Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/243)
  • Patent number: 7045535
    Abstract: Certain cyclic compounds are presented as well as their use for inhibiting paramyxovirus neuraminidase.
    Type: Grant
    Filed: March 8, 2002
    Date of Patent: May 16, 2006
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Pooran Chand, Yarlagadda S. Babu, R. Scott Rowland, Tsu-Hsing Lin
  • Patent number: 7022725
    Abstract: A compound represented by the formula (I) wherein one of R1 and R2 is a hydrogen atom or a substituent and the other is an optionally substituted cyclic group; W is a bond or a divalent aliphatic hydrocarbon group; Y is a group of the formula: —OR3 (wherein R3 is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group) or an optionally esterified or amidated carboxyl group, or a salt thereof or a prodrug thereof has a superior insulin secretion promoting action and a hypoglycemic action and shows low toxicity. Therefore, the compound is useful as a pharmaceutical agent, particularly as an agent for the prophylaxis or treatment of diabetes and diabetic complications, and the like.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: April 4, 2006
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yu Momose, Tsuyoshi Maekawa, Tomoko Asakawa, Nozomu Sakai
  • Patent number: 7012088
    Abstract: The present invention provides antibacterial agents of formula I described herein and intermediates for their preparation.
    Type: Grant
    Filed: January 22, 2004
    Date of Patent: March 14, 2006
    Assignee: Pharmacia & Upjohn Company
    Inventor: Toni-Jo Poel
  • Patent number: 6974826
    Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.
    Type: Grant
    Filed: July 19, 2004
    Date of Patent: December 13, 2005
    Assignees: Incyte San Diego Inc., Ortho McNeil Pharmaceutical Inc.
    Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul, David P. M. Pleynet, Lyle W. Spruce
  • Patent number: 6946466
    Abstract: The invention relates to the use of aromatics sulfonamides of the general formula I as peroxynitrite rearrangement catalysts, to the preparation thereof and to the use thereof as medicament for the treatment of various disorders.
    Type: Grant
    Filed: April 10, 2003
    Date of Patent: September 20, 2005
    Assignee: Schering AG
    Inventors: Thorsten Blume, Roland Neuhaus, Detlev Suelzle, Iris Pribilla, Gisbert Depke, Joseph S. Beckman
  • Patent number: 6939886
    Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
    Type: Grant
    Filed: July 20, 2004
    Date of Patent: September 6, 2005
    Assignee: Wyeth
    Inventors: Scott Christian Mayer, Eric Gould Gundersen, Hassan Mahmoud Elokdah, David LeRoy Crandall
  • Patent number: 6903216
    Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them. Compounds of formula I, in which R1 to R7 have the meanings stated in the claims, act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. They are therefore suitable as novel antiarrhythmic ingredients, such as for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutter.
    Type: Grant
    Filed: June 12, 2002
    Date of Patent: June 7, 2005
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Joachim Brendel, Thomas Böhme, Stefan Peukert, Heinz-Werner Kleemann
  • Patent number: 6890942
    Abstract: The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integrase and for the treatment of AIDS or ARC by administering compounds of the formula.
    Type: Grant
    Filed: May 5, 2004
    Date of Patent: May 10, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Walker, Hatice Belgin Gulgeze, Jacques Banville, Roger Remillard, Donald Corson
  • Patent number: 6884813
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein A is a structure i, ii, iii, or iv X is CR7; Y is —S(?O)n—, —S(?NR8)—, or —S(?NR8)(?O)—; Z is —NHC(?O)R1, —NHC(?S)R1, —NR-het1, —O-het1, —S-het1, or -het2; and n is independently 0, 1, or 2. The compounds of formula I are useful as antimicrobials against a number of human and veterinary pathogens.
    Type: Grant
    Filed: January 21, 2003
    Date of Patent: April 26, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail F. Gordeev, Adam Renslo, Gary W. Luehr, Stuart Lam, Neil E. Westlund, Dinesh V. Patel
  • Patent number: 6875784
    Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formulea I and II, described herein, or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
    Type: Grant
    Filed: October 2, 2003
    Date of Patent: April 5, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail Fedor Gordeev, Adam Renslo, Dinesh Vinoobhai Patel
  • Patent number: 6852716
    Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: February 8, 2005
    Assignee: Pfizer Inc
    Inventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Jason K. Myers, Vincent E. Groppi, Jr.
  • Patent number: 6841519
    Abstract: The isoxazoline derivative of the present invention is represented by the following general formula [I]: [wherein Q is a group represented by —S(O)n—(CR5R6)m- (wherein n is an integer of 0 to 2, m is an integer of 1 to 3, and R5 and R6 are a hydrogen atom, a cyano group, an alkoxycarbonyl group, if an alkyl group or the like); R1 and R2 are a hydrogen atom, all optionally substituted alkyl group, an alkoxycarbonyl group, an optionally substituted phenyl group or the like; R3 and R4 are a hydrogen atom, an optionally substituted alkyl group, a cycloalkyl group or the like; Y is a hydrogen atom, an alkoxycarbonyl group, a carboxyl group, an alkenyl group, an optionally substituted alkyl group or an optionally substituted phenyl group]. The herbicide of the present invention contains the above isoxazoline derivative as the active ingredient.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: January 11, 2005
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Masao Nakatani, Kouichirou Kaku, Takumi Yoshimura, Masatoshi Tamaru, Hiroshi Kawasaki, Kazunori Kobayashi, Takeshige Miyazawa
  • Publication number: 20040259734
    Abstract: The present invention aims at providing an isoxazoline derivative and a pharmaceutically acceptable salt thereof, both having an excellent herbicidal effect and an excellent selectivity between crop and weed.
    Type: Application
    Filed: June 12, 2004
    Publication date: December 23, 2004
    Inventors: Masao Nakatani, Minoru Ito, Kyoko Kimijima, Masahiro Miyazaki, Makoto Fujinami, Ryohei Ueno, Satoru Takahashi
  • Publication number: 20040254381
    Abstract: The present invention relates to a process for the production of substituted 5-isoxazolidinone antibiotics. More specifically the patent relates to the production of compounds that mimic the antibiotic action of &bgr;-lactams, are resistant to &bgr;-lactamase degradation, and inhibit all classes of &bgr;-lactamase.
    Type: Application
    Filed: August 15, 2003
    Publication date: December 16, 2004
    Inventors: Richard A. Day, Charles Thomas Rentz, Gregory Shannon Huang, Amit B. Patel, Amjad M. Iqbal, Paul M. Gretz, Xiangzhong Shen, Xuefei Cao
  • Patent number: 6828276
    Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C1, C2, C3 are cyclic radicals, X1 is a hetero atom, X2 is a chain of carbon atoms, L is a chain-like element, R1, R2, R3, R4, R5 are various radicals, and Y and Z are monoatomic bridge elements.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: December 7, 2004
    Assignee: Aventis CropScience GmbH
    Inventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Hermann Bieringer, Thomas Auler, Hubert Menne
  • Patent number: 6825225
    Abstract: The present invention provides compounds of formula I useful as anti microbial agents wherein X, Y, R1, and n are as defined in thereof.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: November 30, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael J. Genin, Michael Robert Barbachyn, Jackson B. Hester, Jr., Paul D. Johnson, Fred L. Ciske
  • Patent number: 6809107
    Abstract: This invention provides compounds having the following general structures: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.
    Type: Grant
    Filed: June 14, 2000
    Date of Patent: October 26, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Ramesh M. Kanojia, Alfonzo D. Jordan, Allen B. Reitz, Mark J. Macielag, Boyu Zhao
  • Patent number: 6806369
    Abstract: PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: November 5, 2002
    Date of Patent: October 19, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Kelly M. Aubart, Siegfried B. Christensen, IV, Jacques Briand, Maxwell David Cummings
  • Publication number: 20040204463
    Abstract: The present invention provides antibacterial agents having the formula I described herein.
    Type: Application
    Filed: March 5, 2004
    Publication date: October 14, 2004
    Inventor: Christina Renee Harris
  • Patent number: 6800654
    Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are eachH, alkyl,, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: October 5, 2004
    Assignee: Wyeth
    Inventors: Scott Christian Mayer, Eric Gould Gundersen, Hassan Mahmoud Elokdah, David LeRoy Crandall
  • Publication number: 20040176610
    Abstract: The present invention provides antibacterial agents of formula I described herein and intermediates for their preparation.
    Type: Application
    Filed: January 22, 2004
    Publication date: September 9, 2004
    Inventor: Toni-Jo Poel
  • Patent number: 6784287
    Abstract: Organic dye molecular materials prepared by coupling existing organic chromophore molecules to benzene or carbazole derivatives and nonlinear optical polymeric compounds having polyimide repeating units coupled with the organic dye molecular material are provided. The organic dye molecular material coupled to a polymer main chain in the preparation of the nonlinear optical polymeric compound has one of the following formula: where X1 is carbon, oxygen, sulfur, nitrogen, ester (CO2), or amide (CONR1), where R1 is an alky or phenyl group having 1 to 6 carbon atoms, D is an organic chromophore molecule, and n is an integer from 1 to 10.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: August 31, 2004
    Assignee: Electronics and Telecommunications Research Institute
    Inventors: Jung Yun Do, Myung Hyun Lee, Seung Koo Park, Jung Jin Ju, Suntak Park
  • Patent number: 6784199
    Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, isoxazolidine compounds which have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the isoxazolidine compounds are also taught.
    Type: Grant
    Filed: September 21, 2001
    Date of Patent: August 31, 2004
    Assignee: Aryx Therapeutics
    Inventors: Pascal Druzgala, Peter G. Milner
  • Publication number: 20040147760
    Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.
    Type: Application
    Filed: August 22, 2003
    Publication date: July 29, 2004
    Inventors: Richard Charles Thomas, Toni-Jo Poel, Michael Robert Barbachyn, Mikhail Fedor Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh, Vara Prasad Venkata Nagendra Josyula
  • Publication number: 20040142939
    Abstract: The present invention provides antibacterial agents having the formula I described herein.
    Type: Application
    Filed: November 19, 2003
    Publication date: July 22, 2004
    Inventors: Jackson Boling Hester, Christina R. Harris
  • Publication number: 20040116413
    Abstract: The present invention provides compounds of formula I useful as antimicrobial agents 1
    Type: Application
    Filed: November 14, 2001
    Publication date: June 17, 2004
    Inventors: Michael J. Genin, Michael Robert Barbachyn, Jackson B. Hester, Paul D. Johnson, Fred L. Ciske
  • Publication number: 20040110749
    Abstract: An isoxazoline derivative represented by the following general formula [I]: 1
    Type: Application
    Filed: December 22, 2003
    Publication date: June 10, 2004
    Inventors: Masao Nakatani, Ryotaro Kugo, Masahiro Miyazaki, Koichiro Kaku, Makoto Fujinami, Ryohei Ueno, Satoru Takahashi
  • Patent number: 6746989
    Abstract: The invention relates to novel substituted benzoylpyrazoles of the general formula (I), in which n represents the numbers 0, 1, 2 or 3, A represents a single bond or represents alkanediyl(alkylene), R1 represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkoxycarbonyl or cycloalkyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl, Y represents hydrogen or represents in each case optionally substituted
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: June 8, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Hans-Georg Schwarz, Heinz-Jürgen Wroblowsky, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
  • Publication number: 20040087552
    Abstract: Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Application
    Filed: July 17, 2003
    Publication date: May 6, 2004
    Inventors: Jeffrey J Hale, Charles G. Caldwell, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Malcolm MacCoss, Amy Gentry, Christopher L. Lynch, Christopher A. Willoughby, Yuan Cheng
  • Publication number: 20040065869
    Abstract: Organic dye molecular materials prepared by coupling existing organic chromophore molecules to benzene or carbazole derivatives and nonlinear optical polymeric compounds having polyimide repeating units coupled with the organic dye molecular material are provided.
    Type: Application
    Filed: October 3, 2003
    Publication date: April 8, 2004
    Inventors: Jung Yun Do, Myung Hyun Lee, Seung Koo Park, Jung Jin Ju, Suntak Park
  • Publication number: 20040065870
    Abstract: Organic dye molecular materials prepared by coupling existing organic chromophore molecules to benzene or carbazole derivatives and nonlinear optical polymer compounds having polyimide repeating units coupled with the organic dye molecular material are provided.
    Type: Application
    Filed: October 3, 2003
    Publication date: April 8, 2004
    Inventors: Jung Yun Do, Myung Hyun Lee, Seung Koo Park, Jung Jin Ju, Suntak Park
  • Patent number: 6713507
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: March 30, 2004
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Patent number: 6703422
    Abstract: The present invention relates to novel sulfide and disulfide compounds, compositions comprising sulfide and disulfide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: March 9, 2004
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Publication number: 20040044052
    Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.
    Type: Application
    Filed: February 24, 2003
    Publication date: March 4, 2004
    Inventors: Richard Charles Thomas, Toni-Jo Poel, Michael Robert Barbachyn, Mikhail F. Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh
  • Patent number: 6699910
    Abstract: The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: March 2, 2004
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Patent number: 6696475
    Abstract: The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: February 24, 2004
    Assignee: NeuroSearch A/S
    Inventors: Bjarne H. Dahl, Palle Christophersen
  • Patent number: 6693124
    Abstract: Bisimino-substituted phenyl compounds of the formula I where the substituents have the following meanings: X is a group A or B  where # denotes the bond with the phenyl ring and Ra is halogen, alkyl or alkoxy; Y is halogen, alkyl, haloalkyl or alkoxy; n is 0, 1 or 2, it being possible for the radicals Y to be different if n=2; R1 is alkyl; R2 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl; R3 is hydrogen, alkyl, haloalkyl or substituted or unsubstituted phenyl; R4 is ═CRbRc or ═N—ORd where Rb, Rc independently of one another are hydrogen, alkyl or substituted or unsubstituted phenyl; and Rd is one of the radicals mentioned under R2. Processes and intermediates for their preparation, and their use.
    Type: Grant
    Filed: December 6, 1999
    Date of Patent: February 17, 2004
    Assignee: BASF Aktiengesellschaft
    Inventors: Wassilios Grammenos, Herbert Bayer, Thomas Grote, Hubert Sauter, Andreas Gypser, Reinhard Kirstgen, Bernd Müller, Arne Ptock, Franz Röhl, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
  • Publication number: 20040023999
    Abstract: Compounds of Formula (IA) and Formula (IB) 1
    Type: Application
    Filed: March 21, 2003
    Publication date: February 5, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Rajashehar Betageri, Mario G. Cardozo, Thomas A. Gilmore, Christian Hanke Justus Joachim Harcken, Thomas M. Kirrane, Daniel Kuzmich, John Robert Proudfoot, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell, Hossein Razavi
  • Patent number: 6683104
    Abstract: Urea compounds disclosed herein increase HDL-C levels and as such can be used in prevention and treatment of atherosclerosis, myocardial infarction and related conditions such as peripheral vascular disease and ischemic stroke hypoalphalipoproteinemia.
    Type: Grant
    Filed: June 12, 2003
    Date of Patent: January 27, 2004
    Assignee: A.P. Group, Inc.
    Inventor: Jennifer H. Zhang
  • Patent number: 6677360
    Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
    Type: Grant
    Filed: April 6, 2001
    Date of Patent: January 13, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
  • Patent number: 6667421
    Abstract: This invention relates to a process for the production of an aryl thiol, which comprises hydrogenating an aryl sulfonyl chloride in a solvent in the presence of a palladium catalyst and a base whose conjugate acid has a pKa of about 2 or greater, wherein the base is selected from the group consisting of ionic bases soluble in water and tertiary amines soluble in the solvent, the tertiary amines not having a methyl group attached to the amine nitrogen.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: December 23, 2003
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Stephen E. Jacobson
  • Publication number: 20030232812
    Abstract: The present invention provides a compound of formula I 1
    Type: Application
    Filed: January 21, 2003
    Publication date: December 18, 2003
    Inventors: Mikhail F. Gordeev, Adam Renslo, Gary W. Luehr, Stuart Lam, Neil E. Westlund, Dinesh V. Patel
  • Publication number: 20030232810
    Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.
    Type: Application
    Filed: December 3, 2002
    Publication date: December 18, 2003
    Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • Publication number: 20030212116
    Abstract: A heterocyclic imino compound of the formula (1) and an agrochemically acceptable salt thereof; and an agricultural chemical, fungicide and insecticide containing at least one member selected from the group of such compounds as an active ingredient: 1
    Type: Application
    Filed: June 25, 2002
    Publication date: November 13, 2003
    Inventors: Toshio Niki, Takashi Mizukoshi, Hiroaki Takahashi, Jun Satow, Tomoyuki Ogura, Kazuhiro Yamagishi, Hiroyuki Suzuki, Fumio Hayasaka
  • Publication number: 20030201713
    Abstract: In various embodiments, chromophores are described that include novel electron acceptors, novel electron donors, and/or novel conjugated bridges that are useful in nonlinear optical applications. In some embodiments, the present invention provides chromophore architectures wherein a chromophore contains more than one electron acceptor in electronic communication with a single electron donor, and/or more than one electron donor in electronic communication with a single electron acceptor. Also described is processes for providing materials comprising the novel chromophores and polymer matrices containing the novel chromophores. Electro-optic devices described herein contain one or more of the described electron acceptors, electron donors, conjugated bridges, or chromophores.
    Type: Application
    Filed: March 13, 2003
    Publication date: October 30, 2003
    Inventors: Diyun Huang, Tim Londergan, Galina K. Todorova, Jingsong Zhu
  • Patent number: 6624311
    Abstract: The present invention relates to a process for the enantioselective enzymatic aminolysis of racemic 2-[3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl]acetate ((R/S)-I) by methyl N&agr;-Boc-L-&agr;,&bgr;-diaminoproprionate.p-toluenesulfonic acid. More specifically, this invention pertains to a process for the enantioselective enzymatic aminolysis of racemic isobutyl 2-[3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl]-acetate by methyl N&agr;-Boc-L-&agr;,&bgr;-diaminoproprionate.p-toluene sulfonic acid to produce (R)-methyl-3-[[[3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl]acetyl]amino]-N-(butoxycarbonyl)-L-alanine, an intermediate in the preparation of roxifiban, an isoxazoline-based platelet glycoprotein IIb/IIIa antagonist which has activity as an antithrombotic agent.
    Type: Grant
    Filed: October 25, 2001
    Date of Patent: September 23, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Robert DiCosimo, Philip Ma, Jaan A. Pesti
  • Patent number: 6624167
    Abstract: Pharmaceutical compositions incorporate compounds that are capable of affecting nicotinic cholinergic receptors. A wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic nervous systems can be treated using pharmaceutical compositions incorporating compounds in which an aromatic ring is bridged with an ethylenic or acetylenic unit to an azabicyclic moiety.
    Type: Grant
    Filed: August 4, 2000
    Date of Patent: September 23, 2003
    Assignee: Targacept, Inc.
    Inventors: Thomas Jeffrey Clark, Balwinder Singh Bhatti
  • Publication number: 20030165640
    Abstract: The present invention provides filters for an electronic display device comprising a squarylium compound represented by the general formula (I): 1
    Type: Application
    Filed: January 22, 2003
    Publication date: September 4, 2003
    Applicant: Kyowa Yuka Co., Ltd.
    Inventors: Ikuo Shimizu, Motoharu Kinugasa, Hiroshi Toyoda, Shiho Yamada
  • Publication number: 20030162958
    Abstract: A process for preparing a heteroaromatic compound having a heteroaromatic nucleus substituted with one or more ether groups comprising the step of: condensing at least one hydroxy-group of a compound having said heteroaromatic nucleus, said at least one hydroxy group (—OH) being substituted at &agr;- or &bgr;-positions with respect to a heteroatom of said heteroaromatic nucleus, with an alcohol containing one or more primary or secondary alcohol groups, optionally substituted with nitro, amide, ester, halogen, cyano or (hetero)aromatic groups, using the redox couple of a triaryl- or trialkylphosphine and an azodioxo-compound at a temperature between −40° C. and 160° C.
    Type: Application
    Filed: December 20, 2002
    Publication date: August 28, 2003
    Applicant: AGFA-GEVAERT
    Inventors: John R. Reynolds, Bert Groenendaal, Kyukwan Zong, Luis Madrigal
  • Patent number: 6610687
    Abstract: The invention relates to benzofuranylsulfonates of the general formula (I), their preparation and their use for the treatment of inflammation.
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: August 26, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gabriele Bräunlich, Mazen Es-Sayed, Rüdiger Fischer, Burkhard Fugmann, Rolf Henning, Stephan Schneider, Michael Sperzel, Karl-Heinz Schlemmer, Graham Sturton, Mary F. Fitzgerald, Barbara Briggs, Arnel Concepcion, William Bullock