Additional Nitrogen Containing Hetero Ring (e.g., Thiazetidine, Etc.) Patents (Class 544/111)
  • Patent number: 7015223
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Grant
    Filed: November 20, 2000
    Date of Patent: March 21, 2006
    Assignee: Pharmacia Corporation
    Inventors: Michael S. South, Ashton T. Hamme, II, William L. Neumann, Darin E. Jones, Melvin L. Rueppel
  • Patent number: 6974808
    Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.
    Type: Grant
    Filed: November 27, 2001
    Date of Patent: December 13, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventor: James R. McCarthy
  • Patent number: 6972292
    Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: December 6, 2005
    Assignee: Novartis AG
    Inventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
  • Patent number: 6969730
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: November 29, 2005
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Youssef L. Bennani, Ramin Faghih, Gregory A. Gfesser, Lawrence A. Black
  • Patent number: 6962633
    Abstract: A novel family of amine azides having a cyclic structure therein is disclosed. These compounds have attractive properties as rocket propellants.
    Type: Grant
    Filed: March 18, 2003
    Date of Patent: November 8, 2005
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventor: Michael J. McQuaid
  • Patent number: 6958332
    Abstract: This invention features pyrimidine compounds of formula (I): each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
    Type: Grant
    Filed: September 5, 2003
    Date of Patent: October 25, 2005
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Mitsunori Ono, Teresa Przewloka, Elena Kostik, Yumiko Wada
  • Patent number: 6956037
    Abstract: The invention concerns amide derivatives of Formula (I), wherein R3 is (1-6C)alkyl or halogeno; m is 1-3 and R1 is selected from substituents such as: (A) hydroxy, halogeno, (1-6C)alkyl, (1-6C)alkoxy, aryl, heteroaryl and heterocyclyl; and (B) di-[(1-6C)alkyl]amino-(1-6C)alkyl, (1-6C)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, aryloxy, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 is aryl or cycloalkyl which bears 1-3 substituents such as: (C) hydrogen, hydroxy, halogeno and heterocyclyl; and (D) heteroaryl-(1-6C)alkoxy and heterocyclyl-(1-6C)alkoxy, provided that a substituent on R4 is selected from paragraph (C) only if at least one R1 group is selected from paragraph (B); processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Grant
    Filed: April 28, 2003
    Date of Patent: October 18, 2005
    Assignee: AstraZeneca AB
    Inventors: Dearg S Brown, George R Brown
  • Patent number: 6956036
    Abstract: Substituted 1-(?-alkyl-ethylamino)-1H-indazol-6-ols useful for lowering and controlling IOP and treating glaucoma are disclosed
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: October 18, 2005
    Assignee: Alcon, Inc.
    Inventors: Jesse A. May, Zixia Feng, Anura P. Dantanarayana
  • Patent number: 6951940
    Abstract: The invention relates to the compounds of formula: as well as to the salts thereof with inorganic or organic acids, to solvates thereof and/or to hydrates thereof, which have strong affinity and high selectivity for the human NK1 receptors of substance P. The invention also relates to the process for preparing them, to the intermediate compounds of formula (VII) which are useful for the preparation, to pharmaceutical compositions containing them and to their fuse for the manufacture of medicinal products intended for treating any pathology in which substance P and the human NK1 receptors are involved.
    Type: Grant
    Filed: September 16, 2003
    Date of Patent: October 4, 2005
    Assignee: Sanofi-Aventis
    Inventors: Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
  • Patent number: 6933302
    Abstract: (20) esters of camptothecin analogs are provided. The compounds are (20) esters of an aminoalkanoic acid or an imidoalkanoic acid and homocamptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the homocamptothecin ring. The compounds are useful for treating cancer.
    Type: Grant
    Filed: June 3, 2003
    Date of Patent: August 23, 2005
    Assignees: California Pacific Medical Center, Catholic Healthcare West
    Inventor: Li-Xi Yang
  • Patent number: 6933308
    Abstract: Novel aminoalkylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders responsive to the opening of the KCNQ potassium channels, including pain and migraine.
    Type: Grant
    Filed: December 9, 2003
    Date of Patent: August 23, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kenneth M. Boy, Yong-Jin Wu
  • Patent number: 6924285
    Abstract: The present invention relates to bicyclic heterocyclic groups of general formula wherein Ra, Rb, Rc, Rd and X are defined as in claim 1, the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostate hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: August 2, 2005
    Assignee: Boehringer Ingelheim Pharma GmbH & Co.
    Inventors: Frank Himmelsbach, Birgit Jung, Flavio Solca
  • Patent number: 6906068
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Grant
    Filed: May 17, 2000
    Date of Patent: June 14, 2005
    Assignee: Pharmacia Corporation
    Inventors: Michael S. South, Ashton T. Hamme, II, William L. Neumann, Darin E. Jones
  • Patent number: 6903115
    Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
    Type: Grant
    Filed: January 13, 2003
    Date of Patent: June 7, 2005
    Assignee: AstraZeneca AB
    Inventors: Aaron Rigby, Hitesh Sanganee, Brian Springthorpe, Louise Lawrence
  • Patent number: 6900209
    Abstract: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5- or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.
    Type: Grant
    Filed: November 22, 2001
    Date of Patent: May 31, 2005
    Assignee: Merck sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Philip Jones, Angus Murray MacLeod, Robert James Maxey, Helen Jane Szekeres
  • Patent number: 6890935
    Abstract: The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacyclic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. The present invention also relates to prodrug derivatives of the compounds of the present invention.
    Type: Grant
    Filed: April 30, 2001
    Date of Patent: May 10, 2005
    Assignee: Targacept, Inc.
    Inventors: Gary Maurice Dull, Jeffrey Daniel Schmitt, Balwinder Singh Bhatti, Craig Harrison Miller
  • Patent number: 6884800
    Abstract: Imidazole compounds of the formula I in which R1 and R2, independently of one another, each denote A1, OA1, SA1 or Hal, A1 denotes H, A, alkenyl, cycloalkyl or alkylenecycloalkyl, A denotes alkyl having 1-10 carbon atoms, Hal denotes F, Cl, Br or I, and X denotes O, S, SO or SO2, and their physiologically acceptable salts and/or solvates, as phosphodiesterase VII inhibitors, and their use for the preparation of a medicament.
    Type: Grant
    Filed: October 31, 2000
    Date of Patent: April 26, 2005
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Hans-Michael Eggenweiler, Rochus Jonas, Michael Wolf, Michael Gassen, Thomas Welge
  • Patent number: 6870056
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Grant
    Filed: November 20, 2000
    Date of Patent: March 22, 2005
    Assignee: Pharmacia Corporation
    Inventors: Michael S. South, Qingieng Zeng, Melvin L. Rueppel, Ashton T. Hamme, II
  • Patent number: 6858623
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
    Type: Grant
    Filed: May 29, 2003
    Date of Patent: February 22, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Eugene R. Hickey, Weimin Liu, Usha R. Patel, Denice M. Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young
  • Patent number: 6858606
    Abstract: This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl optionally substituted with Rd and Rem; each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; Rd is halogen, CN, alkyl alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; Re is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g.
    Type: Grant
    Filed: November 26, 2002
    Date of Patent: February 22, 2005
    Assignee: Synta Pharmaceutical Corp.
    Inventors: Lijun Sun, Mitsunori Ono, Elena Kostik, Yumiko Wada
  • Patent number: 6849733
    Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.
    Type: Grant
    Filed: August 22, 1997
    Date of Patent: February 1, 2005
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Yufeng Hong, Vlad Edward Gregor, Anthony Lai Ling, Eileen Valenzuela Tompkins
  • Patent number: 6846827
    Abstract: The invention concerns pyrimidine derivatives of Formula (I) wherein m is 0-3 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R3 is hydrogen, halogeno or (1-6C)alkyl; n is 0-2 and each R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; p is 0-4; and Q1 is aryl or heteroaryl; or pharmaceutically acceptable salts or in vivo cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Grant
    Filed: October 10, 2000
    Date of Patent: January 25, 2005
    Assignee: AstraZeneca AB
    Inventor: John Graham Cumming
  • Patent number: 6838456
    Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: January 4, 2005
    Assignee: Lilly ICOS LLC
    Inventors: Mark W. Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan, Françoise Gellibert, Romain Luc Marie Gosmini
  • Patent number: 6815440
    Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.
    Type: Grant
    Filed: March 3, 2003
    Date of Patent: November 9, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
  • Patent number: 6797709
    Abstract: An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, —NH—Q—R3 (R3 is a substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or —NH—R4 (R4 is a substituted or unsubstituted cycloalkyl group); R2 is a substituted or unsubstituted aryl group; one of Y and Z is ═CH—, and the other is ═N—, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.
    Type: Grant
    Filed: May 1, 2003
    Date of Patent: September 28, 2004
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
  • Patent number: 6797820
    Abstract: Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The hydroxymates are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as matrix metalloproteinases (MMPs). Methods of synthesis and of use of the compounds are also disclosed.
    Type: Grant
    Filed: December 13, 2000
    Date of Patent: September 28, 2004
    Assignee: Vicuron Pharmaceuticals Inc.
    Inventors: Dinesh Patel, Jeffrey W. Jacobs, Rakesh Jain, Zhi-Jie Ni, Zhengyu Yuan
  • Patent number: 6790846
    Abstract: Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis, congestive heart, hypertension, chronic obstructive pulmonary disease, septic shock syndrome, tuberculosis, adult respiratory distress, asthma, atherosclerosis, muscle degeneration, periodontal disease, cachexia, Reiter's syndrome, gout, acute synovitis, anorexia and bulimia nervosa fever, malaise, myalgia and headaches.
    Type: Grant
    Filed: May 7, 2002
    Date of Patent: September 14, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Michael Philip Clark, Jane Far-Jine Djung, Steven Karl Laughlin, Joshua Spector Tullis, Michael George Natchus, Biswanath De
  • Patent number: 6787650
    Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: September 7, 2004
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Osamu Kurasawa, Shinichi Imamura, Shohei Hashiguchi, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba
  • Patent number: 6777431
    Abstract: The present invention provides compounds which have a pyrazinone or pyridinone ring at P3 and an optionally substituted heteroaryl group at P1. These compounds have biological activity as active and potent inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds and pharmaceutical compositions comprising these compounds as therapeutic agents for treatment of disease states in mammals which are characterized by abnormal thrombosis are also described.
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: August 17, 2004
    Assignee: Corvas International, Inc.
    Inventors: Daniel Vanna Siev, Joseph Edward Semple, Mallareddy Komandla, John Eugene Reiner, Scott Jeffrey Kemp
  • Patent number: 6774127
    Abstract: Novel pyridyl and pyrimidinyl substituted pyrazole and pyrazoline compounds and compositions for use in therapy.
    Type: Grant
    Filed: February 19, 2003
    Date of Patent: August 10, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Timothy Gallagher, Irennegbe Kelly Osifo
  • Patent number: 6770641
    Abstract: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.
    Type: Grant
    Filed: June 10, 2003
    Date of Patent: August 3, 2004
    Assignees: Yamanouchi Pharmaceutical Co., Ltd., Ludwig Institute for Cancer Research, Imperial Cancer Research Technology Ltd.
    Inventors: Masahiko Hayakawa, Hiroyuki Kaizawa, Hiroyuki Moritomo, Ken-Ichi Kawaguchi, Tomonobu Koizumi, Mayumi Yamano, Koyo Matsuda, Minoru Okada, Mitsuaki Ohta
  • Patent number: 6770637
    Abstract: Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing.
    Type: Grant
    Filed: August 3, 2001
    Date of Patent: August 3, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thierry Godel, Torsten Hoffmann, Patrick Schnider, Heinz Stadler
  • Publication number: 20040143115
    Abstract: This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists 1
    Type: Application
    Filed: November 5, 2003
    Publication date: July 22, 2004
    Inventors: Clive Leslie Branch, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
  • Patent number: 6762034
    Abstract: Resorufin derivative as a substance for cytochrome P450 enzyme.
    Type: Grant
    Filed: January 2, 2002
    Date of Patent: July 13, 2004
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Jacqueline Carol Bloomer, Richard Leonard Elliott, Colin Andrew Leach
  • Patent number: 6756383
    Abstract: Organi c compounds having the structural formulas I, II, and III are provided where the variables have the values described herein and R1 and R2 in structure I join together to form a 5 to 7 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group in structures I and II. Pharmaceutical formulations include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: June 29, 2004
    Assignee: Chiron Corporation
    Inventors: Paul A. Renhowe, Timothy D. Machajewski, Cynthia M. Shafer, Mary Ellen Wernette Hammond, Sabina Pecchi
  • Patent number: 6750216
    Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formula IIIB have the structure: wherein R1, R2, R, Ar and n are as described in the specification.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: June 15, 2004
    Assignee: Adolor Corporation
    Inventors: Virendra Kumar, Deqi Guo, Michael Anthony Marella, Alan L. Maycock
  • Patent number: 6734196
    Abstract: The invention relates to a compound of formula (I): wherein: A represents pyridine, pyridinium or piperidine R1, R2, R3 and R4 are as defined in the description R5 represents hydrogen, a nitrogen-containing heterocycle or a group of formula (II): R6 represents hydrogen or linear or branched (C1-C6)alkyl. and medicinal products containing the same which are useful in treating pain or deficiencies in memory.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: May 11, 2004
    Assignee: Les Laboratoires Servier
    Inventors: Otto Meth-Cohn, Chu-Yi Yu, Pierre Lestage, Marie-Cécile Lebrun, Daniel-Henri Caignard, Pierre Renard
  • Patent number: 6723718
    Abstract: The present invention relates to novel substituted &agr;,&bgr;-fused butyrolactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, craniocerebral trauma, states of pain or CNS-mediated spasms.
    Type: Grant
    Filed: July 25, 2002
    Date of Patent: April 20, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Andreas Stolle, Horst-Peter Antonicek, Stephen Lensky, Arnd Voerste, Thomas Müller, Jörg Baumgarten, Karsten von dem Bruch, Gerhard Müller, Udo Stropp, Ervin Horváth, Jean-Marie-Viktor de Vry, Rudy Schreiber
  • Publication number: 20040063679
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
    Type: Application
    Filed: September 27, 2002
    Publication date: April 1, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R.R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
  • Publication number: 20040058923
    Abstract: Compounds of formula (I) wherein: R1 represents C1-16 alkyl, C2-6alkenyl, C2-6alkynyl, C2-6alkynyl-Y1—, aryl-Y1—, heteroaryl-Y1—, aryl-(O)t-aryl-Y1—, aryl-(O)t-heteroaryl-Y1—, heteroaryl-(O)t-aryl-Y1—, heteroaryl-(O)t-heteroaryl-Y1—, C2-6 alkenyl-Y1—, aryl-O—Y1—, heteroaryl-O—Y1—, C1-16 alkyl-SO2—Y1—,M—Y1—,J2-Y1—, —CN or C3-8 cycloalkyl-Y1— or C3-8 cycloalkenyl-Y1—, which cycloalkyl or cycloalkenyl may be optionally substituted by one or more hydroxyl or C1-16 Alkyl groups; R2 represents hydrogen or C1-16 alkyl; X represents ethylene or a group of formula CReRf wherein Re and Rf independently represent hydrogen or C1-14 alkyl or Re and Rf may together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R3 and R4 independently represent hydrogen or C1-14 alkyl; Z represents a bond, CO, SO2, CR9R6(CH2)n, (CH2)nCR9R6, CHR6(CH2)nO, CHR6(CH2)nS, CHR6(CH2)nOCO, CHR6(CH2)n
    Type: Application
    Filed: August 15, 2003
    Publication date: March 25, 2004
    Inventors: Rachael Anne Ancliff, Caroline Mary Cook, Colin David Eldred, Paul Martin Gore, Lee Andrew Harrison, Simon Teanby Hodgson, Duncan Bruce Judd, Suzanne Elaine Keeling, Xiao Qing Lewell, Graeme Michael Robertson, Stephen Swanson
  • Publication number: 20040034019
    Abstract: The present invention relates to piperazine and piperidine derivatives, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.
    Type: Application
    Filed: August 8, 2002
    Publication date: February 19, 2004
    Inventors: Ronald Tomlinson, David Lauffer, Michael Mullican
  • Patent number: 6686467
    Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
    Type: Grant
    Filed: October 8, 2002
    Date of Patent: February 3, 2004
    Assignee: Zeneca Limited
    Inventors: Dearg S Brown, George R Brown, Philip Cohen
  • Patent number: 6686468
    Abstract: The present invention relates to specific photochromic h-annellated benzo[f]chromene derivatives and their use in synthetic resins of all types, especially for ophthalmic applications. In particular, the present invention relates to photochromic compounds derived from benzo[f]chromenes, which in the open form have especially long-wave absorption maxima making it possible to obtain violet to blue tints when used in phototropic glasses.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: February 3, 2004
    Assignee: Optische Werke G. Rodenstock
    Inventors: Claudia Mann, Manfred Melzig, Udo Weigand
  • Patent number: 6677338
    Abstract: The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: January 13, 2004
    Assignees: President and Fellows of Harvard College, Organix, Inc.
    Inventors: Bertha K. Madras, Peter C. Meltzer
  • Patent number: 6677483
    Abstract: A new process for the preparation of diethylenetriaminepentaacetic-monoamides in which amines can be reacted with sensitive groups, a higher mono/diamide selectivity is achieved, a higher yield of monoamide is achieved and has a simple reaction scheme and working-up.
    Type: Grant
    Filed: January 28, 2002
    Date of Patent: January 13, 2004
    Assignee: Schering AG
    Inventors: Johannes Platzek, Ulrich Niedballa
  • Publication number: 20040002494
    Abstract: The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
    Type: Application
    Filed: June 19, 2003
    Publication date: January 1, 2004
    Applicant: Pharmacia Corporation
    Inventors: Michael S. South, Brenda Case, Danny J. Garland, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, William L. Neumann, John J. Parlow, David B. Reitz, Melvin L. Rueppel, Ronald K. Webber
  • Publication number: 20040002604
    Abstract: Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
    Type: Application
    Filed: June 17, 2003
    Publication date: January 1, 2004
    Inventors: Richard Apodaca, Xiaohu Deng, Jill A. Jablonowski, Neelakandha Mani, Chennagiri R. Pandit, Wei Xiao
  • Patent number: 6670359
    Abstract: The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.
    Type: Grant
    Filed: November 1, 2002
    Date of Patent: December 30, 2003
    Assignee: AstraZeneca AB
    Inventors: Stefan Berg, Martin Nylöf, Svante Ross, Seth-Olov Thorberg
  • Patent number: 6670368
    Abstract: A pyrimidine derivative of formula (I) wherein V is O or S, Q1 and Q2 are independently selected from phenyl, naphthyl, a 5- or 6-membered monocyclic moiety and a 9- or 10-membered bicyclic heterocyclic moiety; and Q1 is substituted by one substituent of formula (Ia), and Q2 may optionally bear further substituents of formula (Ia) wherein X is CH2—, O—, NH—, NRy— or —S—[wherein Ry is as defined within]; Y1 is H, C1-4alkyl or as defined for Z; Y2 is H or C1-4alkyl; Z is RaO—, RbRcN—, RdS—, ReRfNNRg—, a nitrogen linked heteroaryl or a nitrogen linked heterocycle, wherein Ra, Rb, Rc, Rd, Re, Rf and Rg are as defined within; n is 1, 2 or 3; m is 1, 2 or 3; and Q1 and Q2 may optionally be further substituted; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof; are useful as anti-cancer agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
    Type: Grant
    Filed: October 4, 2001
    Date of Patent: December 30, 2003
    Assignee: AstraZeneca AB
    Inventors: Gloria A. Breault, Stewart R. James, Janet E. Pease
  • Publication number: 20030232802
    Abstract: The invention relates to novel aryl and heteroaryl sulfonates of formula (Ia) and to methods for producing them and to novel aryl and heteroaryl sulfonates of formula (I) for treating and/or preventing diseases, especially for treating pain and neurodegenerative diseases, A representing (C6-C10)-aryl or 5-10-membered heteroaryl, D representing (C6-C10)-arylene or 5-10-membered heteroarylene, R1 representing (C4-C8)-alkyl, (C2-C8)-alkyl, the carbon chain being interrupted by one or two heteroatoms or groups chosen from the following group: —O—, —S—, —SO—and —SO2—, (C2-C8)-alkenyl or (C2-C8)-alkinyl, in formula (Ia); and R1 representing (C3-C8)-alkyl, (C2-C8)-alkyl, the carbon chain being interrupted by one or two heteroatoms or groups chosen from the following group: —O—, —S—,—SO—and —SO2—, (C2-C8)-alkenyl or (C2-C8)-alkinyl.
    Type: Application
    Filed: May 12, 2003
    Publication date: December 18, 2003
    Inventors: Markus Heil, Heinrich Meier, Paul Naab, Arnd Voerste, Jean-Marie-Viktor de Vry, Dirk Denzer, Frank Mauler, Klemens Lustig, Volker Hinz, Swen Allerheiligen