Polycyclo Ring System Having The Plural Nitrogen Containing Additional Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/254.06)
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Patent number: 11787802Abstract: The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.Type: GrantFiled: January 14, 2022Date of Patent: October 17, 2023Assignee: C4 Therapeutics, Inc.Inventors: Roger Norcross, Annick Goergler, Fabian Dey, Eric Andre Kusznir
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Patent number: 11492343Abstract: The present invention discloses novel polymorphs I, II, and V of a [2-(4-(3-trifluoromethyl-benzyl)piperazin-1-yl)ethyl]-2,3-dihydro-1H-benzimidazol-2-one and a preparation method and application thereof. The polymorph I is a trihydrate crystal, the polymorph II is an anhydrous crystal, and the polymorph V is an anhydrous crystal. When compared with an existing crystal form, the novel polymorphs provides significant advantages in terms of solubility and preparation techniques.Type: GrantFiled: February 3, 2017Date of Patent: November 8, 2022Inventor: Xiaoming Meng
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Patent number: 11254672Abstract: The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.Type: GrantFiled: March 4, 2020Date of Patent: February 22, 2022Assignee: C4 Therapeutics, Inc.Inventors: Roger Norcross, Annick Goergler, Fabian Dey, Eric Andre Kusznir
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Patent number: 10913736Abstract: The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.Type: GrantFiled: August 21, 2015Date of Patent: February 9, 2021Assignee: University of WashingtonInventors: Frederick S. Buckner, Ximena Barros Alvarez, Erkang Fan, John Robert Gillespie, Wilhelmus G.J. Hol, Wenlin Huang, Cho Yeow Koh, Ranae M. Ranade, Sayaka Shibata, Christophe L.M. Verlinde, Zhongsheng Zhang
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Patent number: 10246440Abstract: Indazole sulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonists of retinoid-related orphan receptor gamma ROR?t are described. Pharmaceutical compositions including such compounds, as well as the use thereof for the topical and/or oral treatment of ROR?t receptor-mediated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis are also described.Type: GrantFiled: December 18, 2015Date of Patent: April 2, 2019Assignee: GALDERMA RESEARCH & DEVELOPMENTInventors: Branislav Musicki, Gilles Ouvry, Etienne Thoreau, Claire Bouix-Peter
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Patent number: 10166230Abstract: The invention relates to a method for the treatment of vasomotor symptoms comprising the administration of a therapeutically effective amount of flibanserin.Type: GrantFiled: December 26, 2014Date of Patent: January 1, 2019Inventors: Vladimir Hanes, Anna Elizabeth Verbeek
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Patent number: 10085979Abstract: Disclosed are methods of treating neuroblastoma in a cancer patient by administration of a Trk inhibitor in combination with one more chemotherapeutic agents. Also disclosed are pharmaceutical compositions comprising a Trk inhibitor and one or more chemotherapeutic agents.Type: GrantFiled: November 30, 2015Date of Patent: October 2, 2018Assignee: IGNYTA, INC.Inventors: Zachary Dolph Hornby, Gang Li, David Wesley Anderson, Garrett M. Brodeur, Radhika Iyer
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Patent number: 9592208Abstract: A solid pharmaceutical composition suitable for oral administration, comprising: (a) a S1P receptor modulator; (b) a filler, and (c) a cyclodextrin.Type: GrantFiled: March 30, 2012Date of Patent: March 14, 2017Assignee: Novartis AGInventor: Supriya Rane
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Patent number: 9388179Abstract: Disclosed are compounds of Formula AA and Formula AB: wherein “Heteroaryl-1”, RA1, RA2, RB1, and RC are defined herein, which novel compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formulae AA and AB or their salts, and methods of treating neuropathic pain disorders using the same.Type: GrantFiled: October 23, 2013Date of Patent: July 12, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Joseph E. Pero, Hannah D. G. F. Lehman, Mark E. Layton, Michael A. Rossi, Michael J. Kelly, III
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Patent number: 9180191Abstract: The invention concerns methods of treating suicidal ideation or behavior in a subject in need thereof, comprising decreasing endogenous nicotinic acetylcholine receptor (nAChR) activity in the subject; therapeutic packages for treating suicidal ideation or behavior; and methods for determining the efficacy of a treatment for suicidal ideation or behavior. In some embodiments, the treatment methods comprise administering to the subject an effective amount of an inhibitor of a nAChR, such as a lithium compound, mecamylamine, clozapine, or asenapine.Type: GrantFiled: October 15, 2010Date of Patent: November 10, 2015Assignee: UNIVERSITY OF SOUTH FLORIDAInventors: David Vincent Sheehan, Roland Douglas Shytle
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Publication number: 20150148330Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: January 16, 2015Publication date: May 28, 2015Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
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Publication number: 20150126524Abstract: The present invention relates to new crystalline salt forms of flibanserine which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.Type: ApplicationFiled: September 12, 2014Publication date: May 7, 2015Applicant: SPROUT PHARMACEUTICALS, INC.Inventors: Jaroslaw Mazurek, Mihaela Pop
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Publication number: 20150111898Abstract: The invention relates to a method for the treatment of premenstrual and other female sexual disorders comprising the administration of a therpeutically effective amount of flibanserin.Type: ApplicationFiled: September 3, 2014Publication date: April 23, 2015Applicant: Sprout Pharmaceuticals, Inc.Inventor: Robert Pyke
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Patent number: 9012459Abstract: The disclosure is directed to a monohydrate crystalline form of 3-(5-(4-(3-fluoropropyl)piperazin-1-yl)benzimidazol-2-yl)-1-azaazulen-2-one, possessing diffraction peaks of about 12.9°, 15.9°, 17.9°, 21.2°, 22.9°, 23.5° and 24.5°. Its preparation method and pharmaceutical composition thereof are also provided.Type: GrantFiled: August 15, 2013Date of Patent: April 21, 2015Assignee: Industrial Technology Research InstituteInventors: Yen-Fang Wen, Yuan-Jang Tsai, Wan-Ru Chen, Tsan-Lin Hu, Chia-Mu Tu, Chih-Peng Liu
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Patent number: 9012487Abstract: A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.Type: GrantFiled: March 2, 2007Date of Patent: April 21, 2015Assignee: Nerviano Medical Sciences S.r.l.Inventors: Tiziano Bandiera, Jay Aaron Bertrand, Paolo Pevarello, Ettore Perrone, Andrea Lombardi Borgia, Sten Christian Orrenius, Mauro Angiolini, Daniele Fancelli
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Publication number: 20150104439Abstract: The invention provides a method for alleviating discogenic pain by administering a therapeutic agent that disrupts neuronal and/or vascular elements in the disc, which is typically a degenerated disc. Disruption of neuronal elements in the disk includes destroying nerve endings without substantially affecting the central body of the nerve, suppressing activation of the nerve endings, and inhibiting the growth of nerve endings into the disk. Disruption of vascular elements includes causing the vascular extensions to retract from the disk, or suppressing the formation of such extensions. The therapeutic agent may be administered locally via an interbody pump, a bolus or a depot, or may be administered systemically.Type: ApplicationFiled: December 19, 2014Publication date: April 16, 2015Inventors: Josee Roy, Susan J. Drapeau, Jeffrey C. Marx
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Publication number: 20150105397Abstract: The present inventions relate to substituted piperazine derivatives of general formula (I) and to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various medical conditions related to glycine transporter-1 (GlyT1).Type: ApplicationFiled: October 14, 2014Publication date: April 16, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christoph HOENKE, Riccardo GIOVANNINI, Uta LESSEL, Holger ROSENBROCK, Bernhard SCHMID
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Patent number: 9006278Abstract: Controlled release systems release at least one pluribioactive antifungal drug exhibiting at least one additional bioactivity from the group consisting of spermiostatic, antineoplastic, antibacterial, antirestenotic and antiviral activities. The drug release system is designed for use as a spermiostatic contraceptive, intravaginal ringed-mesh which may also exhibit antiviral activity, an in situ-forming implant for treating different forms of cancer and topical film for treating or preventing bacterial and fungal infections.Type: GrantFiled: January 29, 2011Date of Patent: April 14, 2015Assignee: Poly-Med, Inc.Inventors: Shalaby W. Shalaby, Georgios T. Hilas, Sheila Nagatomi
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Patent number: 8999981Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: GrantFiled: January 6, 2012Date of Patent: April 7, 2015Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
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Patent number: 8999993Abstract: The invention relates to novel compounds, processes for their preparation and their use in protecting biological materials from radiation damage (radioprotection).Type: GrantFiled: April 6, 2011Date of Patent: April 7, 2015Assignee: Peter MacCallum Cancer InstituteInventors: Roger Francis Martin, Jonathan White, Pavel Lobachevsky, David Winkler, Colin Skene, Sebastian Marcuccio
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Patent number: 8999968Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.Type: GrantFiled: July 3, 2013Date of Patent: April 7, 2015Assignee: University Health NetworkInventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
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Patent number: 8993779Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.Type: GrantFiled: August 5, 2011Date of Patent: March 31, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
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Patent number: 8987275Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.Type: GrantFiled: February 18, 2011Date of Patent: March 24, 2015Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Wenjun Zhou, Xianming Deng
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Publication number: 20150080410Abstract: Developed here is a mitotic network comprising a signature of up to 54 genes, and including also sub-sets of genes within the signature, which can identify members by requiring higher correlation values for a signature gene. The present mitotic network provides for methods for prognosis and diagnosis of various cancers. The mitotic network is conserved across cancers exhibiting aberrant mitotic activity and several genes in the network act as therapeutic targets. Development of other inhibitors of mitosis can apply expression values of the genes in the mitotic network from patient tissue to select patients during clinical validation of the new drugs.Type: ApplicationFiled: May 19, 2014Publication date: March 19, 2015Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Zhi Hu, Jian-hua Mao, Wen-Lin Kuo, Ge Huang, Joe W. Gray
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Publication number: 20150072994Abstract: The invention relates to a method for the treatment of obesity and related diseases comprising the administration of a therapeutically effective amount of Flibanserin.Type: ApplicationFiled: July 21, 2014Publication date: March 12, 2015Applicant: SPROUT PHARMACEUTICALS, INC.Inventors: Angelo Ceci, Marcus Schindler
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Publication number: 20150065520Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: November 6, 2014Publication date: March 5, 2015Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Publication number: 20150065495Abstract: The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.Type: ApplicationFiled: August 28, 2014Publication date: March 5, 2015Applicant: UNIVERSITY OF UTAHInventors: Hariprasad Vankayalapati, Sunil Sharma, Venkataswamy Sorna
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Patent number: 8969341Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: GrantFiled: November 28, 2012Date of Patent: March 3, 2015Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Publication number: 20150057292Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: November 6, 2014Publication date: February 26, 2015Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Publication number: 20150057290Abstract: The present invention relates to the use of 1-[2-(4-(3-trifluoromethyl-phenyl)piperazin-1-yl)ethyl]-2,3-dihydro-1H-benzimidazol-2-one, optionally in the form of its pharmaceutically acceptable acid addition salts and optionally in the form of its hydrates or solvates, for preparing a pharmaceutical composition with a neuroprotective activity.Type: ApplicationFiled: June 30, 2014Publication date: February 26, 2015Inventor: Franco Borsini
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Publication number: 20150057291Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: November 6, 2014Publication date: February 26, 2015Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Publication number: 20150051222Abstract: The present invention relates to a process for the preparation of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide. Novel solid forms of this compound, their utility in treating diseases caused by deregulated protein kinase activity and pharmaceutical compositions containing them are also object of the present invention.Type: ApplicationFiled: October 30, 2014Publication date: February 19, 2015Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Natale Alvaro BARBUGIAN, Romualdo FORINO, Tiziano FUMAGALLI, Paolo ORSINI
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Publication number: 20150050239Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: July 19, 2013Publication date: February 19, 2015Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Publication number: 20150051221Abstract: The invention relates to the use of flibanserin for the preparation of a medicament for the treatment of post-menopausal Sexual Desire Disorders.Type: ApplicationFiled: June 24, 2014Publication date: February 19, 2015Inventors: Stephane Pollentier, Robert E. Pyke
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Publication number: 20150051203Abstract: A compound of structural formula (I) or (II): as HSP90 inhibitors that possess significantly improved bioavailability over comparative compounds, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders.Type: ApplicationFiled: March 27, 2013Publication date: February 19, 2015Inventors: Dinesh Chimmanamada, Zachary Demko, Weiwen Ying
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Publication number: 20150011564Abstract: The present invention pertains to a compound of formula (I) wherein R1, R2, R3, and R4 are each hydrogen or sulfate monoester with the proviso that R1, R2, R3, and R4 cannot simultaneously be hydrogen, processess for their preparation and their use as pharmaceuticals in the treatment of CNS disorders.Type: ApplicationFiled: May 8, 2014Publication date: January 8, 2015Applicant: Sprout Pharmaceuticals, Inc.Inventors: Astrid Volz, Ralf Lotz, Fabio Paleari
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Publication number: 20150011548Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.Type: ApplicationFiled: October 9, 2012Publication date: January 8, 2015Inventors: Tero Linnanen, Gerd Wohlfahrt, Srinivas Nanduri, Ravi Ujjinamatada, Srinivasan Rajagopalan, Subhendu Mukherjee
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Publication number: 20150011563Abstract: The invention relates to the use of flibanserin, or a pharmaceutically acceptable acid addition salt thereof, for the treatment of disorders of sexual desire.Type: ApplicationFiled: May 5, 2014Publication date: January 8, 2015Inventors: Franco Borsini, Kenneth Robert Evans
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Publication number: 20150004228Abstract: The invention relates to oral pharmaceutical compositions containing flibanserin, methods for the preparation thereof and use thereof as a medicament.Type: ApplicationFiled: May 5, 2014Publication date: January 1, 2015Inventors: Thomas Friedl, Guido Bernhard Edmund Radtke
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Publication number: 20150005288Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: January 22, 2013Publication date: January 1, 2015Applicants: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbHInventors: Frank Süssmeier, Mario Lobell, Sylvia Grünewald, Michael Härter, Bernd Buchmann, Joachim Telser, Hannah Jörissen, Melanie Heroult, Antje Kahnert, Klemens Lustig, Niels Lindner
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Publication number: 20150005316Abstract: The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.Type: ApplicationFiled: May 5, 2014Publication date: January 1, 2015Applicant: SPROUT PHARMACEUTICALS, INC.Inventors: Carlo Bombarda, Enrica Dubini, Antoine Ezhaya
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Publication number: 20140378917Abstract: The present invention provides transdermal therapeutic systems for dispensing a pharmaceutical product, in particular a pharmaceutical product with a low tendency to spontaneously crystallize. The matrix layer or at least one of the matrix layers in said systems contains a silicone hot-melt adhesive, a pharmaceutical product, and particles made of crosslinked polyvinylpyrrolidone. The invention also relates to a method for producing said transdermal therapeutic systems.Type: ApplicationFiled: December 28, 2012Publication date: December 25, 2014Inventors: Horst Dzekan, Hans-Rainer Hoffmann, Michael Horstmann, Walter Mueller, Sandra Wiedersberg
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Publication number: 20140371202Abstract: The present teaching provide indazole compounds represented by Structural Formulae (I) or (I?) or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as TTK protein kinase, polo-like kinase 4 (PLK4) and Aurora kinases having anticancer activity against breast cancer cells, colon cancer cells, and ovarian cancer cells.Type: ApplicationFiled: October 12, 2012Publication date: December 18, 2014Applicant: University Health NetworkInventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter Brent Sampson, Miklos Feher, Donald E. Awrey
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Publication number: 20140364420Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.Type: ApplicationFiled: January 13, 2014Publication date: December 11, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
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Publication number: 20140350012Abstract: The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-Type: ApplicationFiled: August 11, 2014Publication date: November 27, 2014Inventors: Jean-Pierre Andre Marc Bongartz, Lieven Meerpoel, Maria Gustaaf Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
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Publication number: 20140350010Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: November 28, 2012Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Publication number: 20140343075Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: ApplicationFiled: July 30, 2014Publication date: November 20, 2014Applicant: MERCK PATENT GMBHInventors: Kai SCHIEMANN, Melanie SCHULTZ, Wolfgang STAEHLE
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Patent number: 8889673Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.Type: GrantFiled: June 21, 2012Date of Patent: November 18, 2014Assignee: Genentech, Inc.Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Wendy Liu
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Publication number: 20140336200Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.Type: ApplicationFiled: July 23, 2014Publication date: November 13, 2014Applicant: ADAMED SP. Z O.O.Inventors: Marcin KOŁACZKOWSKI, Piotr KOWALSKI, Jolanta Jaskowska, Monika MARCINKOWSKA, Katarzyna MITKA, Adam BUCKI, Anna WESOŁOWSKA, Maciej PAWŁOWSKI
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Publication number: 20140336170Abstract: The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.Type: ApplicationFiled: July 23, 2014Publication date: November 13, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Xuqing Zhang, Marta C. Abad, Alan C. Gibbs, Gee-Hong Kuo, Fengbin Song, Zhihua Sui