Tricyclo Ring System Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.03)
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Publication number: 20110002855Abstract: Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues of the formula (I): are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: ApplicationFiled: June 25, 2008Publication date: January 6, 2011Applicant: NEUROGEN CORPORATIONInventors: Timothy M. Caldwell, Yang Gao, Linghong Xie, Yuelian Xu
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Publication number: 20100324021Abstract: The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: May 25, 2010Publication date: December 23, 2010Applicant: N.V. OrganonInventors: Hubert Jan Jozef Loozen, Cornelius Marius Timmers
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Publication number: 20100317657Abstract: The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives.Type: ApplicationFiled: June 2, 2010Publication date: December 16, 2010Inventors: Pascal FURET, Frank Stephan KALTHOFF, Robert MAH, Christian RAGOT, Frédéric STAUFFER
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Publication number: 20100317672Abstract: The present invention relates to a monomaleate monohydrate salt of 7-methyl-6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4,5-dihydroimidazo[1,5-a]quinoline-3-carboxamide, uses of the salt as a medicament in the treatment of sexual dysfunction and pharmaceutical compositions and dosage forms comprising the salt.Type: ApplicationFiled: January 15, 2009Publication date: December 16, 2010Applicant: GLAXO GROUP LIMITEDInventors: Clare Louise Anderton, Grahame Robert Woollam
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Publication number: 20100311714Abstract: The invention relates to the use of 1H-imidazo[4,5-c]quinolinone compounds and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone compounds for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone compounds to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone compounds, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone compounds; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone compounds.Type: ApplicationFiled: June 2, 2010Publication date: December 9, 2010Inventors: Pascal Furet, Patricia Imbach, Robert Mah, Frédéric Stauffer
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Patent number: 7838521Abstract: The compounds of formula I in which R1, R2 and R3 have the meanings as given in the description, are novel effective PDE4 inhibitors.Type: GrantFiled: September 5, 2005Date of Patent: November 23, 2010Assignee: NYCOMED GmbHInventors: Dieter Flockerzi, Ulrich Kautz, Armin Hatzelmann, Christof Zitt, Andrea Wohlsen, Degenhard Marx, Hans-Peter Kley, Jens Christoffers, Anna Rosiak
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Publication number: 20100280001Abstract: The present invention provides compounds of formula (I) wherein Ra, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: May 6, 2008Publication date: November 4, 2010Inventors: Roger Victor Bonnert, Thomas McInally, Stephen Thom, Hiroki Wada
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Publication number: 20100256112Abstract: Disclosed herein are hydroxylthienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxylthienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxylthienoquinolone or related compound to an animal suffering from a microbial infection.Type: ApplicationFiled: April 5, 2010Publication date: October 7, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Barton James BRADBURY, Milind DESHPANDE, Akihiro HASHIMOTO, Ha Young KIM, Edlaine LUCIEN, Godwin PAIS, Michael PUCCI, Qiuping WANG, Jason Allan WILES, Avinash PHADKE
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Patent number: 7807680Abstract: A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle therefor, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. A method for preparing the controlled release freeze-dried aripiprazole formulation, and a method for treating schizophrenia employing the above formulation are also provided.Type: GrantFiled: October 19, 2004Date of Patent: October 5, 2010Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Janusz W. Kostanski, Takakuni Matsuda, Manoj Nerurkar, Vijay H. Naringrekar
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Publication number: 20100222321Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: June 7, 2006Publication date: September 2, 2010Inventors: Donna J. Armstrong, Essa H. Hu, Michael J. Kelly, III, Mark E. Layton, Yiwei Li, Jun Liang, Kevin J. Rodzinak, Michael A. Rossi, Philip E. Sanderson, Jiabing Wang
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Publication number: 20100216786Abstract: The present invention relates to the adenosine A3 receptor ligands of the general formula (I), within them favourably to the antagonists, to their salts, solvates, N-oxides and isomers, to the pharmaceutical compositions containing the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the use of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the preparation of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, as well as to the new intermediates of the general formula (II), (VI), (XI), (XII) and (XV), and to the preparation thereof.Type: ApplicationFiled: December 4, 2009Publication date: August 26, 2010Applicant: SANOFI-AVENTISInventors: Edit SUSAN, Kinga BOER, Zoltan KAPUI, Geza TIMARI, Sandor BATORI, Endre MIKUS, Judit VARGANE SZEREDI, Michel FINET, Katalin URBAN-SZABO, Tibor SZABO
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Publication number: 20100210629Abstract: The present invention provides for tricyclic compounds having the formula (I), wherein R1, R2, R5, R6, R7, and R8 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.Type: ApplicationFiled: April 23, 2010Publication date: August 19, 2010Inventors: William J. Pitts, James Kempson, Junqing Guo, Jagabandhu Das, Charles M. Langevine, Steven H. Spergel, Scott Hunter Watterson
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Patent number: 7772227Abstract: The invention relates to tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivative having the general Formula (I) wherein X is CH2, O or S; R represents 1-3 substituents independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy and halogen; R1 is (C5-8)cycloalkyl; R2 is H or (C1-4)alkyl; R3, R3?, R4? R4?, R5, R5? and R6? are independently hydrogen or (C1-4)-alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; R6 is hydrogen or (C1-4)alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; or R6 forms together with R7 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; R7 forms together with R6 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; or R7 is H, (C1-4)alkyl or (C3-5)cycloalkyl, the alkyl groups being optionally substituted with OH, halogen or (C1-4)alkyloxy; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 13, 2004Date of Patent: August 10, 2010Assignee: N.V. OrganonInventor: Julia Adam-Worrall
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Publication number: 20100197634Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: September 8, 2008Publication date: August 5, 2010Inventors: Tony Siu, Jonathan Young, Michael Altman, Alan Northrup, Matthew Katcher, Ellalahewage Sathyajith Kumarasinghe, Ekaterina Kozina, Scott Peterson, Matthew Childers
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Publication number: 20100184758Abstract: Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.Type: ApplicationFiled: July 15, 2008Publication date: July 22, 2010Inventors: Peter H. Dobbelaar, Wu Du, Liangqin Guo, William K. Hagmann, Shuwen He, Tianying Jian, Jian Liu, Ravi P. Nargund, Alexander Pasternak, Shrenik K. Shah, Quang T. Truong, Zhixiong Ye, James Deliureficio, Raman Bakshi
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Publication number: 20100179132Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing plasma and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention.Type: ApplicationFiled: March 2, 2010Publication date: July 15, 2010Inventors: Young-Choon Moon, Liangxian Cao, Nadarajan Tamilarasu, Hongyan Qi, Soongyu Choi, William Joseph Lennox, Donald Thomas Corson, Seongwoo Hwang, Thomas Davis
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Publication number: 20100158858Abstract: In accordance with the present invention, compounds are provided which are useful in a method or in the manufacture of a medicament for post-transcriptionally inhibiting the expression of VEGF in a subject in need thereof comprising inhibiting VEGF mRNA translation by orally administering said medicament once, twice or thrice daily to the subject.Type: ApplicationFiled: April 12, 2008Publication date: June 24, 2010Inventors: Liangxian Cao, Samit Hirawat, Langdon Miller, Gary Elfring, Thomas Davis, Marla L. Weetall
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Publication number: 20100120717Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture in comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: October 8, 2007Publication date: May 13, 2010Inventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Michael B. Wallace, Hasanthi Wijesekera
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Publication number: 20100105696Abstract: The invention relates to the use of compounds of formula (I) in the treatment of mammalian target of rapamycin (mTOR) kinase dependent diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical preparations comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.Type: ApplicationFiled: February 19, 2008Publication date: April 29, 2010Applicant: NOVARTIS AGInventors: Carlos Garcia-Echeverria, Paul Leslie Nicklin, Leon Murphy, Sauveur-Michel Maira, Peter Finan, Christine Fritsch, Saskia Maria Brachmann
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Publication number: 20100068181Abstract: The present invention provides compounds of Formula I (wherein R, R1, R3, R4, X, and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.Type: ApplicationFiled: December 19, 2007Publication date: March 18, 2010Inventors: Sunil Paliwal, Hon-Chung Tsui, Jose S. Duca, Charles A. Lesburg, Ronald J. Doll, Neng-Yang Shih
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Patent number: 7667039Abstract: The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.Type: GrantFiled: May 18, 2006Date of Patent: February 23, 2010Assignee: Novartis AGInventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
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Publication number: 20100035841Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.Type: ApplicationFiled: October 7, 2009Publication date: February 11, 2010Applicant: Pharmacyclics, Inc.Inventors: Orion D. JANKOWSKI, James T. Palmer, Lee Honigberg
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Publication number: 20100029616Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters and prodrugs thereof, pharmaceutical compositions containing compounds of formula (I) and the use of said compounds and compositions as urotensin II receptor antagonists.Type: ApplicationFiled: July 31, 2009Publication date: February 4, 2010Inventors: William A. Kinney, Diane K. Luci, Bruce E. Maryanoff, Shyamali Ghosh, Edward C. Lawson
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Publication number: 20100029635Abstract: This invention concerns the compounds the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R2 is hydrogen, aryl substituted with a radical —COOR4; or R2 is substituted C1-10alkyl, C2-10alkenyl or C3-7cycloalkyl; or R2 is a radical of formula: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b(b-5) -a1=a2-a3=a4- is —CH?CH—CH?CH—; —N?CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N— (c-5); wherein one of the hydrogen atoms in (c-1)-(c-5) is replaced by particular radicals; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, substituted carbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1.Type: ApplicationFiled: October 9, 2009Publication date: February 4, 2010Inventors: Bart Rudolf Romanie Kesteleyn, Sandrine Marie Helene Vendeville, Natalie Maria Francisca Kindermans, Dominique Louis Nestor Ghislai Surleraux, Pierre Jean-Marie Bernard Raboisson, Piet Tom Bert Paul Wigerinck, Annick Ann Peeters
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Publication number: 20100015140Abstract: A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.Type: ApplicationFiled: July 17, 2009Publication date: January 21, 2010Applicant: CRITICAL OUTCOME TECHNOLOGIES INC.Inventor: Wayne R. Danter
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Publication number: 20090291921Abstract: Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.Type: ApplicationFiled: November 19, 2008Publication date: November 26, 2009Applicant: Gilead Sciences, Inc.Inventors: Salman Y. Jabri, Haolun Jin, Choung U. Kim, Jiayao Li, Samuel E. Metobo, Michael R. Mish
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Publication number: 20090281081Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.Type: ApplicationFiled: May 6, 2009Publication date: November 12, 2009Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C. B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
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Patent number: 7612205Abstract: A main object is to provide a crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid acetonitrile solvate (Compound B) which is an intermediate for producing preferentially the type III crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl-1-piperazinyl]-4-oxo-4H-[1,3]-thiazeto[3,2-a]quinoline-3-carboxylic acid (Compound A). A crystal of Compound B can be preferentially precipitated by controlling the supersaturation concentration in crystalization using acetonitrile as a solvent. Subsequently, the type III crystal of Compound A can be produced by performing desolvation of the crystal.Type: GrantFiled: April 28, 2004Date of Patent: November 3, 2009Assignee: Nippon Shinyaku Co., Ltd.Inventors: Jun Akai, Hiroshi Nishida
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Publication number: 20090270411Abstract: The present invention relates to new phenanthridine derivatives of formula (I), wherein the variables are as defined in the specification, to processes for producing the same, to pharmacological compositions containing the same and to their use in therapy or prevention of painful and inflammatory processes.Type: ApplicationFiled: December 19, 2006Publication date: October 29, 2009Inventors: Gyula Beke, Eva Bozo, Gabor Czira, Janos Eles, Sandor Farkas, Katalin Hornok, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
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Publication number: 20090253695Abstract: Certain imidazonaphthyridines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-? biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: February 22, 2006Publication date: October 8, 2009Applicant: Coley Pharmaceutical Group, Inc,Inventors: Tushar A. Kshirsagar, Scott E. Langer, Shri Niwas, George W. Griesgraber, Philip D. Heppner, Kyle J. Lindstrom
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Publication number: 20090227561Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.Type: ApplicationFiled: February 25, 2009Publication date: September 10, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Nobuhiro FUJII, Yuya OGURO, Satoshi SASAKI, Shigeru KONDO
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Publication number: 20090186881Abstract: The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3, R4 and X are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, mixtures and salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I in which one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: ApplicationFiled: January 30, 2009Publication date: July 23, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Marco SANTAGOSTINO, Fabio PALEARI, Gerhard SCHAENZLE, Kirsten ARNDT, Henri DOODS
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Publication number: 20090186901Abstract: The present invention relates to new heterocyclic compounds of general formula (1) wherein the groups R1 to R7, k, X and Y have the meanings given in the claims and specification, the isomers and salts thereof as well as the use thereof as medicaments. Background to the invention WO 01/36423 describes 3,4-dihydrospiro[chromene-2,4?-piperidine] derivatives for treating diseases of the central nervous system. Spirocyclic heterocycles as ?-opioid receptor ligands for treating pain and anxiety states as well as diseases of the gastrointestinal tract are known from WO 2005/033073. The aim of the present invention is to indicate new active substances which can be used for the prevention and/or treatment of diseases characterised by excessive or abnormal cell proliferation.Type: ApplicationFiled: May 3, 2007Publication date: July 23, 2009Inventors: Ulrich Reiser, Oliver Kraemer, Peter Sennhenn, Walter Spevak
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Publication number: 20090176757Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2 and R6 are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: ApplicationFiled: November 14, 2006Publication date: July 9, 2009Inventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump, Cory R. Theberge, C. Blair Zartman
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Patent number: 7557107Abstract: Disclosed are novel tricyclic compounds of the formula: and a pharmaceutically acceptable salts or solvates thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I). Also disclosed are uses of the compounds of formula (I) for the manufacture of a medicament for the treatment of cancer.Type: GrantFiled: August 4, 2004Date of Patent: July 7, 2009Assignee: Schering CoporationInventors: Hugh Y. Zhu, Alan B. Cooper, Jagdish A. Desai, James J-S Wang, Ronald J. Doll, F. George Njoroge, Viyyoor M. Girijavallabhan
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Publication number: 20090163512Abstract: There are provided compounds of the formula and pharmaceutically acceptable salts and esters and enantiomers thereof wherein W, X, X?, Y, V, V?, A, B and R are as described herein. The compounds have utility as antiproliferative agents, especially, as anticancer agents.Type: ApplicationFiled: November 18, 2008Publication date: June 25, 2009Inventors: Li Chen, Xingchun Han, Yun He, Song Yang, Zhuming Zhang
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Publication number: 20090156557Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: April 15, 2008Publication date: June 18, 2009Applicant: TAKEDA SAN DIEGO, INC.Inventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Xianchang Gong, Yan Liu, Nicholas Scorah, Michael B. Wallace
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Publication number: 20090156610Abstract: There are provided compounds of the formula and pharmaceutically acceptable salts and esters thereof wherein W, V, X, Y, A, R and R? are as described herein. The compounds are useful as anticancer agents.Type: ApplicationFiled: November 18, 2008Publication date: June 18, 2009Inventors: Qingjie Ding, Nan Jiang, Song Yang, Jing Zhang, Zhuming Zhang
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Publication number: 20090131423Abstract: The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: October 18, 2006Publication date: May 21, 2009Applicant: MERCK & CO., INC.Inventors: Christopher J. Dinsmore, Ana Esther Gabarda Ortega, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Jonathan R. Young
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Publication number: 20090117040Abstract: The present invention relates to pharmaceutical and diagnostic compositions as well as to the use of the active substances contained therein for preparing a pharmaceutical or a diagnostic composition for the treatment or diagnosis of neurodegenerative disorders or amyloid diseases.Type: ApplicationFiled: February 11, 2005Publication date: May 7, 2009Applicant: Max-Delbrug-Centrum Fur Molekulare MedizinInventors: Erich Wanker, Sabine Engemann, Susanne Rautenberg, Annett Boeddrich, Phoebe Markovic, Dagmar Ehrnhofer, Martin Herbst, Jacqueline Walther
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Publication number: 20090093454Abstract: The present invention provides compounds of Formula (I) comprising: including salts, solvates, and physiologically functional derivatives thereof, pharmaceutical formulations containing them, processes for their preparation, and methods of treatment using them.Type: ApplicationFiled: March 1, 2006Publication date: April 9, 2009Inventors: Kristjan Gudmundsson, John G. Catalano, Angilique Svolto
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Publication number: 20090075980Abstract: Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, and prodrugs thereof, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: March 31, 2006Publication date: March 19, 2009Applicant: Coley Pharmaceutical Group, Inc.Inventors: David S. Hays, Michael E. Danielson, John F. Gerster, Shri Niwas, Ryan B. Prince, Tushar A. Kshirsagar, Philip D. Heppner, William H. Moser, Joan T. Moseman, Matthew R. Radmer, Maureen A. Kavanagh, Sarah A. Strong, Jason D. Bonk
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Publication number: 20090069314Abstract: Certain imidazoquinolines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, and an aryl or heteroaryl substituent at the 7-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-? biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: February 22, 2006Publication date: March 12, 2009Applicant: Coley Pharmaceutical Group, Inc.Inventors: Tushar A. Kshirsagar, Bryon A. Merrill, Shri Niwas, Gregory D. Lundquist, JR., Philip D. Heppner, Michael E. Danielson
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Patent number: 7501418Abstract: The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherein the variables are defined as in Claim 1.Type: GrantFiled: August 13, 2003Date of Patent: March 10, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, José Manuel Bartolomé -Nebreda, Francisco Javier Fernández-Gadea, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Megens
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Publication number: 20090054429Abstract: This invention provides novel arylindenopyridines and arylindenopyrimidines of the formula: wherein R1, R2, R3, R4, and X are as defined above, and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing adenosine A2a receptors. This invention also provides therapeutic and prophylactic methods using the instant compounds and pharmaceutical compositions.Type: ApplicationFiled: October 23, 2008Publication date: February 26, 2009Inventors: Geoffrey R. Heintzelman, James Lawrence Bullington, Kenneth C. Rupert
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Publication number: 20090036464Abstract: This invention relates to a method of testing agents, such as sigma ligands for their potential use in treating posterior capsule opacification (PCO). The present invention also relates to the use of sigma ligands, such as sigma-1 antagonists in the manufacture of a medicament for preventing posterior capsule opacification (PCO), as well as methods of treating PCO using sigma ligands.Type: ApplicationFiled: August 26, 2005Publication date: February 5, 2009Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Barbara Ann Spruce, George Duncan, Peter Reid Duncan, Alan Prescott
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Publication number: 20090036441Abstract: 3H-Benzo[e]indol-4,5-dione derivatives with antitumor activity, the processes for the preparation thereof and pharmaceutical compositions containing them.Type: ApplicationFiled: December 22, 2005Publication date: February 5, 2009Applicant: Cell Therapeutics Europe S.R.L.Inventors: Mario Grugni, Mara Cassin, Gennaro Colella, Sergio De Munari, Gianluca Pardi, Paolo Pavesi
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Patent number: 7485645Abstract: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17?-hydroxysteroid dehydrogenase, 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 type 3 17?-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.Type: GrantFiled: August 9, 2007Date of Patent: February 3, 2009Assignee: Schering CorporationInventors: Timothy J. Guzi, Yi-Tsung Liu, Ronald J. Doll, Anil Saksena, Viyyoor M. Girijavallabhan, Jonathan A. Pachter
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Publication number: 20090029939Abstract: Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl, Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.Type: ApplicationFiled: May 25, 2007Publication date: January 29, 2009Inventors: James M. Chen, Xiaowu Chen, Maria Fardis, Haolun Jin, Choung U. Kim, Laura N. Schacherer
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Publication number: 20090029983Abstract: This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to pharmaceutical compositions comprising thienopyridines and to the use of such compositions to treat Hepatitis B and other diseases.Type: ApplicationFiled: January 3, 2008Publication date: January 29, 2009Applicant: Valeant Research & DevelopmentInventors: Huanming Chen, Robert Tam, Anneke K. Raney