Additional Hetero Ring, Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 548/465)
The additional hetero ring is bonded directly to a ring carbon of the bicyclo ring system (Class 548/466)
Substituent on ring carbon of the bicyclo ring system contains the additional hetero ring (Class 548/467)
  • Process for preparing glycidylphthalimide
    Patent number: 6875875
    Abstract: A process for preparing glycidylphtalimide or it optically active compound by reacting a phthalimide alkalimetal salt with an epihalohydrin or an optically active epihalohydrin in an alcohol solvent; or by reacting phthalimide with an epihalohydrin or an optically active epihalohydrin in the presence of an alkali metal carbonate, an alkali metal hydrogencarbonate or a quaternary ammonium salt to obtain a N-(3-halogeno-2-hydroxypropyl)phthalimide and then by cyclizing the product with an alkali metal alkoxide.
    Type: Grant
    Filed: September 25, 2003
    Date of Patent: April 5, 2005
    Assignee: Daiso Co., Ltd.
    Inventors: Yoshiro Furukawa, Yasushi Miki
  • 4-aryl substituted indolinones
    Patent number: 6861418
    Abstract: The present invention relates to 4-arylindolinones, as well as pharmaceutical compositions thereof, capable of modulating protein kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. The present invention also relates to methods for treating protein kinase related disorders.
    Type: Grant
    Filed: December 16, 2003
    Date of Patent: March 1, 2005
    Assignee: Sugen, Inc.
    Inventors: Jingrong Cui, Ruofei Zhang, Hong Shen, Ji Yu Chu, Fang-Jie Zhang, Marcel Koenig, Steven Huy Do, Xiaoyuan Li, Chung Chen Wei, Peng Cho Tang
  • Indole derivatives exhibiting chymase-inhibitory activities and process for preparation thereof
    Patent number: 6852734
    Abstract: According to this invention, there is provided an indole derivative having the general formula (I) wherein A is an oxygen atom or a nitrogen atom which nitrogen atom is optionally substituted with an alkyl group, and (i) R1 and R2 each stand for a hydrogen atom or an alkyl group, independently, or (ii) R1 and R2 as taken together form a cycloalkyl group or an aromatic ring, or (iii) R1 and R2 as taken together form a heterocyclic ring, and R3 is a hydrogen atom, a (C1-C10)alkyl group or others, R4 is a substituted alkyl group and R5 is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group and so on, as novel compounds by a novel chemical synthetic process. The indole derivative of formula (I) exhibits a useful chymase inhibitory activity.
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: February 8, 2005
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Yasuo Yamamoto, Kenzo Hariyama, Yumiko Yanagisawa, Sojiro Shiokawa, Takumi Takeyasu, Osami Takenouchi, Hidenori Kasai
  • Amidine inhibitors of serine proteases
    Patent number: 6838479
    Abstract: Inhibitors of serine proteases are provided having formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.
    Type: Grant
    Filed: September 5, 2001
    Date of Patent: January 4, 2005
    Assignee: Genentech, Inc.
    Inventors: Richard M Pastor, Dean R. Artis, Alan G. Olivero
  • Synthesis of epothilones, intermediates thereto and analogues thereof
    Publication number: 20040260098
    Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.
    Type: Application
    Filed: March 28, 2003
    Publication date: December 23, 2004
    Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin
  • Polymorphs of pyrrole substituted 2-indolinone protein kinase inhibitors
    Publication number: 20040259929
    Abstract: The present invention relates to polymorphs of the 3-pyrrole substituted 2-indolinone compound 5-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide.
    Type: Application
    Filed: February 12, 2004
    Publication date: December 23, 2004
    Applicant: Pharmacis & Upjohn Company
    Inventors: Changquan Sun, Todd P. Foster, Fusen Han, Michael Hawley, Tom Thamann
  • Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
    Publication number: 20040259843
    Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
    Type: Application
    Filed: February 27, 2004
    Publication date: December 23, 2004
    Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
  • Heterocyclylalkoxy-,-alkylthio-and -alkylaminobenzazole derivatives as 5-hydroxytryptamine-6 ligands
    Patent number: 6831094
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: December 14, 2004
    Assignee: Wyeth
    Inventors: Yanfang Li, Ping Zhou
  • Indole derivatives useful for the treatment of diseases
    Publication number: 20040235833
    Abstract: The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Application
    Filed: March 12, 2004
    Publication date: November 25, 2004
    Applicant: Pfizer Inc
    Inventors: Alan Daniel Brown, Justin Stephen Bryans, Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Simon John Mantell
  • Phenyl derivatives as factor XA Inhibitors
    Publication number: 20040235828
    Abstract: Novel compounds of the formula (I), in which D, W, X, Y, T and R1 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 diseases and for the treatment of tumours.
    Type: Application
    Filed: February 9, 2004
    Publication date: November 25, 2004
    Inventors: Dieter Dorsch, Bertram Cezanne, Christos Tsaklakidis, Werner Mederski, Johannes Gleitz, Christopher Barnes
  • Novel compounds
    Publication number: 20040235821
    Abstract: The invention relates to thiophene carboxamides of formula (I), wherein R1, R2, R3, A, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: January 22, 2004
    Publication date: November 25, 2004
    Inventors: David Griffiths, Carig Johnstone
  • Amino acid derivatives and their use as medicines
    Patent number: 6821986
    Abstract: Novel compounds of formula wherein the substituents are defined as in the specification and are useful for inhibiting neuronal NO synthase or inducible NO synthase as well as inhibiting lipidic peroxidation.
    Type: Grant
    Filed: October 31, 2002
    Date of Patent: November 23, 2004
    Assignee: Societe de Conseils de Recherchet et E'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Serge Auvin, Jeremiah Harnett, Pierre-Etienne Chabrier de Lassauniere
  • Novel 2-substituted cyclic amines as calcium sensing receptor modulators
    Publication number: 20040229860
    Abstract: The present invention relates to modulators of the calcium sensing receptor having the formula I 1
    Type: Application
    Filed: January 27, 2004
    Publication date: November 18, 2004
    Inventors: Ashvinikumar V. Gavai, Roy J. Vaz, John K. Dickson, Jacques Y. Roberge, Wu Yang, Timur Gungor, James R. Corte, David P. Rotella, Yufeng Wang
  • Growth hormone secretagogues
    Publication number: 20040229823
    Abstract: The invention relates to compounds of formula I 1
    Type: Application
    Filed: May 4, 2004
    Publication date: November 18, 2004
    Applicant: Zentaris AG
    Inventors: Jean Martinez, Jean-Alain Fehrentz, Vincent Guerlavais
  • Substituted aza-oxindole derivatives
    Patent number: 6815439
    Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase II inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.
    Type: Grant
    Filed: September 23, 2003
    Date of Patent: November 9, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Philip Anthony Harris, Lee Frederick Kuyper, Karen Elizabeth Lackey, James Marvin Veal
  • Light emitting materials based on indole skeleton
    Patent number: 6815093
    Abstract: An indole-based compound represented by Formula (1) disclosed herein is useful in forming a light emitting material for an organic electroluminescent device. The organic electroluminescent device has a multi-layered structure comprising a cathode, an anode and at least one organic layer, wherein the at least one organic layer comprises the indole-based compound. The indole-based compound contains two light-emitting units, each having an indole-based structure, linked with a connecting unit, which is an arylamine. The color of the light emitted by the light emitting material can be adjusted by changing the connecting unit.
    Type: Grant
    Filed: January 14, 2003
    Date of Patent: November 9, 2004
    Assignee: Lightronik Technology, Inc.
    Inventor: Tung-Shen Lin
  • Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids
    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
  • Anti-diabetic agents
    Publication number: 20040220229
    Abstract: The invention provides compounds of formula (I) 1
    Type: Application
    Filed: April 30, 2004
    Publication date: November 4, 2004
    Applicant: Pfizer Inc
    Inventors: Donald L. Bussolotti, Ronald B. Gammill
  • Hydroxyindoles, their use as inhibitors of phosphodiesterase 4 and processes for their preparation
    Publication number: 20040220183
    Abstract: The invention relates to new hydroxyindoles of the Formula, 1
    Type: Application
    Filed: May 27, 2004
    Publication date: November 4, 2004
    Inventors: Norbert Hofgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelenyi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
  • Substituted isoindoles and the e use thereof
    Publication number: 20040215019
    Abstract: The invention relates to coagulation of the blood.
    Type: Application
    Filed: January 30, 2004
    Publication date: October 28, 2004
    Inventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer
  • Quaternary salts of n-substituted cyclic or acyclic amines as pharmaceuticals
    Publication number: 20040214867
    Abstract: In one aspect, the present invention concerns the use of certain quaternary ammonium compounds as active ingredient in the manufacture of a medicament for use in the treatment and/or prevention of cough in warm-blooded animals, including humans, such as compounds of the following formula (I): Y-J-E An− wherein J is independently selected from a group represented by one of formulae (II), (III) and (IV).
    Type: Application
    Filed: February 14, 2003
    Publication date: October 28, 2004
    Inventors: Lewis Siu Leung Choi, Gregory N Beatch, Clive Page
  • Substituted indoles
    Publication number: 20040209868
    Abstract: Compounds of the formula I 1
    Type: Application
    Filed: May 11, 2004
    Publication date: October 21, 2004
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Olaf Ritzeler, Hans Ulrich Stilz, Bernhard Neises, Gerhard Jaehne, Jorg Habermann
  • Pyrrole derivatives
    Publication number: 20040209939
    Abstract: Pyrrole derivatives represented by the following formula: 1
    Type: Application
    Filed: May 7, 2004
    Publication date: October 21, 2004
    Applicant: Sumitomo Pharmaceuticals Co., Ltd.
    Inventors: Teruhisa Tokunaga, William Ewan Hume, Makoto Kitoh, Ryu Nagata
  • Novel 1,3-dihydro-2H-indol-2one derivatives, process for preparing them and pharmaceutical compositions containing them
    Publication number: 20040209938
    Abstract: The invention relates to compounds of formula: 1
    Type: Application
    Filed: April 29, 2004
    Publication date: October 21, 2004
    Inventors: Richard Roux, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
  • Indolylalkylamine derivatives as 5-hydroxytryptamine-6 ligands
    Publication number: 20040209867
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: April 20, 2004
    Publication date: October 21, 2004
    Applicant: Wyeth
    Inventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
  • Fluoroalkoxy-substituted 1,3-dihydro-isoindolyl compounds and their pharmaceutical uses
    Publication number: 20040204448
    Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.
    Type: Application
    Filed: December 29, 2003
    Publication date: October 14, 2004
    Applicant: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man, Weihong Zhang
  • Novel benzothienyl or indole derivatives, preparation and use thereof as inhibitors of prenyl transferase proteins
    Publication number: 20040204417
    Abstract: The invention concerns compounds of general formula (1), wherein, in particular; W represents H, SO2R5. CO(CH2)nR5, (CH2)nR6, CS(CH2)nR5; X represents S or NH; Y represents (CH2)p, CO, (CH2)pCO, CH═CH—CO; Z represents a hetcrocycle, imidazole, benzimidazole, isoxazole, tetrazole, oxadiazole, thiadazole, pyridine, quinazoline, quinoxaline, quinoline, thiophene; R1 represents COOR6, CONR6R7, CO—NH—CH(R6)—COOR7, CH2NR6R7, CH2OR6, (CH2)pR6, CH═CHR6; R2 represents in particular hydrogen, C1-C10 alkyl, a substituted or unsubstituted phenyl; R5 and R6 represents hydrogen, C1—C6 alkyl; R5 represents a substituted or unsubstituted phenyl or naphthyl; R6 and R7, identical or different, represent hydrogen, C1—C15 alkyl, a hetcrocycle. an aryl; n represents 0 to 10; p represents 1 to 6.
    Type: Application
    Filed: May 20, 2004
    Publication date: October 14, 2004
    Inventors: Michel Perez, Marie Lamothe, Bridget Hill, Chantal Etievant
  • 5-sulfonamido-substituted indolinone compounds as protein kinase inhibitors
    Publication number: 20040204407
    Abstract: The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Application
    Filed: March 8, 2004
    Publication date: October 14, 2004
    Applicant: SUGEN Inc.
    Inventors: Peng Cho Tang, Congxin Liang, Todd Miller, Kenneth E. Lipson
  • Heterocyclic compounds
    Patent number: 6803362
    Abstract: Heterocyclic compounds and methods of making them and using them.
    Type: Grant
    Filed: March 8, 2002
    Date of Patent: October 12, 2004
    Assignee: Ortho-McNeil Pharmaceutical inc.
    Inventors: Nicholas I. Carruthers, Wenying Chai, Curt A. Dvorak, James P. Edwards, Cheryl A. Grice, Jill A. Jablonowski, Lars Karlsson, Haripada Khatuya, Jennifer D. Kreisberg, Annette K. Kwok, Timothy W. Lovenberg, Kiev S. Ly, Barbara Pio, Chandravadan R. Shah, Siguan Sun, Robin L. Thurmond, Jianmei Wei, Wei Xiao
  • Indolinone derivatives
    Publication number: 20040198804
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: October 22, 2003
    Publication date: October 7, 2004
    Inventors: John H. Griffin, Roger Briesewitz, Jonathan W. Wary
  • Sulfonamides
    Publication number: 20040198979
    Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
    Type: Application
    Filed: November 7, 2003
    Publication date: October 7, 2004
    Inventors: Dashyant Dhanak, Timothy F. Gallagher, Steven D. Knight
  • 3-(Arylamino)methylene-1, 3-dihydro-2H-indol-2-ones as kinase inhibitors
    Publication number: 20040198720
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: February 20, 2004
    Publication date: October 7, 2004
    Inventors: Steven W. Andrews, Julie A. Wurster, Edward H. Wang, Thomas Malone
  • Prodrugs of a 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
    Patent number: 6797725
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: April 9, 2002
    Date of Patent: September 28, 2004
    Assignee: Sugen, Inc.
    Inventors: Connie Li Sun, Chung Chen Wei, Peng Cho Tang, Marcel Koenig, Yong Zhou, Tomas Vojkovsky, Asaad S. Nematalla
  • Prodrugs of a 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
    Publication number: 20040186161
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Application
    Filed: April 5, 2004
    Publication date: September 23, 2004
    Applicant: Sugen, Inc.
    Inventors: Connie Li Sun, Chung Chen Wei, Peng Cho Tang, Marcel Koenig, Yong Zhou, Tomas Vojkovsky, Asaad S. Nematalla
  • Indole derivatives, process for preparation of the same and use thereof
    Publication number: 20040180885
    Abstract: Indole derivatives represented by formula (I): 1
    Type: Application
    Filed: March 8, 2004
    Publication date: September 16, 2004
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhiko Torisu, Kaoru Kobayashi, Fumio Nambu
  • Phenylindoles for the treatment of HIV
    Publication number: 20040180888
    Abstract: The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier. The compounds of this invention either possess antiviral (i.e., anti-HIV) activity, or are metabolized to a compound that exhibits such activity.
    Type: Application
    Filed: March 22, 2004
    Publication date: September 16, 2004
    Applicant: IDENIX PHARMACEUTICALS INC.
    Inventors: Paulo LaColla, Marino Artico, Jean-Pierre Sommadossi
  • Dipeptidylpeptidase-IV inhibitor
    Publication number: 20040180925
    Abstract: A compound represented by general formula (I):
    Type: Application
    Filed: November 10, 2003
    Publication date: September 16, 2004
    Inventors: Kenji Matsuno, Kimihisa Ueno, Yasuhiro Iwata, Yuichi Matsumoto, Satoshi Nakanishi, Kotaro Tasaki, Hideaki Kusaka, Yuji Nomoto, Akira Ogawa
  • Indolone oxazolidinones and derivatives thereof
    Publication number: 20040176610
    Abstract: The present invention provides antibacterial agents of formula I described herein and intermediates for their preparation.
    Type: Application
    Filed: January 22, 2004
    Publication date: September 9, 2004
    Inventor: Toni-Jo Poel
  • Benzo-fused 5-membered hetrocycle compounds, process for preparation of the same, and use thereof
    Publication number: 20040167171
    Abstract: A compound represented by the formula: 1
    Type: Application
    Filed: December 18, 2003
    Publication date: August 26, 2004
    Inventors: Shigenori Ohkawa, Masaomi Miyamoto, Masahiro Okura, Tetsuya Tsukamoto
  • Vasculostatic agents and methods of use thereof
    Publication number: 20040167198
    Abstract: Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as retinopathies or macular degeneration or other vitreoretinal diseases , inflammatory diseases, vascular leakage syndrome, edema, transplant rejection, adult/acute respiratory distress syndrome (ARDS), and the like.
    Type: Application
    Filed: October 2, 2003
    Publication date: August 26, 2004
    Applicant: TargeGen, Inc.
    Inventors: Wolfgang Wrasidlo, John Doukas, Ivor Royston, Glenn Noronha, John D. Hood, Elena Dneprovskaia, Xianchang Gong, Ute Splittgerber, Ningning Zhao
  • Anti-diabetic agents
    Publication number: 20040157907
    Abstract: The present invention provides compounds of formula (I) 1
    Type: Application
    Filed: November 6, 2003
    Publication date: August 12, 2004
    Applicant: Pfizer Inc
    Inventors: Donald L. Bussolotti, Ronald B. Gammill, Jana Polivkova
  • 4-Aryl substituted indolinones
    Publication number: 20040157909
    Abstract: The present invention relates to 4-arylindolinones, as well as pharmaceutical compositions thereof, capable of modulating protein kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. The present invention also relates to methods for treating protein kinase related disorders.
    Type: Application
    Filed: December 16, 2003
    Publication date: August 12, 2004
    Applicant: Sugen, Inc.
    Inventors: Jingrong Cui, Ruofei Zhang, Hong Shen, Ji Yu Chu, Fang-Jie Zhang, Marcel Koenig, Steven Huy Do, Xiaoyuan Li, Chung Chen Wei, Peng Cho Tang
  • 1-sulfonyl-4-aminoalkoxy indole derivatives and uses thereof
    Patent number: 6774241
    Abstract: The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, R5, R6, and n are as defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.
    Type: Grant
    Filed: June 4, 2003
    Date of Patent: August 10, 2004
    Assignee: Roche Palo Alto LLC
    Inventors: Robin Douglas Clark, Shu-Hai Zhao
  • Sulfonamides
    Publication number: 20040152891
    Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
    Type: Application
    Filed: November 7, 2003
    Publication date: August 5, 2004
    Inventors: Dashyant Dhanak, Timothy F. Gallagher, Steven D. Knight
  • N-(indole-2-carbonyl)-b-alaninamide crystal forms
    Publication number: 20040152758
    Abstract: The instant invention provides crystal forms of 5-chloro-N-[(1S,2R)-3-[3R,4S]-3,4-dihydroxy-1-pyrrolidinyl]-2-hydroxy-3-oxo-1-(phenylmethyl)propyl]-1H-indole-2-carboxamide (I) 1
    Type: Application
    Filed: October 22, 2003
    Publication date: August 5, 2004
    Applicant: Pfizer Inc.
    Inventors: Douglas J. M. Allen, Frank R. Busch, Joseph F. Krzyzaniak, Zheng Jane Li, Susan L. Orrill, Peter R. Rose, Derek L. Tickner, Harry O. Tobiassen
  • Trans-9,10-dehydroepothilone C and D, analogs thereof and methods of making the same
    Publication number: 20040152708
    Abstract: The present invention provides new trans-9,10-dehydroepothilone C and trans-9,10-dehydroepothilone D based derivative compounds, compositions and methods of inhibiting cellular hyperproliferation and/or stabilizing microtubules in vitro and of treatment of hyperproliferative diseases in vivo. Also disclosed are methods of making the compounds.
    Type: Application
    Filed: November 7, 2003
    Publication date: August 5, 2004
    Inventors: Yong Li, Kurt Sundermann, Li Tang, David Myles
  • N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
    Publication number: 20040147760
    Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.
    Type: Application
    Filed: August 22, 2003
    Publication date: July 29, 2004
    Inventors: Richard Charles Thomas, Toni-Jo Poel, Michael Robert Barbachyn, Mikhail Fedor Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh, Vara Prasad Venkata Nagendra Josyula
  • Protease inhibitors of the coagulation cascade isolated from Dysidea sponges
    Publication number: 20040147456
    Abstract: The present invention is directed toward a composition comprising a compound isolated from Dysidea species sponges that is capable of inhibiting serine proteases of the coagulation cascade. In particular, this composition inhibits the TF/VIIa complex of the coagulation cascade. The invention is also directed toward methods employing this composition as a part of anticoagulant therapy.
    Type: Application
    Filed: January 16, 2004
    Publication date: July 29, 2004
    Applicant: Pharmacia Corporation
    Inventors: Gilles H. Goetz, George G. Harrigan, John J. Likos, Thomas P. Kasten
  • Novel hydroxyindoles, their use as inhibitors of phosphodiesterase 4, and processes for preparing them
    Publication number: 20040147759
    Abstract: The invention relates to substituted 4- or/and 7-hydroxyindoles, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active compounds for treating diseases which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 4 activity in immunocompetent cells (e.g. macrophages and lymphocytes).
    Type: Application
    Filed: November 13, 2003
    Publication date: July 29, 2004
    Inventors: Norbert Hofgen, Hildegard Kuss, Ute Egerland, Chris Rundfeldt, Helge Hartenhauer, Antje Gasparic
  • 3-aminoalkyl-2-aryl-indole derivatives and their use as gnrh antagonists
    Publication number: 20040142987
    Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicament, a method of therapeutic treatment using such a compound and processes for producing the compounds.
    Type: Application
    Filed: March 1, 2004
    Publication date: July 22, 2004
    Inventors: James Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall