Plural Nitrogens Attached Directly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/191)
  • Patent number: 10221165
    Abstract: 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: Grant
    Filed: February 3, 2016
    Date of Patent: March 5, 2019
    Assignee: Council of Scientific and Industrial Research
    Inventors: Pradeep Kumar, Jignesh Kantilal Parikh, Eeshwaraiah Begari
  • Patent number: 9023877
    Abstract: 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: Grant
    Filed: June 23, 2010
    Date of Patent: May 5, 2015
    Assignee: Romark Laboratories L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20150064111
    Abstract: 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: Application
    Filed: April 3, 2013
    Publication date: March 5, 2015
    Applicant: APOSENSE LTD.
    Inventors: Joel M. Van Gelder, Menashe Levy, Mirit Argov, Miri Ben-Ami, Ilan Ziv
  • Publication number: 20150051249
    Abstract: 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: Application
    Filed: March 14, 2013
    Publication date: February 19, 2015
    Inventor: Loren D. Walensky
  • Patent number: 8835467
    Abstract: 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: Grant
    Filed: January 23, 2013
    Date of Patent: September 16, 2014
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Publication number: 20140221319
    Abstract: The invention provides methods and compositions for inhibiting CD 38 activity, and methods of treating or preventing various disorders associated with CD38 activity.
    Type: Application
    Filed: April 13, 2012
    Publication date: August 7, 2014
    Applicants: Mayo Foundation for Medical Education and Research, President and Fellows of Harvard College
    Inventors: David A. Sinclair, Nathan L. Price, Eduardo N. Chini, Jon C. Clardy, Shugeng Cao
  • Publication number: 20130143927
    Abstract: 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: Application
    Filed: June 8, 2012
    Publication date: June 6, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Patent number: 8383653
    Abstract: 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: Grant
    Filed: June 30, 2004
    Date of Patent: February 26, 2013
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Patent number: 8158806
    Abstract: 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: Grant
    Filed: September 12, 2008
    Date of Patent: April 17, 2012
    Assignees: Department of Biotechnology
    Inventors: Suparna Sengupta, Kallikat Narayanan Rajasekharan
  • Publication number: 20110178102
    Abstract: 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: Application
    Filed: June 30, 2004
    Publication date: July 21, 2011
    Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Vern L Schramm, Anthony A. Suave
  • Patent number: 7977482
    Abstract: 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: Grant
    Filed: October 19, 2007
    Date of Patent: July 12, 2011
    Assignee: The Procter & Gamble Company
    Inventors: Markus Speckbacher, Jessica Chassot, Hans-Jürgen Braun
  • Publication number: 20100137386
    Abstract: 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: Application
    Filed: July 15, 2009
    Publication date: June 3, 2010
    Inventors: Tesshi YAMADA, Miki SHITASHIGE, Koichi YOKOTA, Masaaki SAWA, Hideki MORIYAMA
  • Patent number: 7572816
    Abstract: 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: Grant
    Filed: July 21, 2004
    Date of Patent: August 11, 2009
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Bruno Tse, Sepehr Sarshar
  • Publication number: 20090118510
    Abstract: 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: Application
    Filed: October 19, 2007
    Publication date: May 7, 2009
    Inventors: Marcus Speckbacher, Jessica Chassot, Hans-Jurgen Braun
  • Publication number: 20090018341
    Abstract: 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: Application
    Filed: September 12, 2008
    Publication date: January 15, 2009
    Applicants: DEPARTMENT OF BIOTECHNOLOGY, RAJIV GANDHI CENTRE FOR BIOTECHNOLOGY, UNIVERSITY OF KERALA
    Inventors: Suparna Sengupta, Kallikat Narayanan Rajasekharan
  • Publication number: 20080227789
    Abstract: 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: Application
    Filed: December 21, 2007
    Publication date: September 18, 2008
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland
  • Publication number: 20080132709
    Abstract: 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: Application
    Filed: April 16, 2004
    Publication date: June 5, 2008
    Applicants: DEPARTMENT OF BIOTECHNOLOGY, RAJIV GANDHI CENTRE OF BIOTECHNOLOGY, UNIVERSITY OF KERALA
    Inventors: Suparna Sengupta, Kallikat Narayanan Rajasekharan
  • Patent number: 7109202
    Abstract: 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: Grant
    Filed: November 19, 2001
    Date of Patent: September 19, 2006
    Assignee: Novartis AG
    Inventors: Neil J Press, Roger J Taylor
  • Patent number: 6818663
    Abstract: 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: Grant
    Filed: May 5, 2003
    Date of Patent: November 16, 2004
    Assignee: Hoffmann-La Roches
    Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Kyungjin Kim, Allen John Lovey, Warren William McComas, John Guifoyle Mullin, Jr., Jefferson Wright Tilley
  • Publication number: 20040210063
    Abstract: 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: Application
    Filed: February 3, 2004
    Publication date: October 21, 2004
    Inventors: Andrew Neil Bowler, Bo Falck Hansen
  • Publication number: 20040072827
    Abstract: A 5-membered cyclic compound of the formula: 1
    Type: Application
    Filed: December 30, 2002
    Publication date: April 15, 2004
    Inventors: Norio Fujiwara, Hitoshi Fujita, Fujio Antoku, Toshinari Sugasawa, Hajime Kawakami
  • Patent number: 6720427
    Abstract: 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: Grant
    Filed: May 13, 2002
    Date of Patent: April 13, 2004
    Assignee: Pfizer Inc.
    Inventors: Mark A. Sanner, Chris J. Helal, Christopher B. Cooper
  • Patent number: 6720346
    Abstract: 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: Grant
    Filed: July 5, 2002
    Date of Patent: April 13, 2004
    Assignee: 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: 20030225147
    Abstract: 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: Application
    Filed: July 5, 2002
    Publication date: December 4, 2003
    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, Michael B. Wallace, Yi Yang
  • Patent number: 6620828
    Abstract: 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: Grant
    Filed: February 15, 2001
    Date of Patent: September 16, 2003
    Assignee: 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: 20030149049
    Abstract: 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: Application
    Filed: December 17, 2001
    Publication date: August 7, 2003
    Inventors: Michelle R. Arkin, Robert S. McDowell, Johan D. Oslob, Brian C. Raimundo, Nathan D. Waal, Chul Hyun Yu
  • Patent number: 6569878
    Abstract: 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: Grant
    Filed: October 27, 1998
    Date of Patent: May 27, 2003
    Assignee: Agouron Pharmaceuticals Inc.
    Inventors: Wesley K. M. Chong, Shao Song Chu, Lin Li, Rohit K. Duvadie, Yi Yang, Wei Xiao
  • Patent number: 6448286
    Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: July 28, 1998
    Date of Patent: September 10, 2002
    Assignee: 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: 20020025976
    Abstract: 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: Application
    Filed: February 15, 2001
    Publication date: February 28, 2002
    Applicant: 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: 20010039275
    Abstract: 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: Application
    Filed: January 31, 2001
    Publication date: November 8, 2001
    Inventors: Andrew Neil Bowler, Preben Houlberg Olesen, Anders Robert Sorensen, Bo Falck Hansen, Helle Worsaae, Peter Kurtzhals
  • Patent number: 6166056
    Abstract: 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: Grant
    Filed: August 24, 1998
    Date of Patent: December 26, 2000
    Assignees: Pharmacia, Upjohn Company
    Inventors: Richard C. Thomas, Toni-Jo Poel, Michael D. Ennis, David J. Anderson, Robert L. Hoffman
  • Patent number: 6110946
    Abstract: 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: Grant
    Filed: July 1, 1998
    Date of Patent: August 29, 2000
    Assignee: Novartis Finance Corporation
    Inventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
  • Patent number: 6096898
    Abstract: One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: August 1, 2000
    Assignee: Dow AgroSciences LLC
    Inventors: David E. Podhorez, John W. Hull, Jr., Christine H. Brady
  • Patent number: 6080772
    Abstract: 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: Grant
    Filed: December 11, 1997
    Date of Patent: June 27, 2000
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, John Yudhistir Ramphal, G. Davis Harris, Jr., Asaad S. Nematalla
  • Patent number: 6022868
    Abstract: 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: Grant
    Filed: December 19, 1997
    Date of Patent: February 8, 2000
    Assignee: Novo Nordisk Als
    Inventors: Preben Houlberg Olesen, John Bondo Hansen
  • Patent number: 5990135
    Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: November 23, 1999
    Assignee: Abbott Laboratories
    Inventors: Daniel W. Norbeck, Hing Leung Sham, Dale J. Kempf, Chen Zhao
  • Patent number: 5935973
    Abstract: 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: Grant
    Filed: January 5, 1998
    Date of Patent: August 10, 1999
    Assignee: Knoll Aktiengesellschaft
    Inventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
  • Patent number: 5919792
    Abstract: 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: Grant
    Filed: October 28, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
  • Patent number: 5712393
    Abstract: 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: Grant
    Filed: November 24, 1995
    Date of Patent: January 27, 1998
    Assignee: Synthelabo
    Inventors: Jean Michel Altenburger, Gilbert Lassalle
  • Patent number: 5700820
    Abstract: 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: Grant
    Filed: June 19, 1996
    Date of Patent: December 23, 1997
    Assignee: Dr. Reddy's Research Foundation
    Inventors: Krishnamurthi Vyas, Chebiyyam Prabhakar, Sreenivas Dharmaraja Rao, Mamillapalli Ramabadhra Sarma, Om Gaddam Reddy, Rajagopalan Ramanujam, Ranjan Chakrabarti
  • Patent number: 5663185
    Abstract: 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: Grant
    Filed: March 20, 1995
    Date of Patent: September 2, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Mueller, Hubert Sauter, Horst Wingert, Hartmann Koenig, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5631376
    Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: May 20, 1997
    Assignee: Abbott Laboratories
    Inventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
  • Patent number: 5621109
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: April 15, 1997
    Assignee: Abbott Laboratories
    Inventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
  • Patent number: 5594016
    Abstract: 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: Grant
    Filed: October 23, 1995
    Date of Patent: January 14, 1997
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Hiroaki Ueno, Takayuki Oe, Ichiro Suehiro, Fumiko Nakamura
  • Patent number: 5461067
    Abstract: 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: Grant
    Filed: February 1, 1994
    Date of Patent: October 24, 1995
    Assignee: Abbott Laboratories
    Inventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
  • Patent number: 5314891
    Abstract: 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: Grant
    Filed: September 10, 1992
    Date of Patent: May 24, 1994
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Philip N. Edwards, Keith Oldham, David Waterson
  • Patent number: 5256682
    Abstract: 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: Grant
    Filed: April 13, 1992
    Date of Patent: October 26, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Martin Kruger, Rolf Russe, Herbert Schneider, Ralph Schmiechen, Lechoslaw Turski
  • Patent number: 5245040
    Abstract: 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: Grant
    Filed: October 16, 1991
    Date of Patent: September 14, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Maienfisch, Odd Kristiansen, Laurenz Gsell
  • Patent number: 5229402
    Abstract: 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: Grant
    Filed: December 13, 1989
    Date of Patent: July 20, 1993
    Assignee: Taiho Pharmaceutical Company, Ltd.
    Inventors: Makoto Kajitani, Etsuo Hasegawa, Akihiro Kawaguchi, Junji Yamamoto, Katsuo Toide, Takaji Honna, Mitsugi Yasumoto, Nobuo Kasahara
  • Patent number: 5219869
    Abstract: 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: Grant
    Filed: September 11, 1992
    Date of Patent: June 15, 1993
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Yumi Hattori, Ikuro Honda, Katsuhiko Shibuya