The Spiro Includes The Six-membered Hetero Ring Patents (Class 546/16)
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Publication number: 20120329773Abstract: This invention relates to bicyclic ring system substituted amide 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: ApplicationFiled: December 13, 2011Publication date: December 27, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Dieter HAMPRECHT, Barbara KISTLER, Iain LINGARD
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Publication number: 20120328691Abstract: The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 29, 2007Publication date: December 27, 2012Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Tzu T. Wong, Praveen K. Tadikonda, M. Arshad Siddiqui, Marc A. Labroli, Cory Poker, Timothy J. Guzi
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Publication number: 20120316159Abstract: 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: ApplicationFiled: December 13, 2011Publication date: December 13, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Dieter HAMPRECHT, Barbara KISTLER, Iain LINGARD
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Patent number: 8329904Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, m, A, R1 and R2 have the significance given in the description. The compounds are useful as HSL inhibitors and may be used in the treatment or prophylaxis of diabetes, dyslipidemia, atherosclerosis or obesity.Type: GrantFiled: May 3, 2010Date of Patent: December 11, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
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Publication number: 20120302540Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Inventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
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Patent number: 8318956Abstract: The present invention relates to novel compounds of the formula (I), in which W, X, Y, Z, G, A and t have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the spiroheterocyclic tetronic acid derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.Type: GrantFiled: May 19, 2010Date of Patent: November 27, 2012Assignee: Bayer Cropscience AGInventors: Thomas Bretschneider, Reiner Fischer, Stefan Lehr, Olga Malsam, Arnd Voerste
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Patent number: 8318931Abstract: 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: October 27, 2006Date of Patent: November 27, 2012Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaya Kokubo, Motoyuki Tanaka, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
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Publication number: 20120295899Abstract: The present application describes modulators of MCP-1 or CCR-2 of formula or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, W, X, R1 and R6, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.Type: ApplicationFiled: February 8, 2011Publication date: November 22, 2012Inventors: Ian K. Mangion, Percy H. Carter, Jingwu Duan, Andrew J. Tebben
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Publication number: 20120295923Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: January 19, 2011Publication date: November 22, 2012Inventors: Christopher William Am Ende, Benjamin Adam Fish, Douglas Scott Johnson, Ricardo Lira, Christopher John O'Donnell, Martin Youngjin Pettersson, Corey Michael Stiff
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Publication number: 20120289494Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.Type: ApplicationFiled: May 11, 2012Publication date: November 15, 2012Applicants: Sanofi, The Regents of the University of MichiganInventors: Shaomeng Wang, Wei Sun, Angelo Aguilar, Carlos Garcia-Echeverria
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Patent number: 8304547Abstract: [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action.Type: GrantFiled: October 23, 2008Date of Patent: November 6, 2012Assignee: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Nomura, Shunichiro Matsumoto, Takashi Shin, Hidenori Azami, Tomoaki Abe, Akira Suga, Ryushi Seo, Masayuki Tanahashi, Toru Watanabe
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Publication number: 20120268706Abstract: The invention relates to compounds of the formula I, and to a liquid-crystalline medium, preferably having a nematic phase and negative dielectric anisotropy, which comprises one or more compounds of formula I, defined herein, for use in an electro-optical display, particularly in an active-matrix display based on the VA, ECB, PALO, FFS or IPS effect, and to the use of the compounds of the formula I for the stabilization of a liquid-crystalline medium which comprises one or more compounds of the formula II and one or more compounds of the formulae III-1 to III-4, defined herein.Type: ApplicationFiled: April 20, 2012Publication date: October 25, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Mark GOEBEL, Rocco FORTTE, Detlef PAULUTH
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Patent number: 8293896Abstract: 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: October 27, 2006Date of Patent: October 23, 2012Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaya Kokubo, Motoyuki Tanaka, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
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Publication number: 20120264748Abstract: The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: December 20, 2010Publication date: October 18, 2012Applicant: NOVARTIS AGInventors: Sangamesh Badiger, Dirk Behnke, Claudia Betschart, Vinod Chaudhari, Simona Cotesta, Jürgen Hans-Hermann Hinrichs, Silvio Ofner, Chetan Pandit, Jürgen Wagner
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Patent number: 8283357Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: GrantFiled: June 7, 2010Date of Patent: October 9, 2012Assignee: Gilead Sciences, Inc.Inventor: Chandrasekar Venkataramani
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Publication number: 20120252815Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, Y1, Y2, V, W, n, m and o have the gleanings given herein, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.Type: ApplicationFiled: November 18, 2010Publication date: October 4, 2012Applicant: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Frank Stieber, Dirk Wienke
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Publication number: 20120245026Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.Type: ApplicationFiled: November 30, 2010Publication date: September 27, 2012Applicant: Syngenta Crop Protection LLCInventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Patent number: 8273341Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: November 8, 2011Date of Patent: September 25, 2012Assignee: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Michael Graupe, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard Mackman, Hyung-Jun Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
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Publication number: 20120238452Abstract: Compounds of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: November 29, 2010Publication date: September 20, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Publication number: 20120238757Abstract: The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I): wherein R1, R2, 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 therefore are disclosed.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Applicant: SANOFIInventors: Zhongli GAO, Ryan HARTUNG, David STEFANY
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Patent number: 8268828Abstract: This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful as a inhibitor of the chemokine receptor CxCR3, and for preventing or treating a CxCR3 chemokine receptor mediated disease or condition related thereto in a patient in need of such.Type: GrantFiled: August 6, 2010Date of Patent: September 18, 2012Assignee: SanofiInventors: David Squire Thorpe, Martin Smrcina, Dagmar Dasha Cabel
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Patent number: 8268853Abstract: Compounds of formula (I) are useful in treating conditions or disorders ameliorated by ?4?2 positive allosteric modulators. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.Type: GrantFiled: June 25, 2010Date of Patent: September 18, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Diana L. Nersesian, Chih-Hung Lee, Ramin Faghih, Gregory A. Gfesser
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Patent number: 8263607Abstract: Provided is a compound useful as an N-type Ca2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Ca2+ channels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings.Type: GrantFiled: May 20, 2008Date of Patent: September 11, 2012Assignee: Astellas Pharma Inc.Inventors: Jun-ichi Shishikura, Makoto Inoue, Takashi Ogiyama, Koichi Yonezawa, Susumu Yamaki, Kazuhiro Yokoyama, Shuichirou Kakimoto, Hidetsugu Okada
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Publication number: 20120220583Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase activity and for the treatment of diseases, including Alzheimer's disease (AD) and related CNS conditions, mediated thereby. In one embodiment, the compounds have a general Formula I or Formula II wherein R1a-1c, B, R3-5 and W of Formula I, and R1a-1c, R2-5, A1-4, W, X, Z, m and n of Formula II are defined herein. The invention further provides compounds of Formula III and IV and sub-Formulas II-A-II-D and III-A-III-D. The compounds may be used in pharmaceutical compositions for treating, prophylactically or therapeutically, disorders related to the activity of beta-secretase protein, including without limitation, AD, cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions.Type: ApplicationFiled: March 1, 2012Publication date: August 30, 2012Applicant: AMGEN INC.Inventors: Wenge ZHONG, Stephen HITCHCOCK, Vinod F. PATEL, Michael CROGHAN, Thomas DINEEN, Scott HARRIED, Daniel HORNE, Ted JUDD, Matthew KALLER, Charles KREIMAN, Patricia LOPEZ, Holger MONENSCHEIN, Thomas NGUYEN, Matthew WEISS, Qiufen XUE, Bryant YANG, Russell GRACEFFA
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Publication number: 20120214832Abstract: Disclosed are isoform selective Phospholipase D inhibitors. In one aspect, the disclosed compounds can have a structure represented by a formula (I): Also disclosed are methods of making and using the compounds. Also disclosed are pharmaceutical compositions and kits comprising the compounds. 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: July 23, 2010Publication date: August 23, 2012Inventors: H. Alex Brown, Craig W. Lindsley, Alex G. Waterson, Sarah A. Scott
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Publication number: 20120214809Abstract: 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 TRPV 1 receptor activator. In one embodiment, the TRPV 1 receptor activator is lidocaine.Type: ApplicationFiled: February 18, 2012Publication date: August 23, 2012Inventors: 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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Publication number: 20120207765Abstract: A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification 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, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.Type: ApplicationFiled: March 8, 2012Publication date: August 16, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya Kokubo, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
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Patent number: 8232288Abstract: Substituted benzimidazoles, benzothiazoles and benzoxazoles, processes for their preparation, pharmaceutical compostions containing these compounds and the use of these compounds for treating or inhibiting disorders or disease states mediated at least in part by bradykinin receptor 1 (BR1).Type: GrantFiled: June 7, 2010Date of Patent: July 31, 2012Assignee: Gruenenthal GmbHInventors: Stefan Schunk, Melanie Reich, Michael Engels, Tieno Germann, Jean De Vry, Ruth Jostock, Sabine Hees
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Publication number: 20120190675Abstract: 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: ApplicationFiled: June 23, 2011Publication date: July 26, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Frank HIMMELSBACH
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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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Publication number: 20120171129Abstract: Disclosure is provided for benzimidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.Type: ApplicationFiled: June 10, 2010Publication date: July 5, 2012Inventors: Christian Melander, Steven A. Rogers, Robert W. Huigens, III
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Publication number: 20120165331Abstract: The invention relates to compounds of the formula I A-D-C(R1)2—B??(I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: December 19, 2011Publication date: June 28, 2012Inventors: Sangamesh BADIGER, Dirk BEHNKE, Claudia BETSCHART, Vinod CHAUDHARI, Simona COTESTA, Samuel HINTERMANN, Andreas LERCHNER, Fatma LIMAM, Silvio OFNER, Chetan PANDIT, Jürgen WAGNER
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Publication number: 20120157432Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: August 17, 2010Publication date: June 21, 2012Applicant: Merck Sharp & Dohme, Corp.Inventors: Scott D. Edmondson, Richard Berger, Lehua Chang, Vincent j. Colandrea, Jeffrey J. Hale, Bart Harper, Nam Fung Kar, Bing Li, Greg J. Morriello, Christopher R. Moyes, Deyou Sha, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
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Publication number: 20120149676Abstract: 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: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
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Publication number: 20120142685Abstract: The present invention provides a compound formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: April 4, 2008Publication date: June 7, 2012Inventors: Markus Rolf Dobler, Charles Francis Jewell, JR., Erik Meredith, Lauren G. Monovich, Sarah Siska, Anette Von Matt, Maurice Van Eis, Taeyoung Yoon, Christoph Gaul, Michael Paul Capparelli
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Patent number: 8193207Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 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.Type: GrantFiled: December 4, 2006Date of Patent: June 5, 2012Assignee: Incyte CorporationInventors: Jincong Zhuo, Ding-Quan Qian, Wenqing Yao
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Publication number: 20120135968Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.Type: ApplicationFiled: May 7, 2010Publication date: May 31, 2012Inventors: Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus Rönn
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Patent number: 8188277Abstract: The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein X1 represents a nitrogen atom or a group —CH?; R1 represents a group —Z—R6, wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group or the like, wherein R3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R4 represents an imidazolyl lower alkyl group or the like.Type: GrantFiled: August 3, 2005Date of Patent: May 29, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Tae Fukushima, Shuji Matsumura, Noriaki Takemura, Hideaki Satou, Nobuaki Ito, Takuya Shitsuta, Hironori Tsutsui, Michinori Tanaka, Keizo Kan, Hitoshi Nagao, Kenji Watanabe, Kuninori Tai, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Keisuke Miyajima, Satoshi Yamada, Yutaka Kojima, Koichi Yasumura, Naoto Ohi, Mitsuhiro Okuno, Kazuhisa Sugiyama, Kunihiko Kiyono, Takashi Suzuki, Seiji Akamatsu, Takeshi Kodama, Yasuo Yanagihara, Takumi Sumida
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Publication number: 20120129833Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of diabetes, obesity, hyperlipidaemia, fatty livers and of disorders of the cardiovascular system.Type: ApplicationFiled: August 19, 2011Publication date: May 24, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ningshu LIU, Kai Thede, Philip Lienau, Arne Scholz, Maher Najjar, Ulf Bomer, Knut Eis, Reiner Fischer
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Publication number: 20120129830Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3, provided that m+n?7 and that o+p?7; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group and the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compounds; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.Type: ApplicationFiled: May 11, 2010Publication date: May 24, 2012Applicant: SANOFIInventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
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Publication number: 20120122858Abstract: 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: January 20, 2012Publication date: May 17, 2012Applicant: Incyte CorporationInventors: Wenqing Yao, Chunhong He, David M. Burns, Jincong Zhuo, Meizhong Xu, Colin Zhang, Ding-Quan Qian, Brian Metcalf
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Patent number: 8178550Abstract: Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.Type: GrantFiled: April 4, 2007Date of Patent: May 15, 2012Assignee: OPKO Health, Inc.Inventors: Mengwei Hu, Sunil Paliwal, Neng-Yang Shih, Frank Bruno Guenter, Ingrid Mergelsberg
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Publication number: 20120115882Abstract: 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: ApplicationFiled: July 15, 2010Publication date: May 10, 2012Inventors: Luigi Piero Stasi, Lucio Rovati
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Publication number: 20120101280Abstract: The invention relates to a compound represented by formula (I): a salt thereof, an N-oxide thereof, or a solvate thereof (symbols in the formula are as described in the specification). The compound of the present invention exhibits very low risk of side effects and also has persistent and strong antagonistic activity against CXCR4, and is therefore useful as pharmaceuticals, for example, preventive and/or therapeutic agent for inflammatory and immune diseases, infections (for example, HIV infection), diseases associated with HIV infection (for example, acquired immunodeficiency syndrome (AIDS)), cancer, cancer metastasis, psychoneurotic diseases and cardiovascular diseases (for example, retinopathy), metabolic diseases, cancerous diseases, or an agent for regeneration therapy.Type: ApplicationFiled: June 15, 2010Publication date: April 26, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Koji Yoshida, Hiroshi Ochiai, Kousuke Tani, Shiro Shibayama, Miki Kasano
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Publication number: 20120101110Abstract: The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: October 18, 2011Publication date: April 26, 2012Inventors: Sangamesh BADIGER, Dirk BEHNKE, Claudia BETSCHART, Simona COTESTA, Samuel HINTERMANN, Silvio OFNER, Chetan PANDIT, Bernard Lucien ROY
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Patent number: 8158643Abstract: The present invention concerns aryl and heteroaryl substituted diaza-spiro-pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.Type: GrantFiled: December 4, 2007Date of Patent: April 17, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Frank Matthias Dautzenberg, Joannes Theodorus Maria Linders
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Patent number: 8153623Abstract: Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same.Type: GrantFiled: August 4, 2010Date of Patent: April 10, 2012Assignee: Convergence Pharmaceuticals LimitedInventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Publication number: 20120083476Abstract: Certain heteroaryl-substituted spirocyclic diamine urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: June 4, 2010Publication date: April 5, 2012Applicant: Janssen Pharmaceutica NVInventors: J. Guy Breitenbucher, John M. Keith, William M. Jone
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Publication number: 20120083557Abstract: The instant invention pertains to hindered amine compounds having at least two nitrogen atoms with different basicity. One part is substituted on the N-atom by alkoxy moieties and the other part is substituted on the N-atom by a hydroxy-alkyl moiety. These materials are particularly effective in stabilizing polymers, especially thermoplastic polyolefins, against the deleterious effects of oxidative, thermal and actinic radiation. The compounds are also particularly effective in stabilizing acid catalyzed and ambient cured coatings systems.Type: ApplicationFiled: June 1, 2010Publication date: April 5, 2012Applicant: BASF SEInventor: Kai-Uwe Schoening
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Publication number: 20120071319Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.Type: ApplicationFiled: May 21, 2010Publication date: March 22, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach