Polycyclo Ring System Having One Of The Two Rings Which Form The Spiro As One Of The Cyclos Patents (Class 546/17)
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Patent number: 8329718Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.Type: GrantFiled: April 16, 2010Date of Patent: December 11, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer X. Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
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Publication number: 20120309778Abstract: The invention relates to fused and spirocycle compounds of Formula (I), or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1, R2, Q1-Q3, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: June 1, 2012Publication date: December 6, 2012Applicant: Purdue Pharma L.P.Inventors: Zhengming CHEN, Laykea TAFESSE, Jiangchao YAO, Khondaker ISLAM
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Publication number: 20120295931Abstract: This invention relates to spiroindoline compounds for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: February 4, 2011Publication date: November 22, 2012Inventors: Jürgen Lutz, Sandra Koch, Manfred Uphoff, Anja Regina Heckeroth, Britta von Oepen, Ulrich Sonderin, Christophe Pierre Alain Chassaing
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Publication number: 20120283243Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: ApplicationFiled: July 11, 2012Publication date: November 8, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis J. Hurley, Ioana Drutu, Gabriel Raffai, Daniele M. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
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Patent number: 8304423Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: June 29, 2011Date of Patent: November 6, 2012Assignee: Vertex Pharmaceutical IncorporatedInventors: Robert J. Davies, Jinwang Xu
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Publication number: 20120277150Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is 0 or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: April 11, 2012Publication date: November 1, 2012Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Munetaka OHKOUCHI
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Publication number: 20120270893Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: April 21, 2012Publication date: October 25, 2012Applicant: PFIZER INC.Inventors: Robert Lee Dow, David James Edmonds, David Andrew Griffith, James Alfred Southers, JR.
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Patent number: 8293900Abstract: Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: September 25, 2006Date of Patent: October 23, 2012Assignee: Merck Sharp & Dohme CorpInventors: Tianying Jian, Jian Liu, Ravi P. Nargund
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Patent number: 8288405Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: GrantFiled: November 8, 2010Date of Patent: October 16, 2012Assignee: Pfizer Inc.Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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Publication number: 20120258949Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C?R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.Type: ApplicationFiled: April 13, 2012Publication date: October 11, 2012Applicant: DAC S.r.I.Inventors: Mario Varasi, Florian Thaler, Raffaella Amici, Agnese Abate, Maria Carmela Fulco, Saverio Minucci, Ciro Mercurio
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Patent number: 8278318Abstract: The present invention relates to certain spirocyclic compounds that are inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 (11?HSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases.Type: GrantFiled: June 20, 2008Date of Patent: October 2, 2012Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Colin Zhang
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Publication number: 20120245136Abstract: The invention relates to chroman spirocyclic piperidine amide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: February 16, 2012Publication date: September 27, 2012Inventors: Sara Sabina HADIDA-RUAH, Mark Thomas Miller, Edward Adam Kallel, Brian Richard Bear, Vijayalaksmi Arumugam, Michael Paul Deninno, Jinglan Zhou, Johnny Uy, Bryan A. Frieman
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Patent number: 8263592Abstract: The present invention is related to novel compounds of formula (I) having equilibrative nucleoside transporter ENT1 inhibiting properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the inhibition of ENT1 receptors in animals, in particular humans.Type: GrantFiled: November 13, 2008Date of Patent: September 11, 2012Assignee: Janssen Pharmaceutica NVInventors: Jean-Paul René Marie André Bosmans, Didier Jean-Claude Berthelot, Serge Maria Aloysius Pieters, Bie Maria Pieter Verbist, Michel Anna Jozef De Cleyn
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Patent number: 8263608Abstract: Melanocortin receptor-specific compounds of formula I below: wherein the variables are as defined in the specification, and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders.Type: GrantFiled: March 29, 2011Date of Patent: September 11, 2012Assignee: Palatin Technologies, Inc.Inventors: Yi-Qun Shi, John H. Dodd, Elizabeth G. Rowley, Gary L. Olson, Axel Metzger
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Publication number: 20120225900Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: October 28, 2010Publication date: September 6, 2012Applicant: PFIZER INC.Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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Publication number: 20120220616Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition, and a method for treating diabetes.Type: ApplicationFiled: November 19, 2010Publication date: August 30, 2012Applicant: ELI LILLY AND COMPANYInventors: Chafiq Hamdouchi, Jayana Pankaj Lineswala, Pranab Maiti
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Publication number: 20120214784Abstract: An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described. ORL-1 antagonists are deemed to be useful in the treatment of depression and/or the treatment of overweight, obesity, and/or weight maintenance post treatment for overweight or obesity. Certain compounds have also demonstrated through animal models that the compounds of the present invention are useful for the treatment of migraines.Type: ApplicationFiled: November 12, 2010Publication date: August 23, 2012Applicant: ELI LILLY AND COMPANYInventors: Ana Belen Benito Collado, Nuria Diaz Buezo, Alma Maria Jimenez-Aguado, Celia Lafuente Blanco, Maria Angeles Martinez-Grau, Concepcion Pedregal Tercero, Miguel Angel Toledo Escribano
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Publication number: 20120202837Abstract: Renin inhibitors which are spirocyclic piperidine derivatives, of formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, wherein: n, for each instance in which it occurs, is independently 0, 1, or 2; W is a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring, A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a first five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to a second five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is —(C?O)—, —CH2— or ?CH—; U is a bond or —CH2-, or, when V iS ?CH—, U is —CH?; X is ?CH—, ?CF—, ?C(OR3)—, or —(C?O)—; and Y is ?CH—, ?CF—, ?N—, or, for the case when X is —(C?O)—, Y is —N(R3)—.Type: ApplicationFiled: October 12, 2010Publication date: August 9, 2012Inventors: Austin Chen, Reneé Aspiotis, Daniel McKay, Yongxin Han, Pierre-André Fournier
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Patent number: 8232289Abstract: An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described.Type: GrantFiled: November 10, 2010Date of Patent: July 31, 2012Assignee: Eli Lilly and CompanyInventors: Ana Belen Benito Collado, Nuria Diaz Buezo, Alma Maria Jimenez-Aguado, Celia Lafuente Blanco, Maria Angeles Martinez-Grau, Concepcion Pedregal-Tercero, Miguel Angel Toledo Escribano
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Patent number: 8232409Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.Type: GrantFiled: October 9, 2009Date of Patent: July 31, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Mark R. Player, Daniel J. Parks, William Parsons, Sanath K. Meegalla, Carl R. Illig, Shelley K. Ballentine
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Publication number: 20120190701Abstract: Renin inhibitors, which are spirocyclic piperidine amides, of structural formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. wherein n, for each instance in which it occurs, is independently 0, 1, or 2; R1 is hydrogen, C1-6-alkyl or C3-6-cycloalkyl, wherein said C1-6-alkyl or C3-6-cycloalkyl group can be independently substituted with 1-3 halogens; A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to another five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is a bond or —(C?O)—, —CH(OH)—, —CH2—or ?CH—; U is a bond or —CH2-, or for the case when V is ?CH—, U is —CH?; X is ?CH—, ?CF—, ?C(OR3)—, or —C?O—; and Y is ?CH—, ?CF—, ?N—, or for the case when X is —C?O—, Y is —N(R3)—.Type: ApplicationFiled: August 17, 2010Publication date: July 26, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Austin Chih-Yu Chen, Sebastien Laliberte, Guillaume Larouche, Yongxin Han, Daniel McKay
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Substituted piperidine spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof
Patent number: 8227481Abstract: The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). wherein R1, R2, R3, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor are disclosed.Type: GrantFiled: June 2, 2011Date of Patent: July 24, 2012Assignee: SanofiInventors: Zhongli Gao, Daniel Hall, Ryan Hartung -
Publication number: 20120184525Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: ApplicationFiled: May 11, 2010Publication date: July 19, 2012Applicants: ADDEX PHARMA S.A., JANSSEN PHARMACEUTICALS, INCInventors: Jose Maria Cid-Nunez, Daniel Oehlrich, Andres Avelino Trabanco-Suarez, Gary John Tresadern, Juan Antonio Vega Ramiro, Gregor James MacDonald
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Patent number: 8217051Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt or ester thereof wherein X, Y, R1, R2 are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.Type: GrantFiled: January 7, 2010Date of Patent: July 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Jing Zhang, Zhuming Zhang
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Publication number: 20120165327Abstract: The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.Type: ApplicationFiled: March 1, 2012Publication date: June 28, 2012Inventors: Michael J. Costanzo, Stephen C. Yabut, Brett Tounge, Bruce E. Maryanoff, Han-Cheng Zhang
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Patent number: 8193208Abstract: The invention relates to fused and spirocycle compounds of Formula I: or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1, R2, Q1-Q3, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: September 8, 2006Date of Patent: June 5, 2012Assignee: Purdue Pharma L.P.Inventors: Zhengming Chen, Laykea Tafesse, Jiangchao Yao, Khondaker Islam
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Publication number: 20120122912Abstract: Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.Type: ApplicationFiled: July 21, 2010Publication date: May 17, 2012Inventors: Jean-Philippe Leclerc, Chun-Sing Li, Oscar Miguel Moradei
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Patent number: 8158792Abstract: The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.Type: GrantFiled: November 19, 2008Date of Patent: April 17, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Michael J. Costanzo, Stephen C. Yabut, Brett Tounge, Bruce E. Maryanoff, Han-Cheng Zhang
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Publication number: 20120077802Abstract: Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: June 9, 2010Publication date: March 29, 2012Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
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Publication number: 20120071467Abstract: Compounds or pharmacologically acceptable salts thereof are provided. In various embodiments the compounds have an antagonistic effect on a neurokinin NK1 receptor, a neurokinin NK2 receptor, and a muscarine M3 receptor. The compounds are useful as therapeutic agents for bronchial asthma, chronic obstructive pulmonary disease, or the like.Type: ApplicationFiled: September 16, 2011Publication date: March 22, 2012Applicant: Daiichi Sankyo Company, LimitedInventors: Takuya Ikeda, Takanori Yamazaki, Hiroshi Tsuchida
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Patent number: 8138206Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.Type: GrantFiled: May 29, 2006Date of Patent: March 20, 2012Assignee: MSD. K.K.Inventors: Shiho Ishikawa, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi, Shigeru Tokita, Toshihiro Wada
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Patent number: 8134001Abstract: There are provided compounds of the formula and pharmaceutically acceptable salts and esters thereof wherein W, V, X, Y, A, R and R? are as described herein. The compounds are useful as anticancer agents.Type: GrantFiled: November 18, 2008Date of Patent: March 13, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Qingjie Ding, Nan Jiang, Song Yang, Jing Zhang, Zhuming Zhang
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Publication number: 20120015933Abstract: The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.Type: ApplicationFiled: September 29, 2011Publication date: January 19, 2012Applicant: SANOFI-AVENTISInventors: Manfred SCHUDOK, Michael WAGNER, Armin BAUER, Anna KOHLMANN
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Publication number: 20120015928Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Publication number: 20120010135Abstract: The present invention provides spiro derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: March 30, 2010Publication date: January 12, 2012Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AGInventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Zaihui Zhang
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Publication number: 20110319378Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.Type: ApplicationFiled: June 3, 2011Publication date: December 29, 2011Applicant: AMGEN INC.Inventors: Michael David BARTBERGER, Ana GONZALEZ BUENROSTRO, Hilary Plake BECK, Xiaoqi CHEN, Richard Victor CONNORS, Jeffrey DEIGNAN, Jason DUQUETTE, John EKSTEROWICZ, Benjamin FISHER, Brian Matthew FOX, Jiasheng FU, Zice FU, Felix GONZALEZ LOPEZ DE TURISO, Michael GRIBBLE, JR., Darin James GUSTIN, Julie Anne HEATH, Xin HUANG, Xianyun JIAO, Michael G. JOHNSON, Frank KAYSER, David John KOPECKY, Sujen LAI, Yihong LI, Zhihong LI, Jiwen LIU, Jonathan Dante LOW, Brian Stuart LUCAS, Zhihua MA, Lawrence McGEE, Joel McINTOSH, Dustin McMINN, Julio Cesar MEDINA, Jeffrey Thomas MIHALIC, Steven Howard Olson, Yosup REW, Philip Marley ROVETO, Daqing SUN, Xiaodong WANG, Yingcai WANG, Xuelei YAN, Ming YU, Jiang ZHU
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Patent number: 8084609Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention are described with formula (I) wherein R1 to R5, R5?, R7 to R9, R7?, R8?, X and Y are as defined in the specification.Type: GrantFiled: December 13, 2007Date of Patent: December 27, 2011Assignee: Hoffman-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20110312952Abstract: Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.Type: ApplicationFiled: February 16, 2010Publication date: December 22, 2011Inventors: Nicolas Lachance, Jean-Philippe Leclerc, Chun Sing Li, Oscar Miguel Moradei
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Publication number: 20110306607Abstract: The invention relates to heterocyclic chromene-spirocyclic piperidine amides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: May 6, 2011Publication date: December 15, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Edward Adam Kallel, Mark Thomas Miller, Joseph Pontillo, Vijayalaksmi Arumugam, Nicole Hilgraf, Jason McCartney, Peter Diederik Jan Grootenhuis, Corey Anderson, Mehdi Numa, Bryan A. Frieman, Brian Richard Bear, James Philip Johnson, JR.
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Publication number: 20110288068Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.Type: ApplicationFiled: July 18, 2011Publication date: November 24, 2011Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
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Publication number: 20110280804Abstract: Compounds having the general formula III?, or IV? wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y is S; Z can be either H, O, S, S—R or NR where R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic, and heterocycliType: ApplicationFiled: June 1, 2011Publication date: November 17, 2011Applicants: The Board of Trustees of the Leland Stanford Junior University, University of MississippiInventors: Christopher R. McCurdy, Christophe Mesangeau, Frederick T. Chin, Michelle L. James, Bin Shen, Sanjiv Gambhir
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Publication number: 20110281903Abstract: There are disclosed bicyclic heterocyclic spiro compounds; pharmaceutical compositions comprising these compounds; and methods for the treatment in a mammal of diseases and conditions which are susceptible to modulation of the M1 muscarinic receptor, including Alzheimer's disease, insulin resistance syndrome and type 2 diabetes. Other embodiments are also disclosed.Type: ApplicationFiled: January 26, 2010Publication date: November 17, 2011Inventors: Abraham Fisher, Nira Bar-Ner, Victoria Nachum
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Publication number: 20110263519Abstract: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.Type: ApplicationFiled: July 5, 2011Publication date: October 27, 2011Applicant: JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINEInventors: Philip A. Beachy, James K. Chen, Anssi Jussi Nikolai Taipale
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Patent number: 8003660Abstract: The present invention relates to benzo-spiro-azaheterocyclic compounds of formula I, wherein R1, R2a, Rsb, R3, R?3, R4, R?4, m, n, q and p are define herein. The compounds of this invention are useful as modulators of muscarinic receptors.Type: GrantFiled: February 22, 2007Date of Patent: August 23, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Davies, Jingwang Xu
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Publication number: 20110201629Abstract: There are described cyclohexyl amide derivatives of Formula I, which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.Type: ApplicationFiled: January 31, 2011Publication date: August 18, 2011Inventors: Benjamin Atkinson, David Beattie, Andrew James Culshaw, James Dale, Nicholas James Devereux, Jeffrey McKenna
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Publication number: 20110196149Abstract: A method for the fluoridation of an iodonium salt with a fluoride ion source which can be carried out in an aqueous reaction solvent.Type: ApplicationFiled: April 18, 2011Publication date: August 11, 2011Applicant: GE HEALTHCARE LIMITEDInventors: HARRY JOHN WADSWORTH, PETER ANTHONY DEVENISH
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Publication number: 20110178001Abstract: The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.Type: ApplicationFiled: August 10, 2009Publication date: July 21, 2011Applicant: TARGANTA THERAPEUTICS CORP.Inventors: Evelyne Dietrich, Ranga Reddy, Kelly Tanaka, Ting Kang, Yanick Lafontaine, Adel Rafai Far
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Publication number: 20110166124Abstract: The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose.Type: ApplicationFiled: July 21, 2009Publication date: July 7, 2011Inventors: Kevin D. McCormick, Robert G. Aslanian, Pietro Mangiaracina, Michael Y. Berlin, Manuel De Lera Ruiz, Christopher W. Boyce, Jianhua Chao, Pauline C. Ting, Junying Zheng, Stuart B. Rosenblum
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Patent number: 7960401Abstract: The use of a compound of formula I Y is a single bond, C?O, C?S or S(O)m m where m is 0, 1 or 2; the ring represented by T is a 5 or 6 membered heteroaromatic and R1, R2, R3, R8 and Ra are specified organic groups and p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2, 3, 4, 5 or 6; p+q is 1, 2, 3, 4, 5 or 6; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs; novel compounds are also provided.Type: GrantFiled: December 9, 2004Date of Patent: June 14, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Jérôme Cassayre, Louis-Pierre Molleyres, Peter Maienfisch, Fredrik Cederbaum
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Publication number: 20110136821Abstract: This invention relates to novel compounds of the Formulae I or II and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD 1 in mammals. Formula (I).Type: ApplicationFiled: February 26, 2009Publication date: June 9, 2011Inventors: David A. Claremon, Colin M. Tice, Yuanjie Ye, Suresh B. Singh, Wei He, Wei Zhao, Robert D. Simpson