Tricyclo Ring System Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.03)
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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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Patent number: 8343957Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: November 29, 2010Date of Patent: January 1, 2013Assignee: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Varsha Gupta
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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: 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: 8299081Abstract: A method for treating drug-resistant cancer, includes: administering to a patient in need thereof, a compound of formula I, a tautomer of the compound, a salt of the compound, a salt of the tautomer, a mixture thereof, or a pharmaceutical composition comprising the compound, the tautomer, the salt of the compound, the salt of the tautomer, or the mixture, wherein the patient is a cancer patient with drug-resistant cancer, wherein the compound of Formula I is as defined in the application.Type: GrantFiled: May 10, 2006Date of Patent: October 30, 2012Assignee: Novartis AGInventors: Glenn C. Michelson, Vivien W. Chan, Carla C. Heise, Marion Wiesmann, Timothy D. Dawes
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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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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: 20120225856Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: May 21, 2012Publication date: September 6, 2012Applicant: Corcept Therapeutics, Inc.Inventors: Robin D. Clark, Nicholas C. Ray, Paul M. Blaney, Christopher A. Hurley, Karen Williams
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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: 20120208792Abstract: 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 Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.Type: ApplicationFiled: December 8, 2011Publication date: August 16, 2012Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Peter C. Chua, Mustapha Haddach, Johnny Y. Nagasawa, Fabrice Pierre, Jeffrey P. Whitten
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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: 20120207751Abstract: The invention relates to a combination comprising compounds of formula (I) and one or more other antiproliferative compounds, hormones or radiation, pharmaceutical preparations comprising the combination thereof, and the application thereof in a process for the treatment of tumors.Type: ApplicationFiled: April 23, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
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Publication number: 20120202801Abstract: Methods for treating breast cancer involving the administration of a compound that selectively inhibits pathological production of human vascular endothelial growth factor (VEGF) are described. The compound can be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: August 9, 2012Inventors: Liangxian Cao, Thomas W. Davis, Samit Hirawat, Harry H. Miao, Langdon Miller, Charles M. Romfo, Marla L. Weetall
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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: 20120190676Abstract: The present invention provides methods and compositions for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR. The invention also provides methods and compositions for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR and modulators of the unfolded protein response.Type: ApplicationFiled: July 23, 2010Publication date: July 26, 2012Inventors: Nathaniel Moorman, Thomas Shenk
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Publication number: 20120178707Abstract: Methods for treating prostate cancer involving the administration of a compound that selectively inhibits pathological production of human vascular endothelial growth factor (VEGF) are described. Methods for treating benign prostatic hyperplasia involving the administration of a compound that selectively inhibits pathological production of human VEGF are also described. The compound may be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: July 12, 2012Inventors: Liangxian Cao, Thomas W. Davis, Samit Hirawat, Harry H. Miao, Langdon Miller, Charles M. Romfo, Marla L. Weetall
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Publication number: 20120157401Abstract: Methods for treating neurofibromatosis involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: June 21, 2012Inventors: Liangxian Cao, Thomas W. Davis, Harry H. Miao, Langdon Miller, Marla Weetall
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Publication number: 20120157460Abstract: The present invention relates to tetrahydro-azacarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.Type: ApplicationFiled: December 20, 2011Publication date: June 21, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Matthew D. SURMAN, Peter R. GUZZO, Emily FREEMAN, Alan J. HENDERSON
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Publication number: 20120157402Abstract: Methods for treating brain tumors involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: June 21, 2012Inventors: Liangxian Cao, Thomas W. Davis, Samit Hirawat, Harry H. Miao, langdon Miller, Marla Weetall
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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: 20120157400Abstract: Methods for treating Kaposi's sarcoma involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: June 21, 2012Inventors: Liangxian Cao, Thomas W. Davis, Samit Hirawat, Harry H. Miao, Langdon Miller, Marla L. Weetall
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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: 20120129841Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and compositions, and methods for the administration and use of those compounds. provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing serum, plasma, and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention.Type: ApplicationFiled: October 17, 2011Publication date: May 24, 2012Inventors: Liangxian Cao, Samit Hirawat, Langdon Miller, Thomas Davis, Marla L. Weetall
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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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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: 20120101065Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.Type: ApplicationFiled: December 22, 2011Publication date: April 26, 2012Applicant: Pharmacyclics, Inc.Inventors: Orion D. Jankowski, James T. Palmer, Lee Honigberg
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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: 20120093917Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical inhibitors of DNA repair proteins (Metnase) and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols.Type: ApplicationFiled: March 31, 2010Publication date: April 19, 2012Inventors: Robert Hromas, Andrei Leitao, Tudor I. Oprea, Larry A. Sklar, Elizabeth A. Williamson, Justin Wray
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Publication number: 20120083470Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.Type: ApplicationFiled: October 5, 2011Publication date: April 5, 2012Applicant: Pharmacyclics, Inc.Inventors: Orion D. Jankowski, James T. Palmer, Lee Honigberg
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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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Patent number: 8138191Abstract: 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: GrantFiled: July 17, 2009Date of Patent: March 20, 2012Assignee: Critical Outcome Technologies Inc.Inventor: Wayne R. Danter
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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: 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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Publication number: 20120022056Abstract: Compounds of formula (I) wherein R1, R2, X, A, Y, B, Z1, Q, p, r and s are defined in the specification for treating inter alia psychotic disorders, depressive disorders, anxiety disorders and sexual dysfunctions.Type: ApplicationFiled: August 29, 2005Publication date: January 26, 2012Inventors: Jonathan Bentley, Markus Bergauer, Babara Bertani, Matteo Biagetti, Manuela Borriello, Steven Mark Bromidge, Massimo Gianotti, Enrica Granci, Colin Philip Leslie, Alessandra Pasquarello, Valeria Zucchelli
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Publication number: 20120010193Abstract: Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.Type: ApplicationFiled: March 8, 2010Publication date: January 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
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Publication number: 20120004218Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein A1 to A3 and R1 to R10 have the significance given in claim 1, can be used as a medicament. These compounds are useful in the treatment or prophylaxis of diseases that are related to AMPK regulation, such as obesity, dyslipidemia, hyperglycemia, type 1 or type 2 diabetes and cancers.Type: ApplicationFiled: June 27, 2011Publication date: January 5, 2012Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Yongfu Liu, Hongying Yun, Mingwei Zhou
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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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Publication number: 20110318321Abstract: The present invention relates to a controlled release pharmaceutical or food formulation comprising at least one active pharmaceutical or food ingredient dispersed in a mixture of a glycogen with a polysaccharide, and the process for its preparation. The invention also relates to a slow release system represented by a mixture of a glycogen with a polysaccharide, and its use for the preparation of slow release pharmaceutical or food formulations.Type: ApplicationFiled: January 8, 2010Publication date: December 29, 2011Applicant: AZIENDE CHIM.RIUN.ANG.FRANC.A.C.R.A.F. S.p.A.Inventors: Stefano Selva, Leonardo Marchitto, Giovanni Battista Ciottoli, Lorella Ragni, Vincenzo Russo, Elisa Liberati
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Publication number: 20110319405Abstract: Embodiments are related to new uses for selective active-site mTOR inhibitors in treating or preventing pulmonary fibrosis in diffuse parenchymal lung disease (DPLD) patients, such as a DPLD of environmental cause, a collagen vascular disease (e.g., scleroderma and rheumatoid arthritis), an idiopathic interstitial pneumonia (e.g., idiopathic pulmonary fibrosis and nonspecific interstitial pneumonia), and sarcoidosis.Type: ApplicationFiled: June 28, 2011Publication date: December 29, 2011Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Glenn D. Rosen, Wen-Teh Chang