Quinoline Or Isoquinoline (including Hydrogenated) Patents (Class 544/363)
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Patent number: 8318769Abstract: Substituted sulfonamide compounds corresponding to formula I: processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment and/or inhibition of pain and other conditions at least partly mediated by the bradykinin 1 receptor.Type: GrantFiled: April 8, 2009Date of Patent: November 27, 2012Assignee: Gruenethal GmbHInventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Michael Franz-Martin Engels, Ruth Jostock, Tieno Germann, Jean De Vry, Klaus Schiene, Sabine Hees
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Publication number: 20120295919Abstract: Provided are opioid receptor antagonists represented by the formula (I) where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.Type: ApplicationFiled: October 12, 2010Publication date: November 22, 2012Applicant: RESEARCH TRIANGLE INSTITUTEInventors: Frank I. Carroll, Juan P. Cueva, James B. Thomas, S. Wayne Mascarella, Scott P. Runyon
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Publication number: 20120288855Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.Type: ApplicationFiled: July 26, 2012Publication date: November 15, 2012Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Jolene A. Bradford, Ching-Ying Cheung, Shih-Jung Huang, Patrick R. Pinson, Stephen T. Yue
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Publication number: 20120283242Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].Type: ApplicationFiled: January 28, 2011Publication date: November 8, 2012Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
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Publication number: 20120283256Abstract: The present invention relates to compounds having the following Formula (I) for use in the prevention and/or the treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs.Type: ApplicationFiled: December 16, 2010Publication date: November 8, 2012Inventors: Andre Delacourte, Patricia Melnyk, Stephane Burlet, Nicolas Lefur
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Publication number: 20120277434Abstract: A method of synthesizing a substituted or unsubstituted 4-amino-3-benzimidazolyl quinolinone compound includes reacting a first compound having the formula I with a second compound having the formula II in a suitable solvent in the presence of a sodium or potassium salt of a base.Type: ApplicationFiled: July 2, 2012Publication date: November 1, 2012Inventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy MacHajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus O. Okhamafe, Marc S. Tesconi
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Publication number: 20120277231Abstract: The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.Type: ApplicationFiled: October 16, 2010Publication date: November 1, 2012Inventors: Axel Ullrich, Robert Torku, Yixiang Zhang, György Kéri, László Örfi, István Szabadkai
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Patent number: 8299055Abstract: The present invention relates to a compound represented by the following formula (1): wherein D1, A1, D2, R1, D3, and R2 each have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKK? inhibiting activity and the like and is useful for the prevention and/or treatment of IKK?-associated diseases or symptoms and the like.Type: GrantFiled: October 1, 2009Date of Patent: October 30, 2012Assignee: Asahi Kasei Pharma CorporationInventors: Shunsuke Kaneko, Kenichiro Sato, Daisuke Shikanai, Rintaro Yamada, Katsuhiko Sakurada
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Publication number: 20120270858Abstract: The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis.Type: ApplicationFiled: June 9, 2010Publication date: October 25, 2012Applicant: CALIFORNIA CAPITAL EQUITY, LLCInventors: Chunlin Tao, Xiaowen Sun, Hongna Han, Lukasz Koroniak, Neil Desai
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Patent number: 8293747Abstract: The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease.Type: GrantFiled: July 17, 2008Date of Patent: October 23, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Panduranga Adulla P. Reddy, Lianyun Zhao, Praveen K. Tadikonda, Tzu Tshin Wong, Shuyi Tang, Luis E. Torres, David F. Cauble, Jr., Timothy J. Guzi, M. Arshad Siddiqui
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Patent number: 8293732Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.Type: GrantFiled: December 4, 2007Date of Patent: October 23, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Ismet Dorange, Magali Madeleine Simone Motte, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
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Publication number: 20120258971Abstract: This invention provides a novel therapeutic agent for chronic pain. The therapeutic agent for chronic pain comprises aripiprazole as an active ingredient.Type: ApplicationFiled: February 26, 2010Publication date: October 11, 2012Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Shin-Ichi Niwa, Shinichi Konno, Satoshi Kasahara, Hirobumi Mashiko, Koji Otani
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Publication number: 20120245176Abstract: A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, —CHF2 or —CH?CH2; V is —H, —CH3 or ?O; W is —NO2, —Cl, —Br, —CH2OH, or —CN; X is —Cl, —Br, —F, —CH3, —OCH3, or —CN; Y is —CH or —N; and Z is —CH or —N. This compound is useful in compositions for the prevention and treatment of influenza virus.Type: ApplicationFiled: September 23, 2011Publication date: September 27, 2012Inventors: Christopher W. Cianci, Samuel Gerritz, Sean Kim, David R. Langley, Guo Li, Bradley C. Pearce, Annapurna Pendri, Shuhao Shi, Weixu Zhai, Shirong Zhu
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Publication number: 20120245150Abstract: The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, B, m, n, W, and R2 are as defined in the disclosure; to the methods of preparing said derivatives, and to the therapeutic uses thereof.Type: ApplicationFiled: June 7, 2012Publication date: September 27, 2012Applicant: SANOFIInventors: Marco BARONI, Françoise BONO, Sandrine DELBARY-GOSSART, Valentina VERCESI
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Publication number: 20120245149Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyI)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.Type: ApplicationFiled: June 7, 2012Publication date: September 27, 2012Applicant: SANOFIInventors: Marco BARONI, Françoise BONO, Sandrine DELBARY-GOSSART, Valentina VERCESI
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Patent number: 8273733Abstract: The disclosure relates to tetrahydroisoquinoline sulfonamide compounds of formula I: wherein R1, R2, n and B are as defined in the disclosure, their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness.Type: GrantFiled: October 8, 2010Date of Patent: September 25, 2012Assignee: SanofiInventors: Juan Antonio Diaz Martin, Maria Dolores Jimenez Bargueno
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Publication number: 20120232088Abstract: This invention relates to piperazinedione compounds shown in the specification. These compounds are tyrosine kinase inhibitors and can be used to treat cancer.Type: ApplicationFiled: February 24, 2012Publication date: September 13, 2012Applicants: National Taiwan University, Taipei Medical UniversityInventors: Hui-Po Wang, Che-Ming Teng, Chun-Li Wang, Jih-hwa Guh, Shiow-Lin Pan, Yuan-Yi Wang, Jang-Feng Lian
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Publication number: 20120220587Abstract: Compounds of the formula (I), in which X1, X2, L, Y, R2, R3, R4, R5, R6, R7, R8, R9, R10 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.Type: ApplicationFiled: September 6, 2010Publication date: August 30, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Ulrich Emde, Hans Peter Buchstaller, Markus Klein, Christina Esdar, Joerg Bomke
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Publication number: 20120214990Abstract: A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Applicants: TAISHO PHARMACEUTICAL CO., LTD., TOYAMA CHEMICAL CO., LTD.Inventors: Taro KIYOTO, Tadashi Tanaka, Yasuhiro Tsutsui, Junichi Ando, Mai Motono, Yasuko Kawaguchi, Toshiya Noguchi, Yasunobu Ushiki, Fumihito Ushiyama, Hiroki Urabe
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Publication number: 20120214790Abstract: The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar1 and Ar2 are aryl or heteroaryl; V is nitrogen, or CR3; W1 is a single bond, —C(O)—, etc.; W2 is C1-alkylene; W3 is a single bond, methylene, —NH—, —CR4?CR5—, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R1a, R1b and R1c are each, same or different, hydrogen, hydroxyl, halogen, cyano, C1-6 alkyl, etc.; or pharmaceutically acceptable salts thereof are provided.Type: ApplicationFiled: March 11, 2011Publication date: August 23, 2012Inventors: Megumi Maruyama, Naoya Kinomura, Satoshi Nojima, Masahiro Takamura, Keisuke Kakiguchi, Hiroto Tatamidani
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Patent number: 8247420Abstract: The present invention provides novel quinolinone derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.Type: GrantFiled: May 21, 2008Date of Patent: August 21, 2012Assignee: Reviva Pharmaceuticals, Inc.Inventors: Laxminarayan Bhat, Prabhu P. Mohapatra, Seema Rani Bhat
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Publication number: 20120208798Abstract: Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: November 3, 2010Publication date: August 16, 2012Inventors: Emmanuel Hubert Demont, Neil Stuart Garton, Romain Luc Marie Gosmini, Thomas George Christopher Hayhow, Jonathan Seal, David Matthew Wilson, Michael David Woodrow
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Publication number: 20120208790Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.Type: ApplicationFiled: April 27, 2012Publication date: August 16, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
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Publication number: 20120208814Abstract: Tetrahydroquinoline compounds of formula (I) or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicted.Type: ApplicationFiled: November 3, 2010Publication date: August 16, 2012Inventors: Emmanuel Hubert Demont, Romain Luc Marie Gosmini
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Publication number: 20120208825Abstract: The present invention relates to non-hydrate crystalline forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts, solid pharmaceutical formulations containing the same and methods of use. The present invention also relates to crystalline hydrates of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-l-yl)-lH-benzimidazol-2-yl]-lH-quinolin-2-one lactic acid salts, pharmaceutical formulations containing the same and methods of use related thereto. The present invention further relates to crystalline solvates of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-l-yl)-lH-benzimidazol-2-yl]-lH-quinolin-2-one lactic acid salts.Type: ApplicationFiled: April 27, 2012Publication date: August 16, 2012Inventors: Augustus O. Okhamafe, Joyce Chou, Rampurna Gullapalli, Eric Harwood, David Ryckman, Shuguang Zhu, Xiao Shang
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Publication number: 20120202782Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).Type: ApplicationFiled: April 12, 2012Publication date: August 9, 2012Applicant: IRM LLCInventors: Badry Bursulaya, Dai Cheng, Jiqing Jiang, Donald S. Karanewsky, Yi Liu, Shifeng Pan, Yongqin Wan, Xia Wang, Yun Feng Xie, Yang Yang
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Patent number: 8236796Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle oType: GrantFiled: April 2, 2009Date of Patent: August 7, 2012Assignees: Albany Molecular Research, Inc., Bristol-Myers Squibb CompanyInventors: Bruce F. Molino, Shuang Liu, Peter R. Guzzo, James P. Beck
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Patent number: 8236947Abstract: Disclosed are quinoline compounds having affinity for the 5-HT6 receptor and having the formula: where R1, R2, R3, R4, R5, n, m, p and A are defined herein, and salts thereof, compositions containing these compounds and salts and processes for making and using the same.Type: GrantFiled: June 3, 2011Date of Patent: August 7, 2012Assignee: Glaxo Group LimitedInventors: Mahmood Ahmed, Christopher Norbert Johnson, Martin C Jones, Gregor James MacDonald, Stephen Frederick Moss, Mervyn Thompson, Charles Edward Wade, David R Witty
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Publication number: 20120195887Abstract: A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.Type: ApplicationFiled: February 1, 2012Publication date: August 2, 2012Applicant: CRITICAL OUTCOME TECHNOLOGIES INC.Inventor: Wayne R. Danter
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Publication number: 20120197013Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: April 9, 2012Publication date: August 2, 2012Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch
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Publication number: 20120184563Abstract: [Summary] An external preparation formulation superior in the transdermal absorbability has been desired as a new administration route of aripiprazole. Transdermal absorption of aripiprazole has been enabled for the first time by appropriately combining aripiprazole and an organic acid (particularly fatty acid with low lipophilicity). That is, it has been found that more superior transdermal absorbability can be achieved by forming a salt by using a compound showing lipophilicity within the range of ?1.5-2, such as fatty acid and the like. It has been further found that the transdermal absorbability is remarkable improved by appropriately selecting the solvent composition. As a result, since a new dosage form of aripiprazole other than oral preparation has been developed, a new transdermal absorption preparation of aripiprazole can be provided.Type: ApplicationFiled: June 17, 2010Publication date: July 19, 2012Applicant: MEDRX CO., LTD.Inventor: Noritaka Hanma
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Publication number: 20120184523Abstract: 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: March 22, 2012Publication date: July 19, 2012Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takbuchi, Yong Wang, Wei Xu
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Publication number: 20120178934Abstract: The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I), and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.Type: ApplicationFiled: September 16, 2010Publication date: July 12, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Sandrine Chambon, Laurence Clary, Marlene Schuppli
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Publication number: 20120178713Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion 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, including for example the treatment of pain.Type: ApplicationFiled: March 14, 2012Publication date: July 12, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Esther Martinborough, Lev T.D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
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Publication number: 20120172349Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: December 29, 2011Publication date: July 5, 2012Inventors: Francesco G. Salituro, Jeffrey Saunders, Shunqi Yan
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Publication number: 20120165324Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: December 29, 2011Publication date: June 28, 2012Inventors: Francesco G. Salituro, Jeffrey Saunders
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Publication number: 20120165321Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: ApplicationFiled: March 5, 2012Publication date: June 28, 2012Inventors: Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerrard Darcy, Carla A. Donatelli, Steven David Knight, Kenneth Allen Newlander, Lance Ridgers, Martha A. Sarpong, Stanley J. Schmidt
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Publication number: 20120157463Abstract: The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.Type: ApplicationFiled: August 31, 2010Publication date: June 21, 2012Applicant: PIERRE FABRE MEDICAMENTInventors: Pierre Sokoloff, Thierry Imbert, Jean-François Patoiseau, Jean-Pierre Rieu
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Patent number: 8202870Abstract: The invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, R3, Y1, Y2, m, n, W, X, B and Z are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseasesType: GrantFiled: March 23, 2006Date of Patent: June 19, 2012Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Hervé Geneste
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Publication number: 20120149713Abstract: An oral film comprising 7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one base or salts or hydrates thereof.Type: ApplicationFiled: March 25, 2010Publication date: June 14, 2012Applicant: HEXAL AGInventors: Andreas Krekeler, Nicole Buggele, Max Born, Sigrid Grundsteiner
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Patent number: 8198280Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: December 16, 2010Date of Patent: June 12, 2012Assignee: Merck Serono SAInventors: Dominique Swinnen, Jerome Gonzalez
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Publication number: 20120142635Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: February 8, 2012Publication date: June 7, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
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Patent number: 8193194Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.Type: GrantFiled: May 21, 2008Date of Patent: June 5, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
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Publication number: 20120132870Abstract: The present invention relates to indeno-fused naphthopyrans, and in particular indeno[2?,3?:3,4]naphtho[1,2-b]pyrans having certain groups bonded to the 3, 6, 7, 11, and 13 positions thereof. The indeno-fused naphthopyrans of the present invention have an ethylenically unsaturated group selected from (C1-C6 alkyl)acrylate and (C1-C6 alkyl)acrylamide, that is linked to the 11 position or 13 position thereof. The present invention also relates to photochromic articles and photochromic compositions containing such indeno-fused naphthopyrans.Type: ApplicationFiled: December 15, 2011Publication date: May 31, 2012Applicant: TRANSITIONS OPTICAL INC.Inventors: Wenjing Xiao, Barry Van Gemert
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Publication number: 20120135984Abstract: Provided are compounds, compositions, and methods for treating diseases and conditions wherein an inhibitor of a kinase, such as rho kinase (ROCK), and an inhibitor of one or more of the monoamine transporters, such as NET or SERT, act in concert to improve the condition.Type: ApplicationFiled: May 1, 2010Publication date: May 31, 2012Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty, Geoffrey Richard Heintzelman, Jeffrey D. Yingling, Casey Kopczynski
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Patent number: 8188087Abstract: The present invention relates to novel crystalline forms of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl)piperazin-1-yl]methanone phosphate and to pharmaceutical compositions containing said forms.Type: GrantFiled: April 24, 2007Date of Patent: May 29, 2012Assignee: Merck Patent GmbHInventors: Susan Marie Reutzel-Eden, Gregory Alan Stephenson
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Publication number: 20120129871Abstract: A crystalline form of (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one, which is useful in the treatment of a disease or disorder associated with the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively,Type: ApplicationFiled: November 17, 2011Publication date: May 24, 2012Applicant: NOVARTIS AGInventors: Joerg BERGHAUSEN, Haixia REN
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Patent number: 8183374Abstract: Compounds of general formula (Ia): in which R1, A1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.Type: GrantFiled: January 22, 2007Date of Patent: May 22, 2012Assignee: M's Science CorporationInventors: Connie L. Sun, Xiaoyuan Li
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Patent number: 8178526Abstract: 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 dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).Type: GrantFiled: June 12, 2008Date of Patent: May 15, 2012Assignee: IRM LLCInventors: Badry Bursulaya, Dai Cheng, Jiqing Jiang, Donald S. Karanewsky, Yi Liu, Shifeng Pan, Yongqin Wan, Xia Wang, Yun Feng Xie, Yang Yang
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Patent number: 8178668Abstract: 2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.Type: GrantFiled: February 4, 2009Date of Patent: May 15, 2012Assignee: OSI Pharmaceuticals, LLCInventors: Arno G. Steinig, Mark J. Mulvihill, Jing Wang, Douglas S. Werner, Qinghua Weng, Heather Coate, Xin Chen