002Assignee: Kowa Co., Ltd.Inventors: Hiroyuki Ishiwata, Mototsugu Kabeya, Hiromichi Shigyo, Masami Shiratsuchi, Yukio Hattori, Hiroshi Nakao, Takao Nagoya, Seiichi Sato, Soichi Oda, Makoto Suda, Manabu Shibasaki
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Publication number: 20010036942Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: ApplicationFiled: April 26, 2001Publication date: November 1, 2001Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
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Patent number: 6303611Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formula having the structure: wherein R1, R2, and X Y, Z, Ar and n are as described in the specification.Type: GrantFiled: September 9, 1998Date of Patent: October 16, 2001Assignee: Adolor CorporationInventors: Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
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Patent number: 6143893Abstract: The compound of formula is useful as chain extender in the preparation of polymers, in particular of linear and cross-linkable, heparinizable, biocompatible polymers.Type: GrantFiled: May 12, 1999Date of Patent: November 7, 2000Assignee: Tecnobiomedica S.p.A.Inventor: Maria Cristina Tanzi
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Patent number: 6057323Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compound of formula I, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X; and ArY, Z and n are as described in the specification.Type: GrantFiled: October 30, 1998Date of Patent: May 2, 2000Assignee: Adolor CorporationInventors: Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
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Patent number: 6022873Abstract: Compounds of formula (I) ##STR1## wherein n, V, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are matrix metalloproteinase inhibitors.Type: GrantFiled: July 23, 1998Date of Patent: February 8, 2000Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Fionna Mitchell Martin, Andrew Miller, Richard Simon Todd, Mark Whittaker
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Patent number: 6001835Abstract: 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 the farnesylation of the oncogene protein Ras.Type: GrantFiled: March 25, 1997Date of Patent: December 14, 1999Assignee: Merck & Co., Inc.Inventors: Christopher J. Dinsmore, Theresa M. Williams
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Patent number: 5977114Abstract: The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R.sup.1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group,x represents a group of formula ##STR2## R.sup.2 and R.sup.3 independently of one another represent hydrogen; cycloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substituted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, orR.sup.2 and R.sup.3 together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl,R.sup.4 represents hydrogen, lower alkyl or lower alkoxy,R.sup.Type: GrantFiled: November 10, 1997Date of Patent: November 2, 1999Assignee: LG Chemical Ltd.Inventors: Yeong Soo Oh, Sang Soo Kim, Sang Yeul Hwang, Mi Kyung Yun, Seong Ryul Hwang, Seong Won Hong, Yong Hee Lee, Yi Na Jeong, Koo Lee, You Seung Shin
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Patent number: 5929077Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected b ##STR1## its enantiomers, diastereomers, and pharmaceutically acceptable salts and solvates thereof.Type: GrantFiled: October 17, 1997Date of Patent: July 27, 1999Inventor: Katerina Leftheris
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Patent number: 5892039Abstract: The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.Type: GrantFiled: August 30, 1996Date of Patent: April 6, 1999Assignee: Schering CorporationInventors: Ho-Jane Shue, Neng-Yang Shih, David J. Blythin, Xiao Chen, John J. Piwinski, Kevin D. McCormick
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Patent number: 5886181Abstract: Optically active piperazine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are inter alia hydrogen, alkyl or acyl and X is alkoxy or a (substituted) amino group, are prepared by asymmetric hydrogenation of the corresponding 1,4,5,6-tetrahydropyrazines, catalyzed by optically active rhodium, ruthenium or iridium complexes. The compounds of the Formula 1 are intermediates for the preparation of pharmaceutical active ingredients, for example, HIV protease inhibitors.Type: GrantFiled: May 23, 1996Date of Patent: March 23, 1999Assignee: Lonza, Ltd.Inventors: Rudolf Fuchs, Jean-Paul Roduit
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Patent number: 5869554Abstract: Weatherable polycarbonate compositions (formulations or blends) comprise at least one of a piperazinone and piperazine dione based HALS, and at least one of a benzotriazole, benzophenone, triazine, oxanilide, and cyanoacrylate based UVA. The combination of these HALS and UVA exhibits a synergy that results in enhanced protection of the polycarbonate compositions by imparting photostability to the polycarbonate formulations, thereby reducing yellowing or other forms of light induced degradation.Type: GrantFiled: September 2, 1997Date of Patent: February 9, 1999Assignee: General Electric CompanyInventors: James Edward Pickett, Randall Lee Carter
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Patent number: 5756504Abstract: Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl, --CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkyl-carbonyl, --Z--R.sup.13, ##STR3## or substituted C.sub.Type: GrantFiled: September 23, 1996Date of Patent: May 26, 1998Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Ben E. Evans, J. Christopher Culberson, Kevin F. Gilbert, Kenneth E. Rittle, Peter D. Williams
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Patent number: 5756742Abstract: Polymerizable compounds based on N-acylamido-piperazines are provided. Such compounds have the formula: ##STR1## wherein: a, b, c and d are independently 0 or 1 and the sum of a, b, c and d is at least 3.R.sup.1, R.sup.2, and R.sup.3 are hydrogen and/or lower alkyl,B.sup.1, B.sup.2, B.sup.3, and B.sup.4 are independently carbonyl, sulfonyl, amide, or carboxyl;m, n, x, and y are independently one or zero;R.sup.23 is a group selected from, substituted and unsubstituted phenyl and phenonyl.These compounds are particularly useful as polymerizable monomers in radiation curable coatings. The compound preferably has at least one group ##STR2## substituted on R.sup.23 wherein M is H or a counterion to the carboxyl group which can be present in place of a ##STR3## group.Type: GrantFiled: December 22, 1995Date of Patent: May 26, 1998Assignee: Henkel CorporationInventor: Paul E. Share
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Patent number: 5756505Abstract: An N-acylpiperazine derivative or a salt thereof in accordance with the present invention is represented by the following formula 1: ##STR1## wherein R.sub.1 represents a lower alkyl, hydroxy lower alkyl, lower acyl, or arylcarbonyloxy lower alkyl group;R.sub.2 represents hydrogen atom or a lower alkyl, lower alkoxy, lower alkenyl, amino, or nitro group;R.sub.3 and R.sub.4, which are identical to or different from each other, represent hydrogen atoms, halogen atoms, or cyano, nitro, lower alkyl, or lower alkoxy groups; andn represents 0 or 1.The N-acylpiperazine derivative has anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulsers.Type: GrantFiled: April 1, 1996Date of Patent: May 26, 1998Assignee: Shiseido Co., Ltd.Inventors: Chikao Nishino, Fumitaka Sato, Tomohiro Uetake, Hirotada Fukunishi, Nao Kojima, Koji Kobayashi
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Patent number: 5736539Abstract: 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 the farnesylation of the oncogene protein Ras.Type: GrantFiled: November 16, 1995Date of Patent: April 7, 1998Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, Theresa M. Williams
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Patent number: 5670505Abstract: A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl;Y is a direct bond or lower alkylene; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein. The compounds are advantageously used as Tachykinin antagonists in the treatment of respiratory diseases, ophthalmic diseases and inflammatory diseases, for example.Type: GrantFiled: November 28, 1994Date of Patent: September 23, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Daijiro Hagiwara, Takashi Manabe, Nobukiyo Konishi, Shinji Shigenaga, Kenji Murano, Hiroshi Matsuda, Hiroshi Miyake
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Patent number: 5654465Abstract: This invention provides a process for producing cyanocinnamamides. More particularly, the invention provides a process for condensing an cyanoacetamide with a carbonyl-containing compound to produce cyanocinnamamides in good yield.Type: GrantFiled: October 15, 1996Date of Patent: August 5, 1997Assignee: AlliedSignal Inc.Inventors: Zhenrong Qian, Heng Su, Chempolil Thomas Mathew
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Patent number: 5650412Abstract: Compounds of formula ##STR1## are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 26, 1995Date of Patent: July 22, 1997Assignee: Merck & Co., Inc.Inventors: Byeong Moon Kim, Joseph P. Vacca
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Patent number: 5646151Abstract: Compounds, compositions and method of treating hyperalgesia comprising a compound of formula I, II, III and IV as defined in the specification.Type: GrantFiled: March 8, 1996Date of Patent: July 8, 1997Assignee: Adolor CorporationInventors: Lawrence I. Kruse, Virendra Kumar, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Alan L. Maycock
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Patent number: 5612479Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.Type: GrantFiled: August 17, 1994Date of Patent: March 18, 1997Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5607937Abstract: The present invention relates to D,L-, L- and D-phenylalanine piperazides of formula (I) defined in claim 1 that inhibit blood coagulation, and thrombin and/or trypsin, respectively. The compounds are extraordinarily absorbable after oral, intraduodenal and in particular rectal administration and show only a low toxicity.Type: GrantFiled: January 5, 1995Date of Patent: March 4, 1997Assignee: Pentapharm AGInventors: Joerg Stuerzebecher, Helmut Vieweg, Peter Wikstroem, Christoph Adler
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Patent number: 5556852Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 is each --R.sup.5, --CH.dbd.CH--R.sup.5 or --C.tbd.C--R.sup.5, wherein R.sup.5 is optionally substituted aryl or aromatic heterocyclic; R.sup.3 is hydrogen, alkyl, cyano or --R.sup.5 ; X is oxygen or sulfur A is 1,4-piperazin-1,4-diyl or a 1,4-homopiperazin-1,4-diyl; B' is alkylene, carbonyl, thiocarbonyl, sulfinyl or sulfonyl: and R.sup.4 is optionally substituted phenyl and pharmaceutically acceptable salts thereof have valuable PAF antagonist activity.Type: GrantFiled: October 7, 1994Date of Patent: September 17, 1996Assignee: Sankyo Company, LimitedInventors: Norio Nakamura, Nobuyuki Ohkawa, Takeshi Oshima, Masaaki Miyamoto, Yasuteru Iijima
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Patent number: 5491201Abstract: Novel cyclic imino ether compositions containing one or more mesogenic moieties, when polymerized, result in products having improved properties.Type: GrantFiled: February 16, 1995Date of Patent: February 13, 1996Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5432178Abstract: Amidinophenol derivatives of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are (i) H, (ii) C1-4 alkyl, (iii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO.sub.2, (vii) benzoyl, (viii) COOR.sup.4 (in which R.sup.4 is C1-3 alkyl); A is bond, C1-4 alkylene, --C(R.sup.5).dbd.C(R.sup.6)-- (in which R.sup.5 and R.sup.6 are H or C1-4 alkyl; R.sup.3 is (i) CON(R.sup.7)(R.sup.8), (ii) CON(R.sup.9)--CH(R.sup.7)(R.sup.8) or (iii) ##STR2## in which ##STR3## is 4-7 membered, mono-cyclic hetero ring containing 1 or 2 N atom; R.sup.10 is H, C7-10 phenylalkyl or COOR.sup.13 (in which R.sup.13 is H, C1-4 alkyl or C7-10 phenylalkyl)); with the proviso that (i) both R.sup.7 and R.sup.8 do not represent hydrogen at the same time, and (ii) when at least one group in R.sup.7, R.sup.8 and R.sup.9 represents the group containing t-butyl ester, the other groups do not represent tile group containing carboxy; or an acid-addition salt thereof, have inhibitory activities on PLA.sub.Type: GrantFiled: September 16, 1993Date of Patent: July 11, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Masanori Kawamura, Tsumoru Miyamoto
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Patent number: 5414121Abstract: Adducts containing mesogenic or rodlike moieties are prepared by reacting (1) at least one compound containing an average of more than one vicinal epoxide group per molecule with (2) at least one compound containing an average of more than one reactive hydrogen atom per molecule; with the proviso that at least one member of components (1) and (2) contains a mesogenic or rodlike moiety. These compounds are useful as curing agents for epoxy resins.Type: GrantFiled: September 8, 1993Date of Patent: May 9, 1995Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5389680Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds, for example, 3,4,4-trifluoro-3-butene-1-amine or 3,4,4-trifluoro-3-butenoic acid, are particularly useful for systemic control of pests. Novel method and intermediates for the preparation of 3,4,4-trifluoro-3-butene-1-amine are also provided.Type: GrantFiled: October 18, 1993Date of Patent: February 14, 1995Assignee: Monsanto CompanyInventor: Peter G. Ruminski
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Patent number: 5364850Abstract: The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: September 24, 1993Date of Patent: November 15, 1994Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov, Robert K. Husa
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Patent number: 5344830Abstract: Diacylpiperazines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: December 10, 1992Date of Patent: September 6, 1994Assignee: Merck & Co., Inc.Inventors: Sander G. Mills, Richard J. Budhu, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Mu T. Wu