Spiro Patents (Class 544/70)
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Publication number: 20130065881Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease. There is also provided combinations comprising the compounds of formula (I).Type: ApplicationFiled: December 31, 2010Publication date: March 14, 2013Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICASInventors: Joaquin Pastor Fernandez, Francisco Javier Ramos Lima, Ana Isabel Hernandez Higueras, Sonia Martinez Gonzalez, Jose Ignacio Martin Hernando, Carl-Gustave Pierre Saluste, Esther Gonzalez Cantalapiedra, Carmen Blanco Aparicio, Antonio Rodriguez Hergueta, Ana Maria Garcia Collazo, Antonio Salgado Serrano, Beatriz Noya Marino
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Publication number: 20130053346Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.Type: ApplicationFiled: August 23, 2012Publication date: February 28, 2013Applicant: Endo Pharmaceuticals IncInventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
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Publication number: 20130040934Abstract: The invention relates to new triazines (G=Q=U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E1 is CR4 or N; X1 is CHR4, CH2CH2, NR4, NR4?0, or O; and the other substituents are as defined in the specification. The compounds inhibit phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR), DNA-PK and ATM kinase, and may be used as therapeutic agents or diagnostic probes. The invention also relates to methods of using the compounds for treatment of associated pathological conditions.Type: ApplicationFiled: March 11, 2011Publication date: February 14, 2013Inventors: Vladimir Cmiljanovic, Natasa Cmiljanovic, Bernd Giese, Matthias Wymann
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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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Publication number: 20130017170Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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Patent number: 8343965Abstract: Compositions, preferably pharmaceutical compositions, containing micronized tanaproget, or pharmaceutically acceptable salt thereof, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, butylated hydroxyanisole, povidone, and magnesium stearate, are provided. The compositions are useful in contraception and hormone replacement therapy and in the treatment and/or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.Type: GrantFiled: April 26, 2006Date of Patent: January 1, 2013Assignee: Wyeth LLCInventors: Arwinder S. Nagi, Ramarao Chatlapalli, Shamim Hasan, Rolland W. Carson, Mohamed Ghorab
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Publication number: 20120328627Abstract: 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: August 28, 2012Publication date: December 27, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya KOKUBO, Motoyuki Tanaka, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
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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: 20120302745Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.Type: ApplicationFiled: August 2, 2012Publication date: November 29, 2012Inventors: Tiruvettipuram K. Thiruvengadam, Anantha R. Sudhakar, Ngiap Kie Lim, Daw-Iong Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green
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Publication number: 20120295897Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: July 25, 2012Publication date: November 22, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Publication number: 20120295856Abstract: The invention relates to novel fredericamycin derivatives, to drugs containing said derivatives or the salts thereof, and to the use of the fredericamycin derivatives for treating diseases, especially cancer diseases.Type: ApplicationFiled: July 27, 2012Publication date: November 22, 2012Applicant: ZENTOPHARM GmbHInventors: Ulrich Abel, Werner Simon
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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: 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: 8304423Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: June 29, 2011Date of Patent: November 6, 2012Assignee: Vertex Pharmaceutical IncorporatedInventors: Robert J. Davies, Jinwang Xu
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Publication number: 20120270071Abstract: A chromene compound having a skeleton represented by the following formula (1) and exhibiting double peak characteristic: wherein Z is a group represented by any one of the following formulas: n is an integer of 1 to 3, when n is 2 or 3, Z? s may be the same or different, with the proviso that when n is 1, Z cannot be —CH2—, and when n is 2 or 3, Z's cannot be —CH2— at the same time; R1 is an electron absorbing group having a Hammett constant ?p of more than 0, with the proviso that when there are a plurality of R1's, R1's may be the same or different; and X and Y are each independently an oxygen atom or ?NR2, with the proviso that X and Y cannot be oxygen atoms at the same time.Type: ApplicationFiled: July 21, 2010Publication date: October 25, 2012Inventors: Toshiaki Takahashi, Junji Takenaka
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Publication number: 20120270838Abstract: The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2010Publication date: October 25, 2012Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Toru Esaki, Yoshikazu Nishimura, Yoshiaki Isshiki, Naoki Okamoto, Yoshiyuki Furuta, Akemi Mizutani, Masateru Ohta, Wayne Wen Lai, Tomoya Kotake
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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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Publication number: 20120252780Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 29, 2010Publication date: October 4, 2012Inventors: Pui Yee Ng, Charles Blum, Lauren McPherson, Robert B. Perni, Chi B. Vu, Mohammed Mahmood Ahmed, Jeremy S. Disch
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Publication number: 20120245136Abstract: The invention relates to chroman spirocyclic piperidine amide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: February 16, 2012Publication date: September 27, 2012Inventors: Sara Sabina HADIDA-RUAH, Mark Thomas Miller, Edward Adam Kallel, Brian Richard Bear, Vijayalaksmi Arumugam, Michael Paul Deninno, Jinglan Zhou, Johnny Uy, Bryan A. Frieman
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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: 8263596Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.Type: GrantFiled: April 6, 2011Date of Patent: September 11, 2012Assignee: University Health NetworkInventors: Peter B. Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Radoslaw Laufer
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Publication number: 20120225877Abstract: This invention relates provides novel substituted 1,4-dioxa-8-azaspiro[4,5]decane of general formula (1), wherein R1 is selected from phenethyl, 4,6-dimethoxypyrimidin-2-yl and (2-chloro-5-thiazolyl)methyl and R2 is selected from the group consisting of hydroxy, 4-bromo-2-chlorophenoxy, morpholin-4-yl, (2-chloro-5-thiazolyl)methyloxy, benzyloxy, phenylsulfanyl, benzotriazol-1-yl and 5-chloro-2-fluoroanilino. The present invention also relates to a process for the preparation of novel substituted 1,4-dioxa-8-azaspiro[4,5]decanes of general formula (1). The novel substituted 1,4-dioxa-8-azaspiro[4,5]decane of general formula (1) has fungicidal activity.Type: ApplicationFiled: March 23, 2010Publication date: September 6, 2012Inventors: Mukund Vinayak Deshpande, Sunita Ranjan Deshpande, Fazal Shirazi, Preeti Madhukar Chaudhary, Nelavelli Malleswara Rao, Baidyanath Mohanty, Nageshwar Nath Sharma, Anand Kumar Bachhawat, Ganesan Kaliannan, Sanjoy Paul, Raj Kumar, Bommena Vittal Rao, Bhimrao Bodhanrao Gawali, Vaddu Venkata Narayana Reddy, Jhillu Singh Yadav
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Publication number: 20120226031Abstract: Embodiments of the present invention relate to inhibitors of thioredoxin. Certain embodiments relate to palmarumycin based compounds and methods of using the same. Such compounds may be useful in inhibiting the overexpression of thioredoxin, inhibiting tumor growth and treating cancer.Type: ApplicationFiled: February 2, 2012Publication date: September 6, 2012Inventors: GARTH POWIS, PETER WIPF
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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: 20120214784Abstract: An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described. ORL-1 antagonists are deemed to be useful in the treatment of depression and/or the treatment of overweight, obesity, and/or weight maintenance post treatment for overweight or obesity. Certain compounds have also demonstrated through animal models that the compounds of the present invention are useful for the treatment of migraines.Type: ApplicationFiled: November 12, 2010Publication date: August 23, 2012Applicant: ELI LILLY AND COMPANYInventors: Ana Belen Benito Collado, Nuria Diaz Buezo, Alma Maria Jimenez-Aguado, Celia Lafuente Blanco, Maria Angeles Martinez-Grau, Concepcion Pedregal Tercero, Miguel Angel Toledo Escribano
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Publication number: 20120202782Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).Type: ApplicationFiled: April 12, 2012Publication date: August 9, 2012Applicant: IRM LLCInventors: Badry Bursulaya, Dai Cheng, Jiqing Jiang, Donald S. Karanewsky, Yi Liu, Shifeng Pan, Yongqin Wan, Xia Wang, Yun Feng Xie, Yang Yang
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Publication number: 20120190677Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein R1 to R8, A1 to A3 have the are as described herein and compositions including the compounds.Type: ApplicationFiled: January 19, 2012Publication date: July 26, 2012Inventors: Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Shixiang Yan, Hongying Yun, Mingwei Zhou
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Patent number: 8211932Abstract: The present application describes organic compounds of the Formula I that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: September 10, 2010Date of Patent: July 3, 2012Assignee: Novartis AGInventors: Michael Patane, Prakash Raman, David Thomas Parker, Jiping Fu, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brandl, Francois Lenoir, Pascal Rigollier, Oliver Simic
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Publication number: 20120165327Abstract: The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.Type: ApplicationFiled: March 1, 2012Publication date: June 28, 2012Inventors: Michael J. Costanzo, Stephen C. Yabut, Brett Tounge, Bruce E. Maryanoff, Han-Cheng Zhang
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Publication number: 20120161089Abstract: A chromene compound having a skeleton represented by the following formula (1) and exhibiting double peak characteristic: wherein Z is a group represented by anyone of the following formulas: (R1 is an electron donor group having a Hammett constant ?p of less than ?0.20, with the proviso that when there are a plurality of R1's, R1's may be the same or different, and R2 is a group having a Hammett constant ?p of ?0.Type: ApplicationFiled: August 26, 2010Publication date: June 28, 2012Inventors: Toshiaki Takahashi, Junji Takenaka
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Publication number: 20120145974Abstract: A chromene compound which contains a skeleton represented by the following formula (1) and has high color optical density at the time of exposure, double peak characteristic, little initial coloration, a practical fading speed and durability. (wherein R1 is an electron donor group having a Hammett constant of less than 0, the ring including X is a hetero ring formed together with the 7-position and 8-position carbon atoms, and X is an oxygen atom, sulfur atom or group represented by ?NR2 directly bonded to the 7-position carbon atom.Type: ApplicationFiled: June 22, 2010Publication date: June 14, 2012Inventors: Toshiaki Takahashi, Junji Takenaka, Kazuhiro Teranishi
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Publication number: 20120149686Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.Type: ApplicationFiled: April 6, 2010Publication date: June 14, 2012Applicant: University Health NetworksInventors: Peter B. Sampson, Yong liu, Sze-Wan Le, Brian T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
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Publication number: 20120142914Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.Type: ApplicationFiled: February 10, 2012Publication date: June 7, 2012Inventors: Tiruvettipuram K. Thiruvengadam, Anantha R. Sudhakar, Ngiap Kie Lim, Daw-Iong Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green
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Publication number: 20120129846Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: May 24, 2012Inventors: Zhaoning Zhu, William J. Greenlee, Mihir Baran Mandal, Duane A. Burnett, Chad E. Bennett, Troy McCracken
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Publication number: 20120121934Abstract: A photochromic chromene compound which develops a color of a neutral tint, has high color optical density, a high fading speed and high durability, and has an indeno(2,1-f)naphtho(1,2-b)pyran structure represented by the following formula as the basic skeleton, wherein a sulfur-containing substituent selected from thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group and heteroarylthio group is bonded to the 6-position and/or 7-position carbon atom(s).Type: ApplicationFiled: August 4, 2010Publication date: May 17, 2012Inventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Kazuhiro Teranishi
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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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Publication number: 20120122773Abstract: The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is —N(R1b)—, G2 is —CO—, G3 is —C(R1c)(R1d)—, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.Type: ApplicationFiled: June 24, 2010Publication date: May 17, 2012Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Satoshi Suetsugu, Nobuhisa Fukuda, Yoshio Nakai, Takashi Takada, Yohei Ikuma, Hiroyuki Nakahira
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Publication number: 20120115841Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: ApplicationFiled: May 17, 2010Publication date: May 10, 2012Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20120095001Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: June 7, 2010Publication date: April 19, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
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Publication number: 20120094972Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: ApplicationFiled: June 25, 2010Publication date: April 19, 2012Applicant: AMGEN INC.Inventors: Matthew Brown, Yi Chen, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiao He, Todd J. Kohn, Julia Winslow Lohman, Vatee Pattaropong, Jennifer Seganish, Youngsook Shin, Jillian L. Simard
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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: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Publication number: 20120077802Abstract: Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: June 9, 2010Publication date: March 29, 2012Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
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Publication number: 20120071479Abstract: Compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: September 14, 2011Publication date: March 22, 2012Applicant: NOVARTIS AGInventors: Gurdip Bhalay, Lee Edwards, Catherine Howsham, Peter Hunt, Nichola Smith
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Publication number: 20120022030Abstract: The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending on MK-2 or TNF activity, and ways of manufacturing them.Type: ApplicationFiled: September 13, 2010Publication date: January 26, 2012Inventors: Achim SCHLAPBACH, Lászlo RÉVÉSZ, Guido KOCH
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Publication number: 20120015928Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Publication number: 20120010193Abstract: Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.Type: ApplicationFiled: March 8, 2010Publication date: January 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
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Publication number: 20120004218Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein A1 to A3 and R1 to R10 have the significance given in claim 1, can be used as a medicament. These compounds are useful in the treatment or prophylaxis of diseases that are related to AMPK regulation, such as obesity, dyslipidemia, hyperglycemia, type 1 or type 2 diabetes and cancers.Type: ApplicationFiled: June 27, 2011Publication date: January 5, 2012Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Yongfu Liu, Hongying Yun, Mingwei Zhou
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Publication number: 20110312952Abstract: Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.Type: ApplicationFiled: February 16, 2010Publication date: December 22, 2011Inventors: Nicolas Lachance, Jean-Philippe Leclerc, Chun Sing Li, Oscar Miguel Moradei
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Publication number: 20110300104Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 3, 2011Publication date: December 8, 2011Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or