Carbocyclic Ring Containing Patents (Class 546/194)
  • IMIDAZOLE COMPOUNDS
    Publication number: 20100261898
    Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.
    Type: Application
    Filed: June 4, 2010
    Publication date: October 14, 2010
    Inventors: Daniel J. BUZARD, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
  • Processes for preparing aromatic ethers
    Patent number: 7812159
    Abstract: The present invention relates to processes for preparing aromatic ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity.
    Type: Grant
    Filed: January 9, 2006
    Date of Patent: October 12, 2010
    Assignee: Arena Pharamaceuticals, Inc.
    Inventors: Tawfik Gharbaoui, John R. Fritch, Ashwin M. Krishnan, Beverly Wolgast Throop, Naomi S. Kato
  • Pyrrolidine aryl-ether as NK3 receptor antagonists
    Patent number: 7812021
    Abstract: The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The 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: Grant
    Filed: August 21, 2008
    Date of Patent: October 12, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
  • SULFONYL-PIPERIDIN-4-YL METHYLAMINE AMIDE ANALOGS AS GLYT1 INHIBITORS, METHODS FOR MAKING SAME, AND USE OF SAME IN TREATING PSYCHIATRIC DISORDERS
    Publication number: 20100256186
    Abstract: In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: March 31, 2010
    Publication date: October 7, 2010
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
  • Kallikrein 7 modulators
    Publication number: 20100256144
    Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
    Type: Application
    Filed: June 26, 2008
    Publication date: October 7, 2010
    Inventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Adreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
  • PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
    Publication number: 20100256126
    Abstract: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: March 11, 2010
    Publication date: October 7, 2010
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • RENIN INHIBITORS
    Publication number: 20100249163
    Abstract: The present invention relates to piperidinyl-based renin inhibitor compounds having the formula containing amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: November 26, 2008
    Publication date: September 30, 2010
    Inventors: Daniel Dube, Erich L. Grimm, Dwight MacDonald, Bruce MacKay
  • AZOLECARBOXAMIDE COMPOUND OR SALT THEREOF
    Publication number: 20100249088
    Abstract: [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action.
    Type: Application
    Filed: October 23, 2008
    Publication date: September 30, 2010
    Applicant: Astellas Pharma Inc.
    Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Nomura, Shunichiro Matsumoto, Takashi Shin, Hidenori Azami, Tomoaki Abe, Akira Suga, Ryushi Seo, Masayuki Tanahashi, Toru Watanabe
  • MULTI-RING COMPOUNDS AND USES THEREOF
    Publication number: 20100249111
    Abstract: Chemical agents, such as derivatives of hydroxy benzene 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: April 25, 2008
    Publication date: September 30, 2010
    Applicant: AVALON PHARMACEUTICALS
    Inventors: Norman E. Ohler, Jeffrey W. Watthey, Jeffrey Strovel, Sheela K. Chellappan
  • FACTOR XA INHIBITORS
    Publication number: 20100249117
    Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
    Type: Application
    Filed: May 11, 2010
    Publication date: September 30, 2010
    Inventors: Yonghong SONG, Zhaozhong J. JIA, Anjali PANDEY, Robert M. SCARBOROUGH, Carroll SCARBOROUGH
  • NOVEL DICARBOXYLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS
    Publication number: 20100249187
    Abstract: The present invention relates to new compounds of formula (I) possessing agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents. The invention is also directed to pharmaceutical compositions containing these compounds and use of these compounds for treatment/prevention of immune mediated diseases and conditions or inflammatory diseases and conditions.
    Type: Application
    Filed: June 16, 2008
    Publication date: September 30, 2010
    Inventors: Marc Capet, Nicolas Levoin, Isabelle Berrebi-Bertrand, Philippe Robert, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Jayraj Dilipbhal Aradhye, Muthukumaran Natarajan Pillai, Bhavesh Mohanbhai Panchal, Jignesh Kantilal Jivani, Biswajit Samanta, Ranjan Kumar Pal, Rajamannar Thennati
  • Substituted Heteroarylpiperidine Derivatives As Melanocortin-4 Receptor Modulators
    Publication number: 20100249093
    Abstract: The present invention relates to substituted heteroarylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, amyotrophic lateral sclerosis (ALS), anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.
    Type: Application
    Filed: July 18, 2008
    Publication date: September 30, 2010
    Applicant: SANTHERA PHARMACEUTICALS (SCHWEIZ) AG
    Inventors: Marco Henneböhle, Holger Herzner, Michael Soeberdt, Philipp Weyermann, Sonja Nordhoff, Achim Feurer, Holger Deppe, Hervé Siendt, Miroslav Terinek, Christian Rummey
  • 1,3-DISUBSTITUTED-4-PHENYL-3,4,5,6-TETRAHYDRO-2H,1 H-1,4 BIPYRIDINYL-2-ONES
    Publication number: 20100240688
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as 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: September 12, 2008
    Publication date: September 23, 2010
    Applicants: ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC., ADDEX PHARMA, S.A.
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey, Robert Johannes Lutjens, Patrick Terry Finn
  • TUBULYSINS AND PROCESSES FOR PREPARING
    Publication number: 20100240701
    Abstract: Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations.
    Type: Application
    Filed: October 23, 2008
    Publication date: September 23, 2010
    Applicant: ENDOCYTE, INC.
    Inventors: Iontcho Radoslavov Vlahov, Christopher Paul Leamon, Yu Wang
  • WATER-SOLUBLE THALIDOMIDE DERIVATIVES
    Publication number: 20100240651
    Abstract: A compound of formula (I), wherein R1 represents H, or a C1-4 alkyl group; R2 represents H, a C1-4 alkyl group, C(O)CHR4NR5R6, or C(O)W; or R1 and R2 taken together represent 1,3-propylene; R3 represents H, a C1-4 alkyl group, C(O)CHR4NR5R6, or C(O)W; or R2 and R3 taken together represent 1,3-propylene, 1,4-butylene, 1,5-pentylene, 1,6-hexylene, CH2OCH2, CH2SCH2 or CH2NR7CH2, wherein R7 represents H or a C1-4 alkyl group; and when one of R2 and R3 represents H, or a C1-4 alkyl group, the other one does not represent H; and R8 represents H, or a C1-4 alkyl group.
    Type: Application
    Filed: June 4, 2010
    Publication date: September 23, 2010
    Inventor: Hesheng ZHANG
  • 4-Phenylpiperidine Derivatives as Renin Inhibitors
    Publication number: 20100240679
    Abstract: Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Application
    Filed: May 28, 2010
    Publication date: September 23, 2010
    Inventors: Richard Sedrani, Juergen Klaus Maibaum, Werner Breitenstein, Holger Sellner, Claus Ehrhardt, Nils Ostermann
  • UREIDE DERIVATIVE AND PHARMACEUTICAL APPLICATION THEREOF
    Publication number: 20100234395
    Abstract: Discloses is a pharmaceutical agent comprising an ureide derivative represented by the formula: or a pharmaceutically acceptable salt thereof as an active ingredient. The ureide derivative or the pharmaceutically acceptable salt thereof is useful for the relief of a pain or the treatment or prevention of neurogenic pain.
    Type: Application
    Filed: March 27, 2007
    Publication date: September 16, 2010
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Yuji Sugawara, Naoki Izumimoto, Hideyuki Tsutsui
  • 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
  • Process for Making Substituted Aryl Sulfone Intermediates
    Publication number: 20100234603
    Abstract: The present invention relates to novel substituted aryl sulfone intermediates and processes for preparing the same. An aspect of this invention relates to a process for making substituted aryl sulfone intermediates utilizing a one-pot deacylation-carbon/sulfur bond formation step. The invention also relates to a process for preparing intermediates that are used to make the compounds of formula I. Some of the advantages of the present invention include manufacturing flexibility and efficiency, high yield synthesis using a one pot deacylation and carbon-sulfur bond formation step of a thioester intermediate and the like. This and other aspects of the invention will be realized upon review of the specification as a whole.
    Type: Application
    Filed: March 12, 2010
    Publication date: September 16, 2010
    Inventors: Xin Linghu, Kathleen Linn, Kevin M. Maloney, Mark McLaughlin, Gang Qian
  • 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
  • N-alkyl-4-methyleneamino-3-hydroxy-2-pyridones
    Patent number: 7790748
    Abstract: Compounds of Formula (I): are effective in the treatment of a microbial infection.
    Type: Grant
    Filed: June 18, 2007
    Date of Patent: September 7, 2010
    Assignee: Warner Chilcott Company, LLC
    Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
  • Chemokine receptor binding compounds
    Patent number: 7790747
    Abstract: The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: September 7, 2010
    Assignee: Genzyme Corporation
    Inventors: Yuanxi Zhou, Elyse Bourque, Yongbao Zhu, Jonathan Langille, Markus Metz, Wen Yang, Ernest J. McEachern, Curtis Harwig, Ian R. Baird, Tong-Shuang Li, Renato T. Skerlj
  • INDOL-3-Y-CARBONYL-PIPERIDIN AND PIPERAZIN-DERIVATIVES
    Publication number: 20100222357
    Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.
    Type: Application
    Filed: May 13, 2010
    Publication date: September 2, 2010
    Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • NICOTINAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
    Publication number: 20100222319
    Abstract: The disclosure relates to compounds of formula (I): wherein A, Z, Z?, L, R2 and R3 are as defined in the disclosure, to compositions comprising said compounds, and to methods for the manufacture and therapeutic use thereof.
    Type: Application
    Filed: March 26, 2010
    Publication date: September 2, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Claude BERNHART, Monsif BOUABOULA, Pierre CASELLAS, Samir JEGHAM, Jèrome ARIGON, Romain COMBET, Sandrine HILAIRET, Pierre FRAISSE
  • PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
    Publication number: 20100222366
    Abstract: The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
    Type: Application
    Filed: July 23, 2008
    Publication date: September 2, 2010
    Inventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
  • Substituted Indole Compounds
    Publication number: 20100222324
    Abstract: Substituted indole compounds corresponding to the formula I: In which R8, R9a, R9b, R10, R11, R200, R210, A, D, T, q, s and t have defined meanings, processes for the preparation thereof, pharmaceutical compositions containing such compounds and the use of substituted indole compounds for the treatment or inhibition of pain and other conditions which are at least partly mediated by Bradykinin 1 receptors (B1R).
    Type: Application
    Filed: February 3, 2010
    Publication date: September 2, 2010
    Applicant: Gruenenthal GmbH
    Inventors: Stefan Schunk, Melanie Reich, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
  • Pyridones useful as inhibitors of kinases
    Patent number: 7786120
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: August 25, 2006
    Date of Patent: August 31, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Julian M. C. Golec, Michael Mortimore
  • Soluble Guanylate Cyclase Activators
    Publication number: 20100216764
    Abstract: This inventions relates to compounds having the structure Formula I and pharmaceutically acceptable salts thereof which are soluble guanylate cyclase activators. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
    Type: Application
    Filed: February 24, 2010
    Publication date: August 26, 2010
    Inventors: Ronald M. Kim, Emma R. Parmee, Christopher Joseph Sinz, Olga A. Ziouzina
  • Pim kinase inhibitors and methods of their use
    Publication number: 20100216839
    Abstract: The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.
    Type: Application
    Filed: February 26, 2009
    Publication date: August 26, 2010
    Inventors: Matthew Burger, Jiong Lan, Mika Lindvall, Gisele Nishiguchi, Michelle Tetalman
  • PYRIDINE DERIVATIVES USEFUL AS GLUCOKINASE ACTIVATORS
    Publication number: 20100216794
    Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R3, R4 and D have the meanings indicated in claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.
    Type: Application
    Filed: August 13, 2008
    Publication date: August 26, 2010
    Inventors: Lars Thore Burgdorf, Norbert Beier, Johannes Gleitz, Christine Charon, Daniel Cravo
  • 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
  • Pyridone Compounds
    Publication number: 20100216758
    Abstract: An active ingredient is a compound represented by the general formula [I]: [wherein R1 and R2 represent a lower alkyl group, a C3-6 cycloalkyl group or the like, X1 and X2 represent methine, an Ar—Y1—Y2—Y3-substituted methine or the like, however either of them is an Ar—Y1—Y2—Y3-substituted methine, X3 to X8 represent methine, —N— or the like, Y1 and Y3 represent a single bond, —O— or the like, Y2 represent a single bond, a lower alkylene group or the like, W represent —(O)—(CH2)n-(O)— or the like, n represents an integer of 1 to 4, L and Z2 represent a single bond or a methylene group, Z1 represents a single bond, a C1-4 alkylene group or the like, and Ar represents an aromatic carbocyclic group or the like]. The compound acts as a melanin-concentrating hormone receptor antagonist and useful as a therapeutic agent for obesity or the like.
    Type: Application
    Filed: August 3, 2006
    Publication date: August 26, 2010
    Inventors: Makoto Ando, Etsuko Sekino, Yuji Haga, Norikazu Otake, Minoru Moriya
  • Indol-3-y-carbonyl-piperidin and piperazin-derivatives
    Patent number: 7781436
    Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.
    Type: Grant
    Filed: July 25, 2006
    Date of Patent: August 24, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • HETEROARYLOXY NITROGENOUS SATURATED HETEROCYCLIC DERIVATIVE
    Publication number: 20100210637
    Abstract: Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.
    Type: Application
    Filed: August 13, 2009
    Publication date: August 19, 2010
    Inventors: Norikazu Ohtake, Akira Naya, Yuji Haga, Makoto Jitsuoka, Takuya Suga, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani
  • PYRROLIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
    Publication number: 20100210659
    Abstract: The present invention relates to a compounds of formula I wherein A, Ar, R, R2, R3, R4, p, and o are as defined in the specification and claims or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: February 11, 2010
    Publication date: August 19, 2010
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
  • THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN
    Publication number: 20100210686
    Abstract: Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In one embodiment, the Piperidine Compound has the formula: and pharmaceutically acceptable salts thereof, wherein Ar1, Ar2, X, R3, R4, and m are as disclosed herein.
    Type: Application
    Filed: July 20, 2009
    Publication date: August 19, 2010
    Applicant: Purdue Pharma L.P.
    Inventors: Qun Sun, Kate Xin Wen, Xiaoming Zhou
  • Substituted Aryl Sulfone Derivatives as Calcium Channel Blockers
    Publication number: 20100210620
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Application
    Filed: September 30, 2008
    Publication date: August 19, 2010
    Inventors: Prasun K. Chakravarty, Yanbing Ding, Joseph L. Duffy, Hassan Pajouhesh, Pengeheng Patrick Shao, Sriram Tyagarajan, Feng Ye
  • 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
  • PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
    Publication number: 20100204274
    Abstract: The present application describes modulators of MIP-1? of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.
    Type: Application
    Filed: July 23, 2008
    Publication date: August 12, 2010
    Inventors: Daniel S. Gardner, John V. Duncia, John Hynes, T.G. Murali Dhar, Percy H. Carter, Joseph B. Santella
  • ISOINDOLINE COMPOUNDS AND METHODS OF THEIR USE
    Publication number: 20100204227
    Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.
    Type: Application
    Filed: October 29, 2009
    Publication date: August 12, 2010
    Inventors: George W. MULLER, Alexander L. Ruchelman
  • Amide derivatives as somatostatin receptor 5 antagonists
    Patent number: 7772253
    Abstract: This invention is concerned with compounds of the formula wherein R1 to R5, R5? and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: August 10, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alfred Binggeli, Andreas Christ, Luke Gideon Granville Green, Wolfgang Guba, Hans-Peter Maerki, Rainer Eugen Martin, Peter Mohr
  • PYRIDINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20100197652
    Abstract: The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Application
    Filed: August 7, 2008
    Publication date: August 5, 2010
    Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker, Justin T. Steen
  • BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
    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
  • PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
    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
  • ALKYLAMINO-SUBSTITUTED DICYANOPYRIDINES AND THEIR AMINO ACID ESTER PRODRUGS
    Publication number: 20100197609
    Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: January 29, 2010
    Publication date: August 5, 2010
    Applicant: BAYER SCHERING PHARMA
    Inventors: Alexandros VAKALOPOULOS, Daniel MEIBOM, Barbara ALBRECHT-KÜPPER, Katja ZIMMERMANN, Jörg KELDENICH, Hans-Georg LERCHEN, Peter NELL, Frank SÜSSMEIER, Ursula KRENZ
  • SUBSTITUTED BENZ-AZOLES AND METHODS OF THEIR USE AS INHIBITORS OF RAF KINASE
    Publication number: 20100196368
    Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: March 12, 2010
    Publication date: August 5, 2010
    Applicant: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
    Inventors: Payman Amiri, Wendy Fantl, Teresa Hansen, Barry Haskell Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Leonard Sung
  • 3-Quinolinecarbonitrile protein kinase inhibitors
    Patent number: 7767671
    Abstract: This invention provides a compound of Formula 1 where Ar, X, R1, R2, R3, and R4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhibition of diseases associated with the Ras/Raf/MEK signaling cascade in a mammal, such as neoplasms, strokes, osteoporosis, cancer, rheumatoid arthritis, inflammatory disease, polycystic kidney disease, and colonic polyps, and methods of making the compounds of formula 1 and intermediates.
    Type: Grant
    Filed: September 23, 2008
    Date of Patent: August 3, 2010
    Assignee: Wyeth
    Inventors: Dan Maarten Berger, Dennis William Powell, Biqi Wu
  • Thiazolylimidazole derivatives and their use as inhibitors of microsomal triglyceride transfer protein
    Patent number: 7767819
    Abstract: The present invention relates to thiazolylimidazole derivatives of the general formula (I) in which: G represents a bond or a divalent radical chosen from the groups g1, g2 and g3; and R1, R2, R3, R4, R5, R6, Y and Z are as defined in the description. Application of the compounds of the formula (I) to the treatment of hypertriglyceridaemia, hypercholesterolaemia and dyslipidaemia.
    Type: Grant
    Filed: January 17, 2005
    Date of Patent: August 3, 2010
    Assignee: Merck Patent GmbH
    Inventors: Philippe Guedat, Olivier Chevreuil, Thierry Convard
  • Amide derivatives as kinase inhitors
    Publication number: 20100190788
    Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar1, Ar2, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
    Type: Application
    Filed: July 11, 2006
    Publication date: July 29, 2010
    Inventors: Olivier Defert, Philippe Van Rompaey, Petra Blom, Dirk Leysen, Gert De Wilde, Thomas Brown
  • Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors with Improved Membrane Permeability
    Publication number: 20100190230
    Abstract: Compounds and related compositions and methods as can be used to inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases.
    Type: Application
    Filed: January 25, 2010
    Publication date: July 29, 2010
    Inventors: Richard B. Silverman, Fengtian Xue