Ring Oxygen In The Bicyclo Ring System Patents (Class 546/115)
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Publication number: 20120329772Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.Type: ApplicationFiled: July 9, 2012Publication date: December 27, 2012Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biqin C. Li
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Publication number: 20120322784Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: December 16, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Matthias ECKHARDT, Niklas HEINE, Elke LANGKOPF, Bernd NOSSE
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Patent number: 8334236Abstract: Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C?O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.Type: GrantFiled: February 2, 2010Date of Patent: December 18, 2012Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Fumiaki Takabe, Yuuki Hirano, Akira Funyu, Masami Kobayashi, Takashi Mitsunari
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Publication number: 20120313083Abstract: Provided are an organic compound having high heat stability suitable for use in an organic light-emitting device, and an organic light-emitting device using the organic compound. The organic light-emitting device is an organic light-emitting device, including: an anode; a cathode; and an organic compound layer disposed between the anode and the cathode, in which at least one layer of the organic compound layer has a 6,12-dinaphthylchrysene derivative represented by one of the following general formulae (1) and (2): in the formulae (1) and (2), Z represents a naphthyl group, and Q represents an electron-withdrawing substituent selected from the group consisting of the following general formulae (3) to (5): in the formula (5), R1 represents a hydrogen atom or a methyl group.Type: ApplicationFiled: May 25, 2012Publication date: December 13, 2012Applicant: CANON KABUSHIKI KAISHAInventors: Hironobu Iwawaki, Hiroki Ohrui, Yuko Chishina, Masanori Muratsubaki, Tetsuo Takahashi
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Publication number: 20120309739Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: November 3, 2010Publication date: December 6, 2012Applicant: ALMAC DISCOVERY LIMITEDInventors: Mark Peter Bell, Colin Roderick O'Dowd, James Samuel Shane Rountree, Graham Peter Trevitt, Timothy Harrison, Mary Melissa McFarland
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Publication number: 20120306727Abstract: Provided are a fused polycyclic compound suitable for use mainly as a component for a blue-light-emitting device, and an organic light-emitting device using the compound. The fused polycyclic compound is represented by the general formulae (1), (2), (8) and (9).Type: ApplicationFiled: May 1, 2012Publication date: December 6, 2012Applicant: CANON KABUSHIKI KAISHAInventors: Hiroki Ohrui, Hironobu Iwawaki, Kei Tagami, Masanori Muratsubaki, Ryuji Ishii
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Patent number: 8324387Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: GrantFiled: December 30, 2011Date of Patent: December 4, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsuhiko Iwakoshi, Ippei Uemura
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Patent number: 8324239Abstract: The present invention provides a compound of formula I; 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: GrantFiled: April 19, 2011Date of Patent: December 4, 2012Assignee: Novartis AGInventors: David Barnes, Rajiv Chopra, Scott Louis Cohen, Jiping Fu, Mitsunori Kato, Peichao Lu, Mohindra Seepersaud, Wei Zhang
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Publication number: 20120301427Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HW).Type: ApplicationFiled: January 25, 2012Publication date: November 29, 2012Inventors: Gary BRIDGER, Al KALLER, Curtis HARWIG, Renato SKERLJ, David BOGUCKI, Trevor R. WILSON, Jason CRAWFORD, Ernest J. MCEACHERN, Bem ATSMA, Siqiao NAN, Yuanxi ZHOU, Dominique SCHOLS, Christopher D. SMITH, Maria R. DI FLURI
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Publication number: 20120270864Abstract: The present invention relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation.Type: ApplicationFiled: May 18, 2012Publication date: October 25, 2012Inventors: Andrew Aydon Godfrey, Janelle Comita-Prevoir, Mark Cronin, Bolin Geng, Folkert Reck
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Patent number: 8288548Abstract: The present invention provides oxazolo[5,4-b]pyridin-5-yl compounds useful in the treatment of cancer.Type: GrantFiled: November 17, 2011Date of Patent: October 16, 2012Assignee: Eli Lilly and CompanyInventors: David Andrew Coates, Raymond Gilmour, Jose Alfredo Martin, Eva Maria Martin de la Nava
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Patent number: 8283360Abstract: The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: December 18, 2009Date of Patent: October 9, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Anandan Palani, Ashwin U. Rao, Xiao Chen, Ning Shao, Ying R. Huang, Robert G. Aslanian
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Publication number: 20120252807Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of arboviruses.Type: ApplicationFiled: March 19, 2012Publication date: October 4, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Scott Larsen, Janice Sindac, Scott Barraza, David J. Miller
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Publication number: 20120245167Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: ApplicationFiled: April 17, 2012Publication date: September 27, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Mitsuhiko IWAKOSHI, Ippei UEMURA
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Publication number: 20120238559Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: December 3, 2010Publication date: September 20, 2012Applicant: GLAXO GROUP LIMITEDInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Patent number: 8269008Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.Type: GrantFiled: December 2, 2008Date of Patent: September 18, 2012Assignee: FibroGen, Inc.Inventors: Michael P. Arend, Heng Cheng, Lee A. Flippin, Danny Ng, Eric D. Turtle, Min Wu
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Publication number: 20120232099Abstract: The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: May 14, 2012Publication date: September 13, 2012Inventors: Richard Pracitto, John F. Kadow, John A. Bender, Brett R. Beno, Katherine A. Grant-Young, Ying Han, Piyasena Hewawasam, Andrew Nickel, Kyle E. Parcella, Kap-Sun Yeung, Louis S. Chupak
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Publication number: 20120226035Abstract: Disclosed is a compound represented by the general formula: wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom, or a salt thereof, which is useful as an antibacterial agent.Type: ApplicationFiled: May 10, 2012Publication date: September 6, 2012Applicants: Taisho Pharmaceutical Co., Ltd., Toyama Chemical Co., Ltd.Inventors: Taro KIYOTO, Junichi Ando, Tadashi Tanaka, Yasuhiro Tsutsui, Mai Yokotani, Toshiya Noguchi, Fumihito Ushiyama, Hiroki Urabe, Hiromasa Horikiri
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Publication number: 20120214990Abstract: A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Applicants: TAISHO PHARMACEUTICAL CO., LTD., TOYAMA CHEMICAL CO., LTD.Inventors: Taro KIYOTO, Tadashi Tanaka, Yasuhiro Tsutsui, Junichi Ando, Mai Motono, Yasuko Kawaguchi, Toshiya Noguchi, Yasunobu Ushiki, Fumihito Ushiyama, Hiroki Urabe
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Publication number: 20120208820Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: ApplicationFiled: January 31, 2012Publication date: August 16, 2012Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20120202815Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Y is a 5-membered, fully or partially unsaturated heterocyclic ring containing 2-4 carbon atoms and 2-3 nitrogen atoms as ring members, the ring substituted with Z on a ring member atom connected through an adjacent single ring member atom to the ring member atom attaching the heterocyclic ring to the phenyl ring of Formula 1, and optionally further substituted with up to 2 substituents independently selected from R5 on carbon atom ring members and from R6 on nitrogen atom ring members; Z is an 8-, 9-, 10- or 11-membered fused heterobicyclic ring system containing ring members selected from carbon atoms and 1 to 4 heteroatoms independently selected from up to 2O, up to 2S and up to 4 N atoms, wherein up to 3 carbon atom ring members are independently selected from C(?O) and C(?S), and the sulfur atom ring members are independently selected from S(?O)u(?NR7)z, the ring system optionally substituted wiType: ApplicationFiled: October 12, 2010Publication date: August 9, 2012Applicant: E.I.DU PONT DE NEMOURS AND COMPANYInventors: John Lawrence Andreassi II, Andrew Edmund Taggi
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Publication number: 20120202786Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: ApplicationFiled: April 16, 2012Publication date: August 9, 2012Applicant: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
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Publication number: 20120190709Abstract: This invention relates to novel 4-(indazol-5-yl)-4,7-dihydroisoxazolo[5,4-b]pyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: ApplicationFiled: July 7, 2010Publication date: July 26, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Martin Michels, Markus Follman, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Mario Lobell
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Publication number: 20120183496Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: ApplicationFiled: December 16, 2011Publication date: July 19, 2012Applicant: COCRYSTAL DISCOVERY, INC.Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Publication number: 20120178829Abstract: The instant invention pertains to novel bi- or tricyclic sterically hindered alkoxyamines, their precursors, a process for their preparation and their use as light stabilizers for polymers or coatings, as flame retardants, as peroxide substitutes (rheology modifiers) or carbon radical scavengers.Type: ApplicationFiled: August 3, 2010Publication date: July 12, 2012Applicant: BASF SEInventors: Stefan Hauck, Walter Fischer, Kai-Uwe Schoening
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Patent number: 8211890Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy (notably methoxy); R2 represents H or F; each of R3, R4, R5 and R6 represents independently H or D; V represents CH and W represents CH or N, or V represents N and W represents CH; Y represents CH or N; Z represents O, S or CH2; and A represents CH2, CH2CH2 or CD2CD2; and salts of such compounds.Type: GrantFiled: December 11, 2009Date of Patent: July 3, 2012Assignee: Actelion PharmaceuticalsInventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20120157440Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4, n, and R7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: December 13, 2011Publication date: June 21, 2012Inventors: TODD W. BUTLER, Ramalakshmi Y. Chandrasekaran, Scot R. Mente, Chakrapani Subramanyam, Travis T. Wager
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Publication number: 20120149718Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: ApplicationFiled: December 13, 2011Publication date: June 14, 2012Inventors: Christine E. Brotherton-Pleiss, Keith A. M. Walker
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Publication number: 20120142724Abstract: The present invention provides oxazolo[5,4-b]pyridin-5-yl compounds useful in the treatment of cancer.Type: ApplicationFiled: November 17, 2011Publication date: June 7, 2012Applicant: Eli Lilly and CompanyInventors: David Andrew Coates, Raymond Gilmour, Jose Alfredo Martin, Eva Maria Martin de la Nava
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Patent number: 8193359Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes.Type: GrantFiled: December 23, 2005Date of Patent: June 5, 2012Assignee: Prosidion LimitedInventors: Matthew Colin Thor Fyfe, Gerard Hugh Thomas, Lisa Sarah Bertram, Stuart Edward Bradley, William Gattrell, Chrystelle Marie Rasamison, Vilasben Kanji Shah
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Publication number: 20120129856Abstract: The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.Type: ApplicationFiled: October 18, 2011Publication date: May 24, 2012Applicant: Cerenis Therapeutics SAInventors: Daniela Carmen Oniciu, Jean-Louis Henri Dasseux, Ronald Barbaras, Valery Kochubey, Dmitry Kovalsky, Oleg Gennadievich Rodin, Otto Geoffroy, Anna Rzepiela
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Patent number: 8178553Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: GrantFiled: January 20, 2010Date of Patent: May 15, 2012Assignee: Schering CorporationInventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta Maria Kosinski, Seong-Heon Kim, De-Yi Yang, Razia K. Rizvi
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Publication number: 20120108586Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: ApplicationFiled: December 30, 2011Publication date: May 3, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Mitsuhiko IWAKOSHI, Ippei UEMURA
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Publication number: 20120101101Abstract: Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: April 28, 2010Publication date: April 26, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Noriaki Uesaka, Takashi Sawada, Tomoyuki Kanda
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Patent number: 8163901Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: GrantFiled: January 9, 2009Date of Patent: April 24, 2012Assignee: Evotec AGInventors: Matthew Duncton, Donogh John Roger O'Mahony, Matthew Cox, Maria De Los Angeles Estiarte-Martinez
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Publication number: 20120095075Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells.Type: ApplicationFiled: August 16, 2011Publication date: April 19, 2012Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah MANOHARAN, Kallanthottathil G. Rajeev, David Butler, Narayanannair K. Jayaprakash, Muthusamy Jayaraman, Laxman Eltepu
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Patent number: 8153634Abstract: [Object] To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.Type: GrantFiled: May 29, 2009Date of Patent: April 10, 2012Assignee: Kowa Company, Ltd.Inventors: Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Takayuki Matsuda, Ayumu Okuda, Hisashi Sumida, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya
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Publication number: 20120059019Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: March 9, 2011Publication date: March 8, 2012Inventors: Kap-Sun Yeung, Katharine A. Grant-Young, John F. Kadow
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Publication number: 20120053132Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: November 1, 2011Publication date: March 1, 2012Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan
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Publication number: 20120046267Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.Type: ApplicationFiled: February 11, 2011Publication date: February 23, 2012Inventors: Keith R. Hornberger, Dan M. Berger, Xin Chen, Andrew P. Crew, Hanqing Dong, Andrew Kleinberg, An-Hu Li, Lifu Ma, Mark J. Mulvihill, Bijoy Panicker, Kam W. Siu, Arno G. Steinig, James G. Tarrant, Jing Wang, Qinghua Weng, Rajaram Sangem, Ramesh C. Gupta
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Patent number: 8119635Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: August 19, 2009Date of Patent: February 21, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Patent number: 8119806Abstract: A compound having the structure wherein X is selected from the group consisting of: a bond, —NHCH2(CH2)nCH2OC(O)—, —CH2NHC(O)CH2NHC(O)—, —CH2OC(O)—, —OCH(CH3)OC(O)—, —OCH2OC(O)—, —O—, —NR1—, —CR1R3—, —(CH2)p—, —(CH2)qNR1C(O)—, —CHR5NR2C(O)—, —(CH2)qC(O)—, —(CH2)qC(O)NR1—, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: GrantFiled: July 27, 2009Date of Patent: February 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Iyassu K. Sebhat, Christopher L. Franklin, Kathleen M. Rupprecht, Robert K. Baker, Ravi P. Nargund, Lin Yan, Pei Huo, Dong-Ming Shen, Nicoletta Almirante, Stefano Biondi, Massimiliano Ferrario, Alessia Nicotra
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Publication number: 20120040989Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy; each of U and V represents CH and W represents CH or N, or U represents N, V represents CH and W represents N, or each of U and V represents N and W represents CH; R2 represents hydrogen or fluorine when W represents CH or R2 represents hydrogen when W represents N; A represents O or CH2; Y represents CH or N; Q represents O or S; and n represents 0 or 1; and salts of such compounds.Type: ApplicationFiled: April 8, 2010Publication date: February 16, 2012Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
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Publication number: 20120028940Abstract: In its many embodiments, the present invention provides a novel class of azanitrile compounds as inhibitors of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: September 15, 2009Publication date: February 2, 2012Applicant: MERCK SHARP & DOHME CORP.Inventors: Christopher W. Boyce, Jianhua Chao, Kevin D. McCormick
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Publication number: 20120027796Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).Type: ApplicationFiled: November 10, 2009Publication date: February 2, 2012Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, David Butler, Jayaprakash K. Narayanannair, Muthusamy Jayaraman, Laxmab Eltepu
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Publication number: 20120029190Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, psychiatric disorders, neuro-muscular disorders, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds provided herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: April 1, 2010Publication date: February 2, 2012Inventors: Douglas Burdi, Kerry L. Spear, Larry Wendell Hardy
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Patent number: 8101632Abstract: Compounds are disclosed. The compounds act as MCH1 modulators. Other embodiments are also disclosed.Type: GrantFiled: January 9, 2008Date of Patent: January 24, 2012Assignee: Albany Molecular Research, Inc.Inventors: Peter Robert Guzzo, Matthew David Surman
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Publication number: 20120015926Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: November 9, 2009Publication date: January 19, 2012Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K.C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
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Publication number: 20120015907Abstract: The present invention provides a compound of formula I; 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: April 19, 2011Publication date: January 19, 2012Applicant: NOVARTIS AGInventors: David BARNES, Rajiv CHOPRA, Scott Louis COHEN, Jiping FU, Mitsunori Kato, Peichao LU, Mohindra SEEPERSAUD, Wei ZHANG
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Publication number: 20110319434Abstract: The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: December 18, 2009Publication date: December 29, 2011Applicant: Schering Plough CorporationInventors: Anandan Palani, Ashwin U. Rao, Xiao Chen, Ning Shao, Ying R. Huang, Robert G. Aslanian