The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/361)
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Patent number: 8367654Abstract: The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.Type: GrantFiled: May 7, 2010Date of Patent: February 5, 2013Assignee: Tetraphase Pharmaceuticals, Inc.Inventors: Roger B. Clark, Minsheng He, Louis Plamondon, Xiao-Yi Xiao, Magnus P. Rönn
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Publication number: 20130023521Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.Type: ApplicationFiled: January 17, 2011Publication date: January 24, 2013Applicant: HYBRIGENICS SAInventors: Roman Lopez, Frederic Colland
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Publication number: 20130012505Abstract: The present invention relates to benzonaphthyridinamines of the formula (I) as autotaxin inhibitors and to the use thereof in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in which the inhibition, regulation and/or modulation of phosphodiesterase or lysophospholipase autotaxin plays a role, in particular of various types of cancer and autoimmune and inflammatory diseases.Type: ApplicationFiled: February 28, 2011Publication date: January 10, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
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Publication number: 20130004458Abstract: Chemical compounds that disrupt retroviral assembly and maturation are presented herein. More particularly, this disclosure provides small molecule compounds that disrupt the formation and maturation of virus particles and methods of using such small molecules to treat HIV-1 infection.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: NEW YORK BLOOD CENTER, INC.Inventors: Asim Kumar Debnath, Hongtao Zhang, Francesca Curreli
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Publication number: 20130005675Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji OTSUBO, Takahito YAMAUCHI, Yuji OCHI
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Publication number: 20120329785Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases.Type: ApplicationFiled: April 23, 2012Publication date: December 27, 2012Applicant: Origenis GmbhInventors: Michael Thormann, Andreas Treml, Michael Almstetter, Roland Koestler, Nasser Yehia
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Patent number: 8338411Abstract: The present invention relates to the adenosine A3 receptor ligands of the general formula (I), within them favourably to the antagonists, to their salts, solvates, N-oxides and isomers, to the pharmaceutical compositions containing the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the use of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the preparation of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, as well as to the new intermediates of the general formula (II), (VI), (XI), (XII) and (XV), and to the preparation thereof.Type: GrantFiled: December 4, 2009Date of Patent: December 25, 2012Assignee: SanofiInventors: Edit Susan, Kinga Boer, Zoltan Kapui, Geza Timari, Sandor Batori, Zoltan Szlavik, Endre Mikus, Judit Vargane Szeredi, Michel Finet, Katalin Urban Szabo, Tibor Szabo
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Patent number: 8338408Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: GrantFiled: October 27, 2008Date of Patent: December 25, 2012Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew A. Protter, Rajendra P. Jain, Sundeep Dugar, Sarvajit Chakravarty, Sergey O. Bachurin, Anatoly K. Ustinov, Bogdan K. Beznosko, Nadezhda Sergeevna Beznosko, legal representative, Elena F. Shevtsova, Vladimir V. Grigoriev
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Publication number: 20120323006Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: June 28, 2010Publication date: December 20, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlene Schuppli
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Publication number: 20120302563Abstract: Described herein are substituted norindenoisoquinoline compounds, and pharmaceutical compositions and formulations comprising the norindenoisoquinoline compounds. Also described herein are methods for using the compounds for the treatment and/or prevention of topoisomerase mediated diseases, such as cancer.Type: ApplicationFiled: January 27, 2011Publication date: November 29, 2012Applicant: PURDUE RESEARCH FOUNDATIONInventors: Mark S. Cushman, Yunlong Song
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Publication number: 20120302580Abstract: Anti-infection levorotatory optically active compound (S-configuration) of prulifloxacin represented by the following formula (1) and preparation method thereof are disclosed. Said method utilizes levorotatory ulifloxacin as the raw material and the reaction is conducted in organic solvent in the presence of alkaline materials, wherein the reaction temperature is ?20° C.˜60° C. and the reaction time is 15 minutes to 24 hours.Type: ApplicationFiled: October 22, 2010Publication date: November 29, 2012Inventors: Jun Ying, Feng Peng, Yuping Wang, Suiwei An, Jinqiang Liang, Beimei Liang, Qingchun Ni, Cheng Luo
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Publication number: 20120295882Abstract: This application relates to tricyclic compounds of Formula I: including all stereoisomers, mixtures of stereoisomers, and salts thereof. This application also relates to compositions comprising compounds of Formula I and uses therefore.Type: ApplicationFiled: June 21, 2012Publication date: November 22, 2012Applicant: Cephalon, Inc.Inventors: Edward R. Bacon, Thomas R. Bailey, Derek D. Dunn, Greg A. Hostetler, Robert J. McHugh, George C. Morton, Gerard C. Rosse, Joseph M. Salvino, Babu G. Sundar, Rabindranath Tripathy
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Publication number: 20120277214Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: November 24, 2010Publication date: November 1, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
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Patent number: 8288387Abstract: The present invention provides the compounds of general formula 5 and 9 useful as potential antitumour agents against human cancer cell lines. The present invention further provides the process for preparation of napthalimide-benzimidazole hybrids of general formula 5 and 9, n-1-2, R=n-methylpiperazine or morpholine (Formula 9), wherein: n=2-3, m=2-3 and R=n-methylpiperazine or morpholine.Type: GrantFiled: March 3, 2009Date of Patent: October 16, 2012Assignee: Council of Scientific & Industrial ResearchInventors: Kamal Ahmed, Praveen Kumar Pogula
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Publication number: 20120252740Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.Type: ApplicationFiled: July 2, 2010Publication date: October 4, 2012Inventors: Alan Kozikowski, Kyle V. Butler, Jay H. Kalin
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Patent number: 8273760Abstract: Disclosed herein are indolo[3,2-c]quinoline compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein R and m are given the definitions as set forth in the Specification and Claims. These compounds can be used to inhibit both growth of cancer cells and activity of telomerase.Type: GrantFiled: August 31, 2009Date of Patent: September 25, 2012Assignee: Kaohsiung Medical UniversityInventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Jing-Jer Lin, Chih-Ming Lu
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Publication number: 20120231995Abstract: There is provided the use of compounds of formula I wherein R1, R2, R3 and X have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula I per se.Type: ApplicationFiled: May 17, 2012Publication date: September 13, 2012Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Petra Helga Beck, Marc Barry Brown, David Edward Clark, Anthony Coates, Hazel Joan Dyke, Yanmin Hu, Derek John Londesbrough, Keith Mills, Thomas David Pallin, Gary Patrick Reid, Gerlinda Stoddart
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Publication number: 20120220565Abstract: The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: August 26, 2011Publication date: August 30, 2012Applicant: Corcept Therapeutics, Inc.Inventors: Robin Clark, Tony Johnson, Hazel Hunt, Ian McDonald
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Publication number: 20120208809Abstract: The invention relates to novel 9H-pyrrolo[2,3-b:5,4-c?]dipyridine azacarbolines of formula (I), where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH alkyl, CONH cycloalkyl; CONH heterocycloalkyl; CON(alkyl)2; CON(alkyl)(heterocycloalkyl); CONHN(alkyl)2; C(O)heterocycloalkyl; Rs is H; Hal, OH; O-alkyl(C1-C10); NH2; N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NHC(O)R3a; N(alkyl(C1-C10)C(O)R3a; NHS(O2)R3a; N(alkyl)(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; Ra and Rs optionally form a cycle; R3a is selected from among Hal, CF3, C1-C10 alkyl; C3-C7 cycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; OH; O-alkyl(C1-C10); (C3-C7); heterocycloalkyl (C3-C7); NH2; NH-(alkyl(C1-C10) or cycloalkyl(C3-C7)); N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NH-(alkyl(C1-C10) or heterocycloalkyl(C3-C7)); N(alkyl(C1-C10) or heterocycloalkyl(C3-C7))2, as well as to the isomers anType: ApplicationFiled: November 30, 2009Publication date: August 16, 2012Applicant: SANOFIInventors: Didier Babin, Olivier Bedel, Thierry Gouyon, Serge Mignani, David Papin
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Publication number: 20120202763Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.Type: ApplicationFiled: May 27, 2010Publication date: August 9, 2012Applicant: PTC THERAPEUTICS, INCInventors: Neil Almstead, Tamil Arasu, Soongyu Choi, Liangxian Cao, Jeffrey Allen Campbelll, Donald Corson, Thomas W. Davis, Jason D. Graci, Zhengxian Gu, Peter Seong Woo Hwang, William Lennox, Harry H. Miao, Langdon Miller, Young-Choon Moon, Hongyan Qi, Christopher Trotta, Marla L. Weetall
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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: 20120196854Abstract: A pharmaceutical composition comprising as an active ingredient, an aromatic heterocyclic compound represented by the formula (I): [wherein Q1 represents CR2 (wherein R2 represents a hydrogen atom or the like) or the like; Q2 represents CR3 (wherein R3 represents a hydrogen atom or the like) or the like; Q3 represents a nitrogen atom or the like; R1 represents —C(?O)OR16 (wherein R16 represents a hydrogen atom or the like) or the like; R5 represents a hydrogen atom or the like; R6 represents optionally substituted cycloalkyl or the like; X and Y may be the same or different and each represent CH in which H may be substituted with a substituent or the like; and Z represents a nitrogen atom or the like] or the like is provided.Type: ApplicationFiled: October 6, 2010Publication date: August 2, 2012Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Chie Takada, Koji Saeki, Hirokazu Kawasaki, Miho Tagaya, Masato Komai, Toshihide Ikemura, Shinpei Yamaguchi, Kyoichiro Iida
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Publication number: 20120196845Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: October 1, 2010Publication date: August 2, 2012Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. Dipardo
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Publication number: 20120165522Abstract: Various 14-Nitro, 14-amino, and 14-substituted amino camptothecin derivatives are useful in the treatment of cancer and other hyperproliferative diseases. Various 14-nitro camptothecin derivatives are conveniently prepared by reacting a camptothecin derivative with fuming nitric acid, optionally employing acetic anhydride as a solvent.Type: ApplicationFiled: June 16, 2010Publication date: June 28, 2012Inventors: Xiaohong Cai, Jian-Xin Duan, Mark Matteucci, Yeyu Cao, Hailong Jiao
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PIPERAZINONE-SUBSTITUTED TETRAHYDRO-CARBOLINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USES THEREOF
Publication number: 20120157469Abstract: The present invention relates to piperazinone-substituted tetrahydro-carboline 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 -
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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Patent number: 8188277Abstract: The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein X1 represents a nitrogen atom or a group —CH?; R1 represents a group —Z—R6, wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group or the like, wherein R3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R4 represents an imidazolyl lower alkyl group or the like.Type: GrantFiled: August 3, 2005Date of Patent: May 29, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Tae Fukushima, Shuji Matsumura, Noriaki Takemura, Hideaki Satou, Nobuaki Ito, Takuya Shitsuta, Hironori Tsutsui, Michinori Tanaka, Keizo Kan, Hitoshi Nagao, Kenji Watanabe, Kuninori Tai, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Keisuke Miyajima, Satoshi Yamada, Yutaka Kojima, Koichi Yasumura, Naoto Ohi, Mitsuhiro Okuno, Kazuhisa Sugiyama, Kunihiko Kiyono, Takashi Suzuki, Seiji Akamatsu, Takeshi Kodama, Yasuo Yanagihara, Takumi Sumida
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Publication number: 20120122848Abstract: A novel (+)-3-hydroxymorphinan derivatives and a pharmaceutical composition comprising the same as an active ingredient, which are useful for preventing or treating a neurodegenerative disease, are provided.Type: ApplicationFiled: July 28, 2010Publication date: May 17, 2012Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Jong Yup Kim, Kwang-Seop Song, Jeongmin Kim, Kwang Woo Ahn, Yonggyu Kong
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Publication number: 20120121651Abstract: Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, and prodrugs thereof, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: January 26, 2012Publication date: May 17, 2012Inventors: David S. Hays, Michael E. Danielson, John F. Gerster, Shri Niwas, Ryan B. Prince, Tushar A. Kshirsagar, Philip D. Heppner, William H. Moser, Joan T. Moseman, Matthew R. Radmer, Maureen A. Kavanagh, Sarah A. Strong, Jason D. Bonk
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Patent number: 8173636Abstract: Disclosed herein are hydroxylthienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxylthienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxylthienoquinolone or related compound to an animal suffering from a microbial infection.Type: GrantFiled: April 5, 2010Date of Patent: May 8, 2012Assignee: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Milind Deshpande, Akihiro Hashimoto, Ha Young Kim, Edlaine Lucien, Godwin Pais, Michael Pucci, Qiuping Wang, Jason Allan Wiles, Avinash Phadke
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Publication number: 20120108569Abstract: The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.Type: ApplicationFiled: May 7, 2010Publication date: May 3, 2012Inventors: Roger B. Clark, Minsheng He, Louis Plamondon, Xiao-Yi Xiao, Magnus P. Rönn
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Patent number: 8168639Abstract: Novel heterocyclic compounds of formula I: A-B-D??Formula I or a pharmaceutically acceptable salt thereof, wherein: A is selected from the group consisting of a moiety having general Formula II and a moiety having general Formula III: B is a moiety selected from the group consisting of: D is a moiety selected from the group consisting of: ?which exhibit a dopamine receptor (preferably a D4 receptor) and/or a serotonine receptor (preferably 5HTA1 agonistic activity), processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with the dopaminergic and/or serotonergic systems (e.g., sexual disorders, dyskinesia, anxiety) are disclosed.Type: GrantFiled: September 24, 2007Date of Patent: May 1, 2012Assignee: ATIR Holding S.A.Inventor: Vladimir Kogan
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Publication number: 20120095016Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I in the manufacture of a medicament for the treatment of GABAA receptor associated disorders. The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: ApplicationFiled: October 11, 2011Publication date: April 19, 2012Applicant: Helicon Therapeutics, Inc.Inventors: Varsha Gupta, Joel Renick, Graeme Freestone, Alan P. Kaplan
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Publication number: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Publication number: 20120077820Abstract: The present invention is directed to methods of use of a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.Type: ApplicationFiled: December 2, 2011Publication date: March 29, 2012Applicant: CRITICAL OUTCOME TECHNOLOGIES INC.Inventors: Wayne R. Danter, Martyn Brown, Franck LePifre
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Publication number: 20120071463Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: November 29, 2011Publication date: March 22, 2012Inventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
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Publication number: 20120071493Abstract: The invention relates to novel substituted 8-sulfonyl-2,3,4,5-tetrahydro-1H-?-carbolines of the general formula 1 and their pharmaceutically acceptable salt—ligands exhibiting biological activity simultaneously towards alpha-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors, sigma receptors, norepinefrine receptors, serotonin receptors, to active components, pharmaceutical compositions, comprising as an active component novel ligands, to novel medicaments intended for treatment of conditions and diseases of central nervous system. In the general formula 1 R1 represents a substituent selected from hydrogen, optionally substituted C1-C3 alkyl or C1-C4 alkyloxycarbonyl; R2 represents a cyclic system substituent selected from hydrogen, optionally substituted C1-C3 alkyl, optionally substituted C2-C3 alkenyl or substituted sulfonyl; R3 represents optionally substituted aryl or substituted amino group.Type: ApplicationFiled: April 30, 2010Publication date: March 22, 2012Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Oleg Dmitrievich Mitkin, Volodymyr Mikhailovich Kysil
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Publication number: 20120058939Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: March 8, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, Mark HADDEN, Emily Elizabeth FREEMAN
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Patent number: 8119654Abstract: The present invention relates to Indenoisoquinolinone Analogs, compositions comprising an effective amount of an Indenoisoquinolinone Analog and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of an Indenoisoquinolinone Analog.Type: GrantFiled: February 28, 2008Date of Patent: February 21, 2012Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Duy-Phong Pham-Huu, Frederick Cohen, Xiaojing Wang
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Publication number: 20120040959Abstract: The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Applicant: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Jason Allan Wiles, Qiuping Wang, Akhiro Hashimoto, Edlaine Lucien, Godwin Clarence Gilroy Pais, Milind Deshpande, Michael John Pucci, Ha Young Kim
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Publication number: 20120034250Abstract: [Problem] The present invention provides a condensed pyrrolopyridine derivative which is useful as an active ingredient for a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases caused by undesirable cytokine signal transduction or diseases caused by abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied a compound having a JAK inhibitory action, and as a result, they have found that a condensed pyrrolopyridine derivative which is the compound of the present invention has an excellent JAK inhibitory action, and is therefore useful as an agent for preventing or treating diseases caused by undesirable cytokine signal transduction or diseases caused by abnormal cytokine signal transduction, thereby completing the present invention.Type: ApplicationFiled: April 13, 2010Publication date: February 9, 2012Applicant: Astellas Pharma Inc.Inventors: Shohei Shirakami, Yutaka Nakajima, Jun Maeda, Hiroaki Tominaga, Hiroaki Yamagishi, Takeshi Hondo, Masamichi Inami, Hiroki Morio, Takayuki Inoue, Tsuyoshi Mizutani, Hiroki Ishioka
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Publication number: 20120022060Abstract: Disclosed are dipyridyl-pyrrole derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.Type: ApplicationFiled: December 3, 2009Publication date: January 26, 2012Applicant: MERCK PATENT GMBHInventors: Bayard R. Huck, Amanda E. Sutton, Benny C. Askew, JR., Christopher Charles Victor Jones, Garry R. Smith, Nadia Brugger
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Patent number: 8088790Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: November 3, 2006Date of Patent: January 3, 2012Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
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Patent number: 8071587Abstract: The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: May 25, 2010Date of Patent: December 6, 2011Assignee: N. V. OrganonInventors: Hubert Jan Jozef Loozen, Cornelius Marius Timmers
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Patent number: 8071600Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: GrantFiled: August 31, 2006Date of Patent: December 6, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20110294799Abstract: The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: August 12, 2008Publication date: December 1, 2011Inventors: Samuel Hintermann, Konstanze Hurth, Joachim Nozulak, Marina Tintelnot-Blomley
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Publication number: 20110288091Abstract: The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.Type: ApplicationFiled: October 16, 2009Publication date: November 24, 2011Applicants: Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Jae Won Chang, Jianming Zhang, Carson C. Thoreen, Seong Woo Anthony Kang, David M. Sabatini, Qingsong Liu
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Publication number: 20110281862Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the description, to their pharmaceutical compositions and use thereof for the treatment of cancer expressing oncogenic ALK protein, particularly anaplastic large cell lymphoma (ALCL), diffuse large B cell lymphoma (DLBCL), inflammatory myofibroblastic tumours (IMT) and non-small cell lung cancer (NSCLC).Type: ApplicationFiled: August 27, 2009Publication date: November 17, 2011Applicants: Universita' Degli Studi di Milano - Bicocca, Universite' Claude Bernard de Lyon 1, Universite' de GeneveInventors: Carlo Gambacorti Passerini, Luca Mologni, Leonardo Scapozza, Shaheen Ahmed, Peter G. Goekjian, David Gueyrard, Florence Popowycz, Benoit Joseph, Cedric Schneider, Pierre Garcia
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Publication number: 20110269705Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.Type: ApplicationFiled: December 4, 2009Publication date: November 3, 2011Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi
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Publication number: 20110263581Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules.Type: ApplicationFiled: February 25, 2011Publication date: October 27, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Peter C. CHUA, Fabrice Pierre, Jeffrey P. Whitten