Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Acyclic Nitrogen Patents (Class 546/265)
  • Patent number: 7375100
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Grant
    Filed: June 3, 2004
    Date of Patent: May 20, 2008
    Assignee: Pfizer Inc
    Inventors: Alan Daniel Brown, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite
  • Patent number: 7371747
    Abstract: The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: May 13, 2008
    Assignee: Merck Frosst Canada & Co.
    Inventors: Cameron Black, Sheldon N. Crane, Dana Davis, Eduardo L. Setti
  • Patent number: 7338950
    Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Grant
    Filed: October 7, 2004
    Date of Patent: March 4, 2008
    Assignee: Renovis, Inc.
    Inventors: Michael G. Kelly, Satyanarayana Janagani, Guoxian Wu, John Kincaid
  • Patent number: 7332608
    Abstract: The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds 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. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: February 19, 2008
    Assignee: SANOFI-AVENTIS Deutschland GmbH
    Inventors: Joachim Brendel, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • Patent number: 7262210
    Abstract: The present invention describes compounds of Formula I or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal. The present invention also relates to a novel method of N-oxidation of nitrogen containing heteroaryls.
    Type: Grant
    Filed: March 21, 2006
    Date of Patent: August 28, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kevin Kreutter, Tianbao Lu, Yu Kai Lee, Christopher Teleha, Mark Player, Xizhen Zhu
  • Patent number: 7262209
    Abstract: The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.
    Type: Grant
    Filed: October 2, 2002
    Date of Patent: August 28, 2007
    Assignee: Novartis Animal Health US, Inc.
    Inventors: Thomas Goebel, Pierre Ducray
  • Patent number: 7241745
    Abstract: The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: July 10, 2007
    Assignee: Astellas Pharma GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
  • Patent number: 7235690
    Abstract: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds 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. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: June 26, 2007
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • Patent number: 7169779
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: September 8, 2003
    Date of Patent: January 30, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Francesco Salituro, Guy Bemis, Huai Gao, Ghotas Evindar
  • Patent number: 7074742
    Abstract: Compounds of Formula (I), their N-oxides and agriculturally suitable salts are disclosed which are useful as fungicides formula (I), (II) wherein A is a substituted pyridinyl ring; B is a substituted pyridinyl ring; W is C=L or SOn is O or S; R1 and R2 are each independently H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, each optionally substituted; R3 is H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl or C3-C8 dialkylaminocarbonyl; R4 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, each optionally substituted; X is O or S; and n is 1 or 2; provided that when W is C?O and R1, R2 and R3 are H; then B is other than 4-trifluoromethyl-3-pyridinyl, 2-chloro-4-pyridinyl and 2,6-dihalo-4-pyridinyl.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: July 11, 2006
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Timothy Donald Neubert, David Walter Piotrowski, Michael Paul Walker
  • Patent number: 7057067
    Abstract: The present invention provides a process for producing 2-halobenzoic acids of the general formula (I), characterized by reacting a benzoic acid of formula (II) with a halogenating agent in the presence of Pd catalyst: (wherein A is —OH, —OM (M is alkali metal), —N(R6)R7 (R6 and R7 are each H, C1–C6 alkyl, optionally substituted phenyl, or the like); R is H, C1–C6 alkyl, C1–C6 alkylcarbonyl, carboxyl, C1–C12 alkoxycarbonyl, optionally substituted phenylcarbonyl, or the like; n is 0 to 4; X is Cl, Br or I, or alternatively (R)n may be present on benzene-constituting carbon atoms adjacent to each other and form a C3–C4 alkylene- or C3–C4 alkenylene-fused ring).
    Type: Grant
    Filed: April 27, 2001
    Date of Patent: June 6, 2006
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Hiroki Kodama, Takeshi Katsuhira, Tateki Nishida, Tomokazu Hino, Kenji Tsubata
  • Patent number: 6875764
    Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I): where Y is S or O and R is as defined in the specification.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: April 5, 2005
    Assignee: New Pharma Research Sweden AB
    Inventors: Sabrina Muzi, Shoaá Abdul Rahman
  • Patent number: 6833378
    Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.
    Type: Grant
    Filed: January 17, 2001
    Date of Patent: December 21, 2004
    Assignee: Pfizer Inc
    Inventor: Yuhpyng L. Chen
  • Patent number: 6831080
    Abstract: There is provided novel cinnamide derivatives of Formula I: wherein R is C1-4 alkyl or trifluoromethyl; R1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, chromanyl, indanyl, biphenylyl, phenyl and substituted phenyl in which said substituted phenyl is substituted with one or two substituents each independently selected-from the group consisting of halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy and nitro; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-4 alkyl, and halogen; R4 is selected from the group consisting of di(C1-4 alkyl)amino, trifluoromethoxy and optionally substituted morpholin-4-yl, pyridinyl, pyrimidinyl, piperazinyl, and pyrazinyl with one or two substituents in which said substituent is independently selected from the group consisting of C1-4 alkyl, aminomethyl, hydroxymethyl, chloro or fluoro; R5 is hydrogen, chloro or fluoro; or R4 and R5 taken t
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: December 14, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Li-Quang Sun, Jie Chen, Huan He, Alexandre L'Heureux, Pierre Dextraze, Jean-Paul Daris, Gene G. Kinney, Steven I. Dworetzky, Piyasena Hewawasam
  • Patent number: 6726854
    Abstract: An inhibitor mixture containing, as components, a) at least one nitroxyl radical (derivative), b) at least one phenol (derivative) and c) at least one chemical compound which contains at least one phosphorus atom which has the oxidation state +3 is preferably used for stabilizing compounds capable of free radical polymerization.
    Type: Grant
    Filed: July 25, 2002
    Date of Patent: April 27, 2004
    Assignee: BASF Aktiengesellschaft
    Inventors: Heinz Friedrich Sutoris, Gerhard Wagenblast, Volker Schliephake, Jürgen Schröder, Harald Keller, Thomas Jaworek
  • Patent number: 6716860
    Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: April 6, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Lauffer, Michael Mullican
  • Patent number: 6677359
    Abstract: The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Grant
    Filed: January 3, 2002
    Date of Patent: January 13, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Lauffer, Brian Ledford, Michael Mullican
  • Patent number: 6610701
    Abstract: Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.
    Type: Grant
    Filed: February 8, 2002
    Date of Patent: August 26, 2003
    Assignee: Merck & Co., Inc.
    Inventors: James C. Barrow, Craig Coburn, Harold G. Selnick, Phung L. Ngo
  • Patent number: 6586466
    Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
    Type: Grant
    Filed: April 20, 2001
    Date of Patent: July 1, 2003
    Assignee: SmithKline Beecham Corporation
    Inventor: Dennis Shinji Yamashita
  • Patent number: 6586459
    Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: July 1, 2003
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Junior, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6583173
    Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: June 24, 2003
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffrey Bernard Franciskovich, Theodore Goodson, Junior, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6576642
    Abstract: Compounds having the formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyindeny, pyridyl, indolyl,isoindolyl, quinolyl or isoquinolyl group which are optionally substituted; X is optionally substituted alicyclic, aromatic, imino or heterocyclic groups or —S— or —O—; Y is a single bond or an alkylene group; Z is an unsubstituted aliphatic group or divalent residue of benzene or pyridine, which is optionally substituted; anis hydrogen, lower alkyl, cycloalkyl, aryl or aralkyl; with certain provisos. These compounds exhibit an inhibitory effect on the production of IgE antibodies and are, hence, useful as antiallergic agents.
    Type: Grant
    Filed: May 17, 2001
    Date of Patent: June 10, 2003
    Assignee: Kowa Co., Ltd.
    Inventors: Hiroyuki Ishiwata, Mototsugu Kabeya, Masami Shiratsuchi, Yukio Hattori, Hiroshi Nakao, Takao Nagoya, Seiichi Sato, Soichi Oda, Makoto Suda, Manabu Shibasaki
  • Patent number: 6531495
    Abstract: Compounds of the formula I, in which R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(8), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel and antiarrythmic active compounds, in particular for the treatment and prophylaxis of atrial arrythmias, e.g. atrial fibrillation (AF), or atrial flutter.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: March 11, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Joachim Brendel, Wolfgang Schmidt, Peter Below
  • Publication number: 20030013857
    Abstract: Reagents and methods are provided for crosslinking and immobilizing biomolecules, drugs and synthetic polymers. The reagents possess (i) a thiol or amino reactive group; and (ii) a hydrazino or oxyamino moiety. Conjugates and immobilized biomolecules are also provided.
    Type: Application
    Filed: March 22, 2001
    Publication date: January 16, 2003
    Applicant: Solulink Incorporated
    Inventor: David A. Schwartz
  • Patent number: 6479519
    Abstract: The invention is directed to physiologically active compounds of formula (I): wherein: R1 is hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR10; and one of X3, X4 and X5 represents CR11 and the others independently represents N or CR10; where R10 is hydrogen, amino, halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, nitro or trifluoromethyl; and R11 represents a group —L1—Ar1—L2—Y; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).
    Type: Grant
    Filed: April 26, 2000
    Date of Patent: November 12, 2002
    Assignee: Aventis Pharma Limited
    Inventors: Peter Charles Astles, David Edward Clark, Alan John Collis, Paul Joseph Cox, Paul Robert Eastwood, Neil Victor Harris, Justine Yeun Quai Lai, Andrew David Morley, Barry Porter
  • Patent number: 6476056
    Abstract: An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are the same or different, and are each a substituted or unsubstituted phenyl group, a substituted or unsubstituted pyridyl group or a naphthyl group, provided that Ar1 and Ar2 are not both phenyl or both naphthyl and are not phenyl and naphthyl, R1 is a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, a substituted or unsubstituted phenyl group or a group of the formula: —NR2(R3) (wherein R2 and R3 are the same or different, and are each a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, X1 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a phenoxy group, a halogen atom, a trifluoromethyl group, a carbamoyl group or an aminosulfonyl group, Y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; and pharmaceutically acceptabl
    Type: Grant
    Filed: August 7, 2001
    Date of Patent: November 5, 2002
    Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.
    Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshio Nakamura, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Kenji Yamamoto, Koichiro Harada, Masanori Yoshida
  • Patent number: 6472414
    Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X,  are as defined herein.
    Type: Grant
    Filed: May 18, 1999
    Date of Patent: October 29, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
  • Patent number: 6451791
    Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: September 17, 2002
    Assignee: Monsanto Company
    Inventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
  • Patent number: 6407120
    Abstract: The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
    Type: Grant
    Filed: January 28, 2000
    Date of Patent: June 18, 2002
    Assignee: Pfizer Inc.
    Inventors: Philip A. Carpino, Marlys Hammond, Richard F. Hank
  • Patent number: 6391918
    Abstract: Novel &agr;-amino acid amides of formula (I) as well as possible isomers and mixtures of isomers thereof, wherein the substituents are defined as follows: n is the number zero or one; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; or a group NRaRb wherein Ra and Rb are each independently of the other hydrogen, alkyl or form together an alkylene bridge; R2 is hydrogen or alkyl; R3 is optionally substituted aryl or heteroaryl; A is alkylene; and B is optionally substituted aryl; with the exception of the following compounds 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methylphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-chlorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-nitrolphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methoxyphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-fluorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-phenyl-sulfonylamino-acetamide and 2-phenyl-N-(1-p
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: May 21, 2002
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: André Jeanguenat, Martin Zeller
  • Patent number: 6355805
    Abstract: The present invention is directed to multibinding compounds which are &bgr;3 adrenergic receptor agonists and are therefore useful in the treatment and prevention of metabolic disorders such as obesity, diabetes, and the like.
    Type: Grant
    Filed: June 8, 1999
    Date of Patent: March 12, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: Seok-Ki Choi, Edmund J. Moran
  • Patent number: 6331542
    Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: December 18, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Thomas Joseph Carr, Renee Louise Desjarlais, Timothy Francis Gallagher, Stacie Marie Halbert, Hye-Ja Oh, Scott Kevin Thompson, Daniel Frank Veber, Dennis Shinji Yamashita, Jack Hwekwo Yen
  • Patent number: 6329550
    Abstract: The present application relates to novel aminomalonamides of the formula and pharmaceutical composition thereof which are useful for inhibiting matrix metalloproteinases.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: December 11, 2001
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Alan M. Warshawsky, Michael J. Janusz
  • Patent number: 6313151
    Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: November 6, 2001
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6313148
    Abstract: Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a —CH(R3)N(R2)B—R1 and —OD groups positioned in a 1,2 relationship to one another on ring carbon atoms. The 3-position ring-atom is not substituted. B is an optionally-substituted pyridyl ring and the group R1 is positioned on B in a 1,3 or 1,4 relationship with the —CH(R3)N(R2)B- linking group. R1, R2 and R3 and D can be a number of different organic or halogen moieties. N-oxides of —NR2 and S-oxides of sulphur containing rings are disclosed as are processes for the preparation of the compounds, intermediates in their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: November 6, 2001
    Assignee: Zeneca Limited
    Inventor: Gloria Anne Breault
  • Patent number: 6297283
    Abstract: The present invention relates to compounds represented by the following general formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyl, indenyl, pyridyl, indolyl, isoindolyl, quinolyl or isoquinolyl group which may be substituted; X is a lower alkylene group which may be substituted, or the like; Y is a single bond or an alkylene group; Z is a group of —CH═CH—, —C≡C—, —(CH═CH)2—, —C≡C—CH═CH— or —CH═CH—C≡C—, or the like; and R is a hydrogen atom, a lower alkyl group or the like, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: October 2, 2001
    Assignee: Kowa Co., Ltd.
    Inventors: Hiroyuki Ishiwata, Mototsugu Kabeya, Masami Shiratsuchi, Yukio Hattori, Hiroshi Nakao, Takao Nagoya, Seiichi Sato, Soichi Oda, Makoto Suda, Manabu Shibasaki
  • Patent number: 6291491
    Abstract: Amide derivatives are selective &bgr;3 adrenergic receptor agonists with very little &bgr;1 and &bgr;2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
    Type: Grant
    Filed: October 12, 2000
    Date of Patent: September 18, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ann E. Weber, Emma R. Parmee, Robert Mathvink, Wallace T. Ashton, Elizabeth M. Naylor
  • Patent number: 6284777
    Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, inducing osteoporosis; gingival disease including gingivitis and periodontists; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: September 4, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Stacie Marie Halbert, Scott Kevin Thompson
  • Patent number: 6277865
    Abstract: This invention is directed to a compound of formula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
    Type: Grant
    Filed: March 22, 1999
    Date of Patent: August 21, 2001
    Assignee: Aventis Pharmaceuticals Products Inc.
    Inventors: Scott I. Klein, Kevin R. Guertin
  • Patent number: 6268384
    Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compounds and the compositions and methods that utilize them can be used, either alone or in conjunction with a neurotrophic factor, such as nerve growth factor, to promote repair of neuronal damage caused by disease or physical trauma.
    Type: Grant
    Filed: May 27, 1998
    Date of Patent: July 31, 2001
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Perry M. Novak, Michael Mullican
  • Patent number: 6211176
    Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 1, 1999
    Date of Patent: April 3, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 6194437
    Abstract: The compounds of the instant invention are novel compounds of Formula I or a pharmaceutically acceptable salt thereof wherein Ar is phenyl or pyridyl unsubstituted or substituted. Ar1 can be independently selected from Ar and can also include pyridyl-N-oxide, indolyl, imidazole, and pyridyl; R3 can be independently selected from Ar or is hydrogen, hydroxy, NMe2, N-methyl-pyrrole, imidazole, tetrazole, thiazole (a), (b), (c), or (d), wherein Ar2 is phenyl or pyridyl. The instant compounds antagonize the bombesin receptors in mammals and are therefore effective in treating and/or preventing depression, psychoses, seasonal affective disorders, cancer, feeding disorders, gastrointestinal disorders, inflammatory bowel disease, sleep disorders, and memory impairment.
    Type: Grant
    Filed: February 3, 1999
    Date of Patent: February 27, 2001
    Assignee: Warner-Lambert Company
    Inventors: David Christopher Horwell, Martyn Clive Pritchard
  • Patent number: 6184237
    Abstract: Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, suchas pain and diabetes. The inventin encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermedates useful in such processes.
    Type: Grant
    Filed: November 1, 1999
    Date of Patent: February 6, 2001
    Assignee: Amgen Inc.
    Inventors: Nathan B. Mantlo, Stephen T. Schlachter, John A. Josey
  • Patent number: 6133442
    Abstract: Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;R.sup.2 signifies phenyl or substituted phenyl;R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ;R.sup.4 signifies hydrogen or lower-alkyl;R.sup.5 signifies hydrogen or a residue R.sup.7, andR.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; orR.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue;R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl;R.sup.a signifies hydrogen, lower-alkyl or hydroxy;R.sup.b signifies hydrogen or lower-alkyl;Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --OC(O)OR.sup.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: October 17, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 6124332
    Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.
    Type: Grant
    Filed: February 3, 1999
    Date of Patent: September 26, 2000
    Assignee: British Biotech Pharmaceuticals Ltd.
    Inventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
  • Patent number: 6124333
    Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.
    Type: Grant
    Filed: February 3, 1999
    Date of Patent: September 26, 2000
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
  • Patent number: 6103761
    Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.
    Type: Grant
    Filed: October 19, 1994
    Date of Patent: August 15, 2000
    Assignee: Warner-Lambert Company
    Inventors: Bradley Dean Tait, Michael William Wilson
  • Patent number: 6015900
    Abstract: Disclosed are compounds of formula (I) or the pharmaceutically acceptable salts thereof wherein: ##STR1## G represents a group of the formula (a), (b) or (c) where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents; A is an optionally substituted alkylene; R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents; R.sub.5 is hydrogen or lower alkyl; R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members; Z is nitrogen or carbon; and W is optionally susbtituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.
    Type: Grant
    Filed: November 23, 1998
    Date of Patent: January 18, 2000
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 6002010
    Abstract: A process for preparing carboxylic acid derivatives of the formula I ##STR1## where X is OR.sup.2 or NH.sub.2,R.sup.1 is C.sub.1 -C.sub.20 -alkyl, C.sub.l -C.sub.20 -hydroxyalkyl, C.sub.3 -C.sub.12 -cycloalkyl, C.sub.4 -C.sub.12 -alkylcycloalkyl, C.sub.4 -C.sub.12 -cycloalkylalkyl, C.sub.5 -C.sub.20 -alkylcycloalkylalkyl, aryl, C.sub.7 -C.sub.20 -aralkyl, C.sub.7 -C.sub.20 -alkylaryl, a heteroaliphatic or heteroaromatic ring with 5 to 8 carbon atoms andR.sup.2 is C.sub.1 -C.sub.20 -alkyl,from carbonitriles of the formula IIR.sup.1 --C.tbd.N (II),where R.sup.1 has the abovementioned meanings, and alcohols of the formula IIIR.sup.2 --OH (III),where R.sup.2 has the abovementioned meanings, at from 50 to 300.degree. C. under from 0.1 to 350 bar in the presence of a heterogeneous catalyst, wherein the reaction is carried out in liquid phase.
    Type: Grant
    Filed: November 10, 1997
    Date of Patent: December 14, 1999
    Assignee: BASF Aktiengesellschaft
    Inventor: Eberhard Fuchs
  • Patent number: 5962682
    Abstract: Compounds of formula (I) ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl; R.sup.2 signifies phenyl or substituted phenyl; R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ; R.sup.4 signifies hydrogen or lower-alkyl; R.sup.5 signifies hydrogen or a residue R.sup.7, and R.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; or R.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue; R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl; R.sup.a signifies hydrogen, lower-alkyl or hydroxy; R.sup.b signifies hydrogen or lower-alkyl; Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.
    Type: Grant
    Filed: August 18, 1997
    Date of Patent: October 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz