Plural Ring Nitrogens In The Tricyclo Ring System Patents (Class 514/292)
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Publication number: 20100035912Abstract: Chemical compounds that disrupt retroviral assembly and maturation are presented herein. More particularly, this disclosure provides small molecule compounds that disrupt the formation and maturation of virus particles and methods of using such small molecules to treat HIV-1 infection.Type: ApplicationFiled: August 6, 2009Publication date: February 11, 2010Inventors: Asim Kumar Debnath, Hongtao Zhang, Francesca Curreli
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Patent number: 7659270Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: August 8, 2007Date of Patent: February 9, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Publication number: 20100029706Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, and diseases of aging such as diabetes and cancer with hydrogenated pyrido[4,3-b]indoles such as dimebolin, are disclosed.Type: ApplicationFiled: July 29, 2009Publication date: February 4, 2010Applicant: Edison Parmaceuticals, Inc. a Delaware CorporationInventors: Guy M. Miller, Kieron E. Wesson
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Publication number: 20100029634Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, tautomers, stereoisomers, and/or esters thereof.Type: ApplicationFiled: March 30, 2009Publication date: February 4, 2010Inventors: Michael P. Clark, Florence F. Wagner, Brandon C. Doroh, Tricia L. Johnson, Yesim Altas Tahirovic, Lawrence Wilson, John M. Wiseman, Jason W. Skudlarek, Mark A. Lockwood, Michael G. Natchus
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Publication number: 20100029580Abstract: The present invention relates to the constitutive activity of the Hedgehog pathway in non-small cell lung carcinoma (NSCLC). A method for diagnosing NSCLC by detecting the level of a component of the Hedgehog pathway is provided, as is a method for identifying subjects that will respond positively to treatment with a Hedgehog pathway antagonist. Methods for treating subjects with cancer or cancers resistant to Hedgehog pathway antagonists are also provided.Type: ApplicationFiled: April 12, 2006Publication date: February 4, 2010Inventors: David J. Robbins, Ziqiang Yuan, John A. Goetz
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Publication number: 20100029635Abstract: This invention concerns the compounds the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R2 is hydrogen, aryl substituted with a radical —COOR4; or R2 is substituted C1-10alkyl, C2-10alkenyl or C3-7cycloalkyl; or R2 is a radical of formula: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b(b-5) -a1=a2-a3=a4- is —CH?CH—CH?CH—; —N?CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N— (c-5); wherein one of the hydrogen atoms in (c-1)-(c-5) is replaced by particular radicals; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, substituted carbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1.Type: ApplicationFiled: October 9, 2009Publication date: February 4, 2010Inventors: Bart Rudolf Romanie Kesteleyn, Sandrine Marie Helene Vendeville, Natalie Maria Francisca Kindermans, Dominique Louis Nestor Ghislai Surleraux, Pierre Jean-Marie Bernard Raboisson, Piet Tom Bert Paul Wigerinck, Annick Ann Peeters
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Publication number: 20100022506Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: October 5, 2009Publication date: January 28, 2010Inventors: Donald J.P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith
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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: 20100022580Abstract: This disclosure relates to new tricyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds are described, including new 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole compounds. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: January 26, 2009Publication date: January 28, 2010Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
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Patent number: 7652031Abstract: Compounds which mimic the chemical and/or biological activity of discodermolide are provided.Type: GrantFiled: August 6, 2002Date of Patent: January 26, 2010Assignee: The Trustees Of The University of PennsylvaniaInventors: Amos B Smith, III, Thomas Beauchamp, Matthew J. Lamarche, Paul V. Rucker
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Publication number: 20100004230Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: July 3, 2007Publication date: January 7, 2010Applicant: GLAXO GROUP LIMITEDInventors: Gerald Brooks, Timothy James Miles, Neil David Pearson
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Patent number: 7638640Abstract: Compositions of purified and biologically active ellagitannins are provided by separation from pomegranate husk using a method of extraction and purification using a solid polymeric adsorbent and the uses of the said compounds.Type: GrantFiled: March 30, 2006Date of Patent: December 29, 2009Assignee: The Regents of the University of CaliforniaInventors: Navindra P. Seeram, David Heber
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Publication number: 20090318491Abstract: The present invention relates to compounds which are derivatives of cytisine or acetylcholine which exhibit activity as agonists, partial agonists or antagonists of nicotinic acetylcholine receptors and may be used in modulating these receptors and in treating mood disorders in patients in need of therapy.Type: ApplicationFiled: January 26, 2007Publication date: December 24, 2009Applicants: Yale Univeristy, Reheinische Friedrich-Wilhelms- Univeristy BonnInventors: Marina Picciotto, Daniela Gundisch, Lenka Munoz, Matthias Andra, Yann Mineur
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Publication number: 20090312288Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: April 16, 2009Publication date: December 17, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Jason W. Brown, Qing Dong, Anthony R. Gangloff, Bheema R. Paraselli, Nicholas Scorah, Jeffrey A. Stafford, Sanjib Das, Jonathon S. Salsbury
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Publication number: 20090306054Abstract: Tricyclic compounds of formulae I-III, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.Type: ApplicationFiled: May 16, 2007Publication date: December 10, 2009Applicant: Gilead Sciences ,Inc.Inventors: Zhenhong R. Cai, Salman Y. Jabri, Haolun Jin, Rachel A. Lansdown, Samuel E. Metobo, Michael R. Mish, Richard M. Pastor
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Publication number: 20090306055Abstract: The present invention is directed to compounds represented by the formula (1): B-D-Z (1), wherein B represent the following formula (B-1), A represents an optionally substituted imidazole or pyrazole group; E represents the following formula (1a): X represents an oxygen atom, the formula: SOu, or the formula: N—R9; Y represents a carbon atom or a nitrogen atom; D represents an oxygen atom, a sulfur atom or the formula (1a); Z represents (a chroman-2-yl group, a chroman-4-yl group, a 2,3-dihydrobenzofuran-2-yl group, a 2,3-dihydrobenzofuran-3-yl group, etc.) which is substituted with NHR10 or OR11)] or pharmaceutically acceptable salts thereof, and to antioxidants, therapeutic agents for kidney diseases or cerebrovascular disorder, and retinal oxidative damage inhibitors, which include the compounds as the active ingredient.Type: ApplicationFiled: May 15, 2009Publication date: December 10, 2009Applicant: NIPPON SODA CO., LTD.Inventors: Nobuhiro Umeda, Nobuo Mochizuki, Seiichi Uchida, Mitsumasa Takada, Seiichi Ikeyama, Shiro Tsubokura, Yasuyuki Shiinoki, Fumie Shirato, Hiroko Moroe
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Patent number: 7626025Abstract: A novel ?-carboline guanidine derivative tiruchenduramine (1) and its derivatives are disclosed. These compounds have been isolated from the Indian ascidian Synoicum macroglossum. These compounds are useful in the treatment of diabetic disorder by providing inhibition of ? (alpha)glucosidase.Type: GrantFiled: March 30, 2004Date of Patent: December 1, 2009Assignees: Council of Scientific and Industrial Research, Department of Ocean DevelopmentInventors: Yenamandra Venkateswarlu, Kodela Ravinder, Jhillu S. Yadav, Yandrapu Sarathkumar, Sistla Ramakrishna, Prakash V. Diwan, Janapala V. Rao, Ratnam Ramesh, Hartmut Laatsch
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Patent number: 7626026Abstract: Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 and optionally also R3 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumors. The prodrug is expected to be activated preferentially in tumor cells, where it will act as a DNA alkylating agent preventing cell division.Type: GrantFiled: February 22, 2002Date of Patent: December 1, 2009Assignee: University of BradfordInventors: Mark Searcey, Laurence Hylton Patterson
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Publication number: 20090291921Abstract: Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.Type: ApplicationFiled: November 19, 2008Publication date: November 26, 2009Applicant: Gilead Sciences, Inc.Inventors: Salman Y. Jabri, Haolun Jin, Choung U. Kim, Jiayao Li, Samuel E. Metobo, Michael R. Mish
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Publication number: 20090291941Abstract: The present invention relates to pyrido[3,2-c]benzazocinone derivatives and related compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: October 18, 2006Publication date: November 26, 2009Inventors: Christopher J. Dinsmore, Jongwon Lim, Alan B. Northrup
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Publication number: 20090291976Abstract: A method of inhibiting excitotoxicity by indirectly activating ?4?2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed. Inhibitors of ?7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate ?4?2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis.Type: ApplicationFiled: June 26, 2007Publication date: November 26, 2009Inventors: Peter Andrew Ferchmin, Vesna Ana Eterovic, Hector Manuel Maldonado
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Patent number: 7618980Abstract: The present application provides pyrrolo(oxo)isoquinolines as modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.Type: GrantFiled: July 13, 2005Date of Patent: November 17, 2009Assignee: Bristol-Myers Squibb CompanyInventors: John M. Fevig, Jianxin Feng, Saleem Ahmad
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Publication number: 20090275554Abstract: The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.Type: ApplicationFiled: December 12, 2005Publication date: November 5, 2009Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu Habashita, Haruto Kurata, Shinji Nakade
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Publication number: 20090275590Abstract: Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5; is H, optionally substituted alkyl, optionally substituted heterocycle, —C(?O)—R6, —C(?O)—O—R7, or —C(?O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH?CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.Type: ApplicationFiled: January 9, 2009Publication date: November 5, 2009Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter Robert GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG, Mark Hadden, James Grabowski, Alexander Usyatinsky
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Publication number: 20090275568Abstract: The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.Type: ApplicationFiled: July 7, 2009Publication date: November 5, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Nicholas William Hird, Naoki Tarui, Hiroshi Banno, Yasuhiko Kawano, Nobuhiro Inatomi
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Patent number: 7612083Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and urea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.Type: GrantFiled: May 19, 2005Date of Patent: November 3, 2009Assignee: Coley Pharmaceutical Group, Inc.Inventor: George W. Griesgraber
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Publication number: 20090270442Abstract: Polymorphic forms of the hydrochloride salt of 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide (referred to herein as Compound 1) which has the formula: and compositions thereof, wherein the Compound 1 is present in one or more polymorphic forms. Also provided are novel methods for the preparation of the polymorphs of Compound 1, and kits and articles of manufacture of the compositions, and methods of using the compositions to treat various diseases.Type: ApplicationFiled: April 13, 2009Publication date: October 29, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Lauren Graham, Paul Isbester, Olga V. Lapina, Bingidimi I. Mobele, Grant J. Palmer, Karl Reineke, Jonathon S. Salsbury, Luckner Ulysse
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Patent number: 7608643Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: The present invention provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.Type: GrantFiled: March 7, 2006Date of Patent: October 27, 2009Assignee: Schering CorporationInventors: Ronald J. Doll, Ronald Herbst, Wolfgang Seghezzi, Emma M. Lees, William F. Estacio
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Patent number: 7608625Abstract: The present invention provides a preventive or therapeutic agent for bruxism or bruxism-related diseases that contains as an active ingredient at least one selected from the group consisting of proton pump inhibitors, histamine H2 receptor antagonists, and acid pump antagonists. Examples of the proton pump inhibitors include rabeprazole, omeprazole, esomeprazole, lansoprazole, pantoprazole, or tenatoprazole, or salts thereof, or hydrates thereof.Type: GrantFiled: January 30, 2004Date of Patent: October 27, 2009Assignee: Eisai R & D Management Co., Ltd.Inventors: Shouichi Miyawaki, Teruko Yamamoto
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Publication number: 20090264457Abstract: The present invention relates to a Combination of at least two 5HT6-Ligands of which one is a partial or agonist while the other is a full antagonist or an inverse agonist, a medicament comprising this comination, the use of the combiantion in the manufacture of a medicament for the treatment of memory disorders ADHD, and methods of treatment using the combination or its members.Type: ApplicationFiled: August 1, 2008Publication date: October 22, 2009Inventors: Xavier Codony-Soler, Jose-Miguel Vela-Hernandez, Helmut H. Buschmann
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Publication number: 20090258893Abstract: The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.Type: ApplicationFiled: June 2, 2009Publication date: October 15, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Nicholas William Hird, Naoki Tarui, Hiroshi Banno, Yasuhiko Kawano, Nobuhiro Inatomi
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Publication number: 20090258892Abstract: The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like.Type: ApplicationFiled: April 30, 2009Publication date: October 15, 2009Applicant: ARENA PHARMACEUTICALS, INC.Inventors: P. Douglas Boatman, Thomas O. Schrader, Graeme Semple, Philip J. Skinner, Jae-Kyu Jung
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Patent number: 7601734Abstract: An object of the present invention is to provide a cyclic amine compound which has a potent inhibitory effect on the binding of ?2C-adrenoceptor and is useful in preventing and treating disorders attributable to ?2C-adrenoceptor. The above-described object is solved by the following cyclic amine compound, etc., wherein X is O, S, SO, SO2 or NR2, etc.; R1 is a hydrogen atom, a cyano group, a carboxyl group, a C2-C13 alkoxycarbonyl group, a carbamoyl group, etc.; Ar1 and Ar2 are the same or different and each represent an aryl or heteroaryl group which may be substituted by 1 to 3 substituents and so on; ring B is a benzene ring may be substituted by 1 to 3 substituents and so on; n is an integer from 1 to 10; and p and q are the same or different and each represent an integer of 1 or 2.Type: GrantFiled: April 8, 2005Date of Patent: October 13, 2009Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Toshihito Kumagai, Toshio Nakamura, Yuri Amada, Yoshinori Sekiguchi
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Patent number: 7601840Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and/or in the treatment of cancer, diabetic retinopathy or exudative macular degeneration are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the inhibition of angiogenesis, and/or the treatment of cancer, diabetic retinopathy or exudative macular degeneration using the compounds of the invention.Type: GrantFiled: March 15, 2005Date of Patent: October 13, 2009Assignee: PTC Therapeutics, Inc.Inventors: Young-Choon Moon, Liangxian Cao, Nadarajan Tamilarasu, Hongyan Qi, Soongyu Choi, William Joseph Lennox, Donald Thomas Corson, Seongwoo Hwang
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Publication number: 20090247537Abstract: Methods for preventing or treating bruxism, including alleviating or eliminating one or more symptoms, diseases or conditions associated with or resulting from bruxism, using dopaminergic agents such as monoamine oxidase inhibitors that increase dopaminergic activity and dopamine agonists, are disclosed.Type: ApplicationFiled: November 4, 2008Publication date: October 1, 2009Inventor: William Dale Overfield
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Publication number: 20090238761Abstract: This invention provides novel aryl piperazine derivatives having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, D2-like and 5-HT2 receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders incl. schizophrenia.Type: ApplicationFiled: January 2, 2006Publication date: September 24, 2009Applicant: Universita Degli Studi Di SienaInventors: Giuseppe Campiani, Stefania Butini, Caterina Fattorusso, Francesco Trotta, Silvia Franceschini, Meri De Angelis, Karin Sandager Nielsen
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Publication number: 20090239854Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: October 27, 2008Publication date: September 24, 2009Inventors: David T. HUNG, Andrew A. PROTTER, Rajendra P. JAIN, Sundeep DUGAR, Sarvajit CHAKRAVARTY, Sergey O. BACHURIN, Anatoly K. USTINOV, Bogdan K. BEZNOSKO, Elena F. SHEVTSOVA, Vladimir V. GRIGORIEV, Nadezhda Sergeevna Beznosko
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Patent number: 7592454Abstract: The present application provides novel compounds according to Formula (I): including all stereoisomers, solvates, prodrug esters and pharmaceutically acceptable salt forms thereof, wherein R1, R4a, R5, R6, R7, R8, R9, m, and X are described herein. Additionally, the present application provides novel pharmaceutical compositions comprising at least one compound according to Formula (I). Further, the present application provides methods of treating a patient in need comprising administering a therapeutically effective amount of at least one compound according to Formula (I).Type: GrantFiled: April 13, 2005Date of Patent: September 22, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Taekyu Lee, Wei Deng, Albert J. Robichaud
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Harmine derivatives, intermediates used in their preparations, preparation processes and use therefo
Publication number: 20090227619Abstract: This invention relates to compounds of general formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the specification; intermediates used in their preparation, preparation processes and use thereof. The present invention produces new harmine derivatives with enhanced antitumour activity and lower nervous system toxicity by structurally modification of the parent structure of ?-carboline of harmines at position 1, 2, 3, 7 and 9. The compounds of the present invention can be prepared easily with high yield. They can be used in manufacture of a variety of antitumour medicines and medicines used in treatment of tumour diseases in combination of light or radiation therapy.Type: ApplicationFiled: June 2, 2004Publication date: September 10, 2009Inventors: Jialin Wu, Qi Chen, Rihui Cao, Fusheng Yu, Zihou Wang, Wenlie Peng -
Publication number: 20090227571Abstract: Provided herein are compounds that bind to androgen receptors and modulate the activity and/or the amount of androgen receptors and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: ApplicationFiled: June 30, 2006Publication date: September 10, 2009Inventors: Jon C. Loren, Todd Miller, Bijan Pedram, Charlene V. Rowley, Yixing Shen, Cornelis Arjan Van Oeveren, Lin Zhi
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Publication number: 20090221627Abstract: Some exemplary embodiments comprise fluoro-containing derivatives of pyrido[4,3-b]indoles (and exemplary methods of making the same) that may be administered to a mammal (including a human) in an effective amount for potential use in the treatment or prophylaxis of neurological disorders including AD, mild cognitive impairment, senile and vascular dementia, HD, ALS, Parkinson's disease, AIDS-related dementia, ischaemic cerebral pathologies, neuropathic pain, ADHD (attention deficit disorder/hyperactivity syndrome), eating disorders such as anorexia and bulimia, panic attacks, withdrawal from drug abuse such as cocaine, ethanol, nicotine and benzodiazepines, schizophrenia (in particular the cognitive deficit of schizophrenia), stroke and also disorders associated with spinal trauma and/or head injury. These derivatives may also be useful for the treatment of borderline personality disorder, obesity, and for use as geroprotectors.Type: ApplicationFiled: September 19, 2008Publication date: September 3, 2009Inventors: Alexey Aksinenko, Sergey Bachurin, Sergey Sablin, Bogdan Beznosko, Vladimir Sokolov, Nadezhcla Besnosko, Julia Beznosko
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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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Patent number: 7572805Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions, comprising at least one compound according to Formula I and optionally at least one additional therapeutic agent and methods of treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impaired glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using compounds according to Formula I or pharmaceutically acceptable salt forms thereof, wherein A, B, D, E, m, n, R3, R7, R8, R9, R10, R11 and X are described herein.Type: GrantFiled: July 13, 2005Date of Patent: August 11, 2009Assignee: Bristol-Myers Squibb CompanyInventors: John M. Fevig, Jianxin Feng, Saleem Ahmad
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Publication number: 20090170891Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: April 6, 2007Publication date: July 2, 2009Inventors: Steven L. Colletti, James R. Tata, Weichun Chen, Richard T. Beresis, Fa-Xiang Ding, Darby Rye Schmidt, Hong Shen, Subharekha Raghavan
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Publication number: 20090163511Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, D, E, J, T, p, q and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: December 12, 2008Publication date: June 25, 2009Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Ihab S. Darwish, Jiaxin Yu, Hui Hong, Rajinder Singh, Sambaiah Thota, Xiang Xu
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Publication number: 20090156630Abstract: This invention relates to polycyclic carboxamide compounds of the formula I: with cytotoxicity, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment and/or prophylaxis of cellular proliferative disorders such as cancer.Type: ApplicationFiled: February 17, 2009Publication date: June 18, 2009Inventors: Bruce Charles Baguley, Leslie William Deady, William Alexander Denny, Thomas Rodemann, Michael Leslie Rogers
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Publication number: 20090155185Abstract: A pharmaceutical composition comprising an anticholinergic and a betamimetic of formula 2 optionally together with a pharmaceutically acceptable excipient, the anticholinergic and the betamimetic optionally in the form of their enantiomers, mixtures of their enantiomers, their racemates, their solvates, or their hydrates, processes for preparing them, and their use in the treatment of asthma, COPD, or other inflammatory or obstructive respiratory complaints.Type: ApplicationFiled: January 7, 2009Publication date: June 18, 2009Inventors: Christopher John Montague Meade, Michel Pairet, Michael P. Pieper, Ingo Konetzki
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Publication number: 20090155210Abstract: The present invention discloses 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 the compounds of the present invention.Type: ApplicationFiled: December 4, 2008Publication date: June 18, 2009Inventors: YONGHUA GAI, Yat Sun Or, Zhe Wang
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Publication number: 20090156581Abstract: Pharmaceutical compositions and method using aminergic compounds and complement compounds. Compositions are provided comprising: (a) a subefficacious amount of a non-adrenergic aminergic compound or of an adrenergic antagonist; and (b) a safe and effective amount of a complement compound. Methods are also provided comprising the administration of: (a) a low dose of a non-adrenergic aminergic compound or of any adrenergic antagonist; and (b) a safe and effective amount of a complement compound. Non-adrenergic aminergic compounds can comprise a histaminergic, dopaminergic, muscarinergic, serotoninergic, octopaminergic, or trace aminergic compound. Complement compounds include ascorbates, opioids, polycarboxylic acid chelators, resveratrols, cysteines, substituted derivatives and analogs thereof, and mixtures thereof. Preferred complements include ascorbates, particularly ascorbic acid.Type: ApplicationFiled: April 14, 2006Publication date: June 18, 2009Applicant: BOARD OF TRUSTREES OF MICHIGAN STATE UNIVERSITYInventors: Patrick F. Dillon, Robert S. Root-Bernstein
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Publication number: 20090143419Abstract: A method of treating or preventing ectoparasite infestation in a plant or animal host is provided comprising applying an effective amount of at least one metalloprotease inhibitor and/or at least one metal chelating agent, wherein the metal chelating agent is a compound comprising at least two heteroatoms able to simultaneously coordinate with a metal ion, at least one of the two heteroatoms being selected from nitrogen, sulfur, oxygen and phosphorus, wherein the compound comprises at least one carbocyclic ring substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom, or the compound comprises at least one heterocyclic ring containing at least one heteroatom, wherein said heterocyclic ring is optionally substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom.Type: ApplicationFiled: January 11, 2006Publication date: June 4, 2009Applicant: HATCHTECH PTY LTDInventor: Vernon M. BOWLES