Chalcogen Bonded Directly To Ring Carbon Of The Additional Six-membered Nitrogen Containing Hetero Ring Patents (Class 514/253.12)
  • Publication number: 20110034463
    Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.
    Type: Application
    Filed: April 1, 2009
    Publication date: February 10, 2011
    Inventors: Jon Goguen, Ning Pan, Kyungae Lee
  • Publication number: 20110009407
    Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.
    Type: Application
    Filed: April 27, 2010
    Publication date: January 13, 2011
    Inventors: Ying-Zi Xu, Shendong Yuan, David Wone, Andrei Konradi
  • Publication number: 20110003812
    Abstract: Magnesium salts/complexes of compounds useful for inhibiting the ADAM-IO protein and methods of making and purifying them are provided. Further provided are compositions comprising magnesium salts/complexes of the compounds in combination with a pharmaceutically acceptable carrier. The compounds well as such compositions comprising them are useful for the treatment of cancer, arthritis, diseases related to angiogenesis, such as renal diseases, heart diseases, such as heart failure, atherosclerosis, and stroke, inflammation, ulcer, infertility, scleroderma, endometriosis, mesothelioma, and diabetes. In addition, methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role are provided.
    Type: Application
    Filed: October 15, 2008
    Publication date: January 6, 2011
    Applicant: SYMPHONY EVOLUTION, INC.
    Inventors: Sriram Naganathan, JoAnn Wilson, Daniel Dickman
  • Publication number: 20110003825
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    Type: Application
    Filed: August 23, 2010
    Publication date: January 6, 2011
    Applicant: Schering Corporation
    Inventors: Ying Huang, Guoqing Li, Andrew W. Stamford
  • Patent number: 7858643
    Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
    Type: Grant
    Filed: August 26, 2005
    Date of Patent: December 28, 2010
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
  • Publication number: 20100324061
    Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
    Type: Application
    Filed: September 1, 2010
    Publication date: December 23, 2010
    Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
  • Publication number: 20100305097
    Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.
    Type: Application
    Filed: July 28, 2010
    Publication date: December 2, 2010
    Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
  • Publication number: 20100298325
    Abstract: a compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: wherein X and Y are independently NR5 or O; W and Z are independently a bond or (CH2)mCH(R7)(CH2)n; m=0-1, n=0-2; R is hydrogen or halogen; R1 and R2 are independently selected from hydrogen halogen, CF3, CN, OR8, NR9R10, NR9COR11, NR9SO2R11 or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10; R3 is hydrogen, halogen, CF3, CN, OR8, SR8 or SO2R11; R4 is hydrogen, halogen, CF3, OR9, NR9R10, NR9COR11, NR9SO2R11 or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10; R5 is hydrogen or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10; R6 is hydrogen, fluorine, C1-6 alkyl, or C1-6 alkoxy; R6 is hydrogen, fluorine, C1-6 alkyl, or C1-6 alkoxy; R7 is hydrogen, C1-6 alkyl, phenyl or C1-3 alkylphenyl wherein said phenyl groups are optionally substituted by one or more substituents selected from halogen, C1-6 alkyl, CF3, OCF3 or OR9; R8 is hydrogen or C1-6 alkyl optionally substitut
    Type: Application
    Filed: October 6, 2008
    Publication date: November 25, 2010
    Applicant: SENEXIS LIMITED
    Inventors: David Ian Carter Scopes, David Christopher Horwell
  • Publication number: 20100292247
    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: Application
    Filed: October 24, 2007
    Publication date: November 18, 2010
    Applicant: F. HOFFMANN-LA ROCHE AG
    Inventors: Frederick Brookfield, Jonathan Gridley, Lothar Kling, Michael Prime, Ulrike Reiff, Wolfgang von der Saal, Thomas von Hirschheydt
  • Publication number: 20100267701
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Application
    Filed: July 1, 2010
    Publication date: October 21, 2010
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Publication number: 20100210635
    Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
    Type: Application
    Filed: March 23, 2007
    Publication date: August 19, 2010
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Benjamin Jones, Andre A. Kiryanov, Stephen W. Kaldor
  • Publication number: 20100203039
    Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
    Type: Application
    Filed: April 16, 2010
    Publication date: August 12, 2010
    Inventor: Chu-Biao Xue
  • Publication number: 20100197667
    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: April 14, 2010
    Publication date: August 5, 2010
    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
  • Publication number: 20100197697
    Abstract: The present invention relates to a compounds of formula I wherein A, Ar1, Ar2, R1, R2, R3, R4, R5, R6, m, n, o, p, s, t, and u are as defined herein or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: January 25, 2010
    Publication date: August 5, 2010
    Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Publication number: 20100183606
    Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.
    Type: Application
    Filed: March 19, 2010
    Publication date: July 22, 2010
    Inventors: ROBERT M BORZILLERI, Lyndon A.M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
  • Patent number: 7754724
    Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.
    Type: Grant
    Filed: June 30, 2006
    Date of Patent: July 13, 2010
    Assignee: Dow AgroSciences LLC
    Inventors: Beth Anne Lorsbach, James Melvin Ruiz, Thomas Clarence Sparks, Michael Thomas Sullenberger, Irene Mae Morrison, Jeffery Dale Webster
  • Publication number: 20100173886
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity.
    Type: Application
    Filed: May 22, 2008
    Publication date: July 8, 2010
    Inventors: Jason Bloxham, Stuart Edward Bradley, Tom Banksia Dupree, Peter Timothy Fry, Patrick Eric Hanrahan, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth, Alan John Stewart
  • Publication number: 20100166655
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Application
    Filed: March 15, 2007
    Publication date: July 1, 2010
    Applicants: JANSSEN PHARMACEUTICA N.V., ADDEX PHARMACEUTICALS S.A.
    Inventors: Hassan Julien Imogai, Vincent Mutel, Jose Maria Cid-Nunez, Jose Ignacio Andres-Gil, Andres Avelino Trabanco-Suarez, Julen Oyarzabal Santamarina, Frank Matthias Dautzenberg, Gregor James MaCdonald, Shirley Elizabeth Pullan, Robert Johannes Lutjens, Guillaume Albert Jacques Duvey, Vanthea Nhem, Terry Palrick Finn, Gagik Melikyan
  • Publication number: 20100168127
    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: December 23, 2009
    Publication date: July 1, 2010
    Applicant: AVON PRODUCTS, INC.
    Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W. Lyga
  • Publication number: 20100168126
    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: December 29, 2008
    Publication date: July 1, 2010
    Applicant: Avon Products, Inc.
    Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W. Lyga
  • Publication number: 20100160292
    Abstract: Methods of inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, methods of treating patients by inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, chemical entities that bind to BTK and inhibited complexes are provided.
    Type: Application
    Filed: September 11, 2007
    Publication date: June 24, 2010
    Applicant: CGI PHARMACEUTICALS, INC
    Inventors: James A. Whitney, Julie Di Paolo, Mark Velleca, David R. Brittelli, Kevin S. Currie, James W. Darrow, Jeffrey E. Krope, Seung H. Lee, Steven L. Gallion, Scott A. Mitchell, Doughlas A.I. Pippen, Peter A. Blomgren, Doughlas Gregory Stafford
  • Publication number: 20100125079
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 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 25, 2010
    Publication date: May 20, 2010
    Applicant: THERAVANCE, INC.
    Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
  • Publication number: 20100113467
    Abstract: The invention relates to naphthalene carboxylic acid and isoquinoline carboxylic acid amides, and related compounds of formula I and their uses as pharmaceuticals.
    Type: Application
    Filed: April 17, 2008
    Publication date: May 6, 2010
    Inventors: Paul W. Manley, Joseph Schoepfer
  • Publication number: 20100105693
    Abstract: The present invention relates to substituted piperazine compounds that are useful modulators of muscarinic receptors. The present invention also provides compositions comprising such compounds, and methods for treating muscarinic receptor mediated diseases.
    Type: Application
    Filed: January 5, 2010
    Publication date: April 29, 2010
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Lewis Makings, Dennis Hurley, Miguel Gracia-Guzman Blanco, Daniele Bergeron, Akiko Nakatani
  • Patent number: 7700599
    Abstract: The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.
    Type: Grant
    Filed: June 26, 2007
    Date of Patent: April 20, 2010
    Assignee: Glaxo Group Limited
    Inventors: Mervyn Thompson, Susan Marie Westaway
  • Patent number: 7700628
    Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. An example of a compound of formula (I) is (a).
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: April 20, 2010
    Assignee: Eli Lilly and Company
    Inventors: Ankush Baburao Argade, Theodore Goodson, Jr., David Kent Herron, Sajan Joseph, Salvatore Donato Lepore, Angela Lynn Marquart, John Joseph Masters, David Mendel, Leander Merritt, Andrew Michael Ratz, Gerald Floyd Smith, Anne Louise Tebbe, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 7700586
    Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
    Type: Grant
    Filed: September 4, 2002
    Date of Patent: April 20, 2010
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
  • Publication number: 20100075982
    Abstract: The invention provides 3-(methyloxy)-1-{4-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]butyl}-2(1H)-pyridinone of formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 3, 2008
    Publication date: March 25, 2010
    Inventors: Gabriella Gentile, Valeria Zucchelli
  • Publication number: 20100063040
    Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.
    Type: Application
    Filed: September 25, 2006
    Publication date: March 11, 2010
    Inventor: Akira Kugimiya
  • Publication number: 20100009971
    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: Application
    Filed: August 19, 2009
    Publication date: January 14, 2010
    Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
  • Publication number: 20100009972
    Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and 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: Application
    Filed: August 19, 2009
    Publication date: January 14, 2010
    Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
  • Publication number: 20090312344
    Abstract: The present invention relates to ?1, and/or ?1d adrenergic receptor antagonists, which can function as ?1a and/or ?1d adrenergic receptor antagonist and can be used for the treatment of a disease or disorder mediated through ?1a and/or an adrenergic receptor. Compounds disclosed herein can be used for the treatment of benign prostatic hyperplasia (BPH) and the related symptoms thereof. Further, compounds disclosed herein can be used for the treatment of lower urinary tract symptoms associated with or without BPH. Also provided are processes for preparing such compounds, pharmaceutical compositions thereof, and the methods of treating BPH or related symptoms thereof.
    Type: Application
    Filed: May 31, 2005
    Publication date: December 17, 2009
    Inventors: Mohammad Salman, Somesh Sharma, Gyan Chand Yadav, Gobind Singh Kapkoti, Anurag Mishra, Praful Gupta, Nitya Anand, Anita Chugh, Kamna Nanda
  • Patent number: 7615550
    Abstract: The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: November 10, 2009
    Assignee: Glaxo Group Limited
    Inventors: Thomas Daniel Heightman, Simon Teanby Hodgson, Matthew J Lindon, David Matthew Wilson
  • Patent number: 7589090
    Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the compounds being of formula (I): wherein R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: February 27, 2008
    Date of Patent: September 15, 2009
    Assignee: Roche Palo Alto LLC
    Inventors: Michael Patrick Dillon, Alam Jahangir
  • Publication number: 20090203711
    Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: wherein: G is —N? or —CH?; B is an optionally substituted divalent mono- or bicyclic aryl or heteroaryl radical having 5-13 ring members; R2 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2)z-L1-Y1—R wherein A, z, Y1, and L1 are as defined in the specification; R is a radical of formula (X) or (Y) wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl or heteroaryl or —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; and D is a monocyclic heterocycl
    Type: Application
    Filed: May 1, 2007
    Publication date: August 13, 2009
    Applicant: CHROMA THERAPEUTICS LTD.
    Inventor: David Charles Festus Moffat
  • Publication number: 20090186894
    Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: December 21, 2007
    Publication date: July 23, 2009
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
  • Patent number: 7544683
    Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
    Type: Grant
    Filed: June 10, 2008
    Date of Patent: June 9, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Matthias Nettekoven, Jean-Marc Plancher, Olivier Roche, Sebastien Schmitt, Tadakatsu Takahashi
  • Publication number: 20090131417
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Application
    Filed: November 17, 2008
    Publication date: May 21, 2009
    Inventors: Michael A. Letavic, Kiev S. Ly
  • Publication number: 20090124633
    Abstract: The present invention relates to heterocyclic substituted N-Oxides of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
    Type: Application
    Filed: March 26, 2007
    Publication date: May 14, 2009
    Inventors: Alfred Jonczyk, Wilfried Rautenberg
  • Publication number: 20090036429
    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: February 16, 2007
    Publication date: February 5, 2009
    Inventors: Norman E. Ohler, Jeffrey W. Watthey, Qin Zong, Paul Young, Kathryn J. Strand
  • Patent number: 7482348
    Abstract: The present invention relates to piperazine substituted cyclohexane-1,4-diamine compounds of Formula (I) and pharmaceutically acceptable forms thereof, as ?1a/?1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as methods of treatment.
    Type: Grant
    Filed: March 15, 2006
    Date of Patent: January 27, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: George Chiu, Shengjian Li, Peter J. Connolly, Virginia L. Pulito, Jingchun Liu, Steven A. Middleton
  • Publication number: 20090011994
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
    Type: Application
    Filed: June 18, 2008
    Publication date: January 8, 2009
    Inventors: Philip D. Stein, Sharon N. Bisaha, Saleen Ahmad, Khehyong Ngu, William N. Washburn
  • Publication number: 20080318924
    Abstract: The invention provides acid addition salts of the compounds represented by formula (1) or (2), or crystals thereof, and processes for preparing the same. The salts or crystals have HGFR inhibitory activity and excellent physical properties (solubility, safety, etc.) and are therefore useful as anti-tumor agents, angiogenesis inhibitors and inhibitors for metastasis for a various types of tumor.
    Type: Application
    Filed: February 14, 2008
    Publication date: December 25, 2008
    Applicant: Eisai R&D Management Co., Ltd
    Inventors: Tomohiro MATSUSHIMA, Shuji Shirotori, Keiko Takahashi, Atsushi Kamada, Kazunori Wakasugi, Takahisa Sakaguchi
  • Publication number: 20080293720
    Abstract: The present invention relates to compounds of following formula: or pharmaceutically acceptable salts thereof; pharmaceutical compositions containing them, and their use in the treatment of disorders mediated by the CCR-2 receptor.
    Type: Application
    Filed: December 4, 2006
    Publication date: November 27, 2008
    Applicant: Glaxo Group Limited
    Inventors: Pamela A. Cleary, Krista B. Goodman, Simon Peace, Joanne Philp, Clark A. Sehon
  • Publication number: 20080280905
    Abstract: The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
    Type: Application
    Filed: May 8, 2008
    Publication date: November 13, 2008
    Applicant: Bristol Myers Squibb Company
    Inventors: Hannguang J. Chao, Huji Tuerdi, Timothy F. Herpin, Jaques Yves Roberge, Yalei Liu, R. Michael Lawrence, Robert P. Rehfuss, Charles G. Clark, Jennifer X. Qiao, Timur Gungor, Patrick Y. S. Lam, Tammy Wang, Rejean Ruel, Alexandre L'Heureux, Carl Thibeault, Gilles Bouthillier, Dora M. Schnur
  • Publication number: 20080275027
    Abstract: The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis: wherein R1 and R2 are as defined in the specification.
    Type: Application
    Filed: July 17, 2006
    Publication date: November 6, 2008
    Inventors: Rachael Ann Ancliff, Mark James Bamford, Simon Teanby Hodgson, Christopher Allan Parr, Panayiotic Alexandrou Procopiou, David Matthew Wilson, Michael Woodrow
  • Publication number: 20080249082
    Abstract: The present invention relates to the treatment of compulsive, impulsive and pervasive developmental disorders. More particularly, the methods described herein comprise administration of memantine to an individual suffering from such a disorder in an amount effective to relieve one or more symptoms of said disorder.
    Type: Application
    Filed: September 19, 2005
    Publication date: October 9, 2008
    Applicant: Mount Sinai School of Medicine
    Inventor: Eric Hollander
  • Publication number: 20080242666
    Abstract: The present invention relates to Compound S of Formula (I).
    Type: Application
    Filed: December 22, 2005
    Publication date: October 2, 2008
    Inventors: Colin Andrew Leach, John Liddle, Simon Peace, Joanne Philp, Ian Edward David Smith, Lamont Roscoe Terrell, Jing Zhang
  • Patent number: 7423039
    Abstract: The invention relates to substituted (4-phenylpiperazin-1-yl)acylpiperidine derivatives of formula (I) in the form of a base or an addition salt with an acid, and also in the form of a hydrate or solvate, and their preparation process and therapeutic application.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: September 9, 2008
    Assignee: Sanofi-aventis
    Inventors: Victor Dos Santos, Jean Wagnon
  • Patent number: 7410970
    Abstract: The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS.
    Type: Grant
    Filed: October 7, 2003
    Date of Patent: August 12, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck, Gaston Stanislas Marcella Diels