1,4-diazine As One Of The Cyclos Patents (Class 514/249)
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Patent number: 8906911Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: GrantFiled: March 29, 2013Date of Patent: December 9, 2014Assignee: AbbVie Inc.Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
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Publication number: 20140356430Abstract: Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition.Type: ApplicationFiled: May 28, 2014Publication date: December 4, 2014Applicant: Signal Pharmaceuticals, LLCInventors: Marie Georges BEAUCHAMPS, Antonio Christian FERRETTI, Juan Antonio GAMBOA, Kevin KLOPFER, William Edward KONNECKE, Matthew Michael KREILEIN, Anil MENON, Amanda Nicole MIKLOS, John Fitzgerald TRAVERSE
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Publication number: 20140357640Abstract: The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 18, 2012Publication date: December 4, 2014Applicant: SANOFIInventors: Marc Nazare, Nis Halland, Friedemann chmidt, Tilo Weiss, Uwe Dietz, Armin Hofmeister
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Publication number: 20140357611Abstract: A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.Type: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Inventors: Krzysztof Palczewski, Akiko Maeda, Marcin Golczak
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Publication number: 20140357641Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.Type: ApplicationFiled: January 11, 2013Publication date: December 4, 2014Applicant: NOVARTIS AGInventors: Gurdip Bhalay, Steven Carl Chatlton, Mark Patrick Healy, Catherine Leblanc, Stephen Carl McKeown
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Publication number: 20140357632Abstract: Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: August 13, 2012Publication date: December 4, 2014Inventors: Rajan Anand, Vincent J. Colandrea, Maud Reiter, Petr Vachal, Aaron Zwicker, Jonathan E. Wilson, Fengqi Zhang, Kake Zhao
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Publication number: 20140356360Abstract: The present invention relates to piperazinyl derivatives of formula (I) and the use thereof as a drug, particularly for the treatment of cancer, the pharmaceutical compositions containing said derivatives, and the method for synthesising same.Type: ApplicationFiled: December 28, 2012Publication date: December 4, 2014Inventor: Marc-Henry PITTY
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Publication number: 20140357639Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: June 19, 2014Publication date: December 4, 2014Inventors: Jan Kehler, Jacob Nielsen, Mauro Marigo, John Paul Kilburn, Morten Langgârd
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Patent number: 8901117Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: GrantFiled: December 23, 2011Date of Patent: December 2, 2014Assignee: The Regents of The University of MichiganInventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
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Patent number: 8901125Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: June 19, 2013Date of Patent: December 2, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
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Patent number: 8900565Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: GrantFiled: November 21, 2012Date of Patent: December 2, 2014Assignee: Pharmacyclics, Inc.Inventors: Joseph J. Buggy, Sriram Balasubramanian, Erik Verner, Vincent W. F. Tai, Chang-Sun Lee
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Publication number: 20140350024Abstract: The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a substituted bicyclic heteroaromatic ring compound of formula I: wherein two of X1 to X8 are N and the remaining of X1 to X8 are CH; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: January 11, 2013Publication date: November 27, 2014Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Malvika Kaul
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Publication number: 20140350023Abstract: The present invention claims amorphous solid state forms of sitagliptin salts, processes for their preparation, and pharmaceutical compositions thereof. As salt forming anions are claimed: The maleate, fumarate, besylate, mesylate and succinate.Type: ApplicationFiled: December 7, 2012Publication date: November 27, 2014Inventors: Suresh Babu Jayachandra, Jigar Bhaskarbhai Shah, Chiguru Sailu, Sandeep Thakaji Kanawade
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Publication number: 20140349986Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.Type: ApplicationFiled: July 24, 2014Publication date: November 27, 2014Applicant: SANOFIInventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
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Publication number: 20140350022Abstract: The present invention relates to a beneficial treatment of tumours in patients suffering from NSCLC, and to a clinical marker useful as as predictive variable of the responsiveness of tumours in patients suffering from NSCLC. The present invention further relates to a method for selecting patients likely to respond to a given therapy, wherein said method optionally comprises the use of a specific clinical marker. The present invention further relates to a method for delaying disease progression and/or prolonging patient survival of NSCLC patients, wherein said method comprises the use of a specific clinical marker.Type: ApplicationFiled: May 2, 2014Publication date: November 27, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Birgit GASCHLER-MARKEFSKI, Ralf KAISER
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Patent number: 8895557Abstract: Ecteinascidin formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided.Type: GrantFiled: October 28, 2005Date of Patent: November 25, 2014Assignee: Pharma Mar, S.A., Sociedad UnipersonalInventors: Jacob Hendrik Beijnen, Bastiaan Nuijen, Pilar Calvo Salve, Maria Tobio Barreira
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Patent number: 8895558Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.Type: GrantFiled: September 23, 2009Date of Patent: November 25, 2014Assignee: Green Cross CorporationInventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
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Patent number: 8895559Abstract: A variety of specific compounds within the scope of formula I which are useful as PI3K inhibitors and can be employed for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours, and pharmaceutical compositions and kits containing said specific compounds.Type: GrantFiled: September 22, 2011Date of Patent: November 25, 2014Assignee: Merck Patent GmbHInventors: Markus Klein, Ulrich Emde, Hans-Peter Buchstaller, Christina Esdar, Oliver Poeschke
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Patent number: 8895750Abstract: The present invention encompasses compounds of the formula (I) wherein the groups ring A and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: GrantFiled: March 13, 2014Date of Patent: November 25, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Todd Bosanac, Michael J. Burke, Darren Disalvo, Wang Mao, John Westbrook
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Patent number: 8895740Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: July 27, 2012Date of Patent: November 25, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Luca Settimo, Damien Fraysse, Guy Brenchley, Christopher John Davis, Andrew W. Miller
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Patent number: 8895560Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.Type: GrantFiled: March 10, 2014Date of Patent: November 25, 2014Assignee: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec, Allan James Goodman
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Publication number: 20140343066Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.Type: ApplicationFiled: December 20, 2013Publication date: November 20, 2014Inventors: Irini Akritopoulou-Zanze, Brian D. Wakefield, Helmut Mack, Sean C. Turner, Alan F. Gasiecki, Vijaya J. Gracias, Kathy A. Sarris, Douglas M. Kalvin, Melissa J. Michmerhuizen, Qi Shuai, Jyoti R. Patel, Margaretha H.M. Bakker, Nicole Teusch, Eric F. Johnson, Peter J. Kovar, Stevan W. Djuric, Andrew J. Long, Anil Vasudevan, Dawn M. George, Lu Wang, Biqin Li, Nigel S. Moore, Adrian D. Hobson, Keith W. Woods, Julie M. Miyashiro, Steven L. Swann, Jr., Thomas D. Penning
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Publication number: 20140343069Abstract: One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine.Type: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Applicant: Sunovion Inc.Inventors: Karim LALJI, Timothy BARBERICH, Judy CARON, Thomas WESSEL
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Publication number: 20140343068Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. Specifically quinoxaline derivatives of Formula I and their use in modulating the activity of Braf and/or mutant Braf kinase to regulate and modulate abnormal or inappropriate cell proliferation, differentiation, or metabolism are disclosed. Also disclosed are methods of treating cancer associated with Braf and/or mutant Braf kinase activity in a subject, comprising administering the compounds of Formula I.Type: ApplicationFiled: September 28, 2012Publication date: November 20, 2014Inventors: Xiangping Qian, Yong Zhu
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Publication number: 20140341968Abstract: Biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 10 days and one year or longer.Type: ApplicationFiled: August 1, 2014Publication date: November 20, 2014Inventors: Michael R. Robinson, Wendy M. Blanda, Patrick M. Hughes, Guadalupe Ruiz, Werhner C. Orilla, Scott M. Whitcup, Lon T. Spada, Devin F. Welty, Joan-En Lin
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Publication number: 20140343067Abstract: The present invention relates to a method of reducing cutaneous facial flushing caused by systemic use of phosphodiesterase type 5 (PDE5) inhibitors by topical facial dermatological application of an effective dose of a composition comprising at least one alpha adrenergic receptor agonist.Type: ApplicationFiled: October 12, 2012Publication date: November 20, 2014Inventors: Warren J. Scherer, Arthur Clapp, Philippe Andres
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Publication number: 20140343480Abstract: Various agents and additives for cross-linking treatments are identified in disclosed studies. The characteristics of the various agents and additives may be advantageously employed in formulations applied in cross-linking treatments of the eye. In some embodiments, riboflavin is combined with Iron(II) to enhance the cross-linking activity generated by the riboflavin. In other embodiments, cross-linking treatments employ an Iron(II) solution in combination with a hydrogen peroxide pre-soak. In yet other embodiments, 2,3-butanedione is employed to increase the efficacy of corneal cross-linking with a photosensitizer, such as riboflavin. In further embodiments, folic acid is employed in combination with a photosensitizer, such as riboflavin, to enhance cross-linking activity. In yet further embodiments, 2,3-butanedione, folic acid, a quinoxaline, a quinoline, dibucaine, Methotrexate, menadione, or a derivative thereof is applied as a cross-linking agent.Type: ApplicationFiled: May 19, 2014Publication date: November 20, 2014Applicant: AVEDRO, INC.Inventors: Pavel Kamaev, Marc D. Friedman, Evan Sherr, David Muller
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Publication number: 20140343046Abstract: The present invention relates to the pharmaceutical use of selective GABA A ?5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Inventors: Rodolfo Gasser, Maria-Clemencia Hernandez, Andrew Thomas
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Patent number: 8889194Abstract: Disclosed is a compound and methods for use by an individual attempting to reduce or cease tobacco smoking or one exposed to environmental tobacco smoke. The compound includes a first component blocking nicotine receptor sites to reduce nicotine cravings or withdrawal symptoms, a second component increasing serotonin levels and acting synergistically with the first component to reduce nicotine cravings or withdrawal symptoms, assisting in maintaining body weight and reducing increased stress and anxiety, and a third component acting synergistically with the first and/or second component to reduce nicotine cravings or withdrawal symptoms, maintain body weight, and/or reduce increased stress and anxiety. The third component comprises a supplement that replenishes depleted body substance(s), repairs damaged body substance(s), and/or ameliorates the impaired function of body substance(s). Some combination of the first, second, and third component alters the perceived taste of tobacco smoke.Type: GrantFiled: September 29, 2010Date of Patent: November 18, 2014Inventor: Harlan Clayton Bieley
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Patent number: 8889686Abstract: L malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are disclosed for decreasing the bitterness of eszopiclone dosage formsType: GrantFiled: July 1, 2013Date of Patent: November 18, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
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Patent number: 8889684Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R6, A, X, Y and m are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: GrantFiled: January 27, 2012Date of Patent: November 18, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Heinz Stadtmueller
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Patent number: 8889685Abstract: Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The salts are useful for treating sleep disorders.Type: GrantFiled: June 27, 2013Date of Patent: November 18, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
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Patent number: 8889683Abstract: The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: September 23, 2011Date of Patent: November 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Clifford Cheng, Gerald W. Shipps, Jr., Xiaohua Huang, Ying Huang, Ning Shao, Ashwin Rao, Anandan Palani, Peter Orth, Johannes H. Voigt, Robert J. Herr, Lana Michele Rossiter, Qi Zeng, Xianfeng Sun
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Patent number: 8889664Abstract: The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.Type: GrantFiled: April 28, 2011Date of Patent: November 18, 2014Assignee: Exelixis, Inc.Inventors: William Bajjalieh, Lynne Canne Bannen, S. David Brown, Patrick Kearney, Morrison Mac, Charles K. Marlowe, John M. Nuss, Zerom Tesfai, Yong Wang, Wei Xu
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Publication number: 20140336177Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.Type: ApplicationFiled: December 11, 2012Publication date: November 13, 2014Inventors: Barbara Pio, Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Shawn Walsh
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Publication number: 20140336196Abstract: The present invention relates to novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, and polymorphs, hydrates and solvates thereof, which are potent inhibitors of dipeptidyl peptidase-IV useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The present invention also relates to the process for preparing the novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, as well as pharmaceutical compositions containing the novel phosphoric acid salts, and methods of use thereof for the treatment of diabetes, obesity, and high blood pressure.Type: ApplicationFiled: May 22, 2012Publication date: November 13, 2014Applicant: Merck Sharp & Dohme Corp.Inventor: Jerry L. Atwood
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Publication number: 20140336164Abstract: Biodegradable non-ophthalmic implants include one or more agents dispersed within a biodegradable polymer component. The implants release the agents from the biodegradable polymer component to a target site of a patient as the implant degrades. The agents provided in the implants can be therapeutic agents or diagnostic agents and are useful in medical treatments of non-ocular regions of a patient.Type: ApplicationFiled: July 23, 2014Publication date: November 13, 2014Inventors: Steven Pal, Mitchell Brin
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Publication number: 20140336189Abstract: Compounds corresponding to the general formula (I) wherein R2 represents a group C1-10-alkyl, C3-10-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl-C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6-alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy-C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10-fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; X6 represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt, and the therapeutic use thereof.Type: ApplicationFiled: July 23, 2014Publication date: November 13, 2014Inventors: Sylvain COTE-DES-COMBES, Jacques FROISSANT, Jean-Francois GIBERT, Frank MARGUET, Christophe PACAUD, Frederic PUECH, Antoine RAVET
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Publication number: 20140336169Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: May 9, 2014Publication date: November 13, 2014Applicant: GILEAD CONNECTICUT, INC.Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
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Publication number: 20140336141Abstract: The invention exploits the elucidation of a connection between the S-adenosylmethionine one-carbon cycle and MAO-B levels and describes drug efficacy testing methods and the use of compounds of the S-adenosylmethionine one-carbon cycle as MAO-B inhibitors in disease prevention and treatment.Type: ApplicationFiled: December 21, 2012Publication date: November 13, 2014Inventors: Maria Zellner, Ellen Umlauf
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Patent number: 8883744Abstract: The canonical Wnt signaling pathway is implicated in many disorders including neural tube defects, limb malformations, and heart defects, developmental disorders associated with alcohol exposure (fetal alcohol syndrome) or exposure to bipolar medications (i.e. lithium), wound healing, and Alzheimer's disease. Elevated plasma homocysteine (HCy), which results from folate (folic acid, FA) deficiency, the mood-stabilizing drug lithium (Li), and alcohol (ethanol) are linked to the induction of human congenital heart and neural tube defects. FA supplementation ameliorates the observed developmental errors in the Li-HCy, or alcohol-exposed mouse embryos and normalized heart function. Li, HCy or Wnt3A suppress Wnt-modulated Hex and Islet-1 expression. FA protects from the gene misexpression that is induced by all three factors. Administration of myo-inositol with FA synergistically enhances the protective effect.Type: GrantFiled: October 8, 2013Date of Patent: November 11, 2014Assignee: University of South FloridaInventor: Kersti K. Linask
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Patent number: 8883784Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: GrantFiled: August 12, 2013Date of Patent: November 11, 2014Assignee: AbbVie Inc.Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
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Publication number: 20140329798Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119.Type: ApplicationFiled: November 9, 2012Publication date: November 6, 2014Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
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Publication number: 20140329795Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: August 28, 2012Publication date: November 6, 2014Inventors: Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson, Celia Dominguez, Leticia M. Toledo-Sherman, Ignacio Munoz
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Publication number: 20140329821Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: July 9, 2014Publication date: November 6, 2014Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Publication number: 20140329794Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: ApplicationFiled: December 20, 2013Publication date: November 6, 2014Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
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Publication number: 20140328860Abstract: This disclosure demonstrates that blockade of TGF? signaling after a hematopoietic stress (e.g., chemotherapy, transplantation, and infection) accelerates hematopoietic reconstitution and delays the return of cycling hematopoietic stem and progenitor cells (HSPCs) to quiescence. TGF? blockade in these settings promotes multilineage hematopoietic regeneration by prolonging HSPC cycling and by promoting HSC self-renewal, and is useful for treating hematologic deficiencies caused various hematopoietic stresses.Type: ApplicationFiled: November 21, 2012Publication date: November 6, 2014Applicant: CORNELL UNIVERSITYInventors: Joseph Scandura, Fabienne Brenet
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Patent number: 8877743Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: GrantFiled: June 14, 2013Date of Patent: November 4, 2014Assignee: Naeja Pharmaceutical Inc.Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
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Patent number: 8877755Abstract: The present invention generally relates to pharmaceutical compositions comprising a dopamine agonist and sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine; and the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. The pharmaceutical compositions of the invention are useful in the treatment of restless-leg syndrome and periodic-limb-movement disorder, as well as various sleep disorders.Type: GrantFiled: August 14, 2009Date of Patent: November 4, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventor: Timothy J. Barberich
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Patent number: 8877757Abstract: The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: GrantFiled: August 31, 2011Date of Patent: November 4, 2014Assignee: Merck Serono SAInventors: Pascale Gaillard, Anna Quattropani, Vincent Pomel, Thomas Rueckle, Jasna Klicic, Dennis Church