Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
Type:
Application
Filed:
August 19, 2003
Publication date:
May 20, 2004
Inventors:
Mark T. Goulet, Ravi P. Nargund, Iyassu K. Sebhat, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner, Zhixiong Ye, Jonathan R. Young, Raman K. Bakshi
Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
Type:
Application
Filed:
August 19, 2003
Publication date:
May 13, 2004
Inventors:
Mark T. Goulet, Ravi P. Nargund, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner
Abstract: The present invention relates to biguanide derivatives of formula (I), wherein R1, R2, R3 and R4 have the meanings as given in claim (1). Compounds are useful in the treatment of pathologies associated with hyperglycaemia, such as diabetes.
Abstract: The invention relates to a compound of formula (I):
wherein:
A represents pyridine, pyridinium or piperidine
R1, R2, R3 and R4 are as defined in the description
R5 represents hydrogen, a nitrogen-containing heterocycle or a group of formula (II):
R6 represents hydrogen or linear or branched (C1-C6)alkyl.
and medicinal products containing the same which are useful in treating pain or deficiencies in memory.
Type:
Grant
Filed:
November 27, 2002
Date of Patent:
May 11, 2004
Assignee:
Les Laboratoires Servier
Inventors:
Otto Meth-Cohn, Chu-Yi Yu, Pierre Lestage, Marie-Cécile Lebrun, Daniel-Henri Caignard, Pierre Renard
Abstract: Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
Type:
Application
Filed:
July 17, 2003
Publication date:
May 6, 2004
Inventors:
Jeffrey J Hale, Charles G. Caldwell, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Malcolm MacCoss, Amy Gentry, Christopher L. Lynch, Christopher A. Willoughby, Yuan Cheng
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
Abstract: Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
Type:
Application
Filed:
October 23, 2003
Publication date:
May 6, 2004
Inventors:
Richard L. Apodaca, Curt A. Dvorak, Chandravadan R. Shah, Wei Xiao
Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more substituents selected from halogen, cyano, nitro, and C1-C8-alkyl optionally substituted by cyano or halogen, Ar2 is phenyl optionally which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is C1-C8-alkyl substituted by hydroxy, C1-C8-alkoxy, acyloxy, —N(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, phenyl-C1-C8-alkoxycarbonyl, -CON(R4)R5 or by a monovalent cyclic organic group, R2 and R?3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen, C1-C8-alkyl optionally substituted by hydroxy or phenyl, or phenyl optionally substituted by C1-C8-alkyl, halogen, cyano or C1-C8-alkoxy, or R4
Type:
Application
Filed:
April 8, 2003
Publication date:
May 6, 2004
Inventors:
Gurdip Bhalay, Trevor John Howe, Darren Mark Le Grand
Abstract: The present invention is directed to N-benzyl substituted (piperidin-4-yl)aminobenzamido derivatives which are delta-opioid receptor modulators.
Abstract: The invention relates to novel pyrrolidyl-substituted para-phenylenediamine derivatives, to dye compositions containing them and to the process for dyeing keratin fibers using these compositions.
Abstract: The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated disorder.
Type:
Application
Filed:
August 15, 2003
Publication date:
April 22, 2004
Inventors:
Bart De Corte, William A. Kinney, Bruce E. Maryanoff, Shyamali Ghosh, Li Liu
Abstract: The invention concerns a compound of formula (I), wherein Ar1 represents phenyl, naphthyl or phenyl fused by a C3-8cycloalkyl, where each group is substituted by a group —O-Z and optionally one to three further groups independently represented by R1; Ar2 represents phenyl or 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from halogen, C1-4 alkyl and C1-4 alkoxy; Ar3 represents a phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from hydroxy, alkyl, C1-4 alkoxy, C2-4 alkenyl, C2-4 alkenyloxy, C1-4 perfluoroalkoxy, C1-4 acylamino or an electron withdrawing group; A represents —C(H)—; E represents —C1-6alkylene-; X represents —CON(H or C1-4alkyl)- or —N(H or C1-4alkyl)CO—; Y represents a direct link, —N(H or C1-4alkyl)CO— or —CON(H or C1-4alkyl)-; Z represents a metabolically labile group; R1 re
Type:
Application
Filed:
October 20, 2003
Publication date:
April 15, 2004
Inventors:
Anne Marie Jeanne Bouillot, Agnes Bombrun, Bernard Andre Dumaitre, Rontain Luc Gosmini, Miles Stuart Congreve, Nigel Grahame Ramsden
Abstract: A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.
Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject.
Type:
Application
Filed:
January 14, 2003
Publication date:
April 15, 2004
Inventors:
Mohammad R. Marzabadi, John M. Wetzel, Chien-An Chen, Yu Jiang, Kai Lu
Abstract: The present invention discloses a new and improved process for the preparation 1-substituted diaryl-4-amino-piperidinyl compounds by a one-pot double arylation followed by optional deprotection step(s).
Abstract: Provided herein are racemic or enantiomerically enriched benzoyl piperidine compounds and pharmaceutically useful salts thereof, pharmaceutical compositions comprising an effective amount of racemic or enantiomerically enriched benzoyl piperidine compounds to treat central nervous system diseases and methods of treating central nervous system diseases in a mammal, in particular psychoses and cognition disorders.
Type:
Application
Filed:
August 26, 2002
Publication date:
March 4, 2004
Inventors:
Yong-Moon Choi, Yong-Kil Kim, Jin-Uk Yoo, Eun-Ah Paek, Chun-Eung Park, Sung-Yong Seo, Coo-Min Chung, Joon Heo
Abstract: The present invention relates to a class of compounds represented by the Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula (I), and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or &agr;v &bgr;5 integrin.
Type:
Application
Filed:
August 21, 2003
Publication date:
March 4, 2004
Inventors:
Ish Kurmar Khanna, Michael Clare, Alan Gasiecki, Thomas Rogers, Barbara B. Chen, Mark Russell, Hwang-Fun Lu
Abstract: Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.
Type:
Application
Filed:
August 8, 2002
Publication date:
February 26, 2004
Inventors:
Bertrand Le Bourdonnec, Roland Ellwood Dolle
Abstract: Compounds of general formula (I)
are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
Type:
Grant
Filed:
August 19, 2002
Date of Patent:
February 17, 2004
Assignee:
AstraZeneca Canada Inc.
Inventors:
Daniel Delorme, Edward Roberts, Zhongyong Wei
Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
Type:
Grant
Filed:
May 10, 2002
Date of Patent:
February 10, 2004
Assignee:
Pharmacia Corporation
Inventors:
John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
Type:
Application
Filed:
November 12, 2002
Publication date:
February 5, 2004
Inventors:
John N. Freskos, Y vette M. Fobian, Alok K. Awasthi, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Nizal S. Chandrakumar, Gary A. DeCrescenzo, Bipin N. Desai, Marcia I. Heron, Susan L. Hockerman, Sara M. Jull, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Patrick B. Mullins, Monica B. Norton, Joseph G. Rico, John J. Talley, Mahima Trivedi, Clara I. Villamil, Lijuan Jane Wang
Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
Type:
Grant
Filed:
October 8, 2002
Date of Patent:
February 3, 2004
Assignee:
Zeneca Limited
Inventors:
Dearg S Brown, George R Brown, Philip Cohen
Abstract: The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: 1
Type:
Application
Filed:
June 25, 2003
Publication date:
January 29, 2004
Applicant:
Sloan-Kettering Institute for Cancer Research
Inventors:
William G. Bornmann, Francis Sirotnak, Howard Scher, Ephraim Vidal, Christopher Borelle, David Scheinberg
Abstract: The invention concerns novel lipoic acid derivatives, which have an inhibiting action with respect to NO-synthase enzymes producing nitrogen monoxide NO and/or are agents enabling the regeneration of antioxidants or entities trapping reactive oxygen species (ROS) and intervening in a more general manner in the redox status of thiol groups. The invention also concerns methods for preparing them, pharmaceutical compositions containing them and their use for therapeutic purposes, particularly their use as NO-synthase inhibitors and/or as agents acting more generally in the redox status of thiol groups.
Type:
Application
Filed:
April 21, 2003
Publication date:
January 29, 2004
Applicant:
SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATION SCIENTIFIQUES (S.C.R.A.S)
Inventors:
Jeremiah Harnett, Michel Auguet, Pierre-Etienne Chabrier de Lassauhyere
Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
Type:
Application
Filed:
June 11, 2003
Publication date:
January 22, 2004
Applicant:
Agouron Pharmaceuticals, Inc.
Inventors:
Mark B. Anderson, Lance Christopher Christie, Quyen-Quyen Thuy Do, Jun Feng, Yufeng Hong, Haitao Li, Ved P. Pathak, Ranjan Jagath Rajapakse, Eric T. Sun, Eileen Valenzuela Tompkins
Abstract: This invention provides non-immunosuppressive rapamycin dialdehydes, which are useful as neurotrophic agents, in the treatment of solid tumors, and vascular disease.
Abstract: There are disclosed compounds of the formula I: 1
Type:
Application
Filed:
November 12, 2002
Publication date:
January 15, 2004
Applicant:
Schering Corporation
Inventors:
Richard J. Friary, Joseph A. Kozlowski, Bandarpalle B. Shankar, Michael K.C. Wong, Guowei Zhou, Brian J. Lavey, Neng-Yang Shih, Ling Tong, Lei Chen, Youheng Shu
Abstract: The present invention relates to compounds which comprise a 4-substituted piperidine ring linked to a substituted or unsubstituted hydrocarbyl ring.
Type:
Application
Filed:
April 9, 2003
Publication date:
January 15, 2004
Inventors:
Frank Hallock Ebetino, Xuewei Liu, Mark Gregory Solinsky, John August Wos, Rashid Naeem Mumin
Abstract: The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a 4-substituted piperidine compound fluoride represented by the following formula, a pharmaceutically acceptable salt thereof or hydrates thereof (provided that 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine, a pharmaceutically acceptable salt thereof and hydrates thereof are excluded).
wherein R1 and R2 represent substituents.
Abstract: This invention provides non-immunosuppressive rapamycin 29-enols, which are useful as neurotrophic agents, in the treatment of solid tumors, and vascular disease.
Abstract: Selected substituted piperidine compounds are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Application
Filed:
July 24, 2002
Publication date:
January 8, 2004
Inventors:
Christopher H. Fotsch, Michael Croghan, Elizabeth M. Doherty, Michael G. Kelly, Mark H. Norman, Duncan M. Smith, Nuria Tamayo, Ning Xi, Shimin Xu
Abstract: Compounds of formula (I), compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
Type:
Application
Filed:
December 10, 2002
Publication date:
January 8, 2004
Inventors:
Jeremy Burrows, Anne Cooper, John Cumming, Thomas McInally, Howard Tucker
Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyrone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
Type:
Application
Filed:
January 31, 2003
Publication date:
January 8, 2004
Inventors:
Michael S. South, Chun C Ma, Kevin J Koeller, Hayat K Rahman, William L Neumann
Abstract: Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives, 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.
Abstract: The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
Type:
Application
Filed:
June 19, 2003
Publication date:
January 1, 2004
Applicant:
Pharmacia Corporation
Inventors:
Michael S. South, Brenda Case, Danny J. Garland, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, William L. Neumann, John J. Parlow, David B. Reitz, Melvin L. Rueppel, Ronald K. Webber
Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
Abstract: The invention relates to novel aryl and heteroaryl sulfonates of formula (Ia) and to methods for producing them and to novel aryl and heteroaryl sulfonates of formula (I) for treating and/or preventing diseases, especially for treating pain and neurodegenerative diseases, A representing (C6-C10)-aryl or 5-10-membered heteroaryl, D representing (C6-C10)-arylene or 5-10-membered heteroarylene, R1 representing (C4-C8)-alkyl, (C2-C8)-alkyl, the carbon chain being interrupted by one or two heteroatoms or groups chosen from the following group: —O—, —S—, —SO—and —SO2—, (C2-C8)-alkenyl or (C2-C8)-alkinyl, in formula (Ia); and R1 representing (C3-C8)-alkyl, (C2-C8)-alkyl, the carbon chain being interrupted by one or two heteroatoms or groups chosen from the following group: —O—, —S—,—SO—and —SO2—, (C2-C8)-alkenyl or (C2-C8)-alkinyl.
Type:
Application
Filed:
May 12, 2003
Publication date:
December 18, 2003
Inventors:
Markus Heil, Heinrich Meier, Paul Naab, Arnd Voerste, Jean-Marie-Viktor de Vry, Dirk Denzer, Frank Mauler, Klemens Lustig, Volker Hinz, Swen Allerheiligen
Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”) , apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.
Type:
Application
Filed:
December 6, 2002
Publication date:
December 18, 2003
Applicant:
Vertex Pharmaceuticals Incorporated
Inventors:
Marion M. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
Abstract: The invention relates to new compounds of formula I
or the pharmaceutically acceptable salts thereof,
wherein
R1, R2, R3, R4, X and Ar1 have the meanings given in the specification, as well as the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
Type:
Grant
Filed:
October 16, 2001
Date of Patent:
December 16, 2003
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Horst Dollinger, Franz Esser, Birgit Jung, Gerd Schnorrenberg, Kurt Schromm, Georg Speck