The Chalcogen And The Nitrogen Are In The 1,5-positions Of The Bicyclo Ring System (e.g., 1,5-benzothiazepinone, Etc.) Patents (Class 540/491)
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Patent number: 11578078Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The compounds may have a structure according to Formula I The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.Type: GrantFiled: November 6, 2020Date of Patent: February 14, 2023Assignee: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Jiaxin Yu, Simon Shaw, Ihab Darwish, Vanessa Taylor, Somasekhar Bhamidipati, Zhushou Luo, Rao Kolluri
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Publication number: 20150038488Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.Type: ApplicationFiled: July 31, 2014Publication date: February 5, 2015Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
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Publication number: 20150038489Abstract: Described herein is a method of treating long QT syndrome by administration of an effective amount of a potent and selective late sodium ion channel blockerType: ApplicationFiled: July 31, 2014Publication date: February 5, 2015Applicant: Gilead Sciences, Inc.Inventors: Luiz Belardinelli, Sridharan Rajamani, Dewan Zeng
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Patent number: 8895545Abstract: In part, the present invention is directed to antibacterial compounds.Type: GrantFiled: October 4, 2012Date of Patent: November 25, 2014Assignee: Debiopharm International SAInventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
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Publication number: 20140343277Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.Type: ApplicationFiled: June 25, 2014Publication date: November 20, 2014Inventors: Shinichi TAIRA, Kunio OSHIMA, Takashi OSHIYAMA, Yasuhiro MENJO, Yasuo KOGA, Hokuto YAMABE, Sunao NAKAYAMA, Kenji TSUJIMAE, Toshiyuki ONOGAWA, Kuninori TAI, Motohiro ITOTANI
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Patent number: 8685960Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).Type: GrantFiled: May 5, 2009Date of Patent: April 1, 2014Assignee: Elexopharm GmbHInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20140031334Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: September 20, 2013Publication date: January 30, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
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Patent number: 8609648Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 15, 2010Date of Patent: December 17, 2013Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
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Publication number: 20130261101Abstract: The present invention provides bicyclic azaheterocyclobenzylamines of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.Type: ApplicationFiled: April 1, 2013Publication date: October 3, 2013Inventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr.
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Patent number: 8541404Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: GrantFiled: November 3, 2010Date of Patent: September 24, 2013Assignee: ElexoPharm GmbHInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20130237523Abstract: In part, the present invention is directed to antibacterial compounds.Type: ApplicationFiled: October 4, 2012Publication date: September 12, 2013Applicant: AFFINIUM PHARMACEUTICALS, INC.Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
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Patent number: 8501727Abstract: The present invention relates to short-acting calcium channel blocking compounds and their use to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension in general, hypertension been.) fore, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.Type: GrantFiled: August 20, 2009Date of Patent: August 6, 2013Assignee: Milestone Pharmaceuticals Inc.Inventors: Martin P. Maguire, Dominik Herbart, Harry J. Leighton
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Publication number: 20130172215Abstract: This disclosure concerns methods for producing a spinosyn producing strain that comprises modifying a nucleic acid molecule encoding for spinactin by introducing, mutating, deleting, replacing or inactivating a nucleic acid sequence encoding one or more activities encoded by said nucleic acid molecule. Methods for producing a modified Saccharopolyspora spinosa organism are also disclosed.Type: ApplicationFiled: December 13, 2012Publication date: July 4, 2013Applicant: DOW AGROSCIENCES LLCInventor: DOW AGROSCIENCES LLC
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Publication number: 20120328599Abstract: The present invention provides moieties that bind to the asymmetric contact interface of a receptor tyrosine kinase (RTK), wherein the moieties inhibit ligand induced trans autophosphorylation of the RTK. The present invention also provides methods of treating or preventing an RTK-associated disease and methods for identifying moieties that bind to an asymmetric contact interface of an RTK.Type: ApplicationFiled: January 13, 2011Publication date: December 27, 2012Applicant: YALE UNIVERSITYInventors: Jae Hyun Bae, Irit Lax, Joseph Schlessinger
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Patent number: 8318720Abstract: In part, the present invention is directed to antibacterial compounds.Type: GrantFiled: July 19, 2007Date of Patent: November 27, 2012Assignee: Affinium Pharmaceuticals, Inc.Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
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Publication number: 20120028920Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Inventors: Hiroshi YAMASHITA, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Patent number: 7994161Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.Type: GrantFiled: November 10, 2008Date of Patent: August 9, 2011Assignee: Sanofi-AventisInventors: Jidong Zhang, Yannick Benedetti, Alain Commerçon
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Publication number: 20110144087Abstract: The present invention relates to short-acting calcium channel blocking compounds and their use to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension in general, hypertension been.) fore, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.Type: ApplicationFiled: August 20, 2009Publication date: June 16, 2011Applicant: Milestone Pharmaceuticals Inc.Inventors: Martin P. Maguire, Dominik Herbart, Harry J. Leighton
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Publication number: 20110136788Abstract: [Problem] The present invention aims to provide an agent for the prophylaxis or treatment of irritable bowel syndrome. [Solving Means] An agent for the prophylaxis or treatment of irritable bowel syndrome, containing a compound having a TGR5 receptor agonist activity, a fused ring compound represented by the formula wherein ring A is an optionally substituted aromatic ring, and ring B? is a 5- to 9-membered ring having one or more substituents, or a salt thereof as an active ingredient.Type: ApplicationFiled: August 6, 2009Publication date: June 9, 2011Inventor: Minoru Maruyama
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Publication number: 20110118232Abstract: The invention relates to novel pyrimidine compounds of general formula (I), in which: A represents a group C?W or CRfRg; B represents a chemical bond or a group CRhRi; X represents O, S, a group N—Rk or a group CRmRn; D represents C?O or a chemical bond; E represents a linear or branched 2- to 10-membered alkylene chain that, as members of a chain, can have 1 or 2 non-adjacent heteroatom group(s) K, which is selected among O, S, S(O), S(O)2 and N—Rp and which can comprise a carbonyl group and/or a cycloalkanediyl group and/or a double or triple bond; W represents oxygen or sulfur; Z, together with the carbon atoms, to which it is bound, represents a condensed, optionally substituted 5-, 6- or 7-membered carbocyclic compound or heterocyclic compound that has 1, 2, 3 or 4 heteroatoms, which are selected among N, O and S; J represents CH2, CH2—CH2 or CH2—CH2—CH2; M represents CH or N; Y represents CH2, CH2—CH2 or CH2—CH2—CH2 or M-X, together, represent CH?C or CH2—CH?C; n is 0 or 1, and; Ra, Rb, Rc, Rd, Re, Rf,Type: ApplicationFiled: July 23, 2010Publication date: May 19, 2011Applicant: Abbott GmbH & Co. KGInventors: Hervè Geneste, Andreas Haupt, Wilfried Braje, Wilfried Lubisch, Gerd Steiner
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Publication number: 20110112067Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20110098273Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.Type: ApplicationFiled: September 3, 2008Publication date: April 28, 2011Applicant: Nektar TherapeuticsInventors: Zhongxu Ren, Bo-Liang Deng, Jennifer Riggs-Sauthier, Micah Harvey
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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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Publication number: 20110008288Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 15, 2010Publication date: January 13, 2011Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
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Patent number: 7858776Abstract: Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit ? secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.Type: GrantFiled: January 26, 2009Date of Patent: December 28, 2010Assignee: AstraZeneca ABInventors: Bruce Thomas Dembofsky, Robert Jacobs, Cyrus Ohnmacht
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Patent number: 7842686Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.Type: GrantFiled: January 21, 2009Date of Patent: November 30, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Corey Don Anderson, Andreas P. Termin, Pramod Joshi, Sara S. Hadida Ruah, Daniele Bergeron, Sanghee Yoo, Jingrong Cao
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Patent number: 7829713Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.Type: GrantFiled: February 27, 2007Date of Patent: November 9, 2010Assignee: Helicon Therapeutics, Inc.Inventors: Terrence P. Keenan, Alan P. Kaplan
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Patent number: 7786105Abstract: The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.Type: GrantFiled: June 3, 2005Date of Patent: August 31, 2010Assignee: Abbott GmbH & Co. KGInventors: Herve Geneste, Andreas Haupt, Wilfried Braje, Wilfried Lubisch, Gerd Steiner
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Publication number: 20100203135Abstract: Methods of forming soft connective tissue compositions such as skin equivalents, compositions made by the methods and their uses.Type: ApplicationFiled: March 14, 2006Publication date: August 12, 2010Inventors: Paul Kemp, David Shering, Andrew Shering, Penny Johnson, Damian Marshall
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Publication number: 20100160627Abstract: Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit ? secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.Type: ApplicationFiled: January 26, 2009Publication date: June 24, 2010Applicant: ASTRAZENECA ABInventors: Bruce Thomas Dembofsky, Robert Jacobs, Cyrus Ohnmacht
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Publication number: 20100144715Abstract: The present invention is directed to substituted benzodiazepinones, benzoxazepinones and benzothiazepinones compounds that are sodium channel blockers useful for the treatment of chronic and neuropathic pain. The compounds of the present invention are also useful for the treatment of other conditions, including disorders of the CNS such as anxiety, depression, epilepsy, manic depression and bipolar disorder. This invention also provides pharmaceutical compositions comprising a compound of the present invention, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. This invention further comprises methods for the treatment of acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain and disorders of the CNS including, but not limited to, epilepsy, manic depression, depression, anxiety and bipolar disorder comprising administering the compounds and pharmaceutical compositions of the present invention.Type: ApplicationFiled: February 25, 2008Publication date: June 10, 2010Inventors: Scott B. Hoyt, Dong Ok, Hyun Ok, Clare London, Joseph I. Duffy
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Publication number: 20100137282Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials. Z1 and Z2 are independently selected from CH and N.Type: ApplicationFiled: April 16, 2008Publication date: June 3, 2010Inventors: David Evan Davies, David Thomas Davies, Ilaria Giordano, Alan Joseph Hennessy, Neil David Pearson
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Publication number: 20100130470Abstract: In part, the present invention is directed to antibacterial compounds.Type: ApplicationFiled: July 19, 2007Publication date: May 27, 2010Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
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Patent number: 7718646Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogenType: GrantFiled: June 24, 2008Date of Patent: May 18, 2010Assignee: Sanofi-AventisInventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
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Patent number: 7622460Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogenType: GrantFiled: June 24, 2008Date of Patent: November 24, 2009Assignee: sanofi-aventisInventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
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Patent number: 7550453Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.Type: GrantFiled: May 24, 2007Date of Patent: June 23, 2009Assignee: Aventis Pharma SAInventors: Jidong Zhang, Neerja Bhatnagar, Jean-Marie Ruxer
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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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Patent number: 7541131Abstract: The invention provides a resist composition for use in the production process of a semiconductor such as IC, in the production of a circuit substrate of liquid crystal, thermal head and the like or in other photofabrication processes, a compound for use in the resist composition and a pattern forming method using the resist composition, which are a resist composition comprising (A) a sulfonium salt represented by the following formula (I); and a pattern forming method using the resist composition: wherein R1 represents an alkyl group or an aryl group, R2 to R9 each independently represents a hydrogen atom or a substituent and may combine with each other to form a ring, Z represents an electron-withdrawing divalent linking group, Xn? represents an n-valent anion, n represents an integer of 1 to 3, and m represents the number of anions necessary for neutralizing the electric charge.Type: GrantFiled: February 17, 2006Date of Patent: June 2, 2009Assignee: FUJIFILM CorporationInventor: Yasutomo Kawanishi
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Publication number: 20090093457Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: December 10, 2008Publication date: April 9, 2009Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
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Publication number: 20090093459Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzothiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds and to intermediate precursors to such compounds.Type: ApplicationFiled: November 10, 2008Publication date: April 9, 2009Applicant: SANOFI-AVENTISInventors: Jidong ZHANG, Yannick BENEDETTI, Frederico NARDI, Alain COMMERCON
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Publication number: 20090075971Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.Type: ApplicationFiled: November 10, 2008Publication date: March 19, 2009Applicant: SANOFI-AVENTISInventors: Jidong Zhang, Yannick Benedetti, Alain Commercon
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Publication number: 20090042858Abstract: The present invention discloses novel methods and compositions for viral inhibition, particularly inhibition of HCV and SARS. The invention also provides compositions including novel oxoazepanylacetamide derivatives useful for viral inhibition.Type: ApplicationFiled: June 16, 2006Publication date: February 12, 2009Inventors: Paul Barsanti, Nathan Brammier, Bryan Chang, Zhi-Jie Ni, Weibo Wang, Amy Weiner
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Publication number: 20080311609Abstract: The present invention relates to novel molecular probes having the formula (I) (I) useful for the characterization, detection, localization and isolation of the ?-secretase enzyme.Type: ApplicationFiled: December 14, 2005Publication date: December 18, 2008Applicant: ASTRAZENECA ABInventors: Barry Greenberg, Daniel C. Hill, Robert Jacobs, Sangram S. Sisodia
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Publication number: 20080261949Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen aType: ApplicationFiled: June 24, 2008Publication date: October 23, 2008Applicant: SANOFI-AVENTISInventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
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Patent number: 7425550Abstract: A compound of formula I is provided having the structure wherein W is as defined herein; X is —CHR5O—; Y is a bond; Z is an aryl or heteroaryl group; and R1, and R2, are as described herein. Further provided is a method for treating diabetes and related diseases employing the above compound, either alone or in combination with another therapeutic agent.Type: GrantFiled: February 13, 2006Date of Patent: September 16, 2008Assignee: Bristol-Meyers Squibb CompanyInventors: Philip Sher, Gang Wu, Terry Stouch, Bruce Ellsworth
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Patent number: 7361648Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: August 22, 2006Date of Patent: April 22, 2008Assignee: Roche Palo Alto LLCInventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
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Patent number: 7354914Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: November 29, 2004Date of Patent: April 8, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard E. Olson
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Patent number: 7294622Abstract: Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit ? secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.Type: GrantFiled: October 2, 2003Date of Patent: November 13, 2007Assignee: Astrazeneca ABInventors: Christopher Becker, Bruce Dembofsky, Robert Jacobs, James Kang, Cyrus Ohnmacht, James Rosamond, Ashokkumar Bhikkappa Shenvi, Thomas Simpson, James Woods
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Patent number: 7211573Abstract: The invention relates to compounds of the formula I wherein R, R1, R2, R3, X, and n are defined in the specification. The invention also provides pharmaceutically suitable acid addition salts thereof and all forms of optically pure enantiomers, recemates or diastereomers and diastereomeric mixtures thereof. Compounds of the invention are useful for the treatment of Alzheimer's disease.Type: GrantFiled: November 30, 2005Date of Patent: May 1, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl