Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/243)
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Publication number: 20130230499Abstract: The present invention provides methods for early diagnosis of amyotrophic lateral sclerosis (ALS) and for determining the efficacy of a treatment for ALS in an ALS patient, i.e., monitoring ALS progression, utilizing cellular blood markers; as well as kits for carrying out these methods.Type: ApplicationFiled: March 10, 2011Publication date: September 5, 2013Inventors: Michal Eisenbach-Schwartz, Ester Yoles, Hadas Schori
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Patent number: 8524196Abstract: The invention relates to a method of relieving nicotine craving comprising the steps of providing at least one chewing gum comprising tobacco alkaloid to a user, providing relief of nicotine craving to said user by transferring of tobacco alkaloid from the chewing gum to the human body of said user by chewing of said chewing gum, said chewing of said chewing gum comprising a chewing process involving a transfer of tobacco alkaloid from said chewing gum above a threshold transfer rate in the period of about ½ minute to about 2½ minutes from initiation of said chewing process.Type: GrantFiled: November 30, 2004Date of Patent: September 3, 2013Assignee: Fertin Pharma A/SInventor: Carsten Andersen
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Publication number: 20130224306Abstract: There is provided a method for treating pulmonary hypertension in a subject, comprising: administering to the subject in need thereof a daily dose of ambrisentan from 1 mg to about 15 mg, wherein the method is carried out without drug labeling instruction to monitor liver aminotransferase levels during ambrisentan treatment.Type: ApplicationFiled: June 28, 2012Publication date: August 29, 2013Applicant: Gilead Sciences, Inc.Inventors: Hunter Campbell Gillies, Tobias Peschel, David J. Pizzuti
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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: 20130224151Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors alone or in combination for the treatment or prevention of abdominal, visceral or pelvic pain. Also described herein are pharmaceutical compositions comprising a FAAH inhibitor, alone or in combination with an additional therapeutic agent for the treatment of abdominal, visceral or pelvic pain.Type: ApplicationFiled: March 31, 2011Publication date: August 29, 2013Applicants: UNITED STATES OF AMERICA, IRONWOOD PHARMACEUTICALS, INCInventors: James Philip Pearson, Mark G. Currie, Yvette Tache, Muriel Larauche
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Publication number: 20130217685Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.Type: ApplicationFiled: January 8, 2013Publication date: August 22, 2013Applicant: UNIVERSITY OF MASSACHUSETTSInventor: University of Massachusetts
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Publication number: 20130210824Abstract: The present application relates to novel substituted fused imidazoles and pyrazoles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof producing medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: January 8, 2013Publication date: August 15, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: BAYER INTELLECTUAL PROPERTY GMBH
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Publication number: 20130196972Abstract: This invention relates to novel compounds of reverse-turn mimetics, having pyrazino-triazinone as a basic framework, and a method of preparing the same, and the use thereof to treat diseases such as cancer, in particular, acute myeloid leukemia.Type: ApplicationFiled: October 14, 2011Publication date: August 1, 2013Applicant: JW PHARMACEUTICAL CORPORATIONInventors: Jae-Uk Chung, Mi-Jung Kim, Yong-Sil Lee, Sang-Ho Ma, Young-Seok Cho, Sang-Hak Lee, Young-Jun Na, Myoung-Joo Kang, Woul-Seong Park
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Patent number: 8487096Abstract: The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.Type: GrantFiled: February 2, 2011Date of Patent: July 16, 2013Assignee: Incyte CorporationInventors: Jincong Zhuo, Chunhong He, Wenqing Yao
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Patent number: 8486943Abstract: The present invention provides a compound of the Formula (I), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating or preventing physiological disorders, particularly reduced bone mass, osteoporosis, osteopenia, reduced muscle mass or strength, or erectile dysfunction comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 14, 2009Date of Patent: July 16, 2013Assignee: Eli Lilly and CompanyInventors: Prabhakar Kondaji Jadhav, Venkatesh Krishnan, Euibong Jemes Kim
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Patent number: 8481536Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.Type: GrantFiled: December 28, 2010Date of Patent: July 9, 2013Assignee: TargeGen, Inc.Inventors: Xianchang Gong, Kathy Barrett, Jianguo Cao, Colleen Gritzen, Glenn Noronha, John D. Hood, Chi Ching Mak, Andrew McPherson, Ved Prakash Pathak, Joel Renick, Richard M. Soll, Ute Splittgerber, Wolfgang Wrasidlo, Binqi Zeng, Ningning Zhao, Elena Dneprovskaia
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Publication number: 20130172356Abstract: Disclosed is a medicament characterized by the combination of: epigallocatechin gallate, methylated epigallocatechin gallate, or a pharmacologically permitted salt thereof; and a phosphodiesterase inhibitor.Type: ApplicationFiled: June 23, 2011Publication date: July 4, 2013Applicant: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATIONInventor: Hirofumi Tachibana
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Patent number: 8476430Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation, wherein R1, R2, R3, R4, Q, A and B are as defined herein.Type: GrantFiled: July 23, 2009Date of Patent: July 2, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Chunjian Liu, Katerina Leftheris, Andrew J. Tebben
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Publication number: 20130165445Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-5 and 7-8, D?, L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: ApplicationFiled: February 1, 2013Publication date: June 27, 2013Applicant: AMGEN INC.Inventor: AMGEN INC.
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Patent number: 8471005Abstract: The present invention provides a compound of formula I or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula I has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.Type: GrantFiled: June 15, 2011Date of Patent: June 25, 2013Assignee: Cephalon, Inc.Inventors: Henry J. Breslin, Sankar Chatterjee, James L. Diebold, Bruce D. Dorsey, Derek D. Dunn, Diane E. Gingrich, Greg A. Hostetler, Robert L. Hudkins, Rachael Hunter, Kurt A. Josef, Joseph Lisko, Eugen F. Mesaros, Karen L. Milkiewicz, Gregory R. Ott, Babu G. Sundar, Jay P. Theroff, Tho Thieu, Rabindranath Tripathy, Theodore L. Underiner, Linda Weinberg, Gregory J. Wells, Craig A. Zificsak
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Publication number: 20130158037Abstract: The present invention provides compounds which are potent inhibitors against Lpd activity, PDH activity, and/or the growth of tubercle bacillus, and thus are useful in the treatment of tuberculosis infection and associated conditions. The present invention is further directed to in vitro- and in vzivo-based methods of inhibiting Lpd and/or PDH activity. In certain embodiments, these methods are useful in inhibiting Lpd and/or PDH activity key to a pathogen's survival.Type: ApplicationFiled: June 28, 2011Publication date: June 20, 2013Applicant: Academia SinicaInventors: Chi-Huey Wong, Ying-Ta Wu
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Publication number: 20130158023Abstract: Provided herein are methods for predicting the LKB1 status of a patient or a biological sample, comprising the measurement of particular gene expression levels relative to a set of reference levels that represent the gene expression level of a biological wild-type sample without LKB1 gene or protein loss or mutation and the gene expression level of a reference sample with LKB1 gene or protein loss or mutation. Further provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by particular gene expression levels.Type: ApplicationFiled: August 2, 2012Publication date: June 20, 2013Applicant: SIGNAL PHARMACEUTICALS, LLCInventors: Yuhong L. Ning, Weiming Xu, Rajesh Chopra, Peter Worland, Shuichan Xu
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Publication number: 20130158028Abstract: The present invention relates to the novel use of stimulators and activators of soluble guanylate cyclase for the treatment of sickle cell anemia and for the preservation of blood substitutes. The present invention furthermore relates to the use of stimulators and activators of soluble guanylate cyclase in combination with PDE5 inhibitors for the treatment of sickle cell anemia and for the preservation of blood substitutes.Type: ApplicationFiled: June 21, 2011Publication date: June 20, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Johannes-Peter Stasch, Eva-Maria Becker, Hubert Trübel, Herbert Himmel
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Publication number: 20130158000Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.Type: ApplicationFiled: December 14, 2012Publication date: June 20, 2013Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventor: BAYER INTELLECTUAL PROPERTY GmbH
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Publication number: 20130150370Abstract: Pharmaceutical composition for oral administration comprises at least one phosphodiesterase inhibitor and at least one sugar alcohol selected from mannitol, sorbitol, xylitol, maltitol, lactitol, erythritol, threitol and Isomalt, and sodium hydrogen carbonate as pharmaceutical excipients in the following weight proportions: phosphodiesterase inhibitor: about 10 to about 150 parts by weight in total; sugar alcohol: about 50 to about 600 parts by weight in total; and sodium hydrogen carbonate: about 2 to about 100 parts by weight. The above composition for use in a method of treating male erectile dysfunction with an accelerated onset of action is also disclosed.Type: ApplicationFiled: June 24, 2011Publication date: June 13, 2013Inventor: Hartwig Steckel
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Publication number: 20130150351Abstract: Methods for treating a central nervous system (CNS) injury in a subject are provided. As of the methods include administering to the subject an effective amount of gamma aminobutyric acid (GABA) receptor signaling inhibitor to treat the subject for the CNS injury. Also provided are compositions useful in embodiments of the methods. Methods and compositions of the invention find use in the treatment of a variety of different CNS injuries, including but not limited to, treating a subject for CNS injury associated with the occurrence of stroke.Type: ApplicationFiled: June 2, 2011Publication date: June 13, 2013Inventors: Stanley T. Carmichael, Istvan Mody, Ben Huang, Andrew N. Clarkson
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Publication number: 20130150369Abstract: Benzotriazine doxides are disclosed as drugs targeting mycobacterium tuberculosis, including novel compounds of formula I:Type: ApplicationFiled: December 23, 2012Publication date: June 13, 2013Applicant: SRI INTERNATIONALInventors: Peter Madrid, Sidharth Chopra, Kenneth Ryan, Gary Koolpe
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Patent number: 8461330Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.Type: GrantFiled: June 10, 2010Date of Patent: June 11, 2013Assignee: Incyte CorporationInventors: Jincong Zhuo, Meizhong Xu, Chunhong He, Colin Zhang, Ding-Quan Qian, David M. Burns, Yun-Long Li, Brian Metcalf, Wenqing Yao
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Patent number: 8455488Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: GrantFiled: June 5, 2009Date of Patent: June 4, 2013Assignee: PRISM BioLab CorporationInventors: Takenao Odagami, Yuji Kogami, Hiroyuki Kouji
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Publication number: 20130131064Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.Type: ApplicationFiled: January 14, 2013Publication date: May 23, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Patent number: 8445676Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of such as Jak2 and CK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: GrantFiled: October 8, 2009Date of Patent: May 21, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Ashok Vinayak Purandare, David B. Frennesson, Muthoni G. Kamau, Lalgudi S. Harikrishnan, Mark G. Saulnier
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Publication number: 20130123264Abstract: Compositions and formulations useful for treating inflammatory bowel diseases, intestinal cancers, and improving the integrity of the luminal surface of the gastrointestinal tract are disclosed. Typically, the composition increases level of cGMP in the intestinal mucosa or increases the activity of a PKG, preferably PKG2, in the intestinal mucosa. Preferably, the composition includes a phosphodiesterase type 5 (PDE5) inhibitor and is targeted to the intestinal mucosa, for example by enteric coating or attachment of an intestinal specific targeting moiety. Methods of using the compositions to treat intestinal and bowel diseases, and intestinal cancers, and methods of improving one or more physiological parameters of intestinal luminal integrity including, but are not limited to, reduced proliferation for example in the intestinal crypts, reduced apoptosis for example at the luminal surface, and induction of downstream effectors of PKG-mediated signaling are also disclosed.Type: ApplicationFiled: October 17, 2012Publication date: May 16, 2013Inventor: Darren D. Browning
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Patent number: 8440813Abstract: The invention provides compounds of Formula (I), as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.Type: GrantFiled: January 11, 2008Date of Patent: May 14, 2013Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, V. Satish Kumar, Pravin L. Kotian, Minwan Wu
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Patent number: 8440671Abstract: The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiestersa-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.Type: GrantFiled: May 19, 2008Date of Patent: May 14, 2013Assignee: Vivus, Inc.Inventor: Jerry M. Held
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Publication number: 20130116257Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.Type: ApplicationFiled: December 21, 2012Publication date: May 9, 2013Applicant: GILEAD COLORADO, INC.Inventor: GILEAD COLORADO, INC.
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Patent number: 8431695Abstract: This invention relates to novel compounds of formula (I). Formula (I) in which the variable groups are as defined in the specification and claims, to pharmaceutical compositions containing them, and to a method of treatment using them for treatment of cancer.Type: GrantFiled: November 2, 2006Date of Patent: April 30, 2013Assignee: Bayer Intellectual Property GmbHInventors: Stephen O'Connor, Jacques Dumas, Wendy Lee, Julie Dixon, David Cantin, David Gunn, Jennifer Burke, Barton Phillips, Derek Lowe, Tatiana Shelekhin, Gan Wang, Xin Ma, Shihong Ying, Andrea McClure, Furahi Achebe, Mario Lobell, Frederick Ehrgott, Christiana Iwuagwu, Kyle Parcella
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Publication number: 20130096114Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or a pharmaceutically acceptable salt, stereoisomer, or hydrate thereof.Type: ApplicationFiled: December 7, 2012Publication date: April 18, 2013Applicant: SURFACE LOGIX, INC.Inventor: SURFACE LOGIX, INC.
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Publication number: 20130096109Abstract: An object of the present invention is to provide a novel integrase inhibitor. The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.Type: ApplicationFiled: April 11, 2011Publication date: April 18, 2013Applicant: SHIONOGI & CO., LTD.Inventors: Kazunari Hattori, Kenji Tomita
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Publication number: 20130096129Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).Type: ApplicationFiled: July 20, 2012Publication date: April 18, 2013Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
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Patent number: 8420645Abstract: The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.Type: GrantFiled: May 20, 2009Date of Patent: April 16, 2013Assignee: Incyte CorporationInventors: Lingkai Weng, Lei Qiao, Jiacheng Zhou, Pingli Liu, Yongchun Pan
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Patent number: 8420810Abstract: A compound of a formula (I): wherein R1 represents a C3-10 branched alkyl group which may be substituted; R2 represents a hydrogen atom or a C1-4 alkyl group which may be substituted; R3 represents a C1-4 alkyl group which may be substituted or a halogen atom; R4 represents a C1-4 alkyl group which may be substituted; and ring 1 represents a cyclic group which has planarity and may have a substituent group, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a medicinal component having CRF antagonistic activity for the prevention and/or treatment of a neuropsychiatric disease, a peripheral organ disease and the like.Type: GrantFiled: April 25, 2008Date of Patent: April 16, 2013Assignee: Ono Pharmaceutical, Co., Ltd.Inventors: Tetsuji Saito, Tetsuo Obitsu, Yoshifumi Kagamiishi
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Patent number: 8410264Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: GrantFiled: August 19, 2010Date of Patent: April 2, 2013Assignee: Novartis AGInventors: Miao Dai, Xingnian Fu, Feng He, Lei Jiang, Yue Li, Fang Liang, Lei Liu, Yuan Mi, Yao-chang Xu, Guoliang Xun, Xiaoxia Yan, Zhengtian Yu, Ji Yue Zhang
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Patent number: 8410098Abstract: Disclosed are N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-oxo-1,2,4-triazin-6-yl]ethyl}butyramide (which is represented by formula III and utilized for preparing vardenafil), its preparation method, intermediates during preparation procedure, preparation method for such intermediates and a method for preparing vardenafil from the compound.Type: GrantFiled: December 28, 2007Date of Patent: April 2, 2013Assignee: Topharman Shanghai Co., Ltd.Inventors: Guanghui Tian, Zheng Liu, Jin Zheng, Jingshan Shen
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Publication number: 20130078306Abstract: The invention relates to a method for producing medicaments that contain vardenafil hydrochloride, essentially as trihydrate in solid form, and to medicaments that can be obtained according to this methodType: ApplicationFiled: September 24, 2012Publication date: March 28, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: Bayer Intellectual Property GMBH
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Publication number: 20130071415Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula I.Type: ApplicationFiled: May 27, 2011Publication date: March 21, 2013Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pravin L. Kotian, Minwan Wu
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Publication number: 20130059854Abstract: Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, particularly anti-migraine agents to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.Type: ApplicationFiled: October 18, 2012Publication date: March 7, 2013Applicant: NAL PHARMACEUTICALS LTD.Inventor: NAL Pharmaceuticals Ltd.
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Publication number: 20130059844Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.Type: ApplicationFiled: March 26, 2012Publication date: March 7, 2013Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jorg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
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Patent number: 8389570Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: August 12, 2011Date of Patent: March 5, 2013Assignee: Pharmacyclics, Inc.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Patent number: 8377933Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.Type: GrantFiled: June 16, 2011Date of Patent: February 19, 2013Assignee: Gilead Colorado, Inc.Inventors: Michael J. Gerber, Christopher Dufton
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Publication number: 20130040928Abstract: The present invention relates to compounds having general formula I characterised in that wherein in particular: R1 represents one or a plurality of groups such as: trifluoromethyl, halogen such as F, Cl, Br, methyl, nitro. R represents nitrogen T-U represents C?C, V represents N, W represents C?O, R2 represents Cl or H, R3=H and R4=Me, A represents wherein n=m=1, X represents —CH2— and E represents —CH—, and D represents oxygen, along with the various isomers and mixtures thereof in any proportions, and the pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 15, 2011Publication date: February 14, 2013Applicant: PIERRE FABRE MEDICAMENTInventors: Isabelle Leroy, Elisabeth Dupont-Passelaigue, Samuel Mialhe, Didier Junquero, Karine Valeille
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Patent number: 8372971Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: GrantFiled: September 23, 2011Date of Patent: February 12, 2013Assignee: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
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Publication number: 20130035340Abstract: The present invention relates to soluble guanylate cyclase (sGC) and to phosphodiesterases (PDEs) and the pharmacology of sGC stimulators, sGC activators and PDE inhibitors. More particularly, the invention relates to the use of sGC stimulators and sGC activators in combination with PDE5 inhibitors for preparation of medicaments for the treatment of Cystic Fibrosis (CF).Type: ApplicationFiled: February 3, 2011Publication date: February 7, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Peter Sandner, Georges Von Degenfeld, Johannes-Peter Stasch
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Publication number: 20130029982Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130023514Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) pyrrolotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: March 30, 2011Publication date: January 24, 2013Applicant: Bristol-Myers Squibb CompanyInventors: Jay A. Markwalder, Brian E. Fink, Ashvinikumar V. Gavai, Liqi He, Soong-Hoon Kim, Steven P. Seitz
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Publication number: 20130012515Abstract: A series of fused bicyclic pyridine and pyrazine derivatives, substituted directly on the pyridine or pyrazine ring by a functional group attached via a sulphur-containing linkage, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: November 11, 2010Publication date: January 10, 2013Applicant: UCB PHARMA S.A.Inventors: Gilles Raphy, Roland Bürli, Alan Findlay Haughan