Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/243)
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Publication number: 20120122872Abstract: Provided are methods of treating or preventing a fungal infection in a subject. The methods comprise identifying a subject with or at risk of developing a fungal infection and administering to the subject a therapeutically effective amount of an inhibitor or a fungal phosphoinositide-dependent kinase 1 (PDK-1) or a homolog thereof. Inhibition of the fungal PDK-1 or homolog thereof results in the treatment or prevention of a fungal infection in the subject. Also provided are compositions comprising an inhibitor of a fungal phosphoinositide-dependent kinase 1 (PDK-1) or a homolog thereof, and a pharmaceutically acceptable carrier.Type: ApplicationFiled: November 17, 2011Publication date: May 17, 2012Applicant: UNIVERSITY OF ROCHESTERInventors: Damian Krysan, Louis DiDone, Bonnie K. Baxter
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Publication number: 20120107328Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: November 3, 2008Publication date: May 3, 2012Inventors: William J. Greenlee, Zhaoning Zhu, Theodros Asberom, Xianhai Huang, Hubert B. Josien
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Publication number: 20120107274Abstract: Provided are methods for treating Orthomyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: wherein R2 is halogen. The compounds, compositions, and methods provided are particularly useful for the treatment of Human Influenza virus infections.Type: ApplicationFiled: September 12, 2011Publication date: May 3, 2012Applicant: Gilead Sciences, Inc.Inventors: Michael O'Neil Hanrahan Clarke, Choung U. Kim, Willard Lew
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Publication number: 20120108594Abstract: Processes are provided for selectively preparing novel stable crystalline salt forms, selectively and consistently, namely, preparing Form N-1 of the methanesulfonic acid salt, and Form N-1 and Form N-4 of the hydrochloric acid salt of the p38 kinase inhibitor 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide. The processes preferably employ solvent systems including formic acid/acetone and formic acid/methylethyl ketone which produce crystals having suitable flow properties and desired particle size, and solvents such as N,N-dimethylformamide and N,N-dimethylacetamide may be employed as well. Novel Form N-1 crystals of the Form N-1 and Form N-4 crystals of the hydrochloride salt and Form N-1 crystals of the methanesulfonic acid salt of the above free base, pharmaceutical compositions containing such novel forms and a method of treating p38 kinase associated conditions, including rheumatoid arthritis are also provided.Type: ApplicationFiled: November 10, 2011Publication date: May 3, 2012Inventors: Soojin Kim, Mary F. Malley, Zhongping Shi
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Publication number: 20120094947Abstract: Methods for treating diseases in humans and vertebrate animals are provided using competitive antagonists of cellular metabolites combined with a protective agent for protecting host cells from toxic effects of the drugs. Also provided are kits comprising competitive antagonists and suitable protective agents. In addition, screening methods for identifying competitive antagonists, protective agents and potentiating agents, for use according to the methods of the invention, are provided.Type: ApplicationFiled: August 15, 2008Publication date: April 19, 2012Inventors: Adam Lubin, Martin Lubin
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Publication number: 20120088770Abstract: 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 chemical library 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: ApplicationFiled: May 7, 2010Publication date: April 12, 2012Applicant: Prism BioLab CorporationInventors: Takenao Odagami, Yiji Kogami, Hiroyuki Kouji
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Patent number: 8148375Abstract: The invention relates to (cyclopropylphenyl) phenyloxamides and their physiologically tolerated salts, and their use as a medicament.Type: GrantFiled: March 16, 2010Date of Patent: April 3, 2012Assignee: Sanofi-AventisInventors: Elisabeth Defossa, Thomas Klabunde, Viktoria Dietrich, Siegfried Stengelin, Guido Haschke, Andreas Herling, Johanna Kuhlmann-Gottke, Stefan Bartoschek
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Patent number: 8148522Abstract: The invention relates to 2,4-dibromoropyrrolo[1,2-f][1,2,4]triazine, which is an intermediate useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and a process for preparing the intermediate.Type: GrantFiled: January 2, 2008Date of Patent: April 3, 2012Assignee: Bristol-Myers Squibb CompanyInventor: Upender Velaparthi
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Patent number: 8148523Abstract: The invention relates to 4-chloro-2-iodopyrrolo[1,2-f][1,2,4]triazine, which is an intermediate useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and a process for preparing said intermediate.Type: GrantFiled: January 7, 2008Date of Patent: April 3, 2012Assignee: Bristol-Myers Squibb CompanyInventor: Brian E. Fink
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Publication number: 20120077814Abstract: The disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof, compositions containing these compounds, and methods of using these compounds in a variety applications, such as treatment of diseases or disorders associated with E1 type activating enzymes, and with Nedd8 activating enzyme (NAE) in particular.Type: ApplicationFiled: September 12, 2011Publication date: March 29, 2012Inventors: Zhong Wang, Emilie D. Smith, James M. Veal, Kenneth H. Huang, Robert N. Atkinson, Rong Jiang
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Patent number: 8143393Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: GrantFiled: December 1, 2006Date of Patent: March 27, 2012Assignee: Bayer HealthCare LLCInventors: Julie A. Dixon, Barton Phillips, Furahi Achebe, Harold C. E. Kluender, Jason Newcom, Kyle Parcella, Steven Magnuson, Zhenqiu Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler, Stephen O'Connor
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Patent number: 8143251Abstract: The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, 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: February 24, 2011Date of Patent: March 27, 2012Assignee: Incyte CorporationInventors: Jincong Zhuo, Colin Zhang, Meizhong Xu, Ding-Quan Qian, Wenqing Yao, Ravi Kumar Jalluri
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Patent number: 8143237Abstract: Selenopheno triazene analogs, their compositions, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts and mixtures thereof are useful for the treatment of metastatic malignant melanoma and other cancers. The selenopheno triazene analogs have the general formulae (I) or (II): wherein the substituents R1, R2, R3, R6, and R7 are as described in the specification. Other cancers include which may be treated with these compounds include, but are not limited to, malignant melanoma, leukemia, lymphomas (Hodgkins and non-Hodgkins), sarcomas (Ewing's sarcoma), brain tumors, central nervous system (CNS) metastases, gliomas, carcinomas such as breast cancer, prostate cancer, lung cancer (small cell and non-small cell), colon cancer, pancreatic cancer, Head and Neck cancers and oropharyngeal squamous cell carcinoma.Type: GrantFiled: April 26, 2010Date of Patent: March 27, 2012Assignee: Kasina Laila Innova Pharmaceuticals Private LimitedInventors: Ganga Raju Gokaraju, Sudhakar Kasina, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Venkateswarlu Somepalli, Trimurtulu Golakoti, Kiran Bhupathiraju, Sengupta Krishanu, Venkata Krishna Raju Alluri
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Publication number: 20120071478Abstract: The invention provides compounds of the formula (1): or salts or tautomers thereof; wherein X1 is N or N+(O?); X2 is N or CH; Q is a C1-3 alkylene group; R1 is selected from hydrogen, C1-4 hydrocarbyl and hydroxy-C2-4 hydrocarbyl; R2, R3 and R4 are the same or different and each is selected from hydrogen, fluorine, chlorine and methyl; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring and Ar2 is an optionally substituted monocyclic 5 or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S. The compounds of formula (1) are inhibitors of p70S6 kinase and are useful in the treatment of proliferative diseases.Type: ApplicationFiled: May 26, 2010Publication date: March 22, 2012Applicant: Sentinel Oncology LimitedInventors: Robert George Boyle, David Winter Walker
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Patent number: 8138336Abstract: 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 22, 2008Date of Patent: March 20, 2012Assignee: Bayer HealthCare LLCInventors: Steven Magnuson, Philip Wickens, Zhonghua Zhang, Ning Qi, Xin Ma
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Patent number: 8138337Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: December 29, 2009Date of Patent: March 20, 2012Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen, Soo Jin Lee
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Patent number: 8133995Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.Type: GrantFiled: November 30, 2006Date of Patent: March 13, 2012Assignee: Bayer HealthCare LLCInventors: Julie Dixon, Steven Magnuson, Barton Phillips, Yamin Wang, Tandy Li, Kyle Parcella, Jason Newcom, Harold Kluender, Zhenqiu Hong, Brent Chandler, Zhonghua Zhang, Kristen Allegue, Zheng Liu
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Publication number: 20120059000Abstract: Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: May 20, 2011Publication date: March 8, 2012Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
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Patent number: 8129379Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: GrantFiled: September 2, 2009Date of Patent: March 6, 2012Assignee: Bayer HealthCare LLCInventors: Julie A. Dixon, Barton Phillips, Furahi Achebe, Harold C. E. Kluender, Jason Newcom, Kyle Parcella, Steven Magnuson, Zhenqiu Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler, Stephen O'Connor
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Patent number: 8124759Abstract: Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: GrantFiled: May 9, 2008Date of Patent: February 28, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Michaelides, Zhiqin Ji
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Publication number: 20120035050Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.Type: ApplicationFiled: March 25, 2009Publication date: February 9, 2012Applicant: BAYER CROPSCIENCE AGInventors: Peter Jeschke, Robert Velten, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20120035178Abstract: 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: October 10, 2011Publication date: February 9, 2012Inventors: James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor
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Publication number: 20120035177Abstract: A tablet formulation is provided which includes a medicament which is a pharmaceutically acceptable salt of a p38 inhibitor, such as the p38 HCl salt of the structure Formula (I) and which has good physical stability when stored at up to 25 C./60% RH in closed containers with desiccant. The tablet formulation will contain crospovidone as a tablet disintegrant, which, unlike croscarmellose sodium, will not cause disproportionation of the HCl salt to the free base of P38 inhibitor and thus will have acceptable dissolution properties even after storage at room temperature.Type: ApplicationFiled: April 15, 2010Publication date: February 9, 2012Applicant: Bristol-Myers Squibb CompanyInventors: Manisha M. Dali, Charles E. Dahlheim, Vijay H. Naringrekar, Gary McGeorge
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Patent number: 8106049Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility as diagnostic and therapeutic agents for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. In one embodiment, these reverse-term mimetics have a general structure of formula (VI): wherein Ra, Rb, Rc, X1, X2 and X3 are defined as provided herein.Type: GrantFiled: September 3, 2009Date of Patent: January 31, 2012Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Publication number: 20120022046Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: February 24, 2010Publication date: January 26, 2012Inventors: Chelsea M. Byrd, Dongcheng Dai, Robert Jordan, Dennis E. Hruby
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Publication number: 20120022071Abstract: The invention provides a method of treating comorbid premature ejaculation and erectile dysfunction. In particular, the method comprises administering an effective amount of a tramadol material and an effective amount of a phosphodiesterase inhibitor. The invention also provides a pharmaceutical composition comprising a pharmaceutically-acceptable carrier, a tramadol material and a phosphodiesterase inhibitor. The invention further provides a kit comprising a tramadol material and a phosphodiesterase inhibitor.Type: ApplicationFiled: September 28, 2011Publication date: January 26, 2012Inventors: James V. Winkler, Kevin Bilyard, David Bar-Or
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Publication number: 20120018333Abstract: The invention provides methods of reducing the side effects of tramadol. Accordingly, in one embodiment, the invention provides a method of reducing the incidence of newly-discovered side effects related to sexual function in human males taking a tramadol material. The method comprises administering a phosphodiesterase inhibitor to a male taking the tramadol material. The invention also provides pharmaceutical compositions. In one embodiment, the composition comprises a tramadol material and a phosphodiesterase inhibitor. The invention further provides kits. In one embodiment, the kit comprises a tramadol material and a phosphodiesterase inhibitor.Type: ApplicationFiled: September 28, 2011Publication date: January 26, 2012Inventors: David Bar-Or, Kevin Bilyard, James V. Winkler
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Publication number: 20120022028Abstract: 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 male erectile dysfunction (MED) in particular for the MED treatment of difficult to treat patients and patients not or not fully responding to PDE5 inhibitors.Type: ApplicationFiled: January 7, 2010Publication date: January 26, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Peter Sandner, Johannes-Peter Stasch, Michael-Friedrich Böttcher
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Patent number: 8101751Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: August 14, 2009Date of Patent: January 24, 2012Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Publication number: 20120015949Abstract: A method of decreasing renal ischemic damage comprising a) identifying an organism having a kidney that is susceptible to renal ischemic damage from an ischemic event; and b) administering to the organism one or more than one effective dose of an agent prior to the ischemic event; where administering to the organism the one or more than one effective dose of the agent serves to at least partially protect the organism's kidney from damage during a subsequent ischemic event. A composition for decreasing renal ischemic damage comprising one or more than one phosphodiesterase inhibitor, and one or more than one HMG-CoA reductase inhibitor.Type: ApplicationFiled: August 4, 2011Publication date: January 19, 2012Applicant: LOMA LINDA UNIVERSITYInventor: Dalton D. Baldwin
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Publication number: 20120015910Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: Bayer CropScience AGInventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
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Publication number: 20120010073Abstract: The present invention relates to novel active compound combinations which include of the insecticidally active compounds of the formula (I) in combination with fungicidally active compounds (II) and are highly suitable for controlling unwanted animal pests, such as insects, and unwanted phytopathogenic fungi.Type: ApplicationFiled: July 7, 2011Publication date: January 12, 2012Applicant: BAYER CROPSCIENCE AGInventors: Christian FUNKE, Heike HUNGENBERG, Rüdiger FISCHER
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Publication number: 20120004233Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: January 26, 2010Publication date: January 5, 2012Applicant: AMIRA PHARMACEUTICALS, INCInventors: Brian Andrew Stearns, Ryan Clark
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Patent number: 8080657Abstract: Conformationally constrained compounds that are novel and mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins and having bicyclic framework are disclosed, as well as their prodrugs. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. The invention also relates to a use of such compounds for the preparation of a medicament for treating or preventing cancer including an acute myeloid leukemia.Type: GrantFiled: October 15, 2008Date of Patent: December 20, 2011Assignee: Choongwae Pharma CorporationInventors: Jae Uk Chung, Kyung-Yun Jung, Min-Wook Jeong, Hee-Kyung Jung, Hyun-Ju La
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Patent number: 8076335Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.Type: GrantFiled: July 21, 2010Date of Patent: December 13, 2011Assignee: Schering Corp.Inventors: Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Lenore C. Witchey-Lakshmanan
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Patent number: 8071764Abstract: Conformationally constrained compounds that are novel and mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins and having bicyclic frame-work are disclosed, as well as their prodrugs. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. The invention also relates to the use of such compounds for the preparation of a medicament for treating or preventing cancer including an acute myeloid leukemia.Type: GrantFiled: October 15, 2008Date of Patent: December 6, 2011Assignee: Choongwae Pharma CorporationInventors: Jae Uk Chung, Kyung-Yun Jung, Sang-Hwi Lee, Myoung-Joo Kang
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Patent number: 8071581Abstract: The present disclosure relates to triazolopyridazine protein kinase modulators of Formula (I), methods of using these compounds to treat diseases mediated by kinase activity.Type: GrantFiled: October 18, 2007Date of Patent: December 6, 2011Assignee: SGX Pharmaceuticals, Inc.Inventors: Christopher Ronald Smith, Pierre-Yves Bounaud, Elizabeth Anne Jefferson, Patrick S. Lee, Eduardo Torres
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Publication number: 20110294815Abstract: This invention relates to novel prostacyclin analogs and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel prostacyclin analogs that are derivatives of treprostinil. This invention also provides compositions comprising a compound of this invention and a carrier and the use disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering analogues of prostacyclin, such as treprostinil.Type: ApplicationFiled: June 26, 2009Publication date: December 1, 2011Inventor: Scott L. Harbeson
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Publication number: 20110294816Abstract: 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: ApplicationFiled: October 8, 2009Publication date: December 1, 2011Inventors: Ashok Vinayak Purandare, David B. Frennesson, Muthoni G. Kamau, Lalgudi S. Harikrishnan, Mark G. Saulnier
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Publication number: 20110294797Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: July 29, 2011Publication date: December 1, 2011Applicant: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Publication number: 20110294776Abstract: 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: ApplicationFiled: November 2, 2006Publication date: December 1, 2011Applicant: BAYER HEALTHCARE AGInventors: 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: 20110294796Abstract: 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: ApplicationFiled: December 28, 2010Publication date: December 1, 2011Applicant: TargeGen, Inc.Inventors: Xianchang Gong, Kathy Barrett, Jianguo Cao, Colleen Gritzen, John D. Hood, Chi Ching Mak, Andrew McPherson, Ved Prakash Pathak, Joel Renick, Richard M. Soll, Ute Splittgerber, Wolfgang Wrasidlo, Ningning Zhao, Elena Dneprovskaia, Binqi Zeng, Glenn Noronha
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Patent number: 8063208Abstract: Crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol of the formula are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol, as well as a method of using one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol in the treatment of cancer and other proliferative diseases.Type: GrantFiled: February 15, 2007Date of Patent: November 22, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Chenkou Wei, Derek J. Norris
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Publication number: 20110269740Abstract: Provided herein are pyrrolotriazine compounds for treatment of JAK kinase, including JAK2 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: July 2, 2009Publication date: November 3, 2011Inventors: Sunny Abraham, Qi Chao, Michael Hadd, Mark Holladay, Gang Liu, Mitchell Nambu, Eduardo Setti
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Patent number: 8048882Abstract: The invention relates to novel pharmaceutical combinations with improved sodium channel blocking effect. Further, the invention relates to the use of said pharmaceutical combinations in chronic pain, in disturbances of the motor system, in epilepsy, as well as in other therapeutic fields where the use of sodium channel blockers is acceptable.Type: GrantFiled: December 18, 2004Date of Patent: November 1, 2011Inventors: Pal Kocsis, Istvan Tarnawa, Marta Than, Karoly Tihanyi, Gyorgy Nemeth
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Patent number: 8049008Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: April 7, 2010Date of Patent: November 1, 2011Assignee: Choongwae Pharma CorporationInventors: Jae Uk Chung, Masakatsu Eguchi
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Publication number: 20110263605Abstract: The disclosure provides compounds of formula I, including Ia, Ib, Ic, or Id, 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: October 19, 2010Publication date: October 27, 2011Inventors: Ivar M. McDonald, Robert A. Mate, James H. Cook, II, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, Matthew D. Hill, Haiquan Fang, John E. Macor
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Publication number: 20110257185Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: June 29, 2011Publication date: October 20, 2011Applicant: CHOONGWAE PHARMA CORPORATIONInventors: SUNG HWAN MOON, JAE UK CHUNG, SUNG CHAN LEE, MASAKATSU EGUCHI, MICHAEL KAHN, KWANG WON JEONG, CU NGUYEN
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Publication number: 20110257167Abstract: 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 a LKB1 and/or AMPK gene or protein loss or mutation.Type: ApplicationFiled: February 3, 2011Publication date: October 20, 2011Inventors: Rajesh Chopra, Yuhong Ning, Sabita Sankar, Shuichan Xu, Weiming Xu
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Publication number: 20110257184Abstract: A method of treating SHP-2 phosphatase associated diseases in a subject includes administering a SHP-2 inhibitor to the subject.Type: ApplicationFiled: November 15, 2010Publication date: October 20, 2011Inventors: Cheng-Kui Qu, Wen-Mei Yu, Olgun Guvench, Alexander D. Mackerell, JR.