Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
-
Patent number: 8383638Abstract: The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: December 13, 2010Date of Patent: February 26, 2013Assignee: Merck Sharp & DohmeInventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng DiMarco, Thomas J. Greshock
-
Publication number: 20130045229Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.Type: ApplicationFiled: April 20, 2011Publication date: February 21, 2013Applicant: KINETA, INC.Inventors: Shawn P. Iadonato, Kristin Bedard
-
Patent number: 8377951Abstract: Pharmaceutical compositions for interfering with neuronal transmission comprising an effective amount of at least one tricyclic 3,4-propinoperhydropurine are disclosed. Preparations for facial rejuvenation are provided that comprise an effective amount of the composition of the invention and a facial cream. Methods of interfering with neuronal transmission comprising topical application of an effective amount of the pharmaceutical compositions of the invention are provided. In another aspect of the invention, effective amounts of the pharmaceutical compositions and a transdermal therapeutic system are provided for transdermal administration of at least one tricyclic 3,4-propinoperhydropurine. The pharmaceutical composition contains at least one at least one tricyclic 3,4-propinoperhydropurine, and may be formulated for transdermal drug delivery. The transdermal drug delivery system may be a laminated composite comprising a backing layer, a drug reservoir, and a means for affixing the composite to the skin.Type: GrantFiled: May 6, 2005Date of Patent: February 19, 2013Assignee: Phytotox LimitedInventor: Nestor Antonio Lagos Wilson
-
Publication number: 20130039976Abstract: The invention concerns a sodium channel blocker for the treatment of a reduction or loss of superficial sensitivity or sense of touch of a human being or another mammal.Type: ApplicationFiled: February 10, 2011Publication date: February 14, 2013Applicant: PHYTOTOX LIMITEDInventors: Max Rutman, Jean J. Pilorget, Constanza Sigala, Pablo Valenzuela
-
Publication number: 20130035348Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.Type: ApplicationFiled: April 6, 2011Publication date: February 7, 2013Applicant: BRIGHAM YOUNG UNIVERSITYInventor: Marc Hansen
-
Publication number: 20130028945Abstract: The present invention relates to a novel pharmaceutical composition free of gastric coating comprising anagrelide hydrochloride in combination with a non-pH dependent polymer and a pharmaceutically acceptable watersoluble acid and its use for the treatment of essential thrombocythemia.Type: ApplicationFiled: March 25, 2011Publication date: January 31, 2013Applicant: AOP ORPHAN PHARMACEUTICALS AGInventors: Rudolf Widmann, Georg Strieder
-
Publication number: 20130023538Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: September 26, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
-
Publication number: 20130022671Abstract: Provided are prophylactic and therapeutic methods of treatment of subjects for the purpose of inhibiting vaso-occlusive events, including embolism, by administering agents, including anagrelide and anagrelide derivatives, which reduce the number of circulating platelets to low normal or to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.Type: ApplicationFiled: July 17, 2012Publication date: January 24, 2013Inventors: Paul F. Glidden, Alison J. Pilgrim, Stephen R. Hanson
-
Patent number: 8357707Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase.Type: GrantFiled: July 2, 2010Date of Patent: January 22, 2013Assignee: Novartis AGInventors: Robin Alec Fairhurst, Marc Gerspacher, Robert Mah
-
Patent number: 8357694Abstract: The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 30, 2009Date of Patent: January 22, 2013Assignee: ArQule, Inc.Inventors: Syed Ali, Mark Ashwell, Manish Tandon, Nivedita Namdev, Jean-Marc Lapierre, Neil Westlund, Rocio Palma, Rui-Yang Yang, Yanbin Liu, David Vensel, Sudharshan Eathiraj, Hui Wu, Eugene Kelleher
-
Publication number: 20130018051Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
-
Publication number: 20130018063Abstract: The invention provides novel 7,8-dihydro-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2H]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C2-9 alkyl, C3-9 cycloalkyl, heteroarylalkyl, or substituted arylalkyl, in free, salt or prodrug form, processes for their production, their use as pharmaceuticals, particularly as PDE1 inhibitors, and pharmaceutical compositions comprising them.Type: ApplicationFiled: July 18, 2012Publication date: January 17, 2013Inventors: Peng LI, Haiyan Wu
-
Patent number: 8354418Abstract: The present invention relates to compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.Type: GrantFiled: January 9, 2009Date of Patent: January 15, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Trixi Brandl, Udo Maier, Christoph Hoenke, Anne T. Joergensen, Alexander Pautsch, Steffen Breitfelder, Matthias Grauert, Matthias Hoffmann, Stefan Scheuerer, Klaus Erb, Michael Pieper, Ingo Pragst
-
Patent number: 8349858Abstract: The present invention relates to Polycyclic Guanine Derivatives, compositions comprising the Polycyclic Guanine Derivatives and methods of using the Polycyclic Guanine Derivatives to treat pain or an inflammatory disease.Type: GrantFiled: June 18, 2008Date of Patent: January 8, 2013Assignee: Merck Sharp & DohmeInventors: Deen Tulshian, William B. Geiss, Gregory S. Martin, Van-Duc Le, James C. Haber, Jr., Julius J. Matasi, Michael F. Czarniecki, Stephanie Nicole Cooke
-
Patent number: 8343983Abstract: The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: March 31, 2010Date of Patent: January 1, 2013Assignee: ArQule, Inc.Inventors: Manish Tandon, Jianqiang Wang, Nivedita Namdev
-
Patent number: 8338408Abstract: 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: GrantFiled: October 27, 2008Date of Patent: December 25, 2012Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew A. Protter, Rajendra P. Jain, Sundeep Dugar, Sarvajit Chakravarty, Sergey O. Bachurin, Anatoly K. Ustinov, Bogdan K. Beznosko, Nadezhda Sergeevna Beznosko, legal representative, Elena F. Shevtsova, Vladimir V. Grigoriev
-
Publication number: 20120322818Abstract: Pharmaceutical compositions for interfering with neuronal transmission comprising an effective amount of at least one tricyclic 3,4-propinoperhydropurine and at least one additional compound are disclosed. Preparations for topical applications are provided that comprise an effective amount of the composition of the invention and a pharmacologically acceptable carrier. Methods of interfering with neuronal transmission comprising topical application of an effective amount of the at least one tricyclic 3,4-propinoperhydropurine are provided for treatment of a variety of indications that relate to muscle relaxation, anesthesia, muscle spasms and similar causes.Type: ApplicationFiled: June 19, 2012Publication date: December 20, 2012Applicant: Phytotox LimitedInventor: Nestor Antonio Lagos Wilson
-
Publication number: 20120316176Abstract: The present invention relates to derivatives of 7,8-dihydro-1H-imidazo[2,1-b]purin-4(5H)-one, compositions thereof and methods of use thereof for treating or preventing pain or an inflammatory disease.Type: ApplicationFiled: December 16, 2010Publication date: December 13, 2012Inventors: Deen Tulshian, Michael F. Czarniecki, Julius Matasi, Stephanie N. Brumfield
-
Publication number: 20120316136Abstract: The present patent application relates to treatment of a respiratory disorder using TRPA1 antagonists. Particularly, the present patent application relates to treatment of a respiratory disorder using a TRPA1 antagonist, wherein the TRPA1 antagonist is administered by inhalation route to a subject in need thereof.Type: ApplicationFiled: June 13, 2012Publication date: December 13, 2012Applicant: GLENMARK PHARMACEUTICALS S.A.Inventors: Neelima KHAIRATKAR-JOSHI, Abhay KULKARNI, Indranil MUKHOPADHYAY, Vidya Ganapati KATTIGE, Vikram Mansingh BHOSALE, Dinesh Pradeep WALE, Abraham THOMAS, Sukeerthi KUMAR, Sachin Sundarlal CHAUDHARI
-
Publication number: 20120316184Abstract: Compounds of formula (I) wherein G1 represents together with the two ring atoms of the pyrimidine ring to which it is attached, a 5- to 6-membered aromatic heterocyclic ring system which contains one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the other substituents are as defined in claim 1, are suitable for use as micro-biocides.Type: ApplicationFiled: February 18, 2011Publication date: December 13, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Martin Pouliot, David Guillaume Claude Francois Lefranc, Laura Quaranta, Clemens Lamberth, Nityakalyani Srinivas
-
Patent number: 8329715Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-? or by PDE4, including but not limited to rheumatoid arthritis.Type: GrantFiled: March 2, 2012Date of Patent: December 11, 2012Assignee: High Point Pharmaceuticals, LLCInventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel
-
Patent number: 8329714Abstract: (?)-5-(3-Chlorophenyl)-?-(4-chlorophenyl)-?-(1-methyl-1H-imidazol-5-yl)tetrazolo-[1,5-a]quinazoline-7-methanamine and its pharmaceutically acceptable acid addition salts, and the use of such compounds in medicine especially for the treatment of cancer.Type: GrantFiled: January 31, 2007Date of Patent: December 11, 2012Assignee: Janssen Pharmaceutica NVInventors: Marc Gaston Venet, Patrick René Angibaud, David William End
-
Patent number: 8324228Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z are as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors, such as, for example, inflammation.Type: GrantFiled: September 19, 2011Date of Patent: December 4, 2012Assignee: University of Tennessee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa, Patrick Allison
-
Patent number: 8324227Abstract: The present invention discloses novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.Type: GrantFiled: September 5, 2008Date of Patent: December 4, 2012Assignee: FDC LimitedInventors: Hanumant Bapurao Borate, Suleman Riyajsaheb Maujan, Sangmesher Prabhakar Sawargave, Sheerang Vidhyadhar Joshi, Sharangi Vaiude, Mohan Anand Chandavarkar
-
Publication number: 20120302533Abstract: The present invention relates to derivatives of pyrimido[6,1-a]isoquinolin-4-one and their application as inhibitors of phosphodiesterase (PDE) isoenzymes. More particularly the invention relates to derivatives of pyrimido[6,1-a]isoquinolin-4-one and their use in medicine for example as bronchodilators with anti-inflammatory properties.Type: ApplicationFiled: August 7, 2012Publication date: November 29, 2012Applicant: Verona Pharma plcInventors: Alexander William Oxford, David Jack
-
Patent number: 8318753Abstract: (?)-5-(3-Chlorophenyl)-?-(4-chlorophenyl)-?-(1-methyl-1H-imidazol-5-yl)tetrazolo-[1,5-a]quinazoline-7-methanamine and its pharmaceutically acceptable acid addition salts, and the use of such compounds in medicine especially for the treatment of cancer.Type: GrantFiled: October 29, 2007Date of Patent: November 27, 2012Assignee: Janssen Pharmaceutica NVInventors: Marc Gaston Venet, Patrick René Angibaud, David William End
-
Patent number: 8314114Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: GrantFiled: May 2, 2011Date of Patent: November 20, 2012Assignee: Duquesne University of The Holy GhostInventor: Aleem Gangjee
-
Publication number: 20120289523Abstract: The invention relates to novel compounds useful in the treatment and prophylaxis of disease. Compounds of the formula (I) wherein X is halogen, independently selected form chlorine and fluorine and n is 0, 1 or 2, and their pharmaceutically acceptable salts are useful in the treatment and prophylaxis of diseases caused by activation of microglia, particularly Alzheimer's disease.Type: ApplicationFiled: October 7, 2010Publication date: November 15, 2012Applicants: BTG INTERNATIONAL LIMITED, SENEXIS LIMITEDInventor: David Scopes
-
Publication number: 20120289524Abstract: The invention relates to novel compounds useful in the treatment and prophylaxis of disease. Compounds of the formula (I): wherein X is halogen, independently selected form chlorine and fluorine and their pharmaceutically acceptable salts are useful in the treatment and prophylaxis of diseases caused by activation of microglia, particularly Alzheimer's disease.Type: ApplicationFiled: October 7, 2010Publication date: November 15, 2012Applicant: Senexis LimitedInventors: David Scopes, David Horwell
-
Patent number: 8309561Abstract: Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: December 21, 2007Date of Patent: November 13, 2012Assignee: Ajinomoto Co., Inc.Inventors: Kazuyuki Sagi, Tatsuya Okuzumi, Tatsuhiro Yamada, Shunsuke Kageyama, Yoichiro Shima, Tadakiyo Nakagawa, Munetaka Tokumasu, Masayuki Sugiki, Hajime Ito, Itsuya Tanabe, Tamotsu Suzuki, Akira Nakayama, Kazuyuki Ubukata, Kenji Shinkai, Yasuhiro Tanaka, Misato Noguchi, Ayatoshi Andou, Yoriko Yamamoto, Noriyasu Kataoka, Koichi Fujita
-
Patent number: 8309564Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: GrantFiled: June 2, 2011Date of Patent: November 13, 2012Assignee: Duquesne University of The Holy SpiritInventor: Aleem Gangjee
-
Publication number: 20120283238Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: January 10, 2012Publication date: November 8, 2012Applicant: NIMBUS IRIS, INC.Inventors: Donna L. Romero, Matthew David Wessel, Shaughnessy Robinson, Jeremy Robert Greenwood, Karl Shawn Watts, Leah Lynn Frye, Geraldine C. Harriman, Alan Franklin Corin, Craig E. Masse
-
Publication number: 20120277100Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; A is O, S, NR3e or C(R3c)?C(R3d); Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 1, 2 or 3; and R1, R2, R3a—R3e, R4, R5, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: August 3, 2010Publication date: November 1, 2012Inventors: Wenming Zhang, Caleb William Holyoke, JR., Kenneth Andrew Hughes, George Philip Lahm, Thomas Francis Pahutski, JR., My-Hanh Thi Tong, Ming Xu
-
Publication number: 20120276088Abstract: Methods and compositions relating to TIC10 are described according to aspects of the present invention. The compositions and methods have utility in treating disease, particularly cancer in a subject in need thereof, including a human subject as well as subjects of other species. The compositions have utility in treating brain cancer in a subject in need thereof.Type: ApplicationFiled: April 30, 2012Publication date: November 1, 2012Applicant: The Penn State Research FoundationInventors: Wafik S. El-Deiry, Joshua E. Allen, Gen Sheng Wu
-
Publication number: 20120264768Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.Type: ApplicationFiled: February 2, 2012Publication date: October 18, 2012Inventor: Aleem Gangjee
-
Publication number: 20120264761Abstract: The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: December 13, 2010Publication date: October 18, 2012Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng DiMarco, Thomas J. Greshock
-
Patent number: 8288376Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: GrantFiled: January 24, 2012Date of Patent: October 16, 2012Assignee: SanofiInventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
-
Patent number: 8288400Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: August 8, 2011Date of Patent: October 16, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
-
Patent number: 8288399Abstract: Method for treating Alzheimer's disease, Parkinson's disease, Huntington's chorea or Pick's disease by administering to a patient a compound of formula (I) wherein R1 represents hydrogen; R2 represents hydrogen, a C1-C6 alkyl group or C3-C6 cycloalkyl group; A represents nitrogen; D represents a methylene group, a methyl methylene group, a halogen atom substituted methylene group or a halogen substituted methyl methylene group; E represents CH2, CHR3 wherein R3 represents a C1-C6 alkyl group, CH or a carbon atom substituted by a C1-C6 alkyl group; Arom represents aryl, aryl having from 1 to 3 identical or different substituent groups selected from halogen, C1-C6 alkyl, and C1-C6 alkyloxy, heteroaryl or heteroaryl having from 1 to 3 substituent groups, selected from halogen, C1-C6 alkyl and C1-C6 alkyloxy. The part represented by is a single bond or double bond.Type: GrantFiled: August 12, 2008Date of Patent: October 16, 2012Assignee: BTG International LimitedInventors: Tomiichiro Oda, Shigeko Uryu, Shinya Tokuhiro
-
Publication number: 20120252828Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: December 9, 2010Publication date: October 4, 2012Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
-
Publication number: 20120244110Abstract: Compounds of Formula I are useful inhibitors of CDK 4, CDK6, and FLT3. Such compounds are useful in treating cancer and various other disease conditions. Compounds of Formula I have the following structure: where R1 is a group of Formula IA, Formula IB, Formula IC, or Formula ID and the definitions of the other variables are provided herein.Type: ApplicationFiled: March 21, 2012Publication date: September 27, 2012Applicant: Amgen Inc.Inventors: Xiaoqi Chen, Kang Dai, Jason Duquette, Michael W. Gribble, JR., Justin N. Huard, Kathleen S. Keegan, Zhihong Li, Sarah E. Lively, Lawrence R. McGee, Mark L. Ragains, Xianghong Wang, Margaret F. Weidner, Jian Zhang
-
Publication number: 20120245118Abstract: Methods of treating stuttering include treating people with gamma-aminobutyric acid (GABA) receptor modulators, including cyclopyrrolones. A second active agent may be used with GABA receptor modulators. Active enantiomers, active metabolites, and pharmaceutically acceptable salts of gamma-aminobutyric acid receptor modulators, including cyclopyrrolones, are acceptable components of the compositions. The cyclopyrrolone class of modulators includes pagoclone, suriclone, zopiclone, 2-(7-chloro-2-naphthyridin-1,8-yl)-3-(5-methyl-2-oxohexyl)isoindolin-1-one, 2-(7-chloro-2-naphthyridin-1,8-yl)isoindolin-1-yl-4-acetamidobutyrate, and 2-(7-chloro-1,8-naphthyridin-2yl)-3-(5-methyl-5-hydroxy-2-oxohexyl)-1-isoindolinone.Type: ApplicationFiled: June 6, 2012Publication date: September 27, 2012Applicant: Endo Pharmaceuticals Solutions Inc.Inventors: John J. Murphy, Kay Jorgenson D'Orlando
-
Patent number: 8273758Abstract: Compounds of formula (I): wherein: Z, R1, R2, R3, n, and m are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.Type: GrantFiled: December 15, 2010Date of Patent: September 25, 2012Assignees: Sanofi, Mitsubishi Tanabe Pharma CorporationInventors: Antonio Almario Garcia, Alistair Lochead, Mourad Saady, Philippe Yaiche
-
Publication number: 20120238592Abstract: Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided.Type: ApplicationFiled: June 4, 2012Publication date: September 20, 2012Applicant: Phytotox S.A.Inventor: Nestor Antonio Lagos Wilson
-
Publication number: 20120238542Abstract: Compounds of general formula (I) wherein the groups R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.Type: ApplicationFiled: July 20, 2011Publication date: September 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Matthias Treu
-
Patent number: 8268846Abstract: Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein.Type: GrantFiled: July 10, 2009Date of Patent: September 18, 2012Assignee: Abbott LaboratoriesInventors: Brian D. Wakefield, Robert J. Altenbach, Lawrence A. Black, Marlon D. Cowart, Irene Drizin, Huaqing Liu
-
Patent number: 8268833Abstract: This invention comprises the novel compounds of formula (I) wherein n, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: February 18, 2009Date of Patent: September 18, 2012Assignee: Janssen Pharmaceutica, N.V.Inventors: Patrick René Angibaud, Isabelle Noëlle Constance Pilatte, Sven Franciscus Anna Van Brandt, Bruno Roux, Peter Ten Holte, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Alexey Borisovich Dyatkin
-
Publication number: 20120232086Abstract: The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.Type: ApplicationFiled: November 12, 2010Publication date: September 13, 2012Applicant: MERCK SHARP & DOHME CORP.Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew W. Stampford
-
Publication number: 20120225894Abstract: This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.Type: ApplicationFiled: May 11, 2012Publication date: September 6, 2012Applicant: Ardea Biosciences, Inc.Inventors: Jean-Luc GIRARDET, Zhi HONG, Stephanie SHAW, Yung-hyo KOH
-
Publication number: 20120225845Abstract: The invention provides novel compounds useful for the treatment of disorders associated with a defect in vesicular transport (e.g., axonal transport). The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.Type: ApplicationFiled: May 4, 2012Publication date: September 6, 2012Applicant: Myrexis, Inc.Inventors: Christine Klein, Andrew D. Gassman, Leena Bhoite, John Manfredi