Plural Nitrogens Attached Directly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/191)
-
Patent number: 10221165Abstract: The present invention discloses a novel EGFR inhibitor compound of formula (1), process for preparation thereof and methods of treating abnormal cell growth in mammals by administering the compounds of formula (1) wherein, R is selected from hydrogen, alkyl, nitro, halogens such as chlorine, bromine, fluorine and iodine; R1=hydrogen, alkyl, alkoxy, aryl, nitro, halogens such as chlorine, bromine, fluorine and iodine, trifluoromethyl, thioalkyl, trifluromethoxy, trialkylsilyl.Type: GrantFiled: February 3, 2016Date of Patent: March 5, 2019Assignee: Council of Scientific and Industrial ResearchInventors: Pradeep Kumar, Jignesh Kantilal Parikh, Eeshwaraiah Begari
-
Patent number: 9023877Abstract: This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.Type: GrantFiled: June 23, 2010Date of Patent: May 5, 2015Assignee: Romark Laboratories L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
-
Publication number: 20150064111Abstract: The invention relates to compounds and use thereof in the diagnosis and/or in treatment of medical disorders. In some embodiments, the compounds may be used for detecting a cancer. The compound may include a di-acid moiety. In some embodiments the di-acid moiety comprises a di-carboxylic acid and in some embodiments the di-acid moiety comprises a di-tetrazole.Type: ApplicationFiled: April 3, 2013Publication date: March 5, 2015Applicant: APOSENSE LTD.Inventors: Joel M. Van Gelder, Menashe Levy, Mirit Argov, Miri Ben-Ami, Ilan Ziv
-
Publication number: 20150051249Abstract: This disclosure features compounds and pharmaceutically acceptable salts thereof that inhibit MCL-1 and/or BFL-1/A1 and compositions containing the same. This disclosure also features combinations that include one or more of the MCL-1/BFL-1/A1 inhibitor compounds described herein, or a pharmaceutically acceptable salt thereof; and one or more additional therapeutic agents (e.g., one or more chemotherapeutic agents (including small molecule and/or anti-body based chemotherapy and/or radiation); e.g., one or more therapeutic agents that modulate apoptosis; e.g., one or more therapeutic agents that bind to and inhibit anti-apoptotic proteins or modulate them indirectly; e.g., one or more therapeutic agents that bind to and inhibit, or indirectly modulate, anti-apoptotic BCL-2, BCL-XL, BCL-w, MCL-1, and/or BFL-1/A1; e.g., one or more therapeutic agents that directly bind to and inhibit anti-apoptotic BCL-2/BCL-XL; e.g., agents such as ABT-199, ABT-263 and ABT-737; e.g.Type: ApplicationFiled: March 14, 2013Publication date: February 19, 2015Inventor: Loren D. Walensky
-
Patent number: 8835467Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: GrantFiled: January 23, 2013Date of Patent: September 16, 2014Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
-
Publication number: 20140221319Abstract: The invention provides methods and compositions for inhibiting CD 38 activity, and methods of treating or preventing various disorders associated with CD38 activity.Type: ApplicationFiled: April 13, 2012Publication date: August 7, 2014Applicants: Mayo Foundation for Medical Education and Research, President and Fellows of Harvard CollegeInventors: David A. Sinclair, Nathan L. Price, Eduardo N. Chini, Jon C. Clardy, Shugeng Cao
-
Publication number: 20130143927Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: June 8, 2012Publication date: June 6, 2013Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
-
Patent number: 8383653Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: GrantFiled: June 30, 2004Date of Patent: February 26, 2013Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
-
Patent number: 8158806Abstract: A synthetic diaminoketothiazole, its process of preparation and its use as a microtubule inhibitor, a probe for tubulin-microtubule system and a cytotoxic agent. Diaminoketothiazole of the formula (I) wherein Ar is 4-OMe-C6H5, Ar? is C6H5.Type: GrantFiled: September 12, 2008Date of Patent: April 17, 2012Assignees: Department of BiotechnologyInventors: Suparna Sengupta, Kallikat Narayanan Rajasekharan
-
Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
-
Patent number: 7977482Abstract: The present invention relates to a) a non-oxidative coloring agent for keratin fibers, in particular human hair, comprising at least one dye according to formula (I) or (II), b) an oxidative coloring agent for keratin fibers, in particular human hair, which comprises at least one oxidizing agent (e.g. hydrogen peroxide), at least one oxidative dye precursor and at least one dye according to formula (I) or (II), and c) a lightening agent for keratin fibers, in particular human hair, which comprises at least one oxidizing agent (e.g. hydrogen peroxide) and at least one dye according to formula (I) or (II), with R4 being a cationic group.Type: GrantFiled: October 19, 2007Date of Patent: July 12, 2011Assignee: The Procter & Gamble CompanyInventors: Markus Speckbacher, Jessica Chassot, Hans-Jürgen Braun
-
Publication number: 20100137386Abstract: The present invention relates to compositions and methods for the treatment of cancer patients with Traf2- and Nck-interacting kinase (TNIK) inhibitors. More particularly, the present invention relates to pharmaceutical compositions comprising TNIK inhibitor and a pharmaceutically acceptable carrier, and to methods for treating the TNIK inhibitor administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. And the present invention relates to a novel aminothiazole derivatives.Type: ApplicationFiled: July 15, 2009Publication date: June 3, 2010Inventors: Tesshi YAMADA, Miki SHITASHIGE, Koichi YOKOTA, Masaaki SAWA, Hideki MORIYAMA
-
Patent number: 7572816Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.Type: GrantFiled: July 21, 2004Date of Patent: August 11, 2009Assignee: Auspex Pharmaceuticals, Inc.Inventors: Bruno Tse, Sepehr Sarshar
-
Publication number: 20090118510Abstract: The present invention relates to a) a non-oxidative colouring agent for keratin fibres, in particular human hair, comprising at least one dye according to formula (I) or (II), b) an oxidative colouring agent for keratin fibres, in particular human hair, which comprises at least one oxidizing agent (e.g. hydrogen peroxide), at least one oxidative dye precursor and at least one dye according to formula (I) or (II), and c) a lightening agent for keratin fibres, in particular human hair, which comprises at least one oxidizing agent (e.g. hydrogen peroxide) and at least one dye according to formula (I) or (II), with R4 being a cationic group.Type: ApplicationFiled: October 19, 2007Publication date: May 7, 2009Inventors: Marcus Speckbacher, Jessica Chassot, Hans-Jurgen Braun
-
Publication number: 20090018341Abstract: A synthetic diaminoketothiazole, its process of preparation and its use as a microtubule inhibitor, a probe for tubulin-microtubule system and a cytotoxic agent. Diaminoketothiazole of the formula (I) wherein Ar is 4-OMe-C6H5, Ar? is C6H5.Type: ApplicationFiled: September 12, 2008Publication date: January 15, 2009Applicants: DEPARTMENT OF BIOTECHNOLOGY, RAJIV GANDHI CENTRE FOR BIOTECHNOLOGY, UNIVERSITY OF KERALAInventors: Suparna Sengupta, Kallikat Narayanan Rajasekharan
-
Publication number: 20080227789Abstract: Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 21, 2007Publication date: September 18, 2008Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland
-
Publication number: 20080132709Abstract: A synthetic diaminoketothiazole, its process of preparation and its use as a microtubule inhibitor, a probe for tubulin-microtubule system and a cytotoxic agent. Diaminoketothiazole of the formula (I) wherein Ar is 4-OMe-C6H5, Ar? is C6H5.Type: ApplicationFiled: April 16, 2004Publication date: June 5, 2008Applicants: DEPARTMENT OF BIOTECHNOLOGY, RAJIV GANDHI CENTRE OF BIOTECHNOLOGY, UNIVERSITY OF KERALAInventors: Suparna Sengupta, Kallikat Narayanan Rajasekharan
-
Patent number: 7109202Abstract: Compounds of formula (I) in free or salt form, where A is a C6-C15 monovalent aromatic group. R1 is hydrogen, phenyl optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, C1–C8-alkyl, C1–C8-haloalkyl, C1–C8-alkoxy, C1–C8-alkoxy-C1–C8-alkyl or acyloxy, or a 5- or 6-membered monovalent heterocyclic group, R2 is hydrogen, C1-C8-alkyl, acyl or CON(R3)R4, provided that R2 is C1–C8-alkyl, acyl or CON(R3)R4 when R1 is hydrogen, R3 and R4 are each independently hydrogen, or C1–C8-alkyl, together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, and Zl, Z2, Z3 and Z4 are each independently N or CR5, at least one of them being CR5, and R5 is hydrogen, C1–C8-alkyl or C1–C8-alkoxy.Type: GrantFiled: November 19, 2001Date of Patent: September 19, 2006Assignee: Novartis AGInventors: Neil J Press, Roger J Taylor
-
Patent number: 6818663Abstract: The present invention is directed to novel diaminothiazoles of formula These compounds inhibit cyclin-dependent kinase 4 (Cdk4) and are selective against Cdk2 and Cdk1. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung and colon and prostate tumors.Type: GrantFiled: May 5, 2003Date of Patent: November 16, 2004Assignee: Hoffmann-La RochesInventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Kyungjin Kim, Allen John Lovey, Warren William McComas, John Guifoyle Mullin, Jr., Jefferson Wright Tilley
-
Publication number: 20040210063Abstract: Novel 2,4-diaminothiazole derivatives of the general formula (I) which inhibit GSK-3 (glycogen synthase kinase-3), use of these compounds as medicaments, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful for the treatment of disorders, syndromes, diseases and conditions, wherein an inhibition of GSK-3 (glycogen synthase kinase-3) is beneficial, especially IGT (impaired glucose tolerance), type 1 diabetes, type 2 diabetes, obesity, Alzheimer's disease and bipolar disorder.Type: ApplicationFiled: February 3, 2004Publication date: October 21, 2004Inventors: Andrew Neil Bowler, Bo Falck Hansen
-
Publication number: 20040072827Abstract: A 5-membered cyclic compound of the formula: 1Type: ApplicationFiled: December 30, 2002Publication date: April 15, 2004Inventors: Norio Fujiwara, Hitoshi Fujita, Fujio Antoku, Toshinari Sugasawa, Hajime Kawakami
-
Patent number: 6720427Abstract: The invention provides compounds of formula 1 wherein R1, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and those affected by dopamine neurotransmission are described.Type: GrantFiled: May 13, 2002Date of Patent: April 13, 2004Assignee: Pfizer Inc.Inventors: Mark A. Sanner, Chris J. Helal, Christopher B. Cooper
-
Patent number: 6720346Abstract: Aminothiazole compounds with mono-/di-substituted benzamide are represented by the Formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, pharmaceutically active metabolites, and pharmaceutically acceptable salts of said metabolites are described. These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.Type: GrantFiled: July 5, 2002Date of Patent: April 13, 2004Assignee: Agouron Pharmaceuticals, Inc.Inventors: Shao Song Chu, Larry Andrew Alegria, Ted Michael Bleckman, Wesley Kwan Mung Chong, Rohit K. Duvadie, Lin Li, Siegfried Heinz Reich, William Henry Romines, III, Michael B. Wallace, Yi Yang
-
Publication number: 20030225147Abstract: Aminothiazole compounds with mono-/di-substituted benzamide are represented by the Formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, pharmaceutically active metabolites, and pharmaceutically acceptable salts of said metabolites are described.Type: ApplicationFiled: July 5, 2002Publication date: December 4, 2003Inventors: Shao Song Chu, Larry Andrew Alegria, Ted Michael Bleckman, Wesley Kwan Mung Chong, Rohit K. Duvadie, Lin Li, Siegfried Heinz Reich, William Henry Romines, Michael B. Wallace, Yi Yang
-
Patent number: 6620828Abstract: Diaminothiazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: February 15, 2001Date of Patent: September 16, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Shao Song Chu, Larry Andrew Alegria, Steven Lee Bender, Suzanne Pritchett Benedict, Allen J. Borchardt, Robert Steve Kania, Mitchell David Nambu, Anna Maria Tempczyk-Russell, Sepehr Sarshar, Dilip Bhumralkar, Zhengwei Peng, Michelle Yang
-
Publication number: 20030149049Abstract: Compounds of formulae I and I′, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are antagonists of IL-2/IL-2R binding; and are useful for the treatment of interleukin-2 mediated diseases, such as autoimmune diseases (such as rheumatoid arthritis, multiple sclerosis, uveitis, and psoriasis), allograft rejection, and graft-versus-host disease.Type: ApplicationFiled: December 17, 2001Publication date: August 7, 2003Inventors: Michelle R. Arkin, Robert S. McDowell, Johan D. Oslob, Brian C. Raimundo, Nathan D. Waal, Chul Hyun Yu
-
Patent number: 6569878Abstract: Pharmaceutical compositions containing effective amounts of CDK-inhibiting diaminothiazole compounds of the following formula (where R1 and R2 are as defined in the specification) or their salts, or prodrugs or active metabolites of such compounds or salts, are useful for treating disorders and diseases such as cancer: In preferred embodiments, R1 and R2 are independently unsubstituted or substituted carbocyclic or heterocyclic aryl ring structures. Compounds where R2 is ortho-substituted aryl are especially potent inhibitors of CDKs such as CDK4.Type: GrantFiled: October 27, 1998Date of Patent: May 27, 2003Assignee: Agouron Pharmaceuticals Inc.Inventors: Wesley K. M. Chong, Shao Song Chu, Lin Li, Rohit K. Duvadie, Yi Yang, Wei Xiao
-
Patent number: 6448286Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 28, 1998Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
-
Publication number: 20020025976Abstract: Diaminothiazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: ApplicationFiled: February 15, 2001Publication date: February 28, 2002Applicant: Agouron Pharmaceuticals, Inc.Inventors: Shao Song Chu, Larry Andrew Alegria, Steven Lee Bender, Suzanne Pritchett Benedict, Allen J. Borchardt, Robert Steve Kania, Mitchell David Nambu, Anna Maria Tempczyk-Russell, Sepehr Sarshar, Dilip Bhumralkar, Zhengwei Peng, Michelle Yang
-
Publication number: 20010039275Abstract: 2,4-Diaminothiazole derivatives which inhibit GSK-3 (glycogen synthase kinase-3) and which are useful for the treatment and/or prevention disorders and diseases wherein an inhibition of GSK-3 is beneficial, especially especially Alzheimer's disease, bipolar disorder, IGT (impaired glucose tolerance), Type 1 diabetes, Type 2 diabetes and obesity.Type: ApplicationFiled: January 31, 2001Publication date: November 8, 2001Inventors: Andrew Neil Bowler, Preben Houlberg Olesen, Anders Robert Sorensen, Bo Falck Hansen, Helle Worsaae, Peter Kurtzhals
-
Patent number: 6166056Abstract: A compound of Formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1 ; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -aryl, --COR.sub.1-1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1-1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h -aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h -aryl, or halo; R.sub.3 and R.sub.4 are independently H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy; m and n taken together are 1 or 2. The compounds are useful antimicrobial agents.Type: GrantFiled: August 24, 1998Date of Patent: December 26, 2000Assignees: Pharmacia, Upjohn CompanyInventors: Richard C. Thomas, Toni-Jo Poel, Michael D. Ennis, David J. Anderson, Robert L. Hoffman
-
Patent number: 6110946Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.Type: GrantFiled: July 1, 1998Date of Patent: August 29, 2000Assignee: Novartis Finance CorporationInventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
-
Patent number: 6096898Abstract: One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.Type: GrantFiled: October 22, 1999Date of Patent: August 1, 2000Assignee: Dow AgroSciences LLCInventors: David E. Podhorez, John W. Hull, Jr., Christine H. Brady
-
Patent number: 6080772Abstract: The present invention relates to thiazole containing compounds capable of inhibiting protein tyrosine phosphatase activity. The invention further relates to the use of such compounds to modulate or regulate signal transduction by inhibiting protein tyrosine phosphatase activity. Finally, the invention relates to the use of such compounds to treat various disease states including diabetes mellitus.Type: GrantFiled: December 11, 1997Date of Patent: June 27, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, John Yudhistir Ramphal, G. Davis Harris, Jr., Asaad S. Nematalla
-
Patent number: 6022868Abstract: Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.Type: GrantFiled: December 19, 1997Date of Patent: February 8, 2000Assignee: Novo Nordisk AlsInventors: Preben Houlberg Olesen, John Bondo Hansen
-
Patent number: 5990135Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: May 31, 1995Date of Patent: November 23, 1999Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing Leung Sham, Dale J. Kempf, Chen Zhao
-
Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, 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 neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
-
Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
-
Patent number: 5712393Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.Type: GrantFiled: November 24, 1995Date of Patent: January 27, 1998Assignee: SynthelaboInventors: Jean Michel Altenburger, Gilbert Lassalle
-
Patent number: 5700820Abstract: Novel polymorphic forms of Troglitazone and methods for preparing the polymorphic forms of Troglitazone. The polymorphic forms of Troglitazone can be used to treat diabetic ailments.Type: GrantFiled: June 19, 1996Date of Patent: December 23, 1997Assignee: Dr. Reddy's Research FoundationInventors: Krishnamurthi Vyas, Chebiyyam Prabhakar, Sreenivas Dharmaraja Rao, Mamillapalli Ramabadhra Sarma, Om Gaddam Reddy, Rajagopalan Ramanujam, Ranjan Chakrabarti
-
Patent number: 5663185Abstract: Heteroaromatic compounds of the formulae IA and IB ##STR1## where the dashed line is a double bond between the carbon atom and a Z atom, and the index and the substituents have the following meanings:R.sup.1alkyl, alkoxy, alkylaminoR.sup.2alkyl;Aa direct bond; alkylene, alkenylene, alkynylene; O, S, S-oxides, N and alkylene derivatives or oxime radicals thereofBhydrogen, halogen,alkyl, alkenyl, alkynyl; cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, aryl, hetarylUCH.sub.2, CHCl, CHR.sup.2 or NOR.sup.2 ;Xhydrogen, cyano, nitro, halogen,alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, hetaryl; oxi- and thio derivatives thereof, carbonyl derivatives thereof, carbonyloxy derivatives thereof, amino derivatives thereof, oxime derivatives thereof,amino which may bear one or two of the abovementioned groups;m1 or 2,Yoxygen or sulfur;Z.sup.1 -Z.sup.2, Z.sub.3 -Z.sub.Type: GrantFiled: March 20, 1995Date of Patent: September 2, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Horst Wingert, Hartmann Koenig, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
-
Patent number: 5631376Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: May 31, 1995Date of Patent: May 20, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
-
Patent number: 5621109Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein the terms R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y, Y', m and n are herein defined.Type: GrantFiled: May 31, 1995Date of Patent: April 15, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
-
Patent number: 5594016Abstract: Naphthalene derivatives represented by the formula (I): ##STR1## wherein the symbol ##STR2## --X-- represents --O-- or --S--, .dbd.Y-- represents .dbd.N-- or .dbd.CR.sup.5 --, R.sup.1, C.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent hydrogen, halogen, alkyl and the like,R.sup.6 represents hydrogen, alkyl, aryl and the like,n represents an integer of 0 to 3, --- represents a single bond or a double bond, which are useful for reducing blood sugar and blood lipid levels are provided.Type: GrantFiled: October 23, 1995Date of Patent: January 14, 1997Assignee: Mitsubishi Chemical CorporationInventors: Hiroaki Ueno, Takayuki Oe, Ichiro Suehiro, Fumiko Nakamura
-
Patent number: 5461067Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y.sub.m and Y'.sub.n are herein defined.Type: GrantFiled: February 1, 1994Date of Patent: October 24, 1995Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
-
Patent number: 5314891Abstract: The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 and R.sup.3 together form --A.sup.2 --X.sup.2 --A.sup.3 -- which defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio or imino;Ar is optionally substituted phenylene;R.sup.4 is (1-4C)alkyl, fluoro-(2-4C)alkyl or optionally substituted phenyl or a heterocyclic moiety;R.sup.5 is hydrogen or (1-4C)alkyl; andR.sup.6 is hydrogen, halogeno, trifluoromethyl, (1-4C)alkyl or (1-4C)alkoxy;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: September 10, 1992Date of Patent: May 24, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Philip N. Edwards, Keith Oldham, David Waterson
-
Isoxazolylimidazole derivatives, process for their production and their use in pharmaceutical agents
Patent number: 5256682Abstract: 4-Isoxazolyl-imidazole derivatives of formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings indicated, as well as their production and use in pharmaceutical agents, are described.Type: GrantFiled: April 13, 1992Date of Patent: October 26, 1993Assignee: Schering AktiengesellschaftInventors: Martin Kruger, Rolf Russe, Herbert Schneider, Ralph Schmiechen, Lechoslaw Turski -
Patent number: 5245040Abstract: A process for the preparation of 1,3-disubstituted 2-nitroguanidines of the formula I ##STR1## in which R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or a radical --CH.sub.2 B; A is an unsubstituted or mono- to tetrasubstituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, which may contain one or two substituents from the group comprising C.sub.1 -C.sub.3 haloalkyl having 1 to 7 halogen atoms, cyclopropyl, halocyclopropyl having 1 to 3 halogen atoms, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, C.sub.2 -C.sub.3 haloalkenyl and C.sub.2 -C.sub.3 haloalkynyl having 1 to 4 halogen atoms, C.sub.1 -C.sub.3 haloalkoxy having 1 to 7 halogen atoms, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkylthio having 1 to 7 halogen atoms, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro and one to four substituents from the group comprising C.sub.1 -C.sub.3 alkyl, C.sub.Type: GrantFiled: October 16, 1991Date of Patent: September 14, 1993Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Odd Kristiansen, Laurenz Gsell
-
Patent number: 5229402Abstract: The present invention provides a carbamoyl-2-pyrrolidinone compound which has the following formula (2) and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.3 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having lower alkoxyl, lower alkylamino, a halogen atom or halogenomethyl as a substituent.Further, the present invention provides novel carbamoyl-2-pyrrolidinone compounds represented by the formula ##STR2## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.2 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having methoxy or lower alkylamino as a substituent, provided that when R.sup.1 is a hydrogen atom or unsubstituted lower alkyl, R.sup.2 is not unsubstituted phenyl.Type: GrantFiled: December 13, 1989Date of Patent: July 20, 1993Assignee: Taiho Pharmaceutical Company, Ltd.Inventors: Makoto Kajitani, Etsuo Hasegawa, Akihiro Kawaguchi, Junji Yamamoto, Katsuo Toide, Takaji Honna, Mitsugi Yasumoto, Nobuo Kasahara
-
Patent number: 5219869Abstract: Insecticidal nitro-substituted heterocyclic compounds of the formula ##STR1## wherein R.sup.1 represents hydrogen, cyano or C.sub.1-4 alkyl,m represents 0 or 1,n represents 0 or 1,R.sup.2 represents hydrogen or C.sub.1-4 alkyl,R.sup.3 represents hydrogen, C.sub.1-6 alkyl optionally substituted substituted by cyano, halogen or C.sub.1-4 alkoxy, C.sub.3-4 alkenyl, C.sub.3-4 alkynyl, optionally substituted phenyl, optionally substituted benzyl or optionally substituted heterocyclic-methyl,T represents an optionally substituted two- or three-membered divalent or trivalent chain comprising hetero atoms and/or carbon atom, andA represents optionally substituted phenyl or an optionally substituted five- or six-membered heterocyclic radical comprising at least one hetero atom selected from the group consisting of N, O and S.Type: GrantFiled: September 11, 1992Date of Patent: June 15, 1993Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Yumi Hattori, Ikuro Honda, Katsuhiko Shibuya