Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 540/521)
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Publication number: 20110118231Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: ApplicationFiled: November 19, 2010Publication date: May 19, 2011Applicants: ABBOTT LABORATORIES, ABBOTT GMBH & CO. KGInventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
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Publication number: 20110086834Abstract: Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.Type: ApplicationFiled: June 26, 2009Publication date: April 14, 2011Applicant: AMGEN INC.Inventors: Guoqing Chen, Timothy D. Cushing, Paul Faulder, Benjamin Fisher, Xiao He, Kexue Li, Zhihong Li, Wen Liu, Lawrence R. Mcgee, Vatee Pattaropong, Jennifer L. Seganish, Youngshook Shin, Zhulun Wang
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Publication number: 20110053910Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: July 3, 2006Publication date: March 3, 2011Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Patent number: 7897595Abstract: The present invention relates to pyridoazepine derivatives that act as 5-HT ligands, e.g., 5-HT2 C. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: GrantFiled: May 23, 2007Date of Patent: March 1, 2011Assignee: Forest Laboratories Holdings LimitedInventors: Gian-Luca Araldi, Alexander Bischoff, Nhut K. Diep
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Patent number: 7888344Abstract: A series of 5,6-dihydro-1,3-benzothiazol-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PD 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: GrantFiled: April 25, 2006Date of Patent: February 15, 2011Assignee: UCB Pharma S.A.Inventors: Rikki Peter Alexander, Pavandeep Aujla, Mark James Batchelor, Daniel Christopher Brookings, George Martin Buckley, Karen Viviane Lucile Crepy, Claire Louise Kulisa, James Petrie Turner
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Publication number: 20110034438Abstract: The invention relates to compounds of general formula (I), which can be used particularly as structural mimetics of proline-rich peptides and are therefore capable of binding PRM binding domains (proline-rich motif binding domains) of proteins. The invention also relates to the use of said compounds as pharmaceutical active agents and the use of these pharmaceutical active agents for treating bacterial diseases, neurodegenerative diseases and tumours.Type: ApplicationFiled: September 25, 2007Publication date: February 10, 2011Applicant: FORSCHUNGSVERBUND BERLIN E.V.Inventors: Ronald Kuehne, Hartmut Oschkinat, Christoph Brockmann, Hans-Guenther Schmalz
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Publication number: 20110028450Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: July 27, 2010Publication date: February 3, 2011Applicant: N.V. OrganonInventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
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Publication number: 20110003793Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: January 6, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. Guzzo, Matthew David Surman, James Francis Grabowski, JR., Emily Elizabeth Freeman
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Publication number: 20100324022Abstract: Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same.Type: ApplicationFiled: August 4, 2010Publication date: December 23, 2010Applicant: GLAXO GROUP LIMITEDInventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Publication number: 20100305066Abstract: A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 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: June 4, 2007Publication date: December 2, 2010Applicant: UCB PHARMA S.A.Inventors: Rikki Peter Alexander, Stuart Bailey, Stephen Brand, Daniel Christopher Brookings, Julien Alistair Brown, Alan Findlay Haughan, Natasha Kinsella, Christopher Lowe, Stephen Robert Mack, William Ross Pitt, Marianna Dilani Richard, Andrew Sharpe, Laura Jane Tait
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Publication number: 20100298292Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: ApplicationFiled: May 21, 2010Publication date: November 25, 2010Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
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Patent number: 7838517Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: May 15, 2009Date of Patent: November 23, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
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Publication number: 20100280004Abstract: This invention provides compounds of Formula I. The compounds are correctors of ?F508 CFTR trafficking. Also provided are uses of compounds of Formula I for treatment, as well as methods of treatment, of cystic fibrosis.Type: ApplicationFiled: July 3, 2008Publication date: November 4, 2010Inventors: Raymond Andersen, Robert Keyzers, Christopher Anthony Gray, David Y. Thomas, John W. Hanrahan, Graeme W. Carlile
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Publication number: 20100273724Abstract: This invention is directed to PEGlyated derivatives, drug conjugates and isotopic derivatives of certain ion channel modulating compounds.Type: ApplicationFiled: July 7, 2010Publication date: October 28, 2010Applicant: CARDIOME PHARMA CORP.Inventors: Elizabeth L. S. Cheu, Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Alan M. Ezrin, Grace Jung, Bertrand M.C. Plouvier, Aregahegn S. Yifru
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Publication number: 20100267692Abstract: The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.Type: ApplicationFiled: November 5, 2008Publication date: October 21, 2010Inventors: Carlo Scolastico, Leonardo Pierpaolo Manzoni, Pierfausto Seneci, Laura Belvisi, Domenico Delia, Martino Bolognesi, Eloise Mastrangelo, Mario Milani, Ilaria Motto, Carmelo Drago
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Publication number: 20100256115Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: ApplicationFiled: March 18, 2010Publication date: October 7, 2010Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20100249102Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: ApplicationFiled: April 6, 2010Publication date: September 30, 2010Applicant: ALANTOS PHARMACEUTICALS HOLDINGS, INC.Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgürtel, Hongbo Deng, Brian M. Gallagher, JR., Irving Sucholeiki, Arthur Taveras
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Publication number: 20100234588Abstract: Methods are provided for preparing compounds of the general formula (I) wherein X1 is an aryl hydrocarbon group optionally substituted with one or more groups independently selected from —R, —NH2, —NHR, —NR2, —OH, —OR, —F, —Cl, —Br, —I, —CF3, —C(?O)OH, —C(?O)OR, —C(?O)NH2, —C(?O)NHR, and —C(?O)NR2; X2 is —H, —R, —NHR, —NR2, —OR, —F, —Cl, —Br, or —I; and R is C1 to C10 hydrocarbyl. The methods comprise a double-dehydrogenation reaction step in which a functionalized aminohydroazepinone skeleton comprising an aminoimidazole ring is reacted with 2-iodoxybenzene to form the imidazo[4,5-d]azepine ring system present in formula (I). Example methods comprising the double-dehydrogenation reaction step are provided as efficient synthetic routes to ceratamine A, ceratamine B, and the des-methyl analogs thereof.Type: ApplicationFiled: March 11, 2010Publication date: September 16, 2010Applicant: THE OHIO STATE UNIVERSITYInventors: Robert S. Coleman, Erica L. Campbell, Daniel J. Carper
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Publication number: 20100222320Abstract: Compounds of formula I: Selectively attenuate production of A?(1-42) and hence find use in treatment or prevention of diseases associated with deposition of A? in the brain, in particular Alzheimer's disease.Type: ApplicationFiled: June 9, 2008Publication date: September 2, 2010Inventors: Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
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Patent number: 7786119Abstract: This invention is directed to drug conjugates of certain ion channel modulating compounds having the following formula: wherein A, X, R1, R2, R3, R4, R5, LB, L and DM are defined herein, including isolated enantiomeric and diastereomeric isomers thereof, and mixtures thereof. Pharmaceutical compositions and methods of use are also disclosed.Type: GrantFiled: March 31, 2005Date of Patent: August 31, 2010Assignee: Cardiome Pharma Corp.Inventors: Elizabeth L. S. Cheu, Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Alan M. Ezrin, Grace Jung, Bertrand M. C. Plouvier, Aregahegn S. Yifru
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Publication number: 20100190773Abstract: Heterocyclic compounds and analogues thereof and their use as inhibitors of Mitogen-Activated Protein Kinase-Activated Protein kinase-2 (MAPKAP-k2), and also to a method for preventing or treating a disease or disorder that can be treated or prevented by modulating the activity of MAPKAP-K2 in a subject and to pharmaceutical compositions and kits that include these MAPKAP-K2 inhibitors.Type: ApplicationFiled: March 19, 2010Publication date: July 29, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha ABEYWARDANE, Craig Andrew MILLER, Tina Marie MORWICK, Neil MOSS, Matthew Russell NETHERTON, Roger John SNOW, Ji WANG, Jiang-Ping WU, Zhaoming XIONG
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Publication number: 20100179126Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: December 4, 2009Publication date: July 15, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Indu T. Bharathan, Matthew Duffey, Amy Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
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Publication number: 20100143499Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.Type: ApplicationFiled: July 24, 2007Publication date: June 10, 2010Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventor: Stephen M. Condon
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Publication number: 20100137283Abstract: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIV”) integrase enzyme.Type: ApplicationFiled: February 1, 2010Publication date: June 3, 2010Inventors: Klaus Ruprecht Dress, Qiyue Hu, Ted William Johnson, Michael Bruno Plewe, Steven Paul Tanis, Huichun Zhu, Junhu Zhang
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Patent number: 7713958Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3?, Bcr-abl, Flt-3, c-Kit, PDGFR?, Src, Mek1 and CK1.Type: GrantFiled: August 6, 2008Date of Patent: May 11, 2010Assignee: IRM LLCInventors: Yongqin Wan, Nathanael S. Gray
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Publication number: 20100075952Abstract: The invention provides new pyrrolo-nitrogenous heterocyclic derivatives represented by formula (I) or their salts, the preparation thereof, pharmaceutical compositions containing such derivatives and the use of such derivatives as therapeutic agents, especially as protein kinase inhibitors, wherein each substituent in formula (I) is same as defined in the description.Type: ApplicationFiled: May 14, 2008Publication date: March 25, 2010Inventors: Peng Cho ChoTang, Yidong Su, Yali Li, Lei Zhang, Fuqiang Zhao, Jialiang Yang, Ying Zhou, Pingyan Bie, Guangtao Qian, Minggang Ju
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Publication number: 20100069360Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1, R2, R3, R7 and X are as defined in the specification.Type: ApplicationFiled: August 28, 2007Publication date: March 18, 2010Inventors: Laszlo Revesz, Achim Schlapbach, Rudolf Walchli
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Publication number: 20090298809Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: May 28, 2009Publication date: December 3, 2009Applicant: Albany Molecular Research, Inc.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Publication number: 20090291941Abstract: The present invention relates to pyrido[3,2-c]benzazocinone derivatives and related compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: October 18, 2006Publication date: November 26, 2009Inventors: Christopher J. Dinsmore, Jongwon Lim, Alan B. Northrup
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Publication number: 20090281082Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: May 15, 2009Publication date: November 12, 2009Applicant: Vertex Pharmaceuticals IncorporatedInventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
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Publication number: 20090264411Abstract: A series of 4,5,6,7-tetrahydrothieno[2,3-c]azepin-8-one derivatives, and analogues thereof, which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.Type: ApplicationFiled: February 13, 2009Publication date: October 22, 2009Applicant: UCB Pharma S.A.Inventors: Victoria Elizabeth Laing, Daniel Christopher Brookings, Rachel Jane Carbery, Jose Miguel Gascon Simorte, Martin Clive Hutchings, Barry John Langham, Martin Alexander Lowe
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Publication number: 20090258856Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
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Publication number: 20090221614Abstract: Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.Type: ApplicationFiled: September 26, 2006Publication date: September 3, 2009Applicant: The Regents of the University of CaliforniaInventors: Jack Taunton, Michael Cohen, Kevin Shokat, Chao Zhang
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Patent number: 7553833Abstract: There are provided compounds of the general formulas wherein X, Y, R1, R2, R3, R4 and R5 are as described herein. The compounds exhibit anticancer activity.Type: GrantFiled: April 11, 2008Date of Patent: June 30, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Jin-Jun Liu, Jefferson Wright Tilley, Zhuming Zhang
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Publication number: 20090156578Abstract: In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.Type: ApplicationFiled: December 1, 2006Publication date: June 18, 2009Inventors: Henry Pauls, Judd M. Berman
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Publication number: 20090137555Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3?, Bcr-abl, Flt-3, c-Kit, PDGFR?, Src, Mek1 and CK1.Type: ApplicationFiled: August 6, 2008Publication date: May 28, 2009Applicant: IRM LLCInventors: Yongqin Wan, Nathanael S. Gray
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Publication number: 20090124597Abstract: Described herein are compounds that have a spiro structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of steroid hormone nuclear receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent diseases or conditions associated with the activity of steroid hormone nuclear receptors.Type: ApplicationFiled: February 16, 2006Publication date: May 14, 2009Inventors: Pierre-Yves Michellys, Chi Ching Mak, Wei Pei
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Publication number: 20090029939Abstract: Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl, Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.Type: ApplicationFiled: May 25, 2007Publication date: January 29, 2009Inventors: James M. Chen, Xiaowu Chen, Maria Fardis, Haolun Jin, Choung U. Kim, Laura N. Schacherer
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Publication number: 20090012058Abstract: The present invention provides a pharmaceutical composition for use in the prophylaxis or treatment of allergic ophthalmic diseases or allergic nasal diseases, which comprises 7,8-dimethoxy-4(5H),10-dioxo-1H-1,2,3-triazolo[4,5-c][1]benzazepine, 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine or a pharmaceutically acceptable salt thereof. The pharmaceutical composition according to the present invention has few side effects, exerts strong prophylactic and therapeutic effects in the late phase exhibiting pharmaceutical resistance to conventional instillations, and can be used appropriately for topical applications.Type: ApplicationFiled: March 2, 2007Publication date: January 8, 2009Inventors: Takashi Shishikura, Tsuneyoshi Inaba, Yukari Hoshina, Hirotomo Akabane, Mitsuhiro Uchida
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Publication number: 20090005359Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: ApplicationFiled: June 30, 2008Publication date: January 1, 2009Applicant: Sunesis Pharmaceuticals, IncInventors: Jennifer Cossrow, Bing Guan, Alexey Ishchenko, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
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Patent number: 7470680Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: May 1, 2007Date of Patent: December 30, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang, Xiaojun Han, Guanglin Luo, Gene M. Dubowchik, Graham S. Poindexter
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Patent number: 7470679Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: May 1, 2007Date of Patent: December 30, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Stephen E. Mercer, Prasad V. Chaturvedula
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Publication number: 20080312211Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described: formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: December 19, 2006Publication date: December 18, 2008Applicant: ASTRAZENECA ABInventors: Gregory Basarab, Haihong Ni, Brian Sherer, Fei Zhou
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Publication number: 20080306257Abstract: The present invention relates to a process for preparing racemic narwedine (which can be can be kinetically resolved) to yield (?)-narwedine and which is the biogenic precursor of (?)-galanthamine) and the use thereof as a starting material for producing (?)-galanthamine. The invention further includes processes for preparing (?)-galanthamine and (?)-galanthamine hydrobromide, as well as related novel compounds.Type: ApplicationFiled: May 3, 2006Publication date: December 11, 2008Applicant: MEDICHEM, S.A.Inventors: Gabriel Tojo Suarez, Ernesto Duran Lopez, Jordi Bosch I Llado
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Patent number: 7459448Abstract: The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: October 3, 2005Date of Patent: December 2, 2008Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Christopher F. Claiborne, Courtney A. Cullis, Natalie A. Dales, Michael Patane, Matthew Stirling, Omar Stradella, Gabriel S. Weatherhead
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Publication number: 20080287420Abstract: The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.Type: ApplicationFiled: March 7, 2008Publication date: November 20, 2008Applicant: Infinity Discovery, Inc.Inventors: Alfredo Castro, Michael J. Grogan, Andre Lescarbeau, Martin Tremblay
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Publication number: 20080287421Abstract: There are provided compounds of the general formulas wherein X, Y, R1, R2, R3, R4 and R5 are as described herein. The compounds exhibit anticancer activity.Type: ApplicationFiled: April 11, 2008Publication date: November 20, 2008Inventors: Jin-Jun Liu, Jefferson Wright Tilley, Zhuming Zhang
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Publication number: 20080287423Abstract: This invention relates to the use of azapaullones, particularly in combination with immunomodulating agents, in the prevention, and/or treatment of pancreatic autoimmune disorders, e.g. type I diabetes or LADA and neurodegenerative disorders.Type: ApplicationFiled: May 4, 2006Publication date: November 20, 2008Inventors: Rainer Mussmann, Conrad Peter Kunick, Hendrik Stukenbrock, Marcus Geese, Simone Kegel, Ulrike Burk
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Publication number: 20080287422Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: ApplicationFiled: April 18, 2008Publication date: November 20, 2008Inventors: Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang
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Publication number: 20080242658Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula IType: ApplicationFiled: April 6, 2005Publication date: October 2, 2008Inventors: Mark G Palermo, Sushil Kumar Sharma, Christopher Straub, Run-Ming Wang, Leigh Zawel, Yanlin Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He