Chalcogen Bonded Directly To Ring Carbon Of The Additional Six-membered Nitrogen Containing Hetero Ring Patents (Class 514/253.12)
  • PREPARATION OF 1-(SUBSTITUTED ARYL)-5-TRIFLUOROMETHYL-2-(1H)PYRIDONE COMPOUNDS AND SALTS THEREOF AND THEIR APPLICATIONS
    Publication number: 20120142688
    Abstract: A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof.
    Type: Application
    Filed: May 24, 2010
    Publication date: June 7, 2012
    Applicant: CENTRAL SOUTH UNIVERSITY
    Inventors: Gaoyun Hu, Lijian Tao, Jun Chen
  • PREPARATION OF 1-(SUBSTITUTED BENZYL)-5-TRIFLUOROMETHYL-2(1H)PYRIDONE COMPOUNDS AND SALTS THEREOF AND THEIR APPLICATIONS
    Publication number: 20120129859
    Abstract: 1-(substituted benzyl)-5-trifluoromethyl-2(1H)pyridone compounds and their pharmaceutical acceptable salts are disclosed. The preparation methods of the compounds and their salts and the use of the same for preparing the medicaments for treating fibrosis are also disclosed. New pyridine compounds and their salts are obtained from trifluoromethyl pyridone as starting material.
    Type: Application
    Filed: May 24, 2010
    Publication date: May 24, 2012
    Inventors: Gaoyun Hu, Lijian Tao, Jun Chen
  • BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
    Publication number: 20120122850
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Application
    Filed: January 11, 2012
    Publication date: May 17, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
  • Methods of Suppressing Appetite by the Administration of Antagonists of the Serotonin HTR1a or HTR2b Receptors or Inhibitors of TPH2
    Publication number: 20120115778
    Abstract: Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof.
    Type: Application
    Filed: July 15, 2010
    Publication date: May 10, 2012
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Gerard Karsenty, Vijay Yadav, Franck Oury
  • N-BENZYL-4-METHYLENEAMINO-3-HYDROXY-2-PYRIDONES
    Publication number: 20120115876
    Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.
    Type: Application
    Filed: December 26, 2011
    Publication date: May 10, 2012
    Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
  • NOVEL BENZAMIDES, PRODUCTION THEREOF, AND USE THEREOF AS MEDICAMENTS
    Publication number: 20120108572
    Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
    Type: Application
    Filed: August 26, 2009
    Publication date: May 3, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger Wagner, Elke Langkopf, Frank Himmelsbach, Rolf Goeggel, Birgit Jung
  • Cosmetic use of 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carbomamides and related compounds
    Patent number: 8168640
    Abstract: Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: May 1, 2012
    Assignee: Avon Products, Inc.
    Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W. Lyga
  • ANTHELMINTIC AGENTS AND THEIR USE
    Publication number: 20120094981
    Abstract: This invention is directed to compounds of the formula (I) and salts therefore that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds of this invention, pharmaceutical compositions and kits comprising the compounds of this invention, uses of the compounds of this invention to make medicaments, and treatments comprising the administration of the compounds of this invention to animals in need of the treatments.
    Type: Application
    Filed: June 16, 2010
    Publication date: April 19, 2012
    Inventors: Christophe Pierre Alain Chassaing, Thorsten Meyer
  • EGFR INHIBITORS AND METHODS OF TREATING DISORDERS
    Publication number: 20120094999
    Abstract: The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Application
    Filed: May 5, 2010
    Publication date: April 19, 2012
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Pasi Janne, Michael J. Eck, Wenjun Zhou
  • SALTS OF ARYLSULFONAMIDE CCR3 ANTAGONISTS
    Publication number: 20120088769
    Abstract: Provided herein are arylsulfonamide salts, e.g., a salt of a compound of Formula I, which are useful for modulating CCR3 activity, and their pharmaceutical compositions. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: October 10, 2011
    Publication date: April 12, 2012
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventor: Tai Wei LY
  • BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISTS
    Publication number: 20120083489
    Abstract: The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.
    Type: Application
    Filed: June 2, 2010
    Publication date: April 5, 2012
    Inventors: Siegfried Benjamin Christensen IV, Donghui Qin, Shenglin Chen, Xing Huang, Di Li, Fei Li, Lei Li, Xiaojuan Lin, Shi Lu, Zhen Lu, Maoyun Lv, Chuanning Wang, Chengde Wu, Mei Xiao, Haiyu Yu, Weina Zhang, Zhiliu Zhang
  • BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
    Publication number: 20120077794
    Abstract: The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.
    Type: Application
    Filed: June 2, 2010
    Publication date: March 29, 2012
    Applicant: GLAXSMITHKLINE LLC
    Inventors: Siegfried Benjamin Christensen, IV, Donghui Qin, Shenglin Chen, Xing Huang, Di Li, Fei Li, Xiaojuan Lin, Shi Lu, Maoyun Lv, Chengde Wu, Weiliang Xu, Gang Yan, Jianxing Yuan, Weina Zhang, Zhiliu Zhang
  • DERIVATIVES OF N-ACYL-N'-PHENYLPIPERAZINE USEFUL (INTER ALIA) FOR THE PROPHYLAXIS OR TREATMENT OF DIABETES
    Publication number: 20120071489
    Abstract: The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.
    Type: Application
    Filed: April 16, 2010
    Publication date: March 22, 2012
    Inventors: Shizuo Kasai, Kevin Francis McGee, JR.
  • N-benzyl-4-methyleneamino-3-hydroxy-2-pyridones
    Patent number: 8133894
    Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: March 13, 2012
    Assignee: Akebia Therapeutics Inc.
    Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
  • Substituted N-heterocyclic compounds and their use as dopamine Dreceptor ligands
    Patent number: 8114875
    Abstract: The invention relates to substituted N-heterocyclic compounds of general formula (I.A) and to the tautomers of the compounds the physiologically acceptable salts of the compounds and the physiologically acceptable salts of the tautomers of the compounds. The invention also relates to the use of these compounds and their pharmacologically acceptable salts in the production of a pharmaceutical agent for treating diseases that respond to the influence exerted by dopamine D3 receptor ligands, especially for treating diseases of the central nervous system, especially schizophrenia and/or depression.
    Type: Grant
    Filed: December 20, 2005
    Date of Patent: February 14, 2012
    Assignee: Abbott GmbH & Co. KG
    Inventors: Herve Geneste, Daryl R. Sauer
  • Triaryl-sulphonium compounds, kit and methods for labeling positron emitting isotopes
    Publication number: 20120020881
    Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).
    Type: Application
    Filed: December 4, 2009
    Publication date: January 26, 2012
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Lutz Lehmann, Timo Stellfeld, Keith Graham, Jessica Becaud, Linjing Mu
  • Disubstituted ureas and uses thereof in treating heart failure
    Patent number: 8101617
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: September 25, 2008
    Date of Patent: January 24, 2012
    Assignee: Amgen, Inc.
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, Jr.
  • Dihydropyridinone derivatives
    Patent number: 8097629
    Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.
    Type: Grant
    Filed: February 5, 2005
    Date of Patent: January 17, 2012
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Heike Gielen-Haertwig, Barbara Albrecht, Marcus Bauser, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
  • NEW PYRIDONE DERIVATES WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS
    Publication number: 20120010185
    Abstract: The present invention relates to compounds of general formula I wherein the groups and radicals B, k, L, U, V, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their 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: Application
    Filed: September 22, 2011
    Publication date: January 12, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dirk STENKAMP, Stephan Georg MUELLER, Gerald Juergen ROTH, Joerg KLEY, Klaus RUDOLF, Armin HECKEL, Marcus SCHINDLER, Ralf LOTZ, Thorsten LEHMANN-LINTZ
  • PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
    Publication number: 20110319378
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: June 3, 2011
    Publication date: December 29, 2011
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana GONZALEZ BUENROSTRO, Hilary Plake BECK, Xiaoqi CHEN, Richard Victor CONNORS, Jeffrey DEIGNAN, Jason DUQUETTE, John EKSTEROWICZ, Benjamin FISHER, Brian Matthew FOX, Jiasheng FU, Zice FU, Felix GONZALEZ LOPEZ DE TURISO, Michael GRIBBLE, JR., Darin James GUSTIN, Julie Anne HEATH, Xin HUANG, Xianyun JIAO, Michael G. JOHNSON, Frank KAYSER, David John KOPECKY, Sujen LAI, Yihong LI, Zhihong LI, Jiwen LIU, Jonathan Dante LOW, Brian Stuart LUCAS, Zhihua MA, Lawrence McGEE, Joel McINTOSH, Dustin McMINN, Julio Cesar MEDINA, Jeffrey Thomas MIHALIC, Steven Howard Olson, Yosup REW, Philip Marley ROVETO, Daqing SUN, Xiaodong WANG, Yingcai WANG, Xuelei YAN, Ming YU, Jiang ZHU
  • PYRIDINE DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS RELATED TO INSULIN RESISTANCE OR HYPERGLYCEMIA
    Publication number: 20110312970
    Abstract: The present invention provides novel compounds represented by the general formula (I): their stereoisomers, pharmaceutically acceptable salts and their pharmaceutically acceptable solvates thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. The invention also relates to a process for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them.
    Type: Application
    Filed: August 31, 2011
    Publication date: December 22, 2011
    Applicant: PIRAMAL LIFE SCIENCES LIMITED
    Inventors: Nabajyoti DEKA, Sivaramakrishnan HARIHARAN, Swapnil Ramesh BAJARE, Rosalind Adaikalasamy MARITA
  • GLYCINE TRANSPORTER-1 INHIBITORS, METHODS OF MAKING THEM, AND USES THEREOF
    Publication number: 20110312931
    Abstract: The compounds of the present invention are represented by the following formula (I): wherein the substituents R1, R2, R3, R4, (R5)m, R6, A, X, and Y are as defined herein. The compounds are useful in methods of treating a disorder which is created by or is dependent upon inhibiting GlyT-1.
    Type: Application
    Filed: June 2, 2011
    Publication date: December 22, 2011
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Christopher L. CIOFFI, Mark A. WOLF, Peter R. GUZZO, Shuang LIU, Kashinath SADALAPURE, Visweswaran PARTHASARATHY, Jun-Ho MAENG
  • Heterocyclyl compounds
    Patent number: 8071586
    Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y1, Y2, Y3, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.
    Type: Grant
    Filed: July 8, 2009
    Date of Patent: December 6, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
  • BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
    Publication number: 20110281851
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Application
    Filed: July 29, 2011
    Publication date: November 17, 2011
    Applicant: THERAVANCE, INC.
    Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
  • Inhibitor of binding of S1P
    Patent number: 8048898
    Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: (wherein Y1 represents a nitrogen atom or a group represented by CRA, Y2 represents a nitrogen atom or a group represented by CRB, Y3 represents a nitrogen atom or a group represented by CRC, RA, RB and RC, which may be the same or different, each represent a hydrogen atom, etc. (excluding the case where Y1 is CRA, Y2 is CRB and Y3 is CRC), X represents an oxygen atom, etc., R1 represents a C1-C6 alkyl group, etc., R2 represents a C1-C6 alkyl group, etc., R3 represents an optionally substituted phenyl group, etc., R4 represents a hydrogen atom, etc., and R5 represents an optionally substituted phenyl group, etc.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: November 1, 2011
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Naoya Ono, Fumiyasu Shiozawa, Tetsuya Yabuuchi, Hironori Katakai
  • Oxidase inhibitors and their use
    Publication number: 20110263604
    Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.
    Type: Application
    Filed: April 18, 2011
    Publication date: October 27, 2011
    Applicant: Oryzon Genomics, S.A.
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
  • COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY
    Publication number: 20110263557
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119; such as, but not limited to, diabetes, obesity and associated metabolic disorders. Formula (I) is a compound, in which A can have up to 2 ring —CH2- group substituted with —C(O)— and can be partially unsaturated with up to 2 double bonds; Wi and W2 are independently selected from CR10 and N; wherein R10 is selected from hydrogen and C1_6alkyl; Yi is selected from NRn, O and S; wherein Rn is selected from hydrogen and C1_6alkyl; Y2 and Y3 are independently selected from CH and N; Y4 is selected from CH2, OCH2 and NR15; wherein R15 is selected from hydrogen and C1_6alkyl; or the pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 3, 2009
    Publication date: October 27, 2011
    Applicant: IRM LLC
    Inventors: Christopher Cow, Robert Epple
  • Cosmetic Use of 1-Aroyl-N-(2-oxo-3-piperidinyl)-2-Piperazine Carbomamides and Related Compounds
    Publication number: 20110257195
    Abstract: Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.
    Type: Application
    Filed: June 21, 2011
    Publication date: October 20, 2011
    Applicant: Avon Products, Inc.
    Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W. Lyga
  • APOPTOSIS PROMOTERS
    Publication number: 20110256129
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: April 25, 2011
    Publication date: October 20, 2011
    Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Andrew Petros, Xiaohong Song, Xilu Wang, Noah Tu, Michael Wendt, Alexander Shoemaker, Michael Mitten
  • Cosmetic Use of 1-Aroyl-N-(2-oxo-3-piperidinyl)-2-Piperazine Carbomamides and Related Compounds
    Publication number: 20110251213
    Abstract: Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.
    Type: Application
    Filed: June 21, 2011
    Publication date: October 13, 2011
    Applicant: Avon Products, Inc.
    Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W. Lyga
  • LACTAM ACETAMIDES AS CALCIUM CHANNEL BLOCKERS
    Publication number: 20110230459
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Application
    Filed: March 10, 2011
    Publication date: September 22, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
  • COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY
    Publication number: 20110224185
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
    Type: Application
    Filed: May 23, 2011
    Publication date: September 15, 2011
    Inventors: Phillip B. Alper, Mihai Azimioara, Christopher Cow, Robert Epple, Songchun Jiang, Gerald Lelais, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin, Lucas Westcott-Baker
  • Cosmetic use of 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and related compounds
    Patent number: 7993663
    Abstract: Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: August 9, 2011
    Assignee: Avon Products, Inc.
    Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W. Lyga
  • Cosmetic use of 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and related compounds
    Patent number: 7994175
    Abstract: Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.
    Type: Grant
    Filed: December 29, 2008
    Date of Patent: August 9, 2011
    Assignee: Avon Products, Inc
    Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W Lyga
  • Compounds, compositions and methods
    Patent number: 7989455
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: December 14, 2006
    Date of Patent: August 2, 2011
    Assignee: Cytokinetics, Inc.
    Inventors: Bradley P. Morgan, David J. Morgans, Jr., Alex Muci, Pu-Ping Lu, Erica A. Kraynack, Todd Tochimoto
  • 5HT7 RECEPTOR LIGANDS AND COMPOSITIONS COMPRISING THE SAME
    Publication number: 20110183991
    Abstract: The present invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, especially as agonists, identified by using a pharmacophore and a descriptor's profile filter as well as to pharmaceutical compositions comprising them. These compounds are useful in therapy in particular for the treatment and or prophylaxis of a disease in which 5-HT7 is involved, such as CNS disorders.
    Type: Application
    Filed: July 31, 2009
    Publication date: July 28, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Rosalia Pascual-Ramon, Helmut H. Buschmann
  • Hydroxypiperidine derivatives and uses thereof
    Publication number: 20110178066
    Abstract: Chemical agents, such as derivatives of hydroxypiperidine moieties, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of enzymes and structural polypeptides present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
    Type: Application
    Filed: July 21, 2010
    Publication date: July 21, 2011
    Inventors: Norman E. Ohler, Jeffrey W. Watthey, Qin Zong, Paul E. Young, Kathryn J. Strand, Stanislaw Pikul
  • NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO
    Publication number: 20110166116
    Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.
    Type: Application
    Filed: June 23, 2010
    Publication date: July 7, 2011
    Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.
    Inventors: Brian DYCK, Joe A. TRAN, Junko TAMIYA, Florence JOVIC, Troy VICKERS, Chen CHEN, Nicole HARRIOTT, Timothy COON, Neil J. ASHWEEK
  • Piperazinyl-sulfonamide derivatives useful in the treatment of GPR38 receptor mediated diseases
    Patent number: 7964597
    Abstract: Disclosed are motilin agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: June 21, 2011
    Assignee: Glaxo Group Limited
    Inventors: Darren Jason Mitchell, Jonathan Thomas Seal, Geoffrey Stemp, Mervyn Thompson, Susan Marie Westaway
  • Biaryl compounds useful as agonists of the Gpr38 receptor
    Patent number: 7964602
    Abstract: The present invention relates to novel biaryl derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders.
    Type: Grant
    Filed: December 1, 2006
    Date of Patent: June 21, 2011
    Assignee: Glaxo Group Limited
    Inventors: Gregor James MacDonald, Darren Jason Mitchell, Mervyn Thompson, Susan Marie Westaway
  • PIPERAZIN-1-YL-TRIFLUOROMETHYL-SUBSTITUTED-PYRIDINES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS
    Publication number: 20110130408
    Abstract: The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Application
    Filed: July 29, 2009
    Publication date: June 2, 2011
    Inventors: José Manuel l Bartolmé-Nebreda, Gregor James Macdonald, Michiel Luc,Maria Van Gool
  • Piperazines, pharmaceutical compositions and methods of use thereof
    Patent number: 7943622
    Abstract: Disclosed are novel piperazine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
    Type: Grant
    Filed: June 6, 2007
    Date of Patent: May 17, 2011
    Assignee: Cornerstone Therapeutics, Inc.
    Inventors: Roger B. Clark, Daniel Elbaum
  • PROLYL HYDROXYLASE INHIBITORS
    Publication number: 20110110961
    Abstract: Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1?), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.
    Type: Application
    Filed: November 5, 2010
    Publication date: May 12, 2011
    Inventors: Joseph H. Gardner, Robert Shalwitz
  • COMPOSITIONS AND METHODS FOR TREATING COLITIS
    Publication number: 20110112055
    Abstract: Disclosed herein are compositions and methods for treating colitis and other inflammatory bowel diseases, inter alia, indeterminate colitis, Crohn's disease, irritable bowel syndrome and ischemic colitis.
    Type: Application
    Filed: November 5, 2010
    Publication date: May 12, 2011
    Inventors: Joseph H. Gardner, Robert Shalwitz
  • METHODS FOR INCREASING THE STABILIZATION OF HYPOXIA INDUCIBLE FACTOR-1 ALPHA
    Publication number: 20110111058
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Application
    Filed: November 5, 2010
    Publication date: May 12, 2011
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Heterocyclyl pyridyl sulfonamide derivatives, their manufacture and use as pharmaceutical agents
    Patent number: 7939532
    Abstract: Objects of the present invention are the compounds of formula I, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: May 10, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Frederick Brookfield, Jonathan Gridley, Lothar Kling, Michael Prime, Ulrike Reiff, Wolfgang Von Der Saal, Thomas Von Hirschheydt
  • OXYCARBAMOYL COMPOUNDS AND THE USE THEREOF
    Publication number: 20110098276
    Abstract: The invention relates to oxycarbamoyl compounds of Formula I: The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: June 11, 2009
    Publication date: April 28, 2011
    Inventor: Hidenori Mikamiyama
  • Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound
    Patent number: 7915261
    Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: March 29, 2011
    Assignee: Astellas Pharma, Inc.
    Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 7906509
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: March 15, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joshua Kennedy-Smith, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
  • Alkyne-substituted pyridone compounds and methods of use
    Patent number: 7893061
    Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A1-3, R1 and R3-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: February 22, 2011
    Assignee: Amgen Inc.
    Inventor: Ryan White