Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/233)
  • Publication number: 20100056794
    Abstract: Process for the preparation of 2,5-bis(2,2,2-trifluoroethoxy)-N-(2-piperidylmethyl)benzamide, its pharmaceutically acceptable salts and important intermediates thereof that involves 1,4-dihalotoluenes as starting material. The method involves a technique for preparing the starting material 2,5-bis(2,2,2-trifluoroethoxy)toluene in high yields by reacting 1,4-dibromotoluene with 2,2,2-trifluoroethanol in presence of a base and a copper-containing catalyst.
    Type: Application
    Filed: November 2, 2007
    Publication date: March 4, 2010
    Applicant: GRINDEKS A JOINT STOCK COMPANY
    Inventors: Daina Zicane, Janis Jaunbergs
  • Publication number: 20090306141
    Abstract: The invention provides compounds of general formula (I) wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: May 4, 2009
    Publication date: December 10, 2009
    Inventors: Tomas Eriksson, Tomas Klingstedt, Tesfaledet Mussie
  • Publication number: 20090286765
    Abstract: A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.
    Type: Application
    Filed: June 13, 2006
    Publication date: November 19, 2009
    Inventors: Wesley Peter Blackaby, Ian Thomas Huscroft, Linda Elizabeth Keown, Richard Thomas Lewis, Piotr Antoni Raubo, Leslie Joseph Street, Christopher George Thomson, Joanne Thomson
  • Publication number: 20090270451
    Abstract: The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
    Type: Application
    Filed: October 27, 2006
    Publication date: October 29, 2009
    Applicants: MERCK & CO., INC., MERCK SHARP & DOHME LIMITED
    Inventors: David Hallett, Craig W. Lindsley, Elizabeth M. Naylor, Zhijian Zhao, Cory R. Theberge, Scott E. Wolkenberg, M. Brad Nolt
  • Publication number: 20090253701
    Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Application
    Filed: June 12, 2009
    Publication date: October 8, 2009
    Inventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, holger Sellner
  • Patent number: 7592373
    Abstract: Compounds of formula (I) wherein A, B, b, W, X, Y, Z, R1, R2, and R3 have the meanings given in claim 1, pharmaceutical compositions these compounds, and methods of preventing or treating metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes using these compounds.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: September 22, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Lehmann-Lintz, Ralf R. H. Lotz, Philipp Lustenberger, Stephan Georg Mueller, Gerald Juergen Roth, Klaus Rudolf, Marcus Schindler, Dirk Stenkamp, Leo Thomas
  • Publication number: 20090203740
    Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
    Type: Application
    Filed: March 21, 2005
    Publication date: August 13, 2009
    Applicant: Dompe' pha.r.ma S.p.A
    Inventors: Marcello Allegretti, Maria Candida Cesta, Riccardo Bertini, Marco Mosca, Francesco Colotta
  • Publication number: 20090181943
    Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.
    Type: Application
    Filed: April 9, 2008
    Publication date: July 16, 2009
    Applicant: METHYLGENE INC.
    Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
  • Publication number: 20090124664
    Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    Type: Application
    Filed: November 24, 2006
    Publication date: May 14, 2009
    Inventors: Marcello Allegretti, Alessio Moriconi, Andrea Aramini, Maria Candida Cesta, Andrea Beccari, Riccardo Bertini
  • Patent number: 7524963
    Abstract: In one embodiment, the present invention describes the synthesis of (4-bromophenyl) (4-piperidyl)methanone-(Z)-O-ethyloxime and its acid salts, and similar compounds, in high stereochemical purity.
    Type: Grant
    Filed: April 4, 2005
    Date of Patent: April 28, 2009
    Assignee: Schering Corporation
    Inventors: George S. K. Wong, Jeonghan Park, Weidong Tong, Ramani R. Raghavan
  • Publication number: 20090062296
    Abstract: Nitroderivatives of prostaglandin amides having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
    Type: Application
    Filed: June 28, 2006
    Publication date: March 5, 2009
    Inventors: Francesca Benedini, Valerio Chiroli, Wesley Kwan Mung Chong, Achim Hans-Peter Krauss, Michael Ross Niesman, Ennio Ongini
  • Publication number: 20090053721
    Abstract: The present invention provides novel methods and compositions for identifying ion channel modulating compounds, including atrial-selective antiarrhythmic agents and ion channel modulating compounds that preferentially modulate K+ channels. The ion channel modulating compounds identified according to these methods are associated with a reduced incidence of ventricular proarrhythmia.
    Type: Application
    Filed: August 8, 2008
    Publication date: February 26, 2009
    Applicant: CARDIOME PHARMA CORP.
    Inventor: David Fedida
  • Publication number: 20080312446
    Abstract: Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagnosis of Parkinson's disease. Another aspect of the present invention relates to piperidine monoamine transporter ligands, comprising a functional group capable of chelating a radionuclide, e.g., technetium, and methods of use thereof.
    Type: Application
    Filed: October 31, 2007
    Publication date: December 18, 2008
    Inventors: John W. Babich, Miles P. Smith
  • Patent number: 7459560
    Abstract: Processes and intermediates for preparing 2-substituted piperidines such as 2-substituted d-threo piperidines are provided, including processes and intermediates for resolution of piperidyl acetamide stereoisomers.
    Type: Grant
    Filed: February 23, 2006
    Date of Patent: December 2, 2008
    Assignee: Celgene Corporation
    Inventors: Vikram Khetani, Yalin Luo, Sowmianarayanan Ramaswamy
  • Patent number: 7459467
    Abstract: The present invention discloses selective and complete reduction of pyridine ring in a biaryl system comprising ?-substituted or non-substituted benzene ring and relates more specifically, not exclusively, for the manufacture of methylphenidate, which is used for treatment of Attention Deficit Hyperactive Disorder (ADHD) and also acts as central nervous system stimulant, by using palladium/C in a solvent such as C1-C4 alcohols in presence of molar quantities of organic and/or inorganic acids.
    Type: Grant
    Filed: June 10, 2005
    Date of Patent: December 2, 2008
    Assignee: IPCA Laboratories, Ltd.
    Inventors: Ashok Kumar, Dharmendra Singh, Swapnali Hemant Patil, Ganesh Devidas Mahale, Uttamrao Arjunrao Sawant
  • Publication number: 20080275028
    Abstract: The present invention relates to compounds with ?7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.
    Type: Application
    Filed: July 19, 2005
    Publication date: November 6, 2008
    Inventors: Giovanni Gaviraghi, Chiara Ghiron, Hendrik Bothmann, Renza Roncarati, Georg Christian Terstappenn
  • Patent number: 7427632
    Abstract: Compounds of formula (I) in which R1, n, Z, R3 and R4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment of thrombotic disorders.
    Type: Grant
    Filed: December 22, 2003
    Date of Patent: September 23, 2008
    Assignee: Eli Lilly and Company
    Inventors: Scott Martin Sheehan, Brian Morgan Watson, John Walter Liebeschuetz
  • Publication number: 20080207694
    Abstract: Compounds of structure (I) having histone deacetylase (HDAC) inhibitor activity are described. The compounds are chemically characterised by the presence of hydroxamic acid, with zinc as chelator, and an aromatic nucleus connected by a linker in which either a bicyclic aromatic system or a piperidino ring are present.
    Type: Application
    Filed: March 14, 2006
    Publication date: August 28, 2008
    Inventors: Cristina Rossi, Marina Porcelloni, Piero D'Andrea, Daniela Fattori, Elena Marastoni
  • Publication number: 20080200467
    Abstract: Disclosed are alpha keto amide and alpha hydroxy amide compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.
    Type: Application
    Filed: November 2, 2007
    Publication date: August 21, 2008
    Inventors: Dinesh Patel, Richard D. Gless, Heather K. Webb Hsu, Sampath Kumar Anandan, Bhaskar R. Aavula
  • Publication number: 20080194520
    Abstract: The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Application
    Filed: December 19, 2005
    Publication date: August 14, 2008
    Inventors: Dominique Swinnen, Agnes Bombrun, Patrick Gerber, Catherine Jorand-Lebrun
  • Publication number: 20080166332
    Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis.
    Type: Application
    Filed: August 26, 2005
    Publication date: July 10, 2008
    Applicant: ELAN PHARMACEUTICALS, INC.
    Inventors: Roy Hom, Lawrence Fang, Varghese John
  • Patent number: 7381721
    Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Grant
    Filed: March 17, 2003
    Date of Patent: June 3, 2008
    Assignee: Adolor Corporation
    Inventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
  • Publication number: 20080108663
    Abstract: The present invention is directed to cyclopropyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neuro-transmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
    Type: Application
    Filed: September 26, 2005
    Publication date: May 8, 2008
    Inventors: Craig W. Lindsley, David D. Wisnoski, Scott E. Wolkenberg
  • Patent number: 7351719
    Abstract: The present invention relates to amide compounds of general formula I wherein the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one amide according to the invention. In view of the MCH receptor-antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
    Type: Grant
    Filed: October 31, 2003
    Date of Patent: April 1, 2008
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Philipp Lustenberger, Klaus Rudolf, Thorsten Lehmann-Lintz, Kirsten Arndt, Ralf Lotz, Martin Lenter, Heike-Andrea Wieland
  • Patent number: 7335681
    Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
    Type: Grant
    Filed: September 15, 2006
    Date of Patent: February 26, 2008
    Assignee: The Regents of the University of Michigan
    Inventor: James A. Shayman
  • Patent number: 7291632
    Abstract: The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R3c? or N?; R1 is C2–C6 alkyl, substituted C2–C6 alkyl, C3–C7 cycloalkyl, substituted C3–C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1–C3 n-alkyl, C3–C6 cycloalkyl-C1–C3 alkyl, or a group of formula II (II) provided that when R1 is C2–C6 alkyl or substituted C2–C6 alkyl, R2 is hydrogen or methyl; R3a, R3b, and, when X is C(R3c)?, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1–C3 alkyl; R5 is hydrogen, C1–C3 alkyl, or C3–C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1–C6 alkyl; and n is an integer from 1 to 6 inclusively.
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: November 6, 2007
    Assignee: Eli Lilly and Company
    Inventors: Maria-Jesus Blanco-Pillado, Michael Philip Cohen, Sandra Ann Filla, Kevin John Hudziak, Daniel Timothy Kohlman, Dana Rae Benesh, Frantz Victor, Yao-Chang Xu, Bai-Ping Ying, DeAnna Piatt Zacherl, Deyi Zhang, Brian Michael Mathes
  • Patent number: 7279582
    Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Grant
    Filed: October 25, 2002
    Date of Patent: October 9, 2007
    Assignee: Abbott Laboratories
    Inventors: Eric J. Stoner, Arthur J. Cooper, Lawrence Kolaczkowski, Ketan M. Patel, Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Daniel A. Dickman, Patricia A. Oliver, Jien-Heh J. Tien
  • Patent number: 7214798
    Abstract: Compound corresponding to the general formula (I): in which A=N or CR2; R2=H, F, OH, CN, CF3, C1-6-alkyl, C1-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3=CHR4CONHR5; R4=H or C1-6-alkyl; R5=H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1–C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate. Therapeutic uses thereof.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: May 8, 2007
    Assignee: Sanofi-Aventis
    Inventors: Ahmed Abouabdellah, Philippe Burnier, Christian Hoornaert, Jean Jeunesse, Frederic Puech
  • Patent number: 7199158
    Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7?, R8, R30–R34, X?, Y, Y?, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 18, 2005
    Date of Patent: April 3, 2007
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 7196197
    Abstract: Process for the preparation of Flecainide, its pharmaceutically acceptable salts and important intermediates thereof that involves the use of the 2-halobenzoic acid and its derivatives as a starting material. The use of this process also allows for the synthesis of a novel intermediate useful in the production of Flecainide. This new process is an inexpensive and efficient process for the manufacture of these compounds.
    Type: Grant
    Filed: September 17, 2003
    Date of Patent: March 27, 2007
    Assignee: Apotex Pharmachem Inc.
    Inventors: Zhi-Xian Wang, Yuanqiang Li, Bhaskar Reddy Guntoori
  • Patent number: 7148251
    Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: December 12, 2006
    Assignee: The Regents of the University of Michigan
    Inventor: James A. Shayman
  • Patent number: 7129251
    Abstract: The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase and/or at least one nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent.
    Type: Grant
    Filed: July 14, 2005
    Date of Patent: October 31, 2006
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, Chia-En Lin, Tiansheng Wang
  • Patent number: 7129228
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
    Type: Grant
    Filed: January 7, 2004
    Date of Patent: October 31, 2006
    Assignee: Sepracor Inc.
    Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
  • Patent number: 7119203
    Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: October 10, 2006
    Assignee: Pharmacia Corporation
    Inventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, David L. Brown, Jeffery N. Carroll, Yiyuan Chen, Yvette M. Fobian, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Robert M. Heintz, Susan L. Hockerman, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Mark A. Massa, Joseph J. McDonald, Brent V. Mischke, Deborah A. Mischke, Patrick B. Mullins, Mark A. Nagy, Monica B. Norton, Joseph G. Rico, Michelle A. Schmidt, Nathan W. Stehle, John J. Talley, William F. Vernier, Clara I. Villamil, Lijuan J. Wang, Thomas A. Wynn
  • Patent number: 7105545
    Abstract: The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alky
    Type: Grant
    Filed: April 2, 2002
    Date of Patent: September 12, 2006
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Walter Kunz, Clemens Lamberth, Fredrik Cederbaum, Martin Zeller
  • Patent number: 7105544
    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: Grant
    Filed: January 14, 2003
    Date of Patent: September 12, 2006
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Mohammad R. Marzabadi, John M. Wetzel, Chien-An Chen, Yu Jiang, Kai Lu
  • Patent number: 7101878
    Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, 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: Grant
    Filed: August 20, 1999
    Date of Patent: September 5, 2006
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Mark Brian Anderson, Haresh N. Vazir, David Robert Luthin, Genevieve DeGuzman Paderes, Ved P. Pathak, Lance Christopher Christie, Yufeng Hong, Eileen Valenzuela Tompkins, Haitao Li, James Faust
  • Patent number: 7049441
    Abstract: According to the process as shown in the following scheme having a step for reacting Compound (I) with Compound (II) to produce Compound (III), benzylpiperidine compounds useful as synthesis starting materials of pharmaceutical agents, agricultural chemicals and the like can be produced conveniently by a short step: wherein R1 is a hydrogen atom or an amino-protecting group, R2 is a hydrogen atom, a hydrocarbon group optionally having substituents, an alkoxy group optionally having substituents or a heterocyclic group optionally having substituents, and R3 is a lower alkyl group.
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: May 23, 2006
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shokyo Miki, Mitsuhiro Takeda, Koji Nakamoto
  • Patent number: 6998488
    Abstract: A novel process is provided for the preparation of 4-aryl piperidines, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, male sexual dysfunction, and female sexual dysfunction.
    Type: Grant
    Filed: March 8, 2004
    Date of Patent: February 14, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Genevieve N. Boice, Karen M. Conrad, Edward G. Corley, Louis Matty, Jr., Jerry A. Murry, Cecile G. Savarin
  • Patent number: 6984637
    Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: January 10, 2006
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
  • Patent number: 6962997
    Abstract: Processes and intermediates for preparing 2-substituted piperidines such as 2-substituted d-threo piperidines are provided, including processes and intermediates for resolution of piperidyl acetamide stereoisomers.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: November 8, 2005
    Assignee: Celgene Corporation
    Inventors: Vikram Khetani, Yalin Luo, Sowmianarayanan Ramaswamy
  • Patent number: 6916802
    Abstract: The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
    Type: Grant
    Filed: May 5, 2004
    Date of Patent: July 12, 2005
    Assignees: Genzyme Corporation, The Regents of the University of Michigan
    Inventors: James A. Shayman, David J. Harris, Craig Siegel, Carol A. Nelson, Diane P. Copeland
  • Patent number: 6914142
    Abstract: In one embodiment, the present invention describes the synthesis of (4-bromophenyl) (4-piperidyl)methanone-(Z)—O-ethyloxime and its acid salts, and similar compounds, in high stereochemical purity.
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: July 5, 2005
    Assignee: Schering Corporation
    Inventors: George S. K. Wong, Jeonghan Park, Weidong Tong, Ramani Raghavan
  • Patent number: 6903120
    Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4,-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: June 7, 2005
    Assignee: A. Carlsson Research AB
    Inventors: Clas Sonesson, Ingela Marianne Svan, Anders Kristoffer Lilja, Liselott Lilja Rönnqvist, Jenny Maria Carlberg, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
  • Patent number: 6890937
    Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical.
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: May 10, 2005
    Assignee: Pharmacia Corporation
    Inventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrezcenzo, Theresa R. Fletcher, John N. Freskos, Daniel P. Getman, Gunnar J. Hanson, Susan L. Hockerman, Carol P. Howard, Stephen A. Kolodziej, Madeleine H. Li, Joseph J. McDonald, Deborah A. Mischke, Patrick B. Mullins, Joseph G. Rico, Nathan W. Stehle, Clara I. Villamil
  • Patent number: 6844440
    Abstract: The invention provides a process for the preparation of a compound of the formula 6 comprising the hydrolysis and decarboxylation of a compound of the formula 5 according to the reaction: wherein R and R2 independently a C1-C4 alkyl group or an aralkyl group.
    Type: Grant
    Filed: June 11, 2003
    Date of Patent: January 18, 2005
    Assignee: Chemagis Ltd.
    Inventors: Ori Lerman, Joseph Kaspi, Oded Arad, Mohammed Alnabari, Yana Sery
  • Patent number: 6838468
    Abstract: Compounds of general formula I[Chemical formula should be inserted here. Please see paper copy] R1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, and pyridine N-oxide; where each R1 phenyl ring and 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 phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.
    Type: Grant
    Filed: May 16, 2002
    Date of Patent: January 4, 2005
    Assignee: AstraZeneca AB
    Inventors: William Brown, Christopher Walpole, Zhongyong Wei
  • Publication number: 20040254218
    Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Application
    Filed: June 16, 2003
    Publication date: December 16, 2004
    Inventors: Bertrand Le Bourdonnec, Roland E. Dolle
  • Patent number: RE39263
    Abstract: There is disclosed substituted thiocarboxamides of the general formula (I) useful as herbicides.
    Type: Grant
    Filed: December 12, 2003
    Date of Patent: September 5, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karl-Heinz Linker, Kurt Findeisen, Roland Andree, Mark-Wilhelm Drewes, Andreas Lender, Otto Schallner, Wilhelm Haas, Hans-Joachim Santel, Markus Dollinger
  • Patent number: RE39558
    Abstract: Compounds of this formula are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: April 10, 2007
    Assignee: Pfizer Inc.
    Inventors: Kimberly O. Cameron, Paul A. DaSilva Jardine, Robert L. Rosati