Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Nitrogen Of The Hetero Ring Patents (Class 540/607)
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Patent number: 6887866Abstract: The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.Type: GrantFiled: January 24, 2003Date of Patent: May 3, 2005Assignee: Theravance, Inc.Inventors: Thomas E. Jenkins, Sabine Axt, Jennifer Bolton
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Patent number: 6855706Abstract: 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: GrantFiled: May 20, 2002Date of Patent: February 15, 2005Assignee: 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
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Patent number: 6835831Abstract: 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: GrantFiled: November 26, 2002Date of Patent: December 28, 2004Assignee: Genzyme CorporationInventor: Bradford H. Hirth
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Publication number: 20040259860Abstract: Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula 1Type: ApplicationFiled: May 26, 2004Publication date: December 23, 2004Inventors: John K. Dickson, R. Michael Lawrence, Jacques Y. Roberge, David P. Rotella, Wu Yang
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Publication number: 20040254166Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1Type: ApplicationFiled: April 1, 2004Publication date: December 16, 2004Inventors: Kevin D. Kreutter, Lily Lee, Tianbao Lu, Venkatraman Mohan, Sharmila Patel, Hui Huang, Guozhang Xu, Mark Fitzgerald
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Publication number: 20040254165Abstract: 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: ApplicationFiled: January 30, 2004Publication date: December 16, 2004Inventors: Amala Soumyanath, Robert Charles Hider, Radhakrishnan Venkatasamy
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Publication number: 20040254157Abstract: 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: ApplicationFiled: August 4, 2004Publication date: December 16, 2004Inventors: Thomas Rlle, Thomas Lehmann, Markus Albers, Gerhard Muller, Gerhard Hessler, Rudiger Fischer, Masaomi Tajimi, Karl Ziegelbauer, Kevin Bacon, Haruki Hasegawa, Hiromi Okigami
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Publication number: 20040248882Abstract: 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: ApplicationFiled: March 25, 2004Publication date: December 9, 2004Applicant: Tularik Inc.Inventors: Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein
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Publication number: 20040220401Abstract: 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: ApplicationFiled: May 25, 2004Publication date: November 4, 2004Applicant: Genentech, Inc.Inventors: Brent Blackburn, Alan G. Olivero, Kirk Robarge
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Patent number: 6790978Abstract: 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: GrantFiled: September 28, 2001Date of Patent: September 14, 2004Assignee: Novartis AGInventor: Paivi Jaana Kukkola
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Publication number: 20040171608Abstract: 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: ApplicationFiled: December 18, 2003Publication date: September 2, 2004Applicant: Millennium Pharmaceuticals, Inc.Inventors: Francois Soucy, Louis Flamondon, Mark Behnke, William Roush
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Publication number: 20040142980Abstract: 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: ApplicationFiled: June 30, 2003Publication date: July 22, 2004Inventors: Barry Craig Finzel, Hua Gao, Meredith L. Greene, Rebecca J. Gross, Richard Allen Nugent, Jeffrey A. Pfefferkorn
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Publication number: 20040143115Abstract: This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists 1Type: ApplicationFiled: November 5, 2003Publication date: July 22, 2004Inventors: Clive Leslie Branch, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
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Publication number: 20040127485Abstract: 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 conType: ApplicationFiled: February 26, 2004Publication date: July 1, 2004Inventor: Guiseppe Alvaro
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Publication number: 20040127487Abstract: An agent comprising the benzoic acid of formula (I) 1Type: ApplicationFiled: December 18, 2003Publication date: July 1, 2004Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Kousuke Tani, Kaoru Kobayashi, Takayuki Maruyama
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Publication number: 20040127486Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.Type: ApplicationFiled: December 12, 2003Publication date: July 1, 2004Applicants: Elan Pharmaceuticals, Inc., American Home Products CorporationInventors: 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
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Publication number: 20040106792Abstract: A novel biphenyl compound having GPR 14 antagonistic activity.Type: ApplicationFiled: December 20, 2002Publication date: June 3, 2004Inventors: Naoki Tauri, Takashi Santo, Hiroyuki Watanabe, Kazuyoshi Aso, Tetsuo Miwa, Shiro Takekawa
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Publication number: 20040097487Abstract: 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: ApplicationFiled: October 27, 2003Publication date: May 20, 2004Applicant: 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
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Publication number: 20040087570Abstract: 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: ApplicationFiled: October 16, 2003Publication date: May 6, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Mark Czekaj, Scott I. Klein, Heinz W. Pauls
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Publication number: 20040058904Abstract: 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: ApplicationFiled: September 29, 2003Publication date: March 25, 2004Inventors: Thomas Rolle, Thomas Lehmann, Markus Albers, Gerhard Hebler, Gerhard Muller, Rudiger Fischer, Masaomi Tajimi, Karl Ziegelbauer, Kevin Bacon, Haruki Hasegawa, Hiromi Okigami
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Publication number: 20040048851Abstract: 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: ApplicationFiled: June 3, 2003Publication date: March 11, 2004Inventors: Uros Urleb, Anamarija Zega, Mojca Stegnar, Bakija Alenka Trampus, Tomas Solmajer, Gregor Mlinsek
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Publication number: 20040010030Abstract: Novel anti-infectives and methods of using them are provided.Type: ApplicationFiled: November 5, 2002Publication date: January 15, 2004Inventors: Dashyant Dhanak, Thomas Carr
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Patent number: 6677354Abstract: 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, OType: GrantFiled: December 16, 2002Date of Patent: January 13, 2004Assignee: SmithKline Beecham p.l.c.Inventors: Clive Leslie Branch, Christopher Norbert Johnson, Geoffrey Stemp, Kevin Thewlis
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Patent number: 6653472Abstract: 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: GrantFiled: April 26, 2002Date of Patent: November 25, 2003Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Christine Le Breton, Eric Manginot, Jean-Bernard Cazaux
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Publication number: 20030216381Abstract: A carboxylic acid derivative of formula (1) 1Type: ApplicationFiled: February 20, 2003Publication date: November 20, 2003Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
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Publication number: 20030207864Abstract: 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: ApplicationFiled: March 11, 2003Publication date: November 6, 2003Applicant: Tulark Inc.Inventor: Jonathan B. Houze
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Publication number: 20030195190Abstract: 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: ApplicationFiled: January 30, 2003Publication date: October 16, 2003Inventors: Bernd Peschke, Ingrid Pettersson
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Publication number: 20030186958Abstract: The invention provides compounds of formula 1Type: ApplicationFiled: February 6, 2003Publication date: October 2, 2003Applicant: The Procter & Gamble CompanyInventors: Biswanath De, Stanislaw Pikul, Menyan Cheng, Neil Gregory Almstead, Randall Stryker Matthews, Michael George Natchus, Yetunde Olabisi Taiwo
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Publication number: 20030153554Abstract: The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.Type: ApplicationFiled: January 24, 2003Publication date: August 14, 2003Inventors: Thomas E. Jenkins, Sabine Axt, Jennifer Bolton
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Publication number: 20030149021Abstract: 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: ApplicationFiled: May 28, 2002Publication date: August 7, 2003Applicant: Medinox, Inc.Inventors: Runtao Li, Tieming Cheng, Jingrong Cui, Tingmin Wang
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Patent number: 6602825Abstract: 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: GrantFiled: August 15, 2001Date of Patent: August 5, 2003Assignee: BASF AktiengesellschaftInventors: Olaf Menke, Ingo Sagasser, Gerhard Hamprecht, Robert Reinhard, Cyrill Zagar, Karl-Otto Westphalen, Martina Otten, Helmut Walter
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Publication number: 20030105078Abstract: The invention relates to novel diphenyl derivatives, to processes for their preparation and to their use in medicaments.Type: ApplicationFiled: February 26, 2002Publication date: June 5, 2003Inventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vohringer, Peter Ellinghaus
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Publication number: 20030096802Abstract: The compound of the formula (I) 1Type: ApplicationFiled: July 15, 2002Publication date: May 22, 2003Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Shuichi Ohuchida, Kazuo Kishimoto, Narito Tateishi, Hiroyuki Ohno
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Publication number: 20030092698Abstract: 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: ApplicationFiled: May 10, 2002Publication date: May 15, 2003Inventors: Mark Czekaj, Scott I Klein, Heinz W. Pauls
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Publication number: 20030069223Abstract: 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: ApplicationFiled: June 14, 2002Publication date: April 10, 2003Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 6544986Abstract: 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: GrantFiled: October 9, 2001Date of Patent: April 8, 2003Assignee: Dalhousie UniversityInventors: Sultan Darvesh, David Magee, Zdenek Valenta, Earl Martin
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Patent number: 6534536Abstract: 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: GrantFiled: March 16, 1994Date of Patent: March 18, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau
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Publication number: 20030050299Abstract: 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: ApplicationFiled: July 16, 2002Publication date: March 13, 2003Applicant: Genzyme CorporationInventors: Bradford H. Hirth, Craig Siegel
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Publication number: 20030045518Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): 1Type: ApplicationFiled: July 10, 2002Publication date: March 6, 2003Applicant: Shionogi BioResearch Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono, Zhi-Qiang Xia
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Publication number: 20030004138Abstract: Compound of formula (I): 1Type: ApplicationFiled: June 18, 2002Publication date: January 2, 2003Inventors: Michel Wierzbicki, Jean-Marie Fourquez, Nigel Levens, Bernadette Hussson-Robert, Olivier Nosjean, Michelle Boulanger
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Publication number: 20030004337Abstract: 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, 1Type: ApplicationFiled: May 4, 2001Publication date: January 2, 2003Inventors: Kyung Woon Jung, Cheol Hwan Yoon
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Publication number: 20020177721Abstract: 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: ApplicationFiled: December 4, 2001Publication date: November 28, 2002Inventors: 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
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Publication number: 20020156063Abstract: The present invention thus provides compounds of Formula I: 1Type: ApplicationFiled: April 8, 2002Publication date: October 24, 2002Inventors: Eduardo L. Setti, Shankar Venkatraman
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Patent number: 6451824Abstract: 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: GrantFiled: May 8, 1998Date of Patent: September 17, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Publication number: 20020119965Abstract: 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: ApplicationFiled: April 11, 2002Publication date: August 29, 2002Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.p.A.Inventors: Oreste Piccolo, Roberto Castagnani, Paolo De Witt
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Publication number: 20020107390Abstract: Compounds of the formula 1Type: ApplicationFiled: August 16, 2001Publication date: August 8, 2002Inventor: Paivi J. Kukkola
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Publication number: 20020107235Abstract: 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: ApplicationFiled: October 26, 2001Publication date: August 8, 2002Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
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Publication number: 20020103183Abstract: 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: ApplicationFiled: September 6, 2001Publication date: August 1, 2002Inventors: Louise Robinson, Prasad V.V.S.V. Manchem, Nicolas Cairns, Steven R. Schow
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Patent number: 6423689Abstract: 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: GrantFiled: December 16, 1998Date of Patent: July 23, 2002Assignees: Warner-Lambert Company, Neurex CorporationInventors: 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
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Publication number: 20020095050Abstract: 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: ApplicationFiled: June 12, 2001Publication date: July 18, 2002Inventor: Andrea Vaupel