Plural Nitrogens In The Additional Five-membered Hetero Ring Patents (Class 514/254.05)
  • Publication number: 20040116417
    Abstract: The invention relates to 2-thiohydantoin derivative compounds selected from compounds of general formula (I): 1
    Type: Application
    Filed: September 26, 2003
    Publication date: June 17, 2004
    Inventors: Benaissa Boubia, Evelyne Chaput, Khan Ou, Philippe Ratel
  • Publication number: 20040116416
    Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the formula I 1
    Type: Application
    Filed: January 28, 2004
    Publication date: June 17, 2004
    Inventors: Stefan Laufer, Dunja Kotschenreuther, Philipp Merckle, Karola Tollmann, Hans-Gunter Striegel
  • Patent number: 6747030
    Abstract: Piperazine derivatives of formula(1), processes for their preparation, pharmaceutical compositions containing them in the treatment of CNS and other disorders and in their use in therapy as 5-HT1B antagonists are disclosed herein.
    Type: Grant
    Filed: March 25, 2002
    Date of Patent: June 8, 2004
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Howard Marshall, Mervyn Thompson, Paul Adrian Wyman
  • Publication number: 20040106607
    Abstract: The present invention relates to new compounds of formula I, 1
    Type: Application
    Filed: August 8, 2003
    Publication date: June 3, 2004
    Applicant: AstraZeneca AB and NPS Pharmaceuticals, Inc.
    Inventors: Jalaj Arora, Louise Edwards, Methvin Isaac, Abdelmalik Slassi, Tomislav Stefanac, David Wensbo, Tao Xin
  • Publication number: 20040102454
    Abstract: Methods of using a compound, its pharmaceutically acceptable salts, and/or its pro-drug esters, in isolated form, to treat cancer, and methods for isolating, for formulating, and for administering the compound, salt, and/or pro-drug ester as an antitumor agent, wherein the compound, salt, or pro-drug ester has the following structure: 1
    Type: Application
    Filed: August 1, 2003
    Publication date: May 27, 2004
    Inventors: Yoshio Hayashi, Michael A. Palladino, Jennifer Grodberg
  • Patent number: 6740661
    Abstract: Disclosed are compounds of the formula: wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain between the amide group and the R13 imidazole group is substituted, or R8 represents a substituent such as arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R8 is H, and the alkyl chain between the amide group and the R13 imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: May 25, 2004
    Assignee: Schering Corporation
    Inventors: Arthur G. Taveras, Ronald J. Doll, Alan B. Cooper, Johan A. Ferreira, Timothy Guzi, Alan K. Mallams, Dinanath F. Rane, Viyyoor M. Girijavallabhan, Adriano Afonso, Cynthia J. Aki, Jianping Chao, Carmen Alvarez, Joseph M. Kelly, Tarik Lalwani, Jagdish A. Desai, James J-S Wang, Jay Weinstein
  • Publication number: 20040092518
    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
    Inventor: Shalini Sharma
  • Publication number: 20040092524
    Abstract: The invention concerns compounds corresponding to general formula (I), wherein, in particular: W represents hydrogen, COR6, CSR6, SO2R6, CO(CH2)nR6, (CH2)nR7; X represents CH or N; Y represents (CH2)n, CO, CH2CO, CH═CHCO, CH2CH2CO; Z represents a heterocycle. When Z=pyridine, then Y is other than CO. R1 represents hydrogen, C1-C6 alkyl, halogen OCH3, CF3; R2 and R3, identical or different, represent hydrogen, C1-C6 alkyl; R4 represents a) hydrogen, b) C1-C6 alkyl, c) an aryl, d) a heterocycle; R5 represents hydrogen, COR7R8, SO2R7, CO(CH2)nSR7, CO(CH2)nOR7, CONR7R8, CO(CH2)mCOR7; R6 represents a) a phenyl or a naphthyl, b) a C1-C6 alkyl, a cycloalkyl, c) a heterocycle, d) NR7R8; R7 and R8, identical or different, represent a) hydrogen, C1-C15 alkyl, b) a heterocycle, c) an aryl; n represents 0 to 10; m represents 2 to 10; provided that when Z represents a quinozaline or benzimidazole group, then R5 is other than CH2Ph or methyl and n is other than zero.
    Type: Application
    Filed: November 12, 2003
    Publication date: May 13, 2004
    Inventors: Michel Perez, Marie Lamothe, Anna Kruczynski, Bridget Hill
  • Publication number: 20040082577
    Abstract: Amino methyl imidazoles of Formula I are provided: 1
    Type: Application
    Filed: August 21, 2003
    Publication date: April 29, 2004
    Applicant: Neurogen Corporation
    Inventors: Andrew Thurkauf, He Zhao, Suoming Zhang, Yang Gao
  • Publication number: 20040082551
    Abstract: This invention is directed generally to pyrazoles that, inter alia, inhibit p38 kinase, TNF, and/or cyclooxygenase-2 activity.
    Type: Application
    Filed: June 5, 2003
    Publication date: April 29, 2004
    Inventors: Alan G. Benson, Thomas P. Fraher, Michael E. Hepperle, Kevin D. Jerome, Win Naing, Shaun R. Selness, John K. Walker
  • Patent number: 6720317
    Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Grant
    Filed: September 15, 2000
    Date of Patent: April 13, 2004
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Bing-Yan Zhu, Zhaozhong Jon Jia, Wenrong Huang, Yonghong Song, James Kanter, Robert M. Scarborough
  • Publication number: 20040067960
    Abstract: This invention relates to compounds of the formula 1 1
    Type: Application
    Filed: September 26, 2003
    Publication date: April 8, 2004
    Inventors: Jamie Marie Davis, Tracy Fay Gregory, Michael Anthony Walters
  • Publication number: 20040063691
    Abstract: This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
    Type: Application
    Filed: September 24, 2002
    Publication date: April 1, 2004
    Inventors: Roger A. Smith, Stephen J. O'Connor, Stephan-Nicholas Wirtz, Wai C. Wong, Soongyu Choi, Harold C.E. Kluender, Ning Su, Gan Wang, Furahi Achebe, Shihong Ying
  • Patent number: 6713480
    Abstract: Methods of using a compound, its pharmaceutically acceptable salts, and/or its pro-drug esters, in isolated form, to treat cancer, and methods for isolating, for formulating, and for administering the compound, salt, and/or pro-drug ester as an antitumor agent, wherein the compound, salt, or pro-drug ester has the following generic structure: wherein R1, R2, R3, R4, R5, R6, R7, R8, X1 and X2 are selected from specified residues, as described, and the dashed bond represents either a carbon-carbon single bond or a carbon-carbon double bond.
    Type: Grant
    Filed: November 27, 2001
    Date of Patent: March 30, 2004
    Assignee: Nereus Pharmaceuticals Inc.
    Inventors: Kenji Fukumoto, Shinkichi Kohno, Kaneo Kanoh, Tohru Asari, Hiroshi Kawashima, Hirokatsu Sekiya, Kazunori Ohmizo, Takeo Harada
  • Publication number: 20040058918
    Abstract: The present invention relates to compounds having the general formula 1
    Type: Application
    Filed: September 8, 2003
    Publication date: March 25, 2004
    Inventors: Celia Dominguez, Dawei Zhang
  • Publication number: 20040058913
    Abstract: A cyclic diamine compound of formula (1): 1
    Type: Application
    Filed: August 13, 2003
    Publication date: March 25, 2004
    Applicant: KOWA CO., LTD.
    Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Takeshi Doi, Yoshinori Kyotani
  • Patent number: 6710049
    Abstract: The present invention relates to the derivatives of specially substituted azole compounds which have improved antifungal activity as compared with presently available agents in this class and the processes for the preparation thereof. This invention also relates to pharmaceutical preparations containing the compounds of the present invention and their use in treating and/or preventing the fungal infections in mammals, preferably humans.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: March 23, 2004
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Mohammed Salman, Rita Katoch, Ashwani Kumar Verma, Jitendra Sattigeri, Ashok Rattan
  • Publication number: 20040048862
    Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.
    Type: Application
    Filed: August 8, 2003
    Publication date: March 11, 2004
    Inventors: Giuseppe Alvaro, Romano Di Fabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini
  • Publication number: 20040043995
    Abstract: The invention relates to a compound of formula 1
    Type: Application
    Filed: December 12, 2002
    Publication date: March 4, 2004
    Inventors: Eric Bignon, Jean Pierre Bras, Paul De Cointet, Pierre Despeyroux, Daniel Frehel, Danielle Gully
  • Patent number: 6699864
    Abstract: The present invention provides compounds of the formula: wherein R1-R8, X, Y, Z, n and m are defined in the application. The compounds of the invention have affinity for the 5-HT1A receptor.
    Type: Grant
    Filed: June 20, 2002
    Date of Patent: March 2, 2004
    Assignee: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Christian Krog-Jensen, Mario Rottländer, Gitte Mikkelsen, Ejner Knud Moltzen, Kim Andersen
  • Publication number: 20040038982
    Abstract: This invention relates to substituted heterocyclic compounds which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis, or idiopathic pulmonary fibrosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, treating and/or preventing rejection of transplanted organs, and inflammatory bowel disease, all in mammals, by the use of substituted heterocyclic compounds which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD.
    Type: Application
    Filed: February 5, 2003
    Publication date: February 26, 2004
    Inventors: William E. Bondinell, Michael J. Neeb
  • Patent number: 6696447
    Abstract: The present application describes compounds of general formula I where R1 is selected from any one of pyridinyl, thienyl, furanyl, imidazolyl, and triazolyl; and where each R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the heteroaromatic ring may take place in any position on the ring system. The invention also includes enantiomers, salts and pharmaceutical compositions containing the compounds. The compounds may be used in treating patients for pain.
    Type: Grant
    Filed: September 27, 2002
    Date of Patent: February 24, 2004
    Assignee: AstraZeneca AB
    Inventors: William Brown, Niklas Plobeck, Christopher Walpole
  • Publication number: 20040029887
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: April 29, 2003
    Publication date: February 12, 2004
    Inventors: Pramila A. Bhatia, Jerome F. Daanen, Ahmed A. Hakeem, Teodozyj Kolasa, Mark A. Matulenko, Kathleen H. Mortell, Meena V. Patel, Andrew O. Stewart, Xueqing Wang, Zhiren Xia, Henry Q. Zhang
  • Publication number: 20040029875
    Abstract: A compound of formula (I): 1
    Type: Application
    Filed: April 11, 2003
    Publication date: February 12, 2004
    Inventors: Jean-Luc Fauchere, Jean-Claude Ortuno, Nigel Levens, Susana Chamorro, Jean Albert Boutin
  • Publication number: 20040019046
    Abstract: Phenylacetamido-pyrazoles and, more particularly, N-(5-cycloalkyl-1H-pyrazol-3-yl)phenylacetamido derivatives, optionally further substituted as reported in the description; or pharmaceutically acceptable salts thereof; are useful in the treatment of cell proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
    Type: Application
    Filed: May 19, 2003
    Publication date: January 29, 2004
    Inventors: Paolo Pevarello, Paolo Orsini, Gabriella Traquandi, Gabriella Brasca, Raffaella Amici, Manuella Villa, Claudia Piutti, Mario Varasi, Antonio Longo
  • Publication number: 20040019045
    Abstract: This invention provides a compound of the formula (I): 1
    Type: Application
    Filed: April 9, 2003
    Publication date: January 29, 2004
    Inventors: Misato Hirano, Kazunari Nakao, Seiji Nukui, Tatsuya Yamagishi
  • Publication number: 20040009976
    Abstract: This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.
    Type: Application
    Filed: April 30, 2002
    Publication date: January 15, 2004
    Inventors: Kumiko Takeuchi, Michael Robert Jirousek, Michael Paal, Gerd Ruhter, Theo Schotten
  • Publication number: 20040010014
    Abstract: This invention is directed towards novel compounds as opioid receptor modulators, antagonists, and agonists useful for the treatment of opioid modulated disorders such as pain and gastrointestinal disorders.
    Type: Application
    Filed: March 26, 2003
    Publication date: January 15, 2004
    Inventors: Henry J. Breslin, Wei He, Robert W. Kavash
  • Patent number: 6670363
    Abstract: The present invention relates to the derivatives of specially substituted azole compounds which have improved antifungal activity as compared to known compounds such as fluconazole and itraconazole and the processes for the preparation thereof. This invention also relates to pharmaceutical compositions containing the compounds of the present invention and their use in treating and/or preventing fungal infections in mammals, preferably humans.
    Type: Grant
    Filed: May 22, 2000
    Date of Patent: December 30, 2003
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Ashwani Kumar Verma, Sudershan K. Arora, Jasbir Singh Arora, Ashok Rattan
  • Publication number: 20030232836
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: May 23, 2002
    Publication date: December 18, 2003
    Inventors: Andrew O. Stewart, Teodozyj Kolasa
  • Publication number: 20030232807
    Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.
    Type: Application
    Filed: October 4, 2002
    Publication date: December 18, 2003
    Inventors: Graham S. Poindexter, Guanglin Luo, Ling Chen
  • Publication number: 20030229094
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: May 23, 2003
    Publication date: December 11, 2003
    Inventors: Pramila A. Bhatia, Jerome F. Daanen, Ahmed A. Hakeem, Teodozyj Kolasa, Mark A. Matulenko, Kathleen H. Mortell, Meena V. Patel, Andrew O. Stewart, Xueqing Wang, Zhiren Xia, Henry Q. Zhang
  • Patent number: 6660732
    Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: September 25, 2001
    Date of Patent: December 9, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashehar Betageri, Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, Thomas M. Kirrane, Monica H. Moriak, Neil Moss, Usha R. Patel, John R. Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi
  • Publication number: 20030225146
    Abstract: Provided is a method of treating or ameliorating a number of indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I or IA, 1
    Type: Application
    Filed: May 19, 2003
    Publication date: December 4, 2003
    Inventors: Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
  • Publication number: 20030225072
    Abstract: The invention provides compounds of formula I: 1
    Type: Application
    Filed: February 7, 2003
    Publication date: December 4, 2003
    Inventors: William J. Welsh, Seong Jae Yu, Anil Nair
  • Publication number: 20030225103
    Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells.
    Type: Application
    Filed: March 25, 2003
    Publication date: December 4, 2003
    Applicant: DMI BioSciences, Inc.
    Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K.R. Rao, Greg Thomas
  • Patent number: 6656933
    Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: September 25, 2001
    Date of Patent: December 2, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Eugene R. Hickey
  • Publication number: 20030220319
    Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: 1
    Type: Application
    Filed: January 31, 2003
    Publication date: November 27, 2003
    Inventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova
  • Publication number: 20030220323
    Abstract: The invention relates to new &agr;-arylethylpiperazine derivatives, which are useful as neurokinin receptor antagonists (NK1antagonists). It also relates to processes for the preparation of said &agr;-arylethylpiperazine derivatives, to their use for the prevention and/or treatment of a condition associated with pathogical levels of substance P in a patient and to pharmaceutical compositions containing them.
    Type: Application
    Filed: August 30, 2002
    Publication date: November 27, 2003
    Inventors: Francoise Stiernet, Christophe Genicot, Marie-Agnes Lassoie, Florence Moureau, Thomas Ryckmans, Thierry Taverne, Jean-Pierre Henichart, Michel Neuwels, Solo Goldstein
  • Patent number: 6649609
    Abstract: The present invention relates to novel 1-phenylbenzimidazole derivatives having particular alkoxycarbonyl substituents in the 5-position of the benz ring and having particular cyclic substituents in the meta-position of the phenyl ring, as well as to pharmaceutical compositions containing these compounds and to methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of GABAA receptor complex, and in particular for inducing and maintaining anaesthesia, sedation, and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: November 18, 2003
    Assignee: Neurosearch A/S
    Inventors: Lene Teuber, Frank Watjen
  • Patent number: 6649611
    Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof; wherein a, b, c, d, e, j, R1, R2, R3, and R4 are as defined herein and are useful to treat inflammation and other immune disorders.
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: November 18, 2003
    Assignee: Pfizer, Inc.
    Inventors: Laura C. Blumberg, Matthew F. Brown, Ronald P. Gladue, Molly A. McGlynn, Christopher S. Poss
  • Publication number: 20030207874
    Abstract: Compounds of formula (I), (IIa) or (IIb) wherein R1-R6, Z, Q and n are as defined in claim 1 and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. Compositions comprising a compound of formula (I), (IIa) or (IIb) are also described.
    Type: Application
    Filed: April 23, 2003
    Publication date: November 6, 2003
    Inventors: Iain Mair McDonald, Caroline Minli Rachel Low, Katherine Isobel Mary Steel, John Spencer
  • Patent number: 6632828
    Abstract: Compounds of the formula I or a pharmaceutically acceptable salt, solvate or N-oxide thereof, wherein X is ═CH— or ═N—; Y is H, halogen, trihaloalkyl, alkyl, alkenyl, cycloalkyl, cycloalkyl, SH, —S-alkyl, or —CN. R is alkyl, —CF3, cycloalkyl, heterocycloalkyl, heterocycloalkyl-alkyl, heteroarylalky or adamantyl, or optionally substituted phenyl, phenoxyalkyl, phenylthioalkyl, pyridyl, thienyl, thiazolyl, pyrazinyl, 1,2,5,6-tetrahydropyridine or  wherein R10 and R11 are hydrogen, alkyl or together form a cycloalkyl, are disclosed, as well as pharmaceutical compositions and methods of using said compounds in the treatment of eating disorders and diabetes.
    Type: Grant
    Filed: July 23, 2002
    Date of Patent: October 14, 2003
    Assignee: Schering Corporation
    Inventors: Andrew W. Stamford, Craig D. Boyle, Ying Huang
  • Publication number: 20030191132
    Abstract: Compound of formula (I): 1
    Type: Application
    Filed: November 12, 2002
    Publication date: October 9, 2003
    Inventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
  • Publication number: 20030191134
    Abstract: Non-peptide somatostatin receptor ligands with conformationally restricted side chains exhibiting high binding affinity toward somatostatin receptors are provided. The compounds exhibit a high selectivity and act as agonists at human subtype 2 somatostatin receptors. The compounds are long acting for advantageous use as medicaments in peripheral diseases where somatostatinergic therapy is indicated. Furthermore, many of the compounds are lipophilic and are particularly useful for treating central nervous system and ophthalmic diseases where penetration of the blood brain and blood retinal barriers is required. It is a further object to describe the preferred stereoisomers of these somatostatin agonists and processes for their preparation. Further objects will become apparent from reading the following description.
    Type: Application
    Filed: November 7, 2002
    Publication date: October 9, 2003
    Inventors: Gideon Shapiro, Michael G. Natchus, Mark A. Lockwood, Simona Jurczyk
  • Publication number: 20030176426
    Abstract: Provided is a method of treating or ameliorating an indication of the invention in an animal, including a human, by administering an effective amount of a compound of the formula I: 1
    Type: Application
    Filed: January 30, 2003
    Publication date: September 18, 2003
    Applicant: Alteon, Inc.
    Inventors: Dilip Wagle, Sara Vasan, Martin Gall
  • Patent number: 6620826
    Abstract: Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
    Type: Grant
    Filed: January 29, 2003
    Date of Patent: September 16, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Joseph Weinstock, Jia-Ning Xiang
  • Publication number: 20030171377
    Abstract: The present invention provides compounds of Formula (I): 1
    Type: Application
    Filed: August 22, 2002
    Publication date: September 11, 2003
    Inventors: Christopher Franklin Bigge, Alexander James Bridges, Agustin Casimiro-Garcia, Stephen Alan Fakhoury, Helen Tsenwhei Lee, Jessica Reed, Robert Schaum, Kevin Matthew Schlosser, Karen Sexton, Hairong Zhou
  • Patent number: 6617324
    Abstract: A class of pyrazole derivatives described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
    Type: Grant
    Filed: April 2, 2002
    Date of Patent: September 9, 2003
    Assignee: G. D. Searle & Company
    Inventors: Ashok S. Naraian, Michael Clare, Paul W. Collins, Joyce Zuowu Crich, Rajesh Devraj, Daniel L. Flynn, Lifeng Geng, Matthew J. Graneto, Cathleen E. Hanau, Gunnar J. Hanson, Susan J. Hartmann, Michael Hepperle, He Huang, Francis J. Koszyk, Shuyuan Liao, Suzanne Metz, Richard A. Partis, Thao D. Perry, Shashidhar N. Rao, Shaun Raj Selness, Michael S. South, Michael A. Stealey, John Jeffrey Talley, Michael L. Vazquez, Richard M. Weier, Xiangdong Xi, Ish K. Khanna, Yi Yu
  • Publication number: 20030166616
    Abstract: Excellent tachykinin receptor antagonistic activity is provided by 2-phenylpiperazine derivatives. The piperazine derivatives exhibit a strong inhibitory action against a tachykinin-induced increase of vascular permeability in in vivo tests. Moreover, the derivatives show a preferred transfer into blood, a long half-life in blood in pharmacokinetic tests of oral administration to rats or guinea pigs, and are very stable in blood plasma of various animals. Consequently, a piperazine derivative of the present invention is very useful as a tachykinin antagonist.
    Type: Application
    Filed: February 20, 2003
    Publication date: September 4, 2003
    Inventors: Takashi Ogino, Yukari Konishi, Kunihiko Higashiura, Kazuhito Furukawa