1,4-thiazines Patents (Class 514/227.5)
Additional hetero ring attached directly or indirectly to the 1,4-thiazine by nonionic bonding (Class 514/227.8)
  • Method for treating fibrotic diseases or other indications IIIC
    Publication number: 20040097495
    Abstract: Provided is a method of treating or ameliorating certain fibrotic diseases or other indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I:
    Type: Application
    Filed: October 23, 2003
    Publication date: May 20, 2004
    Inventors: Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
  • Compounds to treat Alzheimer's disease
    Patent number: 6737420
    Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII): useful in treating Alzheimer's disease and other similar diseases.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: May 18, 2004
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
  • Heteroarylakanoic acids as intergrin receptor antagonists
    Publication number: 20040092497
    Abstract: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the &agr;&ngr;&bgr;3 and/or the &agr;&ngr;&bgr;5 integrin without significantly antagonizing the IIb/IIIa integrin.
    Type: Application
    Filed: September 5, 2003
    Publication date: May 13, 2004
    Inventors: Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B, Mohler, Barbara B. Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark L. Boys, Nizal S. Chandrakumar, Hwang-Fun Lu
  • Compounds for the treatment of metabolic disorders
    Publication number: 20040092516
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Application
    Filed: October 14, 2003
    Publication date: May 13, 2004
    Inventors: Shalini Sharma, Reid W. von Borstel
  • Phenyl derivatives
    Publication number: 20040087582
    Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.
    Type: Application
    Filed: December 18, 2003
    Publication date: May 6, 2004
    Inventors: Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Bertram Cezanne, Johannes Gleitz, Christopher Barnes
  • Heterocyclylalkylamines as muscarinic receptor antagonists
    Publication number: 20040087581
    Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1
    Type: Application
    Filed: October 14, 2003
    Publication date: May 6, 2004
    Inventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
  • Amino-thio-acrylonitriles as MEK inhibitors
    Publication number: 20040087583
    Abstract: This invention relates generally to amino-thio-acrylonitriles of formula Ia or Ib: 1
    Type: Application
    Filed: October 30, 2003
    Publication date: May 6, 2004
    Inventor: Frank Worden Hobbs
  • Compounds and methods for modulation of estrogen receptors
    Publication number: 20040082575
    Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-&bgr;. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
    Type: Application
    Filed: May 7, 2003
    Publication date: April 29, 2004
    Applicant: Signal Pharmaceuticals, Inc.
    Inventors: Shripad S. Bhagwat, Leah Marie Gayo-Fung, Bernd M. Stein, Qi Chao, Anthony R. Gangloff, Jeffrey A. McKie, Kenneth D. Rice
  • Malonyl-coa decarboxylase inhibitors useful as metabolic modulators
    Publication number: 20040082576
    Abstract: The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.
    Type: Application
    Filed: July 21, 2003
    Publication date: April 29, 2004
    Inventors: Thomas Arrhenius, Mi Chen, Jie Fei Cheng, Yujin Huang, Alex Michael Nadzan, Richard Julius Penuliar, David Mark Wallace, Lin Zhang
  • Phenyl derivatives 3
    Publication number: 20040082563
    Abstract: Novel compounds of the formula (I) formula (I) in which W, E, X, Y, T, R1, R2, R2′, and R2″ are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.
    Type: Application
    Filed: September 16, 2003
    Publication date: April 29, 2004
    Inventors: Dieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
  • Fused cycloalkyl amides and acids and their therapeutic applications
    Publication number: 20040077617
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: October 22, 2002
    Publication date: April 22, 2004
    Inventors: Youssef L. Bennani, Sou-Jen Chang, Sanjay R. Chemburkar, Michael J. Dart, Dilinie P. Fernando, Timothy A. Grieme
  • Cycloalkylamides and their therapeutic applications
    Publication number: 20040077618
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: October 22, 2002
    Publication date: April 22, 2004
    Inventors: Youssef L. Bennani, Steve A. Chamberlin, Sanjay R. Chemburkar, Jinhua Chen, Michael J. Dart, Ashok K. Gupta, Lei Wang
  • Methods for the treatment of respiratory diseases and conditions using a selective iNOS inhibitor
    Publication number: 20040077639
    Abstract: Therapeutic methods for the prevention and treatment of respiratory diseases or conditions are described, the methods including administering to a subject in need thereof a respiratory disease or condition effective amount of a selective inhibitor of inducible nitric oxide synthase.
    Type: Application
    Filed: May 16, 2003
    Publication date: April 22, 2004
    Inventor: Pamela T. Manning
  • Novel integrin receptor antagonists
    Publication number: 20040077638
    Abstract: The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the &agr;v&bgr;3 integrin receptor, and pharmaceutical preparations comprising these compounds.
    Type: Application
    Filed: September 8, 2003
    Publication date: April 22, 2004
    Inventors: Herve Geneste, Andreas Kling, Arnulf Lauterbach, Claudia Isabella Graef, Thomas Subkoski, Wilfried Hornberger
  • Spirocyclopropyl amides and acids and their therapeutic applications
    Publication number: 20040077616
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: October 22, 2002
    Publication date: April 22, 2004
    Inventors: Youssef L. Bennani, William H. Bunnelle, Sou-Jen Chang, Sanjay R. Chemburkar, Jinhua Chen, Michael J. Dart, Dilinie P. Fernando, Yi-Yin Ku, Mark Lockwood, Lei Wang
  • Pharmaceutically active sulfanilide derivatives
    Publication number: 20040072816
    Abstract: The present invention relates to sulfanilide derivatives of formula (I), in which R1 and R2 are optionally substituted aryl and heteroaryl groups and the other variables are as defined in the claims, for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such sulfanilide derivatives. Said derivatives are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to sulfanilide derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor.
    Type: Application
    Filed: September 25, 2003
    Publication date: April 15, 2004
    Inventors: Anna Quattropani, Matthias Schwarz, Catherine Joran-Lebrun, Dennis Church, Alexander Scheer
  • Beta-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-alpha
    Publication number: 20040072802
    Abstract: The present application describes novel &bgr;-amino acid derivatives of formula I: 1
    Type: Application
    Filed: October 9, 2002
    Publication date: April 15, 2004
    Inventors: Jingwu Duan, Bryan W. King, Carl Decicco, Thomas P. Maduskuie, Mathew E. Voss
  • Organic compound having cyano group and insecticides/miticides
    Publication number: 20040072826
    Abstract: The present invention is directed to compounds represented by Formula (1); 1
    Type: Application
    Filed: October 8, 2003
    Publication date: April 15, 2004
    Inventors: Yasushi Shibata, Renpei Hatano, Takao Iwasa, Satoru Makita, Daisuke Hanai, Masao Yamaguchi, Naomi Ichikawa
  • Quaternary amines and related inhibitors of factor xa
    Publication number: 20040067938
    Abstract: Novel quaternary amine containing compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.
    Type: Application
    Filed: November 3, 2003
    Publication date: April 8, 2004
    Inventors: Penglie Zhang, Robert M. Scarborough, Bing-Yan Zhu
  • Acetylenic &agr;-amino acid-based sulfonamide hydroxamic acid tace inhibitors
    Patent number: 6716833
    Abstract: Compounds of the formula: are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: April 6, 2004
    Assignee: Wyeth Holdings Corporation
    Inventors: Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
  • Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme
    Publication number: 20040063698
    Abstract: The present invention provides compounds of Formula (I): 1
    Type: Application
    Filed: July 31, 2003
    Publication date: April 1, 2004
    Inventor: Thomas P. Maduskuie
  • Hydroxamic acid derivatives
    Patent number: 6713477
    Abstract: A hydroxamic acid derivative represented by formula (1) or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which has a matrix metalo-proteinase inhibitor.
    Type: Grant
    Filed: November 9, 2001
    Date of Patent: March 30, 2004
    Assignee: Sumitomo Pharmaceuticals Company, Limited
    Inventors: Gerard Robert Scarlato, Sara Sabina Hadida Ruah, Tamiki Nishimura, Masashi Nakatsuka, Fumio Samizo, Yumiko Kamikawa, Hitoshi Houtigai
  • Compounds
    Publication number: 20040058916
    Abstract: A compound having general formula 1
    Type: Application
    Filed: June 11, 2003
    Publication date: March 25, 2004
    Inventor: Ashokkumar Bhikkappa Shenvi
  • Beta-amino acid derivatives as integrin receptor antagonists
    Publication number: 20040058904
    Abstract: The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory diseases.
    Type: Application
    Filed: September 29, 2003
    Publication date: March 25, 2004
    Inventors: Thomas Rolle, Thomas Lehmann, Markus Albers, Gerhard Hebler, Gerhard Muller, Rudiger Fischer, Masaomi Tajimi, Karl Ziegelbauer, Kevin Bacon, Haruki Hasegawa, Hiromi Okigami
  • Carbamate caspase inhibitors and uses thereof
    Publication number: 20040053920
    Abstract: This invention provides caspase inhibitors of formula I: 1
    Type: Application
    Filed: August 21, 2003
    Publication date: March 18, 2004
    Inventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M.C. Golec
  • Aromatic sulfone hydroxamic acid metalloprotease inhibitor
    Publication number: 20040048852
    Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical.
    Type: Application
    Filed: January 7, 2003
    Publication date: March 11, 2004
    Inventors: Thomas E. Barta, Daniel P. Becker, Terri L. Boehm, Gary A. DeCrezcenzo, John N. Freskos, Daniel P. Getman, Joseph J. McDonald, Clara I. Villamil, Louis John Bedell, Jeffery N. Carroll, Theresa R. Fletcher, Susan Landis Hockerman, Stephen A. Kolodziej, Madeleine H. Li, Deborah A. Mischke, Patrick B. Mullins, Carol Pearcy Howard, Joseph Gerace Rico, Nathan W. Stehle
  • Monoamine reuptake inhibitors for treatment of CNS disorders
    Publication number: 20040048856
    Abstract: The present invention relates to compounds that are useful exhibit activity as serotonin, norepinephrine and dopamine reuptake inhibitors, and their pharmaceutically acceptable salts, and their use in the treatment of central nervous system and other disorders.
    Type: Application
    Filed: September 4, 2003
    Publication date: March 11, 2004
    Applicant: Pfizer Inc
    Inventors: Harry R. Howard, Christopher J. Schmidt, Thomas F. Seeger, Mark L. Elliott
  • Gem-substituted alpha v beta 3 antagonists
    Publication number: 20040043994
    Abstract: The present invention relates to a class of compounds represented by the Formula I.
    Type: Application
    Filed: January 21, 2003
    Publication date: March 4, 2004
    Inventors: Ish Kumar Khanna, Yi Yu, Hwang-Fun Lu, Nizal S. Chandrakumar, Renee M. Huff, Mark Russell, Mark L. Boys, Lori A. Schretzman, Barbara B. Chen, Bipinchandra N. Desai, Srinivasan Raj Nagarajan, Alan F. Gasiecki, Thomas D. Penning, Thomas Rogers, John Adam Wendt, Albert Khilevich, Yaping Wang
  • Biphenyl compounds and their use as oestrogenic agents
    Publication number: 20040043993
    Abstract: Compounds of formula (I), wherein R 5 is an [A]—CH 3 , —[A]—C(OH)ZZ′ or —[A]—C(O) Z″ grouping where —[A]— is an alkylene, alkenylene or alkynylene radical or a single bond, and Z, Z′ and Z″ are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl radical; and R 1, R 2, R 3, R 4, R 6, R 7 and R 8 are as defined in the description; the use thereof as a drug, pharmaceutical compositions containing same, a preparation method therefor, and intermediates of said method, are disclosed.
    Type: Application
    Filed: July 8, 2002
    Publication date: March 4, 2004
    Applicant: Aventis Pharma S.A.
    Inventors: Dominique Lesuisse, Jean-Georges Teutsch
  • Benzocycloalkylenylamine derivatives as muscarinic receptor antagonists
    Publication number: 20040034018
    Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1
    Type: Application
    Filed: August 1, 2003
    Publication date: February 19, 2004
    Inventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
  • 4-fluoroalkyl-2h-benzopyrans anti-estogenic activity
    Publication number: 20040034017
    Abstract: This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, 1
    Type: Application
    Filed: January 7, 2003
    Publication date: February 19, 2004
    Inventors: Hermann Kuenzer, Rolf Jautelat, Ludwig Zorn, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
  • Aromatic amides
    Publication number: 20040029874
    Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt 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: Application
    Filed: July 29, 2003
    Publication date: February 12, 2004
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milet, Marta Maria Pinelro-Nunez, 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
  • Fused ring heteroaryl and heterocyclic compounds which inhibit leukocyte adhesion mediated by VLA-4
    Publication number: 20040029873
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: December 11, 2002
    Publication date: February 12, 2004
    Inventors: Francine S. Grant, Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
  • Substituted N-phenyl 2-hydroxy-2-methyl-3,3,3-trifluoropropanamide derivatives which elevate pyruvate dehydrogenase activity
    Patent number: 6689909
    Abstract: A compound of formula (I) wherein: n is 1 or 2; R1 is chloro, fluoro, bromo, methyl or methoxy; R2 is as defined within; R3 is as defined within; and R4 is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.
    Type: Grant
    Filed: June 17, 2002
    Date of Patent: February 10, 2004
    Assignee: AstraZeneca AB
    Inventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows
  • Metalloprotease inhibitors
    Patent number: 6686348
    Abstract: A compound of formula (I): wherein: R1 represents hydrogen, halogen, alkyl or alkoxy, X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: February 3, 2004
    Assignee: Les Laboratoires Servier
    Inventors: Guillaume De Nanteuil, Alain Benoist, Philippe Pastoureau, Massimo Sabatini, John Hickman, Alain Pierre, Gordon Tucker
  • Biphenyl sulfonamides useful as matrix metalloproteinase inhibitors
    Patent number: 6686355
    Abstract: Inhibitors of MMP enzymes are cyclic sulfonamides of Formula I or a pharmaceutically acceptable salt thereof, and cyclic sulfonamides of Formula III or a pharmaceutically acceptable salt thereof, wherein R1 and R2 include hydrogen, alkyl, and substituted alkyl; R3 and R4 include hydrogen, halo, and alkyl; X is OH or NHOH: Z is (CH2)n: and Y is S, SO or SO2. The compounds of Formulas I and III are useful for the treatment of diseases mediated by an MMP enzyme, including cancer, osteoarthritis, rheumatoid arthritis, heart failure, and inflammation.
    Type: Grant
    Filed: February 13, 2002
    Date of Patent: February 3, 2004
    Assignee: Warner-Lambert Company
    Inventors: Nicole Chantel Barvian, Patrick Michael O'Brien, William Chester Patt, Drago Robert Sliskovic
  • Inhibitors of &agr;4&bgr;1 mediated cell adhesion
    Patent number: 6685617
    Abstract: The present invention relates to compound of formula (I), that are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: February 3, 2004
    Assignees: Pharmacia & Upjohn Company, Tanabe Seiyaku Co., Ltd.
    Inventors: James Blinn, Robert Chrusciel, Jed Fisher, Steven Tanis, Edward Thomas, Thomas Lobl, Bradley Teegarden
  • IL-8 receptor antagonists
    Patent number: 6680317
    Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: September 17, 2002
    Date of Patent: January 20, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
  • Novel potassium channels modulators
    Publication number: 20040009973
    Abstract: The invention relates to compounds having the Formula (I) 1
    Type: Application
    Filed: March 11, 2003
    Publication date: January 15, 2004
    Applicant: 4SC AG
    Inventors: Heiko Rauer, Gabriel Garcia, Bernd Kramer, Juergen Kraus, Claudia Klemenz, Wael Saeb
  • Pharmaceutical compositions for headache, migraine, nausea and emesis
    Publication number: 20040006044
    Abstract: S-alkylsiothiouronium derivatives such as S-ethylisothiouronium diethylphosphate are used for the treatment of headaches, in particular, migraines, as well as for the prevention or treatment of nausea and vomiting. The compositions of the invention are also effective in preventing or alleviating emesis associated with migraines or other medical conditions such as chemotherapy or radiotherapy, as well as other symptoms of migraines including phonophobia and photophobia.
    Type: Application
    Filed: March 5, 2003
    Publication date: January 8, 2004
    Applicant: MEDITOR PHARMACEUTICALS LTD.
    Inventors: Raphael Barkan, Alexander Mirimsky
  • Benzoic acid derivatives and pharmaceutical agents comprising the same as active ingredient
    Publication number: 20040002493
    Abstract: A pharmaceutical composition, which comprises a benzoic acid derivative of formula (I) 1
    Type: Application
    Filed: February 27, 2003
    Publication date: January 1, 2004
    Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
  • Beta-thioamino acids
    Publication number: 20030236253
    Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.
    Type: Application
    Filed: March 14, 2003
    Publication date: December 25, 2003
    Applicant: Gruenenthal GmbH
    Inventors: Boris Chizh, Matthias Gerlach, Michael Haurand, Claudia Puetz, Gero Gaube, D. Enders
  • Benzenesulfonamide-derivatives and their use as medicaments
    Patent number: 6667342
    Abstract: Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a halocycloalkyl ring; R5 is a substituent as defined within; Y—Z is a linking group as defined within; are useful in the production of a elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.
    Type: Grant
    Filed: August 22, 2000
    Date of Patent: December 23, 2003
    Assignee: Astrazeneca AB
    Inventors: David S Clarke, Jeremy N Burrows, Paul Ro Whittamore, Roger J Butlin, Thorsten Nowak
  • Anthranilic acid derivative
    Publication number: 20030232811
    Abstract: The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.
    Type: Application
    Filed: January 31, 2003
    Publication date: December 18, 2003
    Applicant: TEIJIN LIMITED
    Inventors: Naoki Tsuchiya, Susumu Takeuchi, Takumi Takeyasu, Naoki Hase, Takao Yamori, Takashi Tsuruo
  • FAP-activated anti-tumor compounds
    Publication number: 20030232742
    Abstract: The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP&agr;), said prodrug is chemically stable under physiological conditions and can be used for the manufacture of physically stable aqueous formulations. It has a cleavage site which is recognised by FAP&agr;, and the drug released by the enzymatic activity of FAP&agr; is cytotoxic or cytostatic under physiological conditions.
    Type: Application
    Filed: November 9, 2001
    Publication date: December 18, 2003
    Inventors: Stefan Peters, Dietmar Leipert, Christian Eickmeier, John Edward Park, Martin Lenter, Pilar Garin-Chesa, Juergen Mack
  • Compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them
    Publication number: 20030229083
    Abstract: The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I), 1
    Type: Application
    Filed: November 27, 2002
    Publication date: December 11, 2003
    Applicant: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Bhuniya Debnath, Saibal Kumar Das, Gurram Ranga Madhavan, Javed Iqbal, Ranjan Chakrabarti, Reeba Kannimel Vikramadithyan
  • Cyclic compounds
    Publication number: 20030229089
    Abstract: A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, 1
    Type: Application
    Filed: October 25, 2002
    Publication date: December 11, 2003
    Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
  • Cyclohexylamine derivatives as subtype selective nmda receptor antagonists
    Publication number: 20030225164
    Abstract: Described are cyclohexylamine derivatives of Formula (I), Formula (II) or Formula (III) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease. The substituents are described in the specification.
    Type: Application
    Filed: December 2, 2002
    Publication date: December 4, 2003
    Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
    Publication number: 20030225071
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: June 11, 2002
    Publication date: December 4, 2003
    Inventors: Stacie S. Canan Koch, Therese N. Alexander, Mark Barvian, Gary Bolton, Fredrick E. Boyer, Benjamin J. Burke, Tod Holler, Tanya M. Jewell, Vara Prasad Josyula, David J. Kucera, Maria A. Linton, Jeffrey J. Machak, Lennert J. Mitchell, Sean T. Murphy, Siegfried H. Reich, Donald J. Skalitzky, John H. Tatlock, Michael D. Varney, Scott C. Virgil, Stephen E. Webber, Stephen T. Worland, Michael Melnick
  • Acyl-3-carboxyphenylurea derivatives, processes for preparing them and their use
    Publication number: 20030216370
    Abstract: The invention relates to acyl-3-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives.
    Type: Application
    Filed: April 10, 2003
    Publication date: November 20, 2003
    Inventors: Elisabeth Defossa, Dieter Kadereit, Karl Schoenafinger, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Alfons Enhsen