The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/510)
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Patent number: 5912260Abstract: Described herein are compounds of formula (I) or a pharmaceutically acceptable salt thereof, ##STR1## wherein L is N or C, one of X and Y is --NH--CH.sub.2 --R.sup.2 and the other is the substituent of formula (II). The compounds are potent gastrin and/or CCK antagonists.Type: GrantFiled: December 19, 1996Date of Patent: June 15, 1999Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Nigel Paul Shankley, Robert Antony David Hull, Atul Kotecha, Sonia Patricia Roberts, Elaine Anne Harper
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Patent number: 5886191Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.Type: GrantFiled: August 18, 1997Date of Patent: March 23, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
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Patent number: 5856517Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.1' are independently alkyl, aryl, alkenyl or alkynyl;R.sup.2 and R.sup.2' are independently hydrogen or alkyl;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently are ##STR2## CH.sub.2 OR.sup.10, CHO, CH.sub.2 NR.sup.11 R.sup.12, hydrogen, halogen, cyano, alkyl, hydroxy, alkoxy, aryloxy, haloalkyl, nitro, amino, acylamino, aralkyloxy, monoalkylamino, dialkylamino, alkylthio, alkylsulphinyl or alkylsulphonyl, provided that at least one of R.sup.4, R.sup.5, R.sup.6 or R.sup.7 is cyano, ##STR3## CH.sub.2 OR.sup.10, CH.sub.2 NR.sup.11 R.sup.12, or CHO ; R.sup.8 is alkyl, aralkyl or aryl;R.sup.10 is hydrogen, alkyl, aralkyl or aryl;R.sup.11 and R.sup.Type: GrantFiled: July 24, 1997Date of Patent: January 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Donna Mary Huryn, Dennis Dalton Keith
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Patent number: 5777162Abstract: Described herein are compounds of Formula (XX) and Formula (XXIV), shown below, and processes of making same. ##STR1## wherein p is 0 ##STR2## wherein p is 1, and Y is chlorine or bromine.Type: GrantFiled: November 12, 1996Date of Patent: July 7, 1998Assignee: Zeneca LimitedInventors: Ian Richard Matthews, Christopher Richard Ayles Godfrey, John Martin Clough
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Patent number: 5773618Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 represents halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, cycloalkyl, or cycloalkyloxy; R.sup.2 represents hydrogen or halogen; R.sup.3 represents hydrogen, alkyl, or cycloalkyl; and the dotted line represents a single or double carbon--carbon bond!; and salts thereof have valuable fungicidal activities which make them of considerable value in agriculture and horticulture.Type: GrantFiled: May 14, 1997Date of Patent: June 30, 1998Assignee: Sankyo Company, LimitedInventors: Hideo Takeshiba, Chiaki Imai, Hiroshi Ohta, Shigehiro Kato, Hiroyuki Itoh
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Patent number: 5750564Abstract: Compounds having anti-inflammatory and anti-oxidant activity are disclosed. The compounds are useful in preventing and treating inflammatory disorders through several mechanisms. Methods of treatment employing these properties of the compounds and corresponding pharmaceutical compositions are disclosed.Type: GrantFiled: September 12, 1995Date of Patent: May 12, 1998Inventors: Mark Hellberg, Pete Delgado, Jon C. Nixon
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Patent number: 5747420Abstract: Novel herbicidal tetrazolinone derivatives of the formula ##STR1## and intermediates therefor of the formula ##STR2## wherein R.sup.1 is alkyl substituted by halogen, andR.sup.2 and R.sup.3 each independently is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or substituted phenyl, orR.sup.2 and R.sup.3 together with the N-atom to which they are attached, which may form a 5- or 6-membered heterocyclic ring.Type: GrantFiled: November 3, 1995Date of Patent: May 5, 1998Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Seishi Ito, Kazuhiro Ukawa, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
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Patent number: 5739353Abstract: This invention relates to substituted N-arylindoles, a process for producing them and their use as herbicides. In particular, this invention relates to substituted N-arylindoles of the formula ##STR1## wherein R, R.sup.3, X, Z, n and k are defined herein.Type: GrantFiled: November 1, 1996Date of Patent: April 14, 1998Assignee: Zeneca LimitedInventors: Ferenc M. Pallos, Christopher J. Mathews
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Patent number: 5719144Abstract: Fibrinogen receptor antagonists having the formula ##STR1## where L is L is (CH.sub.2).sub.p, where p is 1 or 2; and Z is --CR.sup.1 .dbd.CR.sup.Type: GrantFiled: February 22, 1995Date of Patent: February 17, 1998Assignee: Merck & Co., Inc.Inventors: George D. Hartman, John H. Hutchinson, Wasyl Halczenko
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Patent number: 5674876Abstract: The present invention provides an antiproliferative p-heteroatom-substituted phenol compound having the structure formula ##STR1## wherein m is 0 to 3, n is 0 to 4 when Het is nitrogen, wherein R is selected from the group consisting of hydrogen, alkyl, arylmethyl and acyl; R.sup.1 is alkyl; R.sup.2 is selected from the group consisting of hydrogen and alkyl; R.sup.3 is selected from the group consisting of alkyl and acyl when Het is nitrogen, R.sup.4 is selected from the group consisting of hydrogen and alkyl; R.sup.5 is selected from the group consisting of hydrogen and alkyl; and R.sup.6 and R.sup.7 are selected from the group consisting of hydrogen, alkyl and R.sup.6 and R.sup.7 together may represent oxygen. Also provided are various methods for the treatment of a pathological cell proliferative disease comprising administering to an animal) a pharmacologically and therapeutically effective dose of a pharmaceutical composition comprising a p-heteroatom-substituted phenols or an analog thereof.Type: GrantFiled: January 20, 1995Date of Patent: October 7, 1997Assignee: Research Development FoundationInventors: John C. Gilbert, Kimberly Kline, Kathiresan Krishnan, Maria Simmons Menchaca, Marian Pinto, Robert G. Sanders
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Patent number: 5639781Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Type: GrantFiled: June 27, 1995Date of Patent: June 17, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
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Patent number: 5624939Abstract: Compounds of formula I ##STR1## wherein the substituents are as defined herein, are disclosed as treatments for disorders linked to CCK and gastrin. Processes for preparing the compounds are also taught.Type: GrantFiled: June 28, 1995Date of Patent: April 29, 1997Assignee: Rhone-Poulenc Rorer, S.A.Inventors: Marc Capet, Marie-Christine Dubroeucq
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Patent number: 5614555Abstract: Amidinophenol derivatives of the formula (I) ##STR1## wherein the various symbols are as defined herein; which have inhibitory activities on PLA.sub.2 and on various proteases such as trypsin, plasmin, thrombin, kallikrein, especially trypsin, and are useful for the prevention and/or the treatment of various inflammatory diseases, allergic diseases, disseminated intravascular coagulation, pancreatitis, severity in pancreatitis and multiple organ failure.Type: GrantFiled: June 5, 1995Date of Patent: March 25, 1997Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Masanori Kawamura, Tsumoru Miyamoto
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Patent number: 5604253Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: May 22, 1995Date of Patent: February 18, 1997Assignee: Merck Frosst Canada, Inc.Inventors: Cheuk K. Lau, Cameron Black, Daniel Guay, Jacques Y. Gauthier, Yves LeBlanc, Patrick Roy, Yves Ducharme, Pierre Hamel
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Patent number: 5599774Abstract: Substituted N-arylindoles, a process for producing them and their use as herbicides. In particular, substituted N-arylindoles of the formula ##STR1## are disclosed in which: R is hydrogen; halogen; nitro; cyano; alkyl; alkoxy; alkenyloxy; alkynyloxy; alkoxyalkyl; carbonylalkoxy; alkyloxyalkoxy; cyanoalkoxy; benzyloxy; alkoxycarbonylalkoxy; alkylcarbonylalkoxy; haloalkyl; hydroxalkyl; formyl; azido; carboxy or its salts; COOalkyl; amino; substituted amino wherein the substituents are alkyl, alkoxy, hydroxy, formyl, alkylcarbonyl, substituted alkylcarbonyl substituted with carboxy or alkoxycarboxy, alkylsulfonyl, haloalkylsulfonyl, aminocarbonyl, (di)alkylaminocarbonyl, alkoxycarbonyl, alkoxyalkyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, amino or (di)alkyl amino; carboxyamido; substituted carboxyamido wherein said substituents can be selected from alkyl, alkylsulfonyl, and haloalkylsulfonyl; sulfonamido wherein the N is substituted with hydrogen and/or alkyl; YR.sup.4 wherein Y is O or S(O).sub.m and R.sup.Type: GrantFiled: December 31, 1992Date of Patent: February 4, 1997Assignee: Imperial Chemical Industries PLCInventors: Ferenc M. Pallos, Christopher J. Mathews
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Patent number: 5583149Abstract: A series of novel serotonergic indolyl derivatives of cycloalkanyl- and cycloalkenyl-amines of Formula I are intended for use in the alleviation of vascular headaches.Type: GrantFiled: August 21, 1995Date of Patent: December 10, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Joseph A. Cipollina, Jonas A. Gylys, Ronald J. Mattson, Charles P. Sloan
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Patent number: 5510379Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.Type: GrantFiled: December 19, 1994Date of Patent: April 23, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5488114Abstract: A labelling color of pentamethine, its intermediate and a method for preparing and using the same to detect methamphetamine with high sensitivity.The invention is exemplified by pentamethine of the following Formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are a C.sub.1-6 alkyl group, and X is an anion.A method for using the labelling color to detect methamphetamine. The method comprises preparing a solution of the labelling color and methamphetamine-antibody in a buffer, measuring its fluorescent intensity at 660 nm in a 600 nm excited state, adding methamphetamine in a buffer to the solution, measuring its fluorescent intensity similarly, and examining the change in fluorescent intensity between both solutions.Type: GrantFiled: September 16, 1994Date of Patent: January 30, 1996Assignee: Matsushita Electric Industrial Co., Ltd.Inventors: Nobuyuki Shigetoh, Jipsei Miyazaki, Hiroshi Nakayama, Keiko Yugawa, Tadayasu Mitsumata
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Patent number: 5468768Abstract: A series of novel serotonergic indolyl derivatives of cycloalkanyl- and cycloalkenyl-amines of Formula I are intended for use in the alleviation of vascular headaches.Type: GrantFiled: January 6, 1994Date of Patent: November 21, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Joseph A. Cipollina, Jonas A. Gylys, Ronald J. Mattson, Charles P. Sloan
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Patent number: 5399714Abstract: The invention relates to a novel process for the preparation of compounds of formula I ##STR1## wherein R is straight-chain C.sub.2 -C.sub.4 alk-1-en-1-yl, and salts thereof, and to a novel starting material and the use thereof.Type: GrantFiled: July 5, 1994Date of Patent: March 21, 1995Assignee: Ciba-Geigy CorporationInventors: Marc Gerspacher, Alfred Sallman
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Patent number: 5395840Abstract: Heterocyclically substituted phenyl-cyclohexanecarboxylic acid derivatives are prepared by reacting appropriate heterocyclic compounds with cyclohexanebenzyl halides.The compounds can be employed as active compounds in medicaments for the treatment of arterial hypertension and atherosclerosis.Type: GrantFiled: February 8, 1994Date of Patent: March 7, 1995Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Jurgen Dressel, Peter Fey, Rudolf H. Hanko, Walter Hubsch, Thomas Kramer, Matthias Muller-Gliemann, Martin Beuck, Stanisiav Kazda, Stefan Wohlfeil, Andreas Knorr, Johannes-Peter Stasch, Siegfried Zaiss
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Patent number: 5391758Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: June 6, 1994Date of Patent: February 21, 1995Assignee: Zeneca, Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 5380722Abstract: Novel indole-carboxamides of the formula ##STR1## and their non-toxic pharmaceutically acceptable acid addition salts having remarkable anti-arrhytmic properties.Type: GrantFiled: May 25, 1993Date of Patent: January 10, 1995Assignee: Roussel-UclafInventors: Francois Clemence, Jacques Guillaume, Gilles Hamon
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Patent number: 5380857Abstract: A process for the production of 7-acylindoles of the general formula: ##STR1## starting from indoline of the formula: ##STR2## Indoline is cyanized in a first stage to 7-cyanoindoline of the formula: ##STR3## The latter is catalytically dehydrogenated in a second stage to 7-cyanindole of the formula: ##STR4## The latter is then acylated in a third stage with an organometallic compound of the formula:R--Q Vinto the end product according to formula I.Type: GrantFiled: June 30, 1993Date of Patent: January 10, 1995Assignee: Lonza Ltd.Inventors: Jean-Paul Roduit, Alain Wellig
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Patent number: 5330986Abstract: This invention relates to indole-7-carboxamide derivatives of the formula ##STR1## where R.sub.1 through R.sub.6 are independently H, loweralkyl, aryl, and aralkyl; and in addition R.sub.3 and R.sub.5 can be joined together to form a piperazine ring of the formula ##STR2## where R.sub.7 is H, loweralkyl, aryl, arylloweralkyl, pyrimidyl; and R.sub.4 and R.sub.5 can be joined together to form a pyrrolidine ring of the formula ##STR3## where R.sub.8 is H, loweralkyl, aryl, arylloweralkyl; X is H, loweralkyl, halogen, NO.sub.2, CF.sub.3, NH.sub.2, and OR.sub.9 ; where R.sub.9 is loweralkyl, arylloweralkyl and n is an integer of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and the optical isomers thereof where such isomers exist.Type: GrantFiled: November 24, 1992Date of Patent: July 19, 1994Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 5280039Abstract: A compound of the formula ##STR1## wherein R is defined herein is useful as an anti-inflammatory agent.Type: GrantFiled: November 4, 1992Date of Patent: January 18, 1994Assignee: Pfizer Inc.Inventor: James F. Eggler
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Patent number: 5248693Abstract: The invention relates to compounds of formula I ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.7 alkyl, or wherein R is the structural element-alk-R.sub.1 in which alk is C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.7 alkylidene or C.sub.3 -C.sub.6 cycloalkylidene and R.sub.1 is hydroxy, C.sub.1 -C.sub.7 alkoxy, phenyl-C.sub.1 -C.sub.7 alkoxy or C.sub.2 -C.sub.7 alkanoyloxy;in free form or in the form of a salt; processes for their preparation, their use, and also pharmaceutical compositions comprising a compound of formula I in free form or in the form of a pharmaceutically acceptable salt.Type: GrantFiled: October 21, 1992Date of Patent: September 28, 1993Assignee: Ciba-Geigy CorporationInventors: Marc Gerspacher, Alfred Sallmann, Rolf Schurter
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Patent number: 5225436Abstract: Certain aryl substituted naphthalene, benzoxepine, benzazepine and henzocycloheptene derivatives are disclosed. The compounds are useful in treating hyperproliferative skin disease, allergic reactions and inflammation.Type: GrantFiled: October 15, 1991Date of Patent: July 6, 1993Assignee: Schering CorporationInventors: Neng-Yang Shih, Pietro Mangiaracina, Michael J. Green, Ashit K. Ganguly
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Patent number: 5219859Abstract: The invention relates to indole derivatives of formula 1, ##STR1## in which: R.sub.1 and R.sub.2 represent H, alkyl, alkenyl, cycloalkyl, N-alkylamino- or N,N-dialkylaminoalkyl, benzyl, pyridylmethyl or phenyl, optionally substituted,R.sub.3 and R.sub.4 represent H, halogen, alkyl, alkoxy, alkylthio, CF.sub.3, NO.sub.2, N-alkylamino or N,N-dialkylamino, benzyl or phenyl, optionally substituted,R.sub.5 represents H, alkyl, cycloalkyl or optionally substituted benzyl,R.sub.6 denotes an alkyl, phenyl or heterocyclic radical, optionally substituted,Z denotes the bivalent radicals --(CH.sub.2).sub.n --C(R.sub.7 R.sub.8)--(CH.sub.2).sub.p --, --CH=CH--C(R.sub.7 R.sub.8)-- in which n=0--2, p=0--2 and n+p.ltoreq.2, R.sub.7 and R.sub.Type: GrantFiled: March 20, 1992Date of Patent: June 15, 1993Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Didier Festal, Denis Descours, Robert Bellemin, Jacques Decerprit
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Patent number: 5210214Abstract: A process for preparing indolenines of the formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are independently of one another hydrogen, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, C.sub.3 -C.sub.8 -cycloalkyl, aryl, C.sub.7 -C.sub.20 -alkylphenyl, C.sub.7 -C.sub.20 -phenalkyl, or R.sup.1 and R.sup.2 or R.sup.1 and R.sup.3 together are an unsubstituted or C.sub.1 -C.sub.12 -alkyl-substituted C.sub.3 -C.sub.8 -alkylene chain,X and Y are independently of one another hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.2 -C.sub.8 -alkoxyalkyl, C.sub.2 -C.sub.8 -alkoxycarbonyl, C.sub.1 -C.sub.4 -alkylsulfonyl, halogen, nitro or cyano,by reacting a 4-methylene-1,3-dioxolan-2-one of the formula II ##STR2## where R.sup.1, R.sup.2 and R.sup.3 are each as defined above, with an aniline of the formula III ##STR3## where X and Y are each as defined above, in the presence of a Lewis acid and in the presence or absence of a halide of main group 1 or 2 of the Periodic Table at from 100.degree.Type: GrantFiled: April 10, 1992Date of Patent: May 11, 1993Assignee: BASF AktiengesellschaftInventors: Klaus Diehl, Martin Fischer, Manfred Dimmler
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Patent number: 5162550Abstract: Bisphthalide lactones of formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently of one another hydrogen, alkyl of at most 12 carbon atoms which is unsubstituted or substituted by halogen, hydroxy, cyano, tetrahydrofuryl or lower alkoxy; or are acyl of 1 to 12 carbon atoms, cycloalkyl of 5 to 10 carbon atoms or unsubstituted aralkyl or aryl, or aralkyl or aryl each substituted by halogen, cyano, nitro, trifluormethyl, lower alkyl, lower alkoxy, lower alkoxycarbonyl, --NX'X"-- or 4--NX'X--"phenylamino, wherein X' and X" are each independently of the other hydrogen, lower alkyl, cyclohexyl, benzyl or phenyl, or the pairs of substituents --NR.sub.1 R.sub.2 and --NR.sub.3 R.sub.4 are each a 5- or 6-membered, preferably saturated, heterocyclic radical, V.sub.1 and V.sub.2 are hydrogen, halogen, lower alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.Type: GrantFiled: August 24, 1990Date of Patent: November 10, 1992Assignee: Ciba-Geigy CorporationInventors: Rudolf Zink, Ian J. Fletcher
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Patent number: 5132319Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: March 28, 1991Date of Patent: July 21, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Yves Girard, Pierre Hamel, Daniel Delorme, Rejean Fortin
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Patent number: 5118697Abstract: Novel cyclic beta-ketoamides which contain an aryl moiety having utility as blood cholesterol lowering agents rendering them useful in the treatment of atherosclerosis.Type: GrantFiled: March 6, 1991Date of Patent: June 2, 1992Assignee: Warner-Lambert CompanyInventors: Corinne E. Augelli-Szafran, Bharat K. Trivedi
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Patent number: 5110986Abstract: This application relates to a process for preparing a N-t-alkyl-1,2-diacylhydrazine by reacting a 1,3,4-oxadiazole with a tertiary alkyl cation precursor in the presence of a strong acid catalyst. Preferably, the 1,3,4-oxadiazole is a 2,5-disubstituted-1,3,4-oxadiazole and more preferably a 2,5-diaryl-1,3,4-oxadiazole. The strong acid catalyst is preferably a sulfur containing acid and more preferably sulfuric acid.Type: GrantFiled: April 26, 1988Date of Patent: May 5, 1992Assignee: Rohm and Haas CompanyInventor: Martha J. Kelly
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Patent number: 5106990Abstract: The present invention relates to a dye represented by formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, each represents a C.sub.1 -C.sub.5 alkyl group or a C.sub.1 -C.sub.5 alkyl group having a substituent selected from the group consisting of a sulfonic group, carboxyl group and hydroxyl group, and Z.sup.1 and Z.sup.2 each represents a group of non-metallic atoms necessary for the formation of a benzo-condensed of naphtho-condensed ring, or a benzo-condensed or naphtho-condensed ring having a substituent selected from the group consisting of a sulfonic group, a carboxyl group, an hydroxyl group, a halogen atom, a cyano group, an amino group and a C.sub.1 -C.sub.5 alkyl group connected to the ring directly or through a divalent connection group, with a proviso that R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, Z.sup.1 and Z.sup.Type: GrantFiled: March 28, 1989Date of Patent: April 21, 1992Assignee: Fuji Photo Film Co., Ltd.Inventors: Shigeru Ohno, Yuji Mihara, Keiichi Adachi
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Patent number: 5097034Abstract: Color formers of the formula ##STR1## in which X.sup.1 denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy or acyloxy,R.sup.1 denotes hydrogen, halogen, alkyl or alkoxy,R.sup.2 denotes hydrogen, alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sup.1 and Y.sup.2, independently of one another, denote alkyl, cycloalkyl or aralkyl,R.sup.2 can form a heterocyclic ring with A in the o-position, in which a benzene ring can be additionally fused onto ring A in the o-/m-position with respect to R.sup.2,R.sup.3 denotes hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl, or R.sup.3 is linked to ring B in the o-position with respect to the nitrogen,Z.sup.1 stands for the remaining members of a partially hydrogenated or completely hydrogenated ring, with the proviso that Z.sup.Type: GrantFiled: May 14, 1991Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventor: Udo Eckstein
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Patent number: 5096917Abstract: Novel trisubstituted indole compounds of formula ##STR1## wherein R is straight-chain C.sub.2 -C.sub.4 alk-1-en-1-yl, and their salts can be used as pharmaceutical active ingredients and can be manufactured in a manner known per se.Type: GrantFiled: April 29, 1991Date of Patent: March 17, 1992Assignee: Ciba-Geigy CorporationInventors: Alfred Sallmann, Willy Meyer
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Patent number: 5097044Abstract: Pyran-containing phthalides of the formula ##STR1## in which R is hydrogen, alkyl which has not more than 12 carbon atoms and is unsubstituted or substituted by halogen, cyano, hydroxyl or lower alkoxy, or is cycloalkyl, phenalkyl or phenyl each of which is unsubstituted or substituted, or an unsubstituted or substituted heterocyclic radical, R' is hydrogen, or R together with R' is C.sub.2 -C.sub.3 alkylene which is unsubstituted or substituted by methyl,X is hydrogen, alkyl having 1 to 12 carbon atoms or a monocyclic or polycyclic aromatic or heteroaromatic radical and the ring A is a benzene or naphthalene ring which is unsubstituted or monosubstituted or polysubstituted by halogen, lower alkyl, lower alkoxy or lower alkoxycarbonyl, and the ring B is an aromatic or heteroaromatic radical which has 6 ring atoms and which can contain an aromatic fused ring, it being possible for both the ring B and the fused ring to be substituted.Type: GrantFiled: September 20, 1990Date of Patent: March 17, 1992Assignee: Ciba-Geigy CorporationInventor: Rox Phaff
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Patent number: 5093351Abstract: Provided are substituted indoles, benzofurans, and benzothiophenes of the formula ##STR1## wherein X, R.sup.2 and R.sup.3 are described in the specification. These compounds are 5-lipoxygenase inhibitors and are useful as antiinflammatory agents.Type: GrantFiled: January 5, 1989Date of Patent: March 3, 1992Assignee: Du Pont Merck Pharmaceutical CompanyInventor: Douglas G. Batt
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Patent number: 5091379Abstract: Topical polyethylene glycol based formulations for the delivery of 2-substituted-1-naphthols and indoles and particularly, 2-phenylmethyl-1-naphthol are provided. Said topical formulations exert excellent localized antiinflammatory activity while demonstrating low levels of skin penetration in vitro and in vivo thereby reducing unwanted side effects and reducing systemic toxicity associated with the active drug compounds.Type: GrantFiled: August 31, 1989Date of Patent: February 25, 1992Assignee: Du Pont Merck Pharmaceutical CompanyInventor: Bruce J. Aungst
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Patent number: 5041460Abstract: This invention provides a series of novel heter-aliphatic carboxamides of formula I in which the group >Z--Y--X< is selected from >C.dbd.CH--N<, >N--CH.dbd.C<, >C.dbd.N--N< and >N--N.dbd.C< and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.Type: GrantFiled: April 12, 1989Date of Patent: August 20, 1991Assignee: ICI Americas Inc.Inventor: Victor G. Matassa
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Patent number: 5021430Abstract: Disclosed are compound of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, or each said grouping substituted by lower alkyl; R and R.sub.o independently represent lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl; A represents methylene; or A represents methylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by aryl-lower alkylthio-lower alkyl, by arylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by aryl-lower alkyloxy-lower alkyl, by aryloxy-lower alkyl, by amino-lower alkyl, by acylamino-lower alkyl, by guanidino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.Type: GrantFiled: June 29, 1987Date of Patent: June 4, 1991Assignee: Ciba-Geigy CorporationInventor: Gary M. Ksander
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Patent number: 4981977Abstract: (2,3,3-Trimethyl-3-H-indol-5-yl)-acetic acid has been synthesized. Additionally, derivatives of (2,3,3-Trimethyl-3-H-indol-5-yl)-acetic acid have been prepared as intermediates for preparation of fluorescent cyanine biolabels. A derived dye, 5.5'-Dicarboxymethyl-3,3,3',3'-tetramethyl-1,1'-diethylindocarboc yanine, is a biolabeling substance with a brilliant red fluorescence.Type: GrantFiled: June 9, 1989Date of Patent: January 1, 1991Assignee: Carnegie-Mellon UniversityInventors: Philip L. Southwick, Alan S. Waggoner
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Patent number: 4963548Abstract: Novel fungicidally active compounds of the formula ##STR1## in which R represents alkyl, cyanoalkyl or in each case optionally substituted alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl or phenylalkyl,R.sup.1 represents the --OR.sup.2 or --NR.sup.3 R.sup.4 groups, andR.sup.3 and R.sup.4 have special special definitions.Type: GrantFiled: May 27, 1988Date of Patent: October 16, 1990Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Wilhelm Brandes, Gerd Hanssler
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Patent number: 4921982Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.Type: GrantFiled: June 14, 1989Date of Patent: May 1, 1990Assignee: Eli Lilly and CompanyInventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
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Patent number: 4866087Abstract: Carboxyalkyl urea compounds and derivatives thereof are disclosed which are useful as angiotensin converting enzyme (ACE) inhibitors and as antihypertensives. These compounds and derivatives are represented by the general formula: ##STR1## An illustrative specie falling within this general formula is:N-(2-carboxy-4-phenylbutyl-N-isopropylaminocarbonyl-L-tryptophan.Type: GrantFiled: June 27, 1983Date of Patent: September 12, 1989Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, David G. Hangauer, Jr., Arthur A. Patchett
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Patent number: 4859692Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: April 16, 1986Date of Patent: August 22, 1989Assignee: ICI Americas Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying Kwong Yee
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Patent number: 4837235Abstract: This invention provides a series of novel keto sulfones of formula I ##STR1## in which the group .dbd.A-- is selected from .dbd.C(Ra)-- and .dbd.N-- and the other radicals have the meanings defined in the following specification.The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.Type: GrantFiled: October 16, 1986Date of Patent: June 6, 1989Assignee: ICI Americas Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 4812162Abstract: Compounds of the formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 and R.sup.2, which are the same or different, are hydrogen, cyano or halogen (fluorine, chlorine, bromine or iodine) or optionally substituted alkyl; V is either oxygen or sulphur; W, X, Y and Z, which may be the same or different, are hydrogen, halogen, nitro, cyano, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted aryl, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted arylalkoxy, optionally substituted alkenyl S(O).sub.n R.sup.3 (wherein n is 0, 1 or 2), or optionally substituted heteroaryl, or W, X or X, Y or Y, Z together form methylenedioxy; and R.sup.3 is optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl or optionally substituted heteroaryl.Type: GrantFiled: November 20, 1987Date of Patent: March 14, 1989Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Christopher R. A. Godfrey, Paul J. de Fraine
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Patent number: 4791109Abstract: Novel indole-carboxamides of the formula ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and aralkyl of 7 to 12 carbon atoms optionally substituted with 1 to 3 members of the group consisting of halogen, methyl, ethyl, methoxy, ethoxy, --CF.sub.3, CH.sub.3 S--, --NH.sub.2 and --NO.sub.2 or R.sub.1 and R taken together with the nitrogen atom form an optionally unsaturated heterocycle optionally containing a member of the group consisting of --O--, --S-- and ##STR2## R' is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, naphthyl, aralkyl of 7 to 12 carbon atoms and substituted phenyl, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 3 carbon atoms, chlorine, bromine, iodine, --NO.sub.2, --NH.sub.Type: GrantFiled: July 10, 1986Date of Patent: December 13, 1988Assignee: Roussel UclafInventors: Francois Clemence, Jacques Guillaume, Gilles Hamon