Ring Chalcogen In The Tricyclo Ring System Patents (Class 548/430)
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Publication number: 20030045565Abstract: The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: ApplicationFiled: September 16, 2002Publication date: March 6, 2003Applicant: Pharmacia & Upjohn CompanyInventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao
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Patent number: 6514984Abstract: A method is disclosed for the prevention and treatment of Alzheimer's disease by administering to a human in need thereof an effective amount of a substituted tricyclic sPLA2 inhibitor.Type: GrantFiled: April 12, 2000Date of Patent: February 4, 2003Assignee: Eli Lilly and CompanyInventor: August Masaru Watanabe
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Patent number: 6469171Abstract: The present invention relates to methods for preparing a variety of Lamellarin compounds and analogues via a synthetic intermediate, which methods involved the step of performing an intramolecular cyclization of a compound of Formula (I) to produce compounds of Formula(II), wherein the variables are given in the specification.Type: GrantFiled: February 2, 2001Date of Patent: October 22, 2002Assignee: The Australian National UniversityInventors: Martin Gerhardt Banwell, Bernard Luke Flynn
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Publication number: 20020055499Abstract: Compounds of the formula (I) are disclosed which are dual fibrinogen receptor and vitronectin receptor antagonists and are useful in the treatment of atherosclerosis, in the prevention of restenosis and in the prevention of tumor metastasis and tumor growth: 1Type: ApplicationFiled: December 12, 2001Publication date: May 9, 2002Inventors: Dirk Heerding, James Martin Samanen
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Patent number: 6384050Abstract: The present invention relates to a compound having a tricyclic amine substituent which may have various substituents, the compound being represented by formula (I), a salt or hydrate thereof, and a hydrate of the salt and a drug containing them as an active ingredient. They exhibit excellent antimicrobial activity against Gram negative bacteria and Gram positive bacteria with a satisfactory fate and safety and are useful in the treatment of infectious diseases.Type: GrantFiled: April 22, 1999Date of Patent: May 7, 2002Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Kenichi Kimura, Rie Miyauchi, Hitoshi Ohki, Katsuhiro Kawakami
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Patent number: 6365605Abstract: Compounds of formula (I): wherein: m is 0 to 3 inclusive, n is 0 to 3 and 2≦m+n≦3, p is 1 to 6 inclusive, X represents cyano or —CO—NR4R5, R4 and R5 being selected from hydrogen, linear or branched (C1-C6)-alkyl, (C3-C7)-cycloalkyl, and aryl, R1 and R2 each independently represent hydrogen or linear or branched (C1-C6)-alkyl, R3 represents hydrogen, optionally substituted phenyl, naphthyl or heteroaryl, or aryloxy or arylthio, or aryl or heteroaryl substituted by A′-Cy, A′ and Cy being as defined in the description, and medicinal products containing the same which are useful as D3 receptor ligands.Type: GrantFiled: January 10, 2000Date of Patent: April 2, 2002Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Thierry Dubuffet, Patrick Hautefaye, Françoise Lejeune, Mark Millan
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Publication number: 20020035140Abstract: The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: ApplicationFiled: May 24, 2001Publication date: March 21, 2002Inventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao
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Publication number: 20020032204Abstract: The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: ApplicationFiled: May 24, 2001Publication date: March 14, 2002Inventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Peng Cho Tang
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Publication number: 20020004079Abstract: A process for extracting a compound or composition of matter from a raw material containing that compound or composition as a constituent part is described. The process comprises the steps of (1) contacting a sample of the raw material with an extraction solvent comprising a C1-4 (hydro)fluorocarbon alone or with a co-solvent, and (2) separating the solvent liquor thus obtained containing the extract from the raw material. The process may be used to extract natural products, such as flavored or aromatic oils, and biologically active compounds, such as pesticides and pharmaceuticals.Type: ApplicationFiled: April 26, 2001Publication date: January 10, 2002Inventors: Richard Llewellyn Powell, Timothy James Noakes
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Patent number: 6326377Abstract: Compounds of formula (I): wherein: m is 0 to 3 inclusive, n is 0 to 3 and 2≦m+n≦3, p is 1 to 6 inclusive, X represents cyano or —CO—NR4R5, R4 and R5 being selected from hydrogen, linear or branched (C1-C6)-alkyl, (C3-C7)-cycloalkyl,and aryl, R1 and R2 each independently represent hydrogen or linear or branched (C1-C6)-alkyl, R3 represents hydrogen, optionally substituted phenyl, naphthyl or heteroaryl, or aryloxy or arylthio, or aryl or heteroaryl substituted by A′—Cy, A′ and Cy being as defined in the description, and medicinal products containing the same which are useful as D3 receptor ligands.Type: GrantFiled: January 10, 2000Date of Patent: December 4, 2001Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Thierry Dubuffet, Patrick Hautefaye, Françoise Lejeune, Mark Millan
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Publication number: 20010037030Abstract: The present invention relates to a compound having a tricyclic amine substituent which may have various substituents, the compound being represented by formula (I), a salt or hydrate thereof, and a hydrate of the salt and a drug containing them as an active ingredient. They exhibit excellent antimicrobial activity against Gram negative bacteria and Gram positive bacteria with a satisfactory fate and safety and are useful in the treatment of infectious diseases.Type: ApplicationFiled: June 8, 2001Publication date: November 1, 2001Inventors: Makoto Takemura, Hisashi Takahashi, Kenichi Kimura, Rie Miyauchi, Hitoshi Ohki, Katsuhiro Kawakami
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Patent number: 6201004Abstract: Compounds of formula I and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neType: GrantFiled: September 1, 1999Date of Patent: March 13, 2001Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, Paul Anthony Bradley
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Patent number: 6177440Abstract: A class of novel tricyclics is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: April 21, 1998Date of Patent: January 23, 2001Assignee: Eli Lilly and CompanyInventors: Nicholas James Bach, Susan Elizabeth Draheim, Robert Delane Dillard, Edward David Mihelich, Jason Scott Sawyer, Douglas Wade Beight, Michael LeRoy Phillips, Tulio Suarez, Daniel Jon Sall, Jolie Anne Bastian, Michael Lyle Denney, Gary Alan Hite, Michael Dean Kinnick, Robert Theodore Vasileff, John Michael Morin, Jr., Ho-Shen Lin, Michael Enrico Richett, Richard Waltz Harper, John McNeill McGill, III, Benjamin Alan Anderson, Nancy Kay Harn, Richard James Loncharich, Richard Walter Schevitz
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Patent number: 6162822Abstract: A compound of formula (I) ##STR1## in which: m, and n, which may be identical or different, represent 0 or 1,X and Y, which may be identical or different, represent hydrogen or halogen or alky, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino or dialkylamino,Z represent a linear or branched C.sub.4 to C.sub.12 alkylene chain in which one or more --CH.sub.2 -- are optionally replaced by any one of the following atoms or groups: --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --CONH--, or by a substituted or unsubstituted heterocylcic,A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, ##STR2## and medicinal products containing the same are useful as anticancer agent.Type: GrantFiled: December 28, 1998Date of Patent: December 19, 2000Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Ghanem Atassi, Alain Pierre, Laurence Kraus-Berthier, Stephane Leonce
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Patent number: 6090837Abstract: Compounds of formula (I): ##STR1## wherein: m is 0 to 3 inclusive,n is 0 to 3 and 2.ltoreq.m+n.ltoreq.3,p is 1 to 6 inclusive,X represents cyano or --CO--NR.sub.4 R.sub.5, R.sub.4 and R.sub.5 being selected from hydrogen, linear or branched (C.sub.1 -C.sub.6)-alkyl, (C.sub.3 -C.sub.7)-cycloalkyl, and aryl,R.sub.1 and R.sub.2 each independently represent hydrogen or linear or branched (C.sub.1 -C.sub.6)-alkyl,R.sub.3 represents hydrogen, optionally substituted phenyl, naphthyl or heteroaryl, or aryloxy or arylthio, or aryl or heteroaryl substituted by A'-Cy, A' and Cy being as defined in the description, andmedicinal products containing the same which are useful as D.sub.3 receptor ligands.Type: GrantFiled: June 23, 1998Date of Patent: July 18, 2000Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Thierry Dubuffet, Patrick Hautefaye, Fran.cedilla.oise Lejeune, Mark Millan
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Patent number: 6080752Abstract: A compound of formula (I): ##STR1## wherein R.sup.1 represents a group of formula (A) or (B): ##STR2## R.sup.2, R.sup.3, Ar, Y Ar.sup.Type: GrantFiled: December 14, 1998Date of Patent: June 27, 2000Assignee: SmithKline Beecham PLCInventors: Geoffrey Stemp, Stephen Allan Smith, Christopher Norbert Johnson, Phillip Jeffrey
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Patent number: 6018054Abstract: The invention relates to intermediate compounds for preparing novel quinolone derivatives- and naphthyridone derivatives which are substituted in the 7-position by a partially hydrogenated isoindolinyl ring, to processes for their preparation and to antibacterial agents and feed additives containing them.Type: GrantFiled: November 26, 1997Date of Patent: January 25, 2000Assignee: Bayer AktiengesellschaftInventors: Thomas Philipps, Stephan Bartel, Andreas Krebs, Uwe Petersen, Thomas Schenke, Klaus-Dieter Bremm, Rainer Endermann, Karl Georg Metzger, Burkhard Mielke
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Patent number: 5998459Abstract: The invention relates to a pharmaceutical composition comprising a pyrrole derivative of the following formula [1] or a pharmaceutically acceptable salt thereof, or a solvate of either of them, as an active ingredient. ##STR1## (wherein R.sup.1 represents hydrogen or alkoxycar91 bonylamino, R.sup.2 represents alkyl, aryl which may be substituted, aromatic heterocyclyl which may be substituted, unsubstituted amino, monoalkylamino, dialkylamino, or cyclic amino which may be substituted; R.sup.3 represents cyano or carbamoyl; R.sup.4 represents hydrogen or alkyl; E represents alkylene; q is equal to 0 or 1, A represents methyl, aryl which may be substituted, or aromatic heterocyclyl which may be substituted). The pharmaceutical composition of the invention is effective for the treatment of pollakiuria or urinary incontinence.Type: GrantFiled: December 8, 1997Date of Patent: December 7, 1999Inventors: Masami Tsuda, Mitsushi Tanaka, Ayatsugu Nakamura
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Patent number: 5929106Abstract: Dihydroisoindole compounds of formula (I), wherein the substituents are as defined herein, are disclosed as being useful as endothelin receptor antagonists. The compounds are applied in the treatment of cardiovascular and renal diseases.Type: GrantFiled: October 27, 1997Date of Patent: July 27, 1999Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Robert Gene Franz, M. Amparo Lago, Aiming Gao
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Patent number: 5888432Abstract: The present invention has for subjects, novel benzopyran derivatives, substituted in position 2 with an adamantyl group as well as the compositions and (co)polymer matrices containing such derivatives. Said derivatives possess interesting photochromic properties.Type: GrantFiled: December 3, 1997Date of Patent: March 30, 1999Assignee: Corning IncorporatedInventor: You-Ping Chan
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Patent number: 5886192Abstract: A method for the preparation of a lactam compound of formula ##STR1## wherein R'.sub.1 and R".sub.1 independently are acyl or aroyl, or taken together form an optionally substituted methylene, and G.sub.1 is hydrogen or an amino protecting group, comprising oxidizing a bis O-protected 1R-2-azadihydroxybicyclo-?2.2.1!heptane compound of formula ##STR2## with about 0.1 mol % to about 1 mol % of RuO.sub.2 or hydrate thereof in the presence of about 3 equivalents of an oxidant to form the lactam compound with an enantiomeric excess of greater than or equal to about 95%.Type: GrantFiled: June 10, 1997Date of Patent: March 23, 1999Assignee: Rhone-Poulenc Rorer S.A.Inventors: Patrick Leon, Denis Largeau, Thierry Durand, Michael O'Brien, Matthew Powers
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Patent number: 5831096Abstract: A method for the preparation of a compound of formula ##STR1## wherein R is hydrogen or, respectively, a group of formula ##STR2## R.sub.1 is alkyl; Ar is optionally substituted aryl; andR.sub.3' and R.sub.3" are hydrogen, alkyl or phenyl, or R.sub.3' and R.sub.3" taken together with the carbon atom to which they are attached form cycloalkyl, or salt thereof, comprising acid facilitated acetalizing or ketalizing of a compound of formula ##STR3## wherein R.sub.3' and R.sub.3" are as defined above, and R.sub.4' and R.sub.4" are alkoxy, or taken together with the carbon atom to which they are attached form carbonyl, with a compound of formula ##STR4## wherein * represents an R chirality;R, R.sub.1 and Ar are as defined above, or salt thereof in isopropanol.Type: GrantFiled: June 10, 1997Date of Patent: November 3, 1998Assignee: Rhone-Poulenc Rorer S.A.Inventors: Patrick Leon, Michael O'Brien, Denis Largeau, Matthew Powers, Ching Tsuei
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Patent number: 5827799Abstract: An object of the invention is to provide herbicides which are completely selective to crops such as paddy rice, soybeans and cotton and have an excellent herbicidal activity on weeds.The invention relates to ether compounds of the general formula (I) ##STR1## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the same meanings as defined in the text and herbicides containing said compounds as active components.Type: GrantFiled: July 19, 1996Date of Patent: October 27, 1998Assignee: Mitsui Chemicals, Inc.Inventors: Kiyoshi Arai, Fumiaki Koizumi, Hiroyuki Suzuki, Takeshi Kakimoto, Sadafumi Koda
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Patent number: 5767141Abstract: Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseasesPropane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the preparation of these compounds, their use as pharmaceuticals, and pharmaceutical products are described. Also described are novel intermediates for preparing the compounds of the formula I.Type: GrantFiled: March 8, 1995Date of Patent: June 16, 1998Assignee: Hoechst AktiengesellschaftInventors: Gerrit Schubert, Horst Hemmerle, Peter Below, Andreas Herling, Hans-Jorg Burger
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Patent number: 5756320Abstract: Bioactive substances K93-0711 I-1 and I-2 having inhibitory action on IL-6 activity, are produced by culturing a microorganism belonging to the genus Streptomyces in a medium, whereby the bioactive substances K93-0711 I-1 and I-2 accumulate in the medium. These bioactive substances K93-0711 I-1 and I-2 are then isolated therefrom. The substances are effective for treatment of IL-6-involving diseases such as cancer cachexia, multiple myeloma and rheumatoid arthritis.Type: GrantFiled: January 21, 1997Date of Patent: May 26, 1998Assignee: The Kitasato InstituteInventors: Satoshi Omura, Kanki Komiyama, Masahiko Hayashi, Satoshi Takamatsu
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Patent number: 5754271Abstract: The invention relates to photochromic compounds of general formula: ##STR1## wherein R.sup.a, R.sup.b and R.sup.c is denote hydrogen; alkyl; aryl; OR, SR, COR or COOR, in which R denotes hydrogen, alkyl or aryl, amino of formula NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2 denote hydrogen, alkyl, cycloalkyl or an aryl; a halogen atom; a mono- or polyhaloalkyl group; or an NO.sub.2, CN or SCN group; n and m denote integers from 1 to 5; p is equal to 1 or 2; and H is a 5-members aromatic heterocycle containing one or more heteroatoms selected from nitrogen, oxygen and sulfur, these heterocyclic nuclei being eventually substituted by one or more alkyl, alkoxy, amino, aryl or aralkyl groups or condensed with a phenyl nucleus, a substituted phenyl nucleus or a 6-members cycloaliphatic nucleus and to their use in ophtalmic optics.Type: GrantFiled: June 3, 1996Date of Patent: May 19, 1998Assignee: Essilor International (Compagnie General d'Optique)Inventors: Robert Guglielmetti, Jean Luc Pozzo, Andre Samat
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Patent number: 5705509Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: July 28, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5663191Abstract: Compounds of formula (I): ##STR1## in which: n represents 1 or 2,R.sub.1 represents hydrogen or alkyl, benzyl, acetyl, benzoyl, allyl, pyridinecarbonyl, pyridinemethyl, acylaminoalkyl (optionally substituted), pyridineaminocarbonyl, phthalimidoalkyl, thiochromanyloxyalkyl or (benzodioxanyloxy)alkyl,R.sub.2, R.sub.3 or R.sub.4, which may be identical or different, represent hydrogen or halogen or alkyl, alkoxy, hydroxyl, acetyl, aminocarbonyl, aminomethyl, cyano, nitro, amino, phenyl (which may or may not be substituted), furyl, pyridinyl, thienyl or pyridyl, or alternatively,when they are located on adjacent carbons, R.sub.2 and R.sub.3 form, with the carbon atoms which bear them, a furan or phenyl ring,the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same are useful for the treatment of diseases requiring a ligand to the 5-HT.sub.2C receptors.Type: GrantFiled: July 5, 1995Date of Patent: September 2, 1997Assignee: Adir Et CompagnieInventors: Gilbert Lavielle, Thierry Dubuffet, Mark Millan, Adrian Newman-Tancredi
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Patent number: 5646300Abstract: There are disclosed neuroprotective compounds having the formula ##STR1## wherein the moieties are defined in the specification, and processes for making them.Type: GrantFiled: June 1, 1995Date of Patent: July 8, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Denise M. Flanagan, Lawrence L. Martin, Peter A. Nemoto
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Patent number: 5646298Abstract: The present invention describes cyclopropylindole cytotoxic prodrugs of formulas (I), (II) and (III) as shown in the specification. The present invention is also directed to a method for the site-specific treatment of neoplastic diseases in a mammal which method includes the following steps: (i) administering to an afflicted mammal an effective amount of a targeting agent- enzyme donor peptide conjugate wherein the targeting agent is selected from the group of antibodies, monoclonal antibodies, adhesion molecules and tumor cell surface binding ligands; (ii) administering to the afflicted mammal an effective amount of an enzyme acceptor dimer thereby forming active enzymatic sites at a tumor cell surface; and (iii) administering to the afflicted mammal a therapeutically effective amount of an enzyme-activateable, cytotoxic pro-drug thereby releasing the cytotoxic drug at the tumor site.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: ProCoron, Inc.Inventor: Michael J. Powell
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Patent number: 5646173Abstract: The invention relates to tricyclic pyrrole derivatives useful as 5-HT selective agents of the formula ##STR1## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower alkyl, phenyl, cycloalkyl or lower alkoxy and R.sup.2 additionally is lower alkoxycarbonyl, acyloxy or mesyloxy;R.sup.5 to R.sup.7 are, independently, hydrogen or lower alkyl;X is --CH.sub.2 CH(C.sub.6 H.sub.5)--, --CH.dbd.C(C.sub.6 H.sub.5)--, --YCH.sub.2 --, --CH.dbd.CH-- or --(CR.sup.11 R.sup.12).sub.n ;R.sup.11 and R.sup.12 are, independently, hydrogen, phenyl, lower alkyl or halogen;n is 1 to 3 andy is O or S,as well as pharmaceutically acceptable salts of basic compounds of formula I with pharmaceutically acceptable acids.Type: GrantFiled: February 21, 1996Date of Patent: July 8, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Jurgen Wichmann, Ulrich Widmer
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Patent number: 5633276Abstract: A compound of formula (I) ##STR1## wherein, R.sup.1 is hydrogen, halogen or C.sub.1-6 alkyl;R.sup.2 is a group of formula --CR.sup.3 R.sup.4 (CH.sub.2).sub.p NR.sup.5 COR.sup.6 ;R.sup.3, R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or C.sub.l-6 alkyl;R.sup.6 is C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl;n is an integer of 2, 3 or 4;p is an integer of 1, 2, 3 or 4;and pharmaceutically acceptable salts and solvates thereof. A compound of formula (I) is useful in the treatment of conditions associated with a disturbed functioning of the melatonin system.Type: GrantFiled: June 14, 1996Date of Patent: May 27, 1997Assignee: Glaxo Group LimitedInventors: Peter C. North, Malcolm C. Carter
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Patent number: 5631383Abstract: Novel derivatives of 1R- or 1S-2-azabicyclo[2.2.Type: GrantFiled: June 7, 1995Date of Patent: May 20, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Denis Largeau, Patrick Leon
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Patent number: 5545636Abstract: The present invention discloses compounds of the general formula: ##STR1## The compounds are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.Type: GrantFiled: October 18, 1994Date of Patent: August 13, 1996Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., John H. McDonald, III, Michael Paal, Gerd R uhter, Theo Schotten, Wolfgang Stenzel
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Patent number: 5536721Abstract: The present invention relates to therapeutically active heterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system related to the metabotropic glutamate receptor system.Type: GrantFiled: March 14, 1995Date of Patent: July 16, 1996Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Anders Kanstrup, Peter Faarup, Preben H. Olesen
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Patent number: 5510366Abstract: An indole derivative represented by formula (1), ##STR1## wherein A is a group ##STR2## wherein R.sup.10 is hydrogen or lower alkyl, dotted lines may optionally be present, and R.sup.1 -R.sup.9 represents various substitutional groups. The compound (1) exhibits a positive inotropic action on cardiac muscle, an anti-arrhythmic action, and a vasodilation action without increasing the heart rate. A heart affection therapeutic agent comprising this compound as an effective component is extremely effective for treating heart failures and arrhythmia.Type: GrantFiled: October 28, 1994Date of Patent: April 23, 1996Assignee: Kowa Co., Ltd.Inventors: Yoshinori Kyotani, Katsumi Kawamine, Tsutomu Toma, Tadaaki Ohgiya, Takashi Yamaguchi, Kazuhiro Onogi, Seiichi Sato, Noboru Shimizu, Hiromichi Shigyo, Tomio Ohta, Toshiaki Oda, Yukihiro Okuno, Kimiyuki Shibuya, Yoshio Takahashi, Mikio Fujii, Yasumi Uchida
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Patent number: 5475092Abstract: Novel cytotoxic agents comprising a cell binding agent chemically linked to one or more analogue or derivative of CC-1065 are described. The therapeutic use of the cytotoxic agents is also described. These cytotoxic agents have therapeutic use because they deliver the cytotoxic drugs to a specific cell population in a targeted fashion.Type: GrantFiled: March 21, 1994Date of Patent: December 12, 1995Assignee: Immunogen Inc.Inventors: Ravi V. J. Chari, Viktor S. Goldmakher, Walter A. Blattler
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Patent number: 5436250Abstract: A compound having the formula ##STR1## wherein R.sup.4 and R.sup.5 independently are hydrogen, halogen, CF.sub.3, CN, NO.sub.2 or SO.sub.2 NR.sup.1 R.sup.2 whereinR.sup.1 is hydrogen or C.sub.1-6 -alkyl which may be straight, branched or cyclic,R.sup.2 is hydrogen or C.sub.1-6 -alkyl which may be straight, branched or cyclic, or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --A--(CH.sub.2).sub.m --, wherein A is O, S, CH.sub.2 or NR.sup.I, wherein R.sup.I is H, C.sub.1-6 -alkyl which may be straight, branched or cyclic, n is 0, 1, 2, 3, 4, 5 and m is 0, 1, 2, 3, 4, 5;R.sup.II is hydrogen, benzyl, (C.dbd.O)CF.sub.3, C.sub.1-6 -carboxylic acid acyl, C.sub.1-6 -alkoxy which may be branched or cyclic, or C.sub.1-6 -alkyl which may be straight, branched or cyclic, CH.sub.2 CO.sub.2 R.sup.VI wherein R.sup.VI is hydrogen or C.sub.Type: GrantFiled: July 7, 1993Date of Patent: July 25, 1995Assignee: NeuroSearch A/SInventors: Frank Watjen, Bjarne H. Dahl, Jorgen Drejer, Lein H. Jensen
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Patent number: 5380746Abstract: The present invention provides bis-(1H-indol-3-yl)maleinimide derivatives and the pharmacologically acceptable salts thereof, processes for the preparation of these compounds, and pharmaceutical compositions containing them for the treatment of heart and blood vessel diseases, such as thromboses, arteriosclerosis, hypertension, of inflammatory processes, allergies, cancer, and certain degenerative damages of the central nervous system, as well as of diseases of the immune system and viral diseases.Type: GrantFiled: March 9, 1993Date of Patent: January 10, 1995Assignee: Goedecke AktiengesellschaftInventors: Hubert Barth, Johannes Hartenstein, Claus Rudolph, Christoph Schachtele, Hans-Jurgen Betche, Reinhard Reck, Hartmut Osswald
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Patent number: 5378723Abstract: Substituted carbamates of tricyclic compounds which have a cyclic sulfer atom, provide highly potent and selective cholinergic agonist and blocking activity are useful as pharmaceutical agents. Cholinergic disease are treated with these compounds such as glaucoma, Myasthenia Gravis, Alzheimer's disease. Methods for inhibiting esterases, acetylcholinesterase and butyrylcholinesterase are also provided.Type: GrantFiled: January 18, 1994Date of Patent: January 3, 1995Assignee: The United States of America as represented by the Secretary of the Dept. of Health and Human ServicesInventors: Arnold Brossi, Xiao-shu He, Nigel H. Greig
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Patent number: 5334591Abstract: Conformationally constrained tricyclic thienothiopyran compounds are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.Type: GrantFiled: March 4, 1993Date of Patent: August 2, 1994Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Kenneth L. Shepard, Gerald S. Ponticello, Theresa M. Williams
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Patent number: 5324742Abstract: The present invention relates to a novel aldose reductase inhibitor of the formula: ##STR1## wherein X is methylene or carbonyl;R is ##STR2## R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each is hydrogen or lower alkyl, to a method for producing the inhibitor by culturing Crucibulum sp. RF-3817 or its variants, and to an agent for inhibiting an aldose reductase comprising the inhibitor.Type: GrantFiled: May 8, 1991Date of Patent: June 28, 1994Assignee: Shionogi & Co., Ltd.Inventors: Tadashi Yoshida, Toshiyuki Kato, Yoshimi Kawamura, Koichi Matsumoto, Hiroshi Itazaki
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Patent number: 5302599Abstract: A therapeutically useful compound of formula I ##STR1## or pharmaceutically acceptable salts thereof where A and B are oxygen, sulfur or CH.sub.2, X is an amine moiety as defined herein and R.sub.1 and R.sub.2 are as defined herein having 5HT.sub.1A neuronal activity and/or dopamine receptor activity useful in the treatment of central nervous system and cardiovascular system disorders.Type: GrantFiled: September 15, 1992Date of Patent: April 12, 1994Assignee: The Upjohn CompanyInventors: Michael D. Ennis, Mark E. Baze
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Patent number: 5288748Abstract: A compound of Formula I ##STR1## or pharmaceutically acceptable salts of Formula I, where R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, --(CH.sub.2).sub.n CONH.sub.2 where n is 2 to 6, (CH2).sub.n -1-(4,4-dimethylpiperidine-2,6-dione-yl), or cyclopropylmethyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl or combined with R.sup.1 to form a C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 akynyl, (CH.sub.2).sub.n --R"--Ar where R" is O, S, or NH, 3,3,3-trifluoropropyl, --(CH.sub.2).sub.m --R.sup.9 where m is 2 or 3 and R.sup.9 is phenyl, 2-thienyl or 3-thienyl; R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, formyl, CN, halogen, CH.sub.2 OR.sup.2, C(O)C(O)OR.sup.1, C(O)CO NR.sup.1 R.sup.2, --(CH.sub.2).sub.q --NR.sup.1 R.sup.2 where q is 0 to 5, C.dbd.NOR.sup.2, 2(4,5-dihydro)oxazolyl, or COR.sup.10 where R.sup.10 is H, R.sup.1, NR.sup.1 R.sup.2 or CF.sub.3 ; R.sup.4 is hydrogen, C.sub.1 -C.sub.3 alkyl, cyclopropylmethyl, CF.Type: GrantFiled: July 1, 1992Date of Patent: February 22, 1994Assignee: The Upjohn CompanyInventors: Hakan V. Wikstrom, Per A. E. Carlsson, Bengt R. Andersson, Kjell A. I. Svensson, Stig T. Elebring, Nils P. Stjernlof, Arthur G. Romero, Susanne R. Haadsma-Svensson, Chiu-Hong Lin, Michael D. Ennis
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Patent number: 5276053Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: October 6, 1992Date of Patent: January 4, 1994Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5258511Abstract: Heterocyclic compounds of the formula ##STR1## in which R represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,A represents C--R.sup.1, N,R.sup.1 represents substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,X, Y represent O, NH,Z represents hydrogen, --CN, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,W represents O, N--R.sup.5,R.sup.5 represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic radical andB represents a substituted or unsubstituted carbocyclic-aromatic or heterocyclic ring onto which one or more further rings can be fused,and the use of these compounds as dyestuffs or pigments.Type: GrantFiled: July 20, 1992Date of Patent: November 2, 1993Assignee: Bayer AktiengesellschaftInventor: Hans Hochstetter
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Patent number: 5248691Abstract: This invention provides novel furanoindoline compounds effective in inhibiting the growth of solid tumors.Type: GrantFiled: September 3, 1992Date of Patent: September 28, 1993Assignee: Eli Lilly and CompanyInventor: Fariborz Mohamadi
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Patent number: 5242918Abstract: A compound having the formula ##STR1## wherein R.sup.4 and R.sup.5 independently are hydrogen, halogen, CF.sub.3, CN, NO.sub.2 or SO.sub.2 NR.sup.1 R.sup.2 whereinR.sup.1 is hydrogen or straight, C.sub.1-6 -alkyl which may be branched or cyclic,R.sup.2 is hydrogen or straight, C.sub.1-6 -alkyl which may be branched or cyclic,or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --A--(CH.sub.2).sub.m --, wherein A is O, S, CH.sub.2 or NR.sup.I, wherein R.sup.I is H, C.sub.1-6 -alkyl which may be straight, branched or cyclic, n is 0, 1, 2, 3, 4, 5 and m is 0, 1, 2, 3, 4, 5;Q is NOH or O;Z=O, S, N--R.sup.II, ##STR2## wherein R.sup.II, R.sup.III, R.sup.IV and R.sup.V independently are hydrogen, benzyl, C.sub.1-6 carboxylic acid-acyl, C.sub.1-6 -alkoxy which may be branched or cyclic, or C.sub.1-6 -alkyl which may be branched or cyclic;X is --(CH.sub.2).sub.o -- wherein o is 0, 1, 2, or 3;Y is --(CH.sub.2).sub.p -- wherein p is 0, 1, 2 or 3;.alpha. and .beta.Type: GrantFiled: August 27, 1992Date of Patent: September 7, 1993Assignee: NeuroSearch A/SInventors: Frank Watjen, Bjarne H. Dahl, Jorgen Drejer, Leif H. Jensen
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Patent number: 5221681Abstract: The present invention relates to new substituted benzoxazepines and benzothiazepines of the general formula I ##STR1## in which X, R.sup.1, R.sup.2 and R.sup.3 have the meaning given in the description, processes for their preparation and their use in medicaments having vaso- and muscle-relaxing properties, in particular as circulatory agents.Type: GrantFiled: January 16, 1992Date of Patent: June 22, 1993Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Kabbe, Helmut Heitzer, Andreas Knorr, Claudia Hirth-Dietrich
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Patent number: 5180736Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: May 17, 1991Date of Patent: January 19, 1993Assignee: Warner-Lambert CompanyInventor: Graham Johnson