Exactly Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/303)
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Patent number: 8921560Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: December 30, 2014Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Patent number: 8921377Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: GrantFiled: March 27, 2013Date of Patent: December 30, 2014Assignee: Bayer Intellectual Property GmbHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Walter Kroh, Andreas Knorr, Eva-Maria Becker, Frank Wunder, Volkhart Min-Jian Li, Elke Hartmann, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat, Donald Bierer
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Patent number: 8921391Abstract: This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.Type: GrantFiled: April 22, 2010Date of Patent: December 30, 2014Assignee: RaQualia Pharma Inc.Inventors: Yukinori Take, Shinichi Koizumi, Takako Okumura, Kazuhiko Nonomura
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Publication number: 20140378449Abstract: 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: ApplicationFiled: September 11, 2014Publication date: December 25, 2014Applicant: 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: 20140378447Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.Type: ApplicationFiled: September 4, 2014Publication date: December 25, 2014Inventors: Akihiro OKANO, Muneyoshi MAKABE, Kouki OGAWA
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Publication number: 20140378448Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.Type: ApplicationFiled: September 4, 2014Publication date: December 25, 2014Inventors: Akihiro OKANO, Muneyoshi MAKABE
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Patent number: 8916708Abstract: Compounds of formula (I) are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory wherein R1 is a radical of formula (IA) or (IB) or (IC): 10 Y is —O— or —S(O)p—wherein p is 0, 1 or 2; A is an optionally substituted cycloalkylene radical having 5, 6 or 7 ring atoms fused to a phenyl ring; and R2, R3b and R4b are as defined in the claims.Type: GrantFiled: June 9, 2011Date of Patent: December 23, 2014Assignee: Chiesi Farmaceutici S.p.A.Inventors: Chi-kit Woo, Monique Bodil Van Niel
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Publication number: 20140371238Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:Type: ApplicationFiled: March 13, 2014Publication date: December 18, 2014Applicant: FLATLEY DISCOVERY LABInventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
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Publication number: 20140371263Abstract: The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in particular cystic fibrosis, comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:Type: ApplicationFiled: March 13, 2014Publication date: December 18, 2014Applicant: FLATLEY DISCOVERY LABInventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
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Patent number: 8912330Abstract: This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: December 11, 2009Date of Patent: December 16, 2014Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Jiwei Qi, Yihan Wang, Feng Li, William C. Shakespeare, Anna Kohlmann, David C. Dalgarno, Xiaotian Zhu
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Patent number: 8912181Abstract: A novel bicyclic compound having an HSP90 inhibitory effect and a carcinostatic effect. A pharmaceutical agent based on the HSP90 inhibitory effect and useful in the prevention and/or treatment of a disease involving HSP90, particularly cancer. The compound has a general formula (I) or is a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are each independently C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are each independently CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.Type: GrantFiled: January 6, 2012Date of Patent: December 16, 2014Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
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Publication number: 20140364444Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.Type: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Hayato TAKYO, Masaki TAKAHASHI, Takamasa TANABE, Yoshihiko NOKURA, Mai ITO, Atsushi IWATA
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Publication number: 20140364438Abstract: Provided is a novel triazolopyridine derivative having irreversible tyrosine kinase inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of inflammatory diseases, autoimmune diseases, proliferative diseases or hyperproliferative diseases, immunologically mediated diseases, cancers or tumors.Type: ApplicationFiled: January 23, 2013Publication date: December 11, 2014Applicant: HANMI PHARM. CO., LTD.Inventors: Jae Yi Sim, Kyung Ik Lee, Ho Seok Kim, Tae Hee Ha, Kwee Hyun Suh
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Publication number: 20140364441Abstract: Novel [1,2,4]triazolo[1,5-a]pyridinyl-6-yl-substituted tetrahydroisoquinolines are described in the present invention. These compounds and crystalline forms SA1 and N-2 are used in the treatment of various neurological and physiological disorders. Methods of making these compounds and crystalline forms SA-1 and N-2 are also described in the present invention.Type: ApplicationFiled: August 22, 2014Publication date: December 11, 2014Inventors: Chenkou Wei, Victor W. Rosso, Qi Gao
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Publication number: 20140364411Abstract: Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: June 5, 2014Publication date: December 11, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Chi-Kit WOO, Lilian ALCARAZ, Carmelida CAPALDI
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Publication number: 20140364450Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: April 15, 2014Publication date: December 11, 2014Inventors: Juan-Miguel Jimenez, Philip Collier, Gregory Henkel, Michael Liu, Timothy Neuberger, Jeremy Green
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Publication number: 20140364412Abstract: Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tractType: ApplicationFiled: June 5, 2014Publication date: December 11, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Lilian Alcaraz, Christopher Hurley, Andrew Peter Cridland, Andrew Stephen Robert Jennings
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Publication number: 20140357633Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.Type: ApplicationFiled: December 12, 2012Publication date: December 4, 2014Inventors: Daniel Ford, John Robert Porter, Michael Scott Visser, Naeem Yusuff
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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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Publication number: 20140357623Abstract: 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3-aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4-(dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboType: ApplicationFiled: September 14, 2011Publication date: December 4, 2014Applicant: PROXIMAGEN LIMITEDInventors: David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
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Publication number: 20140357617Abstract: The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.Type: ApplicationFiled: August 20, 2014Publication date: December 4, 2014Applicant: FAB PHARMA S.A.S.Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Alexis Denis
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Publication number: 20140357663Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.Type: ApplicationFiled: August 21, 2014Publication date: December 4, 2014Inventors: Caroline SPRINGER, Ion NICULESCU-DUVAZ, Richard MARAIS, Dan NICULESCU-DUVAZ, Alfonso ZAMBON, Delphine MENARD
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Publication number: 20140357650Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.Type: ApplicationFiled: January 17, 2013Publication date: December 4, 2014Applicant: Fox Chase Cancer CenterInventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
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Publication number: 20140357618Abstract: The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.Type: ApplicationFiled: August 21, 2014Publication date: December 4, 2014Inventors: Matthew P. Christopher, Francesc Xavier Fradera Llinas, Michelle Machacek, Michelle Martinez, Michael Hale Reutershan, Manami Shizuka, Binyuan Sun, Christopher Francis Thompson, B. Wesley Trotter, Matthew E. Voss, Michael D. Altman, Stephane L. Bogen, Ronald J. Doll
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Patent number: 8901309Abstract: The present invention provides a heterocycle derivative having a superior amyloid ? production inhibitory activity and/or a superior ?-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.Type: GrantFiled: September 1, 2011Date of Patent: December 2, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Tatsuki Koike, Minoru Nakamura, Takafumi Takai, Yuichi Kajita, Makoto Kamata
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Patent number: 8901136Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: GrantFiled: June 6, 2013Date of Patent: December 2, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mitzutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
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Publication number: 20140349990Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 20, 2014Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Jutta BLANK, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
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Publication number: 20140350011Abstract: This application relates to compounds of the Formula I as defined herein, and/or salts thereof. This application further relates to compositions and methods of using these compounds and/or salts thereof. The compounds of Formula I are useful as ALK and JAK modulators for the treatment of proliferative disorders.Type: ApplicationFiled: July 30, 2014Publication date: November 27, 2014Inventors: Henry J. Breslin, Matthew A. Curry, Diane E. Gingrich, Keith S. Learn, Gregory R. Ott, Jason C. Wagner
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Publication number: 20140350002Abstract: The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are 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.Type: ApplicationFiled: June 14, 2012Publication date: November 27, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Hannah D. Fiji, Michael J. Kelly, III, Jeffrey C. Kern, Mark E. Layton, Joseph E. Pero, Alexander J. Reif, Michael A. Rossi
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Publication number: 20140350006Abstract: The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.Type: ApplicationFiled: December 13, 2012Publication date: November 27, 2014Inventors: Chantal Alcouffe, Kirsten Bjegarde, Jacques Mauger
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Publication number: 20140350046Abstract: The present invention relates to novel pyrazolopyridinone derivatives according to formula (I) and a process of manufacturing thereof. These pyrazolopyridinone derivatives can be used as LPA receptor antagonists for the treatment of various herein disclosed diseases.Type: ApplicationFiled: August 6, 2014Publication date: November 27, 2014Applicant: Merck Patent GmbHInventors: Kai SCHIEMANN, Wolfgang STAEHLE, SR., Dirk WIENKE
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Patent number: 8895544Abstract: A method of treating a disease or condition for which a JAK inhibitor is indicated in a subject in need of such treatment, comprising administering to the subject a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, and particularly, a method for the treatment of various inflammatory diseases, particularly psoriasis, asthma and COPD.Type: GrantFiled: September 30, 2013Date of Patent: November 25, 2014Assignee: Pfizer LimitedInventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Steven Wade Korturn, Yogesh Anil Sabnis, Florian Michel Wakenhut, Gavin Alistair Whitlock
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Patent number: 8895550Abstract: Provided herein are methods of treating diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases by administering to a mammal in need thereof a therapeutically effective amount of a compound of Formula I: in which B, R1, R1a, R2, R3, R4, R5, R6, R7, R10 and R11 have the meanings given in the specification.Type: GrantFiled: October 15, 2013Date of Patent: November 25, 2014Assignee: Array BioPharma Inc.Inventors: Shelley Allen, Robert Kirk DeLisle, Julie Marie Hicks, Erik James Hicken, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, John E. Robinson, Qian Zhao
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Publication number: 20140343065Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.Type: ApplicationFiled: May 12, 2014Publication date: November 20, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Riccardo GIOVANNINI, Yunhai CUI, Henri DOODS, Marco FERRARA, Stefan JUST, Raimund KUELZER, Iain LINGARD, Rocco MAZZAFERRO, Klaus RUDOLF
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Publication number: 20140343056Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: September 12, 2012Publication date: November 20, 2014Applicant: GlaxoSmithKline LLCInventors: Joelle Lorraine Burgess, Neil W. Johnson, Steven David Knight, Louis Vincent LaFrance, III, William Henry Miller, Kenneth Allen Newlander, Stuart Paul Romeril, Meagan B. Rouse, Dominic Suarez, Xinrong Tian, Sharad Kumar Verma
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Publication number: 20140343055Abstract: Compounds of formula (I): wherein R2, W, A, Y, and R1 are as defined in the specification, and pharmaceutically acceptable salts thereof, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Applicant: Chiesi Farmaceutici S.p.AInventors: Monique Bodil Van Niel, Nicholas Charles Ray, Andrew Peter Cridland, Christopher Hurley, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani
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Publication number: 20140343092Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).Type: ApplicationFiled: September 18, 2012Publication date: November 20, 2014Inventors: Simon N. Haydar, Brian Alvin Johns, Emile Johann Velthuisen
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Publication number: 20140343053Abstract: The present invention is directed to triazolopyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: November 9, 2012Publication date: November 20, 2014Applicant: Merck Sharpe & Dohme Corp.Inventors: James C. Barrow, Christopher D. Cox, Mark B. Nolt, William D. Shipe
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Patent number: 8889711Abstract: The present invention concerns compounds of following general formula (I): (Formula I) and their pharmaceutically acceptable salts, their method of preparation and their uses, notably as anticancer agent.Type: GrantFiled: October 13, 2010Date of Patent: November 18, 2014Assignee: Pierre Fabre MedicamentInventors: Karim Bedjeguelal, Rémi Rabot, El Bachir Kaloun, Patrice Mayer, Arnaud Marchand, Nicolas Rahier, Philippe Schambel, Hugues Bienayme
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Patent number: 8889704Abstract: Compounds of Formula I: in which R1, R2, R3, R4 and R10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.Type: GrantFiled: February 24, 2012Date of Patent: November 18, 2014Assignee: Array BioPharma Inc.Inventors: James F. Blake, Robert Kirk Delisle, Lisa A. De Meese, James M. Graham, Yvan Le Huerou, Michael Lyon, John E. Robinson, Eli M. Wallace, Bin Wang, Rui Xu
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Publication number: 20140335178Abstract: The present invention relates to a Factor Xa inhibitor dosage form comprising apixaban in a solubility-improved form wherein the dosage form provides controlled release of apixaban and methods for preventing or treating venous thromboembolisms, deep vein thrombosis and acute coronary syndrome with said dosage form.Type: ApplicationFiled: May 19, 2014Publication date: November 13, 2014Applicants: BRISTOL-MYERS SQUIBB COMPANY, PFIZER INC.Inventor: Richard G. Nause
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Patent number: 8883822Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.Type: GrantFiled: May 3, 2013Date of Patent: November 11, 2014Assignee: Samumed, LLCInventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Patent number: 8883820Abstract: The invention relates to compounds of formula (I); wherein X and R1 to R5 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of Itk or PI3K, for the treatment or prophylaxis of immunological, inflammatory or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.Type: GrantFiled: August 30, 2007Date of Patent: November 11, 2014Assignee: Cellzome Ltd.Inventors: Francis Wilson, Nigel Ramsden, Kathryn Bell, Andrew Cansfield, Svenja Burckhardt, Jess Taylor, Mihiro Sunose, David Middlemiss
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Patent number: 8883821Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.Type: GrantFiled: November 27, 2012Date of Patent: November 11, 2014Assignee: Pierre Fabre MedicamentInventors: El Bachir Kaloun, Karim Bedjeguelal, Rémi Rabot, Anna Kruczynski, Philippe Schmitt, Michel Perez, Nicolas Rahier
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Publication number: 20140329755Abstract: The present invention relates to method of treating arrhythmias or heart failure comprising co-administration of a late INa inhibitor and a CAMK II inhibitor.Type: ApplicationFiled: April 30, 2014Publication date: November 6, 2014Applicant: Gilead Sciences, Inc.Inventors: Luiz Belardinelli, Peidong Fan, Faquan Liang, Lina Yao
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Publication number: 20140329853Abstract: The present invention relates to novel [1,2,4]triazolopyridine compounds with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.Type: ApplicationFiled: December 19, 2012Publication date: November 6, 2014Inventors: Simon Feldbæk Nielsen, Jens Christian Højland Larsen
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Publication number: 20140329807Abstract: The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.Type: ApplicationFiled: July 20, 2012Publication date: November 6, 2014Applicant: TOLERO PHARMACEUTICALS, INC.Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael Saunders, Koc-Kan Ho
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Publication number: 20140329852Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: July 15, 2014Publication date: November 6, 2014Inventors: Liming Wang, Mohammed I. Dibas, Michael E. Garst, KEN CHOW, Santosh C. Sinha
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Patent number: 8877779Abstract: Provided is an ORL-1 receptor agonist having improved bioavailability based on superior metabolic stability and strong and high selectivity, as compared to conventional compounds. A compound represented by the formula (I) wherein each symbol is as defined in the claims.Type: GrantFiled: February 28, 2008Date of Patent: November 4, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masakazu Nakano, Masanori Minoguchi, Tokushi Hanano, Shin-ichiro Ono, Hideki Horiuchi, Koji Teshima
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Publication number: 20140323479Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:Type: ApplicationFiled: July 15, 2014Publication date: October 30, 2014Inventors: John Hood, Sunil Kumar KC, David Mark Wallace