Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 546/199)
  • TRIAZOLE FUSED HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20100292234
    Abstract: The present invention comprises a new class of compounds useful for modulating the activity of p38 MAP kinase. The compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R1 and R5 are defined herein. The invention further provides pharmaceutical compositions including one or more compounds of Formula I, use of such compounds and compositions for treatment of p38 MAP kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
    Type: Application
    Filed: September 19, 2008
    Publication date: November 18, 2010
    Applicant: Amgen Inc.
    Inventors: Liping H. Pettus, Kelvin K.C. Sham, Andrew Tasker, Shimin Xu
  • New Compounds
    Publication number: 20100286202
    Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
    Type: Application
    Filed: October 14, 2009
    Publication date: November 11, 2010
    Applicant: AstraZeneca AB
    Inventors: Yevgeni Besidski, Martin Nylöf, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin
  • PHARMACEUTICALLY ACCEPTABLE SALTS OF 2--2H-INDAZOLE-7-CARBOXAMIDE
    Publication number: 20100286203
    Abstract: The present invention relates to pharmaceutically acceptable salts of an amide substituted indazole which are inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), previously known as poly(ADP-ribose)synthase and poly(ADP-ribosyl) transferase. The compounds of the present invention are useful as mono-therapies in tumors with specific defects in DNA-repair pathways and as enhancers of certain DNA-damaging agents such as anticancer agents and radiotherapy. Further, the compounds of the present invention are useful for reducing cell necrosis (in stroke and myocardial infarction), down regulating inflammation and tissue injury, treating retroviral infections and protecting against the toxicity of chemotherapy.
    Type: Application
    Filed: January 8, 2009
    Publication date: November 11, 2010
    Inventors: Jennifer R. Foley, Robert Darrin Wilson
  • HEDGEHOG PATHWAY ANTAGONISTS AND THERAPEUTIC APPLICATIONS THEREOF
    Publication number: 20100286114
    Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.
    Type: Application
    Filed: December 10, 2008
    Publication date: November 11, 2010
    Applicant: SIENA BIOTECH S.P.A.
    Inventors: Russell John Thomas, Gal.la Pericot Mohr, Giacomo Minetto, Annette Cornelia Bakker, Pietro Ferruzzi
  • 2-Arylthiazole Derivatives as CXCR3 Receptor Modulators
    Publication number: 20100286191
    Abstract: The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
    Type: Application
    Filed: December 8, 2006
    Publication date: November 11, 2010
    Inventors: Rachel G. Samuel, Conrad Santini
  • TETRAHYDRO-CYCLOPENTYL PYRAZOLE CANNABINOID MODULATORS
    Publication number: 20100279991
    Abstract: This invention is directed to a tetrahydro-cyclopentyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
    Type: Application
    Filed: July 15, 2010
    Publication date: November 4, 2010
    Inventors: Fina Liotta, Mingde Xia, Michael P. Wachter, Scott A. Beers
  • PYRAZOLINE COMPOUNDS
    Publication number: 20100280016
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.
    Type: Application
    Filed: July 12, 2010
    Publication date: November 4, 2010
    Inventors: Marvin J. Meyers, Graciela B. Arhancet, XiangYang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
  • BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
    Publication number: 20100280071
    Abstract: Compounds of formula (I), salts and solvates are provided: Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.
    Type: Application
    Filed: March 20, 2007
    Publication date: November 4, 2010
    Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
  • Hexahydro-cyclooctyl pyrazole cannabinoid modulators
    Patent number: 7825151
    Abstract: This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
    Type: Grant
    Filed: March 20, 2007
    Date of Patent: November 2, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Mingde Xia, Fina Liotta, Huajun Lu, Meng Pan, Michael P. Wachter, Mark J. Macielag
  • Substituted 4-anilinoquinazolines and their use in tumor treatment
    Patent number: 7825245
    Abstract: The present invention relates to quinazoline derivatives of formula I: wherein X, Y, Z, R1, R2, R3, and R4 are as defined herein. The invention also relates to a method of preparing these compounds, and use of these compounds for inhibiting tumor growth.
    Type: Grant
    Filed: November 13, 2007
    Date of Patent: November 2, 2010
    Inventors: Wenlin Huang, Xiaohong Zhou
  • TRICYCLIC PYRAZOLE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS
    Publication number: 20100273791
    Abstract: The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
    Type: Application
    Filed: April 29, 2010
    Publication date: October 28, 2010
    Inventors: Braj Bhushan LOHRAY, Vidya Bhushan Lohray, Brijesh Srivastava
  • Benzimidazolone Compounds Having 5-HT4 Receptor Agonistic Activity
    Publication number: 20100273794
    Abstract: This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
    Type: Application
    Filed: July 7, 2010
    Publication date: October 28, 2010
    Applicant: Pfizer Inc.
    Inventors: Yasuhiro Katsu, Satoru Iguchi, Hiroki Sone, Chikara Uchida, Takashi Kojima
  • Use of Compounds Having a Mongalactosydiacylglycerol Syhnthase Inhibitory Activity as Herbicide or Algaecide, Herbicide and Algaecide Compositions
    Publication number: 20100273653
    Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.
    Type: Application
    Filed: June 2, 2008
    Publication date: October 28, 2010
    Applicants: COMMISSARIAT A L'ENERGIE ATOMIQUE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Helene Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • Imidazolothiazole compounds for the treatment of disease
    Patent number: 7820657
    Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
    Type: Grant
    Filed: March 16, 2007
    Date of Patent: October 26, 2010
    Assignee: Ambit Biosciences Corporation
    Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
  • Modulators of muscarinic receptors
    Patent number: 7820817
    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: Grant
    Filed: May 31, 2005
    Date of Patent: October 26, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Lewis Makings, Dennis Hurley, Miguel Gracia-Guzman Blanco, Daniele Bergeron, Akiko Nakatani
  • Cyclohexylimidiazole lactam derivatives as inhibitors of 11-?-hydroxysteroid dehydrogenase 1
    Patent number: 7820659
    Abstract: The present invention discloses novel compounds of Formula I: (I) having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.
    Type: Grant
    Filed: April 19, 2007
    Date of Patent: October 26, 2010
    Assignee: Eli Lilly and Company
    Inventors: Ashraf Saeed, Owen Brendan Wallace, Yanping Xu, Thomas Edward Mabry, Rebecca Lynn Rezac Guenther, Nancy June Snyder
  • Autophagy Inducing Compounds and Uses Thereof in Treating Autophagy Associated Diseases
    Publication number: 20100267704
    Abstract: This invention pertains to a class of autophagy inducing compounds that treat diseases caused by misfolded protein aggregates and a screening method for identifying these compounds.
    Type: Application
    Filed: October 10, 2008
    Publication date: October 21, 2010
    Applicants: President an Fellows of Harvard Colege, Shangha Institute of Organic Chemistry Chineesse Academy of Sciences
    Inventors: Junying Yuan, Dawei Ma, Lihong Zhang
  • N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS
    Publication number: 20100267710
    Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: June 28, 2010
    Publication date: October 21, 2010
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
  • Cyclic amides
    Patent number: 7816376
    Abstract: The invention relates to compounds of the formula (I) and pharmaceutically usable derivatives, salts, solvates and stereoisomers and mixtures thereof, in which X, Y, Z, R1, R3, R4, R8, p, k, E, G, Z and Q are as defined in claim 1, which are employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's, Parkinson's or Huntington's disease, cerebral ischaemia, infarction or psychoses.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: October 19, 2010
    Assignee: Merck Patent GmbH
    Inventors: Oliver Schadt, Joachim Leibrock, Helmut Pruecher, Christoph Seyfried
  • N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS
    Publication number: 20100261717
    Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: June 28, 2010
    Publication date: October 14, 2010
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
  • INDOL-3-YL-CARBONYL-PIPERIDIN-BENZOIMIDAZOL DERIVATIVES
    Publication number: 20100256140
    Abstract: The present invention relates to Indol-3-yl-carbonyl-piperidin-benzoimidazol derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R7 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephritic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.
    Type: Application
    Filed: June 21, 2010
    Publication date: October 7, 2010
    Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • NEW COMPOUNDS
    Publication number: 20100256188
    Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.
    Type: Application
    Filed: March 4, 2010
    Publication date: October 7, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
  • Compositions And Methods For Transmucosal Delivery Of Domperidone
    Publication number: 20100255096
    Abstract: Compositions of domperidone formulated for transmucosal delivery are provided. Also provided are methods for the treatment of nausea, vomiting, and gastrointestinal motility disorders, and methods for the enhancement of breast milk production. The methods utilize domperidone compositions formulated for transmucosal administration, administered to patients in an amount effective to treat nausea, vomiting, or gastrointestinal motility disorders, or to enhance breast milk production.
    Type: Application
    Filed: April 25, 2008
    Publication date: October 7, 2010
    Inventor: Craig A. Aronchick
  • Piperazine and Piperidine Derivatives
    Publication number: 20100256162
    Abstract: Compounds of general formula (I) in which R1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Application
    Filed: October 10, 2006
    Publication date: October 7, 2010
    Applicant: AGY THERAPEUTICS, INC.
    Inventor: Connie L Sun
  • INDAZOLE ACRYLIC ACID AMIDE COMPOUND
    Publication number: 20100256108
    Abstract: A compound of the formula: wherein ring X is benzene or pyridine; R1 is substituted alkyl; R2 is optionally substituted aryl or optionally substituted heterocyclic group; R3 is hydrogen or alkyl; R4 is hydrogen, halogen or alkyl; R5 is hydrogen or alkyl; R6 and R7 are the same or different and each hydrogen or halogen, or a pharmaceutically acceptable salt thereof, which is useful as IKur blocker effective for preventing or treating cardiac arrhythmia such as atrial fibrillation.
    Type: Application
    Filed: September 26, 2008
    Publication date: October 7, 2010
    Inventors: Tetsuo Yamaguchi, Hiroyuki Kawanishi, Hideki Ushirogochi, Tatsuyuki Takahashi, Tohru Takebe
  • Compounds that are ERK inhibitors
    Patent number: 7807672
    Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: October 5, 2010
    Assignee: Schering Corporation
    Inventors: Yongqi Deng, Gerald W. Shipps, Jr., Alan Cooper, Yang Nan, Tong Wang, M. Arshad Siddiqui, Hugh Zhu, Robert Sun, Joseph M. Kelly, Ronald Doll, Jagdish Desai, James J-S Wang, Youhao Dong, Vincent Madison, Li Xiao, Alan Hruza, Neng-Yang Shih
  • HETEROARYL SUBSTITUTED PYRAZOLE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
    Publication number: 20100249085
    Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.
    Type: Application
    Filed: May 8, 2008
    Publication date: September 30, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Stephen Boyer, Michael Härter, Philip L. Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
  • MCH receptor antagonists
    Patent number: 7803816
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of obesity, hyperphagia, anxiety, depression and related disorders and diseases.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: September 28, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, Shawn David Erickson, Nader Fotouhi, Robert Francis Kester, Kyungjin Kim, Steven Gregory Mischke, Yimin Qian, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley, Hong Wang
  • Indol-3-yl-corbonyl-piperidin-benzoimidazol derivatives
    Patent number: 7803815
    Abstract: The present invention relates to Indol-3-yl-carbonyl-piperidin-benzoimidazol derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R7 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephritic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.
    Type: Grant
    Filed: July 20, 2006
    Date of Patent: September 28, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • THIAZOLE DERIVATIVES
    Publication number: 20100240676
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, K, G, E and W
    Type: Application
    Filed: September 19, 2008
    Publication date: September 23, 2010
    Applicant: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober, Wolfgang Staehle
  • Benzimidazolone Chymase Inhibitors
    Publication number: 20100240702
    Abstract: Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.
    Type: Application
    Filed: May 15, 2008
    Publication date: September 23, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha Abeywardane, Brian Nicholas Cook, Stephane De Lombaert, Michel Jose Emmanuel, Xin Guo, Ming-Hong Hao, Jin Mi Kim, Ho Yin Lo, Chuk Chui Man, Tina Marie Morwick, Peter Allen Nemoto, Kevin Chungeng Qian, Hidenori Takahashi, Steven John Taylor
  • Indoles
    Patent number: 7799923
    Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: September 21, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • DERIVATIVES OF N-PHENYL(PIPERIDINE-2-YL) METHYL BENZAMIDE PREPARATION METHOD THEREOF AND APPLICATIONS OF SAME IN THERAPEUTICS
    Publication number: 20100234424
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Application
    Filed: May 20, 2010
    Publication date: September 16, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Gihad DARGAZANLI, Genevieve ESTENNE-BOUHTOU, Pascale MAGAT
  • Amino cyclopentyl heterocyclic and carbocyclic modulators of chemokine receptor activity
    Publication number: 20100234409
    Abstract: Compounds of the formulae (I) and (II): (wherein Q, X, E, G1, G2, R2, R3, R4, R5, R6 and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
    Type: Application
    Filed: May 20, 2005
    Publication date: September 16, 2010
    Inventors: Lihu Yang, Songnian Lin, Gregori Morriello, Liangqin Guo, Changyou Zhou
  • Organic compounds
    Patent number: 7790715
    Abstract: Novel substituted piperidines of the general formulae (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.
    Type: Grant
    Filed: September 30, 2004
    Date of Patent: September 7, 2010
    Assignee: Novartis AG
    Inventors: Peter Herold, Robert Mah, Stefan Stutz, Aleksandar Stojanovic, Vincenzo Tschinke, Nathalie Jotterand
  • Tetrahydro-cyclopentyl pyrazole cannabinoid modulators
    Patent number: 7790718
    Abstract: This invention is directed to a tetrahydro-cyclopentyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
    Type: Grant
    Filed: September 22, 2006
    Date of Patent: September 7, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Fina Liotta, Mingde Xia, Michael P. Wachter, Scott A. Beers
  • Azinyl-3-sulfonylindazole derivatives as 5-hydroxytryptamine-6 ligands
    Patent number: 7790751
    Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: August 14, 2006
    Date of Patent: September 7, 2010
    Assignee: Wyeth LLC
    Inventors: Hassan Mahmoud Elokdah, Alexander Alexei Greenfield, Kevin Liu, Geraldine Ruth McFarlane, Cristina Grosanu, Jennifer Rebecca Lo, Albert Jean Robichaud
  • Pyrroloquinoxalinone inhibitors of poly(ADP-ribose)polymerase
    Patent number: 7790721
    Abstract: Compounds of formula I where X is a bond; A1 and A2, together with the atoms to which they are attached, is pyrrole; and A3 and A4, together with the atoms to which they are attached, are benzene; are poly(ADP-ribose)polymerase inhibitors. The compounds of formula I are useful for the treatment of diseases such as cancer.
    Type: Grant
    Filed: December 27, 2007
    Date of Patent: September 7, 2010
    Assignee: Abbott Laboratories
    Inventors: Vincent L. Giranda, Julie M Miyashiro, Thomas D Penning, Keith W. Woods
  • Derivatives of N-[phenyl(alkylpiperidine-2-yl)methyl]benzamide, preparation method thereof and application of same in therapeutics
    Patent number: 7790753
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 17, 2006
    Date of Patent: September 7, 2010
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Corinne Veronique
  • Monocyclic and bicyclic compounds and methods of use
    Patent number: 7790726
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Grant
    Filed: August 14, 2006
    Date of Patent: September 7, 2010
    Assignee: Chemocentryx, Inc.
    Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
  • LINKED DIBENZIMIDAZOLE DERIVATIVES
    Publication number: 20100221215
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: February 9, 2010
    Publication date: September 2, 2010
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • DRUG ACTIVE IN NEUROPATHIC PAIN
    Publication number: 20100215742
    Abstract: The present invention relates to a compound of formula (I): in which: R is a linear or branched alkyl group containing between 1 and 3 carbon atoms, Y is CH or N, and p is an integer between 0 and 3 and preferably 0 and 1, and salts thereof, either acid-addition salts with a pharmaceutically acceptable organic or mineral acid, or base-addition salts with a pharmaceutically acceptable organic or mineral base. The invention also relates to a process for preparing the compound of formula (I), and to a pharmaceutical composition comprising it. The invention also relates to the use of an indazole for preparing a pharmaceutical composition that is active in the treatment of neuropathic pain.
    Type: Application
    Filed: November 6, 2008
    Publication date: August 26, 2010
    Applicant: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
    Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Angelo Guglielmotti, Lorenzo Polenzani
  • PHARMACEUTICAL COMPOSITIONS
    Publication number: 20100216785
    Abstract: Microemulsions of pharmaceutical compositions comprising, the following components (% by weight), the sum of the components being 100%: S) from 0.01 to 95% of one or more compounds selected from surfactants, polymers, forming organized structures as: aggregates, micelles, liquid crystals, vesicles, in the liquid in which they are solubilized, O) from 0.01 to 95% of one or more oils selected from esters of C4-C32 acids or C4-C32 acids, PA) from 0.001 to 90% of compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors of formula A?: AD) from 0 to 60% by weight of one or more compounds selected from modifiers of the water and/or oil polarity, modifiers of the film curvature of component S), co-surfactants, water or a saline aqueous solution the difference to 100%, wherein the ratio by weight S)/PA) is lower than that of microemulsions wherein component O) is absent.
    Type: Application
    Filed: February 25, 2010
    Publication date: August 26, 2010
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni LORIGA, Ilaria MANCA, Gerard Aime PINNA, Luca PANI
  • PHARMACEUTICAL COMPOUNDS
    Publication number: 20100215741
    Abstract: Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring comprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous system and/or peripheral activity, of formula (I): wherein the various substituents are as defined in the description. The compounds show affinity for the CB1 and/or CB2 cannabinoidergic receptors.
    Type: Application
    Filed: February 25, 2010
    Publication date: August 26, 2010
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
  • BENZIMIDAZOLIDINONE DERIVATIVES AS MUSCARINIC AGENTS
    Publication number: 20100216840
    Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
    Type: Application
    Filed: May 7, 2010
    Publication date: August 26, 2010
    Applicant: ACADIA PHARMACEUTICALS INC.
    Inventors: NICHOLAS MICHAEL KELLY, KRISTIAN NORUP KOCH, BO-RAGNAR TOLF
  • EPOXY COMPOUND AND METHOD FOR MANUFACTURING THE SAME
    Publication number: 20100217005
    Abstract: The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy compound.
    Type: Application
    Filed: May 7, 2008
    Publication date: August 26, 2010
    Inventors: Hidetsugu Tsubouchi, Yoshikazu Haraguchi, Satoshi Hayakawa, Naoto Utsumi, Shinichi Taira, Yoshihisa Tanada, Nobuhisa Fujita, Koichi Shinhama, Kimiyoshi Annaka, Takuya Furuta
  • Substituted 2-phenylbenzimidazoles, the production thereof and their use
    Patent number: 7781596
    Abstract: The invention relates to novel 2-phenylbenzimidazoles of general formula (I) or (II), wherein the radicals have the meanings cited in the description, and to their tautomeric forms, possible enantiomeric and diastereomeric forms, to their prodrugs, and to possible physiologically compatible salts. The invention also relates to the production of said compounds and to their use.
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: August 24, 2010
    Assignee: Abbott Laboratories
    Inventors: Wilfried Lubisch, Michael Kock, Thomas Höger
  • Bicyclic Benzamides of 3-or 4-Substituted 4-(Aminomethyl)-Piperidine Derivatives
    Publication number: 20100210657
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
    Type: Application
    Filed: May 4, 2010
    Publication date: August 19, 2010
    Applicant: JANSSEN PHARMACEUTICA N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
  • CARBOXAMIDE COMPOUNDS AND THEIR USE
    Publication number: 20100210633
    Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
    Type: Application
    Filed: October 12, 2007
    Publication date: August 19, 2010
    Applicant: EPIX Delaware, Inc.
    Inventors: Jian Lin, Dongli Chen, Steffi Koerner, Rosa E. Melendez, Pradyumma Mohanty, Efrat Ben-Zeev, Merav Fichman, Yael Marantz, Oren Becker, Dilara McCauley, Pini Orbach, Ashis K. Saha, Sharon Shacham, Michael Xie
  • Benzimidazolone compounds having 5-HT4 receptor agonistic activity
    Patent number: 7776885
    Abstract: This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
    Type: Grant
    Filed: September 2, 2004
    Date of Patent: August 17, 2010
    Assignee: Pfizer, Inc.
    Inventors: Yasuhiro Katsu, Satoru Iguchi, Hiroki Sone, Chikara Uchida, Takashi Kojima