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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Publication number: 20140080823Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.Type: ApplicationFiled: November 22, 2013Publication date: March 20, 2014Applicant: DAC S.R.L.Inventors: Mario Varasi, Florian Thaler, Agnese Abate, Giacomo Carenzi, Ciro Mercurio, Saverio Minucci
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Patent number: 8673931Abstract: 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: GrantFiled: January 26, 2010Date of Patent: March 18, 2014Inventors: Abraham Fisher, Nira Bar-Ner, Victoria Nachum
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Patent number: 8669365Abstract: The invention provides novel derivatives of cyclopamine having the following formula:Type: GrantFiled: August 27, 2008Date of Patent: March 11, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Brian Austad, Mark L. Behnke, Alfredo C. Castro, André B. Charette, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Martin Tremblay
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Publication number: 20140045875Abstract: 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: July 29, 2013Publication date: February 13, 2014Applicant: Purdue Pharma L.P.Inventors: Zhengming CHEN, Laykea Tafesse, Jiangchao Yao, Khondaker Islam
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Publication number: 20140031378Abstract: An insecticidal compound of formula I wherein X is O or NR11 where R11 is hydrogen, optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; R1, R2, R3, R4, 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 provided that p+q is 1, 2, 3, 4, 5 or 6; or salts or N-oxides thereof; compositions containing them and their using in controlling insects, acarines, nematodes or molluscs.Type: ApplicationFiled: January 15, 2013Publication date: January 30, 2014Inventor: Syngenta Crop Protection LLC
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Patent number: 8637497Abstract: 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: GrantFiled: July 18, 2011Date of Patent: January 28, 2014Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
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Patent number: 8633214Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof processes for their preparation, compositions containing them, and uses thereof in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.Type: GrantFiled: November 21, 2012Date of Patent: January 21, 2014Assignee: Nerre Therapeutics LimitedInventors: Giuseppe Alvaro, Emiliano Castiglioni, Agostino Marasco
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Patent number: 8629102Abstract: [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 O 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: GrantFiled: March 15, 2013Date of Patent: January 14, 2014Assignee: Mochida Pharmaceutical Co., Ltd.Inventor: Munetaka Ohkouchi
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Publication number: 20140011796Abstract: 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: September 12, 2013Publication date: January 9, 2014Applicant: AMGEN INC.Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. 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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Substituted piperidine spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof
Patent number: 8604046Abstract: 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 19, 2012Date of Patent: December 10, 2013Assignee: SanofiInventors: Zhongli Gao, Daniel Hall, Ryan Hartung -
Patent number: 8598164Abstract: 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: GrantFiled: May 6, 2011Date of Patent: December 3, 2013Assignee: 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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Patent number: 8592444Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.Type: GrantFiled: April 14, 2009Date of Patent: November 26, 2013Assignee: DAC S.R.L.Inventors: Mario Varasi, Florian Thaler, Agnese Abate, Giacomo Carenzi, Ciro Mercurio, Saverio Minucci
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Patent number: 8586737Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.Type: GrantFiled: April 26, 2011Date of Patent: November 19, 2013Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Nobuyuki AE, Yuji Fujiwara
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Patent number: 8580808Abstract: A compound, its pharmaceutically acceptable salt, a composition containing the same and method of treatment that can provide analgesia and/or reduce inflammation are disclosed. A contemplated compound has a structure that corresponds to Formula A, wherein G, W, Q, Z, D, E, F, K, Y, d, e, f, k, n, m, and circle B and all R groups are defined within.Type: GrantFiled: October 30, 2009Date of Patent: November 12, 2013Assignee: Pain Therapeutic, Inc.Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Publication number: 20130296354Abstract: The present invention relates to compounds of general formula I, wherein the groups R1 and A 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: May 6, 2013Publication date: November 7, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Matthias ECKHARDT
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Publication number: 20130296319Abstract: 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: ApplicationFiled: July 11, 2013Publication date: November 7, 2013Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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Publication number: 20130296300Abstract: The invention provides certain quinolines and aza-quinolines of the Formula (I), and their pharmaceutically acceptable salts, wherein E, J1, Ja, Jb, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.Type: ApplicationFiled: December 19, 2011Publication date: November 7, 2013Inventors: Christopher W. Boyce, Salem Fevrier, Kevin D. McCormick, Anandan Palani, Robert G. Aslanian, Phieng Siliphaivanh, Joey L. Methot, William Colby Brown, Henry Vaccaro
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Patent number: 8546417Abstract: 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: June 1, 2012Date of Patent: October 1, 2013Assignee: Purdue Pharma L.P.Inventors: Zhengming Chen, Laykea Tafesse
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Patent number: 8541595Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.Type: GrantFiled: November 3, 2009Date of Patent: September 24, 2013Assignee: Merch Sharp & Dohme Corp.Inventors: Peter J. Manley, Kausik K Nanda, B. Wesley Trotter
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Patent number: 8536189Abstract: 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: March 1, 2012Date of Patent: September 17, 2013Assignee: Janssen Pharmaceutica NVInventors: Michael J. Costanzo, Stephen C. Yabut, Brett Tounge, Bruce E. Maryanoff, Han-Cheng Zhang
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Patent number: 8524730Abstract: The invention relates to a compound of a general formula (I): wherein A represents a linking group; Ar1 represents a group formed from an aromatic ring; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; a C1-C6 alkyl group optionally having substituent(s); an aryl or heterocyclic group optionally having substituent(s); or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom, a sulfur atom or an imino group.Type: GrantFiled: June 29, 2009Date of Patent: September 3, 2013Assignee: MSD K.K.Inventors: Hideki Jona, Yoshihiro Shibata, Takeru Yamakawa
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Publication number: 20130225553Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.Type: ApplicationFiled: March 7, 2013Publication date: August 29, 2013Applicant: ASTELLAS PHARMA INC.Inventor: ASTELLAS PHARMA INC.
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Publication number: 20130217690Abstract: [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 O 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: March 15, 2013Publication date: August 22, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Mochida Pharmaceutical Co., Ltd.
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Patent number: 8513232Abstract: The present invention provides compounds of Formula (I): their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceuticals compositions thereof.Type: GrantFiled: July 29, 2010Date of Patent: August 20, 2013Assignees: Cephalon, Inc., Pharmacopeia, LLCInventors: Edward R. Bacon, Nadine C. Becknell, Reddeppa reddy Dandu, Lisa Guise-Zawacki, Tao Guo, Chia-yu Huang, Robert L. Hudkins, Babu G. Sundar, Ming Tao, Minglang Wu, Allison L. Zulli
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Patent number: 8513417Abstract: The problem to be solved by the present invention is to provide a highly-versatile method for producing a nitroxyl radical derivative, in which position-2 and position-6 in a TEMPO-based compound can be easily substituted, and further, a method for producing a nitroxyl radical derivative, in which a nitrogen nucleus is labeled with 15N. The above-described problem can be solved by reacting a triacetoneamine derivative with ketone or aldehyde in the presence of ammonium salt or a 15N-labeled compound thereof to obtain a 2,6-substituted-4-piperidone derivative.Type: GrantFiled: January 30, 2008Date of Patent: August 20, 2013Assignee: Kyushu University, National University CorporationInventors: Hideo Utsumi, Kiyoshi Sakai, Kenichi Yamada
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Publication number: 20130210721Abstract: [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 O 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: March 15, 2013Publication date: August 15, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: MOCHIDA PHARMACEUTICAL CO., LTD.
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Patent number: 8507681Abstract: 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: October 4, 2012Date of Patent: August 13, 2013Assignee: Pfizer Inc.Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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Publication number: 20130196998Abstract: The present invention relates to spiro-cyclic amine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)aType: ApplicationFiled: July 8, 2011Publication date: August 1, 2013Applicant: AbbVie B.V.Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Maria J.P. van Dongen, Nicolas J.-L.D. Leflemme
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Publication number: 20130196992Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—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. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.Type: ApplicationFiled: March 14, 2013Publication date: August 1, 2013Applicants: ADDEX PHARMACEUTICALS S.A, JANSSEN PHARMACEUTICALS, INC.Inventors: Jose Maria CID-NUNEZ, Andres Avelino TRABANCO-SUAREZ, Gregor James MACDONALD, Guillaume Albert Jacques DUVEY, Robert Johannes LÜTJENS, Terry Patrick FINN
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Publication number: 20130190334Abstract: The invention provides a compound of Formula (I) Z N N O N O A1R2 R1 R3R 3 L A2 (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3,Z, A1, L and A 5 2 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: September 20, 2011Publication date: July 25, 2013Applicant: PFIZER INC.Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith
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Publication number: 20130184226Abstract: The present invention provides novel compounds of the Formula (1), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for modulating Protease Activated Receptor-2 (PAR2) and for treating a subject at risk of—or susceptible to—a disease or disorder, or having a disease or disorder associated with undesirable PAR2 activity.Type: ApplicationFiled: July 28, 2011Publication date: July 18, 2013Applicant: THE UNIVERSITY OF QUEENSLANDInventors: David Paul Fairlie, Ligong Liu, Mei Kwan Yau, Jacky Yung Suen
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Patent number: 8476253Abstract: 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: GrantFiled: September 16, 2011Date of Patent: July 2, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Takuya Ikeda, Takanori Yamazaki, Hiroshi Tsuchida
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Publication number: 20130150340Abstract: The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3 and R4 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: October 25, 2012Publication date: June 13, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130137684Abstract: The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin D2 synthase (H-PGDS), to compositions containing them and to their use in treating or preventing conditions and diseases associated with H-PGDS, such as allergies and inflammation.Type: ApplicationFiled: June 1, 2011Publication date: May 30, 2013Applicant: THE UNIVERSITY OF QUEENSLANDInventors: Mark Leslie Smythe, Jack Urquhart Flanagan
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Publication number: 20130123236Abstract: In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: November 10, 2012Publication date: May 16, 2013Applicant: VANDERBILT UNIVERSITYInventor: VANDERBILT UNIVERSITY
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Publication number: 20130109677Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: ApplicationFiled: December 3, 2010Publication date: May 2, 2013Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.Inventors: Liming Shao, John Emmerson Campbell, Michael Charles Hewitt, Una Campbell, Taleen G. Hanania
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Patent number: 8431700Abstract: In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: March 3, 2010Date of Patent: April 30, 2013Assignee: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Publication number: 20130085128Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 27, 2012Publication date: April 4, 2013Applicant: SANOFIInventor: SANOFI
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Patent number: 8399503Abstract: The invention relates to substituted azaindole derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted azaindole derivatives for producing medicaments.Type: GrantFiled: January 15, 2009Date of Patent: March 19, 2013Assignee: Gruenenthal GmbHInventors: Saskia Zemolka, Stefan Schunk, Ellen Bergrath, Babette-Yvonne Kögel, Werner Englberger, Klaus Linz, Hans Schick
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Patent number: 8383629Abstract: 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: GrantFiled: February 26, 2009Date of Patent: February 26, 2013Assignee: Vitae Pharmaceuticals, Inc.Inventors: David A. Claremon, Colin M. Tice, Yuanjie Ye, Suresh B. Singh, Wei He, Wei Zhao, Robert D. Simpson
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Patent number: 8383643Abstract: 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: GrantFiled: July 21, 2010Date of Patent: February 26, 2013Assignee: Merck Canada Inc.Inventors: Jean-Philippe Leclerc, Chun-Sing Li, Oscar Miguel Moradei
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Patent number: 8383642Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition, and a method for treating diabetes.Type: GrantFiled: October 11, 2010Date of Patent: February 26, 2013Assignee: Eli Lilly and CompanyInventors: Chafiq Hamdouchi, Jayana Pankaj Lineswala, Pranab Maiti
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Publication number: 20130046091Abstract: The use of a compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; R1, R2, R3, R4, 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; provided that when p is 2 then q is not 2; p+q is 1, 2, 3, 4, 5 or 6; or salts or N-oxides thereof or compositions containing them and their using incontrolling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: ApplicationFiled: October 23, 2012Publication date: February 21, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventor: Syngenta Crop Protection LLC
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Patent number: 8377954Abstract: The present invention is directed to bicyclic spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: December 28, 2007Date of Patent: February 19, 2013Assignee: Merck, Sharp & Dohme, CorpInventors: Shaun R. Stauffer, Samuel L. Graham
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Patent number: 8367692Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof. wherein R is hydrogen or C1-4 alkyl; R1 is hydrogen, C1-4 alkyl, C(O)OH, C(O)NH2 or (C1-4 alkylene)R10; R2 and R3 are independently hydrogen, C1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C1-4 alkyl, C1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C1-4 alkylene)R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2 or C(O)OH; n is 0, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.Type: GrantFiled: April 29, 2009Date of Patent: February 5, 2013Assignee: Glaxo Wellcome Manufacturing Pte LtdInventors: Giuseppe Alvaro, Emiliano Castiglioni, Agostino Marasco
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Publication number: 20130030181Abstract: 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: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: PFIZER INC.Inventor: Pfizer Inc.
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Publication number: 20130023515Abstract: Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: ApplicationFiled: April 21, 2011Publication date: January 24, 2013Inventors: Fa-Xiang Ding, Jinlong Jiang, Dong-Ming Shen, Hong Shen, Zhi-Cai Shi
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Patent number: 8354545Abstract: The present invention is directed to 3,4-substituted pyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: December 10, 2008Date of Patent: January 15, 2013Assignees: Merck, Sharp & Dohme, Corp., Istituto di Ricerche di Biologia Molecolare P Angeletti SPAInventors: Shawn J. Stachel, Thomas Steele, Alessia Petrocchi
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Patent number: 8354423Abstract: An insecticidal compound of formula I wherein X is O or NR11 where R11 is hydrogen, optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; R1, R2, R3, R4, 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 provided that p+q is 1, 2, 3, 4, 5 or 6; or salts or N-oxides thereof; compositions containing them and their using in controlling insects, acarines, nematodes or molluscs.Type: GrantFiled: December 9, 2004Date of Patent: January 15, 2013Assignee: Syngenta Crop Protection LLCInventors: Jérôme Cassayre, Louis-Pierre Molleyres, Peter Maienfisch, Fredrik Cederbaum
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Publication number: 20120316162Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumours.Type: ApplicationFiled: August 22, 2012Publication date: December 13, 2012Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Kai SCHIEMANN, Melanie SCHULTZ, Andree BLAUKAT, Ingo KOBER