Ring Nitrogen Is Shared By Two Of The Cyclos (e.g., Ergot, Alkaloids, Etc.) Patents (Class 544/346)
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Publication number: 20120232086Abstract: The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.Type: ApplicationFiled: November 12, 2010Publication date: September 13, 2012Applicant: MERCK SHARP & DOHME CORP.Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew W. Stampford
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Publication number: 20120184734Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: June 14, 2010Publication date: July 19, 2012Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
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Publication number: 20120172352Abstract: The present invention is related to pyrazoline dione derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: September 27, 2010Publication date: July 5, 2012Applicant: GENKYOTEX SAInventors: Patrick Page, Francesca Gaggini, Benoît Laleu
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Patent number: 8207169Abstract: The compounds of Formula D are of the class of triazolo-pyrido-pyrazines which are inhibitors of AKT useful for the treatment of cancerType: GrantFiled: May 28, 2009Date of Patent: June 26, 2012Assignee: MSD K.K.Inventors: Hidetomo Furuyama, Yasuhiro Goto, Nobuhiko Kawanishi, Mark E. Layton, Takashi Mita, Akira Naya, Yoshio Ogino, Yu Onozaki, Kevin J. Rodzinak, Toshihiro Sakamoto, Philip E. Sanderson, Jiabing Wang
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Publication number: 20120157460Abstract: The present invention relates to tetrahydro-azacarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.Type: ApplicationFiled: December 20, 2011Publication date: June 21, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Matthew D. SURMAN, Peter R. GUZZO, Emily FREEMAN, Alan J. HENDERSON
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Publication number: 20120135998Abstract: The present invention relates to compounds of formula (I), racemates, isomers and/or salts thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds.Type: ApplicationFiled: November 22, 2011Publication date: May 31, 2012Inventors: Penelope Anne Mayes, Jeffrey Peter Mitchell, Alistair George Draffan, Gary Robert William Pitt, Kelly Helen Anderson, Chin Yu Lim
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Publication number: 20120128662Abstract: The present invention relates to substituted imidazoquinoxaline compounds of general formula (I) as inhibitors of Mps-1 Kinase or TTK, and being active against inflammation and cancer.Type: ApplicationFiled: April 24, 2010Publication date: May 24, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Marcus Koppitz, Benjamin Bader, Ulf Bömer, Bertolt Kreft, Philip Lienau, Tobias Marquardt, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
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Publication number: 20120122835Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: January 18, 2012Publication date: May 17, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20120115875Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: January 18, 2012Publication date: May 10, 2012Inventors: Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Patent number: 8173657Abstract: The invention provides novel compositions comprising imidazoquinoxaline compounds of formula (I) and analogs thereof. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an) other agent(s).Type: GrantFiled: March 23, 2007Date of Patent: May 8, 2012Assignee: Novartis AGInventors: James Sutton, Feng Xu, Nicholas Valiante, Jiong Lan
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Patent number: 8163752Abstract: Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y 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: GrantFiled: June 3, 2008Date of Patent: April 24, 2012Assignee: Merck, Sharp & Dohme Corp.Inventors: Ian Bell, Craig A. Stump
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Publication number: 20120088770Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: ApplicationFiled: May 7, 2010Publication date: April 12, 2012Applicant: Prism BioLab CorporationInventors: Takenao Odagami, Yiji Kogami, Hiroyuki Kouji
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Publication number: 20120082640Abstract: The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.Type: ApplicationFiled: October 4, 2010Publication date: April 5, 2012Inventors: Gunnar J. Hanson, David Thomas, Nizal Chandrakumar, Susan Harran
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Publication number: 20120065187Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Applicants: ALCON RESEARCH, LTD, KALYPSYS, INC.Inventors: Allen J. Borchardt, Clay Beauregard, Travis Cook, Robert L. Davis, Daniel A. Gamache, John M. Yanni
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Patent number: 8133891Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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: GrantFiled: March 5, 2010Date of Patent: March 13, 2012Assignee: Merck, Sharp & Dohme Corp.Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
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Patent number: 8129385Abstract: The present invention is directed to a class of substituted 5-hydroxy-3,4,6,9,9a,10-hexahydro-2H-1-oxa-4a,8a-diaza-anthracene-6,10-diones useful as anti-HIV agents. The compounds have the formula: Z?O; R20, R21, R22, R23, R24 and R25 independently are hydrogen, C1-C8 alkyl, (C6-C14)aryl-(C1-C8)alkyl, C6-C14 aryl, or alkoxy; the stereochemistry of an asymmetric carbon represented by * shows R- or S-configuration, or a mixture thereof; RX is hydrogen; R14 is hydrogen or optionally substituted lower alkyl; R3 is hydrogen; R1 is hydrogen or lower alkyl; R is halogen; and m is 1, 2 or 3; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 28, 2006Date of Patent: March 6, 2012Assignees: Shionogi & Co., Ltd., GlaxoSmithKline LLCInventors: Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Publication number: 20120040990Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20120035172Abstract: The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.Type: ApplicationFiled: October 17, 2011Publication date: February 9, 2012Applicant: INCYTE CORPORATIONInventors: Changsheng Zheng, Chu-Biao Xue, Ganfeng Cao, Michael Xia, Anlai Wang, Hai Fen Ye, Brian Metcalf
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Publication number: 20120022251Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.Type: ApplicationFiled: March 26, 2010Publication date: January 26, 2012Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
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Patent number: 8097628Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof: (relative chemistry shown) pharmaceutical compositions comprising them, their use in therapy especially against tuberculosis, and methods of preparing them are described.Type: GrantFiled: May 21, 2009Date of Patent: January 17, 2012Assignee: Glaxo Group LimitedInventors: Carlos Alemparte-Gallardo, Christopher Barfoot, David Barros-Aguirre, Monica Cacho-Izquierdo, Jose Maria Fiandor Roman, Alan Joseph Hennessy, Neil David Pearson, Modesto Jesus Remuinan-Blanco
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Publication number: 20110319287Abstract: The present invention relates inter alia to methods for identifying modulators of tumour necrosis factor (TNF) signalling. In one aspect, the method involves identifying an agent that modulates a signalling pathway mediated by TNF, comprising the steps of providing a host cell comprising TNF receptor 1 (TNFR1)-associated death domain (TRADD) linked to a reporter molecule, and determining at least one cellular characteristic detectable by the reporter molecule in the host cell in the presence of TNF and in the presence and absence of a candidate modulator. The invention is suitable for high-throughput screening (HTS) and high-content screening (HCS), or a combination of HTS and HCS.Type: ApplicationFiled: January 19, 2010Publication date: December 29, 2011Applicant: ADDEX PHARMA S.A.Inventors: Aurelie Florence Chedal-bornu goiller, Vincent Mutel, Robert Johannes Luetjens
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Publication number: 20110319385Abstract: [Problem] Provided is a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like. [Means for Solution] The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like, and thus, have found that an imidazoquinoxaline compound or a triazoloquinoxaline compound has a PDE9-inhibiting action, thereby completing the present invention. The imidazoquinoxaline compound or the triazoloquinoxaline compound of the present invention has a PDE9-inhibiting action and can be used as an agent for preventing and/or treating storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.Type: ApplicationFiled: March 4, 2010Publication date: December 29, 2011Applicant: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Mari Sugita, Hidenori Azami, Ryushi Seo, Takaho Nomura, Satoshi Yamamoto, Hirofumi Yamamoto, Kazuyuki Tsuchiya, Hideki Kubota, Kazunori Kamijo
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Publication number: 20110311474Abstract: The invention provides compounds of Formula (I) and Formula (II) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: December 1, 2010Publication date: December 22, 2011Applicant: ABBOTT LABORATORIESInventors: Neil WISHART, Maria A. ARGIRIADI, David J. CALDERWOOD, Anna M. ERICSSON, Bryan R. FIAMENGO, Kristine E. FRANK, Michael FRIEDMAN, Dawn M. GEORGE, Eric R. GOEDKEN, Nathan S. JOSEPHSOHN, Biqin C. LI, Michael J. MORYTKO, Kent D. STEWART, Jeffrey W. VOSS, Grier A. WALLACE, Lu WANG, Kevin R. WOLLER
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Publication number: 20110305636Abstract: Briefly described, embodiments of this disclosure include compounds as described herein, labeled compounds as described herein, pharmaceutical composition including compounds described herein, methods of imaging, method of forming a compound as described herein, and the like. In particular, embodiments of the disclosure include a series of triamino-pyridine derivatives and labeled triamino-pyridine derivatives, methods of synthesizing these compounds, intermediate compounds, methods of treatment using these compounds, methods of imaging, diagnosing, localizing, monitoring, and/or assessing a condition (e.g., corticotropin releasing factor type-1 (CRF1)) and/or related biological events, using triamino-pyridine derivatives, and the like. In addition, the present disclosure includes compositions (e.g., labeled triamino-pyridine derivatives that are ligands for the CRF1 receptor) used in and methods relating to non-invasive imaging (e.g., positron emission tomography (PET) imaging or SPECT imaging).Type: ApplicationFiled: March 12, 2010Publication date: December 15, 2011Applicant: EMORY UNIVERSITYInventors: Jeff Stehouwer, Mark Goodman, Clint Kilts, Charles Nemeroff
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Publication number: 20110282055Abstract: A synthesis approach providing an early ring attachment via a bromination to compound 1-1 yielding compound II-II whereby a final product such as AA can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.Type: ApplicationFiled: December 8, 2009Publication date: November 17, 2011Inventors: Hiroshi Yoshida, Yoshiyuki Taoda, Brian Johns, Takashi Kawasuji, Daiki Nagamatsu
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Publication number: 20110275621Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: May 13, 2011Publication date: November 10, 2011Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne
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Publication number: 20110263855Abstract: Processes are provided which create an aldehyde methylene, or hydrated or hemiacetal methylene attached to a heteroatom of a 6 membered ring without going through an olefinic group and without the necessity of using an osmium reagent. In particular, a compound of formula (I) can be produced from (II) and avoid the use of an allyl amine: (formulae I and II) where R, P1P3, R3 and Rx are as described herein.Type: ApplicationFiled: December 9, 2009Publication date: October 27, 2011Applicants: SHIONOGI & CO., LTD., GLAXOSMITHKLINE LLCInventors: Brian Alvin Johns, Maosheng Duan, Toshikazu Hakogi
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Publication number: 20110257137Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: ApplicationFiled: March 10, 2011Publication date: October 20, 2011Applicant: KALYPSYS, INC.Inventors: Allen Borchardt, Robert Davis, Clay Beauregard, Daniel Becker, Daniel Gamache, Stewart A. Noble, Mark Hellberg, Peter Klimko, Zhihai Qiu, Joseph Payne, John Yanni
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Patent number: 8008287Abstract: Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.Type: GrantFiled: May 16, 2007Date of Patent: August 30, 2011Assignee: Gilead Sciences, Inc.Inventors: Zhenhong R. Cai, Salman Y. Jabri, Haolun Jin, Rachael A. Lansdown, Samuel E. Metobo, Michael R. Mish, Richard M. Pastor
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Publication number: 20110207728Abstract: The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.Type: ApplicationFiled: February 8, 2011Publication date: August 25, 2011Applicant: Biota Scientific Management Pty Ltd.Inventors: Jeffrey Peter MITCHELL, Gary PITT, Alistair George DRAFFAN, Penelope Anne MAYES, Laura ANDRAU, Kelly ANDERSON
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Patent number: 7998950Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: July 24, 2009Date of Patent: August 16, 2011Assignee: Gilead Sciences, Inc.Inventors: Evangelos Aktoudianakis, Azim Alan Celebi, Zhimin Du, Salman Y. Jabri, Haolun Jin, Choung U. Kim, Jiayao Li, Samuel E. Metobo, Michael R. Mish, Barton W. Phillips, Joseph H. Saugier, Zheng-Yu Yang, Catalin Sebastian Zonte
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Publication number: 20110190489Abstract: The invention provides a compound of Formula (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ii), (Ij), (Ik), or (Il) as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: December 1, 2010Publication date: August 4, 2011Applicant: Abbott LaboratoriesInventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Bryan R. Fiamengo, Kristine E. Frank, Michael Friedman, Dawn M. George, Eric R. Goedken, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Kent D. Stewart, Jeffrey W. Voss, Grier A. Wallace, Lu Wang, Kevin R. Woller, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal
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Publication number: 20110183940Abstract: The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: July 23, 2009Publication date: July 28, 2011Inventors: Brian Alvin Johns, Jason Gordon Weatherhead, Toshikazu Hakogi, Yasunori Aoyama
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Publication number: 20110160183Abstract: 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: March 11, 2011Publication date: June 30, 2011Applicant: Merck & Co., Inc.Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
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Publication number: 20110158989Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: March 4, 2011Publication date: June 30, 2011Applicant: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20110152280Abstract: Provided herein are novel ergoline derivatives and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and or 5-HT1B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of regulating serotonin transport using the compounds and compositions disclosed herein.Type: ApplicationFiled: December 23, 2010Publication date: June 23, 2011Applicant: MAP Pharmaceuticals, Inc.Inventors: ROBERT O. COOK, Thomas A. Armer, Sergey Alexandrovich Kosarev, Dejian Xie
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Patent number: 7947682Abstract: Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Such compounds include a compound of Formula II, wherein R is H, alkyl, or halogen; R? is H, alkyl, or halogen; X is CH or N; and Y comprises a homocyclic or heterocyclic ring. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating gene expression.Type: GrantFiled: December 29, 2004Date of Patent: May 24, 2011Assignee: University of Southern CaliforniaInventors: Nouri Neamati, Antonio Garofalo
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Patent number: 7947677Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, J, K, T, U, V, W, X, Y and Z 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: GrantFiled: November 14, 2006Date of Patent: May 24, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman, Harold G. Selnick
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Publication number: 20110112104Abstract: Compounds of formula (I): wherein: A represents a 5, 6 or 7-membered (hetero)aromatic or non-aromatic ring, Z1, Z2 and Z3 each independently of the others represents a CH group or a nitrogen atom, it being understood that at least one of these three groups is a nitrogen atom, X represents an alkylene chain as defined in the description, R2 represents an aryl or heteroaryl group, the group R1 represents a group of formula (II) as defined in the description Medicinal products containing the same which are useful in treating conditions involving a defect in apoptosis.Type: ApplicationFiled: July 10, 2009Publication date: May 12, 2011Applicant: LES LABORATOIRES SERVIERInventors: Patrick Casara, Thierry Le Diguarher, Didier Durand, Olivier Geneste, John Hickman
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Publication number: 20110112106Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.Type: ApplicationFiled: January 7, 2011Publication date: May 12, 2011Applicant: Amira Pharmaceuticals, Inc.Inventors: John Howard HUTCHINSON, Thomas Jonathan SEIDERS, Brian Andrew STEARNS, Bowei WANG, Jill Melissa SCOTT, Yen Pham TRUONG
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Publication number: 20110092511Abstract: 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, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity especially Akt1 by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: May 28, 2009Publication date: April 21, 2011Inventors: Hidetomo Furuyama, Yasuhiro Goto, Nobuhiko Kawanishi, Mark E. Layton, Takashi Mita, Akira Naya, Yoshio Ogino, Yu Onozaki, Kevin J. Rodzinak, Toshihiro Sakamoto, Philip E. Sanderson, Jiabing Wang
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Patent number: 7928105Abstract: Disclosed are compounds of the following formula: in which R1, R2, R5, R6, R7, R31, u, and X are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: GrantFiled: January 21, 2010Date of Patent: April 19, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20110071155Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof: wherein: one of Z1 and Z2 is CH or N and the other is CH; L is selected from: —CH2—CH?CH—, —CH?CH—CH2—, —(CH2)p— where p is 2, 3 or 4, —CH2—CH2—O—, —O—CH2—CH2—, —CH2—CH2—NH—, —HN—CH2—CH2—, —C(O)—CH?CH—, —CH?CH—C(O)—, —CH2—C?C— or —C?C—CH2—; U represents a cyclic group; m is 0 or 1, n is independently 0 or 1; and substituent(s) R5 and R6 are independently selected from: halo, CF3, OCF3, C1-3 alkyl, C1-3 alkoxy, nitro and cyano, pharmaceurtical compositions comprising them, their use in therapy especially against tuberculosis, and methods of preparing them.Type: ApplicationFiled: May 20, 2009Publication date: March 24, 2011Inventors: Carlos Alemparte-Gallardo, David Barros-Aguirre, Monica Cacho-Izquierdo, Jose Maria Fiandor Roman, Modesto Jesus Remuinan-Blanco
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Publication number: 20110071136Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These tricyclic compounds and compositions containing them are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, pathogenic infections, and certain immunological disorders.Type: ApplicationFiled: September 16, 2010Publication date: March 24, 2011Applicant: CYLENE PHARMACEUTICALS, INCInventors: Mustapha HADDACH, Fabrice PIERRE
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Publication number: 20110034473Abstract: A novel co-crystal of N?-(7-fluoropyrrolo[1,2a]quinoxalin-4-yl)pyrazine-2-carbohydrazide with oxalic acid is disclosed. The disclosed oxalic acid co-crystal demonstrates cancer cell growth inhibition and is more bioavailable than the corresponding free base when administered as a suspension.Type: ApplicationFiled: April 8, 2009Publication date: February 10, 2011Applicant: NOVELIX PHARMACEUTICALS, INC.Inventors: Victor J. Bauer, Mike H. O'Neill, Barbara J. Kidon, Burkhard Jansen
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Publication number: 20110021425Abstract: The present invention relates to the use of novel compounds of Formulae I-II, wherein the variables R, X1, X2, X3, Y1, Y2, Y3, Z1, and Z2 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: June 29, 2010Publication date: January 27, 2011Inventor: Roland Joseph Billedeau
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Publication number: 20110003802Abstract: The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.Type: ApplicationFiled: July 6, 2010Publication date: January 6, 2011Applicant: Elan Pharmaceuticals, Inc.Inventors: Simeon Bowers, Albert W. Garofalo, Roy K. Hom, Andrei W. Konradi, Matthew N. Mattson, Martin L. Neitzel, Christopher M. Semko, Anh P. Truong, Jing Wu, Ying-zi Xu
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Patent number: 7855206Abstract: The present invention is directed to novel substituted tricyclic heteroaromatic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 9, 2007Date of Patent: December 21, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Hong Dong
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Publication number: 20100298287Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: ApplicationFiled: January 21, 2009Publication date: November 25, 2010Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Publication number: 20100249142Abstract: Imidazo[1,2-a]quinoxaline compounds for the treatment of cancers as well as pharmaceutical compositions that include these compounds and their uses in therapy.Type: ApplicationFiled: October 3, 2008Publication date: September 30, 2010Inventors: Carine Deleuze-Masquefa, Georges Moarbess, Pierre-Antoine Bonnet, Frédéric Pinguet, Ali Bazarbachi, Francoise Bressolle