Three Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 514/211.1)
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Publication number: 20120244149Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: May 22, 2012Publication date: September 27, 2012Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
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Publication number: 20120245144Abstract: Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: March 20, 2012Publication date: September 27, 2012Applicant: Genentech, Inc.Inventors: Timothy Heffron, Brian Safina, Steven Staben, Daniel P. Sutherlin, BinQing Wei, Richard Elliott, Robert Heald, Eileen M. Seward, Emanuela Gancia, Bohdan Waskowycz
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Patent number: 8263586Abstract: 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: GrantFiled: May 14, 2008Date of Patent: September 11, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher D. Cox, David B. Whitman
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Patent number: 8242104Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: September 27, 2010Date of Patent: August 14, 2012Assignee: F. Hoffman-La Roche AGInventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
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Publication number: 20120196848Abstract: Provision of a compound having a serotonin 5-HT2C receptor activating action. A compound represented by the formula (I): wherein each symbol is as described in the description, or a salt thereof.Type: ApplicationFiled: August 3, 2010Publication date: August 2, 2012Inventors: Takahiro Matsumoto, Izumi Nomura
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Publication number: 20120165312Abstract: 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: March 2, 2012Publication date: June 28, 2012Inventors: Junya SHIRAI, Tomokazu Kusumoto, Hiroyuki Nagamiya, Izumi Kamo
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Publication number: 20120157440Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4, n, and R7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: December 13, 2011Publication date: June 21, 2012Inventors: TODD W. BUTLER, Ramalakshmi Y. Chandrasekaran, Scot R. Mente, Chakrapani Subramanyam, Travis T. Wager
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Publication number: 20120135979Abstract: Provided is a compound having a serotonin 5-HT2C receptor activating action, useful for lower urinary tract conditions, obesity and cancer. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: June 14, 2010Publication date: May 31, 2012Inventors: Shigekazu Sasaki, Tomokazu Kusumoto, Izumi Nomura, Hironobu Maezaki
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Publication number: 20120122843Abstract: The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compounds, processes for making said compounds, and their use as medicaments for treatment and/or prevention of A?-related diseases.Type: ApplicationFiled: November 9, 2011Publication date: May 17, 2012Applicant: ASTRAZENECA ABInventors: István MACSÁRI, Kim PAULSEN, Laszlo RAKOS, Britt-Marie SWAHN, Magnus WALDMAN, Didier ROTTICCI, Stefan VON BERG
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Patent number: 8158617Abstract: 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: GrantFiled: May 15, 2007Date of Patent: April 17, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Junya Shirai, Tomokazu Kusumoto, Hiroyuki Nagamiya
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Publication number: 20120071462Abstract: Compounds of formula (I): wherein R1 represents a hydrogen atom or a heterocyclic, cyano, alkoxycarbonyl, alkylsulphonylaminoalkyl or N-hydroxycarboximidamide group. Medicinal products containing the same which are useful as modulators of the AMPA receptor.Type: ApplicationFiled: September 15, 2011Publication date: March 22, 2012Applicant: LES LABORATOIRES SERVIERInventors: Alexis Cordi, Patrice Desos, Pierre Lestage, Laurence Danober
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Publication number: 20120058989Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, D, E, G, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: April 7, 2011Publication date: March 8, 2012Applicant: Achaogen, Inc.Inventors: Allan S. Wagman, Heinz E. Moser, Glenn A. McEnroe, James B. Aggen, Martin S. Linsell, Adam A. Goldblum, John H. Griffin, Lloyd J. Simons, Thomas R. Belliotti, Christina R. Harris, Toni-Jo Poel, Michael J. Melnick, Ricky D. Gaston
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Publication number: 20120015930Abstract: The present invention provides substituted imidazoheterocycles having the general structure of formula I: wherein Y is chosen from —O—, —OCRgRh—, —CRgRhO—, —CRgRh—, —(CRgRh)2—, —NRi—, —CRgRhNRi— and —NRiCRgRh—. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: December 1, 2009Publication date: January 19, 2012Applicant: CARA THERAPEUTICS, INC.Inventors: Stephen J. O'Connor, Jason S. Newcom, Janet L. Ralbovsky, Gary R. Gustafson, R. Paul Beckett, Robert Zhiyong Luo
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Publication number: 20120003291Abstract: Medical devices comprising nanobeads encapsulating one or more bioactive agents and methods of use thereof are provided.Type: ApplicationFiled: September 13, 2011Publication date: January 5, 2012Applicant: Abbott Cardiovascular Systems Inc.Inventors: Charles H. Craig, John E. Papp, Dudley Jayasinghe, Lionel G. Hines, Dennis Orosa
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Publication number: 20110288070Abstract: This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein (I), Q, J, L and Z are as defined in the specification.Type: ApplicationFiled: May 5, 2009Publication date: November 24, 2011Inventors: Kathryn Rogers, Holger Patzke
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Patent number: 8063038Abstract: 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: GrantFiled: August 18, 2005Date of Patent: November 22, 2011Assignee: Vantia LimitedInventor: Gary Robert William Pitt
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Publication number: 20110263567Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.Type: ApplicationFiled: September 11, 2009Publication date: October 27, 2011Applicant: Semmelweis EgyetemInventors: Péter Mátyus, Kálmán Magyar, Marjo Pihlavisto, Klára Gyires, Norbert Haider, Yinghua Wang, Patrick Woda, Petra Dunkel, Éva Tóth-Sarudy, Gÿorgy Túrós
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Patent number: 8039458Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: October 31, 2006Date of Patent: October 18, 2011Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Yasutsugu Ueda, John D. Matiskella, Michael A. Walker, Jacques Banville, Francis Beaulieu, Carl Ouellet, Serge Plamondon
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Patent number: 7998950Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: July 24, 2009Date of Patent: August 16, 2011Assignee: Gilead Sciences, Inc.Inventors: Evangelos Aktoudianakis, Azim Alan Celebi, Zhimin Du, Salman Y. Jabri, Haolun Jin, Choung U. Kim, Jiayao Li, Samuel E. Metobo, Michael R. Mish, Barton W. Phillips, Joseph H. Saugier, Zheng-Yu Yang, Catalin Sebastian Zonte
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Patent number: 7981879Abstract: 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: GrantFiled: March 22, 2006Date of Patent: July 19, 2011Assignee: Instituto di Ricerchi di Biologia Molecolare P. Angeletti S.p.A.Inventors: Vincenzo Summa, Paola Pace
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Publication number: 20110166124Abstract: The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose.Type: ApplicationFiled: July 21, 2009Publication date: July 7, 2011Inventors: Kevin D. McCormick, Robert G. Aslanian, Pietro Mangiaracina, Michael Y. Berlin, Manuel De Lera Ruiz, Christopher W. Boyce, Jianhua Chao, Pauline C. Ting, Junying Zheng, Stuart B. Rosenblum
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Publication number: 20110136782Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof (wherein, R1 to R6 each independently represents a hydrogen atom, unsubstituted or substituted C1-20 alkyl group and the like, R1 and R2, R3 and R4, or R5 and R6 may together form an unsubstituted or substituted 5- to 8-membered ring, A-B, in which A represents a carbon atom and B represents a nitrogen atom, represents the formula: C?N and the like, Y represents an oxygen atom and the like, X and X? each independently represent an unsubstituted or substituted C1-20 alkyl group and the like, m represents an integer of 0 to 2, and n represents an integer of 0 to 4), and a fungicide for agricultural and horticultural use that contains at least one of these compounds as an active ingredient thereof, demonstrates reliable effects and can be used safely.Type: ApplicationFiled: August 10, 2009Publication date: June 9, 2011Applicant: Nippon Soda Co., LtdInventors: Akira Mitani, Jun Inagaki, Raito Kuwahara, Masahiro Yokoyama, Kotaro Shibayama, Motoaki Sato
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Publication number: 20110117214Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 15, 2010Publication date: May 19, 2011Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Ronald C. Newbold, Chengzhi Zhang
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Publication number: 20110118231Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: ApplicationFiled: November 19, 2010Publication date: May 19, 2011Applicants: ABBOTT LABORATORIES, ABBOTT GMBH & CO. KGInventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
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Patent number: 7943607Abstract: 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: GrantFiled: May 23, 2006Date of Patent: May 17, 2011Assignee: AstraZeneca ABInventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20110076292Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 27, 2010Publication date: March 31, 2011Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
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Publication number: 20110071097Abstract: The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.Type: ApplicationFiled: March 3, 2009Publication date: March 24, 2011Applicant: Sloan-Kettering Institute for Cancer ResearchInventors: David Gin, Jeremy Wilmot, Hakim Djaballah
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Publication number: 20110021499Abstract: Urethral suppositories containing a mixed-activity anti-cholinergic drug and methods of use for treatment of over-active bladder are provided. Buffering drugs to pH near their pKas can result in a desired proportion of uncharged drug and can enhance absorption of the agents into urethral tissues.Type: ApplicationFiled: July 22, 2009Publication date: January 27, 2011Inventors: Amie Ellen Franklin, Dennis H. Giesing
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Publication number: 20110015176Abstract: The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: ApplicationFiled: July 27, 2010Publication date: January 20, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Aude FAYOL, Alistair LOCHEAD, Mourad SAADY, Julien VACHE, Philippe YAICHE
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Publication number: 20110015177Abstract: The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: ApplicationFiled: July 27, 2010Publication date: January 20, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Aude FAYOL, Alistair LOCHEAD, Mourad SAADY, Julien VACHE, Philippe YAICHE
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Publication number: 20100298287Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: ApplicationFiled: January 21, 2009Publication date: November 25, 2010Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Publication number: 20100298292Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: ApplicationFiled: May 21, 2010Publication date: November 25, 2010Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
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Publication number: 20100286120Abstract: The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action, which is represented by the formula wherein A is —OR1 or —S(O)pR2, R1 and R2 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), or a heterocyclic group to optionally having substituent(s), and p is 0, 1 or 2, or a salt thereof.Type: ApplicationFiled: November 14, 2008Publication date: November 11, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takahiro Matsumoto, Tomokazu Kusumoto
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Publication number: 20100273767Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2 -a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7 -octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2 -a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: ApplicationFiled: April 22, 2010Publication date: October 28, 2010Applicant: ABBOTT LABORATORIESInventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Bhadra Shelat, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
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Patent number: 7795246Abstract: A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into suspended particles, thereby forming a stable suspension that provides greatly improved bioavailability of orally administered fused pyrrolocarbazole compounds.Type: GrantFiled: November 20, 2003Date of Patent: September 14, 2010Assignee: Cephalon, Inc.Inventors: Dave Dickason, Bradley T. McIntyre, Piyush R. Patel
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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: 20100216769Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: June 28, 2006Publication date: August 26, 2010Inventors: Henning Priepke, Georg Dahmann, Kai Gerlach, Roland Pfau, Wolfgang Wienen, Annette Schuler-Metz, Sandra Handschuh, Herbert Nar
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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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Patent number: 7732435Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: GrantFiled: December 5, 2006Date of Patent: June 8, 2010Assignee: Novartis AGInventors: Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Lee Edwards, Terance William Hart, Timothy John Ritchie
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Publication number: 20100055048Abstract: Methods of treating headache with antipsychotics are provided. A kit for treating headache is also provided, comprising an antipsychotic and a device for rapid delivery of the antipsychotic.Type: ApplicationFiled: November 9, 2009Publication date: March 4, 2010Applicant: Alexza Pharmaceuticals, Inc.Inventors: Ron L. Hale, Peter M. LIoyd, Amy T. Lu, Patrik Munzar, Joshua D. Rabinowitz, Roman Skowronski
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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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Patent number: 7659263Abstract: The present invention relates to a thienopyrrole compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound as an active ingredient. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: GrantFiled: November 10, 2005Date of Patent: February 9, 2010Assignee: Japan Tobacco Inc.Inventors: Ryo Mizojiri, Takahiro Oka, Kenta Aoki, Satoru Noji, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yasushi Niwa
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Publication number: 20100022508Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: July 24, 2009Publication date: January 28, 2010Applicant: Gilead Sciences, Inc.Inventors: Evangelos Aktoudianakis, Azim Alan Celebi, Zhimin Du, Salman Y. Jabri, Haolun Jin, Choung U. Kim, Jiayao Li, Samuel E. Metobo, Michael R. Mish, Barton W. Phillips, Joseph H. Saugier, Zheng-Yu Yang, Catalin Sebastian Zonte
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Publication number: 20100016281Abstract: Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.Type: ApplicationFiled: September 11, 2009Publication date: January 21, 2010Inventors: Curt A. Dvorak, Dale A. Rudolph, Brock T. Shireman
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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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Publication number: 20090318412Abstract: The present invention provides a tricyclic heterocyclic compound having a serotonin 5-HT2C receptor activation action and the like. A 5-HT2C receptor activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: July 10, 2007Publication date: December 24, 2009Inventors: Takahiro Matsumoto, Izumi Kamo, Izumi Nomura
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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: 20090215742Abstract: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as HSP-90 inhibitors.Type: ApplicationFiled: April 21, 2006Publication date: August 27, 2009Inventors: Lee Andrew Funk, Mary Catherine Johnson, Pei-Pei Kung, Zhongxiang Zhou
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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: 20090181942Abstract: The present invention relates to tricyclic compounds each represented by the following formula (I): (wherein, R1, R2, R2?, R3, R4, X, Y and Z have the same meanings as defined in the specification); and a drug containing the compound. Since the compounds according to the present invention exhibit an excellent squalene synthetase inhibitory effect and cholesterol synthesis inhibitory effect so that they are useful as a drug such as preventive and/or remedy for diseases in mammals including humans such as hyperlipemia, e.g., hypercholesterolemia, hypertriglyceridemia, and low HDL cholesterolemia and/or arteriosclerosis.Type: ApplicationFiled: October 23, 2006Publication date: July 16, 2009Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kazuyuki Sugita, Masami Otsuka, Hitoshi Oki, Noriyasu Haginoya, Masanori Ichikawa, Masao Itoh