The Five-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/368)
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Publication number: 20100286123Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: April 27, 2010Publication date: November 11, 2010Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
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Publication number: 20100285470Abstract: Monomethine dyes that have no or minimal fluorescence in buffer or in the presence of single stranded DNA or RNA, but strongly fluoresce in the presence of double-stranded DNA. In one embodiment, the dye is useful in quantitative RT-PCR.Type: ApplicationFiled: September 30, 2008Publication date: November 11, 2010Applicant: Thermo Fisher Scientific (Milwaukee) LLCInventors: Charles K. Brush, Jianqin Liu, Peter Czerney, Matthias Wenzel
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Publication number: 20100280030Abstract: Compounds of the formula (I), in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 8, 2008Publication date: November 4, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Patent number: 7820673Abstract: The present invention provides a urea derivative or a salt thereof, which is useful as a therapeutic agent for thrombosis.Type: GrantFiled: December 15, 2004Date of Patent: October 26, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Keiji Kubo, Yasuhiro Imaeda
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Patent number: 7820657Abstract: 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: March 16, 2007Date of Patent: October 26, 2010Assignee: Ambit Biosciences CorporationInventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Patent number: 7816376Abstract: The invention relates to compounds of the formula (I) and pharmaceutically usable derivatives, salts, solvates and stereoisomers and mixtures thereof, in which X, Y, Z, R1, R3, R4, R8, p, k, E, G, Z and Q are as defined in claim 1, which are employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's, Parkinson's or Huntington's disease, cerebral ischaemia, infarction or psychoses.Type: GrantFiled: March 5, 2003Date of Patent: October 19, 2010Assignee: Merck Patent GmbHInventors: Oliver Schadt, Joachim Leibrock, Helmut Pruecher, Christoph Seyfried
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Patent number: 7807672Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.Type: GrantFiled: February 13, 2007Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: Yongqi Deng, Gerald W. Shipps, Jr., Alan Cooper, Yang Nan, Tong Wang, M. Arshad Siddiqui, Hugh Zhu, Robert Sun, Joseph M. Kelly, Ronald Doll, Jagdish Desai, James J-S Wang, Youhao Dong, Vincent Madison, Li Xiao, Alan Hruza, Neng-Yang Shih
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Patent number: 7795284Abstract: A subject of the present invention is 4,7-dioxobenzothiazole-2-carboxamide derivatives, which inhibit the cdc25 phosphatases, in particular cdc25-C phosphatase. These compounds can in particular be used in the treatment of cancer.Type: GrantFiled: November 7, 2005Date of Patent: September 14, 2010Assignee: Ipsen Pharma S.A.S.Inventors: Marie-Odile Galcera-Contour, Grégoire Prevost, Alban Sidhu
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Patent number: 7790726Abstract: 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: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Patent number: 7790886Abstract: 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: GrantFiled: January 5, 2009Date of Patent: September 7, 2010Assignees: Dr. Reddy's Laboratories, Inc., Dr. Reddy's Laboratories LimitedInventors: Manne Satyanarayana Reddy, Thirumalai Rajan Srinivasan, Venka Bhaskara Rao Uppala, Mummadi Venkatesh, Akundi Surya Prabhakar
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Publication number: 20100222341Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumours.Type: ApplicationFiled: September 19, 2008Publication date: September 2, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HARTUNGInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Patent number: 7786125Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: GrantFiled: April 7, 2009Date of Patent: August 31, 2010Inventor: Leu-Fen H. Lin
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Publication number: 20100216810Abstract: 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: ApplicationFiled: December 1, 2009Publication date: August 26, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masanori OKANIWA, Terufumi TAKAGI
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Publication number: 20100216809Abstract: The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-mType: ApplicationFiled: June 5, 2008Publication date: August 26, 2010Applicant: Janssen Pharmaceutica N.V.Inventors: Jean-Pierre André Marc Bongartz, Lieven Meerpoel, Gustaaf Maria Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
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Publication number: 20100216787Abstract: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula.Type: ApplicationFiled: December 22, 2009Publication date: August 26, 2010Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Masakazu Sato, Yuko Matsunaga, Hajime Asanuma, Hideaki Amada, Takeshi Koami, Tetsuo Takayama, Tetsuya Yabuuchi, Fumiyasu Shiozawa, Hironori Katakai, Hiroki Umemiya, Akiko Ikeda
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Publication number: 20100210663Abstract: Hybrid compounds containing an aminotetralin moiety or a heterocyclic and/or open chain analog thereof linked through an alkylene group to an aryl ring system-substituted piperidiene moiety exhibit high levels of CNS activity, in some cases exhibiting especially high relative binding efficiencies between D3 and D2 dopaminergic receptor subtypes.Type: ApplicationFiled: April 29, 2010Publication date: August 19, 2010Applicant: WAYNE STATE UNIVERSITYInventor: Aloke K. Dutta
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Publication number: 20100210662Abstract: The present invention relates to 3-disubstituted indol-2-one derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: February 9, 2010Publication date: August 19, 2010Applicant: SANOFI-AVENTISInventors: Marco BARONI, Letizia PULEO
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Patent number: 7777037Abstract: A process for preparing ziprasidone having low levels of keto ziprasidone and hydroxy ziprasidone impurities.Type: GrantFiled: October 26, 2005Date of Patent: August 17, 2010Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Sundaram Venkataraman, Uppala Venkata Bhaskara Rao, Venkateswarlu Muvva, Vijayawardhan Chitta
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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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Patent number: 7750013Abstract: The present disclosure relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The disclosure also relates to the use of the compounds for the manufacture of a medicament giving a beneficial effect. The disclosure also relates to the use of the compounds for the manufacture of a medicament for treating a disease or condition. The disclosure further relates to the treatment of CNS-disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive compulsive disorder, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of cognition and memory. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.Type: GrantFiled: August 15, 2006Date of Patent: July 6, 2010Assignee: Solvay Pharmaceuticals, B.V.Inventors: Theodorus S. M. Koopman, Hendrink J. Koster, Peter H. Van Amsterdam, Roelof W. Feenstra, Marinus Verhage, Andrew C. McCreary, Mayke B. Hesselink, Gustaaf J. M. Van Scharrenburg
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Patent number: 7737166Abstract: A 1,6-?-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-?-glucan synthesis inhibition. Also provided is a drug, a salt or hydrate thereof, especially an antifungal that contains the compound.Type: GrantFiled: August 16, 2006Date of Patent: June 15, 2010Assignee: Daiichi Sankyo Company, LimitedInventors: Katsuhiro Kawakami, Kazuo Kanai, Takao Horiuchi, Hiroshi Takeshita, Syozo Kobayashi, Yuichi Sugimoto, Issei Achiwa, Junichi Kuroyanagi
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Publication number: 20100144712Abstract: A triazole derivative of formula 1 or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof is superior to the conventional antifungal drugs in antifungal activity against a wide spectrum of pathogenic fungi, and has advantageously low toxicity.Type: ApplicationFiled: June 12, 2008Publication date: June 10, 2010Applicants: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, CHEMON INC.Inventors: Bum Tae Kim, Yong Ki Min, Jung Nyoung Heo, Hyuk Lee, Sung Youn Chang, No Kyun Park, Si-Whan Song, Jung-Ja Oh
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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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Patent number: 7728136Abstract: A novel method for preparing a compound of formula I which comprises of coupling the piperazine derivative of formula II with alkyl halide containing compound of the formula III by heating in solvent free conditions or, optionally, in a minimum quantity of non-aqueous suspending liquid, in presence of a catalyst and a neutralizing agent to neutralize the hydrohalic acid.Type: GrantFiled: June 16, 2005Date of Patent: June 1, 2010Assignee: Lupin LimitedInventors: Om Dutt Tyagi, Tushar Kumar Srivastava, Yogendra Kumar Chauhan, Vasanth Kumar Nalam
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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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Patent number: 7714130Abstract: Methods of making Gonadotropin Releasing Hormone (“GnRH”) (also known as Leutinizing Hormone Releasing Hormone) receptor antagonists, comprising reacting a compound having Formula I: with a compound having formula Lg—(CR13R14)k—D, are disclosed.Type: GrantFiled: June 16, 2005Date of Patent: May 11, 2010Assignee: WyethInventors: Alexander V. Gontcharov, Gulnaz Khafizova, John R. Potoski, Donna Mary Huryn
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Publication number: 20100113772Abstract: A method for forming an optionally substituted 2-aminobenzoxazole compound includes: contacting an optionally substituted 2-aminophenol compound with (1) an amine of the formula NHR2R3, wherein R2 and R3 are each independently selected from H, an optionally substituted alkyl group or an optionally substituted aryl group, or R2 and R3, taken together with the nitrogen atom to which they are attached, form an optionally substituted heterocyclic ring; and (2) a reactant selected from the group consisting of: (a) C(OR)4, wherein R represents an alkyl group; (b) C(OAr)4, wherein Ar represents an aryl group; and (c) CCl2(OAr)2, wherein Ar represents an aryl group, in combination with a base; thereby forming the optionally substituted 2-aminobenzoxazole compound.Type: ApplicationFiled: October 23, 2009Publication date: May 6, 2010Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventor: Christopher CIOFFI
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Patent number: 7709485Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: October 9, 2007Date of Patent: May 4, 2010Assignee: GlaxoSmithkline LLCInventors: Jakob Busch-Petersen, Michael R Palovich, Katherine L. Widdowson
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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: 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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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: 20100069378Abstract: The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: July 25, 2007Publication date: March 18, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria de las Ermitas Alcalde-Pais, Maria de les Neus Mesquida-Estevez, Sara Lopez-Perez
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Patent number: 7678799Abstract: Provided is crystalline ziprasidone HCl and processes for preparation thereof.Type: GrantFiled: June 3, 2004Date of Patent: March 16, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Anna Balanov, Judith Aronhime, Boaz Gome, Tamas Koltai, Natalia Shenkar, Marioara Mendelovici, Ehud Amir
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Patent number: 7671077Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: GrantFiled: July 19, 2004Date of Patent: March 2, 2010Inventor: Leu-Fen Hou Lin
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Publication number: 20100048555Abstract: Compounds of formula (I): are inhibitors of MARK, and hence useful for treatment of disorders involving 10 hyperphosphorylation of tau.Type: ApplicationFiled: July 20, 2007Publication date: February 25, 2010Inventors: Ian Churcher, Victoria Alexandra Doughty, Peter Hunt, Matthew Stanton
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Publication number: 20100029681Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of heterocyclic compounds are disclosed of the general formula (1) where X1 and X2 are linkers and W is an optionally substituted imidazolyl, oxazolyl, thiazolyl, benzimidazolyl, benzoxazolyl, or benzothiazolyl.Type: ApplicationFiled: May 25, 2007Publication date: February 4, 2010Inventors: Hassan Pajouhesh, Yanbing Ding
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Publication number: 20100029682Abstract: The present invention relates to novel chromene or thiochromene carboxamide derivatives, the preparation of same, pharmaceutical compositions of same and the use of same as dopamine D3 ligands as a medicament for central nervous system disorders.Type: ApplicationFiled: July 20, 2007Publication date: February 4, 2010Inventors: Pierre Sokoloff, Thierry Imbert, Laurent Vergnes, Florence Cuisiat
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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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Patent number: 7642274Abstract: The invention aims to provide a drug having an activity on inhibiting a decrease in pain threshold. Since a ?-opioid receptor agonist effectively inhibits the decrease in pain threshold, it is useful as an inhibitor of pain threshold decrease.Type: GrantFiled: July 2, 2004Date of Patent: January 5, 2010Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kyoichi Shimomura, Hiroyuki Aono, Yaeko Tsukahara, Taeko Hata
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Publication number: 20090312310Abstract: There is provided a novel compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. The present invention provides an imidazothiazole derivative represented by the following formula (1) having various substituents that inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity: wherein R1, R2, R3, R4, and R5 in the formula (1) each has the same meaning as defined in the specification.Type: ApplicationFiled: June 11, 2009Publication date: December 17, 2009Inventors: Haruko Kawato, Masaki Miyazaki, Yuuichi Sugimoto, Hiroyuki Naito, Tooru Okayama, Tsunehiko Soga, Kouichi Uoto
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Publication number: 20090312550Abstract: 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: ApplicationFiled: June 17, 2009Publication date: December 17, 2009Applicant: DIPHARMA FRANCIS SRLInventors: Gianpiero Ventimiglia, Pietro Allegrini, Gabriele Razzetti, Domenico Magrone, Alberto Bologna
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Patent number: 7625902Abstract: The invention is concerned with novel imidazolidinone derivatives of formula (I): wherein R1 to R11 and X are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used in pharmaceutical compositions.Type: GrantFiled: March 24, 2008Date of Patent: December 1, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Ulrike Obst Sander, Stephan Roever, Tanja Schulz-Gasch, Matthew Wright
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Patent number: 7625889Abstract: The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.Type: GrantFiled: July 25, 2007Date of Patent: December 1, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: Paul Robert Eastwood, Hazel Hunt, David Mark Fink, Helen Katherine Smith, Richard Simon Todd
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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: 20090286974Abstract: A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein Ring Q is optionally substituted monocyclic aryl, optionally substituted monocyclic heteroaryl, optionally substituted fused aryl or optionally substituted fused heteroaryl, Y1 is a bond or —NR6— or the like, Ring A is optionally substituted nonaromatic heterocyclediyl, a group of the formula: -Y2Z1- is a group of the formula: R7 are each independently hydrogen, optionally substituted lower alkyl or the like, R8 and R9 are each independently hydrogen or optionally substituted lower alkyl, n is an integer between 1 and 3, Z1 is a bond, —O—, —S— or —NR9—, Ring B is optionally substituted aromatic carbocyclediyl or optionally substituted aromatic heterocyclediyl, Y3 is a bond, optionally substituted lower alkylene optionally intervened by —O—, optionally substituted lower alkenylene or the like, and Z2 is COOR3 or the like.Type: ApplicationFiled: August 24, 2006Publication date: November 19, 2009Inventors: Akiko Itai, Susumu Muto, RYuko Tokuyama, Hiroshi Fukasawa, Takafumi Ohara, Terukazu Kato
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Publication number: 20090281088Abstract: The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.Type: ApplicationFiled: March 25, 2009Publication date: November 12, 2009Applicant: Global Alliance for TB Drug DevelopmentInventors: Charles Z. Ding, Genliang Lu, Keith Combrink, Dianjun D. Chen, Minsoo Song, Jiancheng Wang, Zhenkun Ma, Brian Desmond Palmer, Adrian Blaser, Andrew M. Thompson, Iveta Kmentova, Hamish Scott Sutherland, William Alexander Denny
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Patent number: 7608711Abstract: A process for the preparation of ziprasidone and a novel intermediate useful in its preparation. The process comprises the reduction of a compound (III) to give a compound (V) which is then reduced to compound (II). This is reacted with compound (IV) to give the desired compound.Type: GrantFiled: November 13, 2006Date of Patent: October 27, 2009Assignee: Dipharma Francis SrlInventors: Jacopo Zanon, Oscar Martini, Francesco Ciardella, Luca Gregori, Federico Sbrogio, Andrea Castellin
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Publication number: 20090264405Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: October 30, 2006Publication date: October 22, 2009Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
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Patent number: 7605162Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.Type: GrantFiled: October 27, 2008Date of Patent: October 20, 2009Assignee: Solvay PharmaceuticalsInventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Gerben M. Visser, Bernard J. Van Vliet