The Additional Five-membered Hetero Ring Also Has Chalcogen As A Ring Member Patents (Class 514/254.02)
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Publication number: 20140073624Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: February 19, 2013Publication date: March 13, 2014Applicant: RIB-X PHARMACEUTICALS, INC.Inventor: Rib-X Pharmaceuticals, Inc.
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Publication number: 20140073648Abstract: A method of treating an immunologic disease. The method includes administering an aminothiazole-based inhibitor of myeloid differentiation protein 88 (MyD88) to a patient in need thereof. The inhibitor of MyD88 acts as an immunomodulator for treatment of the immunologic disease including but not limited to rejections after organ transplantation, chronic inflammatory diseases, autoimmune diseases, ischemia-reperfusion injuries, and endotoxemia and sepsis.Type: ApplicationFiled: September 1, 2013Publication date: March 13, 2014Applicants: Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd., Tongji Hospital Tongji Medical College Huazhong University of Science and TechnologyInventors: Ping ZHOU, Fengchao JIANG
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Publication number: 20140057914Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: ApplicationFiled: August 23, 2013Publication date: February 27, 2014Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer CenterInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu
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Patent number: 8658635Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: February 25, 2014Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20140031363Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3-R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.Type: ApplicationFiled: April 15, 2013Publication date: January 30, 2014Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Scott Myers, Yesim Altas Tahirovic
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Publication number: 20140031334Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: September 20, 2013Publication date: January 30, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
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Patent number: 8637559Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or —Y2—C(?O)— wherein Y1 is a group such as —C(?O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.Type: GrantFiled: November 14, 2006Date of Patent: January 28, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Minoru Okada, Masaya Kato, Norifumi Sato, Tetsuyuki Uno, Hideki Kitagaki, Junpei Haruta, Hidetaka Hiyama, Tomonori Shibata
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Publication number: 20140017199Abstract: The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: July 3, 2013Publication date: January 16, 2014Inventors: Manoj C. Desai, Allen Yu Hong, Hon Chung Hui, Hongtao Liu, Randall W. Vivian, Lianhong Xu
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Patent number: 8629102Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: GrantFiled: March 15, 2013Date of Patent: January 14, 2014Assignee: Mochida Pharmaceutical Co., Ltd.Inventor: Munetaka Ohkouchi
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Publication number: 20140004155Abstract: 2-aminothiazole derivatives represented by formula (I), where R1 and R2 represent cycloalkyls, respectively; or R1 represents a substituted aromatic group, and R2 represents H, a C1-C11 alkyl, —CH2Ph (benzyl), or a methyl ether including a C1-C11 alkyl. R3 is a substituent including an amino group. X represents a carbonyl or a methylene and n is an integer from 0 to 5.Type: ApplicationFiled: September 1, 2013Publication date: January 2, 2014Applicants: Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd., Huazhong University of Science & TechnologyInventors: Fengchao JIANG, Ping ZHOU, Jianguo CHEN, Yue WANG, Baoshuai CAO, Jia YAN
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Publication number: 20140005164Abstract: The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: ApplicationFiled: March 23, 2012Publication date: January 2, 2014Applicant: Siena Biotech S.p.A.Inventors: Maurizio Varrone, Massimiliano Travagli, Giacomo Minetto, Lucia Cesari, Simone Galeazzi, Andrea Caricasole, Antonio Chiumiento, Massimiliano Salerno
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Patent number: 8618110Abstract: The present invention includes and relates generally to compounds of structural Formula (I), or a salt, solvate, or prodrug thereof, which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.Type: GrantFiled: February 9, 2010Date of Patent: December 31, 2013Assignee: VM Discovery Inc.Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20130331380Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.Type: ApplicationFiled: February 21, 2013Publication date: December 12, 2013Applicant: LES LABORATOIRES SERVIERInventors: Vincent Lacoste, Pauline Lacoste, LES LABORATOIRES SERVIER
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Publication number: 20130331396Abstract: Certain piperazinyl and piperidinyl urea compounds 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. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: August 13, 2013Publication date: December 12, 2013Applicant: Janssen Pharmaceutica NVInventors: Richard Apodaca, J. Guy Breitenbucher, Kanaka Pattabiraman, mark Seierstad, Wei Xiao
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Patent number: 8604198Abstract: The present invention provides 3-{(2S,4S)-4-[4-(3-methyl -1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2 -ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and reproducible crystal structure, and a production method thereof.Type: GrantFiled: July 29, 2011Date of Patent: December 10, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Tomohiro Yoshida, Hiroshi Sakashita, Naoko Ueda, Shinji Kirihara, Satoru Uemori, Reiko Tsutsumiuchi, Fumihiko Akahoshi
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Patent number: 8604037Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.Type: GrantFiled: August 18, 2011Date of Patent: December 10, 2013Assignee: Purdue Pharma, L.P.Inventors: Qun Sun, Laykea Tafesse, Sam Victory
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Publication number: 20130324544Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.Type: ApplicationFiled: November 25, 2011Publication date: December 5, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
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Patent number: 8598162Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: GrantFiled: October 11, 2011Date of Patent: December 3, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Jun Matsubara, Yohji Sakurai
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Patent number: 8598179Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 17, 2010Date of Patent: December 3, 2013Assignee: SanofiInventors: Marc Nazaré, Gernot Zech, Jochen Goerlitzer, Melitta Just, Tilo Weiss, Gerhard Hessler, Werngard Czechtizky, Sven Ruf
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Publication number: 20130316999Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: ApplicationFiled: August 7, 2013Publication date: November 28, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
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Publication number: 20130309197Abstract: The present application provides for a compound of formula I, or a salt thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: December 20, 2011Publication date: November 21, 2013Applicant: Gilead Sciences, Inc.Inventors: Manoj C. Desai, Hon Chung Hui, Hongtao Liu, Jianyu Sun, Lianhong Xu
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Publication number: 20130310396Abstract: This invention provides deuterated thiazolidine derivatives and compositions comprising these compounds, which are useful agents for the treatment of hyperglycemia diseases or disorders, in particular diabetes mellitus. The disclosure also provides a method of treating hyperglycemia diseases or disorders, in particular diabetes mellitus, using these deuterated thiazolidine derivatives.Type: ApplicationFiled: January 18, 2012Publication date: November 21, 2013Inventors: Hongwen Zhu, Qiang Zhang
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Patent number: 8586589Abstract: The present invention relates to piperidine and piperazine phenyl sulfonamides 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, including for example the treatment of pain.Type: GrantFiled: October 2, 2012Date of Patent: November 19, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Esther Martinborough, Lev T. D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
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Patent number: 8586583Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: GrantFiled: October 2, 2012Date of Patent: November 19, 2013Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Nigel James Parr
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Patent number: 8586590Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: GrantFiled: October 2, 2012Date of Patent: November 19, 2013Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Nigel James Parr
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Patent number: 8580797Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: GrantFiled: April 28, 2010Date of Patent: November 12, 2013Assignee: Glaxo Smith Kline Intellectual Property Development LimitedInventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Nigel James Parr
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Publication number: 20130296335Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: March 29, 2013Publication date: November 7, 2013Inventors: Bradley P. MORGAN, Erica A. KRAYNACK, Pu-Ping LU, Alex MUCI, David J. MORGANS
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Publication number: 20130296310Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Patent number: 8569307Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.Type: GrantFiled: June 11, 2012Date of Patent: October 29, 2013Assignee: LG Life Sciences Ltd.Inventors: Soon Ha Kim, Hyoung Jin Kim, Sun Young Koo, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Seung Yup Paek, Hyo Shin Kwak, Dong Ook Seo, Eok Park
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Patent number: 8569348Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.Type: GrantFiled: January 12, 2010Date of Patent: October 29, 2013Assignee: Aerpio Therapeutics Inc.Inventors: Robert Shalwitz, Kevin G. Peters
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Publication number: 20130281406Abstract: The present invention relates to thiazole derivatives of Formula (I) and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: ApplicationFiled: April 21, 2010Publication date: October 24, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Eva CAROFF, Kurt HILPERT, Francis HUBLER, David LEHMANN, Emmanuel MEYER, Dorte RENNEBERG
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Publication number: 20130274254Abstract: The present application provides for a compound of formula I, and related compounds, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: December 20, 2011Publication date: October 17, 2013Applicant: Gilead Sciences, Inc.Inventors: Carina Cannizzaro, Manoj C. Desai, Hon Chung Hui, Melody S. Lee, Hongtao Liu, Jianyu Sun, Lianhong Xu
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Patent number: 8557824Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, K, G, E and WType: GrantFiled: September 19, 2008Date of Patent: October 15, 2013Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober, Wolfgang Staehle
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Patent number: 8557810Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: GrantFiled: January 24, 2012Date of Patent: October 15, 2013Assignee: Ambit Biosciences CorporationInventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Patent number: 8552000Abstract: A therapeutic/preventive agent for cognitive dysfunctions, which comprises as an active ingredient an imide derivative of the following formula [1]: wherein Z is a group of the formula [2]: D is a group of —(CH2)p-A-(CH2)q—; G is ?N—, —CH—, etc.; and Ar is an aromatic heterocyclic group, etc.Type: GrantFiled: February 29, 2012Date of Patent: October 8, 2013Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Yukihiro Ohno, Takeo Ishiyama
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Patent number: 8552001Abstract: Sulfoxide derivatives of the formula Ia to Im as described, and pharmaceutically usable salts, solvates, enantiomers, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for the treatment of tumors.Type: GrantFiled: September 14, 2010Date of Patent: October 8, 2013Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Wolfgang Staehle
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Publication number: 20130259800Abstract: The invention described herein pertains to the use of oxazolidinone antibiotics, alone or in combination, in the treatment of cancer. In particular, the invention pertains to the treatment of malignant gliomas, thyroid cancer or melanoma, or borderline forms of malignant glioma, thyroid cancer or melanoma.Type: ApplicationFiled: December 15, 2011Publication date: October 3, 2013Applicant: BIOVISTA, INC.Inventors: Andreas Persidis, Spyros Deftereos
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Publication number: 20130252969Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein one of R1 and R2 is H, and the other is selected from C1-8-alkyl, C3-6-cycloalkyl and C1-8-alkyl-C5-10-aryl; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl, cyclohexyl and 1-methylcyclopentyl; R9 is selected from the following: wherein: R4 is selected from C1-8-alkyl and C3-8-cycloalkyl; G is selected from: CH, CMe and N; E is selected from: O, S, SO2, NH, NMe and N-oxide (N?O); J and R are independently selected from: CH, N and N-oxide (N?O); and R41 is selected from amino, methylamino, dimethylamino, isopropylamino, isopropyl(methyl)amino, cyclopropylamino, cyclopropyl(methyl)amino, cyclopentylamino, morpholino, piperidin-1-yl, piperidin-1-ylmethyl, morpholinomethyl, 4-methylpiperazin-1-yl, 4-(2-methoxyethyl)piperazin-1-yl, 1-morpholinoethyl, 1-(dimethylamino)ethyl, 1-(methylamino)ethyl, 4-fluoro-1-methylpyrrolidin-2-yl, 4,4-difluoropiperidin-Type: ApplicationFiled: May 23, 2013Publication date: September 26, 2013Applicant: Amura Therapeutics LimitedInventors: Martin Quibell, John P. Watts
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Publication number: 20130245022Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl 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, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Applicant: Janssen Pharmaceutica NVInventors: J. GUY BREITENBUCHER, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Sierestad
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Publication number: 20130231349Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3 ; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteType: ApplicationFiled: March 14, 2013Publication date: September 5, 2013Applicant: MEDIVIR ABInventors: Lourdes Salvador ODEN, Magnus NILSSON, Pia KAHNBERG, Bertil SAMUELSSON, Urszula GRABOWSKA
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Publication number: 20130231321Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.Type: ApplicationFiled: April 16, 2013Publication date: September 5, 2013Applicant: H. LUNDBECK A/SInventors: Mathivanan Packiarajan, Allen Hopper, Anette Graven Sams, Gitte Kobberoee Mikkelsen, Michel Grenon
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Publication number: 20130210769Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: IRM LLCInventors: Hong Liu, Xiaohui He, Dean Paul Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
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Publication number: 20130210721Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: MOCHIDA PHARMACEUTICAL CO., LTD.
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Patent number: 8507538Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.Type: GrantFiled: November 15, 2010Date of Patent: August 13, 2013Assignee: Receptos, Inc.Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
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Publication number: 20130203730Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: March 13, 2013Publication date: August 8, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
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Publication number: 20130203772Abstract: The present invention is directed to a polymorph of a compound and salts of a compound and polymorphs thereof, which compound is an inhibitor of kinase activity.Type: ApplicationFiled: October 25, 2011Publication date: August 8, 2013Inventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Nigel James Parr, Robert David Willacy
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Publication number: 20130203709Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDAInventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
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Patent number: 8501781Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).Type: GrantFiled: October 27, 2010Date of Patent: August 6, 2013Assignee: Bayer Cropscience AGInventors: Pierre Cristau, Nicola Rahn, Tomoki Tsuchiya, Joachim Kluth, Pierre Wasnaire, Sebastian Hoffmann, Jürgen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
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Patent number: 8497274Abstract: Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.Type: GrantFiled: January 10, 2012Date of Patent: July 30, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Masanori Okaniwa, Terufumi Takagi, Masaaki Hirose
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Patent number: 8492374Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).Type: GrantFiled: April 28, 2010Date of Patent: July 23, 2013Assignee: Industrial Technology Research InstituteInventors: On Lee, Chih-Hung Chen, Chi-Y Hung, Yow-Lone Chang, Ting-Shou Chen