Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Nitrogen Of The Hetero Ring Patents (Class 540/607)
  • Patent number: 6887866
    Abstract: The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: May 3, 2005
    Assignee: Theravance, Inc.
    Inventors: Thomas E. Jenkins, Sabine Axt, Jennifer Bolton
  • Patent number: 6855706
    Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ? 4 integrin. They are used as therapeutic agents for various diseases concerning ? 4 integrin.
    Type: Grant
    Filed: May 20, 2002
    Date of Patent: February 15, 2005
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
  • Patent number: 6835831
    Abstract: Disclosed is a method of preparing a composition comprising a compound represented Structural Formula (I): The method comprises the step of reacting an aldehyde compound R10CHO with an isonitrile compound represented by Structural Formula (II):
    Type: Grant
    Filed: November 26, 2002
    Date of Patent: December 28, 2004
    Assignee: Genzyme Corporation
    Inventor: Bradford H. Hirth
  • Publication number: 20040259860
    Abstract: Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula 1
    Type: Application
    Filed: May 26, 2004
    Publication date: December 23, 2004
    Inventors: John K. Dickson, R. Michael Lawrence, Jacques Y. Roberge, David P. Rotella, Wu Yang
  • Publication number: 20040254166
    Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1
    Type: Application
    Filed: April 1, 2004
    Publication date: December 16, 2004
    Inventors: Kevin D. Kreutter, Lily Lee, Tianbao Lu, Venkatraman Mohan, Sharmila Patel, Hui Huang, Guozhang Xu, Mark Fitzgerald
  • Publication number: 20040254165
    Abstract: The present invention provides compounds of formula (I) and analogues or derivatives thereof for the treatment of skin conditions, such as Vitiligo, which are treatable by the stimulation of melanocyte proliferation and also for treating skin cancer. The compounds may also be used to cosmetically enhance the natural coloration of the skin.
    Type: Application
    Filed: January 30, 2004
    Publication date: December 16, 2004
    Inventors: Amala Soumyanath, Robert Charles Hider, Radhakrishnan Venkatasamy
  • Publication number: 20040254157
    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: August 4, 2004
    Publication date: December 16, 2004
    Inventors: Thomas Rlle, Thomas Lehmann, Markus Albers, Gerhard Muller, Gerhard Hessler, Rudiger Fischer, Masaomi Tajimi, Karl Ziegelbauer, Kevin Bacon, Haruki Hasegawa, Hiromi Okigami
  • Publication number: 20040248882
    Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
    Type: Application
    Filed: March 25, 2004
    Publication date: December 9, 2004
    Applicant: Tularik Inc.
    Inventors: Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein
  • Publication number: 20040220401
    Abstract: Halo-alkoxycarbonyl derivatives are provided as prodrug moieties for pharmaceutical agents containing a basic or polar nitrogen containing functionality. The prodrugs are provided as pharmaceutical compositions as well as in methods of treatment.
    Type: Application
    Filed: May 25, 2004
    Publication date: November 4, 2004
    Applicant: Genentech, Inc.
    Inventors: Brent Blackburn, Alan G. Olivero, Kirk Robarge
  • Patent number: 6790978
    Abstract: Compounds of the present invention of the formula are thyromimetic agents which can be used to prevent and/or treat diseases associated with an imbalance of thyroid hormones, such as hypo- and hyper-thyroidism, obesity, osteoporosis and depression. The compounds of the invention are, in particular, hypolipedemic agents which enhance the clearance of cholesterol from circulation, particularly the clearance of cholesterol in the form of low density lipoproteins (LDL). The compounds are useful for reducing total cholesterol plasma levels in mammals, in particular for reducing levels of LDL-cholesterol. Furthermore, such compounds also lower elevated lipoprotein (a) [Lp(a)] levels, an independent cardiovascular risk factor, in mammals.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: September 14, 2004
    Assignee: Novartis AG
    Inventor: Paivi Jaana Kukkola
  • Publication number: 20040171608
    Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteasome inhibitors.
    Type: Application
    Filed: December 18, 2003
    Publication date: September 2, 2004
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Francois Soucy, Louis Flamondon, Mark Behnke, William Roush
  • Publication number: 20040142980
    Abstract: The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases.
    Type: Application
    Filed: June 30, 2003
    Publication date: July 22, 2004
    Inventors: Barry Craig Finzel, Hua Gao, Meredith L. Greene, Rebecca J. Gross, Richard Allen Nugent, Jeffrey A. Pfefferkorn
  • 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
  • Publication number: 20040127485
    Abstract: The present invention relates to diazepine derivatives of formula (I) wherein R represents hydrogen or C1-4 alkyl; R1 represents hydrogen or C1-4 alkyl; R2 represents trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy or halogen; R3represents halogen or C1-4 alkyl; R4 represents hydrogen, halogen, C1-4 alkyl or COR6; R5 represents hydrogen, C1-4 alkyl or R5 together within the R1 represents C3-7 cycloalkyl; R6 represents hydroxy, amino, methylamino, dimethylamino, 5 membered heteroaryl group containing 1 to 3 heteroatoms selected independently from oxygen, sulphur and nitrogen or a 6 membered heteroaryl group containing 1 to 3 nitrogen atoms; m or n are independently zero or an integer from 1 to 3; X and Y are independently NR7 or methylene; provided that when X is NR7, Y is methylene and when X is methylene, Y is NR7; R7 represents hydrogen, C1-4 alkyl or C3-7 cycloalkyl; and pharmaceutically acceptable salts and solvates thereof; to process for their preparation and their use in the treatment of con
    Type: Application
    Filed: February 26, 2004
    Publication date: July 1, 2004
    Inventor: Guiseppe Alvaro
  • Publication number: 20040127487
    Abstract: An agent comprising the benzoic acid of formula (I) 1
    Type: Application
    Filed: December 18, 2003
    Publication date: July 1, 2004
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kousuke Tani, Kaoru Kobayashi, Takayuki Maruyama
  • Publication number: 20040127486
    Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.
    Type: Application
    Filed: December 12, 2003
    Publication date: July 1, 2004
    Applicants: Elan Pharmaceuticals, Inc., American Home Products Corporation
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
  • Publication number: 20040106792
    Abstract: A novel biphenyl compound having GPR 14 antagonistic activity.
    Type: Application
    Filed: December 20, 2002
    Publication date: June 3, 2004
    Inventors: Naoki Tauri, Takashi Santo, Hiroyuki Watanabe, Kazuyoshi Aso, Tetsuo Miwa, Shiro Takekawa
  • Publication number: 20040097487
    Abstract: An aromatic sulfonyl alpha-cycloamino hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-cycloamino hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Application
    Filed: October 27, 2003
    Publication date: May 20, 2004
    Applicant: G.D. Searle & Co.
    Inventors: Hui Li, Daniel P. Becker, Clara I. Villamil, Terri L. Boehm, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo
  • Publication number: 20040087570
    Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
    Type: Application
    Filed: October 16, 2003
    Publication date: May 6, 2004
    Applicant: AVENTIS PHARMA DEUTSCHLAND GMBH
    Inventors: Mark Czekaj, Scott I. Klein, Heinz W. Pauls
  • 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
  • Publication number: 20040048851
    Abstract: The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. The compounds are used as thrombon inhibitors.
    Type: Application
    Filed: June 3, 2003
    Publication date: March 11, 2004
    Inventors: Uros Urleb, Anamarija Zega, Mojca Stegnar, Bakija Alenka Trampus, Tomas Solmajer, Gregor Mlinsek
  • Publication number: 20040010030
    Abstract: Novel anti-infectives and methods of using them are provided.
    Type: Application
    Filed: November 5, 2002
    Publication date: January 15, 2004
    Inventors: Dashyant Dhanak, Thomas Carr
  • Patent number: 6677354
    Abstract: Disclosed are compounds of formula (I): wherein: Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R3 and R4 is hydrogen or optionally substituted (C1-4)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R3 and R4 together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted; R2 represents phenyl or a 5- or 6-membered heteroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: January 13, 2004
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Clive Leslie Branch, Christopher Norbert Johnson, Geoffrey Stemp, Kevin Thewlis
  • Patent number: 6653472
    Abstract: New intermediates of the formula (II)B described below for the synthesis of amidine derivatives of (−)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid, such as for example (S)-N-{4-[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)-carbonyl]-1-piperazinyl]phenyl}-2-thiophenecarboximidamide wherein A′ is X is —Z1—CO; &rgr; is a bond or a heterocycle selected from the group consisting of piperidine, piperazine, homopiperazine, 2-methylpiperazine, 2,5-dimethyl-piperazine and 4-aminopiperidine; Y is —Z2— or —NR3—Z2, R3 is hydrogen, alkyl of 1 to 6 carbon atoms or —COR4, R4 is alkyl of 1 to 6 carbon atoms; Z1 and Z2 independently are a single bond or alkylene of 1 to 6 carbon atoms; and R6 is hydrogen or OH.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: November 25, 2003
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Christine Le Breton, Eric Manginot, Jean-Bernard Cazaux
  • Publication number: 20030216381
    Abstract: A carboxylic acid derivative of formula (1) 1
    Type: Application
    Filed: February 20, 2003
    Publication date: November 20, 2003
    Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
  • Publication number: 20030207864
    Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Application
    Filed: March 11, 2003
    Publication date: November 6, 2003
    Applicant: Tulark Inc.
    Inventor: Jonathan B. Houze
  • Publication number: 20030195190
    Abstract: Novel amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
    Type: Application
    Filed: January 30, 2003
    Publication date: October 16, 2003
    Inventors: Bernd Peschke, Ingrid Pettersson
  • Publication number: 20030186958
    Abstract: The invention provides compounds of formula 1
    Type: Application
    Filed: February 6, 2003
    Publication date: October 2, 2003
    Applicant: The Procter & Gamble Company
    Inventors: Biswanath De, Stanislaw Pikul, Menyan Cheng, Neil Gregory Almstead, Randall Stryker Matthews, Michael George Natchus, Yetunde Olabisi Taiwo
  • Publication number: 20030153554
    Abstract: The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.
    Type: Application
    Filed: January 24, 2003
    Publication date: August 14, 2003
    Inventors: Thomas E. Jenkins, Sabine Axt, Jennifer Bolton
  • Publication number: 20030149021
    Abstract: In accordance with the present invention, there is provided a new class of compounds, i.e., mono(dithio)carbamate esters of piperazine and analogs thereof, with or without substituents. Also provided are methods for the preparation of invention compounds and the pharmaceutical use thereof in the treatment of a variety of pathological conditions, especially for the treatment of cancers. A lead compound has shown good anticancer activity with low toxicity.
    Type: Application
    Filed: May 28, 2002
    Publication date: August 7, 2003
    Applicant: Medinox, Inc.
    Inventors: Runtao Li, Tieming Cheng, Jingrong Cui, Tingmin Wang
  • Patent number: 6602825
    Abstract: Novel 1-aryl-4-thiotriazines I where the variables have the following meanings: R1=H, NH2, C1-C4-alkyl, C1-C4-haloalkyl; R2=H, NH2, C1-C4-alkyl, C1-C4-haloalkyl; R3=H, halogen; R4=CN, halogen; Y=nitrogen, the methine group or, together with R5, a bridge >C—O—C(R6)═N—; R5=one of the meanings given in the description; R6=H, halogen, substituted or unsubstituted C1-C6-alkyl, C3-C6-alkenyl, C3-C6-alkynyl, C1-C6-alkoxy, C3-C6-alkenyloxy, C3-C6-alkynyloxy, C3-C6-cycloalkyl or C3-C6-cycloalkoxy; their salts and enol ethers, the preparation of the novel compounds I and their use as herbicides.
    Type: Grant
    Filed: August 15, 2001
    Date of Patent: August 5, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Olaf Menke, Ingo Sagasser, Gerhard Hamprecht, Robert Reinhard, Cyrill Zagar, Karl-Otto Westphalen, Martina Otten, Helmut Walter
  • Publication number: 20030105078
    Abstract: The invention relates to novel diphenyl derivatives, to processes for their preparation and to their use in medicaments.
    Type: Application
    Filed: February 26, 2002
    Publication date: June 5, 2003
    Inventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vohringer, Peter Ellinghaus
  • Publication number: 20030096802
    Abstract: The compound of the formula (I) 1
    Type: Application
    Filed: July 15, 2002
    Publication date: May 22, 2003
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shuichi Ohuchida, Kazuo Kishimoto, Narito Tateishi, Hiroyuki Ohno
  • Publication number: 20030092698
    Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
    Type: Application
    Filed: May 10, 2002
    Publication date: May 15, 2003
    Inventors: Mark Czekaj, Scott I Klein, Heinz W. Pauls
  • Publication number: 20030069223
    Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
    Type: Application
    Filed: June 14, 2002
    Publication date: April 10, 2003
    Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
  • Patent number: 6544986
    Abstract: This invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof; in which preferably R3, R4 and R6 are each hydrogen; X is C═O or CH2; and R7 and R8 are each independently selected from the group consisting of hydrogen, (C1-C12)alkyl, (C3-C8)cycloalkyl and (C1-C12)alkyl (C6-C14)aryl; or R7 and R8 when taken together form a (C2-C7)alkylene group; or —NR7R8 together forms a (C2-C14)heterocyclic or substituted (C2-C14)heterocyclic. Such compounds modulate the activity of serine hydrolases and can be used in pharmaceutical compositions for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: April 8, 2003
    Assignee: Dalhousie University
    Inventors: Sultan Darvesh, David Magee, Zdenek Valenta, Earl Martin
  • Patent number: 6534536
    Abstract: Alkylsulfonamido heterocyclic thrombin inhibitors are provided which have the structure wherein G is  wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; R is hydrogen, hydroxyalkyl, aminoalkyl, alkyl, cycloalkyl, amidoalkyl, arylalkyl, alkenyl, aryl, alkynyl, arylalkoxyalkyl, or an amino acid side chain; R1 and R2 are independently hydrogen, lower alkyl, cycloalkyl, aryl, hydroxy, alkoxy, oxo, thioketal, thioalkyl, thioaryl, amino or alkylamino; or R1 and R2 can be taken together with the carbons to which they are attached to form a cycloalkyl, aryl or heteroaryl ring.
    Type: Grant
    Filed: March 16, 1994
    Date of Patent: March 18, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau
  • Publication number: 20030050299
    Abstract: Disclosed is a novel enantiomeric synthesis cermamide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
    Type: Application
    Filed: July 16, 2002
    Publication date: March 13, 2003
    Applicant: Genzyme Corporation
    Inventors: Bradford H. Hirth, Craig Siegel
  • Publication number: 20030045518
    Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): 1
    Type: Application
    Filed: July 10, 2002
    Publication date: March 6, 2003
    Applicant: Shionogi BioResearch Corp.
    Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono, Zhi-Qiang Xia
  • Publication number: 20030004138
    Abstract: Compound of formula (I): 1
    Type: Application
    Filed: June 18, 2002
    Publication date: January 2, 2003
    Inventors: Michel Wierzbicki, Jean-Marie Fourquez, Nigel Levens, Bernadette Hussson-Robert, Olivier Nosjean, Michelle Boulanger
  • Publication number: 20030004337
    Abstract: Lactams, libraries of lactams, and an efficient method of synthesizing a lactam, including a &ggr;-lactam, in which an a-diazoacetamide of the general structure (I) is reacted under conditions promoting intramolecular C-H insertion, for example in the presence of a rhodium salt such as Rh2(OAc)4, 1
    Type: Application
    Filed: May 4, 2001
    Publication date: January 2, 2003
    Inventors: Kyung Woon Jung, Cheol Hwan Yoon
  • Publication number: 20020177721
    Abstract: One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
    Type: Application
    Filed: December 4, 2001
    Publication date: November 28, 2002
    Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory C. Cuny, James R. Hauske, Michele L.R. Heffernan, Michael Z. Hoemann, Donald W. Kessler, Liming Shao, Xinhe Wu, Roger L. Xie
  • Publication number: 20020156063
    Abstract: The present invention thus provides compounds of Formula I: 1
    Type: Application
    Filed: April 8, 2002
    Publication date: October 24, 2002
    Inventors: Eduardo L. Setti, Shankar Venkatraman
  • Patent number: 6451824
    Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: September 17, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
  • Publication number: 20020119965
    Abstract: Carnitine derivatives of formula (I) are described in racemic and/or optically active form, as well as the process for their preparation and their use as pharmaceutical anti-angina active ingredients for the treatment of ischaemic heart disease.
    Type: Application
    Filed: April 11, 2002
    Publication date: August 29, 2002
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.p.A.
    Inventors: Oreste Piccolo, Roberto Castagnani, Paolo De Witt
  • Publication number: 20020107390
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: August 16, 2001
    Publication date: August 8, 2002
    Inventor: Paivi J. Kukkola
  • Publication number: 20020107235
    Abstract: The present invention provides non-steroidal compounds of Formula I, and prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.
    Type: Application
    Filed: October 26, 2001
    Publication date: August 8, 2002
    Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
  • Publication number: 20020103183
    Abstract: Compounds of Formula I, and pharmaceutical compositions containing these compounds, activate the insulin receptor kinase, which leads to an increased sensitivity to insulin and an increase in glucose uptake, and are therefore useful for the treatment of animals, especially humans, with hyperglycemia, especially for the treatment of type 2 diabetes. Processes for preparation of the compounds, and their use in assays, are also disclosed.
    Type: Application
    Filed: September 6, 2001
    Publication date: August 1, 2002
    Inventors: Louise Robinson, Prasad V.V.S.V. Manchem, Nicolas Cairns, Steven R. Schow
  • Patent number: 6423689
    Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: July 23, 2002
    Assignees: Warner-Lambert Company, Neurex Corporation
    Inventors: Richard John Booth, Louis Brogley, Wayne Livingston Cody, David Thomas Connor, Harriet Wall Hamilton, John Xiaoqiang He, Lain-Yen Hu, Leonard Joseph Lescosky, Thomas Charles Malone, Laszlo Nadasdi, Michael Francis Rafferty, Bruce David Roth, Diego F. Silva, Yuntao Song, Balazs G. Szoke, Laszlo Urge
  • Publication number: 20020095050
    Abstract: The present invention relates to new phenylserine derivatives as integrin antagonists with a broad spectrum of action having, inter alia, antiosteoporotic, antirestenotic, anticarcinogenic and antiatherosclerotic activity. The present invention moreover relates to the preparation of these compounds and their use for the production of medicaments, and also medicaments comprising them.
    Type: Application
    Filed: June 12, 2001
    Publication date: July 18, 2002
    Inventor: Andrea Vaupel