The Additional Five-membered Hetero Ring Consists Of Three Ring Carbons, And Of Nitrogen And Chalcogen In Adjacent Ring Positions (e.g., Isoxazolyl, Isothiazolyl, Etc.) Patents (Class 514/254.04)
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Publication number: 20100197630Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.Type: ApplicationFiled: June 16, 2008Publication date: August 5, 2010Inventors: Julianne A. Hunt, Rogelio L. Martinez, Peter J. Sinclair, Ramzi F. Sweis
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Publication number: 20100179138Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.Type: ApplicationFiled: February 19, 2010Publication date: July 15, 2010Applicants: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., The Institute Of Cancer ResearchInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20100168121Abstract: Compositions and methods for treating disorders of the outer retina with compounds with 5-HT1A agonist activity are disclosed.Type: ApplicationFiled: March 8, 2010Publication date: July 1, 2010Applicant: ALCON, INC.Inventors: Robert J. Collier, JR., Michael A. Kapin, Mark R. Hellberg, Thomas R. Dean
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Publication number: 20100160323Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: December 22, 2009Publication date: June 24, 2010Inventors: Alexander Bischoff, Hosahalli Subramanya, Kumar Sundaresan, Srinivasa Raju Sammeta, Anil Kumar Vaka
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Publication number: 20100159034Abstract: The present invention relates to new pyrrolidinone inhibitors of PDE-4 activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 15, 2009Publication date: June 24, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100137329Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.Type: ApplicationFiled: February 8, 2010Publication date: June 3, 2010Applicant: SANOFI-EVENTISInventors: Ahmed ABOUABDELLAH, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
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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: 20100119622Abstract: The present invention relates to new 3H-benzooxazol-2-one modulators of D2 receptors and/or 5-HT1A receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 15, 2009Publication date: May 13, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100105697Abstract: The present invention is directed to therapeutic agents of the formula (I) which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. wherein; R1 is C1-6alkyl, which is unsubstituted or substituted with 1-6 fluoro, wherein R1 and the hydroxyl group on the ring are attached to the same carbon atom; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 3, 2008Publication date: April 29, 2010Inventors: Mark T. Bilodeau, Kausik K. Nanda, B. Wesley Trotter
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Publication number: 20100099676Abstract: A compound represented by the general formula (I): wherein R1 is wherein R26 and R28 are each independently lower alkyloxy and the like; n1 is an integer of 0 to 3; Z is a optionally substituted C1-C5 alkynylene which may be interrupted with a substituent selected from Substituent group a and the like; A is a group represented by the formula: wherein R6 and R7 are each independently lower alkyl and the like; m and n are each independently 0, 1, or 2; R2 is a hydrogen atom and the like; R3 is optionally substituted lower alkyl and the like; R4 is a hydrogen atom; or R3 and R4 may be taken together with an adjacent carbon atom to from a ring; R5 is hydroxyl and the like, or an optically active isomer, a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: October 31, 2007Publication date: April 22, 2010Applicant: SHIONOGI & CO., LTD.Inventors: Takeshi Endoh, Yasuhiko Fujii, Eiichi Kojima, Genta Tadano, Naoko Yamaguchi, Yo Adachi, Sachie Tagashira, Yuki Tachibana, Naohiro Onodera
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Patent number: 7691889Abstract: Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts act as antibacterial agents. Also mentioned is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai., including administering an antimycobacterially effective amount of the compound and/or pharmaceutically acceptable salts. There is also mentioned a process for the manufacture of the compound or its pharmaceutically acceptable salts.Type: GrantFiled: March 18, 2005Date of Patent: April 6, 2010Assignee: Lupin LimitedInventors: Sudershan Kumar Arora, Vijaykumar Jagdishwar Patil, Prathap Sreedharan Nair, Prasad Purushottam Dixit, Shankar Ajay, Rakesh Kumar Sinha
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Publication number: 20100081668Abstract: The present invention provides pharmaceutically applicable compounds and polymorphs belonging to the ziprasidone hydrobromide compound group with antipsychotic effect. The present invention provides hydrobromide polymorphs of 5-{-2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-ethyl}-6-chloro-1,3-dihydro-2H-indol-2-one, ziprasidone of Formula (I) having neuroleptic activity.Type: ApplicationFiled: November 23, 2007Publication date: April 1, 2010Inventors: József Neu, Adám Demeter, Zoltán Varga, Balázs Havasi, Sándor Garadnay, Béla Hegedüs
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Patent number: 7687503Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.Type: GrantFiled: June 22, 2006Date of Patent: March 30, 2010Assignee: Sanofi-AventisInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
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Publication number: 20100074973Abstract: The present invention relates to new thioxanthene modulators of dopamine D2 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: August 21, 2009Publication date: March 25, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manouchehr M. Shahbaz, Sepehr Sarshar
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Publication number: 20100075985Abstract: The present invention provides compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders.Type: ApplicationFiled: September 16, 2009Publication date: March 25, 2010Inventors: Kimberly J. Prior, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Publication number: 20100075984Abstract: Compounds of formula (I), and their pharmaceutically acceptable salts and solvates, wherein X represents —O—, —NH—, —S—, —NHC(?O)— or —NHC(?S)—; R1 represents —H or a hydrocarbon chain; R2 represents —H, alkoxy, amino, a hydrocarbon chain or a radical of a cycle; R3 represents —H, a hydrocarbon chain or a radical of a cycle; R4 represents —H or a hydrocarbon chain; alternatively R3 and R4 form together a cycle; R5 and R6 represent —H or halogen, and R7 represents —H, a hydrocarbon chain or heteroaryl, are useful against bacterial infections in animals, including humans.Type: ApplicationFiled: January 18, 2007Publication date: March 25, 2010Applicant: LABORATORIOS SALVAT, S.A.Inventors: José Hidalgo Rodríguez, Juan Lorenzo Catena Ruiz, Isabel Masip Masip, Maria del Carmen Serra Comas, Oscar Rey Puiggrós, Carmen Lagunas Arnal, Carolina Salcedo Roca, Dolors Balsa López
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Publication number: 20100022511Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.Type: ApplicationFiled: September 5, 2008Publication date: January 28, 2010Inventors: Fang-Yu Liu, Zhi-qun Shen
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Patent number: 7652047Abstract: The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones.Type: GrantFiled: July 11, 2008Date of Patent: January 26, 2010Assignee: Ardea Biosciences, Inc.Inventors: Hassan El Abdellaoui, Robert Tam, Huanming Chen, Varaprasad Chamakura, Dinesh Barawkar, Andreas Maderna, Zhi Hong, Stanley Lang
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Publication number: 20100015195Abstract: Novel injectable depot compositions are provided comprising at least one active agent(s) optionally with one or more pharmaceutically acceptable excipient(s) in the form of a multi-component system preferably comprising at least two components which when administered to a subject in need thereof forms an in situ gel depot or implant at the site of injection upon contact with body fluids. Also described are process for preparation of such compositions and method of using such compositions.Type: ApplicationFiled: October 3, 2007Publication date: January 21, 2010Inventors: Rajesh Jain, Kour Chand Jindal, Sampath Kumar Devarajan
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Publication number: 20100016299Abstract: The present application relates to novel substituted benzoxepinoisoxazole derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis, restenosis and ischemias.Type: ApplicationFiled: June 28, 2007Publication date: January 21, 2010Applicant: BAYER HEALTHCARE AGInventors: Nils Griebenow, Anja Buchmüller, Peter Kolkhof, Hilmar Bischoff
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Publication number: 20100004254Abstract: 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: ApplicationFiled: July 8, 2009Publication date: January 7, 2010Applicant: Purdue Pharma L.P.Inventors: Qun Sun, Laykea Tafesse, Sam Victory
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Publication number: 20090311347Abstract: Treatment regimens for mood disorders that include administration of buprenorphine, alone or in combination with additional pharmacological agents are described. Specifically, treatment regimens that alleviate racing thoughts associated with bipolar disorder, and pharmaceutical compositions and kits for use therein are described. Dosing regimens, compositions, and kits including buprenorphine for treating mania associated with opioid withdrawal are also described.Type: ApplicationFiled: April 10, 2009Publication date: December 17, 2009Inventors: Bryan T. Oronsky, Neil C. Oronsky
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Publication number: 20090298806Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: January 5, 2009Publication date: December 3, 2009Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Publication number: 20090291939Abstract: Certain atypical antipsychotic medications (particularly clozapine) or combinations of medications are useful to treat alcohol or other substance abuse, particularly in the general (non-schizophrenic) population. Generally stated, one aspect of the invention features a method of treating a patient suffering from alcohol or other substance abuse by administering to the patient medication effective to rectify an abuse-associated dysfunction in the DA-mediated brain reward circuit. A second aspect of the invention features administering medication that strongly antagonizes ?2 andrenergic receptors and weakly antagonizes dopamine D2 receptors. Preferably, the ratio of ?2 receptor blockade to D2o receptor blockade is similar to that of clozapine. The medication may be a single compound (such as clozapine or risperidone), or it may include two or more compounds which together achieve the specified function.Type: ApplicationFiled: August 5, 2009Publication date: November 26, 2009Inventors: Alan I. Green, Wing Ming Keung, Joseph Schildkraut, David Chau
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Publication number: 20090291963Abstract: Substituted indoles of the formula (I) and physiologically acceptable derivatives and salts thereof, in which R1, D, E, R12, p, X1, E, G, X2 and Z are as defined in claim 1, exhibit particular actions on the central nervous system, especially 5HT reuptake-inhibiting and 5 HTx-agonistic and/or -antagonistic actions and in particular serotonin-agonistic and -antagonistic properties and can be employed as antipsychotics, neuroleptics, antidepressants, anxiolytics and/or antihypertonics.Type: ApplicationFiled: July 29, 2009Publication date: November 26, 2009Inventors: Oliver SCHADT, Henning Böttcher, Joachim Leibrock, Kai Schiemann, Timo Heinrich, Günter Hölzemann, Christoph van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
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Publication number: 20090286806Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of isoxazole containing compounds are disclosed of the general formula (1) where Z is N or CHNR3 and (Ar1)2CR4 is optionally substituted benzhydryl.Type: ApplicationFiled: April 17, 2007Publication date: November 19, 2009Inventors: Hassan Pajouhesh, Richard Holland, Hossein Pajouhesh
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Publication number: 20090281078Abstract: The invention relates to adjunctive and simultaneous combination therapies for the treatment of psychotic disorders in which sabcomeline or a pharmaceutically acceptable salt thereof and at least one other neuroleptic agent are administered adjunctively or simultaneously. The invention provides methods of treatment of psychotic disorders utilising such adjunctive or simultaneous therapeutic combination therapies, therapeutic combinations for use therein and pharmaceutical compositions comprising them.Type: ApplicationFiled: July 16, 2009Publication date: November 12, 2009Inventors: Carol ROUTLEDGE, James Joseph Hagan, Stuart Paul Cuffe
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Publication number: 20090275594Abstract: The present invention is directed to novel 3-hydrazone piperazinyl rifamycin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.Type: ApplicationFiled: May 4, 2009Publication date: November 5, 2009Inventors: Mark J. MACIELAG, Manomi Tennakoon
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Patent number: 7612060Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: October 11, 2005Date of Patent: November 3, 2009Assignee: Amgen Inc.Inventors: Toshihiro Aya, Guolin Cai, Jian J. Chen, Derin D'Amico, Thomas Nguyen, Wenyuan Qian
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Publication number: 20090264416Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.Type: ApplicationFiled: August 19, 2008Publication date: October 22, 2009Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett
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Publication number: 20090247544Abstract: Certain substituted urea derivatives modulate diskeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and are useful in the treatment of obesity, sarcopenia, wasting syndrome, frailty, muscle spasm, cachexia, neuromuscular diseases (e.g., amyotrophic lateral sclerosis, spinal muscular atrophy, familial or acquired myopathies or muscular dystrophies), post-surgical and post-traumatic muscle weakness, and other conditions.Type: ApplicationFiled: February 13, 2009Publication date: October 1, 2009Inventors: Bradley P. MORGAN, Fady MALIK, David J. MORGANS, JR.
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Publication number: 20090221583Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: June 23, 2008Publication date: September 3, 2009Applicants: FOREST LABORATORIES HOLDINGS LIMITED, AURIGENE DISCOVERY TECHNOLOGIES LIMITEDInventors: Alexander BISCHOFF, Hosahalli SUBRAMANYA, Kumar SUNDARESAN, Srinivasa Raju SAMMETA, Anil Kumar VAKA
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Publication number: 20090192154Abstract: A sultam derivative of Formula (1) described below having inhibitory action for aggrecanase activity is provided. The sultam derivative of Formula (1) and a salt thereof exhibit strong inhibitory action for aggrecanase activity in a living body of a mammalian animal including human, and is useful, for example, as an active ingredient of a pharmaceutical agent for preventing and/or treating various diseases caused by degradation of aggrecan.Type: ApplicationFiled: December 23, 2008Publication date: July 30, 2009Applicant: Asahi Kasei Pharma CorporationInventors: Naomi MAEKAWARA, Masakazu Atobe, Masashi Kawanishi, Eiichi Tanaka
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Patent number: 7563794Abstract: Ziprasidone base or a pharmaceutically acceptable salt thereof free from colored impurities, in particular those giving the product a “slightly pink to pink” coloration.Type: GrantFiled: March 7, 2006Date of Patent: July 21, 2009Assignee: Dipharma Francis S.r.l.Inventors: Gianpiero Ventimiglia, Pietro Allegrini, Gabriele Razzetti, Domenico Magrone, Alberto Bologna
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Publication number: 20090176800Abstract: A method of evaluating memory/learning functions with the use of a model with glutamic acid N-methyl-D-aspartate (NMDA) type receptor hypofunction as an animal model for schizophrenia and with the use of reference memory task, wherein there has been found concrete means for detecting any differences in activity between typical anti-psychosis drugs and atypical anti-psychosis drugs is found. An in vivo animal model for screening of a therapeutic agent for improving cognitive dysfunction by schizophrenia is provided.Type: ApplicationFiled: March 11, 2009Publication date: July 9, 2009Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventor: Takeo ISHIYAMA
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Publication number: 20090176768Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.Type: ApplicationFiled: March 17, 2009Publication date: July 9, 2009Inventors: JAY P. POWERS, Daqing Sun, Xuelei Yan
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Publication number: 20090163508Abstract: An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.Type: ApplicationFiled: October 9, 2008Publication date: June 25, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni KORI, Mitsunori Kouno
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Publication number: 20090163514Abstract: The invention includes benzisoxazole piperazine compositions and methods of using them for modulating sleep.Type: ApplicationFiled: February 11, 2009Publication date: June 25, 2009Inventors: Daniel Coughlin, James F. White, Kazumi Shiosaki, David G. Hangauer, Michael Solomon, Dale M. Edgar
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Patent number: 7550469Abstract: The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: GrantFiled: December 21, 2006Date of Patent: June 23, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: James A Hendrix, Joseph T Strupczewski, Kenneth Bordeau, Matthias Urmann, Gregory Shutske, Horst Hemmerle, John G Jurcak, Harpal Gill, Franz J Weiberth, Thaddeus Nieduzak, Sharon Anne Jackson, Xu-Yang Zhao, Paul Justin Mueller
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Publication number: 20090143404Abstract: A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1?R,2?S,3?R,4?S)-2,3-bicyclo[2,2,1]-heptanedicarboxyimide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied.Type: ApplicationFiled: May 26, 2006Publication date: June 4, 2009Inventor: Kazuyuki Fujihara
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Publication number: 20090143365Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.Type: ApplicationFiled: December 15, 2008Publication date: June 4, 2009Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Tak Adrien Li
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Publication number: 20090137605Abstract: The present invention is related to crystalline forms of ziprasidone and its hydrochloride salt and an amorphous form of ziprasidone hydrochloride and the process for the preparation thereof. The crystalline forms and amorphous form of the invention are suitable for pharmaceutical purposes in the treatment of psychosis. The processes of the invention are simple, non-hazardous and commercially suitable.Type: ApplicationFiled: January 5, 2009Publication date: May 28, 2009Applicants: DR. REDDY'S LABORATORIES LIMITED, DR. REDDY'S LABORATORIES, INC.Inventors: Manne Satyanarayana Reddy, Thirumalai Rajan Srinivasan, Venka Bhaskara Rao Uppala, Mummadi Venkatesh, Akundi Surya Prabhakar
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Publication number: 20090131397Abstract: The present application is directed to a new class of isoxazoles and their use as estrogen modulators.Type: ApplicationFiled: October 31, 2008Publication date: May 21, 2009Inventors: Simon Bailey, Stephen Douglas Barrett, Larry Don Bratton, Stephen Alan Fakhoury, Sandra Marie Jennings, Lorna Helen Mitchell, Raj Kumar Raheja, Veerabahu Shanmugasundaram
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Patent number: 7524848Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.Type: GrantFiled: March 22, 2007Date of Patent: April 28, 2009Assignee: Amgen Inc.Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan
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Publication number: 20090099170Abstract: 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: February 15, 2008Publication date: April 16, 2009Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch
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Publication number: 20090099199Abstract: The invention relates to compound of the formula I wherein the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: October 15, 2008Publication date: April 16, 2009Inventors: Joachim Nozulak, David Orain, Simona Cotesta
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Patent number: 7511046Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: July 21, 2006Date of Patent: March 31, 2009Assignee: Aventis Hoklings Inc.Inventors: David M Fink, Brian S Freed, Nicholas J Hrib, Raymond W Kosley, George E Lee, Gregory H Merriman, Barbara S Rauckman
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Publication number: 20090076027Abstract: The present application describes deuterium-enriched lurasidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090075974Abstract: Disclosed is a pharmaceutical composition for prophylaxis and treatment of pancreatitis comprising a 5-HT2A receptor antagonist as an effective component, wherein the binding activity (pKi) of the 5-HT2A receptor antagonist to a 5-HT2A receptor is higher at least by 1.0 than the binding activities to a 5-HT2B receptor and a 5-HT2C receptor. Preferably the binding activity (pKi) of the 5-HT2A receptor antagonist to the 5-HT2A receptor is at least 7.0, and more preferably at least 8.0. The present invention also provides a method of identifying a candidate substance for prophylactic and therapeutic agent for pancreatitis, comprising determining whether a test substance has a 5-HT2A receptor antagonistic activity.Type: ApplicationFiled: April 27, 2006Publication date: March 19, 2009Applicant: UMN Pharma Inc.Inventors: Isamu Yamaguchi, Kentaro Hamada, Yasunari Kashihara
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Publication number: 20090062294Abstract: 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 23, 2008Publication date: March 5, 2009Inventors: Richard Apodaca, J. Guy Breitenbucher, Natalie A. Hawryluk, William M. Jones, John M. Keith, Jeffrey E. Merit, Mark S. Tichenor, Amy K. Timmons