Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Isoquinoline Ring System By Nonionic Bonding Patents (Class 546/146)
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Patent number: 8648067Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.Type: GrantFiled: December 22, 2011Date of Patent: February 11, 2014Assignees: Cephalon, Inc., Teva SanteInventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allison L. Zulli, Christophe Yue
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Publication number: 20140038821Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: October 7, 2013Publication date: February 6, 2014Applicant: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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Publication number: 20140031387Abstract: Methods of preparation and purification of a compound of Formula I, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed.Type: ApplicationFiled: July 25, 2013Publication date: January 30, 2014Applicant: SARcode Bioscience Inc.Inventors: James Robert Zeller, Sripathy Venkatraman, Elisabeth C. A. Brot, Subashree Iyer, Michael Hall
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Publication number: 20140018356Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: April 4, 2013Publication date: January 16, 2014Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Publication number: 20140005382Abstract: There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action: wherein Ring A represents a partially saturated heteroaryl group, an aryl group or a heteroaryl group, RB represents a C4-18 alkyl group, a C3-8 cycloalkyl group, a partially saturated aryl group, an aryl group, or the following formula (II): wherein V represents the formula —CR11R12—, —CO—, —CO—O—, or —CO—NH—, W represents a single bond or a C1-3 alkylene group, and Ring B represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a partially saturated heteroaryl group, a saturated heterocyclyl group, an aryl group, or a heteroaryl group, Y represents a nitrogen atom or the formula N+(RF), RF represents a C1-4 alkyl group, and m and n, which may be the same or different, each represent an integer of 0 or 1.Type: ApplicationFiled: March 14, 2012Publication date: January 2, 2014Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Tsuyoshi Busujima, Takahiro Oi, Hiroaki Tanaka, Yoshihisa Shirasaki, Kanako Iwakiri, Nagaaki Sato, Shigeru Tokita
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Publication number: 20140004243Abstract: The present invention provides a compound having a salty taste enhance activity, and a salty taste enhancer containing the compound, and the like. The present invention relates to a salty taste enhancer for a food or drink, which contains a compound represented by the following formula: wherein each symbol is as defined in the specification, or an edible salt thereof.Type: ApplicationFiled: September 6, 2013Publication date: January 2, 2014Applicant: AJINOMOTO CO., INC.Inventors: Yuki TAHARA, Yusuke Amino, Takami Maekawa, Yuzuru Eto, Takashi Miyaki, Wakana Saikawa, Yuko Kai, Yutaka Ishiwatari
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Patent number: 8598364Abstract: The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.Type: GrantFiled: March 12, 2008Date of Patent: December 3, 2013Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Lin Cheng, Tacey X. Viegas, Xuyuan Gu, Franco J. Duarte, Wen Zhang
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Publication number: 20130310419Abstract: The present invention is related to pyrrole derivatives of formula I as the modulators of nicotinic acetylcholine receptors particularly the ?7 subtype. The invention includes pyrrole derivatives, analogues, their prodrugs, their isotopes, their metabolites, pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them. Owing to the modulatory activity of the pyrrole derivatives on the nicotinic acetylcholine receptors, the invention finds application in the prophylaxis and therapy of disorders encompassing the involvement of cholinergic transmission in the central and peripheral nervous system.Type: ApplicationFiled: January 31, 2012Publication date: November 21, 2013Applicant: LUPIN LIMITEDInventors: Neelima Sinha, Gourhari Jana, Navnath Popat Karche, Shridhar Keshav Adurkar, Girish Dhanraj Hatnapure, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20130296320Abstract: Provided is a novel bicyclic compound which has an HSP90 inhibitory effect and a carcinostatic effect. Also provided is a pharmaceutical agent which is based on the HSP90 inhibitory effect and is useful in the prevention and/or treatment of a disease involving HSP90, particularly, cancer. The present invention provides a compound represented by the following general formula (I) or a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are the same or different and each represent C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are the same or different and each represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.; R4 represents a hydrogen atom, —CO—R6, —N(R7)(R8) etc.Type: ApplicationFiled: January 6, 2012Publication date: November 7, 2013Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
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Patent number: 8575193Abstract: Compounds of a certain formula (I) wherein R1, R2, R3, X, Y, r, s, t, u and v have the meanings as defined in the specification, and the salts, solvates and hydrates thereof are novel effective HDAC 6 inhibitors.Type: GrantFiled: March 12, 2009Date of Patent: November 5, 2013Assignee: 4SC AGInventors: Thomas Maier, Christian Hesslinger, Barbara Beckers
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Publication number: 20130289280Abstract: Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided.Type: ApplicationFiled: May 7, 2013Publication date: October 31, 2013Applicants: TRANSFORM PHARMACEUTICALS, INC., UNIVERSITY OF SOUTH FLORIDAInventors: University of South Florida, Transform Pharmaceuticals, Inc.
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Patent number: 8569505Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to ?-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.Type: GrantFiled: January 22, 2010Date of Patent: October 29, 2013Assignee: Janssen Pharmaceutica, NVInventors: Ellen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
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Patent number: 8563578Abstract: HIV-protease inhibitors, particularly saquinavir, showed strong anticancer activity but numerous side effects limited its application. In order to overcome its toxicity original compounds were modified by covalent attachment of NO. The efficacy of parental and NO-modified drug was compared in vitro and in vivo. Anticancer activities of NO-modified saquinavir (Saq-NO) was monitored in vitro using assay for cell viability, proliferation, necrotic, autophagic and apoptotic cell death, differentiation, expression of intracellular molecules such as cyclin D3, p53 and Akt. Antitumor properties and toxicity of the compound was estimated in vivo. Saq-NO abrogated the viability of large spectrum of human and rodent tumor cell lines with IC50 significantly lower than parental drug and expressed strong antimelanoma action in vivo. In contrast to saquinavir, there was no detectable toxicity against primary cells in vitro and in vivo.Type: GrantFiled: July 30, 2009Date of Patent: October 22, 2013Assignee: Onconox APSInventors: Ferdinando Nicoletti, Yousef Al-Abed, Gianni Garotta
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Publication number: 20130252940Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: May 7, 2013Publication date: September 26, 2013Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-ming Chan, Jeff Chen, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
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Publication number: 20130245008Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.Type: ApplicationFiled: November 18, 2011Publication date: September 19, 2013Applicant: SANOFIInventor: Alain Pellet
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Publication number: 20130245025Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 3, 2013Publication date: September 19, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Patent number: 8530469Abstract: The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.Type: GrantFiled: October 12, 2011Date of Patent: September 10, 2013Assignee: Astex Therapeutics Ltd.Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford, Maria Grazia Carr, Robert Downham, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
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Patent number: 8518972Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: February 10, 2011Date of Patent: August 27, 2013Assignee: Celgene CorporationInventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
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Publication number: 20130210859Abstract: A compound represented by the general formula (M): (wherein R1 represents a substituted or unsubstituted aromatic heterocyclic group, R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 3 carbon atoms, OR3, N(R3)2, C(?O)OR3 or C(?O)N(R3)2, R3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an acyl group having 1 to 4 carbon atoms, R4 represents a hydrogen atom, an oxygen atom or OR5, and R5 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 1 to 3 carbon atoms); or a pharmaceutically acceptable salt thereof is a cortistatin A analog which is useful as an active ingredient of medicaments for cancer prevention or treatment in that the analog can be mass-produced by chemical synthesis due to its simple chemical structure and retains the same biological activities as those of cortistatin A.Type: ApplicationFiled: September 16, 2011Publication date: August 15, 2013Inventors: Motomasa Kobayashi, Naoyuki Kotoku, Masayoshi Arai, Satoru Tamura
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Publication number: 20130203709Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDAInventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
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Publication number: 20130196996Abstract: One embodiment provides a method, comprising treating or preventing at least one disease selected from the group consisting of bladder cancer, weight loss accompanying bladder cancer, bone pain accompanying bladder cancer, bladder cancer carcinoma in-situ (CIS), TA stage bladder cancer, T1 stage bladder cancer, T2 stage bladder cancer, T3 stage bladder cancer, T4 stage bladder cancer, lymph node metastasis therefrom, solid organ metastasis therefrom, bony metastasis therefrom, cachexia/anorexia associated with bladder cancer, generalized wasting syndrome associated with bladder cancer, or a combination thereof, by administering to a subject in need thereof one or more compounds described herein, prodrug thereof, salt thereof, or a combination thereof.Type: ApplicationFiled: January 19, 2011Publication date: August 1, 2013Applicant: CPSI STOCKHOLDER TRUSTInventors: John Arthur Taylor, III, Thais Sielecki-Dzurdz
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Publication number: 20130184258Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: October 26, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Patent number: 8481532Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: GrantFiled: July 9, 2009Date of Patent: July 9, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20130172384Abstract: This invention relates to the use of triazolone and triazolethione derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones and triazolethiones in the treatment of cancer.Type: ApplicationFiled: September 15, 2011Publication date: July 4, 2013Inventors: Nicholas D. Adams, Christopher Joseph Aquino, Jonathan M. Ghergurovich, David Lee Musso, Cynthia A. Parrish
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Publication number: 20130172553Abstract: Processes for the chiral syntheses of isoxazolines and intermediates are described. Compounds prepared thereby, and methods of using the compounds are also described.Type: ApplicationFiled: November 26, 2010Publication date: July 4, 2013Applicant: CPSI STOCKHOLDER TRUSTInventors: Thais Sielecki-Dzurdz, James Pruitt
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Patent number: 8476298Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: GrantFiled: May 24, 2007Date of Patent: July 2, 2013Assignee: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrisson B. Mac, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wie Xu
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Publication number: 20130157996Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: June 21, 2012Publication date: June 20, 2013Applicant: Amgen Inc.Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
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Publication number: 20130158072Abstract: Kappa opioid recep-tor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor, such as heroin or cocaine addictions.Type: ApplicationFiled: January 19, 2010Publication date: June 20, 2013Applicant: Research Triangle InstituteInventors: Frank Ivy Carroll, James B. Thomas, S. Wayne Mascarella
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Patent number: 8466172Abstract: The present invention relates to methods of stabilizing the alpha subunit of hypoxia inducible factor (HIF). The invention further relates to methods of preventing, pretreating, or treating conditions associated with HIF, including ischemic and hypoxic conditions. Compounds for use in these methods are also provided.Type: GrantFiled: December 2, 2010Date of Patent: June 18, 2013Assignee: FibroGen, Inc.Inventors: Volkmar Guenzler-Pukall, Thomas B. Neff, Qingjian Wang, Michael P. Arend, Lee A. Flippin, Alex Melekhov
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Publication number: 20130150585Abstract: Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.Type: ApplicationFiled: December 13, 2012Publication date: June 13, 2013Applicant: SARCODE BIOSCIENCE, INC.Inventor: SARcode Bioscience, Inc.
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Patent number: 8461329Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.Type: GrantFiled: December 25, 2009Date of Patent: June 11, 2013Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Tetsuo Takayama, Hajime Asanuma, Daisuke Wakasugi, Rie Nishikawa, Yoshinori Sekiguchi, Madoka Kawamura, Naoya Ono, Tetsuya Yabuuchi, Takahiro Oi, Yusuke Oka, Shoichi Kuroda, Fumito Uneuchi, Takeshi Koami
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Patent number: 8461189Abstract: The present invention relates to a novel class of pyridyl and pyrimidinyl derivatives. The pyridyl and pyrimidinyl compounds can be used to treat cancer. The pyridyl and pyrimidinyl compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: June 24, 2008Date of Patent: June 11, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Richard W. Heidebrecht, Jr., Thomas A. Miller, Matthew G. Stanton, David J. Witter
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Patent number: 8455514Abstract: 6- and 7-amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6- and 7-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.Type: GrantFiled: January 17, 2008Date of Patent: June 4, 2013Assignee: Aerie Pharmaceuticals, Inc.Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Geoffrey Richard Heintzelman, Susan M. Royalty
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Patent number: 8455647Abstract: 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.Type: GrantFiled: September 12, 2011Date of Patent: June 4, 2013Assignee: Aerie Pharmaceuticals, Inc.Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Geoffrey Richard Heintzelman, Susan M. Royalty
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Patent number: 8455513Abstract: 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.Type: GrantFiled: January 10, 2007Date of Patent: June 4, 2013Assignee: Aerie Pharmaceuticals, Inc.Inventors: Mitchell A. deLong, Susan M. Royalty, Jill Marie Sturdivant, Geoffrey Richard Heintzelman
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Patent number: 8455520Abstract: Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: July 11, 2008Date of Patent: June 4, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Steven L. Colletti, Hong Shen, Fa-Xiang Ding
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Publication number: 20130137684Abstract: The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin D2 synthase (H-PGDS), to compositions containing them and to their use in treating or preventing conditions and diseases associated with H-PGDS, such as allergies and inflammation.Type: ApplicationFiled: June 1, 2011Publication date: May 30, 2013Applicant: THE UNIVERSITY OF QUEENSLANDInventors: Mark Leslie Smythe, Jack Urquhart Flanagan
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Publication number: 20130131321Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; aType: ApplicationFiled: August 3, 2011Publication date: May 23, 2013Applicant: GRAFFINITY PHARMACEUTICALS GMBHInventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
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Publication number: 20130131018Abstract: The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.Type: ApplicationFiled: June 1, 2011Publication date: May 23, 2013Applicant: Exonhit S.A.Inventors: Bertrand Leblond, Thierry Taverne, Eric Beausoleil, Cédric Chauvignac, Anne-Sophie Casagrande, Laurent Desire
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Publication number: 20130123242Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
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Patent number: 8431704Abstract: The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I).Type: GrantFiled: April 21, 2009Date of Patent: April 30, 2013Assignee: Janssen Pharmaceutica NVInventors: Christopher John Love, Joseph Elisabeth Leenaerts, Ludwig Paul Cooymans, Donald Alec Lebsack, Bryan James Branstetter, Jason Christopher Rech, Elizabeth Ann Gleason, Jennifer Diane Venable, Danielle Wiener, Deborah Margaret Smith, James Guy Breitenbucher
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Patent number: 8420818Abstract: The present invention relates to a novel process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R2, R3 and R4 are each independently selected from the group consisting of hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy and lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by a group consisting of lower alkoxycarbonyl, aryl and heterocyclyl, and the pharmaceutically acceptable salts thereof. The pyrido[2,1-a]isoquinoline derivatives of the formula I are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.Type: GrantFiled: October 17, 2011Date of Patent: April 16, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Stefan Abrecht, Jean-Michel Adam, Alec Fettes
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Patent number: 8420668Abstract: The present invention provides a compound of the formula (I) or a pharmaceutically acceptable salt thereof:Type: GrantFiled: November 27, 2009Date of Patent: April 16, 2013Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Kazuo Hattori, Takehiro Okada, Osamu Kondoh, Toshiyuki Tsukaguchi, Masaki Shibata, Satoshi Tanida
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Publication number: 20130072494Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: ApplicationFiled: September 14, 2012Publication date: March 21, 2013Inventors: Hing L. SHAM, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
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Publication number: 20130065882Abstract: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxyType: ApplicationFiled: October 3, 2012Publication date: March 14, 2013Inventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
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Publication number: 20130059883Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.Type: ApplicationFiled: January 13, 2011Publication date: March 7, 2013Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
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PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE
Publication number: 20130059839Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.Type: ApplicationFiled: April 18, 2011Publication date: March 7, 2013Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.Inventors: Nicholas J. Lawrence, Roberta Pireddu, Said M. Sebti -
Patent number: 8389553Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: June 24, 2008Date of Patent: March 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Paul Harrington, Solomon Kattar, Thomas A. Miller, Matthew G. Stanton, Paul Tempest, David J. Witter
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Publication number: 20130053382Abstract: The instant invention provides for compounds that inhibit PDK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: April 28, 2011Publication date: February 28, 2013Inventors: Sunil Paliwal, Matthew Paul Rainka, Ang Li, May Xiaowu Jiang, Hon-chung Tsui, Ronald J. Doll