The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/373)
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Publication number: 20100092496Abstract: The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.Type: ApplicationFiled: November 2, 2009Publication date: April 15, 2010Applicant: Medarex, Inc.Inventors: Sharon E. Boyd, Liang Chen, Sanjeev Gangwar, Vincent Guerlavais, Killian Horgan, Zhi-Hong Li, Bilal Sufi
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Patent number: 7696198Abstract: Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein.Type: GrantFiled: April 16, 2004Date of Patent: April 13, 2010Assignee: Memory Pharmaceuticals CorporationInventors: Ashok Tehim, Allen Hopper, Ruiping Liu, Erik Kuester, Robert F. Dunn, Thomas E. Renau
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Patent number: 7696229Abstract: The present disclosure provides compounds having affinity for the 5HT6 receptor which are of the formula (I): wherein R1-R3 A, B, D, E, G, Q, and x are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: GrantFiled: February 16, 2007Date of Patent: April 13, 2010Assignee: Memory Pharmaceuticals CorporationInventors: Robert Dunn, Truc Minh Nguyen, Wenge Xie, Ashok Tehim
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Publication number: 20100087446Abstract: 2-Substituted indole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: April 22, 2008Publication date: April 8, 2010Inventors: Prasun K. Chakravarty, Joseph L. Duffy, Min K. Park, Sriram Tyagarajan, Bishan Zhou
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Patent number: 7692005Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: July 12, 2006Date of Patent: April 6, 2010Assignee: Allergan, Inc.Inventors: Julie A. Wurster, Edward H. Wang, Richard C. Yee
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Publication number: 20100075949Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.Type: ApplicationFiled: September 15, 2009Publication date: March 25, 2010Inventors: Christoph BURDACK, Cedric KALINSKI, Vladimir KHAZAK, Gunther ROSS, Lutz WEBER
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Patent number: 7678800Abstract: The present invention relates to 2-(1H-indolylsulfanyl)-aryl amine derivatives of the general formula I as the free base or salts thereof and their use for the treatment of affective disorders, pain, attention deficit hyperactivity disorder (ADHD) and stress urinary incontinence.Type: GrantFiled: July 13, 2005Date of Patent: March 16, 2010Assignee: H. Lundbeck A/SInventors: Jan Kehler, Friedrich Kroll, Karsten Juhl
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Publication number: 20100061982Abstract: The invention relates to 3-substituted-1H-indole, 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula 1: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.Type: ApplicationFiled: September 10, 2009Publication date: March 11, 2010Applicant: WyethInventors: Semiramis Ayral-Kaloustian, Tarek Suhayl Mansour, Hwei-Ru Tsou, Nan Zhang, Aranapakam Mudumbai Venkatesan, Li Di, Edward Harvel Kerns
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Publication number: 20100056544Abstract: The potassium, sodium, ammonium, lysine, diethylamine, tromethamine (TRIS), piperazine, ethylenediamine and ethanolamine salt of a compound of general formula (I): wherein R1 is halo or cyano; R2 is C1-C4 alkyl; and R3 is quinolyl or phenyl substituted with methane sulfonyl; can be synthesised by a novel method and are substantially more soluble than the parent free acids in a range of solvents.Type: ApplicationFiled: March 22, 2007Publication date: March 4, 2010Applicant: Oxagen LimitedInventor: James Matthew Lovell
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Patent number: 7667037Abstract: Provided are processes for preparing ziprasidone from CEI and BIPT.Type: GrantFiled: October 25, 2004Date of Patent: February 23, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Gideon Pilarsky, Natalia Shenkar, Marioara Mendelovici, Tamar Nidam, Anna Balanov
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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: 20100041669Abstract: Compounds including 4-(Heterocyclyl)alkyl-N-(arylsulfonyl)indole compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them as well as 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, Dinkar Amol Deshpande, Venkateswarlu Jasti
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Publication number: 20100041635Abstract: The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation.Type: ApplicationFiled: June 30, 2009Publication date: February 18, 2010Inventors: Mustapha HADDACH, Johnny Yasuo NAGASAWA
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Patent number: 7662824Abstract: The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: GrantFiled: March 16, 2006Date of Patent: February 16, 2010Assignee: Janssen Pharmaceutica NVInventors: Kristi Leonard, Tianbao Lu, Robert W. Tuman, Dana L. Johnson, Anna C. Maroney, Jan L. Sechler, Richard W. Connors, Richard S. Alexander, Maxwell D. Cummings, Robert A. Galemmo, Thomas P. Markotan
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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: 20100029646Abstract: The present application discloses prodrugs of substituted 3,3-diphenyl-1,3-dihydro-indol-2-one compounds having the general formula (I). The 4-position of the phenyl moieties and the N-position of the indole represent useful handles for the introduction of particular prodrug groups, in particular those comprising an amino acid moiety. The prodrug compounds are believed to be useful for the treatment of cancer in a mammal, possibly in combination with one or more other chemotherapeutic agents.Type: ApplicationFiled: December 11, 2007Publication date: February 4, 2010Applicant: Topo Target A/SInventors: Mette Knak Christensen, Fredrik Bjoerkling, Martins Ikaunieks, Andrei Zaichenko, Vija Gailite, Einars Loza, Ivars Kalvinsh, Marina Madre
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Publication number: 20100029645Abstract: This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLA2?). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.Type: ApplicationFiled: June 19, 2009Publication date: February 4, 2010Inventors: John C. McKew, Katherine L. Lee, Lihren Chen, Richard Vargas, James D. Clark, Cara Williams, Valerie Clerin, Suzana Marusic, Kevin Pong
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Publication number: 20100016332Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbomyl-benzofuran-5-yl)-piperazine, crystaline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbomyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.Type: ApplicationFiled: September 25, 2009Publication date: January 21, 2010Inventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Publication number: 20100016312Abstract: This application discloses compounds of generic Formula I: or pharmaceutically acceptable salts thereof, wherein A, R1, R2, R3, R4, Q, X, Y, m, p, and q are defined as described herein, useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: July 15, 2009Publication date: January 21, 2010Inventors: Eun Kyung Lee, Ryan Craig Schoenfeld, Robert James Weikert
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Publication number: 20100009986Abstract: The invention relates to substituted heteroaryl derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted heteroaryl derivatives for producing medicaments.Type: ApplicationFiled: July 17, 2007Publication date: January 14, 2010Applicant: GRUNENTHAL GmbHInventors: Saskia Zemolka, Stefan Schunk, Werner Englberger, Babette-Yvonne Kögel, Klaus Link, Hans Schick, Helmut Sonnenschein, Heinz Graubaum, Claudia Hinze
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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: 20090318471Abstract: The present invention relates to new salts and crystalline salt forms of an indolinone derivative which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.Type: ApplicationFiled: June 6, 2007Publication date: December 24, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter Sieger, Werner Rall, Guenter Linz, Mihaela Pop, Jaroslaw Mazurek
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Publication number: 20090311217Abstract: The invention relates to 3-substituted-1H-indole compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.Type: ApplicationFiled: May 28, 2009Publication date: December 17, 2009Applicant: WyethInventors: Matthew Gregory Bursavich, Nan Zhang, Semiramis Ayral-Kaloustian, James Thomas Anderson, Thai Hiep Nguyen, Sabrina Lombardi, David Malwitz, Natasja Brooijmans, Derek Cecil Cole, Adam Matthew Gilbert, Pawel Wojciech Nowak, Kaapjoo Park, Sasmita Das, Hwei-Ru Tsou, Aranapakam Mudumbai Venkatesan, Mercy Adufa Otteng, Gary Harold Birnberg, Gloria Jean MacEwan
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Publication number: 20090312344Abstract: The present invention relates to ?1, and/or ?1d adrenergic receptor antagonists, which can function as ?1a and/or ?1d adrenergic receptor antagonist and can be used for the treatment of a disease or disorder mediated through ?1a and/or an adrenergic receptor. Compounds disclosed herein can be used for the treatment of benign prostatic hyperplasia (BPH) and the related symptoms thereof. Further, compounds disclosed herein can be used for the treatment of lower urinary tract symptoms associated with or without BPH. Also provided are processes for preparing such compounds, pharmaceutical compositions thereof, and the methods of treating BPH or related symptoms thereof.Type: ApplicationFiled: May 31, 2005Publication date: December 17, 2009Inventors: Mohammad Salman, Somesh Sharma, Gyan Chand Yadav, Gobind Singh Kapkoti, Anurag Mishra, Praful Gupta, Nitya Anand, Anita Chugh, Kamna Nanda
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Patent number: 7629343Abstract: This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: wherein: Cy is independently a cyclyl group; Q1 is independently a covalent bond or cyclyl leader group; the piperazin-1,4-diyl group is optionally substituted; J1 is independently a covalent bond or —C(?; O)—; J2 is independently —C(?O)— or —S(?O)2—; Q2 is independently an acid leader group; wherein: Cy is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is independently: a covalent bond; C1-7alkylene; or C1-7alkylene-X—C1-7alkylene, —X—C1-7alkylene, or C1-7alkylene-X—, wherein X is —O— or —S—; and is optionally substituted; Q2 is independently: C4-8alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or: Q2 is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or, C1-7alkylene-C5-20arylene-C1-7alkylene; and is optionally substituted; and has a backbone leType: GrantFiled: April 3, 2003Date of Patent: December 8, 2009Assignee: Topotarget UK LimitedInventors: Clare J. Watkins, Maria-Rosario Romero-Martin, James Ritchie, Paul W Finn, Ivars Kalvinsh, Einars Loza, Klara Dikovska, Igor Starchenkov, Daina Lolya, Vija Gailite
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Patent number: 7625889Abstract: The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.Type: GrantFiled: July 25, 2007Date of Patent: December 1, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: Paul Robert Eastwood, Hazel Hunt, David Mark Fink, Helen Katherine Smith, Richard Simon Todd
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Publication number: 20090291963Abstract: Substituted indoles of the formula (I) and physiologically acceptable derivatives and salts thereof, in which R1, D, E, R12, p, X1, E, G, X2 and Z are as defined in claim 1, exhibit particular actions on the central nervous system, especially 5HT reuptake-inhibiting and 5 HTx-agonistic and/or -antagonistic actions and in particular serotonin-agonistic and -antagonistic properties and can be employed as antipsychotics, neuroleptics, antidepressants, anxiolytics and/or antihypertonics.Type: ApplicationFiled: July 29, 2009Publication date: November 26, 2009Inventors: Oliver SCHADT, Henning Böttcher, Joachim Leibrock, Kai Schiemann, Timo Heinrich, Günter Hölzemann, Christoph van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
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Publication number: 20090264417Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: ApplicationFiled: September 4, 2008Publication date: October 22, 2009Applicant: KALYPSYS, INC.Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steven P. Govek
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Publication number: 20090264418Abstract: The present invention relates to compounds of formula I wherein G and R1 to R5 and R12 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: June 29, 2009Publication date: October 22, 2009Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Patent number: 7605156Abstract: This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.Type: GrantFiled: May 27, 2005Date of Patent: October 20, 2009Assignee: WyethInventors: John C. McKew, Steve Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark L. Behnke, Baihua Hu, James D. Clark, Wei Li, Valerie Clerin, Suzana Marusic, Kevin Pong
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Patent number: 7601711Abstract: The present invention relates to compounds of formula I wherein G and R1 to R5 and R12 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: GrantFiled: April 5, 2007Date of Patent: October 13, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Publication number: 20090253713Abstract: Compounds of the general formula: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, and X are as defined. Further provided are methods for treatment of sexual dysfunction, including erectile dysfunction and female sexual dysfunction, and combination drugs and method of use thereof, including a compound of the invention and one or more second sexual dysfunction pharmaceutical agents.Type: ApplicationFiled: June 19, 2009Publication date: October 8, 2009Applicant: Palatin Technologies, Inc.Inventor: Shubh D. Sharma
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Publication number: 20090247547Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, Y, Z, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: ApplicationFiled: March 26, 2009Publication date: October 1, 2009Inventors: Michael SHULTZ, Christine Hiu-Tung Chen, Young Shin Cho, Lei Jiang, Jianmei Fan, Gang Liu, Dyuti Majumdar
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Publication number: 20090227538Abstract: The invention relates to compounds of the general formula (I) wherein R1, R2, R3, R4, R5, R6, A, X, m and n have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals and plants.Type: ApplicationFiled: November 2, 2006Publication date: September 10, 2009Inventors: Jörg Früchtel, Noëlle Gauvry, Sandra Schorderet Weber, Jacques Bouvier
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Publication number: 20090221605Abstract: A compound of formula I wherein R, Ra and Rb are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.Type: ApplicationFiled: May 12, 2005Publication date: September 3, 2009Inventors: Maurice Van Eis, Jürgen Wagner, Peter Von Matt
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Publication number: 20090221606Abstract: The present invention relates to novel crystalline forms of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl)piperazin-1-yl]methanone phosphate and to pharmaceutical compositions containing said forms.Type: ApplicationFiled: April 24, 2007Publication date: September 3, 2009Inventors: Susan Marie Reutzel-Eden, Gregory Alan Stephenson
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Patent number: 7582635Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.Type: GrantFiled: December 19, 2003Date of Patent: September 1, 2009Inventors: Qun Sun, Laykea Tafesse, Sam Victory
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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: 20090209553Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: February 12, 2009Publication date: August 20, 2009Inventors: David Scott Carter, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
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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: 20090197817Abstract: 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: ApplicationFiled: January 8, 2009Publication date: August 6, 2009Inventors: Martin Quibell, John Paul Watts
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Publication number: 20090192322Abstract: The present invention relates to a process for preparing a compound of formula (Ia), (Ib), (Ic) or (Id), or a pharmaceutically acceptable salt, hydrate, solvate, complex or prodrug thereof, said process comprising the steps of: (A) (i) treating a compound of formula (IVa), where R48 is alkyl or tosyl, with an oxidising agent to form a compound of formula (Va); and (ii) converting said compound of formula (Va) to a compound of formula (Ia) or (Ic); or (B) (i) treating a compound of formula (IVb), where R48 is alkyl or tosyl, with an oxidising agent to form a compound of formula (Vb); and (ii) converting said compound of formula (Vb) to a compound of formula (Ib) or (Id).Type: ApplicationFiled: January 8, 2009Publication date: July 30, 2009Applicant: Amura Therapeutics LimitedInventors: Martin Quibell, James Nally, Lee Patient, Yikang Wang, Claudio Dagostin, 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: 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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Patent number: 7560481Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.Type: GrantFiled: December 21, 2005Date of Patent: July 14, 2009Assignee: Abbott LaboratoriesInventors: Jennifer M. Frost, Karin R. Tietje, Michael J. Dart, Michael D. Meyer
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Patent number: 7560483Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.Type: GrantFiled: June 21, 2005Date of Patent: July 14, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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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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Patent number: 7557108Abstract: The present invention relates to compounds of formula I wherein one of R1 and R2 is hydrogen and the other one is and wherein A and R1 to R4 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: GrantFiled: January 23, 2008Date of Patent: July 7, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Olivier Roche
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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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Patent number: 7550469Abstract: The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: GrantFiled: December 21, 2006Date of Patent: June 23, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: James A Hendrix, Joseph T Strupczewski, Kenneth Bordeau, Matthias Urmann, Gregory Shutske, Horst Hemmerle, John G Jurcak, Harpal Gill, Franz J Weiberth, Thaddeus Nieduzak, Sharon Anne Jackson, Xu-Yang Zhao, Paul Justin Mueller