Acyclic Nitrogen Bonded Directly To The Carbonyl Patents (Class 546/323)
  • Publication number: 20090131468
    Abstract: The invention provides compounds of formula wherein R1, R2, R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
    Type: Application
    Filed: November 14, 2008
    Publication date: May 21, 2009
    Applicant: AstraZeneca AB
    Inventors: Johan Bylund, Marie E. Ek, Annika Kers, Gunnar Nordvall, Liselotte Ohberg, Jenny Viklund, Stefan Von Berg, Jorg Holenz, Katja Narhi, Daniel Sohn, Martin H. Johansson
  • Publication number: 20090131441
    Abstract: Metabolites of 2-(R)-4-isobutylarylpropionamides and pharmaceutical compositions containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
    Type: Application
    Filed: January 24, 2006
    Publication date: May 21, 2009
    Applicant: DOMPE phar.r.ma S.p.A.
    Inventors: Riccardo Bertini, Cinzia Bizzarri, Marco Mosca, Marcello Allegretti, Francesco Colotta
  • Publication number: 20090111983
    Abstract: Cycloalkylcarbonylamino acid derivatives, which are raw material intermediates of a novel cycloalkane carboxamide derivative that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkylcarbonylamino acid derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: (wherein, R1 and R2 represent alkyl groups, alkenyl groups, alkynyl groups, aromatic hydrocarbon groups, heterocyclic groups or the like, and ring A represents a cyclic alkylidene group having 5, 6 or 7 carbon atoms).
    Type: Application
    Filed: July 10, 2007
    Publication date: April 30, 2009
    Applicant: SEIKAGAKU CORPORATION
    Inventors: Nobuo Kobayashi, Tsuneo Koji, Hisatomo Kunii
  • Patent number: 7507836
    Abstract: The present invention is directed to compounds which are allosteric modulators of metabotropic glutamate receptors, including the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: March 22, 2004
    Date of Patent: March 24, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Mark E. Duggan, Craig W. Lindsley, David D. Wisnoski
  • Publication number: 20090062341
    Abstract: The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
    Type: Application
    Filed: November 28, 2006
    Publication date: March 5, 2009
    Inventors: James T. Dalton, Christina Barrett, Yali He, Seoung-Soo Hong, Duane D. Miller, Michael L. Mohler, Ramesh Narayanan, Zhongzhi Wu
  • Publication number: 20080300240
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. The compounds have the general structure: wherein m, n, p, x, R, R1, R2, R3, R4, R5, A and B, are defined herein, including pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE 10 in a warm-blooded animal in need of the same.
    Type: Application
    Filed: May 20, 2008
    Publication date: December 4, 2008
    Applicant: Omeros Corporation
    Inventors: John E. Bergmann, Neil S. Cutshall, Rene Onrust, Hongkui Zeng, Jennifer Lynn Gage, Derek Johnston, Sandor Cseh, Laszlo Urogdi, Akos Papp
  • Patent number: 7459585
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: December 2, 2008
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Publication number: 20080293680
    Abstract: The invention relates to a compound of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are defined as in the specification and claims and to its use for treating or preventing Alzheimer's disease and other similar diseases.
    Type: Application
    Filed: August 1, 2006
    Publication date: November 27, 2008
    Inventors: Stefan Peters, Christian Eickmeier, Klaus Fuchs, Werner Stransky, Cornelia Dorner-Ciossek, Marcus Kostka, Sandra Handschuh, Herbert Nar, Klaus Bornemann, Klaus Klinder, Margit Bauer
  • Patent number: 7449485
    Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: November 11, 2008
    Assignee: Abbott Laboratories Inc.
    Inventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
  • Publication number: 20080249313
    Abstract: The invention relates to a process for the preparation of pyridylcarboxylic amides and esters I, Formula (I) wherein Hal, X and R1 have the meanings given in claim 1, which comprises the following steps: (a) heating a mixture consisting essentially of trichloromethylpyridine II, Formula (II), wherein Hal has the meaning given, and 1.0 to 1.5 equivalents of concentrated sulfuric acid, characterized in that the trichloromethylpyridine II in a liquid form is added to the concentrated sulfuric acid at a temperature from 110° C. to 160° C.; and (b) reacting the intermediate product obtained in step (a) with an amine or alcohol III, HXR1, wherein X and R1 have the meaning given, optionally in the presence of a solvent and/or a base.
    Type: Application
    Filed: October 26, 2006
    Publication date: October 9, 2008
    Applicant: BASF SE
    Inventors: Monika Brink, Marcus Knell, Jan Hendrik Wevers
  • Publication number: 20080249139
    Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
    Type: Application
    Filed: May 30, 2007
    Publication date: October 9, 2008
    Inventors: Jose Aquino, Varghese John, John Tucker, Roy Hom, Shon Pulley, Ruth Tenbrink
  • Publication number: 20080249140
    Abstract: A novel group of anti-inflammatory compounds are salts composed of the anion of a nonsteroidal anti-inflammatory acid drug (NSAID) and the cation N(1)-methylnicotinamide, which both anion and cation moieties alone exhibit anti-inflammatory activity, and which in this combination have advantages over the individual compounds and in comparison to commercial anti-inflammatory products. The compounds are produced in analogy to processes known in the art. They are used for the preparation of new pharmaceutical formulations with anti-inflammatory and analgesic activity. The new pharmaceutical formulations exhibit several advantageous properties over preparations of prior art.
    Type: Application
    Filed: November 29, 2006
    Publication date: October 9, 2008
    Inventor: Jacques Gosteli
  • Patent number: 7414060
    Abstract: The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for treating CNS disorders.
    Type: Grant
    Filed: February 23, 2006
    Date of Patent: August 19, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
  • Publication number: 20080161365
    Abstract: This invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof; a pharmaceutical composition; a method of treating a disease mediated by an MMP-13 enzyme in a mammal; and a therapeutic combination containing at least two pharmaceutically active components, wherein R1, Q, W1, W2, W2a, R3a, R3b, L1, and L2, the pharmaceutical composition, the method of treating, and the therapeutic combination are as defined in the specification.
    Type: Application
    Filed: December 5, 2005
    Publication date: July 3, 2008
    Applicant: PFIZER INC.
    Inventors: Richard J. Booth, Patrick Michael O'Brien
  • Patent number: 7388008
    Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.
    Type: Grant
    Filed: August 2, 2004
    Date of Patent: June 17, 2008
    Assignee: Ambrilia Biopharma Inc.
    Inventors: Brent Richard Stranix, Valérie Perron
  • Patent number: 7384945
    Abstract: Provided are compounds of the formula I: and pharmaceutically acceptable salts thereof, processes for making said compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compound and pharmaceutically acceptable salts thereof, and methods of using said compounds. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.
    Type: Grant
    Filed: October 25, 2005
    Date of Patent: June 10, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Matthias Heinrich Nettekoven, Philippe Pflieger, Stephan Roever
  • Patent number: 7378448
    Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed
    Type: Grant
    Filed: March 2, 2005
    Date of Patent: May 27, 2008
    Assignee: Eli Lilly and Company
    Inventors: Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
  • Publication number: 20080119526
    Abstract: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of: wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: where RN? is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm alkylene-R2 and the other of RP3
    Type: Application
    Filed: December 5, 2007
    Publication date: May 22, 2008
    Applicant: PHARMAGENE LABORATORIES LIMITED
    Inventors: Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton
  • Patent number: 7351825
    Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: April 1, 2008
    Assignee: Japan Tobacco Inc.
    Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
  • Publication number: 20080058389
    Abstract: The invention relates to novel carboxamides of formula (I), in which M represents a phenyl ring, pyridine ring or pyrimidine, pyridazine or pyrazine ring, respectively monosubstituted by R8, or represents a thiazole ring substituted by R8-A; R8 represents hydrogen, fluorine, chlorine, methyl, isopropyl, methylthio or trifluoromethyl; R8 can also represent methoxy; R8-A represents hydrogen, methyl, methylthio or trifluoromethyl; L1 represents C1-C10 alkene (alkanediyl); Q represents O, S, SO, SO2 or NR9; L2 represents a direct bond, SiR10R11 or CO; R represents hydrogen, C1-C8 alkyl, C1-C8 alkoxy, C1-C4 alkoxy-C1-C4-alkyl, C1-C4 alkylthio-C1-C4-alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C1-C6 haloalkyl, C2-C6-haloalkenyl, C2-C6 haloalkynyl or C3-C6 cycloalkyl; A represents the group of formula (AI); the remaining substituents are defined in claim 1.
    Type: Application
    Filed: January 22, 2005
    Publication date: March 6, 2008
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Benoit Hartmann, Jorg Nico Greul, Stefan Herrmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
  • Patent number: 7320993
    Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: January 22, 2008
    Assignee: Astellas Deutschland GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
  • Patent number: 7223774
    Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
    Type: Grant
    Filed: April 21, 2004
    Date of Patent: May 29, 2007
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Jose Aquino, Varghese John, John Tucker, Roy Hom, Shon Pulley, Ruth Tenbrink
  • Patent number: 7166590
    Abstract: A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO, OCO, O, S, SO, SO2 etc.; R3 is (substituted) alkyl, carbocyclic ring, hetero ring; J is O, NR16 (R16 is H, substituted alkyl); R4 is (substituted) alkyl, carbocyclic ring, hetero ring.] or non-toxic salt thereof, and an N-type calcium channel blocker comprising it as an active ingredient. The compounds of the formula (I) possess an inhibitory action on N-type calcium channel, so they are useful as agent for the prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis or epilepsy etc. or agent for the treatment of pain.
    Type: Grant
    Filed: May 28, 2002
    Date of Patent: January 23, 2007
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Takuya Seko, Masashi Kato
  • Patent number: 7153869
    Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.
    Type: Grant
    Filed: March 12, 2004
    Date of Patent: December 26, 2006
    Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
  • Patent number: 7071219
    Abstract: Mono-acylated o-phenylendiamines derivatives of formula A wherein Ar, R1, and R2 are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as cancer.
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: July 4, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
  • Patent number: 7071175
    Abstract: The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds: to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.
    Type: Grant
    Filed: May 3, 2000
    Date of Patent: July 4, 2006
    Assignee: Astrazeneca AB
    Inventors: Marcel Linschoten, Magnus Polla
  • Patent number: 7015237
    Abstract: Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.
    Type: Grant
    Filed: May 10, 2004
    Date of Patent: March 21, 2006
    Assignee: Warner-Lambert Company
    Inventors: Nicole Chantel Barvian, David Thomas Connor, Patrick Michael O'Brien, Daniel Fred Ortwine, William Chester Patt, Michael William Wilson
  • Patent number: 6995178
    Abstract: This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein A, B, J, R1, R2, R3 and R4 and n are as defined in the disclosure. Also disclosed are methods for controlling arthropods comprising contacting the arthropods or their environment with an arthropodicidally effective amount of a compound of Formula 1 and compositions containing the compounds of Formula 1.
    Type: Grant
    Filed: October 31, 2003
    Date of Patent: February 7, 2006
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: George P. Lahm, Brian J. Myers, Thomas P. Selby, Thomas M. Stevenson
  • Patent number: 6992095
    Abstract: The invention relates to novel stilbene compounds having the general formula (I): as well as to pharmaceutical compositions for use in human or veterinary medicine, including dermatological, rheumatic, respiratory, cardiovascular and ophthalmic conditions and cosmetic compositions and methods of use thereof.
    Type: Grant
    Filed: October 2, 2003
    Date of Patent: January 31, 2006
    Assignee: Galderma Research & Development, S.N.C.
    Inventors: Jean-Michel Bernardon, Bruno Charpentier
  • Patent number: 6953798
    Abstract: Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra?)R??(1) Ar1 is an optionally substituted aromatic or heteroarotic group; L1 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of ?4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: October 11, 2005
    Assignee: Celltech R&D Limited
    Inventors: John Robert Porter, John Clifford Head, Graham John Warrellow, Sarah Catherine Archibald
  • Patent number: 6949556
    Abstract: The present invention relates to compounds of general formula (I), wherein R1-R4 have the meanings given in the specification, A is CH2, CHOH or CH—(C1-C3-alkyl), B and C are independently CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group optionally substituted by the substituents listed in the specification.
    Type: Grant
    Filed: February 13, 2002
    Date of Patent: September 27, 2005
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Hartmut Strobel, Paulus Wohlfart
  • Patent number: 6949539
    Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
    Type: Grant
    Filed: June 1, 2001
    Date of Patent: September 27, 2005
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Mark Furber
  • Patent number: 6936719
    Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: August 30, 2005
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
  • Patent number: 6933298
    Abstract: Pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides of formula I. These compounds are found to possess the property of selectively inhibiting collagenase (MMP). They may therefore be useful in prophylaxis and therapy of diseases whose course involves an increased activity of matrix metalloproteinase 13.
    Type: Grant
    Filed: December 9, 2002
    Date of Patent: August 23, 2005
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Klaus-Ulrich Weithmann, Jörg Habermann, Herbert Kogler, Reinhard Kirsch, Volkmar Wehner
  • Patent number: 6894168
    Abstract: Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1—Y2 represents (R4)C?C(R5), (R6)C?N, N?N, (R7) N—CO, or N?C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.
    Type: Grant
    Filed: January 21, 2003
    Date of Patent: May 17, 2005
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Kazuyuki Tomisawa
  • Patent number: 6806365
    Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: October 19, 2004
    Assignee: Hoffmann-La Rocher Inc.
    Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
  • Patent number: 6780874
    Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in, which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
    Type: Grant
    Filed: June 10, 2003
    Date of Patent: August 24, 2004
    Assignee: Celltech R & D Limited
    Inventors: Timothy John Norman, John Robert Porter, Brian Woodside Hutchinson, Andrew James Ratcliffe, John Clifford Head, Rikki Peter Alexander, Barry John Langham, Graham John Warrellow, Sarah Catherine Archibald, Janeen Marsha Linsley
  • Patent number: 6747041
    Abstract: Heterocyclic dicarboxylic acid diamide derivative represented by the general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Het represents a 5- or 6-membered heterocycle; X and Y represent each halocyano, nitro, optionally halogenated C3-6, cycloalkyl, optionally substituted phenyl, an optionally substituted heterocycle, etc; n is from 0 to 3; m is from 1 to 5; Z1 and Z2 represent each O or S; and B1 to B4 represent each C or N. Agricultural/horticultural insecticides having an excellent controlling effect on pest insects such as diamond-back moth (Pluntella xylostella) and tobacco cutworm (Spodoptera litura).
    Type: Grant
    Filed: April 10, 2002
    Date of Patent: June 8, 2004
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Takeshi Katsuhira, Takashi Furuya, Makoto Gotoh, Masanori Tohnishi, Hideo Takaishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
  • Patent number: 6720425
    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: December 9, 2002
    Date of Patent: April 13, 2004
    Assignee: Allergan, Inc.
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 6703379
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: March 9, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Patent number: 6642252
    Abstract: Compounds having the formula (I), are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, IXa, Xa, and/or XIa, wherein ring B is phenyl or pyridyl, W is preferably C(═O)NR4R5, L is a linker group, X2 comprises nitrogen or carbon, Z is an optionally-substituted monocyclic or bicyclic ring system, and R1, R2, R3, R4, R5 and R6 are as defined in the specification.
    Type: Grant
    Filed: November 7, 2001
    Date of Patent: November 4, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory S. Bisacchi, James C. Sutton, William A. Slusarchyk, Uwe D. Treuner, Guohua Zhao, Daniel L. Cheney, Yan Shi, Shung C. Wu
  • Patent number: 6632823
    Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: October 14, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Jean-Michel Vernier, Nicholas D. P. Cosford, Ian A. McDonald
  • Patent number: 6632816
    Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1 may be, for example, iso-butyl, wherein X and Y, same or different, may be, for example, NH2 and F, and wherein R2 and R3 are as defined herein.
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: October 14, 2003
    Assignee: Pharmacor Inc.
    Inventors: Brent Richard Stranix, Jean-François Lavallée, Nicolas LeBerre, Valérie Perron
  • Patent number: 6630493
    Abstract: Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the meanings stated in the description, their preparation and use as calpain inhibitors.
    Type: Grant
    Filed: October 11, 2000
    Date of Patent: October 7, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
  • Patent number: 6610700
    Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
    Type: Grant
    Filed: April 16, 2001
    Date of Patent: August 26, 2003
    Assignee: Celltech R & D Limited
    Inventors: Timothy John Norman, John Robert Porter, Brian Woodside Hutchinson, Andrew James Ratcliffe, John Clifford Head, Rikki Peter Alexander, Barry John Langham, Graham John Warrellow, Sarah Catherine Archibald, Janeen Marsha Linsley
  • Patent number: 6610853
    Abstract: A herbicide containing as the active ingredient an N-(henylsulfonyl)picolinamide derivative represented by general formula (I) wherein X reprcsents a halogeno, a C1-4 alkyl, a C1-4 haloalkyl, a C1-4 alkoxy, a C1-4 haloalkoxy, a (C1-4 alkoxy)carbonyl, a [di(C1-4 alkyl)amino]sulfonyl, an [N—(C1-4 alkyl)-N—(C1-4 alkoxy)amino]sulfonyl, a (C1-4 alkylamino)sulfonyl, a C1-4 alkylthio, a C1-4 alkylsulfinyl, a C1-4 alkylsulfonyl, or nitro; n is an integer of 0 to 5; Y represets a halogeno, a C1-4 alkyl, a C1-4 haloalkyl, a C1-4 alkoxy, C1-4 haloalkoxy, a C1-4 alkylthio, a C1-4 haloalkylthio, amino, a C1-4 alkylamino, a di(C1-4 alkyl)amino, a (C1-4 alkoxy) C1-4 alkyl, a (C1-4 alkylthio) C1-4 alkyl, or nitro; and m is an integer of 0 to 4.
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: August 26, 2003
    Assignee: Kureha Kagaku Kogyo K.K.
    Inventors: Yoichi Kanda, Koki Sato, Tsutomu Sato
  • Patent number: 6599890
    Abstract: A compound of the formula wherein R1, R2 R3, R4 R5, R6, R7, R8, R9 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: July 29, 2003
    Assignee: Pfizer Inc
    Inventors: Kim F. McClure, Mark C. Noe, Michael A. Letavic, Louis S. Chupak
  • Patent number: 6596752
    Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: July 22, 2003
    Assignees: Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn Company
    Inventors: Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel
  • Patent number: 6586600
    Abstract: Novel sulfur-containing ligands for binding of heavy metals are disclosed. The ligands incorporate a central ring structure and pendant alkyl-thiol chains. The ligands are of the general structure: where n is an integer from 1-4, and X is selected from the group consisting of hydrogen, lithium, sodium, potassium, rubidium, cesium, and francium. The ligands of the present invention are suitable for binding any metal in or capable of being placed in a positive oxidation state, such as cadmium, lead, nickel, zinc, mercury, copper, and the like. Additionally, methods for removal of heavy metals from various substances are disclosed, comprising separating selected heavy metals from selected substances by contacting the substances with an effective amount of the novel sulfur-containing chelate ligands for a sufficient time to form stable, irreversible ligand-metal precipitates, and removing such precipitates.
    Type: Grant
    Filed: December 6, 2000
    Date of Patent: July 1, 2003
    Assignee: University of Kentucky Research Foundation
    Inventors: David A. Atwood, Brock S. Howerton, Matthew Matlock
  • Publication number: 20030055086
    Abstract: Compounds of formula (I): 1
    Type: Application
    Filed: August 12, 2002
    Publication date: March 20, 2003
    Inventors: Bernard P. Roques, Marie-Claude Fournie-Zaluski, Nicolas Inguimbert, Herve Poras, Elizabeth Scalbert, Caroline Bennejean, Pierre Renard