Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 514/313)
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Publication number: 20120165352Abstract: 6-amino quinazoline or 3-cyano quinoline derivatives, preparation methods and pharmaceutical uses thereof are disclosed. Specifically, the present disclosure discloses novel 6-amino quinazoline or 3-cyano quinoline derivatives presented by general formula (I), or tautomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable salts thereof, or metabolites, metabolic precursors or prodrugs thereof, and their uses as treatment agents especially as protein kinase inhibitors, in which each substitutent group of general formula (I) is as defined in the specification.Type: ApplicationFiled: August 26, 2010Publication date: June 28, 2012Applicants: SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD., JIANGSU HENGRUI MEDICINE CO., LTD.Inventors: Peng Cho Tang, Xin Li, Bin Wang, Jun Wang, Lijun Chen
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Publication number: 20120165371Abstract: The present invention relates to spiro (tetracarbon) substituted compound of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.Type: ApplicationFiled: March 5, 2012Publication date: June 28, 2012Applicant: ADVENCHEN LABORATORIES, LLCInventor: Guoqing Paul CHEN
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Patent number: 8207195Abstract: This invention is directed to methods of preventing or treating neurological or neuropathic diseases or conditions associated with excessive inflammation, neurodegeneration, neuro-remodeling, and axonal/neurite retraction. Particularly, this invention relates to methods treating neurological or neuropathic diseases such as cerebral ischemia, stroke, neuropathic pain, spinal cord injury, Alzheimer's disease, and multiple sclerosis, using novel rho kinase inhibitor compounds. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel rho kinase inhibitor compound to treat the disease.Type: GrantFiled: June 26, 2009Date of Patent: June 26, 2012Assignee: Inspire Pharmaceuticals, Inc.Inventors: Tomas Navratil, John W. Lampe, Emilee H. Fulcher, Ward M. Peterson
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Publication number: 20120156244Abstract: Pharmaceutical compositions for the treatment of nasal congestion, wherein the pharmaceutical compositions comprise low concentrations of a super-selective subclass of selective ?-2 adrenergic receptor agonists. Methods of using the compositions for the treatment of nasal congestion, cerebrovascular disease or systemic conditions, and as delivery vehicles to deliver other active agents to treat systemic or cerebrovascular diseases or conditions.Type: ApplicationFiled: February 27, 2012Publication date: June 21, 2012Applicant: ALPHA SYNERGY DEVELOPMENT INC.Inventor: Gerald Horn
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Publication number: 20120156187Abstract: Methods and compositions for modulating blood-neural barrier (BNB) for the treatment of CNS conditions such as edema, and for increased drug delivery efficacy across the BNB. The present invention further relates to improved tPA treatment of ischemic cerebrovascular and related diseases in combination with antagonism of the PDGF signaling pathway. The inventive method and composition is particularly suitable for conjunctive therapy of ischemic stroke using tPA and an anti-PDGF-C antagonist or an anti-PDGFR-? antagonist.Type: ApplicationFiled: February 28, 2012Publication date: June 21, 2012Applicants: LUDWIG INSTITUTE FOR CANCER RESEARCH, THE REGENTS OF THE UNIVERSITY OF MICHIGAN, UNIVERSITY OF MARYLAND, BALTIMOREInventors: Ulf Eriksson, Daniel Lawrence, Enming Joe Su, Dudley Strickland, Manuel Yepes, Linda Fredriksson
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Publication number: 20120157493Abstract: “An indoloquinoline wherein the quarternary N-5 atom is a straight C(1-5) chain, a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring; the 10 position is N—R10, O, S, S?O, CH2, or C?O, where R10 is a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring. In one embodiment the quarternary N-5 atom is —CH3 and the 10 position is N—(CH2)5-Ph.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Applicant: FLORIDA A&M UNIVERSITYInventor: Seth Y. Ablordeppey
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Patent number: 8197848Abstract: A pharmaceutical composition comprises a solid amorphous dispersion of a cholesteryl ester transfer protein inhibitor and a concentration-enhancing polymer.Type: GrantFiled: April 30, 2007Date of Patent: June 12, 2012Assignee: Bend Research, Inc.Inventors: Marshall D. Crew, William J. Curatolo, Dwayne T. Friesen, Michael J. Gumkowski, Douglas A. Lorenz, James A. S. Nightingale, Roger B. Ruggeri, Ravi M. Shanker
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Patent number: 8198301Abstract: A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).Type: GrantFiled: May 26, 2010Date of Patent: June 12, 2012Inventor: Hesheng Zhang
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Publication number: 20120142731Abstract: Compounds, pharmaceutical compositions and methods of inhibiting viral infection in a mammal in need of same, are provided, which employ compounds of the formula wherein each X is independently H or an electrodonating group, each Y is independently H, alkyl of 1-4 carbon atoms, hydroxy, alkoxy or methylene and wherein Substituent Z is a di-or-tri akly amino, or alkyl di or tri amino, optionally substituted with a halogen moiety. This family of compounds, designated FGI-104 herein, inhibits viral infection therapeutically and prophylactically.Type: ApplicationFiled: October 30, 2008Publication date: June 7, 2012Applicant: Functional Genetics, Inc.Inventors: Michael Kinch, Michael Goldblatt
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Patent number: 8193218Abstract: The invention relates to a method of administering N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(quinoloylamino)-piperidines of the formula wherein Y is ?N— or ?N(O)—, R is OH when Y is ?N— and R is H when Y is ?N(O)— and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl, provided that when R is OH and Y is ?N— the ring A is not unsubstituted, for the treatment of disorders induced by substance P, such as: pain, migraines, anxiety, vomiting, schizophrenia, depression; motor disorders such as Parkinson's disease, inflammatory diseases such a rheumatoid arthritis, iritis and conjunctivitis, diseases of the respiratory organs such as asthma and chronic bronchitis, diseases of the gastrointestinal system such as ulcerative colitis and Crohn's disease, and hypertension.Type: GrantFiled: January 20, 2010Date of Patent: June 5, 2012Assignee: Novartis AGInventor: Siem Jacob Veenstra
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Publication number: 20120136026Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m and p have a value of 1; n and o have the same value which is 0 or 1; A is a covalent bond or a C1-8-alkylene group; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl group or a trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The present invention can be used in therapeutics.Type: ApplicationFiled: May 11, 2010Publication date: May 31, 2012Applicant: SANOFIInventors: Ahmed Abouabdellah, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
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Publication number: 20120136018Abstract: The present invention relates to 2-aminoquinolines of formula I wherein R1, R2 and R3 are as defined in the specification, as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.Type: ApplicationFiled: January 27, 2012Publication date: May 31, 2012Inventors: Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Patent number: 8188284Abstract: The present invention relates to compounds of formula (I) wherein A, R1, R2, R3, R4, and R5 are as described herein, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.Type: GrantFiled: February 27, 2009Date of Patent: May 29, 2012Assignee: Hoffman-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Publication number: 20120130144Abstract: In one aspect, the present invention provides a method of treating lung cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor. In another aspect, the present invention provides a method of treating non-small cell lung cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor.Type: ApplicationFiled: February 4, 2010Publication date: May 24, 2012Applicant: BiPar Sciences, Inc.Inventors: Barry M. Sherman, Charles Bradley, Valeria S. Ossovskaya
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Publication number: 20120129854Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the yield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: April 27, 2010Publication date: May 24, 2012Applicant: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
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Patent number: 8183380Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I where R1, R2, R3, R4, R5, R6, A, and n are as defined in the specification and claims, their use 5-HT5A receptor antagonists, their manufacture, and pharmaceutical compositions containing them.Type: GrantFiled: February 26, 2009Date of Patent: May 22, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Publication number: 20120122923Abstract: The invention concerns dual molecules corresponding to formula (I): in which: A represents a molecular residue with antimalarial activity of formula (IIa) or (IIIa) or a residue facilitating bioavailability; B represents a cycloalkyl group potentially substituted, or B represents a bi- or tricyclic group capable of being substituted, or B represents 2 cycloalkyl groups linked together through either a single bond or an alkylene chain; m and n represent independently of one another 0, 1 or 2; R5 represents a hydrogen atom, an alkyl, cycloalkyl or C1-3-alkylene-cycloakyl group; Z1 and Z2 represent an alkyl radical, the group Z1+Z2+Ci+Cj representing a mono- or polycyclic structure, with one of the Z1 or Z2 being able to represent a single bond; R1 and R2, identical or different, represent a hydrogen atom or a functional group capable of increasing hydrosolubility; Rx and Ry forming together a cyclic peroxide including 4 to 8 links and including 1 or 2 additional oxygen atoms in the cyclic structure, possibly suType: ApplicationFiled: December 11, 2008Publication date: May 17, 2012Applicants: SANOFI-AVENTIS, PALUMED S.A., CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S.)Inventors: Frederic COSLEDAN, Bernard MEUNIER, Alain PELLET
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Patent number: 8173812Abstract: Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently —OR6, C1-C6alkyl or C3-C6cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1-C6 alkyl or C3-C6 cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is —CH2—, —S—, or —O—; one of Y and Y1 is hydrogen and the other is OR6, —C(?O)R7, NR8SO2R6 or a heterocyclic group selected from those referred to in the specification; and R6, R7 and R8 are as defined in the specification.Type: GrantFiled: April 3, 2008Date of Patent: May 8, 2012Assignee: Pulmagen Therapeutics (Asthma) LimitedInventors: John Gary Montana, Harry Finch, George Hynd, Michael Colin Cramp, Rosa Arienzo, Neville McLean
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Patent number: 8173676Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: GrantFiled: August 15, 2011Date of Patent: May 8, 2012Assignees: Bayer Pharma AG, AstraZeneca ABInventors: Markus Berger, Jan Dahmen, Hartmut Rehwinkel, Stefan Jaroch, Heike Schäcke
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Publication number: 20120108545Abstract: Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.Type: ApplicationFiled: May 19, 2010Publication date: May 3, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Gary H. Posner, Lauren E. Woodard, David R. Levine, Deuk Kyu Moon, Bryan T. Mott
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Publication number: 20120108528Abstract: The present invention relates to novel compositions which can be used for the treatment of neuroinflammation, in particular in subjects having a neurodegenerative, autoimmune, infectious, toxic or traumatic disorder. More particularly, the invention relates to combined therapies for treating neuroinflammation. The invention also discloses new methods for treating neuroinflammation pathological conditions in a subject.Type: ApplicationFiled: March 29, 2010Publication date: May 3, 2012Applicant: PharnextInventors: Daniel Cohen, Serguei Nabirochkin, Ilya Chumakov
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Publication number: 20120108633Abstract: The present invention relates to an injectable composition for local administration for treating hemorrhoids, which contains hydroxychloroquine. Specifically, the composition contains a solution of hydroxychloroquine in physiological saline for injection, together with a local anesthetic and an antioxidant.Type: ApplicationFiled: June 18, 2010Publication date: May 3, 2012Inventor: Oh-Young Yeo
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Publication number: 20120101116Abstract: The present invention is directed to novel quinolines and quniazolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof which are useful for the treatment of protein kinases mediated diseases and conditions. The compounds of this invention have a general Formula (I) wherein R1 to R11 and X are defined herein.Type: ApplicationFiled: June 24, 2010Publication date: April 26, 2012Applicant: MEDOLUTION LIMITEDInventor: Dawei Zhang
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Publication number: 20120101053Abstract: The present invention relates to compounds capable of inhibiting and/or decreasing the activity of one or more cathepsins, thereby treating and/or preventing various disease states associated with one or more cysteine proteases including, but not limited to, cathepsins and papain-like cysteine proteases. Disease states treated and/or prevented by the compounds of the invention include, but are not limited to, mammalian parasitic diseases in which the parasite utilizes a critical cysteine protease from the papain family. Examples of parasitic diseases to be treated or prevented by the compounds of the invention include, but are not limited to, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, coccidiosis, giardiosis, cryptosporidiosis or schistosomiasis.Type: ApplicationFiled: June 16, 2010Publication date: April 26, 2012Inventors: Cameron Black, Christian Beaulieu
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Publication number: 20120101103Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.Type: ApplicationFiled: December 18, 2009Publication date: April 26, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
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Publication number: 20120095044Abstract: Disclosed herein are compounds that are tissue-nonspecific alkaline phosphatase inhibitors. The disclosed compounds are used to treat, prevent, or abate vascular calcification, arterial calcification and other cardiovascular diseases.Type: ApplicationFiled: December 7, 2011Publication date: April 19, 2012Inventors: Jose Luis Millan, Eduard Sergienko
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Publication number: 20120095045Abstract: The present invention relates to an injectable anticancer composition for local administration comprising hydroxychloroquine. The anticancer composition shows an IC50 value against sarcoma-180 cells, which is about 10 times lower than cisplatin, as determined by the MTT assay in vitro, suggesting that the anticancer composition has an excellent cytotoxic effect. Also, the anticancer composition shows dose-dependent effects against solid cancer induced by sarcoma-80 cells in vivo. In addition, the anticancer composition has the effect of extending the life expectancy of patients having ascites cancer induced by sarcoma-80 cells.Type: ApplicationFiled: June 18, 2010Publication date: April 19, 2012Inventor: Oh-Young Yeo
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Publication number: 20120094976Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.Type: ApplicationFiled: April 19, 2011Publication date: April 19, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald Engelhardt, Christiane Kofink, Darryl McConnell
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Publication number: 20120094983Abstract: A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.Type: ApplicationFiled: March 15, 2011Publication date: April 19, 2012Inventors: James A. Johnson, Yoon Jeon, John Lloyd, Heather Finlay
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Publication number: 20120077811Abstract: The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.Type: ApplicationFiled: March 11, 2010Publication date: March 29, 2012Inventors: Jeffrey Bruce Smaill, Adam Vorn Patterson, Michael Patrick Hay, William Alexander Denny, William Robert Wilson, Guo-Liang Lu, Robert Forbes Anderson, Ho Huat Lee, Amir Ashoorzadeh
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Publication number: 20120076732Abstract: The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.Type: ApplicationFiled: June 23, 2011Publication date: March 29, 2012Inventors: Yan Feng, Ottavio Arancio, Shixian Deng, Donald W. Landry
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Publication number: 20120076770Abstract: THE INVENTION RELATES TO compounds, proteins and methods of treatment therewith. Aspects of embodiments of the invention further relates to compounds and methods of treatment for bone, bone marrow, and bone tissue.Type: ApplicationFiled: March 28, 2011Publication date: March 29, 2012Inventors: Virginia Espina, Lance Liotta, Antonella Chiechi, Alessandra Romano, Emanuel Petricoin, Amy Van Meter
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Publication number: 20120077843Abstract: Described herein are progenitor cancer cells and cell lines isolated from human breast ductal carcinoma in situ (DCIS) lesions and the uses of these cells or cell lines in drug design, drug screening, and monitoring in vivo therapy. The DCIS malignant precursor cells or cell lines are epithelial in origin, are positive for markers of autophagy, show at least one genetic difference from normal cells of said fragment, form 3-D tube-like structures or ball aggregates, or are inhibited in formation of 3-D structures and migration by treatment with chloroquine.Type: ApplicationFiled: March 29, 2010Publication date: March 29, 2012Inventors: Lance A. Liotta, Virginia Espina, Rosa I. Gallagher, Kirsten Edmiston
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Patent number: 8143278Abstract: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase, and/or 11beta-hydroxylase (CYP11B1), and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase and/or CYP11B1. Finally, the present invention also provides a pharmaceutical composition.Type: GrantFiled: December 14, 2007Date of Patent: March 27, 2012Assignee: Novartis AGInventors: Qi-Ying Hu, Gary Michael Ksander
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Publication number: 20120071508Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, t, R1, R2, R3, R4, R5, R6, R7, Q, Y and Z have defined meanings.Type: ApplicationFiled: November 30, 2011Publication date: March 22, 2012Inventors: Jean Fernand Armand Lacrampe, Christophe Meyer, Bruno Schoentjes, Alain Philippe Poncelet, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert, Luc Van Hijfte
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Publication number: 20120071507Abstract: An extended regimen for treatment of HER-2/neu overexpressed/amplified cancer is described, with involves delivering a course of neratinib therapy to HER-2/neu overexpressed/amplified cancer patients following the completion of surgical and adjuvant therapy. The neratinib regimen may be continued for upwards of twelve months to five years. Also provided are pharmaceutical kits designed to facilitate compliance with the regimen.Type: ApplicationFiled: March 24, 2010Publication date: March 22, 2012Inventors: Anna Berkenblit, Florence Marie Helene Binlich, Paul Goss
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Publication number: 20120071417Abstract: Methods of inhibiting cancer cell growth using HDAC10 inhibitors are provided. Methods of treating cancer in a subject using HDAC10 inhibitors are also provided. In certain embodiments, at least one second inhibitor selected from an autophagy inhibitor, an AMPK inhibitor, and methyl pyruvate is also used in the methods. Dose packs comprising HDAC10 inhibitors and at least one second inhibitor are provided. Methods of identifying HDAC10 inhibitors are also provided.Type: ApplicationFiled: November 10, 2009Publication date: March 22, 2012Inventors: Tso-pang Yao, Hitoshi Sasajima, Yoshiharu Kawaguchi, Kai Cui, Chun-Hsiang Lai
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Publication number: 20120065166Abstract: THE INVENTION RELATES TO compositions, compounds, proteins and methods of treatment therewith. Aspects of embodiments also relate to a method of treating a patient by delivering to the tissues of said patient or administering to said patient a therapeutically effective amount of one or more compounds. Aspects of embodiments also relate to a method of detecting the presence of bone disease by machine-assaying detectable serotonin. Aspects of embodiments also relate to methods of treating disease in subjects.Type: ApplicationFiled: August 15, 2011Publication date: March 15, 2012Inventors: Virginia Espina, Lance Liotta, Antonella Chiechi, Alessandra Romano
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Publication number: 20120065204Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
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Publication number: 20120065199Abstract: A compound of formula (I) as well as pharmaceutically acceptable salts thereof and pharmaceutical compositions including a therapeutically effective amount of the compounds. The compound is useful in treatment of cancer, diabetic retinopathy, age-related macular degeneration, inflammation, stroke, ischemic myocardium, atherosclerosis, macular edema and psoriasis.Type: ApplicationFiled: May 20, 2010Publication date: March 15, 2012Applicant: CLANOTECH ABInventors: Johan Malm, Rune Ringom, Patrizia Caldirola, Jacob Westman
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Publication number: 20120058201Abstract: The present invention describes an association between genetic polymorphisms in the FAM13A1 (family with sequence similarity 13, member A1) gene and a predisposition to prolongation of the QT interval, and provides related methods for the prediction of such a predisposition, the administration of QT interval- prolonging compounds to individuals having such a predisposition, and determining whether a compound is capable of inducing QT prolongation.Type: ApplicationFiled: April 5, 2010Publication date: March 8, 2012Applicant: VANDA PHARMACEUTICALS, INC.Inventors: Christian Lavedan, Simona Volpi, Louis Licamele
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Publication number: 20120046269Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: February 4, 2010Publication date: February 23, 2012Applicant: Merck Patent GmbHInventors: Amanda E. Sutton, Ruoxi Lan, Thomas E. Richardson, David Perrey, Harold George Vandeveer, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Lesley Liu-Bujalski, Andreas Goutopoulos, Frank Steiber, Brian L. Hodous, Hui Qiu, Reinaldo C. Jones, Brian H. Heasley
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Publication number: 20120040021Abstract: The invention relates to compositions comprising an acid ceramidase inhibitor and a choline kinase inhibitor as well as to the uses thereof for the treatment of cancer. The invention also relates to methods for the selection of an individualised therapy of a cancer patient based on the detection of the acid ceramidase levels. Moreover, the invention also relates to compositions comprising a choline kinase inhibitor and an alkylating agent and uses thereof for the treatment of cancer. Finally, the invention also relates to compositions comprising a choline kinase inhibitor and an alkylating agent or a death receptor ligand and uses thereof for the treatment of cancer.Type: ApplicationFiled: August 12, 2011Publication date: February 16, 2012Applicant: TRASLATIONAL CANCER DRUGS PHARMA, S.L.Inventors: Ana Ramirez De Molina, Lourdes Garcia Oroz, Juan Carlos Lacal Sanjuan
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Publication number: 20120041024Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4 and R5 are as defined herein, and methods of making and using the same.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Inventors: Adam Kenneth Charnley, Pamela A. Haile, Terry Vincent Hughes
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Publication number: 20120027871Abstract: The invention provides methods for the administration of compounds capable of prolonging a QTc interval and methods for predicting whether an individual is predisposed to such QTc prolongation.Type: ApplicationFiled: April 5, 2010Publication date: February 2, 2012Applicant: VANDA PHARMACEUTICALS, INC.Inventors: Curt D. Wolfgang, Mihael H. Polymeropoulos
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Patent number: 8106073Abstract: The invention provides a compound of formula (I) as defined in the specification, a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharmaceutical composition, and its use in therapy.Type: GrantFiled: November 26, 2008Date of Patent: January 31, 2012Assignee: AstraZeneca ABInventors: Simon David Guile, Toby Thompson
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Publication number: 20120022103Abstract: The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.Type: ApplicationFiled: September 29, 2011Publication date: January 26, 2012Applicant: ABBOTT LABORATORIESInventors: Erol K. Bayburt, Jerome F. Daanen, Arthur R. Gomtsyan, Steven P. Latshaw, Chih-hung Lee, Robert G. Schmidt, JR.
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Publication number: 20120015950Abstract: Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C1-8-alkylene group; R1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a tritluoromethyl group; R4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or oType: ApplicationFiled: November 13, 2009Publication date: January 19, 2012Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Mourad Saady, Julien Vache, Corinne Veronique, Philippe Yaiche
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Publication number: 20120015952Abstract: The invention relates to compounds of formulae (1) and (2): and pharmaceutically acceptable salts thereof for the treatment of cancer, inflammation, auto-immune diseases, diabetes and diabetic complications, infection, cardiovascular disease and ischemia-reperfusion injuries.Type: ApplicationFiled: March 25, 2010Publication date: January 19, 2012Applicant: Profectus Biosciences, Inc.Inventors: Jie Zhang, Drago Robert Sliskovic, Charles E. Ducker
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Patent number: RE43431Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction medType: GrantFiled: August 18, 2009Date of Patent: May 29, 2012Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Anke Baum, Flavio Solca