Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 546/199)
  • PYRROLIDINES AND PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20100197733
    Abstract: The invention relates to compounds of formula (I) wherein Y, A, N and R1 are as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to the use of such compounds as medicaments, especially as orexin receptor antagonists.
    Type: Application
    Filed: September 23, 2008
    Publication date: August 5, 2010
    Inventors: Hamed Aissaoui, Christoph Boss, Ralf Koberstein, Thierry Sifferlen
  • 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
  • INDAZOLE DERIVATIVES AS KINASE INHIBITORS FOR THE TREATMENT OF CANCER
    Publication number: 20100197665
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I).
    Type: Application
    Filed: December 14, 2007
    Publication date: August 5, 2010
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Marcella Nesi, Ettore Perrone, Roberto Bossi, Paolo Polucci
  • METHOD FOR IDENTIFICATION AND FUNCTIONAL CHARACTERIZATION OF AGENTS WHICH MODULATE ION CHANNEL ACTIVITY
    Publication number: 20100191475
    Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.
    Type: Application
    Filed: March 4, 2010
    Publication date: July 29, 2010
    Inventors: Scott Perschke, Ming Liu
  • INHIBITORS OF C-MET AND USES THEREOF
    Publication number: 20100190774
    Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.
    Type: Application
    Filed: April 8, 2010
    Publication date: July 29, 2010
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: David J. Lauffer, Alexander Aronov, Pan Li, David D. Deininger, Kira McGinty, Dean Stamos, Jon H. Come, Michelle Stewart
  • BENZIMIDAZOLE DERIVATIVE
    Publication number: 20100190826
    Abstract: Provided is a novel and excellent method for treating and/or preventing benign prostatic hyperplasia, prostate cancer, and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an indole or benzimidazole derivative, where a nitrogen atom of the indole ring or benzimidazole ring is substituted with a phenyl group substituted with COOH, has a potent selective inhibitory activity against 17?HSD type 5 and may become an agent for treating and/or an agent for preventing a disease associated with 17?HSD type 5, such as benign prostatic hyperplasia, prostate cancer and the like, without accompanying adverse effects due to a decrease in testosterone; and the present invention has thus been completed.
    Type: Application
    Filed: July 23, 2008
    Publication date: July 29, 2010
    Inventors: Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano, Akio Kamikawa, Kentaro Enjo, Takashi Furutani
  • BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
    Publication number: 20100190825
    Abstract: Compounds of formula (I) and salts and solvates are provided: wherein Uses of the compounds for the treatment of psychotic disorders and cognitive mpairment, are also disclosed.
    Type: Application
    Filed: March 20, 2007
    Publication date: July 29, 2010
    Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
  • PYRANO-PYRAZOLE-AMINES
    Publication number: 20100184759
    Abstract: The present invention relates to compounds having the structural formula below and pharmacological activity towards the sigma (?) receptor, and more particularly to pyrano-pyrazole-amines, to processes of preparing such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.
    Type: Application
    Filed: April 16, 2008
    Publication date: July 22, 2010
    Inventors: Bernhard Wünsch, Dirk Schepmann, Torsten Schläger, Daniel Zamanillo-Castanedo
  • BENZIMIDAZOLE COMPOUNDS AND THEIR USE AS ANTICANCER AGENTS
    Publication number: 20100179147
    Abstract: Benzimidazole compounds of formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z1, and Z2 are defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.
    Type: Application
    Filed: December 10, 2009
    Publication date: July 15, 2010
    Inventors: Chih-Shiang Chang, Jih-Hwa Guh, Che-Ming Teng, Shiow-Lin Pan, Wei-Ling Chang, Ju-Fang Liu, Kai-Wei Chang, Sheng-Chu Kuo
  • BICYCLIC PYRAZOLO PROTEIN KINASE MODULATORS
    Publication number: 20100179190
    Abstract: The present invention provides novel bicyclic pyrazolo kinase modulators and methods of using the novel bicyclic pyrazolo kinase modulators to treat diseases mediated by kinase activity.
    Type: Application
    Filed: November 14, 2008
    Publication date: July 15, 2010
    Applicant: SGX PHARMACEUTICALS, INC.
    Inventors: Pierre-Yves Bounaud, Andrew Vaino
  • Diaminoalkane aspartic protease inhibitors
    Patent number: 7754737
    Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Grant
    Filed: October 7, 2005
    Date of Patent: July 13, 2010
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
  • Muscarinic Receptor Agonists that are Effective in the Treatment of Pain, Alzheimer's Disease and Schizophrenia
    Publication number: 20100173935
    Abstract: Compounds of Formula IA, or pharmaceutically acceptable salts thereof: IA wherein G1, G2, G3, G4, R1, R2, X, Y, Z and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
    Type: Application
    Filed: June 8, 2007
    Publication date: July 8, 2010
    Applicant: AstraZeneca AB
    Inventors: Yun-Xing Cheng, Shujuan Jin, Mehrnaz Pourashraf, Miroslaw Tomaszewski
  • Muscarinic Receptor Agonists that are Effective in the Treatment of Pain, Alzheimer's Disease and Schizophrenia
    Publication number: 20100173941
    Abstract: Compounds of Formulae I, or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4, R5, R6, R7, m and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
    Type: Application
    Filed: June 8, 2007
    Publication date: July 8, 2010
    Applicant: AstraZeneca AB
    Inventors: Yun-Xing Cheng, Miroslaw Tomaszewski
  • Piperidinones Useful in the Treatment of Inflammation
    Publication number: 20100168167
    Abstract: There is provided compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, m and n have meanings given in the description, and pharmaceutically acceptable derivatives thereof, which compounds are useful in the treatment of diseases and conditions associated with inflammation.
    Type: Application
    Filed: March 12, 2008
    Publication date: July 1, 2010
    Inventors: Benjamin Pelcman, Christian Krog-Jensen, Yaping Shen, James Gee Kan Yee, Lloyd F. MacKenzie, Yuanlin Zhou, Kang Han, Jeffery R. Raymond
  • Benzimidazole-derivatives as factor Xa inhibitors
    Patent number: 7741341
    Abstract: The present invention relates to compounds of the formula I, wherein R0, R1, R2, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: June 22, 2010
    Assignee: sanofi-aventis Deutschland GmbH
    Inventors: Marc Nazare, Michael Wagner, Volkmar Wehner, Hans Matter, Matthias Urmann, Kurt Ritter
  • SUBSTITUTED BENZIMIDAZOLONE DERIVATIVES, MEDICAMENTS COMPRISING THEM AND THEIR USE
    Publication number: 20100152168
    Abstract: The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.
    Type: Application
    Filed: August 24, 2007
    Publication date: June 17, 2010
    Applicant: ABBOTT GMBH & CO. KG
    Inventors: Torsten Arndt, Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Juliana Ruiz Caro
  • Benzimidazolone carboxylic acid derivatives
    Patent number: 7737163
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, 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 such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: June 15, 2010
    Assignee: Pfizer Inc.
    Inventors: Koji Ando, Satoru Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki
  • IMIDAZOLE DERIVATIVES HAVING ARYL PIPERIDINE SUBSTITUENT, METHOD FOR PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    Publication number: 20100145054
    Abstract: The present invention is directed to a novel imidazole derivative having an aryl piperidine substituent of formula (I) and a method for preparation thereof, and a pharmaceutical composition containing said imidazole derivative as an active ingredient for preventing or treating a MCH (melanine-concentrating hormone)-related disease.
    Type: Application
    Filed: May 13, 2008
    Publication date: June 10, 2010
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Jee Hee Suh, Kyu Yang YI, Nack Jeong KIM, Sung Eun Yoo, Kwang-Seok Oh, Hyae Gyeong Cheon, Mija Ahn, Byung Ho Lee, Won Hoon Jung, Sang Dal Rhee
  • NOVEL 4-CYANO, 4-AMINO, AND 4-AMINOMETHYL DERIVATIVES OF PYRAZOLO[1,5-a]PYRIDINES, PYRAZOLO[1,5-c]PYRIMIDINES AND 2H-INDAZOLE COMPOUNDS AND 5-CYANO, 5-AMINO, AND 5-AMINOMETHYL DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINES, AND IMIDAZO[1,5-a]PYRAZINES AS CYCLIN DEPENDENT KINASE INHIBITORS
    Publication number: 20100137326
    Abstract: In its many embodiments, the present invention provides a novel class of 4-cyano, 4-amino, and 4-aminomethyl derivatives of pyrazolo[1,5-a]pyridine, pyrazolo[1,5-c]pyrimidine, and 2H-Indazole compounds and 5-cyano, 5-amino, and 5-aminomethyl derivatives of imidazo[1,2-a]pyridine and imidazo[1,5-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: February 17, 2010
    Publication date: June 3, 2010
    Inventors: Alan K. Mallams, Vincent Madison, Kamil Paruch
  • JAK-2 Modulators and Methods of Use
    Publication number: 20100136136
    Abstract: This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.
    Type: Application
    Filed: September 28, 2007
    Publication date: June 3, 2010
    Applicant: EXELIXIS, INC.
    Inventors: Adam Antoni Galan, Jeff Chen, Hongwang Du, Timothy Forsyth, Tai Phat Huynh, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Matthew Sangyup Lee, Grace Mann, Brian Hugh Ridgway, Craig Stacy Takeuchi, Peiwen Zhou
  • TARGET PROTEIN AND TARGET GENE IN DRUG DESIGNING AND SCREENING METHOD
    Publication number: 20100136524
    Abstract: The present invention provides a novel target protein and a gene for drug discovery, and a means that enables development of a novel pharmaceutical agent by using the same. More particularly, the present invention provides CARP and genes thereof; screening methods for drugs (e.g., antiallergic drugs); a regulator of diseases (e.g., allergic diseases); a drug derivative production method; a complex comprising a drug and CARP, and a production method thereof; kits comprising a drug or a salt thereof; determination methods for the onset or risk of onset of a specified disease, determination methods for susceptibility to a drug, and determination kits used for said methods, and the like.
    Type: Application
    Filed: October 18, 2005
    Publication date: June 3, 2010
    Applicant: Reverse Proteomics Research Institute Co., Ltd.
    Inventors: Tadakazu Yamauchi, Hideaki Sueoka, Kouichi Tsuchiya, Katsuhisa Murayama, Kazuo Komiya, Morikazu Kito, Takeshi Tsutsumi, Yuko Isono, Motoi Tobita, Yorimasa Suwa
  • Imidazo[1,2-A]pyridine anxiolytics
    Patent number: 7723324
    Abstract: Imidazo[1,2-a]pyridines of the formulae I and II: are disclosed. The compounds are useful to treat anxiety and insomnia. Pharmaceutical compositions and methods are also disclosed.
    Type: Grant
    Filed: October 28, 2004
    Date of Patent: May 25, 2010
    Assignee: Sepracor, Inc.
    Inventors: Q. Kevin Fang, Paul Grover, Thomas P. Jerussi
  • Substituted-3-sulfonylindazole derivatives as 5-hydroxytryptamine-6 ligands
    Patent number: 7723329
    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: May 25, 2010
    Assignee: Wyeth LLC
    Inventors: Hassan Mahmoud Elokdah, Alexander Alexei Greenfield, Kevin Liu, Robert Emmett McDevitt, Geraldine Ruth McFarlane, Cristina Grosanu, Jennifer Rebecca Lo, Yanfang Li, Albert Jean Robichaud, Ronald Charles Bernotas
  • Alkyl-and piperidine-substituted benzimidazole derivatives
    Patent number: 7723360
    Abstract: A compound of general formula 1a wherein R1, R5, R6, A, B, Y, i, j and m are defined as in the description and claims. It is another object of the present invention to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 28, 2005
    Date of Patent: May 25, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Domnic Martyres, Franz Birke, Thierry Bouyssou
  • BENZIMIDAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF
    Publication number: 20100120841
    Abstract: Provided is an ORL-1 receptor agonist having improved bioavailability based on superior metabolic stability and strong and high selectivity, as compared to conventional compounds. A compound represented by the formula (I) wherein each symbol is as defined in the claims.
    Type: Application
    Filed: February 28, 2008
    Publication date: May 13, 2010
    Inventors: Masakazu Nakano, Masanori Minoguchi, Tokushi Hanano, Shin-ichiro Ono, Hideki Horiuchi, Koji Teshima
  • 1,5-Dideoxy-1,5-imino-D-glucitol Compounds
    Publication number: 20100113519
    Abstract: 1,5-Dideoxy-1,5-imino-D-glucitol compounds as shown in the specification. Also disclosed is a method of treating a hexosaminidase-associated disease.
    Type: Application
    Filed: October 30, 2009
    Publication date: May 6, 2010
    Applicant: Academia Sinica
    Inventors: Chun-Hung Lin, Ching-Wen Ho
  • NK1 antagonists
    Patent number: 7709641
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Grant
    Filed: June 30, 2005
    Date of Patent: May 4, 2010
    Assignee: OPKO Health, Inc.
    Inventors: Sapna S. Shah, Neng-Yang Shih, Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang
  • Pyrrolo-quinoxalinone derivatives as antibacterials
    Patent number: 7709483
    Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: May 4, 2010
    Assignee: Glaxo Group Limited
    Inventors: Graham Elgin Jones, Timothy James Miles, Neil David Pearson
  • BENZOPYRANOPYRAZOLES
    Publication number: 20100104659
    Abstract: Compounds of a certain formula I, in which Ra, Rb and Rc have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.
    Type: Application
    Filed: July 12, 2007
    Publication date: April 29, 2010
    Inventors: Matthias Vennemann, Thomas Bär, Thomas Maier, Andreas Lindenmaier, Jürgen Braunger, Markus Boehm, Astrid Zimmermann, Volker Gekeler
  • Benzimidazolone carboxylic acid derivatives
    Patent number: 7705020
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, 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 such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: April 27, 2010
    Assignee: Pfizer Inc.
    Inventors: Koji Ando, Saturu Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki
  • Bicyclic heteroaromatic compounds
    Patent number: 7705005
    Abstract: The invention disclosed herein relates to compounds of formula (I) where the various groups are defined herein, and which are useful for treating inflammatory diseases such as atherosclerosis.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: April 27, 2010
    Assignee: Glaxo Group Limited
    Inventor: Colin Andrew Leach
  • Fused heteroaryl derivatives for use as p38 kinase inhibitors in the treatment of I.A. rheumatoid arthritis
    Patent number: 7687532
    Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
    Type: Grant
    Filed: January 27, 2005
    Date of Patent: March 30, 2010
    Assignee: GlaxoSmithkline LLC
    Inventors: Sebastien Andre Campos, Stephen Swanson, Ann Louise Walker
  • BENZIMIDAZOLE THIOPHENE COMPOUNDS
    Publication number: 20100075960
    Abstract: The present invention provides bezimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
    Type: Application
    Filed: May 29, 2007
    Publication date: March 25, 2010
    Inventors: Kevin Kuntz, Kyle Allen Emmitte, Tara Renae Rheault, Stephon Smith, Keith Hornberger, Hamilton Dickson, Mui Cheung
  • MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
    Publication number: 20100076014
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
    Type: Application
    Filed: October 31, 2007
    Publication date: March 25, 2010
    Inventors: James E. Sheppeck, John l. Gilmore, T.G. Murali Dhar, Hai-Yun Xiao
  • TETRAHYDRO-PYRANOPYRAZOLE CANNABINOID MODULATORS
    Publication number: 20100069341
    Abstract: This invention is directed to a tetrahydro-pyranopyrazole 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: November 19, 2009
    Publication date: March 18, 2010
    Inventors: Fina Liotta, Huajun Lu, Michael P. Wachter, Mingde Xia
  • CYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
    Publication number: 20100063067
    Abstract: The present application describes modulators of MIP-1? of formula (I), or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, A, T, R1, R2 and R8, 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: October 3, 2007
    Publication date: March 11, 2010
    Inventors: Percy H. Carter, Lyndon A.M. Cornelius
  • N-linked aryl heteroaryl inhibitors of LTA4H for treating inflammation
    Patent number: 7674802
    Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: March 9, 2010
    Assignee: deCODE genetics, ehf
    Inventors: Vincent Sandanayaka, Jasbir Singh, Lei Zhao, Mark E. Gurney
  • BENZOFURAN COMPOUNDS USEFUL IN THE TREATMENT OF CONDITIONS MEDIATED BY THE ACTION OF PGE2 AT THE EP1 RECEPTOR
    Publication number: 20100056527
    Abstract: A compound of formula (I): wherein R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
    Type: Application
    Filed: February 14, 2008
    Publication date: March 4, 2010
    Inventors: Andrew John Eatherton, Gerard Martin Paul Giblin, Mairi Gibson, Adrian Hall, David Nigel Hurst
  • 2-ALKYL-INDAZOLE COMPOUNDS FOR THE TREATMENT OF CERTAIN CNS-RELATED DISORDERS
    Publication number: 20100056573
    Abstract: 2-Alkyl-indazole compound and its pharmaceutically acceptable salts of acid addition, method and intermediates for preparing them, a pharmaceutical composition containing them and use of the latter. The 2-alkyl-indazole compound has the following general formula (I) in which R1, R2, R3, R4, R6, R7, X, Y, W, n, p, and m have the meanings stated in the description.
    Type: Application
    Filed: November 19, 2007
    Publication date: March 4, 2010
    Applicant: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.
    Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri, Rosella Ombrato, Lorenzo Polenzani
  • THIENOPYRAZOLES
    Publication number: 20100056514
    Abstract: Thienopyrazoles, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).
    Type: Application
    Filed: March 26, 2009
    Publication date: March 4, 2010
    Applicant: AVENTIS PHARMACEUTICALS INC.
    Inventors: John Gerard JURCAK, Matthieu BARRAGUE, Timothy Alan GILLESPY, Michael Louis EDWARDS, Kwon Yon MUSICK, Philip Marvin WEINTRAUB, Yan DU, Ramalinga M. DHARANIPRAGADA, Ashfaq Ahmad PARKAR
  • BENZIMIDAZOLE DERIVATIVES
    Publication number: 20100048565
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, immune response regulation and cell proliferation. The subject compounds are 2-amino-imidazole derivatives.
    Type: Application
    Filed: October 28, 2009
    Publication date: February 25, 2010
    Inventors: Alexander David Frenkel, Sarah Elizabeth Lively, Jay P. Powers, Andrew Smith, Daqing Sun, Craig Tomooka, Zhulun Wang
  • INDAZOLAMIDES WITH ANALGESIC ACTIVITY
    Publication number: 20100048907
    Abstract: The present invention relates to compounds of formula (II)
    Type: Application
    Filed: October 28, 2009
    Publication date: February 25, 2010
    Applicant: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO S.P.A.
    Inventors: Maria Alessandra ALISI, Nicola Cazzolla, Angelo Guglielmotti, Guido Furlotti, Giuseppe Luna, Lorenzo Polenzani
  • Heteroindanes: a new class of potent cannabimimetic ligands
    Patent number: 7666867
    Abstract: One aspect of the invention is concerned with cannabimimetic heteroindane analogs having affinities and/or selectivities for a cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.
    Type: Grant
    Filed: October 28, 2002
    Date of Patent: February 23, 2010
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Qian Liu, Alexander M Zvonok
  • BENZIMIDAZOLE CANNABINOID AGONISTS
    Publication number: 20100041702
    Abstract: The present invention is related to novel benzimidazole compounds of Formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
    Type: Application
    Filed: March 25, 2008
    Publication date: February 18, 2010
    Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn
  • Indazole having analgesic activity
    Patent number: 7662836
    Abstract: An indazole having analgesic activity, a method for the preparation thereof and a pharmaceutical composition containing the same; the indazole has the following general formula: where X, Ra, Rb, Rc and Rd have the meanings stated in the description.
    Type: Grant
    Filed: April 23, 2004
    Date of Patent: February 16, 2010
    Assignee: 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
  • Unsaturated mTOR inhibitors
    Patent number: 7659274
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Grant
    Filed: January 24, 2007
    Date of Patent: February 9, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Andrew Philip Crew, Douglas S. Werner, Paula A. R. Tavares
  • PIPERIDINE DERIVATIVE OR SALT THEREOF
    Publication number: 20100029687
    Abstract: [Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. [Means for Resolution] It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).
    Type: Application
    Filed: November 14, 2007
    Publication date: February 4, 2010
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
  • ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE
    Publication number: 20100029641
    Abstract: The present invention is directed to aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
    Type: Application
    Filed: August 27, 2009
    Publication date: February 4, 2010
    Applicant: Wyeth
    Inventors: Casey Cameron McComas, Stephen Todd Cohn, Andrew Fensome, Joel Adam Goldberg, Charles William Mann, Michael Anthony Marella, David John O'Neill, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski, An Thien Vu, Richard Page Woodworth, JR., Puwen Zhang
  • 2-(R)-(4-fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide maleate and pharmaceutical compositions thereof
    Patent number: 7652012
    Abstract: The present invention relates to piperidine derivatives of formula (I) specifically 2-(R)-(4-Fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide maleate and pharmaceutical compositions thereof, useful in the treatment of conditions mediated by tachykinins.
    Type: Grant
    Filed: December 11, 2006
    Date of Patent: January 26, 2010
    Assignee: Glaxo Group Limited
    Inventors: Giuseppe Alvaro, Romano Di Fabio, Maria Elvira Tranquillini, Simone Spada
  • Compositions useful as inhibitors of protein kinases
    Patent number: 7652135
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein A, B, Q, R1, and R2 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT or PDK1 kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds, and methods of utilizing those compositions in the treatment of various disorders.
    Type: Grant
    Filed: September 23, 2004
    Date of Patent: January 26, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Simon Everitt, Francesca Mazzei, Daniel Robinson