The Spiro Includes The Six-membered Hetero Ring Patents (Class 546/16)
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Publication number: 20140329986Abstract: The Michael reaction is employed, for example, to condense methyl acrylate with diethyl malonate to prepare the corresponding tetra-ester. Subsequent reaction with primary amines followed by thermal condensation results in spiroimides. A similar series of reaction steps can be performed starting with malonamides.Type: ApplicationFiled: May 1, 2013Publication date: November 6, 2014Inventor: Robert Bernard Login
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Patent number: 8877743Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: GrantFiled: June 14, 2013Date of Patent: November 4, 2014Assignee: Naeja Pharmaceutical Inc.Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
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Publication number: 20140323468Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, R7, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: April 28, 2014Publication date: October 30, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Michael BALESTRA, Jennifer BURKE, Zhidong CHEN, Derek COGAN, Lee FADER, Xin GUO, Bryan MCKIBBEN, Daniel Richard MARSHALL, Peter Allen NEMOTO, Hui YU
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Publication number: 20140323470Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: July 14, 2014Publication date: October 30, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Monique Bodil VAN NIEL, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley
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Patent number: 8871210Abstract: The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.Type: GrantFiled: November 8, 2013Date of Patent: October 28, 2014Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaya Kokubo, Motoyuki Tanaka, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
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Publication number: 20140315923Abstract: The present disclosure relates to a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I). Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s 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, this disclosure also relates to methods of preparation of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I) and intermediates therefor.Type: ApplicationFiled: June 27, 2014Publication date: October 23, 2014Inventors: Zhongli GAO, Daniel HALL, David STEFANY
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Publication number: 20140315876Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: ApplicationFiled: March 12, 2014Publication date: October 23, 2014Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
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Publication number: 20140315912Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor. (I).Type: ApplicationFiled: July 18, 2011Publication date: October 23, 2014Inventors: Gregori J. Morriello, Harvey R. Wendt, Scott D. Edmondson
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Patent number: 8865741Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.Type: GrantFiled: February 18, 2012Date of Patent: October 21, 2014Assignee: Asana Biosciences, LLCInventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
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Patent number: 8865702Abstract: Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.Type: GrantFiled: July 23, 2008Date of Patent: October 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20140309227Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
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Patent number: 8859608Abstract: A spiro-amino compound of Formula (VI) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, such ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, halogen, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridyl, pyrimidyl, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy, methylcarboxy or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 15, 2010Date of Patent: October 14, 2014Assignee: Rottapharm Biotech S.R.L.Inventors: Luigi Piero Stasi, Lucio Rovati
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Publication number: 20140296214Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.Type: ApplicationFiled: October 12, 2012Publication date: October 2, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
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Publication number: 20140296169Abstract: The present disclosure relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: June 18, 2014Publication date: October 2, 2014Inventors: Hauke SZILLAT, Thomas LEEUW, Martin LORENZ
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Publication number: 20140288042Abstract: This invention relates to compounds of Formula I having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R represents a fused bicyclic or spirocyclic aliphatic diamine and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: September 25, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim
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Publication number: 20140288106Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.Type: ApplicationFiled: June 3, 2014Publication date: September 25, 2014Applicant: SanofiInventors: Imre BATA, Peter BUZDER-LANTOS, Attila VASAS, Veronika BARTANE BODOR, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Sandor BATORI, Martin SMRCINA, Marcel PATEK, Aleksandra WEICHSEL, David Squire Thorpe
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Publication number: 20140275005Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s 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, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: ApplicationFiled: May 5, 2014Publication date: September 18, 2014Applicant: SanofiInventor: Zhongli GAO
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Publication number: 20140275025Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
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Patent number: 8822448Abstract: 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: GrantFiled: March 7, 2013Date of Patent: September 2, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
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Publication number: 20140243303Abstract: The present invention relates to spirocyclic compounds of formula I, namely spirocyclic (1H-pyrazol-4-yl)-3-(1-(2,6-dichloro-3-fiuorophenyl)ethoxy)pyridin-2-amines having protein kinase inhibitory activity, and methods of synthesizing and using such compounds. Preferred compounds are c-Met and/or ALK inhibitors useful for the treatment of abnormal cell growth, such as cancers.Type: ApplicationFiled: July 26, 2012Publication date: August 28, 2014Applicant: Beta Pharma Canada Inc.Inventors: Zhaoyin Wang, Lianhai Li, Zhigang Wang
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Patent number: 8815869Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: March 10, 2011Date of Patent: August 26, 2014Assignee: AbbVie Inc.Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
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Publication number: 20140235634Abstract: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.Type: ApplicationFiled: February 14, 2014Publication date: August 21, 2014Applicant: Kala Pharmaceuticals, Inc.Inventors: Winston Zapanta ONG, Pawel Wojciech NOWAK, Ben C. ASKEW, Jinsoo KIM
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Publication number: 20140221349Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Matthias ECKHARDT
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Patent number: 8796257Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: GrantFiled: November 30, 2012Date of Patent: August 5, 2014Assignee: Naeja Pharmaceutical Inc.Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
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Patent number: 8796278Abstract: The present disclosure relates to a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I). Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s 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, this disclosure also relates to methods of preparation of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I) and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: August 5, 2014Assignee: SanofiInventors: Zhongli Gao, Daniel Hall, David Stefany
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Patent number: 8791091Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.Type: GrantFiled: November 29, 2012Date of Patent: July 29, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
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Patent number: 8778925Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.Type: GrantFiled: October 6, 2009Date of Patent: July 15, 2014Assignee: Cancer Research Technology Ltd.Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
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Patent number: 8778929Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Patent number: 8772307Abstract: The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.Type: GrantFiled: May 17, 2006Date of Patent: July 8, 2014Assignee: Gruenenthal GmbHInventors: Robert Frank, Melanie Reich, Ruth Jostock, Gregor Bahrenberg, Hans Schick, Birgitta Henkel, Helmut Sonnenschein
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Publication number: 20140187530Abstract: 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: November 27, 2013Publication date: July 3, 2014Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian W. Metcalf
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Patent number: 8765744Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, R7, A, Z and m are as defined herein. The compounds of formula (I) are inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 (11beta-HSD1) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: GrantFiled: June 23, 2011Date of Patent: July 1, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Frank Himmelsbach
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Publication number: 20140179638Abstract: The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13a and R13b are each independently as defined in the description.Type: ApplicationFiled: July 26, 2012Publication date: June 26, 2014Applicant: KBP BIOSCIENCES CO., LTD.Inventors: Hui Zhang, Yanyan Dong
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Patent number: 8759377Abstract: In one aspect, the invention relates to compounds having a general structure: wherein the variables are defined herein, which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. 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: November 23, 2010Date of Patent: June 24, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Darren W. Engers
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Patent number: 8754097Abstract: 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 tumors.Type: GrantFiled: August 22, 2012Date of Patent: June 17, 2014Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Patent number: 8754095Abstract: The present disclosure relates to a series of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). wherein R, R1, R2, R3, R4, X, 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, this disclosure relates to methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: June 17, 2014Assignee: SanofiInventor: Zhongli Gao
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Publication number: 20140163001Abstract: Provided is a heterocyclic compound having an ROR?t inhibitory activity.Type: ApplicationFiled: July 27, 2012Publication date: June 12, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Satoshi Yamamoto, Junya Shirai, Atsuko Ochida, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Shotaro Miura, Kazuko Yonemori, Ryokichi Koyama
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Publication number: 20140148443Abstract: Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, and methods of using the compounds in the treatment of cancer.Type: ApplicationFiled: November 20, 2013Publication date: May 29, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
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Patent number: 8735385Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s 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, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: May 27, 2014Assignee: SanofiInventor: Zhongli Gao
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Patent number: 8722578Abstract: Herbicidal compositions containing as active ingredients spiroheterocyclic pyrrolidine dione compounds.Type: GrantFiled: October 28, 2009Date of Patent: May 13, 2014Assignee: Syngenta Participations AGInventors: Werner Zambach, Ottmar Franz Hueter, Jean Wenger, Marcela Goeghova, Thomas Pitterna, Peter Maienfisch, Stephane André´Marie Jeanmart, Michel Muehlebach
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Patent number: 8703165Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.Type: GrantFiled: November 30, 2010Date of Patent: April 22, 2014Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Patent number: 8691836Abstract: Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.Type: GrantFiled: June 17, 2011Date of Patent: April 8, 2014Assignee: Altos Therapeutics, LLCInventors: Gary W. Luehr, Arathi Sundaram, Priyadarshini Jaishankar, Philip W. Payne, Pascal Druzgala
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Publication number: 20140080756Abstract: The present invention provides a compound of Formula (I) a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.Type: ApplicationFiled: November 18, 2013Publication date: March 20, 2014Applicant: Pfizer Inc.Inventors: Samit K. Bhattacharya, Kimberly O. Cameron, Dilinie P. Fernando, Kim F. McClure, Daniel W. Kung, Allyn T. Londregan, Suvi T.M. Orr
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Patent number: 8674113Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: GrantFiled: December 8, 2011Date of Patent: March 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
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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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Publication number: 20140073662Abstract: 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: November 22, 2013Publication date: March 13, 2014Applicant: SanofiInventors: Manfred SCHUDOK, Michael WAGNER, Armin BAUER, Anna KOHLMANN
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Publication number: 20140072576Abstract: The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.Type: ApplicationFiled: November 8, 2013Publication date: March 13, 2014Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya KOKUBO, Motoyuki TANAKA, Hiroshi OCHIAI, Yoshikazu TAKAOKA, Shiro SHIBAYAMA
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Publication number: 20140051677Abstract: Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.Type: ApplicationFiled: April 26, 2012Publication date: February 20, 2014Inventors: Christel Jeanne Marie Menet, Alastair James Hodges, Huw David Vater
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Publication number: 20140045813Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
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Patent number: 8648070Abstract: This invention relates to bicyclic ring system substituted sulfonamide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: GrantFiled: December 13, 2011Date of Patent: February 11, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Riccardo Giovannini, Dieter Hamprecht, Barbara Kistler, Iain Lingard
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Publication number: 20140038955Abstract: Heteroaryl amide analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: October 2, 2013Publication date: February 6, 2014Applicant: H. Lundbeck A/SInventors: David C. IHLE, Qin GUO, Kevin HODGETTS, Jun YUAN