Polycyclo Ring System Having The Additional Five-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/254.08)
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Publication number: 20100249133Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.Type: ApplicationFiled: May 3, 2010Publication date: September 30, 2010Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Patent number: 7803803Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl, or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; and R8 is C1-8-alkyl or C3-8-cycloalkyl.Type: GrantFiled: January 8, 2009Date of Patent: September 28, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20100222363Abstract: New bicyclic derivatives of formula (I); wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.Type: ApplicationFiled: June 28, 2006Publication date: September 2, 2010Applicant: PALAU PHARMA, S.A.Inventors: Carmen Almansa Rosales, Marina Virgili Bernadó
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Publication number: 20100222357Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20100222358Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.Type: ApplicationFiled: March 2, 2010Publication date: September 2, 2010Applicant: ABBOTT LABORATORIESInventors: Marlon D. Cowart, Chen Zhao, Minghua Sun, Lawrence A. Black, Guo Zhu Zheng, Robert J. Gregg, Geoff G.Z. Zhang, Ahmad Y. Sheikh, Xiaochun Lou, Rodger F. Henry, David M. Barnes, Lawrence Kolaczkowski, Anthony R. Haight, Sou-Jen Chang, Steven J. Wittenberger, Michael G. Fickes
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Publication number: 20100216811Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: ApplicationFiled: May 4, 2010Publication date: August 26, 2010Applicant: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Patent number: 7781431Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: GrantFiled: September 7, 2004Date of Patent: August 24, 2010Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpAInventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontoria, Michael Rowley
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Publication number: 20100210635Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: March 23, 2007Publication date: August 19, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Benjamin Jones, Andre A. Kiryanov, Stephen W. Kaldor
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Publication number: 20100179145Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygType: ApplicationFiled: October 12, 2007Publication date: July 15, 2010Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
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Publication number: 20100178294Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.Type: ApplicationFiled: October 1, 2009Publication date: July 15, 2010Inventors: Andrew W. Stamford, Ying Huang, Guoqing Li, Corey O. Strickland, Johannes H. Voigt
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Publication number: 20100160303Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.Type: ApplicationFiled: December 17, 2009Publication date: June 24, 2010Inventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
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Publication number: 20100152184Abstract: The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R1 is hydrogen, hydroxy, or O—Rz; R2a is hydroxy, methoxy or O—Rz; provided that at least one of R1 and R2a is O—Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or Lp is a bond, C?O, (C?O)O, (C?O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C?O or (C?O)O; and provided also that O—Rz does not contain an O—O moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims.Type: ApplicationFiled: October 12, 2007Publication date: June 17, 2010Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Miles Stuart Congreve, Lynsey Helen Fazal, Martyn Frederickson, Christopher William Murray, Michael Alistair O'Brien, Andrew James Woodhead, John Francis Lyons, Neil Thomas Thompson
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Patent number: 7737150Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: GrantFiled: January 8, 2009Date of Patent: June 15, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20100130468Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 20, 2008Publication date: May 27, 2010Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
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Publication number: 20100120769Abstract: The present invention relates to compounds of formula I wherein s, R1a and R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 20, 2010Publication date: May 13, 2010Inventors: Matthias Nettekoven, Jean-Marc ` Plancher, Olivier Roche, Tadakatsu Takahashi, Sven Taylor
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Publication number: 20100113476Abstract: The present disclosure provides drug-ligand conjugates that are potent cytotoxins and include a linker between the drug and ligand where the linker has a single amino acid. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.Type: ApplicationFiled: February 20, 2008Publication date: May 6, 2010Inventors: Liang Chen, Sanjeev Gangwar, Vincent Guerlavais, Nils Lonberg, Qian Zhang
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Patent number: 7700583Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.Type: GrantFiled: October 6, 2005Date of Patent: April 20, 2010Assignee: High Point Pharmaceuticals, LLCInventors: Anette Gundertofte, Anker Steen Jorgensen, Gita Camilla Tejlgaard Kampen, Henrik Sune Andersen, Inge Thoger Christensen, Kilburn Paul John
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Publication number: 20100069355Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.Type: ApplicationFiled: September 17, 2009Publication date: March 18, 2010Inventors: Ling Jong, Faming Jiang, Gaoquan Li, Kristien Mortelmans
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Publication number: 20100063048Abstract: A therapeutic agent for subarachnoid hemorrhage or a drug for improving prognosis of subarachnoid hemorrhage, comprising a compound having a PAR1 inhibitory effect, its pharmaceutically acceptable salt or a hydrate thereofType: ApplicationFiled: June 17, 2009Publication date: March 11, 2010Applicants: Eisai R&D Mangement Co., Ltd., Kyushu University, National University CorporationInventors: Katsuya Hirano, Yoshihisa Maeda, Tomio Sasaki, Hideo Kanaide, Yasutoshi Kai
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Publication number: 20100056520Abstract: The present invention is directed to formulations of inhibitors of phospholipase enzymes, such as cytosolic PLA2, compositions containing the same and processes for manufacture thereof.Type: ApplicationFiled: October 30, 2007Publication date: March 4, 2010Inventors: Frances Anne Donahue, Marc Sadler Tesconi, Mannching Sherry Ku
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Publication number: 20100048553Abstract: Spirocyclic cyclohexane compounds corresponding to formula I in which R1 and R2 form a pyrrolidine ring or an azetidine ring and which exhibit increased metabolic stability, a process for producing such spirocyclic cyclohexane compounds, pharmaceutical compositions containing such spirocyclic cyclohexane compounds, and the use of such spirocyclic cyclohexane compounds to treat or inhibit pain and/or other disorders.Type: ApplicationFiled: August 21, 2009Publication date: February 25, 2010Applicant: Gruenenthal GmbHInventors: Stefan SCHUNK, Derek SAUNDERS, Stephanie HARLFINGER, Sonja STEUFMEHL
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Publication number: 20100048554Abstract: Spirocyclic cyclohexane compounds corresponding to formula I In which R1, R2, R3 and R5 through R10 and X have defined meanings, a process for their preparation, pharmaceutical compositions containing such compounds, and the use of such spirocyclic cyclohexane compounds in the treatment and/or inhibition of pain and other conditions mediated by the ORL-1 or the ?-opioid receptor.Type: ApplicationFiled: August 21, 2009Publication date: February 25, 2010Applicant: Gruenenthal GmbHInventors: Stefan Schunk, Saskia Zemolka, Derek Saunders, Michael Gruss, Heinz Graubaum
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Publication number: 20100041673Abstract: Compounds including 5-(Heterocyclyl)alkyl-N-(arylsulfonyl)indole, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them and a process for the preparation of these compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardiovascular diseases and cancer.Type: ApplicationFiled: July 26, 2007Publication date: February 18, 2010Inventors: Venkata Satya Nirogi Ramakrishna, Rama Sastri Kambhampati, Jagadishbabu Konda, Prabhakar Kothmirkar, Vankaleswaru Jasti
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Publication number: 20100035892Abstract: The present disclosure provides novel compounds of the formula (I): wherein R0, R1, R2, R3, R4, R5, and R6 are as defined in the detailed description. Two preferred compounds of formulae (IX) and (X) are disclosed.Type: ApplicationFiled: August 19, 2009Publication date: February 11, 2010Inventors: Sergey A. Kozmin, Jiayue Cui, Robert Haselkorn, Piotr Gornicki, Olesya Ulanovskaya, Stephen Kron
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Publication number: 20100010009Abstract: The present invention relates to compounds of formula (1), and pharmaceutically acceptable salts thereof, A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof (I), wherein: one of R1 and R2 is H, and the other is selected from F and Cl, or R1 and R2 are both F; R3 is selected from cyclopentyl and cyclohexyl; R4 is an optionally substituted 5- or 6-membered monocyclic or an 8- to 10-membered bicyclic aryl or heteroaryl ring which includes up to four heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: ApplicationFiled: January 8, 2009Publication date: January 14, 2010Inventors: Martin Quibell, John Paul Watts
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Publication number: 20090298808Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: January 6, 2009Publication date: December 3, 2009Inventors: Wenqing Yao, Chunhong He, Jingcong Zhuo
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Publication number: 20090298818Abstract: The invention provides the use of a compound for the manufacture of a medicament for the treatment of pain, wherein the compound is a compound of the formula (VI): or a salt, solvate, tautomer or N-oxide thereof; wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n, R1, R2a, R3, R4a, R8 and R10 are as defined in the claims. The invention also provides the use of a compound of the formula (VI) for the manufacture of a medicament for the prophylaxis or treatment of a fungal, protozoal, viral or parasitic disease state or condition (other than a disease state or condition due to Plasmodium falciparum) or for use in the prophylaxis or treatment of Ewing's sarcoma, atherosclerosis or lupus erythematosus.Type: ApplicationFiled: October 12, 2007Publication date: December 3, 2009Inventors: John Francis Lyons, Neil Thomas Thompson
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Publication number: 20090298849Abstract: Compositions, methods, uses and assemblages for the preferential induction of cell division cycle arrest and/or apoptosis, in a first population of cells compared to a second population of cells employ either: (i) an opioid or opioid-like agent and an NF-?B activating agent, which agents are other than the opioid-like agent trans-U50488 in combination with an NF-?B activating agent selected from etoposide and nocodazole; (ii) a ligand for a sigma receptor, or (iii) an opioid or opioid-like agent wherein the cells of the first population are other than tumour cells.Type: ApplicationFiled: July 6, 2009Publication date: December 3, 2009Inventors: Barbara Ann Spruce, Neil Donald Perkins, Jayne Samson, Niall McTavish
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Patent number: 7612066Abstract: The present invention provides a composition containing a benzamidine derivative that does not decompose even when placed under humidification conditions and a method for stabilizing a benzamidine derivative. According to the present invention, decomposition reaction of a benzamidine derivative can be suppressed by adding to a benzamidine derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, at least one type of electrolyte selected from the group consisting of halide salts of alkaline metal or alkaline earth metal and alkaline metal salts or alkaline earth metal salts of perchloric acid.Type: GrantFiled: March 4, 2005Date of Patent: November 3, 2009Assignee: Eisai R&D Management Co., Ltd.Inventors: Yasuyuki Suzuki, Satoshi Fujioka
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Publication number: 20090270414Abstract: The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.Type: ApplicationFiled: December 22, 2005Publication date: October 29, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Anja Fecher, Heinz Fretz, Markus Riederer
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Publication number: 20090233942Abstract: Markers of the ACE, ATP5C3, BCL2L1, CYP2C9, DRD3, FOS, DTNBP1, GABRG3, GRIA4, LAMA4, MAPK1, NPY1R, OPRD1, OPRM1, PER3, PLCB1, PSMD1, ABI1, LOC402382, and NCALD genes, and their association with response to antidepressants are disclosed. Compositions and methods for detecting and using these markers in a variety of clinical applications are disclosed.Type: ApplicationFiled: March 13, 2008Publication date: September 17, 2009Inventors: Maria Athanasiou, Kerri Holick, Carol Reed, Benjamin Salisbury, Alessandro Serretti, Wei Zou
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Publication number: 20090215772Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbylamino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.Type: ApplicationFiled: April 13, 2006Publication date: August 27, 2009Applicant: Astex Therapeutics LimitedInventors: Gianni Chessari, Miles Stuart Congreve, Eva Figueroa Navarro, Martyn Frederickson, Christopher Murray, Alison Jo-Anne Woolford, Maria Grazia Carr, Michael Alistair O'Brien, Andrew James Woodhead, Robert Downham, Theresa Rachel Phillips
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Publication number: 20090215736Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: ApplicationFiled: September 23, 2008Publication date: August 27, 2009Applicant: Vertex Pharmaceuticals, IncorporatedInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Publication number: 20090203714Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; and R4 is optionally substituted C3-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: ApplicationFiled: January 8, 2009Publication date: August 13, 2009Applicant: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20090192170Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof (I), wherein: R3 is cyclopentyl or cyclohexyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: ApplicationFiled: January 8, 2009Publication date: July 30, 2009Inventors: Martin Quibell, John Paul Watts
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Publication number: 20090191153Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: December 3, 2008Publication date: July 30, 2009Inventors: Ying Sun, Deqiang Niu, Guoyou Xu, Yat Sun Or, Zhe Wang
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Publication number: 20090186906Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is ten-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: ApplicationFiled: January 8, 2009Publication date: July 23, 2009Inventors: Martin Quibell, John Paul Watts
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Publication number: 20090176798Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: ApplicationFiled: December 5, 2008Publication date: July 9, 2009Applicant: Biovitrum ABInventors: Joseph W. Boyd, Giles A. Brown, Michael Higginbottom
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Publication number: 20090170835Abstract: Provided is a novel isoindoline compound of the formula (I): The compound is useful for anesthesia by inducing sedation in a mammal.Type: ApplicationFiled: December 30, 2008Publication date: July 2, 2009Inventors: Kouhei Toyooka, Norimasa Kanamitsu, Masakazu Yoshimura, Haruo Kuriyama, Takashi Tamura
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Publication number: 20090143406Abstract: 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: ApplicationFiled: October 27, 2008Publication date: June 4, 2009Inventors: 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
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Publication number: 20090099180Abstract: The present invention discloses novel compounds of Formula (I): having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: ApplicationFiled: April 25, 2007Publication date: April 16, 2009Inventors: Thomas Edward Mabry, Owen Brendan Wallace, Yanping Xu, Nancy June Snyder, Leonard Larry Winneroski, JR.
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Publication number: 20090082346Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.Type: ApplicationFiled: July 29, 2008Publication date: March 26, 2009Applicant: Pfizer Italia S.r.l.Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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Publication number: 20090069343Abstract: Patients suffering from pruritus or itch may be effectively treated by administering a centrally acting histamine H1 receptor antagonist (e.g., diphenhydramine, triprolidine, hydroxyzine, pyrilamine, promethazine, or chlorpheniramine) and a histamine H4 receptor antagonist (e.g., 5-chloro-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanone).Type: ApplicationFiled: April 9, 2007Publication date: March 12, 2009Inventors: Paul J. Dunford, Lars Karlsson, Robin L. Thurmond
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Publication number: 20090036444Abstract: The present invention relates to a fused ring 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. 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: ApplicationFiled: May 18, 2006Publication date: February 5, 2009Applicant: Japan Tobacco Inc.Inventors: Ryo Mizojiri, Shintaro Hirashima, Takahiro Oka, Kenta Aoki, Satoru Noji, Izuru Ando, Toshihiro Sato, Yasushi Niwa
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Publication number: 20090030014Abstract: The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the generic formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.Type: ApplicationFiled: July 20, 2006Publication date: January 29, 2009Inventors: Akira Kugimiya, Michitaka Shichijo, Yoshiharu Hiramatsu, Natsuki Ishizuka
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Patent number: 7459557Abstract: The present invention relates to substituted isoindole-1,3-dione compounds of Formula (I) and pharmaceutically acceptable forms thereof, as ?1a/?1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as methods of treatment.Type: GrantFiled: June 12, 2006Date of Patent: December 2, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: George Chiu, Peter J. Connolly, Jessica J. Liu, Steven A. Middleton, Virginia L. Pulito, Shengjian Li
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Publication number: 20080293699Abstract: Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death.Type: ApplicationFiled: May 23, 2008Publication date: November 27, 2008Applicant: BURNHAM INSTITUTE FOR MEDICAL RESEARCHInventors: John C. Reed, In-Ki Kim
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Patent number: 7456183Abstract: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C?O, C?S, S?O, SO2, S, O, (CR6R7)n, C(?O)—(CR6R7)n, and C(?S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S?O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.Type: GrantFiled: April 8, 2002Date of Patent: November 25, 2008Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Daniel Chu, Rustum Boyce, David Duhl, Bryan Chang
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Publication number: 20080279821Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 24, 2008Publication date: November 13, 2008Inventors: Deqiang Niu, Yat Sun Or, Zhe Wang
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Publication number: 20080261978Abstract: The invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula (I).Type: ApplicationFiled: March 7, 2008Publication date: October 23, 2008Inventors: Michael P. Clark, Mark A. Lockwood, Florence F. Wagner, Michael G. Natchus