2-position Substituent Contains Nitrogen, Other Than As Nitro Or Nitroso Patents (Class 548/238)
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Publication number: 20150119377Abstract: This invention recites substituted azetidine derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in animals. The substituents A, B, R1a, R1b, R1c, R2, R3, R4, R6, and n are as described herein.Type: ApplicationFiled: May 6, 2013Publication date: April 30, 2015Inventors: Susan M. K. Sheehan, Valerie A. Vaillancourt
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Patent number: 8969585Abstract: Provided is a process for producing an optically active compound represented by Formula (3): (wherein R1 is an alkyl group, an alkynyl group, an alkenyl group, an aliphatic heterocyclic group, a cycloalkyl group, an aryl group, an aralkyl group, or an aromatic heterocyclic group, and any hydrogen atom of R1 may be replaced with a substituent; R2 is a hydrogen atom or a group which is not reactive in the reaction below; and * represents a chiral center) or a salt thereof by subjecting a compound represented by Formula (1): (wherein R1 and R2 have the same meanings as defined in Formula (3)) to a ring closure reaction in the presence of a chiral ligand having 1 or more coordination sites, a Lewis acid represented by Formula (2): MmZn??(2) (wherein M is a metal ion, Z is a counter anion of M, and m and n are integers of 1 to 4), and a sulfonyl halide having an optionally substituted alkyl or phenyl group.Type: GrantFiled: January 31, 2012Date of Patent: March 3, 2015Assignee: Nagasaki UniversityInventors: Osamu Onomura, Yutaro Tsuda, Masami Kuriyama, Toshiharu Yanagi, Kazuya Kodama
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Patent number: 8946426Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: GrantFiled: February 2, 2010Date of Patent: February 3, 2015Assignees: Janssen Pharmaceuticals, Inc., Cellzome LimitedInventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
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Patent number: 8846944Abstract: The present invention provides a method for regeneration of chiral 2,2?-cyclopropylidene-bis(oxazolines), such as (3&R,3?aR,8aS,8?aS)-2,2?-cyclopropylidenebis-[3a,8a]-dihydro-8H-indeno-[1,2-d]-oxazole and (45,4?5,5R,5?R)-2,2?-cyclopropylidenebis-4,5-diphenyldihydro-4,5-oxazole, used as a part of complex catalysts for e.g. stereoselective addition reactions, from the reaction mixtures, by selective sorption of 2,2?-cyclopropylidene-bis(oxazolines) on a sorbent, such as silica gel, isolation of the sorbent from reaction mixture, desorption of 2,2?-cyclopropylidene-bis(oxazolines) from the sorbent with suitable organic solvent and final recovery of 2,2?-cyclopropylidene-bis(oxazolines) from the organic solvent used for desorption process. Catalytic quality of recovered compounds does not differ from those in freshly prepared catalysts.Type: GrantFiled: November 30, 2009Date of Patent: September 30, 2014Assignee: Latvian Institute of Organic SynthesisInventors: Ivars Kalvinsh, Antons Lebedevs, Aleksandrs Chernobrovijs, Grigory Veinberg, Maksims Vorona, Agnija Ievina
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Publication number: 20140249192Abstract: The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein R1 is selected from the group consisting of CO2R7 and CON(R7)SO2R7 wherein R1, R2, R3, R4, and R7 are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, EP3, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: February 12, 2014Publication date: September 4, 2014Applicant: Allergan, Inc.Inventors: Jose L. Martos, William R. Carling, David F. Woodward, Jenny W. Wang, Jussi J. Kangasmetsa
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Patent number: 8796253Abstract: This invention relates to novel heteroaryl substituted pyrazole 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 or therapeutic measures.Type: GrantFiled: May 8, 2008Date of Patent: August 5, 2014Assignee: Bayer Intellectual Property GmbHInventors: Stephen Boyer, Michael Härter, Philip Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
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Publication number: 20140012010Abstract: Provided is a process for producing an optically active compound represented by Formula (3): (wherein R1 is an alkyl group, an alkynyl group, an alkenyl group, an aliphatic heterocyclic group, a cycloalkyl group, an aryl group, an aralkyl group, or an aromatic heterocyclic group, and any hydrogen atom of R1 may be replaced with a substituent; R2 is a hydrogen atom or a group which is not reactive in the reaction below; and * represents a chiral center) or a salt thereof by subjecting a compound represented by Formula (1): (wherein R1 and R2 have the same meanings as defined in Formula (3)) to a ring closure reaction in the presence of a chiral ligand having 1 or more coordination sites, a Lewis acid represented by Formula (2): MmZn??(2) (wherein M is a metal ion, Z is a counter anion of M, and m and n are integers of 1 to 4), and a sulfonyl halide having an optionally substituted alkyl or phenyl groupType: ApplicationFiled: January 31, 2012Publication date: January 9, 2014Inventors: Osamu Onomura, Yutaro Tsuda, Masami Kuriyama, Toshiharu Yanagi, Kazuya Kodama
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Patent number: 8623945Abstract: This invention relates to a process for stabilizing polymers with oligomeric carbodiimides containing at least one heterocyclic end group and stabilizers. The oligomeric carbodiimides may be compounds of the general formula (I): where A1, A2 are each independently, identically or differently, hydrocarbon groups having 2 to 20 carbon atoms, B1, B2 are each independently, identically or differently, heterocycles, C1-C30-alcohols, polyetherols, polyesterols, amines, polyether amines, polyester amines, thioalcohols, polyether thiols, polyester thiols; R1, R2 are each independently, identically or differently: n is an integer from 2 to 100, and A1, A2, B1 and B2 may each be substituted at any desired position by C1-C20-alkyl, C2-C20-alkenyl, C2-C20-alkynyl, C1-C20-alkoxy, carbonyl oxygen (?O) or halogen, with the proviso that at least one B1 or B2 substituent is a heterocyclic end group. The invention also relates to compositions of the oligomeric carbodiimides and mixtures.Type: GrantFiled: March 15, 2012Date of Patent: January 7, 2014Assignee: BASF SEInventors: Theo Smit, Laurence Pottie, Simone Schillo, Volker Frenz, Roelof van der Meer
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Patent number: 8609857Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.Type: GrantFiled: May 14, 2012Date of Patent: December 17, 2013Assignee: Intezyne Technologies, Inc.Inventors: Kurt Breitenkamp, Kevin Sill, Habib Skaff
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Publication number: 20130310384Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.Type: ApplicationFiled: October 4, 2011Publication date: November 21, 2013Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Corinne E. Augelli-Szafran, Dai Lu, Hanxun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe
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Patent number: 8507514Abstract: There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitrogen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.Type: GrantFiled: February 5, 2010Date of Patent: August 13, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Hideki Ihara, Koji Kumamoto
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Publication number: 20130197011Abstract: Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.Type: ApplicationFiled: July 27, 2012Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Barbara BERTANI, Marco FERRARA, Iain LINGARD, Rocco MAZZAFERRO, Holger ROSENBROCK
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Patent number: 8415359Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: GrantFiled: August 5, 2011Date of Patent: April 9, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Akihiro Furukawa, Takehiro Fukuzaki, Yukari Onishi, Hideki Kobayashi, Takeshi Honda, Yumi Matsui, Masahiro Konishi, Kenjiro Ueda, Tetsuyoshi Matsufuji
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Patent number: 8377942Abstract: Novel isoxazoline compounds, compositions containing the compounds and methods for making the compounds are disclosed. The compounds and compositions have pesticidal properties and are suitable for controlling ectoparasites on non-human animals.Type: GrantFiled: December 17, 2009Date of Patent: February 19, 2013Assignee: Novartis AGInventors: Steve Nanchen, Noëlle Gauvry, Francois Pautrat
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Publication number: 20120270915Abstract: Compounds of Formula 1 are described herein. These compounds may be administered to a patient for treatment of suffering from pain or other FAAH mediated conditions.Type: ApplicationFiled: April 23, 2012Publication date: October 25, 2012Inventors: David F. Woodward, Jose L. Martos, William R. Carling, Neil J. Poloso, Jenny W. Wang
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Publication number: 20120238676Abstract: Oligomeric carbodiimides comprising at least one heterocyclic end group are used as stabilizers for polymers. The oligomeric carbodiimides may be compounds of the general formula (I), where A1, A2 are each independently, identically or differently, hydrocarbon groups having 2 to 20 carbon atoms, B1, B2 are each independently, identically or differently, heterocycles, C1-C30-alcohols, polyetherols, polyesterols, amines, polyether amines, polyester amines, thioalcohols, polyether thiols, polyester thiols, R1, R2 are each independently, identically or differently, n is an integer from 2 to 100, and wherein A1, A2, B1 and B2 may each be substituted at any desired position by C1-C20-alkyl, C2-C20-alkenyl, C2-C20-alkynyl, C1-C20-alkoxy, carbonyl oxygen (?O) or halogen, with the proviso that at least one B1 or B2 substituent is a heterocyclic end group. Processes for stabilizing polymers against hydrolysis using oligomeric carbodiimides are also disclosed.Type: ApplicationFiled: March 15, 2012Publication date: September 20, 2012Applicant: BASF SEInventors: THEO SMIT, LAURENCE POTTIE, SIMONE SCHILLO, VOLKER FRENZ, ROELOF VAN DER MEER
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Publication number: 20120226050Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.Type: ApplicationFiled: May 14, 2012Publication date: September 6, 2012Applicant: Intezyne Technologies, Inc.Inventors: Kurt Breitenkamp, Kevin N. Sill, Habib Skaff
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Publication number: 20120071526Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. wherein n is 1 or 2; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R3 and R4 is hydrogen or hydroxy and the other is hydrogen; or R3 and R4 together are ?O.Type: ApplicationFiled: August 25, 2011Publication date: March 22, 2012Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, Reid W. von Borstel
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Patent number: 8106052Abstract: The present invention provides methods, compositions, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step methods using luminogenic molecules, e.g. luciferin or coelenterazines, that are cytochrome P450 substrates and that are also bioluminescent enzyme, e.g., luciferase, pro-substrates are provided. Upon addition of the luciferin derivative or other luminogenic molecule into a P450 reaction, the P450 enzyme metabolizes the molecule into a bioluminescent enzyme substrate, e.g., luciferin and/or luciferin derivative metabolite, in a P450 reaction. The resulting metabolite(s) serves as a substrate of the bioluminescent enzyme, e.g., luciferase, in a second light-generating reaction. Luminescent cytochrome P450 assays with low background signals and high sensitivity are disclosed and isoform selectivity is demonstrated.Type: GrantFiled: April 5, 2010Date of Patent: January 31, 2012Assignee: Promega CorporationInventors: James J. Cali, Dieter Klaubert, William Daily, Samuel Kin Sang Ho, Susan Frackman, Erika Hawkins, Keith V. Wood
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Publication number: 20110294840Abstract: There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitrogen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.Type: ApplicationFiled: February 5, 2010Publication date: December 1, 2011Inventors: Hideki Ihara, Koji Kumamoto
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Publication number: 20110263864Abstract: The present invention provides a method for regeneration of chiral 2,2?-cyclopropylidene-bis(oxazolines), such as (3&R, 3?aR,8aS,8?aS)-2,2?-cyclopropylidenebis-[3a,8a]-dihydro-8H-indeno-[1,2-d]-oxazole and (45,4?5,5R,5?R)-2,2?-cyclopropy-lidenebis-4,5-diphenyldihydro-4,5-oxazole, used as a part of complex catalysts for e.g. stereoselective addition reactions, from the reaction mixtures, by selective sorption of 2,2?-cyclopropylidene-bis(oxazolines) on a sorbent, such as silica gel, isolation of the sorbent from reaction mixture, desorption of 2,2?-cyclopropylidene-bis(oxazolines) from the sorbent with suitable organic solvent and final recovery of 2,2?-cyclopropylidene-bis(oxazolines) from the organic solvent used for desorption process. Catalytic quality of recovered compounds does not differ from those in freshly prepared catalysts.Type: ApplicationFiled: November 30, 2009Publication date: October 27, 2011Inventors: Ivars Kalvinsh, Antons Lebedevs, Aleksandrs Chernobrovijs, Grigory Veinberg, Maksims Vorona, Agnija Levina
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Publication number: 20110245274Abstract: Novel isoxazoline compounds, compositions containing the compounds and methods for making the compounds are disclosed. The compounds and compositions have pesticidal properties and are suitable for controlling ectoparasites on non-human animals.Type: ApplicationFiled: December 17, 2009Publication date: October 6, 2011Applicant: Novartis AGInventors: Steve Nanchen, Noëlle Gauvry, Francois Pautrat
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Patent number: 8017610Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: GrantFiled: July 26, 2010Date of Patent: September 13, 2011Assignee: Daiichi Sankyo Company, LimitedInventors: Akihiro Furukawa, Takehiro Fukuzaki, Yukari Onishi, Hideki Kobayashi, Takeshi Honda, Yumi Matsui, Masahiro Konishi, Kenjiro Ueda, Tetsuyoshi Matsufuji
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Publication number: 20110124585Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: ApplicationFiled: February 7, 2011Publication date: May 26, 2011Inventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
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Publication number: 20110105567Abstract: Disclosed herein are compounds represented by: therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 21, 2008Publication date: May 5, 2011Applicant: Allergan, Inc.Inventors: Richard L. Beard, Hiaqing Yuan, John E. Donello, Ken Chow, Liming Wang
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Publication number: 20110098479Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2 ??(1) wherein RType: ApplicationFiled: December 29, 2010Publication date: April 28, 2011Inventors: KAZUSHI MASHIMA, Takashi Ohshima, Takanori Iwasaki, Hironori Maeda, Kenya Ishida
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Publication number: 20100298330Abstract: The present invention is related to the preparation and pharmaceutical In use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:(I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.Type: ApplicationFiled: November 19, 2008Publication date: November 25, 2010Applicant: PHARMAXIS LTD.Inventors: Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
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Publication number: 20100298558Abstract: There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted dihydroazole compound of General Formula (1) or a salt thereof: where A1, A2, A3 and A4 are independently C—Y or N, A5 is —CH2—, etc., G1 is a benzene ring, etc., G2 is G2-1, G2-6, G2-9, etc., X is a halogen atom, C1-2haloalkyl, etc., Z is methyl, —NH2, etc., R1 is —C(O)R1a, etc., R1a is C1-4alkyl, etc., R2 is H, C1-4alkyl, etc., R3 is C1-2haloalkyl, etc., R4 is H, cyano, methyl, etc., m is an integer of 1, 2, 3, etc., n is an integer of 0 or 1; and a pest control agent comprising the compound or the salt thereof.Type: ApplicationFiled: December 5, 2008Publication date: November 25, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takeshi Mita, Eitatsu Ikeda, Hiroaki Takahashi, Mitsuaki Komoda
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Publication number: 20100249085Abstract: This invention relates to novel heteroaryl substituted pyrazole 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 or therapeutic measures.Type: ApplicationFiled: May 8, 2008Publication date: September 30, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Stephen Boyer, Michael Härter, Philip L. Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
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Publication number: 20100227901Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed wherein n is 1 or 2; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R and R is hydrogen or hydroxy and the other is hydrogen; or R3 and R4 together are =0.Type: ApplicationFiled: February 22, 2007Publication date: September 9, 2010Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, Reid W. von Borstel
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Publication number: 20100210647Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.Type: ApplicationFiled: August 18, 2008Publication date: August 19, 2010Applicant: LG Life Sciences Ltd.Inventors: Soon Ha Kim, Hyoung Jin Kim, Sun Young Koo, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Seung Yup Paek, Hyo Shin Kwak, Dong Ook Seo, Eok Park
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Patent number: 7754891Abstract: The present invention relates to a 5,5?-position linked 1,1?-biphenyl axis chiral ligand in chemical industry field. The present invention incorporates both the central chirality of oxazoline and the axial chirality of diphenyls. Such ligand can be used in various asymmetric reactions catalyzed by metal with high reactivity and stereoselectivity, and thus represents a good application outlook. The ligand of the present invention has the formula of: wherein: n=5, 6, 7, 8, 9, 10, 11 or 12; R1=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R2=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R3=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R4=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl.Type: GrantFiled: December 29, 2006Date of Patent: July 13, 2010Assignee: Shanghai Jiaotong UniversityInventors: Wanbin Zhang, Yongjian Zhang, Feijun Wang
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Publication number: 20100063106Abstract: Provided are aminopyrazole derivatives, a process for the preparation thereof, and a composition for preventing or treating an ischemic disease containing the same. Since the aminopyrazole derivatives of the present invention can reduce an ischemic cell death significantly, they can be effectively used for the prevention and treatment of ischemic diseases mediated by ischemic cell death, or protection of organs.Type: ApplicationFiled: October 26, 2007Publication date: March 11, 2010Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Yong-Sam JUNG, Eunhee Kim, Nakjeong Kim, Yun-Sun Lee, Jeehee Suh, Haeyoung Suh, Kyu Yang Yi, Sung-eun Yoo
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Publication number: 20090312379Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: ApplicationFiled: July 24, 2009Publication date: December 17, 2009Inventors: Patrick G. Harran, Xiaodong Wang, Jef D. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
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Publication number: 20090005572Abstract: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.Type: ApplicationFiled: June 6, 2008Publication date: January 1, 2009Inventors: Gunnar HANSON, Charles CALDWELL, Patrick G. HARRAN, Susan HARRAN, Qi WEI, Ming ZHOU
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Patent number: 7285551Abstract: The present invention provides a fused ring compound of the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. The compound of the present invention shows an anti-hepatitis C virus (HCV) action based on the HCV polymerase inhibitory activity, and is useful as a therapeutic agent or prophylactic agent for hepatitis C.Type: GrantFiled: July 8, 2003Date of Patent: October 23, 2007Assignee: Japan Tobacco Inc.Inventors: Hiromasa Hashimoto, Kenji Mizutani, Atsuhito Yoshida
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Publication number: 20070197615Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula (I) wherein R1 and R2 are as defined in the description and claims. The compounds of formula (I) are pharmaceutically active substances.Type: ApplicationFiled: February 15, 2007Publication date: August 23, 2007Inventors: Thomas Hartung, Christian Jenny, Francois Montavon, Pius Waldmeier
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Patent number: 7179828Abstract: The subject invention provides novel compositions of biologically active macrolide compounds which can advantageously be used in blocking cellular proliferation, treatment of cancer, treatment of fungal infections and control of spoilage of food, cosmetic and other consumer items.Type: GrantFiled: June 22, 2004Date of Patent: February 20, 2007Inventors: Amy E. Wright, Shirley A. Pomponi, Peter J. McCarthy
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Patent number: 6809107Abstract: This invention provides compounds having the following general structures: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.Type: GrantFiled: June 14, 2000Date of Patent: October 26, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ramesh M. Kanojia, Alfonzo D. Jordan, Allen B. Reitz, Mark J. Macielag, Boyu Zhao
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Publication number: 20040131969Abstract: A non-resonant two-photon absorbing material is provided, comprising a specified compound and exhibiting far stronger non-resonant two-photon absorption and two-photon emission than conventional materials.Type: ApplicationFiled: October 7, 2003Publication date: July 8, 2004Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Hiroo Takizawa, Masaharu Akiba, Takeharu Tani, Jun Kawamata, Katsumi Kobayashi, Karin Kawahara
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Publication number: 20040044053Abstract: Indolinones of general formula I 1Type: ApplicationFiled: August 22, 2003Publication date: March 4, 2004Applicant: Boehringer Ingelheim Pharma KGInventors: Rainer Walter, Armin Heckel, Gerald Roth, Joerg Kley, Gisela Schnapp, Martin Lenter, Jacobus Van Meel, Walter Spevak, Ulrike Weyer-Czernilofsky
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Patent number: 6683188Abstract: The present invention provides organic dye compounds having their absorption maxima in a region ranging from the ultraviolet region to a relatively short wavelength visible region and uses thereof. The present invention provides specific monomethine cyanine dyes, light absorbents and optical recording media comprising the monomethine cyanine dyes, and a process for producing the monomethine cyanine dyes which comprises a step of reacting a quaternary ammonium salt of nitrogen atom-containing heterocyclic compound having a reactive methyl group with a quaternary ammonium salt of nitrogen atom-containing heterocyclic compound having an appropriate leaving group.Type: GrantFiled: August 17, 2001Date of Patent: January 27, 2004Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Chiaki Kasada, Yasushi Aizawa, Toshio Kawata, Shigeo Yasui
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Publication number: 20030212056Abstract: The present application describes novel &bgr;-sulfone derivatives of formula I: 1Type: ApplicationFiled: November 1, 2002Publication date: November 13, 2003Inventors: Jingwu Duan, Gregory R. Ott
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Patent number: 6642379Abstract: Benzamide derivatives represented by the general formula (I): and insecticides for agricultural and horticultural use and usage thereof, wherein Z1 is O or S; R is H, (substituted) alkyl, or alkoxycarbonyl; X is halogeno, cyano, nitro, C3-C6(halo)cycloalkyl, (substituted) phenyl, a (substituted) heterocyclic group, or —A1—R1 [wherein A1 is —O—, —S—, —SO—, —SO2—, —C(═O)—, or —C(═NOR2)— (wherein R2 is H, C1-C6(halo)alkyl, (substituted) phenylated C1-C4 alkyl, or the like); and R1 is halogeno, C3-C6 cycloalkyl, C3-C6 halocycloalkenyl, (substituted) phenyl, or the like]; n is 0 to 4; Y is halogeno, cyano, nitro, C3-C6 halocycloalkyl, (substituted) phenyl, or the like; m is 1 to 5; Q is a heterocycle such as oxazoline; and B1 to B4 are each CH or N.Type: GrantFiled: April 4, 2002Date of Patent: November 4, 2003Assignee: Nihon Nohyaku Co., Ltd.Inventors: Takashi Furuya, Eiji Kohno, Masanori Tohnishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
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Publication number: 20030153596Abstract: The present invention relates to novel thiourca derivatives as a modulator for vanilloid receptor (VR) and the phar- maceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflam- matory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.Type: ApplicationFiled: July 9, 2002Publication date: August 14, 2003Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Ok Hui Park, Yong Sil Lee, Young Ho Park, Yung Hyup Joo, Jin Kyu Choi, Kyung Min Lim, Sun Young Kim, Jin Kwan Kim, Hyun Ju Koh, Joo Hyun Moh, Yeon Su Jeong, Jung Bum Yi, Young Im Oh
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Patent number: 6586452Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.Type: GrantFiled: July 9, 2001Date of Patent: July 1, 2003Assignee: Merck & Co., Inc.Inventors: Thomas Shih, Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Howard C. H. Kuo, Prasun K. Chakravarty, Matthew J. Wyvratt, Sriram Tyagarajan, Richard Berger
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Publication number: 20030119886Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: September 25, 2002Publication date: June 26, 2003Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Publication number: 20030022884Abstract: The object of the invention is to provide an excellent compound as a drug.Type: ApplicationFiled: June 12, 2002Publication date: January 30, 2003Inventors: Toshiyuki Suzuki, Tomiyoshi Aoki
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Patent number: 6476233Abstract: This invention is to develop novel transition metal catalysts for the practical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral amine oxazolinyl ligands and related ligands. Specially, a direct asymmetric hydrogenation system based on Ru-Ambox catalyst was discovered.Type: GrantFiled: November 15, 2000Date of Patent: November 5, 2002Assignee: The Penn State Research FoundationInventor: Xumu Zhang
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Patent number: 6365747Abstract: The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising treatment of a compound of formula (IV), wherein X is O or S; R1-R2 are each independently selected from hydrogen and C1-6 alkyl, or R1 and R2 together form a C2-5 alkylene chain thereby forming a spiro-ring; R3 is selected from hydrogen and C1-6 alkyl, R4 is selected from hydrogen, C1-6 alkyl, a carboxy group or a precursor group therefore, or R3 and R4 together form a C2-5 alkylene chain thereby forming a spiro-ring, with a dehydration agent or alternatively where X is S, thermally cleavage of the thiazoline ring, or treatment in presence of a radical initiator, to form citalopram. The invention also relates to intermediates used in the new process for the preparation of citalopram, as well as citalopram prepared according to the new process.Type: GrantFiled: June 1, 2001Date of Patent: April 2, 2002Assignee: H. Lundbeck A/SInventors: Leone Dall'Asta, Umberto Casazza, Hans Petersen