Nitrogen Attached Directly To The Diazole Ring By Nonionic Bonding Patents (Class 548/326.5)
  • Publication number: 20040097739
    Abstract: Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.
    Type: Application
    Filed: February 11, 2003
    Publication date: May 20, 2004
    Inventors: Shogo Sakuma, Tsuyoshi Endo, Atsushi Tendo, Toshihiro Takahashi, Shinichi Yoshida, Kunio Kobayashi, Nobutaka Mochizuka, Tomio Yamakawa, Takashi Kanda, Seiichiro Masui
  • Publication number: 20040082795
    Abstract: A novel process for the asymmetric synthesis of substituted cyclic &bgr;-amino-carboxylates of the type shown in the specification from appropriate &bgr;-enamino-ester starting materials is described. These compounds are useful as intermediates for MMP and TACE inhibitors.
    Type: Application
    Filed: September 11, 2003
    Publication date: April 29, 2004
    Inventors: Joerg Deerberg, Douglas D. McLeod, Tai-Yuen Yue
  • Publication number: 20040082542
    Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
    Type: Application
    Filed: March 5, 2003
    Publication date: April 29, 2004
    Inventors: Adnan M.M. Mjalli, Robert C. Andrews, Ramesh Gopalaswamy, Anitha Hari, Kwasi S. Avor, Ghassan Qabaja, Xiao-Chuan Guo, Suparna Gupta, David R. Jones, Xin Chen
  • Publication number: 20040077696
    Abstract: The present invention provides compounds of formula I 1
    Type: Application
    Filed: June 18, 2003
    Publication date: April 22, 2004
    Inventors: Robert M. Borzilleri, Rajeev S. Bhide, John S. Tokarski, Peter Zheng, Ligang Qian, Zhen-Wei Cai
  • Publication number: 20040019085
    Abstract: Compounds having the formula (I), 1
    Type: Application
    Filed: June 17, 2003
    Publication date: January 29, 2004
    Inventors: William A. Slusarchyk, Scott A. Bolton, Timothy Herpin, Gregory S. Bisacchi, Zulan Pi, E. Scott Priestley
  • Publication number: 20040014968
    Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
    Type: Application
    Filed: July 9, 2003
    Publication date: January 22, 2004
    Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
  • Publication number: 20040010023
    Abstract: The invention relates to novel biphenyl derivatives of the general formula (I), wherein R4 represents an aromatic heterocycle, and to the physiologically acceptable salts or solvates thereof. The inventive compounds are integrin inhibitors and are used for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections and restenosis following angioplasty or for pathological processes that are maintained or propagated by angiogenesis.
    Type: Application
    Filed: February 21, 2003
    Publication date: January 15, 2004
    Inventors: Wolfgang Stahle, Gunter Holzemann, Simon Goodman
  • Patent number: 6667310
    Abstract: The present application provides guanidine derivatives of the formula (I) wherein R1, R2, R3, A and Z are as defined herein.
    Type: Grant
    Filed: October 1, 2002
    Date of Patent: December 23, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Wagner, Christoph Erdelen, Wolfram Andersch, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
  • Publication number: 20030229102
    Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders 1
    Type: Application
    Filed: November 15, 2002
    Publication date: December 11, 2003
    Inventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Publication number: 20030229123
    Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: 1
    Type: Application
    Filed: April 29, 2003
    Publication date: December 11, 2003
    Inventors: Keith Roger Bley, Robin Douglas Clark, Alam Jahangir, Bruce Andrew Kowalczyk, Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Thomas Weitao Sun
  • Publication number: 20030220372
    Abstract: This invention provides a compound of the formula (I): 1
    Type: Application
    Filed: April 9, 2003
    Publication date: November 27, 2003
    Inventors: Misato Hirano, Satoru Iguchi, Kazunari Nakao, Tatsuya Yamagishi
  • Patent number: 6653483
    Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: November 25, 2003
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 6653321
    Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: November 25, 2003
    Assignee: Telik, Inc.
    Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
  • Patent number: 6649613
    Abstract: Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1, 2 and R3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis.
    Type: Grant
    Filed: January 14, 2002
    Date of Patent: November 18, 2003
    Assignee: Merck Patent GmbH
    Inventors: Günter Hölzemann, Simon Goodman, Horst Kessler, Christoph Gibson, Gabór Sulyok
  • Publication number: 20030203951
    Abstract: The present invention relates to novel compounds that can be used as antiinflammatory, immunomodulatory and antiproliferatory agents. In particular the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehydrogenase (DHODH).
    Type: Application
    Filed: July 9, 2002
    Publication date: October 30, 2003
    Applicant: 4SC AG
    Inventors: Johan Leban, Bernd Kramer, Wael Saeb, Gabriel Garcia
  • Patent number: 6635630
    Abstract: Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —S—, —SO—, —SO2—, —NR12—, —NCOR12— or —NR12SO2R15;  is selected from the group consisting of X2 is —O—, —S— or —NR5—; Y is ═O, ═S or ═NR11; Y1 is H, C1-C6 alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6—heterocycloalkyl, —(C1-C3)alkyl-NH—C(O)O(C1-C6)alkyl or —NHC(O)R15; R5 is H or —(CH2)n1—G, wherein n1 is 0-5, G is H, —CF3, —CHF2, —CH2F, —OH, —O—(C1-C6 alkyl), —SO2R13, —O—(C3-C8 cycloalkyl), —NR13R14, —SO2NR13R14, —NR13SO2R15, —NR13COR12, —NR12(CONR13
    Type: Grant
    Filed: June 6, 2002
    Date of Patent: October 21, 2003
    Assignee: Schering Corporation
    Inventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
  • Publication number: 20030186967
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: February 6, 2002
    Publication date: October 2, 2003
    Applicant: American Home Products Corporation
    Inventors: Kenneth Lewis Kees, Lloyd M. Garrick, Ariamala Gopalsamy
  • Publication number: 20030187047
    Abstract: A compound of formula I 1
    Type: Application
    Filed: March 19, 2003
    Publication date: October 2, 2003
    Applicant: Allergan Sales, Inc.
    Inventors: Stephen A. Munk, James A. Burke, Michael E. Garst
  • Publication number: 20030181718
    Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
    Type: Application
    Filed: February 10, 2003
    Publication date: September 25, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Lin-Hua Zhang, Lei Zhu
  • Publication number: 20030162822
    Abstract: The present invention relates to 2′-halo-3′,5′-dialkoxyphen-1′-yl-imino-2-imidazolidine, the tautomeric 2′-halo-3′,5′-dialkoxyanilino-2-imidazoline and/or the pharmacologically acceptable salts thereof and their use as pharmaceutical compositions.
    Type: Application
    Filed: January 24, 2003
    Publication date: August 28, 2003
    Applicant: Boehringer Ingelheim Pharma KG
    Inventors: Franz Esser, Pascale Pouzet, Naoki Ishiguro, Hisato Kitagawa, Ikunobu Muramatsu
  • Publication number: 20030158420
    Abstract: A compound of Formula I or of Formula II 1
    Type: Application
    Filed: January 23, 2003
    Publication date: August 21, 2003
    Applicant: Boehringer Ingelheim Pharma GmbH Co. KG
    Inventors: Franz Esser, Pascale Pouzet, Hisato Kitagawa, Kenji Sakai, Ikunobu Muramatsu
  • Publication number: 20030144311
    Abstract: Novel propanoic acid derivatives are integrin receptor antagonists or inhibitors, in particular of the avb3 integrin receptor. The compounds of the invention are for instance useful for the treatment of solid tumors by inhibition of angiogenic growth of tumor vessel network, thus promoting tumor regression, inhibition of metastatic spread, thus avoiding cancer metastases, inhibition of bone resorption, thus controlling osteoporosis, inhibition of smooth muscle cells migration into neointima, thus blocking restenosis after percutaneous coronary angioplasty and the treatment of other pathological conditions mediated by cell adhesion, cell migration or angiogenesis such e.g. diabetic retinopaty, rheumatoid arthritis and inflammation.
    Type: Application
    Filed: November 1, 2002
    Publication date: July 31, 2003
    Inventors: Tiziano Bandiera, Paola Vianello, Paolo Cozzi, Arturo Galvani
  • Publication number: 20030119828
    Abstract: The present application relates to novel guanidine derivatives of the formula (I) 1
    Type: Application
    Filed: October 1, 2002
    Publication date: June 26, 2003
    Inventors: Klaus Wagner, Christoph Erdelen, Wolfram Andersch, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
  • Publication number: 20030109687
    Abstract: Compounds of the formula
    Type: Application
    Filed: August 5, 2002
    Publication date: June 12, 2003
    Inventors: Tae K. Song, Min Teng, Roshantha A. Chandraratna
  • Publication number: 20030100593
    Abstract: The subject invention involves compounds having structure (I): wherein each R1 is independently alkyl, aryl, or heterocycle; each R2, R4, R7, and R8 is independently hydrogen or other substituent; A is aryl or heterocycle; and pharmaceutically acceptable forms thereof.
    Type: Application
    Filed: June 14, 2002
    Publication date: May 29, 2003
    Inventors: Song Liu, Benjamin Eric Blass, David Edward Portlock
  • Publication number: 20030092741
    Abstract: Aspects of the present invention are directed towards compounds of Formula I for the treatment of human erectile disorders including erectile dysfunction in men.
    Type: Application
    Filed: August 9, 2002
    Publication date: May 15, 2003
    Inventors: Duane D. Miller, Seoung-Soo Hong
  • Publication number: 20030073850
    Abstract: Compounds of formula I 1
    Type: Application
    Filed: February 17, 2000
    Publication date: April 17, 2003
    Inventors: Robert J. Altenbach, Michael D. Meyer, James F. Kerwin, Albert Khilevich, Teodozyj Kolasa, Jeffrey Rohde, William A. Carroll, Xenia Searle, Fan Yang
  • Publication number: 20030050330
    Abstract: A class of compounds is described for treating inflammation and inflammation-related disorders.
    Type: Application
    Filed: June 21, 2002
    Publication date: March 13, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Richard M. Weier, Paul W. Collins, Michael A. Stealey, Thomas E. Barta, Renee M. Huff
  • Publication number: 20030036655
    Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: 1
    Type: Application
    Filed: May 31, 2002
    Publication date: February 20, 2003
    Inventors: Keith Roger Bley, Robin Douglas Clark, Alam Jahangir, Bruce Andrew Kowalczyk, Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Thomas Weitao Sun
  • Publication number: 20020188132
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: December 4, 2000
    Publication date: December 12, 2002
    Inventors: Jeremy I. Levin, James M. Chen, Frances C. Nelson
  • Publication number: 20020169193
    Abstract: A compound of formula I or of tautomeric formula II 1
    Type: Application
    Filed: January 28, 2002
    Publication date: November 14, 2002
    Inventors: Pascale Pouzet, Franz Esser, Matthias Hoffmann, Hisato Kitagawa, Kenji Sakai, Ikunobu Muramatsu
  • Patent number: 6479531
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently ═N—, —N(R5)—═CH—, —S— or —O—.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: November 12, 2002
    Assignee: James Black Foundation Limited
    Inventors: Sarkis Barret Kalindjian, Ildiko Maria Buck, Ian Duncan Linney, Paul Trevor Wright, Iain Mair McDonald, Katherine Isobel Mary Steel, Robert Antony David Hull, Sonia Patricia Roberts, John David Gaffen, Jeremy Gilbert Vinter, Martin Keith Walker, James Whyte Black, Gillian Fairfull Watt, Elaine Anne Harper, Nigel Paul Shankley, Matthew John Tozer, David John Dunstone, Michael John Pether, Elliot James Lilley, David Andrew Sykes, Caroline Minli Rachel Low, Eric Peter Griffin, Laurence Wright
  • Patent number: 6465650
    Abstract: The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B′ is a base customary in nucleotide chemistry. The processes include reacting a compound of Formula (II) with a compound of Formula (III) a compound of Formula (V) B′—CH2—CO—R2  (V), a monohaloacetic acid derivative in a suitable solvent with an auxiliary base, or a compound of Formula (VII) B′—CH2—CO—R3  (VII), and converting the resulting compounds to that of Formula I.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: October 15, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gerhard Breipohl, Eugen Uhlmann, Jochen Knolle
  • 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: 20020119963
    Abstract: The invention provides compounds of formula 1 1
    Type: Application
    Filed: July 31, 2001
    Publication date: August 29, 2002
    Inventors: Mark A. Sanner, Chris J. Helal, Christoper B. Cooper, Frank S. Menniti, Michael K. Ahlijanian, Anabella Villalobos, Lit-Fui Lau, Patricia A. Seymour
  • Publication number: 20020107252
    Abstract: The invention relates to heteroaromatic carboxamides of formula (I), 1
    Type: Application
    Filed: February 5, 2002
    Publication date: August 8, 2002
    Inventors: Andrew Baxter, Stephen Brough, Alan Faull, Craig Johnstone, Thomas McInally
  • Patent number: 6395764
    Abstract: This invention involves compounds having the following structure: wherein: a) R1 is hydrogen; or alkyl; bond (a) is a single or a double bond; b) R2 and R3 are each independently selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino and halo; c) R4, R5 and R6 are each independently selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino; halo; and 2-imidazolinylamino; and wherein one and only one of R4, R5 and R6 is 2-imidazolinylamino; d) R7 is selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino and halo;
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: May 28, 2002
    Assignee: The Procter & Gamble Company
    Inventors: Raymond Todd Henry, Russell James Sheldon, William Lee Seibel
  • Publication number: 20020028806
    Abstract: Novel pesticides of formula (I) 1
    Type: Application
    Filed: May 7, 2001
    Publication date: March 7, 2002
    Inventors: Thomas Goebel, Eliane Humbert-Droz, Maurizio Schwarzenbach
  • Patent number: 6310070
    Abstract: A novel purine derivative exhibiting an effect to control inflammatory symptoms characteristic to nephritis and a medicine comprising this compound as an effective ingredient are provided. The compound is represented by the following general formula (I), wherein R1 is a hydrocarbon group having 17 or less carbon atoms and R2 is a hydrocarbon group having 16 or less carbon atoms, wherein one or more CH2 g roups in the hydrocarbon group which 7013 do not directly bind with the carbon atom at 2 or 7 position of the purine ring replaced are by carbonyl groups, sulfonyl groups, O, or S and/or one or more CH groups in the hydrocarbon group which do not directly bind with the carbon atom at 2 or 7 position of the purine ring are replaced by N, C-halogen, or C—C≡N, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 28, 2000
    Date of Patent: October 30, 2001
    Assignee: Japan Energy Corporation
    Inventors: Akihisa Yokoyama, Sumitsugu Kisanuki, Yoshikazu Matsuda, Junko Matsui, Yoshiaki Isobe
  • Patent number: 6268313
    Abstract: The dihalopropene compounds of the general formula [I] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: July 31, 2001
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
  • Patent number: 6262090
    Abstract: Compounds of the formula wherein A is heteroaryl; R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms; W is O, NR6, or is absent; G is aryl or heteroaryl; and X is a bond X is a bond, —NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; and J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; or a pharmaceutical acceptable salt thereof, useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.
    Type: Grant
    Filed: November 22, 1999
    Date of Patent: July 17, 2001
    Assignee: American Home Products Corporation
    Inventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara