Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/552)
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Patent number: 7803792Abstract: A method for inhibiting ileal bile acid transporter activity in a subject, comprising administering to said subject an effective amount of a compound represented by formula (1):Type: GrantFiled: April 30, 2007Date of Patent: September 28, 2010Assignee: Asahi Kasei Pharma CorporationInventors: Takehiko Sasahara, Mitsunobu Mohri
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Publication number: 20100227848Abstract: The present invention is directed to oxo bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors 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 orexin receptors are involved.Type: ApplicationFiled: May 14, 2008Publication date: September 9, 2010Inventors: Christopher D. Cox, David B. Whitman
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Publication number: 20100222323Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: December 7, 2009Publication date: September 2, 2010Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford, James P. Harding
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Publication number: 20100216770Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, s, t, R1, R2, R3, R4, R5, X, Y, Q, Z, G, E and D have defined meanings.Type: ApplicationFiled: September 19, 2008Publication date: August 26, 2010Inventors: Pierre-Henri Storck, Bruno Schoentjes, Arnaud Marcel Pierre Piettre, Philipp Ermert, Virginie Sophie Poncelet, Imre Christian Francis Csoka
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Publication number: 20100197657Abstract: The present invention provides 2-aryl or heteroaryl indole derivatives which are ASIC channel modulators, maceutical compositions containing such compounds, and methods of using them as therapeutic agents.Type: ApplicationFiled: September 22, 2008Publication date: August 5, 2010Inventors: Ronald K. Chang, Christina Ng Di Marco, Scott D. Kuduk
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Publication number: 20100174065Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: January 28, 2009Publication date: July 8, 2010Applicant: GLAXO GROUP LIMITEDInventors: Jag Paul HEER, Thomas Daniel HEIGHTMAN, David Nigel HURST, Christopher Norbert JOHNSON, John SKIDMORE, Ian David WALL
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Publication number: 20100173890Abstract: The present invention relates to new compounds of formula I, or salts, solvates or solvated salts thereof, process for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in the treatment of 5-HT6 mediated disorders such as Alzheimer's disease, cognitive disorders, cognitive impairment associated with schizophrenia, obesity and Parkinson's disease.Type: ApplicationFiled: July 3, 2006Publication date: July 8, 2010Applicant: AstraZeneca ABInventors: Gunnar Nordvall, Fernando Sehgelmeble
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Publication number: 20100173823Abstract: In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as ?2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the ?2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.Type: ApplicationFiled: March 12, 2010Publication date: July 8, 2010Inventors: Kevin D. McCormick, Christopher W. Boyce, Neng-Yang Shih, Robert G. Aslanian, Pietro Mangiaracina, Manuel de Lera Ruiz, Younong Yu, Purakkattle Biju, Chia-Yu Huang, Bo Liang, Ruiyan Liu, Rong-Qiang Liu, Lisa Guise-Zawacki
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Publication number: 20100152440Abstract: The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods.Type: ApplicationFiled: June 8, 2009Publication date: June 17, 2010Inventors: Andrew Robert Marks, Donald W. Landry, Shi Xian Deng, Zhen Zhuang Cheng
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Publication number: 20100144703Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
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Patent number: 7718644Abstract: The present invention provides methods for limiting or preventing a decrease in the level of RyR2-bound FKBP12.6 in a subject. The present invention further provides methods for treating and preventing atrial and ventricular cardiac arrhythmias, heart failure, and exercise-induced sudden cardiac death in a subject. Additionally, the present invention provides use of JTV-519 in a method for limiting or preventing a decrease in the level of RyR2-bound FKBP12.6 in a subject who has, or is a candidate for, atrial fibrillation. Also provided are uses of 1,4-benzothiazepine derivatives in methods for treating and preventing atrial and ventricular cardiac arrhythmias and heart failure in a subject, and for preventing exercise-induced sudden cardiac death. The present invention also provides methods for identifying agents for use in treating and preventing atrial fibrillation and heart failure, and agents identified by these methods.Type: GrantFiled: March 25, 2004Date of Patent: May 18, 2010Assignee: The Trustees of Columbia University in the City of New YorkInventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng, Zhen Zhuang Cheng
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Patent number: 7713966Abstract: The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: GrantFiled: November 20, 2007Date of Patent: May 11, 2010Assignee: Alantos Pharmaceuticals Holding, Inc.Inventors: Christian Gege, Matthias Schneider, Carine Chevrier, Hongbo Deng, Irving Sucholeiki, Brian M. Gallagher, Jr., Michael Bosies, Christoph Steeneck, Xinyuan Wu, Matthias Hochgürtel, Bert Nolte, Arthur Taveras
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Publication number: 20100112090Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.Type: ApplicationFiled: April 16, 2008Publication date: May 6, 2010Applicant: KISSEI PHARMACEUTICAL CO., LTDInventors: Shigeru Yonekubo, Takashi Miyagi, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
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Publication number: 20100105657Abstract: The present invention relates to new compounds of formula (I), or salts, solvates or solvated salts thereof, process for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in the treatment of 5-HT6 mediated disorders such as Alzheimer's disease, cognitive disorders, cognitive impairment associated with schizophrenia, obesity and Parkinson's disease.Type: ApplicationFiled: July 3, 2006Publication date: April 29, 2010Applicant: AstraZeneca ABInventors: Gunnar Nordvall, Carl Petersson, Fernando Sehgelmeble
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Patent number: 7704990Abstract: The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells. Such disorders and diseases include, by way of example only, cardiac disorders and diseases, skeletal muscular disorders and diseases, cognitive disorders and diseases, malignant hyperthermia, diabetes, and sudden infant death syndrome.Type: GrantFiled: August 25, 2005Date of Patent: April 27, 2010Assignee: The Trustees of Columbia University in the City of New YorkInventors: Donald W. Landry, Shixian Deng, Zhen Zhuang Cheng
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Publication number: 20100087418Abstract: Compounds represented by the general formula (I): wherein each symbol is as defined in the description [with the proviso that 9-chloro-7-(1,1-dimethylethyl)-2,3,4,5-tetrahydro-1,4-benz-oxazepine and N-[[(5S)-2-oxo-3-(2,3,4,5-tetrahydro-1,4-benz-oxazepin-7-yl)-5-oxazolidinyl]methyl]acetamide are excluded], salts of the same, and prodrugs thereof have selective activation effect on serotonin 5-HT2C receptor and are useful as preventive and therapeutic agents for lower urinary tract diseases, obesity, and/or pelvic organ prolapse.Type: ApplicationFiled: March 6, 2008Publication date: April 8, 2010Inventors: Junya Shirai, Takahiro Matsumoto, Izumi Kamo
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Publication number: 20100087419Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.Type: ApplicationFiled: October 2, 2009Publication date: April 8, 2010Inventors: Richard C. A. Isaacs, Wayne J. Thompson, Peter D. Williams, Dai-Shi Su, Shankar Venkatraman, Mark W. Embrey, Thorsten E. Fisher, John S. Wai, David C. Dubost, Richard G. Ball, Eric J. Choi, Tao Pei, Sarah L. Trice, Neil Campbell, Matthew Maddess, Peter E. Maligres, Michael Shevlin, Zhiguo Jake Song, Dietrich P. Steinhuebel, Neil A. Strotman, Jingjun Yin
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Publication number: 20100087420Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: ApplicationFiled: December 4, 2009Publication date: April 8, 2010Applicant: ALANTOS PHARMACEUTICALS HOLDINGS, INC.Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgürtel, Hongbo Deng, Brian M. Gallagher, JR., Irving Sucholeiki, Arthur G. Taveras
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Patent number: 7666864Abstract: 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: GrantFiled: March 25, 2009Date of Patent: February 23, 2010Assignee: 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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Publication number: 20100004222Abstract: Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 22, 2007Publication date: January 7, 2010Applicant: Renovis, Inc.Inventors: Michael G. Kelly, Carl J. Kaub, John Kincaid, Satyanarayana Janagani, Guoxian Wu, Zhi-Liang Wei, Kiran Sahasrabudhe, Matthew Duncton, Ravindra B. Upasani, Yunfeng Fang, Matthew Cox, Jianhua He
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Publication number: 20100004221Abstract: Thiazepine derivative or a pharmacologically acceptable salt thereof having an effect of inhibiting 11?-hydroxysteroid dehydrogenase type 1 and having a formula (1): wherein in one embodiment, R1 represents a hydrogen atom, a C1-C6 alkyl group; R2 represents a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C1-C6 hydroxyalkyl group; R1 represents a hydrogen atom or a C1-C6 alkyl group; R4 represents a C6-C10 aryl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group a or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group a; Substituent Group a consists of a halogen atom, a C1-C6 alkyl group, a C6-C10 aryl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group b; Substituent Group b consists of a halogen atom, a C1-C6 alkyl group, and a C1-C6 halogenated alkyl group.Type: ApplicationFiled: June 26, 2009Publication date: January 7, 2010Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Toru Hasegawa, Tsuyoshi Shinozuka
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Patent number: 7625892Abstract: The present invention refers to pharmaceutical preparations including as active compounds 3-aza-bicyclo[3.2.1]octane derivatives of general formula (I) and/or their dimers of general formula (II) and (III) acting as agonists of human neurotrophines. Therefore, such compounds of formula (I), (II) and (III) are useful for treatment of diseases in which the neurotrophine functions are involved in defect, particularly of Nerve Growth Factor (NGF), such as neurodegenerative diseases of central nervous system (CNS), acquired immunodeficiency due to a reduced NGF biodisponibility, or morbous conditions in which the stimulus of neoangiogenesis process is convenient.Type: GrantFiled: June 18, 2003Date of Patent: December 1, 2009Assignee: Mimetech S.r.l.Inventors: Antonio Guarna, Federico Cozzolino, Maria Torcia, Enrico Garaci
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Patent number: 7625887Abstract: It is intended to provide a TGR5 receptor agonist containing a fused ring compound represented by the following general formula, its salt or a prodrug thereof: (1) wherein ring A represents an optionally substituted aromatic ring; and the ring B? represents a 5- to 8-membered ring having one or more substituents; which is useful in treating various diseases.Type: GrantFiled: January 27, 2004Date of Patent: December 1, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Fumio Itoh, Shuji Hinuma, Naoyuki Kanzaki, Yuji Kawamata, Taisuke Tawaraishi, Yuji Ishichi, Mariko Hirohashi
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Publication number: 20090292119Abstract: The present invention provides improved methods for synthesizing novel benzothiazepine compounds. In particular, the invention relates to a new method that generally is used to make the substituted 2,3,4,5-tetrahydro-1,4-benzothiazepine compounds of a general formula which then may be used to make many other benzothiazepine compounds.Type: ApplicationFiled: October 31, 2008Publication date: November 26, 2009Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Donald W. Landry, Shixian Deng, Zhen Z. Cheng
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Publication number: 20090264407Abstract: Substituted sulfonamide compounds corresponding to formula I: a process for their preparation, pharmaceutical compositions comprising such compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment of pain or other disorders or diseases that are mediated at least in part by B1R receptors.Type: ApplicationFiled: April 8, 2009Publication date: October 22, 2009Applicant: GRUENENTHAL GmbHInventors: Stefan OBERBOERSCH, Melanie REICH, Stefan SCHUNK, Michael ENGELS, Ruth JOSTOCK, Tieno GERMANN, Sabine HEES
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Publication number: 20090258856Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
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Publication number: 20090253681Abstract: Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R1, R2, R3, R4, R5, R6, R7; R8, R9 and R10 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HTV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HTV infection and ADDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: March 22, 2006Publication date: October 8, 2009Inventors: Vincenzo Summa, Paola Pace, Philip Jones, Alessia Petrocchi, Maria del Rosario Rico Ferreira, Giuseppe Cecere
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Patent number: 7598237Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 28, 2007Date of Patent: October 6, 2009Assignee: WyethInventors: Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
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Publication number: 20090227788Abstract: The invention provides a process for preparing a 2,3,4,5-tetrahydro[1,4]benzothiazepine of formula: by reacting a [2-(acylaminoethyl)thio]arene of formula with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reacting the [2-(acylaminoethyl)thio]arene with the aldehyde or multimer thereof and a base to form an [N-hydroxymethyl-2-[acylaminoethyl)thio]arene of formula then treating the [N-hydroxymethyl-2-(acylaminoethyl)thio]arene with the acid to form the 2,3,4,5-tetrahydro[1,4]benzothiazepine.Type: ApplicationFiled: March 3, 2009Publication date: September 10, 2009Inventors: Shixian Deng, Sandro Belvedere, Jiaming Yan, Donald Landry
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Patent number: 7566707Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: June 10, 2004Date of Patent: July 28, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Norbert Hauel, Elke Langkopf, Frank Himmelsbach, Iris Kauffmann-Hefner, Mohammad Tadayyon, Michael Mark
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Publication number: 20090182140Abstract: An alicyclic heterocyclic compound represented by the following formula or a pharmaceutically acceptable salt thereof: wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., P1 and P2 are CH or N, q and r are 0 to 2, X is —NH—, —O—, —CH2—, etc., Y is —CH2—, —CO—, —SO2—, etc., Z is —CO—, —SO2—, etc., and R3 is carbocyclic group, heterocyclic group, hydroxyl, alkoxy or amino, is useful as a controlling agent of the function of CCR4 useful for the prevention or treatment for bronchial asthma, atopic dermatitis, etc.Type: ApplicationFiled: November 30, 2006Publication date: July 16, 2009Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Shigeru Furukubo, Hiroshi Miyazaki
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Patent number: 7544678Abstract: The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods.Type: GrantFiled: March 23, 2005Date of Patent: June 9, 2009Assignee: The Trustees of Columbia University In the City of New YorkInventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng, Zhen Zhuang Cheng
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Publication number: 20090131402Abstract: The present invention relates to a serotonin 5-HT2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered ring optionally having substituent(s) other than an oxo group wherein the combination of m and n (m,n) is (1,2), (2,1), (2,2), (3,1), (3,2) or (4,1), or a salt thereof or a prodrug thereof, and a fused heterocyclic compound having a serotonin 5-HT2C receptor activating action and the like.Type: ApplicationFiled: May 15, 2007Publication date: May 21, 2009Inventors: Junya Shirai, Tomokazu Kusumoto, Hiroyuki Nagamiya, Izumi Kamo
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Publication number: 20090105211Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: ApplicationFiled: March 14, 2008Publication date: April 23, 2009Applicant: Exelixis, Inc.Inventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
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Publication number: 20090105214Abstract: Compounds of formula (I), wherein R1, R4, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: May 23, 2006Publication date: April 23, 2009Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20090075973Abstract: The present invention provides benzo-fused heterocyclic compounds having the structure of formula I, as well as prodrugs, stereoisomers, racemates, salts, hydrates, solvates, acid salt hydrates and isomorphic crystalline forms thereof. The compounds directly or indirectly modulate the activity of one or more cannabinoid receptors and can be incorporated into pharmaceutical preparations that are useful for the prevention and treatment of a variety of diseases and conditions, including pain, inflammation and pruritis.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Applicant: CARA THERAPEUTICS, INC.Inventors: Jason S. Newcom, Carla M. Gauss, Gary R. Gustafson
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Publication number: 20090062253Abstract: The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression.Type: ApplicationFiled: August 28, 2008Publication date: March 5, 2009Applicant: KALYPSYS, INC.Inventors: Timothy C. Gahman, Cunxiang Zhao, Hengyuan Lang, Mark Eben Massari
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Patent number: 7491714Abstract: Quinoline and naphthridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.Type: GrantFiled: December 3, 2003Date of Patent: February 17, 2009Assignee: Glaxo Group LimitedInventors: Jeffrey Michael Axten, Catherine Genevieve Yvette Dartois, Guy Marguerite Marie Gerard Nadler, Neil David Pearson
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Publication number: 20090042856Abstract: A pyridazinone derivative compound shown by the following formula (I): wherein R1 is selected from hydrogen, etc.; R2 is selected from substituted or unsubstituted aryl, etc.; R3 is hydrogen, etc.; p is 0, 1 or 2; R4 and R5, are each hydrogen, etc.; R6 and R7, are taken together to form a group of the formula: wherein R8 is hydrogen; X is selected from oxygen, etc; R10 is selected from hydrogen, etc.; R11 is selected from hydrogen, etc.; R12 is selected from hydrogen, etc.; R13 is selected from hydrogen, etc.; R14 is selected from hydrogen, etc.; m and n are each 0, 1, or 2, or a pharmaceutically acceptable salt thereof, which is useful as a medicament.Type: ApplicationFiled: August 31, 2006Publication date: February 12, 2009Applicants: Astellas Pharma Inc, Wakunaga Pharmaceutical Co., Ltd.Inventors: Hitoshi Yamazaki, Chiyoshi Kasahara, Hirokazu Kubota, Toru Kontani, Toru Asano, Hidekazu Mizuhara, Masaharu Yokomoto, Keiji Misumi, Tomohiko Kinoshita
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Publication number: 20090029965Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.Type: ApplicationFiled: August 24, 2005Publication date: January 29, 2009Applicant: Ferring B.V.Inventors: Andrzej Roman Batt, Martin Lee Stockley, Michael Bryan Roe, Celine Marguerite Simone Heeney, Andrew John Baxter, Peter Hudson, Rachel Handy
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Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Publication number: 20080293690Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.Type: ApplicationFiled: April 30, 2008Publication date: November 27, 2008Inventors: John M. Fevig, Dean A. Wacker
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Publication number: 20080261951Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ?O, —O(CH2)pO— or —S(CH2)S—; W1 is either O or S; X1 and X2 are both H, or together are ?O or ?S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.Type: ApplicationFiled: June 23, 2008Publication date: October 23, 2008Inventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Christopher Martyn Yea, Richard Jeremy Franklin
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Publication number: 20080234250Abstract: The invention concerns compounds according to general formulae 1, wherein G1 is an amine. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.Type: ApplicationFiled: August 18, 2005Publication date: September 25, 2008Inventor: Gary Robert William Pitt
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Publication number: 20080207592Abstract: The invention relates to the compound of the formula (A) and also to its physiologically acceptable salts. The compound is suitable as, for example, a hypolipidemic.Type: ApplicationFiled: January 7, 2008Publication date: August 28, 2008Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Wendelin FRICK, Heiner GLOMBIK, Hubert HEUER, Hans-Ludwig SCHAEFER, Stefan THEIS
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Publication number: 20080194539Abstract: The invention relates to annelated phenyl piperazine and phenyl diazepane carboxamides of general formula (I) containing oxygen. The compounds are suitable for medical use.Type: ApplicationFiled: December 27, 2005Publication date: August 14, 2008Applicant: Schwarz Pharma AGInventors: Peter Gmeiner, Harald Hubner, Karin Schlotter
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Patent number: 7407950Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. Said compounds are ligands of the TRPV1 vanilloid receptor, and are therefore, useful for treating diseases associated with TRPV1 receptors, such as pain and inflammation.Type: GrantFiled: June 20, 2007Date of Patent: August 5, 2008Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Publication number: 20080154035Abstract: The present invention relates to a coupling method between intramolecular carbon using the intramolecular cyclization reaction in situ of an allyl-indium compound derived from an allyl derivative containing an unsaturated hydrocarbon compound and indium, in presence of a transition metal compound catalyst. More particularly, the present invention relates to a coupling method between intramolecular carbon for preparing a cyclic compound having a vinyl group as a substituent by bonding a carbon in an allyl derivative containing an unsaturated hydrocarbon compound and a carbon in the unsaturated hydrocarbon compound via intramolecular cyclization reaction in situ of an allyl-indium compound as a coupling agent derived from the allyl derivative containing the unsaturated hydrocarbon and indium (In), in presence of a palladium catalyst.Type: ApplicationFiled: July 17, 2007Publication date: June 26, 2008Applicant: PHIL HO LEEInventors: Phil Ho LEE, Kooyeon LEE, Dong SEOMOON, Hyunseok KIM
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Publication number: 20080081803Abstract: The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: ApplicationFiled: October 15, 2004Publication date: April 3, 2008Inventors: Gabor Butora, Stephen D. Goble, Alexander Pastemak, Lihu Yang, Changyou Zhou, Christopher R. Moyes
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Patent number: 7312208Abstract: Drugs useful for the treatment and prevention of hyperlipidemia, moreover drugs useful for the treatment and prevention of cholestasis-caused hepatopathy, particularly primary biliary cirrhosis and primary sclerosing cholangitis, and drugs for the treatment and prevention of obesity, fatty liver and steatohepatitis, containing as active ingredients benzothiazepine compounds having a thioamide bond and a quaternary ammonium substituent, represented by formula (1) below are provided. Also, drugs containing ileal bile acid transporter inhibiting compounds as active ingredients for the treatment and prevention of cholestasis-caused hepatopathy are provided.Type: GrantFiled: August 26, 2003Date of Patent: December 25, 2007Assignee: Asahi Kasei Pharma CorporationInventors: Takehiko Sasahara, Mitsunobu Mohri