The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/361)
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Publication number: 20090246169Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: February 21, 2007Publication date: October 1, 2009Inventors: Matthias Vennemann, Thomas Bar, Jürgen Braunger, Astrid Zimmermann, Volker Gekeler
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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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Patent number: 7582761Abstract: Therapeutic benzimidazoles having the general structure: and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gasType: GrantFiled: October 16, 2003Date of Patent: September 1, 2009Assignee: Amgen Inc.Inventors: Chenera Balan, Yunxin Bo, Celia Dominguez, Christopher H. Fotsch, Vijay K. Gore, Vu Van Ma, Mark H. Norman, Vassil I. Ognyanov, Yi-xin Qian, Xianghong Wang, Ning Xi, Shimin Xu
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Patent number: 7576087Abstract: 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: GrantFiled: June 19, 2007Date of Patent: August 18, 2009Assignee: WyethInventors: Ronald Charles Bernotas, Yinfa Yan
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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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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: 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: 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: 20090124001Abstract: The invention relates to compounds according to general formula (1) and/or their enantiomers, diastereomers as well as their pharmaceutically compatible salts, and to the use thereof for producing a medicament suited for treating diseases associated with misfolded proteins.Type: ApplicationFiled: February 28, 2006Publication date: May 14, 2009Applicant: HEINRICH-HEINE UNIVERSITÄT DUSSELDORFInventors: Carsten Korth, Ralf Klingenstein, Stefan Lober, Peter Gmeiner
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Patent number: 7531535Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: December 13, 2007Date of Patent: May 12, 2009Assignee: Bristol-Meyers Squibb CompanyInventors: Donald J. P. Pinto, Jennifer X. Qiao
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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: 20090111987Abstract: Disclosed herein are novel imino-indeno[1,2-c]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these derivatives, their synthetic precursors and their uses in the manufacture of pharmaceutical compositions for use in the treatment of cancers.Type: ApplicationFiled: October 31, 2007Publication date: April 30, 2009Applicant: Kaohsiung Medical UniversityInventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Chih-Hua Tseng, Pei-Jung Lu
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Publication number: 20090099161Abstract: Imidazoquinolines and imidazonaphthyridines with a substituent containing a functional group, e.g., an amide, sulfonamide, urea, or heterocyclyl group, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: February 10, 2006Publication date: April 16, 2009Applicant: Coley Pharmaceutial Group, Inc.Inventors: Michael J. Rice, Chad A. Haraldson, John F. Gerster, Joshua R. Wurst, Philip D. Heppner, Bryon A. Merrill, Tushar A. Kshirsagar
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Publication number: 20090093455Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: ApplicationFiled: October 3, 2008Publication date: April 9, 2009Inventors: Johnny Yasuo NAGASAWA, Fabrice PIERRE, Mustapha HADDACH, Michael SCHWAEBE, Levan DARJANIA, Jeffrey P. WHITTEN
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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: 20090088419Abstract: The present invention provides a compound represented by the formula (I): wherein R1 is a C?1-6#191 alkyl group optionally substituted by a C?3-10#191 cycloalkyl group, R2 is a C?2-6#191 alkyl group, R3 is a hydrogen atom, a C?1-6#191 alkyl group or a halogen atom, and X is —OR6 or —NR4R5 wherein R4 and R6 are each independently a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R5 is an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted hydroxy group, or R4 and R5 optionally form, together with the adjacent nitrogen atom, an optionally substituted nitrogen-containing heterocycle, or a salt thereof. The compound of the present invention has a superior peptidase inhibitory action and is useful as an agent for the prophylaxis or treatment of diabetes and the like.Type: ApplicationFiled: February 24, 2006Publication date: April 2, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Hironobu Maezaki, Nobuhiro Suzuki
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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: 20090068577Abstract: The present invention provides a naphthalenetetracarboxylic acid diimide derivative represented by the following general formula (1): wherein R1 and R2, which are identical or different, each represent a substituted or non-substituted alkyl group or a substituted or non-substituted aromatic hydrocarbon group; R3 represents an alkyl group having 1 to 8 carbon atoms or an aromatic hydrocarbon group; R4, R5, R6 and R7, which are identical or different, each represent a hydrogen atom, a substituted or non-substituted alkyl group, or a substituted or non-substituted aromatic hydrocarbon group; and R1 and R2 may be linked to form a substituted or non-substituted heterocyclic group including a nitrogen atom; with compounds where all of R1, R2 and R3 are a methyl group, and compounds where both of R1 and R2 are a methyl group and R3 is a 1-octyl group being excluded.Type: ApplicationFiled: September 5, 2008Publication date: March 12, 2009Applicant: RICOH COMPANY, LTD.Inventors: Masafumi OHTA, Tomoyuki SHIMADA, Yuuji TANAKA, Eiji KURIMOTO, Keisuke SHIMOYAMA
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Publication number: 20090069305Abstract: The present invention relates to substituted nitrogen-containing heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using any of these derivatives and compositions for H4 receptor activity modulation and the treatment of states mediated by histamine H4 receptor activity.Type: ApplicationFiled: September 11, 2008Publication date: March 12, 2009Inventors: Michael D. Gaul, Bao-Ping Zhao, Xizhen Zhu
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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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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: 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
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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: 20090018127Abstract: Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disordersType: ApplicationFiled: May 29, 2006Publication date: January 15, 2009Inventors: Rolf Baenteli, Fraser Glickman, Jiri Kovarik, Ian Lewis, Markus Streiff, Gebhard Thoma, Hans-Gunter Zerwes
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Publication number: 20090018122Abstract: Imidazoquinoline compounds with an aryloxy or arylalkyleneoxy or hydroxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: August 27, 2004Publication date: January 15, 2009Inventors: Kyle J. Lindstrom, Hugues M.H. Martin, Bryon A. Merrill, Michael J. Rice, Joshua R. Wurst, Chad A. Haraldson, Tushar A. Kshirsagar, Philip D. Heppner, Shri Niwas, George W. Griesgraber, Matthew R. Radmer
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Publication number: 20090005365Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: ApplicationFiled: June 6, 2008Publication date: January 1, 2009Applicant: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
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Patent number: 7465742Abstract: 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: GrantFiled: February 3, 2006Date of Patent: December 16, 2008Inventors: Huanming Chen, Robert Tam, Anneke K. Raney
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Publication number: 20080306048Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta
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Publication number: 20080306049Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
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Patent number: 7462717Abstract: The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising themType: GrantFiled: August 19, 2003Date of Patent: December 9, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Encarnacion Matesanz-Ballesteros, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Petrus Megens
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Publication number: 20080293712Abstract: The present invention relates to Benzo[c][2,7]naphthyridine Derivatives, compositions comprising an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for treating or preventing a proliferative disorder or an autoimmune disease, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for modulating PDK-1 activity, PKA activity, Akt activity, S6K activity, or PKC activity, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative. The invention also relates to processes for preparing a Benzo[c][2,7]naphthyridine Derivative.Type: ApplicationFiled: March 4, 2008Publication date: November 27, 2008Applicant: WYETHInventors: Allan WISSNER, Middleton Brawner FLOYD, JR., Russell DUSHIN, Heidi L. FRASER, Yongbo HU, Andreas MADERNA, Thomas NITTOLI, Yanong Daniel WANG
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Publication number: 20080287432Abstract: The invention provides a novel class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.Type: ApplicationFiled: August 15, 2006Publication date: November 20, 2008Applicants: IRM LLC, The Scripps Research InstituteInventors: Barun Okram, Pingda Ren, Nathanael S. Gray
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Patent number: 7446110Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.Type: GrantFiled: September 2, 2004Date of Patent: November 4, 2008Assignee: Merck & Co., Inc.Inventors: Mildred L. Kaufman, Robert S. Meissner, Helen J. Mitchell
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Publication number: 20080261961Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyctosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.Type: ApplicationFiled: April 18, 2008Publication date: October 23, 2008Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20080255110Abstract: This invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Z, m, n, o, p and r are as defined herein, its preparation, pharmaceutical composition and use as an adenosine A3 receptor ligand preferably an antagonist.Type: ApplicationFiled: June 17, 2008Publication date: October 16, 2008Applicant: SANOFI-AVENTISInventors: Peter ARANYI, Laszlo BALAZS, Maria BALOGH, Sandor BATORI, Lajos T. NAGY, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin GERBER, Judit VARGANE SZEREDI, Katalin URBAN-SZABO, Erzsebet WALCZ
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Patent number: 7435726Abstract: This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase inhibitors. A particular composition comprises thalidomide, or a pharmaceutically acceptable salt, solvate, or clathrate thereof, and irinotecan. The invention also relates to methods of treating or preventing cancer which comprise the administration of a thalidomide and another anti-cancer drug to a patient in need of such treatment or prevention. The invention further relates to methods of reducing or avoiding adverse side effects associated with the administration of chemotherapy or radiation therapy which comprise the administration of thalidomide to a patient in need of such reduction or avoidance.Type: GrantFiled: May 14, 2001Date of Patent: October 14, 2008Assignee: Celgene CorporationInventors: Jerome B. Zeldis, Andrew L. Zeitlin, Sol Barer
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Patent number: 7432276Abstract: The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.Type: GrantFiled: December 27, 2006Date of Patent: October 7, 2008Assignee: CV Therapeutics, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki, Dmitry Koltun, Melanie Boze
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Publication number: 20080234287Abstract: The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by incorporating 5- or 6-membered heteroaromatic ring and/or introducing S heteroatom, thus increasing the anti-tumor activity of naphthalimide. The compounds of the invention displays significant inhibiting activities to the proliferation of various tumor cells such as human lung cancer, gastric cancer, liver cancer, leucocythemia and the like. The inhibition of cell proliferation is dose-dependent.Type: ApplicationFiled: May 7, 2008Publication date: September 25, 2008Inventors: Xuhong Qian, Yonggang Li, Yufang Xu, Jian Ding, Liping Lin, Zehong Miao, Hong Zhu, Baoyuan Qu
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Publication number: 20080221118Abstract: Compounds of the formula I, in which s, k, I, W, R1, R2, R3, and U have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 31, 2006Publication date: September 11, 2008Inventors: Wolfgang Staehle, David Bruge, Kai Schiemann, Dirk Finsinger, Hans-Peter Buchstaller, Frank Zenke, Christiane Amendt
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Patent number: 7423045Abstract: The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.Type: GrantFiled: June 28, 2006Date of Patent: September 9, 2008Assignee: CV Therapeutics, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki, Dmitry Koltun
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Publication number: 20080214536Abstract: Compounds of a certain formula (I) in which R1, R2, R3, R31, R4, R5, R51, R6 and R7 have the meanings indicated in the description, are novel effective PDE4 inhibitors.Type: ApplicationFiled: March 9, 2006Publication date: September 4, 2008Applicant: NYCOMED GmbhInventors: Ulrich Kautz, Beate Schmidt, Dieter Flockerzi, Maria Vittoria Chiesa, Armin Hatzelmann, Christof Zitt, Johannes Barsig, Degenhard Marx, Hans-Peter Kley
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Publication number: 20080194579Abstract: 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: ApplicationFiled: May 18, 2006Publication date: August 14, 2008Inventors: Carlos Garcia-Echeverria, Frederic Stauffer, Pascal Furet
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BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20080176847Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 28, 2007Publication date: July 24, 2008Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20080171744Abstract: The present invention is directed to a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.Type: ApplicationFiled: January 11, 2008Publication date: July 17, 2008Applicant: 6441513 CANADA INC.Inventors: Wayne R. Danter, Martyn Brown, Franck LePifre
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Publication number: 20080146546Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.Type: ApplicationFiled: February 4, 2008Publication date: June 19, 2008Inventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
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Patent number: 7388016Abstract: The present invention relates to Dibenzonaphthyridine Derivatives, compositions comprising an effective amount of a Dibenzonaphthyridine Derivative and methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof an effective amount of a Dibenzonaphthyridine Derivative.Type: GrantFiled: December 6, 2006Date of Patent: June 17, 2008Assignee: WyethInventors: Ariamala Gopalsamy, Mengxiao Shi, Kristina Kutterer, Kim Timothy Arndt
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Patent number: 7384939Abstract: The present invention provides a process for preparing a pyridine compound of the formula: wherein R1, R2, R3 and a are those defined herein.Type: GrantFiled: July 5, 2005Date of Patent: June 10, 2008Assignee: Roche Colorado CorporationInventors: Peter J. Harrington, David A. Johnston, L. Mark Hodges
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Publication number: 20080113962Abstract: The invention relates to condensed tricyclic benzimidazoles of formula (I) in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.Type: ApplicationFiled: September 30, 2005Publication date: May 15, 2008Applicant: Aitana Pharma AGInventors: Peter Jan Zimmermann, Wilm Buhr, Christof Brehm, Andreas Palmer, M. Vittoria Chiesa, Wolfgang-Alexander Simon, Stefan Postius, Wolfgang Kromer
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Publication number: 20080108627Abstract: The present invention relates to a quinoline derivative having the general formula (A): in which R1, R2, X, Y and Z are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).Type: ApplicationFiled: June 20, 2007Publication date: May 8, 2008Inventors: Olaf Prien, Knut Eis, Wolfgang Schwede, Judith Guenther, Dieter Zopf
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Patent number: 7354918Abstract: The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical —AR? wherein A represents a heteroatom and R? represents a group selected from the group comprising linear or branched C1-C6 alkyl radicals, C2-C6 alkenyls, C2-C6 alkynyls, arylalkyls; esters comprising the formula —R1— CO—O—R2; amides comprising the formula —R3—CO—NZY, wherein Y and Z together can form a cycloalkyl radical or a heterocyclic radical, optionally substituted by one or more alkyl radicals; a radical selected from the group comprising alkyl radicals, alkenyls or alkynyls, substituted by at least one amine with formula —NZY; or one of the pharmaceutically-acceptable salts thereof, including the isomers, enantiomers and diastereoisomers thereof and mixtures thereof.Type: GrantFiled: October 13, 2006Date of Patent: April 8, 2008Assignee: BiocortechInventors: Paola Ciapetti, Laurence Deyon, Camille-Georges Wermuth, Jean-François Pujol, Dinah Weissmann