1,2-diazole (including Hydrogenated) Patents (Class 546/211)
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Publication number: 20100234395Abstract: Discloses is a pharmaceutical agent comprising an ureide derivative represented by the formula: or a pharmaceutically acceptable salt thereof as an active ingredient. The ureide derivative or the pharmaceutically acceptable salt thereof is useful for the relief of a pain or the treatment or prevention of neurogenic pain.Type: ApplicationFiled: March 27, 2007Publication date: September 16, 2010Applicant: TORAY INDUSTRIES, INC.Inventors: Yuji Sugawara, Naoki Izumimoto, Hideyuki Tsutsui
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Patent number: 7790753Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.Type: GrantFiled: April 17, 2006Date of Patent: September 7, 2010Assignee: sanofi-aventisInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Corinne Veronique
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Patent number: 7790711Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: July 14, 2008Date of Patent: September 7, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Paul Gillespie, Kevin Richard Guertin, Lida Qi, Qiang Zhang
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Patent number: 7786144Abstract: The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.Type: GrantFiled: May 29, 2007Date of Patent: August 31, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Bernard J. Van Vliet
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Publication number: 20100216841Abstract: The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: ApplicationFiled: June 28, 2006Publication date: August 26, 2010Inventors: James C. Barrow, Craig W. Lindsley, William D. Shipe, Zhiqiang Yang, David Wisnoski
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Publication number: 20100210617Abstract: The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y1 and Y2 is CH and the other is selected from CH, CR8 and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y1 or Y2 is CR8; R1 aryl or heteroaryl group of 5 to 10 ring members; R2a and R3a each are hydrogen, C1-4 hydrocarbyl or C1-4 acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR2aR3a forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R18 is hydrogen or methyl; R19 is hydrogen or methyl; R24 is hydrogen or R24, R2a and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R25 is hydrogen or a C1-4 alkyl group wherein the C1-4 alkyl group is optionally substituted by hydroxy or amino provided that there are at least two caType: ApplicationFiled: June 21, 2006Publication date: August 19, 2010Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Steven John Woodhead, Robert Downham, Christopher Hamlett, Steven Howard, Hannah Fiona Sore, Marinus Leendert Verdonk, David Winter Walker, Richard William Arthur Luke
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Publication number: 20100204470Abstract: The present invention provides a new method for preparation and crystallization of hydrochlorides, hydrobromides or hydroiodides of pharmaceutical compounds or their intermediates in which the base or its acid addition salt is reacted in a solvent with a Trialkylsilylhalogenide.Type: ApplicationFiled: June 25, 2007Publication date: August 12, 2010Inventors: Josef Wieser, Hannes Lengauer, Elfriede Klingler, Arthur Pichler, Hubert Sturm
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Publication number: 20100197691Abstract: Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: July 11, 2008Publication date: August 5, 2010Inventors: Steven L. Colletti, Hong Shen, Fa-Xiang Ding
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Patent number: 7767674Abstract: The present invention provides kinase inhibitors of Formula I:Type: GrantFiled: June 15, 2005Date of Patent: August 3, 2010Assignee: Eli Lilly and CompanyInventors: Tiechao Li, Mark Andrew Pobanz, Chuan Shih, Yong Wang, Boyu Zhong, Jesus Andres Blas, Alfonso De Dios, Beatriz Lopez De Uralde-Garmendia, Luisa Maria Martin Cabrejas
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Publication number: 20100190827Abstract: The present invention relates to a novel crystalline polymorph of rimonabant, its method of preparation and the pharmaceutical compositions containing this novel polymorph.Type: ApplicationFiled: October 28, 2008Publication date: July 29, 2010Applicant: SANOFI-AVENTISInventors: Alain ALCADE, Gilles Anne-Archard, Corinne Gavory, Olivier Monnier
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Publication number: 20100190780Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: February 9, 2010Publication date: July 29, 2010Inventors: Christian Laggner, Maria Rosa Cuberes-Altisent, Joerg Holenz, Juana Maria Berrocal-Romero, Maria Montserrat Contijoch-LLobet
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Publication number: 20100190988Abstract: A process for preparation of Pyrazole derivatives adapted for one pot reaction involving the use of a pyclizing agent and involving the step of amidation in the presence of a catalyst. The steps for isolation and purification of found Pyrazole derivatives are also disclosed.Type: ApplicationFiled: April 30, 2007Publication date: July 29, 2010Inventors: Darmesh Mahendrabhai Shah, Guruprasad Wader
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Patent number: 7754750Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.Type: GrantFiled: May 6, 2008Date of Patent: July 13, 2010Assignee: AstraZeneca ABInventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
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Publication number: 20100160377Abstract: The invention relates to derivatives of pyrazole 3,5-carboxylates, of general formula (I): in which R1, R2, R3, R4, R5, X, Y, V, W and n are as defined herein. The invention also relates to salts of these compounds as well as hydrates or of solvates, enantiomers, diastereoisomers and mixtures thereof. Also disclosed are the methods of preparation and application in therapeutics of compounds of formula (I).Type: ApplicationFiled: December 24, 2009Publication date: June 24, 2010Applicant: SANOFI-AVENTISInventors: Yann FORICHER, Martin SMRCINA, Viviane VAN DORSSELAER, Fabienne WEBER
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Publication number: 20100145042Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.Type: ApplicationFiled: February 16, 2010Publication date: June 10, 2010Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A.W. Van Der Neut, Cornelis G. Kruse
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Publication number: 20100144701Abstract: Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH,or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; R4 and R5 are independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy(C1-C4 alkyl)-, cycloalkyl, or fully or partially fluorinated C1-C4 alkyl; R1 (i) a bond; (ii) a divalent radical of formula —(CH2)aB1(CH2)b wherein a and b are independently O, 1, 2 or 3 provided thatType: ApplicationFiled: December 17, 2007Publication date: June 10, 2010Applicant: 7TM PHARMA A/SInventors: Martin Cooper, Jean-Marie Receveur, Thomas Hoegberg, Peter Aadal Nielsen, Jean-Michel Linget, Pia Marina Noeregaard, Anthony Murray, Emelie Bjurling
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Patent number: 7728029Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: March 14, 2007Date of Patent: June 1, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Kevin William Anderson, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Jr., Kevin Richard Guertin, Nancy-Ellen Haynes, Michael Paul Myers, Sherrie Lynn Pietranico-Cole, Lida Qi, Pamela Loreen Rossman, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley, Qiang Zhang
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Publication number: 20100125075Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: ApplicationFiled: December 14, 2006Publication date: May 20, 2010Applicant: British Biotech Pharmaceuticals Ltd.Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Publication number: 20100120757Abstract: The compounds of a certain formula 1, in which R1, R7, R8, R9 and n have the meanings as given in the description, are novel effective inhibitors of the type 4 phosphodiesterase.Type: ApplicationFiled: May 14, 2008Publication date: May 13, 2010Applicant: NYCOMED GmbHInventors: Beate Schmidt, Christian Scheufler, Juergen Volz, Martin Feth, Rolf-Peter Hummel, Armin Hatzelmann, Christof Zitt, Andrea Wohlsen, Degenhard Marx, Hans-Peter Kley, Deborah Ockert, Anke Heuser, Johannes A.M. Christiaans, Geert Jan Sterk, Wiro M.P.B. Menge
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Publication number: 20100113776Abstract: A novel pyrazole derivative of the following formula having a histamine H3 receptor antagonistic effect: or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation comprising the same as an active ingredient is effective for prevention or treatment of dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.Type: ApplicationFiled: December 14, 2007Publication date: May 6, 2010Applicant: TAISHO PHARMACEUTICAL CO.,LTD.Inventors: Toshio Nakamura, Dai Nozawa, Makoto Tatsuzuki, Hiroahi Ohta, Takeshi Kuwada, Tomoko Ishizaka, Tomoko Tamita, Seiji Masuda
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Publication number: 20100105684Abstract: The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the treatment or prophylaxis of various disorders of humans or animals.Type: ApplicationFiled: March 28, 2008Publication date: April 29, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover, Helmut Buschmann
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Publication number: 20100105896Abstract: Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: R is a group selected from C1-C10 alkyl; aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; A is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R? wherein v is equal to 1 or 2; R? is as defined in the present application; a ketone group of formula —C(O)—Z?, wherein Z? is as defined in the present application; a substituent having an hydroxyl function of formula —CH(OH)—Z?, being as defined in the present application; an amide substituent of formula —C(O)—NH-T?, T? being as defined in the present application; B is a group as defined in the present application; D is an heteroaryl optionally substituted.Type: ApplicationFiled: December 22, 2009Publication date: April 29, 2010Applicant: Neuroscienze Pharmaness S.C.a.R.I.Inventors: Paolo Lazzari, Stefania Rulu, Gerard Aime Pinna, Gabriele Murineddu
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Publication number: 20100099712Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals, especially in dyslipidaemia.Type: ApplicationFiled: January 17, 2008Publication date: April 22, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Susana Yenes-Minguez, Antonio Torrens-Jover
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Patent number: 7687481Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: GrantFiled: March 9, 2007Date of Patent: March 30, 2010Assignee: Jenrin Discovery, Inc.Inventors: John Francis McElroy, Robert J. Chorvat
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Publication number: 20100076022Abstract: The present invention discloses novel and stable polymorphs of rimonabant, its hydrates and solvates, to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention further discloses a novel and stable amorphous form of rimonabant, process for its preparation and a pharmaceutical composition comprising it. The present invention also provides an improved process for the preparation of rimonabant crystalline Form II. Thus, for example, rimonabant is dissolved in methylene dichloride, stirred for 10 minutes at 25-30° C. and then the solvent distilled off under vacuum at 40° C. The resulting residue is stirred with water and the separated solid is collected at 25-30° C. to give a stable crystalline rimonabant hydrate.Type: ApplicationFiled: September 1, 2006Publication date: March 25, 2010Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Publication number: 20100076197Abstract: The present invention provides an improved and commercially viable process for the preparation of rimonabant substantially free of amide impurity, namely 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl-4-methyl-pyrazole-3-carboxamide and its pharmaceutically acceptable acid addition salts thereof. Thus, for example, 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl-4-methyl-pyrazole-3-carboxylic acid chloride is reacted with 1-aminopiperidine in the presence of a base and optionally a phase transfer catalyst is used such as tetra-butylammonium bromide in a biphasic reaction medium containing water and a water-immiscible solvent to obtain pure rimonabant.Type: ApplicationFiled: September 11, 2006Publication date: March 25, 2010Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Publication number: 20100075993Abstract: The invention provides flavivirus replication inhibitors of WNV and other flaviviruses, such as, for example, JEV, SLEV, AV, KV, JV, CV, YV, TBEV, DENV-1, DENV-2, DENV-3, DENV-4, YFV and MVEV. The invention further provides pharmaceutical compositions including one or more such flavivirus replication inhibitors. The invention further provides methods of treatment, prevention, inhibition or amelioration of one or more diseases associated with flavivirus replication including administering one or more such inhibitors or pharmaceutical compositions.Type: ApplicationFiled: June 30, 2006Publication date: March 25, 2010Applicant: DREXEL UNIVERSITYInventors: Baohua Gu, Tim Block, Andy Cuconati
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Publication number: 20100076023Abstract: The invention relates to a pyrazole-3-carboxamide in amorphous form, to an amorphous solid solution containing the same, and more generally to pharmaceutical composition containing the sameType: ApplicationFiled: August 19, 2009Publication date: March 25, 2010Applicant: SANOFI-AVENTISInventors: Jean Alié, Jérome MENEGOTTO, Michel BAUER
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Publication number: 20100069364Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals, especially in dyslipidaemia.Type: ApplicationFiled: January 17, 2008Publication date: March 18, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Antonio Torrens-Jover, Susana Yenes-Minguez
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Publication number: 20100063067Abstract: The present application describes modulators of MIP-1? of formula (I), or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, A, T, R1, R2 and R8, are as 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 atherosclerosis using the modulators of formula (I) are disclosed.Type: ApplicationFiled: October 3, 2007Publication date: March 11, 2010Inventors: Percy H. Carter, Lyndon A.M. Cornelius
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Publication number: 20100063050Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.Type: ApplicationFiled: January 10, 2006Publication date: March 11, 2010Inventors: Alexandros Makriyannis, Rajesh Thotapally, Venkata Kiran Rao Vemuri, Teresa Olszewska
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Patent number: 7659407Abstract: Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: R is a group selected from: C1-C10 alkyl; aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; A is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R? wherein v is equal to 1 or 2; R? is as defined in the present application; a ketone group of formula —C(O)—Z?, wherein Z? is as defined in the present application; a substituent having an hydroxyl function of formula —CH(OH)—Z?, Z? being as defined in the present application; an amide substituent of formula —C(O)—NH—T?, T? being as defined in the present application; B is a group as defined in the present application; D is an heteroaryl optionally substituted.Type: GrantFiled: May 23, 2005Date of Patent: February 9, 2010Assignee: Neuroscienze Pharmaness S.C.a.R.I.Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
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Publication number: 20100010219Abstract: Provided is a method capable of efficiently producing a compound having a superior HSD1 inhibitory action and a compound useful as a synthetic intermediate therefor, with superior achievability of asymmetric synthesis (i.e., superior selectivity), superior yield, superior safety and superior industrial workability at a low cost. A method of producing a compound represented by the following formula [8]: or a salt thereof, or a solvate thereof, from a compound represented by the following formula [2]: or a reactive derivative thereof, or a salt thereof, or a solvate thereof.Type: ApplicationFiled: June 5, 2009Publication date: January 14, 2010Applicant: JAPAN TOBACCO INC.Inventors: Kazuhito Harada, Takashi Ito
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Publication number: 20100004243Abstract: The invention provides a cyclin dependent kinase (e.g. cdk-4 kinase) inhibitor of the formula (I) or a salt, tautomer, solvate or N-oxide thereof; wherein R1 is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group containing 0-2 heteroatoms selected from O, N and S wherein the optional substituents are selected from halogen, C1-4 alkyl, C1-4 alkoxy, C3-4 cycloalkyl and cyano, and wherein the C1-4 alkyl and C1-4 alkoxy groups are each optionally further substituted by C1-2 alkoxy or one or more halogen atoms; and E is a group E1, E2, E3 or E4: formulae E1, E2, E3, E4 wherein n, q, A5 B, T, U, V, W, Z, R2, R5, R6 and R7 are as defined in the claims.Type: ApplicationFiled: July 13, 2007Publication date: January 7, 2010Applicants: Astex Therapeutics Limited, Novartis AGInventors: Miles Stuart Congreve, Adrian Liam Gill, Steven Howard, Paul Neil Mortenson, Gillbert Ebai Besong
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Publication number: 20090318500Abstract: The invention provides the compound of formula (I) 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide in a substantially crystalline form, therapeutic uses thereof and pharmaceutical compositions containing the crystalline compound. The invention also provides novel pharmaceutical formulations containing 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide and novel processes for preparing the compound.Type: ApplicationFiled: May 4, 2007Publication date: December 24, 2009Applicant: Astex Therapeutics limitedInventors: Gary Trewartha, Eva Figueroa Navarro, David Charles Rees, Mladen Vinkovic, Andrew James Woodhead, Paul Graham Wyatt
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Publication number: 20090286758Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.Type: ApplicationFiled: May 19, 2009Publication date: November 19, 2009Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Patent number: 7608718Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.Type: GrantFiled: November 3, 2005Date of Patent: October 27, 2009Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Jacobus Tipker, Herman H. van Stuivenberg, Arnoldus H. J. Herremans
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Publication number: 20090253673Abstract: Certain novel N-acylated spiropiperidine derivatives are ligands of the human ghrelin receptor(s) and, in particular, are antagonists/inverse agonists of the human ghrelin receptor. They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of the ghrelin receptor, such as obesity, diabetes, and metabolic syndrome.Type: ApplicationFiled: July 6, 2007Publication date: October 8, 2009Inventors: Min Ge, Eric Cline, Lihu Yang, Sander G. Mills
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Publication number: 20090247525Abstract: The invention relates to compounds of formula I having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: March 2, 2007Publication date: October 1, 2009Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Publication number: 20090215825Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.Type: ApplicationFiled: March 19, 2009Publication date: August 27, 2009Inventors: Emma Parmee, Subharekha Raghavan, Teresa Beeson, Dong-Ming Shen
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Publication number: 20090209578Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, Het and m are as defined in the description. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors.Type: ApplicationFiled: November 27, 2006Publication date: August 20, 2009Inventors: Christopher Gordon Barber, David Clive Blakemore
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Patent number: 7576106Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: October 11, 2006Date of Patent: August 18, 2009Assignee: ChemoCentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, Wei Chen, Kevin Lloyd Greenman, Edward J. Sullivan, Lianfa Li
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Patent number: 7576218Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: October 11, 2006Date of Patent: August 18, 2009Assignee: ChemoCentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, Wei Chen, Kevin Lloyd Greenman, Lianfa Li, Edward J. Sullivan, Valeri V. Martichonok
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Publication number: 20090198060Abstract: Compounds effective for preventing, treatment or improving diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1, R2, R3, L1, L2, L3, X and Y are defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: June 7, 2007Publication date: August 6, 2009Applicant: Nissan Chemical Industries, Ltd.Inventors: Katsuaki Miyaji, Shunsuke Iwamoto, Yukihiro Shigeta, Yutaka Hirokawa, Shingo Oowada, Takanori Nakamura, Norihisa Ishiwata
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Publication number: 20090186895Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: May 17, 2007Publication date: July 23, 2009Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Bradley Teegarden, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, Honnappa Jayakumar, Thuy-Anh Tran, Sonja Strah-Pleynet, Jingdong Xu
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Patent number: 7557102Abstract: Novel compounds of the formula (I), in which R, R1, R2 and R3 have the meanings indicated in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.Type: GrantFiled: March 9, 2004Date of Patent: July 7, 2009Assignee: Merck Patent GmbHInventors: Werner Mederski, Christos Tsaklakidis, Dieter Dorsch, Bertram Cezanne, Johannes Gleitz
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Publication number: 20090170832Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted alkyl or the like, one of R2 and R4 is a group of formula: —Y—R5, wherein Y is —O— or the like, R5 is substituted alkyl (the substituent is optionally substituted cycloalkyl or the like), optionally substituted branched alkyl or the like, the other of R2 and R4 is hydrogen or optionally substituted alkyl, R3 is a group of formula: —C(?O)-Z-R6, wherein Z is —NR7— or —NR7—W—, R6 is optionally substituted cycloalkyl or the like, R7 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, X is ?N— or the like, with the proviso that compounds wherein R2 is 2-(morphorino)ethoxy, R3 is N-(1-adamantyl)carbamoyl and R1 is benzyl are excluded.Type: ApplicationFiled: November 20, 2006Publication date: July 2, 2009Applicant: SHIONOGI & CO., LTD.Inventors: Noriyuki Kurose, Mikayo Hayashi, Tomoyuki Ogawa, Koji Masuda, Eiichi Kojima
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Publication number: 20090170833Abstract: The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.Type: ApplicationFiled: February 27, 2009Publication date: July 2, 2009Applicant: Aventis Pharma S.A.Inventors: Arielle GENEVOIS-BORELLA, Jean-Luc MALLERON, Jean BOUQUEREL, Gilles DOERFLINGER, Andrees BOHME, Gaetan TOUYER, Jean-Francois SABUCO, Corrine TERRIER, Serge MIGNANI, Michel EVERS, Youssef EL-AHMAD
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Publication number: 20090156592Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: July 27, 2007Publication date: June 18, 2009Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Robert James Pasteris, Mary Ann Hanagan, Rafael Shapiro
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Publication number: 20090156642Abstract: The present invention provides 5-membered heterocycle compounds represented by the following general formula (I): The present compounds have a superior acid secretion inhibitory effect, and shows an antiulcer activity and the like.Type: ApplicationFiled: September 24, 2008Publication date: June 18, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Haruyuki Nishida, Yasuyoshi Arikawa, Keizo Hirase