Four Or More Ring Nitrogens In The Tricyclo Ring System Patents (Class 544/251)
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Publication number: 20130338139Abstract: Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.Type: ApplicationFiled: June 18, 2013Publication date: December 19, 2013Inventors: Amy Allan, Bryan Branstetter, James Breitenbucher, Brian Dyck, Tawfik Gharbaoui, Laurent Gomez, Andrew Richard Hudson, Tami Jo Marrone, Troy Vickers, Michael I. Weinhouse
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Publication number: 20130338148Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: August 21, 2013Publication date: December 19, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gabriella Traquandi, Maria Gabriella Brasca, Roberto D'Alessio, Paolo Polucci, Fulvia Roletto, Anna Vulpetti, Paolo Pevarello, Achille Panzeri, Francesca Quartieri, Ron Ferguson, Paola Vianello, Daniele Fancelli
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Publication number: 20130331376Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: August 14, 2013Publication date: December 12, 2013Applicant: Elan Corporation, Inc.Inventors: Robert A. Galemmo, Dean R. Artis, Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Patent number: 8598342Abstract: The present invention provides Wall Teichoic Acid biosynthesis inhibitors such as compound 1835F03 (targocil) and related synthetic analogs. The invention also provides pharmaceutical compositions thereof and methods for treating bacterial infection and the suppression of growth of bacterial cells by administering a Wall Teichoic Acid biosynthesis inhibitor. The invention is particularly useful for the treatment of Methicillin-resistant Staphylococcus aureus (MRSA). The invention further provides procedures for the syntheses of Wall Teichoic Acid biosynthesis inhibitors. The invention also provides methods for the identification of antibacterial therapeutic agents.Type: GrantFiled: June 5, 2009Date of Patent: December 3, 2013Assignee: President and Fellows of Harvard CollegeInventors: Suzanne Walker Kahne, Jonathan G. Swoboda, Timothy C. Meredith, Kyungae Lee, Jennifer Campbell
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Patent number: 8598343Abstract: A process for preparing 7-[2-[4-(6-fluoro-3-methyl-1,2-benzisoxazol-5-yl)-1-piperazinyl]ethyl]-2-(1-propynyl)-7H-pyrazolo-[4,3-e]-[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, intermediates useful in that process, and processes for preparing said intermediates are disclosed.Type: GrantFiled: August 3, 2010Date of Patent: December 3, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Shen-Chun Kuo, Yonggang Chen, Jeffrey M. Eckert, William W. Leong, Nanfei Zou, Gabriel C. Kuklis
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Patent number: 8586598Abstract: The present invention relates to novel crystalline form(s) of water-soluble salts and of free base of a cdk inhibitor. Such crystal salts are for example fumarate, L-malate, maleate, succinate, adipate, malonate, glycolate, phosphate, mesylate, L-lactate, hydrochloride, di-hydrochloride, tri-hydrochloride. Hydrates and polymorphs of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.Type: GrantFiled: April 23, 2010Date of Patent: November 19, 2013Assignee: Nerviano Medical Sciences S.R.L.Inventors: Massimo Zampieri, Annalisa Airoldi, Maria Gioia Fornaretto, Maria Gabriella Brasca
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Publication number: 20130302416Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.Type: ApplicationFiled: January 19, 2012Publication date: November 14, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
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Patent number: 8580793Abstract: The invention provides a low molecular weight ATP-competitive CDK inhibitor and TRKA inhibitor of formula (I) for use in the treatment of thymoma and thymic carcinoma. The compound can be administered together with one or more cytotoxic or cytostatic agents.Type: GrantFiled: March 15, 2010Date of Patent: November 12, 2013Assignee: Nerviano Medical Services S.r.l.Inventors: Angela Scaburri, Maria Adele Pacciarini, Marina Ciomei, Bernard Laffranchi, Silvia Comis
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Patent number: 8580783Abstract: The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives of formula (I) which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.Type: GrantFiled: September 3, 2010Date of Patent: November 12, 2013Assignee: Nerviano Medical Sciences S.r.l.Inventors: Elena Casale, Francesco Casuscelli, Claudio Dalvit, Paolo Polucci, Fabio Zuccotto
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Patent number: 8569318Abstract: The present invention relates to serotonin 5-HT6 receptor antagonists-novel substituted 3-sulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 3-sulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising drug substances as the mentioned above compounds and to the method of prophylaxis and treatment of various conditions and diseases of central nervous system in humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors. In formulas 1 and 2 Ar is optionally substituted aryl or optionally substituted heterocyclyl; R1 is hydrogen, optionally substituted lower C1-C3 alkyl, substituted hydroxyl group, substituted sulfanyl group; R2 is hydrogen or optionally substituted C1-C3 alkyl; R3 is hydrogen, optionally substituted C1-C3 alkyl or tert.-butyloxycarbonyl.Type: GrantFiled: April 30, 2009Date of Patent: October 29, 2013Inventors: Andrey Alexandrovich Ivashchenko, Volodymyr Mikhailovich Kysil, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko
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Patent number: 8569295Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: GrantFiled: July 28, 2010Date of Patent: October 29, 2013Assignee: Merck Patent GmbHInventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
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Publication number: 20130281474Abstract: This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.Type: ApplicationFiled: September 26, 2011Publication date: October 24, 2013Applicant: MERCK SHARP & DOHME CORP.Inventors: Zhaoyang Meng, Panduranga Abdulla Reddy, M. Arshad Siddiqui
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Publication number: 20130274257Abstract: The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: March 15, 2013Publication date: October 17, 2013Inventors: Argyrios G. Arvanitis, James D. Rodgers, Louis Storace, Beverly Folmer
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Patent number: 8552017Abstract: The invention relates to serotonin 5-HT6 receptor antagonists—novel 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising the said drug substances as the said compounds, and also to method of prophylaxis and treatment of various diseases of central nervious system in humans and animals pathogenesis of which is associated with serotonin 5-HT6 receptors including cognitive and neurodegenerative diseases. Substituted 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of the general formula 1 and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of the general formula 2 and pharmaceutically acceptable salts and/or hydrates thereof.Type: GrantFiled: April 30, 2009Date of Patent: October 8, 2013Inventors: Andrey Alexandrovich Ivashchenko, Volodymyr Mikhailovich Kysil, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko
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Publication number: 20130261140Abstract: The present invention is directed to novel tricyclic heterocycles of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: December 1, 2011Publication date: October 3, 2013Inventors: Duane A. Burnett, Zhiqiang Zhao, David Cole, Hubert Josien, Dmitri A. Pissarnitski, Thavalakulamgar Sasikumar, Wen-Lian Wu, Martin Domalski
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Patent number: 8546410Abstract: Heteroaryl-fused macrocyclic 2,4-diaminopyrimidine compounds of formula (I) wherein W, G1, G2, A1 and R1 are defined in the description, 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: May 5, 2009Date of Patent: October 1, 2013Assignee: AbbVie Inc.Inventors: Huaqing Liu, Irene Drizin, Marlon D. Cowart, Robert J. Altenbach
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Publication number: 20130252885Abstract: The present disclosure relates to fused tricyclic compounds of formula (I) or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2A adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2A receptor.Type: ApplicationFiled: September 22, 2011Publication date: September 26, 2013Applicant: Advinus Therapeutics LimitedInventors: Barawkar Dinesh, Basu Sujay, Ramdas Vidya, Naykodi Minakshi, Patel Meena, Shejul Yogesh, Thorat Sachin, Panmand Anil
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Patent number: 8541576Abstract: The present invention relates to substituted pyrazolo[4,3-h]quinazoline compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular PIM kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: December 16, 2011Date of Patent: September 24, 2013Assignee: Nerviano Medical Sciences SRLInventors: Francesco Casuscelli, Claudia Piutti, Antonella Ermoli, Daniela Faiardi
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Publication number: 20130237533Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: ApplicationFiled: April 24, 2013Publication date: September 12, 2013Applicant: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
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Publication number: 20130237534Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: ApplicationFiled: April 24, 2013Publication date: September 12, 2013Applicant: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
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Patent number: 8524722Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.Type: GrantFiled: September 2, 2008Date of Patent: September 3, 2013Assignee: Bayer Intellectual Property GmbHInventors: Hartmut Schirok, Ying Li-Sommer, Michael Brands, Mario Lobell, Adrian Tersteegen, Herbert Himmel, Karl-Heinz Schlemmer, Dieter Lang, Kirstin Petersen, Matthias Renz, Dominik Mumberg, Jens Hoffmann, Gerhard Siemeister, Ulf Bömer
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Publication number: 20130225549Abstract: The present invention relates to dihydropteridinones, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.Type: ApplicationFiled: February 14, 2013Publication date: August 29, 2013Applicant: Boehringer Ingelheim International GmbHInventor: Boehringer Ingelheim International GmbH
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Publication number: 20130225589Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: February 22, 2013Publication date: August 29, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Publication number: 20130217675Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. 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: February 18, 2011Publication date: August 22, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Patent number: 8513270Abstract: The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: December 20, 2007Date of Patent: August 20, 2013Assignee: Incyte CorporationInventors: Argyrios G. Arvanitis, James D. Rodgers, Louis Storace, Beverly Folmer
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Publication number: 20130211084Abstract: To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like.Type: ApplicationFiled: February 21, 2013Publication date: August 15, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Publication number: 20130203789Abstract: The invention includes compounds that inhibit LYN kinase activity. The invention further includes a method of treating, ameliorating or preventing cancer in a subject in need thereof, wherein the cancer is dependent on LYN kinase activity.Type: ApplicationFiled: February 8, 2013Publication date: August 8, 2013Applicant: VASSA INFORMATICSInventor: VASSA INFORMATICS
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Publication number: 20130203989Abstract: To provide a hydrochloride of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90 and a crystal thereof. The present invention provides a hydrochloride of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a crystal thereof, a medicament comprising the same, an anticancer agent comprising the same, and the like.Type: ApplicationFiled: February 21, 2013Publication date: August 8, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Publication number: 20130203746Abstract: 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: November 16, 2012Publication date: August 8, 2013Inventor: Medivation Technologies Inc.
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Publication number: 20130203777Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of TTR tetramers reducing its tendency to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of TTR and therby decreasing aggegate formation by TTR. Also disclosed herein are methods to screen for candidate compounds that increase stability of TTR. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.Type: ApplicationFiled: May 5, 2011Publication date: August 8, 2013Inventors: Isabella A. Graef, Mamoun Alhamadsheh
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Publication number: 20130190305Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R6, A, B, C, n, p, q and r 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 compounds of this kind and their use as medicaments.Type: ApplicationFiled: January 22, 2013Publication date: July 25, 2013Applicant: Boehringer Ingelheim International GmbHInventor: Matthias TREU
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Publication number: 20130190304Abstract: 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: March 12, 2013Publication date: July 25, 2013Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: Medivation Technologies, Inc.
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Publication number: 20130190335Abstract: Disclosed are compounds of the formula (I) which are fluorescently labeled antagonists of the A3 adenosine receptor: wherein A, R1, R2, and Y are as described herein. Also disclosed are diagnostic compositions and a method of diagnosis of a patient for a possible treatment by an antagonist of the A3 adenosine receptor, involving the use of one or more of these compounds as diagnostic agents.Type: ApplicationFiled: January 24, 2013Publication date: July 25, 2013Applicants: The United State of America, as represented by the Secretary, Department of Health and Human Service, UNIVERSITA DEGLI STUDI DI PADOVA, Universita Degli Studi Di TriesteInventors: The United State of America, as represented by th e Department of Health and Human Services, Universita Degli Studi Di Trieste, UNIVERSITA DEGLI STUDI DI PADOVA
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Publication number: 20130190293Abstract: This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-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: February 18, 2011Publication date: July 25, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Patent number: 8471008Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex, which comprises a compound having a specific heterocyclic structure, is described. Also described is an organic electroluminescence device having an anode, a cathode and an organic thin film layer having one or more layers. The organic thin film layer is interposed between the anode and cathode and has a light emitting layer containing a host material in combination with at least one phosphorescent metal complex. At least one layer of the organic thin film layer contains the material for organic electroluminescence devices. The material for organic electroluminescence devices provides an organic electroluminescence device which has a high emitting efficiency, causes little pixel defects, is excellent in heat resistance, and show a long lifetime.Type: GrantFiled: November 25, 2011Date of Patent: June 25, 2013Assignee: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
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Publication number: 20130150353Abstract: This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.Type: ApplicationFiled: August 22, 2011Publication date: June 13, 2013Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyum Zhao, Andrew McRiner
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Patent number: 8445503Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: GrantFiled: December 21, 2010Date of Patent: May 21, 2013Assignee: Elan Pharmaceuticals, Inc.Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Patent number: 8445675Abstract: Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and in the specification, and an amount of a physiologically acceptable acid or mixture of acids sufficient to dissolve the active substance and act as a stabilizer, optionally together with other formulating excipients suitable for parenteral administration, and a process for preparing the infusible or injectable solutions according to the invention.Type: GrantFiled: February 6, 2009Date of Patent: May 21, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Detlef Mohr, Claus Veit, Fridtjof Traulsen
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Publication number: 20130119360Abstract: Disclosed is an organic electroluminescence element comprising an anode, a cathode and a plurality of organic compound layers between the anode and the cathode, provided that one of the organic compound layers is a light emitting layer containing a phosphorescence emitting compound, wherein at least one of the organic compound layers contains a compound represented by Formula (1), wherein, X represents O or S; Y1 to Y3 each represents a hydrogen atom, a substituent or a group represented by Formula (A) disclosed un the specification, provided that at least two of Y1 to Y3 are groups represented by Formula (A), not all of Y1 to Y3 are the same group, and at least one of the groups represented by Formula (A) has Ar of a carbazolyl group, or an azacarbazolyl group containing 2 to 5 nitrogen atoms.Type: ApplicationFiled: December 13, 2012Publication date: May 16, 2013Inventors: Rie KATAKURA, Shuichi SUGITA, Eisaku KATOH, Motoaki SUGINO, Rie FUJISAWA
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Publication number: 20130085123Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 31, 2011Publication date: April 4, 2013Applicant: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
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Publication number: 20130079323Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.Type: ApplicationFiled: September 10, 2010Publication date: March 28, 2013Applicant: TRIUS THERAPEUTICS, INC.Inventors: Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
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Patent number: 8404698Abstract: Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperproliferative disorders are also disclosed.Type: GrantFiled: June 16, 2008Date of Patent: March 26, 2013Assignee: Rexahn Pharmaceuticals, Inc.Inventors: Young Bok Lee, Chang Ho Ahn
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Publication number: 20130071354Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: November 16, 2012Publication date: March 21, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Patent number: 8389532Abstract: The compound having the structural formula I or a pharmaceutically acceptable salt thereof, is disclosed, as well as its use in the treatment of central nervous system diseases, in particular Parkinson's disease, Extra Pyramidal Syndrome, restless legs syndrome and attention deficit hyperactivity disorder, pharmaceutical compositions comprising it, and combinations with other agents.Type: GrantFiled: July 6, 2009Date of Patent: March 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Jean E. Lachowicz
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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
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Publication number: 20130029980Abstract: The present invention relates novel flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives.Type: ApplicationFiled: April 6, 2011Publication date: January 31, 2013Inventors: Philip D. G. Coish, Brian R. Dixon, David Osterman, Paul Adrian Aristoff, Manuel Navia, Frank Sciavolino, Stephanie Avola, Nick Baboulas, Thomas R. Belliotti, Angelica Bello, Judd Berman, Robert A. Chrusciel, Bruce R. Evans, Harpreet Kaur, David Moon, Vinh Pham, Andrew Roughton, Phil Wickens, Jeffrey Wilson, Heinrich J. Schostarez
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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
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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
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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
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Patent number: RE44205Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compType: GrantFiled: April 6, 2012Date of Patent: May 7, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil