1,3-thiazines Patents (Class 544/53)
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Publication number: 20140378444Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.Type: ApplicationFiled: November 22, 2013Publication date: December 25, 2014Applicant: University of Pittsburgh - Of the Commonwealth System of Higher EducationInventors: Peter Wipf, Marie-Celine Frantz
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Publication number: 20140315898Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparationType: ApplicationFiled: December 12, 2012Publication date: October 23, 2014Applicant: BAYER CROPSCIENCE AGInventors: Adeline Koehler, Bernd Alig, Angela Becker, Arnd Voerste, Ulrich Goergens, Reiner Fischer, Wahed Ahmed Moradi, Silvia Cerezo-Galvez, Julia Johanna Hahn, Kerstin Ilg, Hans-Georg Schwarz, Takuya Gomibuchi, Masahito Ito, Daiei Yamazaki, Katsuhiko Shibuya, Eiichi Shimojo
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Patent number: 8852846Abstract: The present invention provides a salt represented by the formula (I): wherein Q1 and Q2 independently each represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents a C1-C20 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, W represents a group represented by the formula (W1), (W2), (W3), (W4) or (W5): and Z+ represents an organic counter ion.Type: GrantFiled: April 4, 2012Date of Patent: October 7, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Yukako Anryu, Koji Ichikawa
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Publication number: 20140058097Abstract: A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene, etc.; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2, R2b, R3a, R3b, R4a and R4b are each independently a hydrogen atom, halogen, hydroxy, etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 1 to 3; and R5 is a hydrogen atom, optionally substituted lower alkyl, etc.; its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.Type: ApplicationFiled: November 1, 2013Publication date: February 27, 2014Applicant: Shionogi & Co., Ltd.Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuuji Kooriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
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Patent number: 8637504Abstract: The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound represented by the formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.Type: GrantFiled: June 11, 2009Date of Patent: January 28, 2014Assignee: Shionogi & Co., Ltd.Inventors: Akihiro Hori, Terukazu Kato
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Patent number: 8546380Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the formula (I): wherein ring A is an optionally substituted heterocyclic group; E is lower alkylene; X is S; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; or its pharmaceutically acceptable salt thereof.Type: GrantFiled: September 23, 2011Date of Patent: October 1, 2013Assignee: Shionogi & Co., Ltd.Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuji Koriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
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Patent number: 8541408Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.Type: GrantFiled: March 12, 2012Date of Patent: September 24, 2013Assignee: Shionogi & Co., Ltd.Inventors: Yuusuki Tamura, Shinji Suzuki, Yukio Tada, Chiaki Fujikoshi, Sae Matsumoto, Yuuji Kooriyama
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Patent number: 8507479Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.Type: GrantFiled: March 12, 2012Date of Patent: August 13, 2013Assignee: Shionogi & Co., Ltd.Inventors: Yuusuki Tamura, Shinji Suzuki, Yukio Tada, Chiaki Fujikoshi, Sae Matsumoto, Yuuji Kooriyama
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Publication number: 20120258961Abstract: The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-? proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, ring A, Y and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: December 22, 2010Publication date: October 11, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Shinji Suzuki, Yuuji Kooriyama
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Publication number: 20120245154Abstract: The present invention relates to an agent for treating or preventing disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound of formula (I), wherein, R1, R2a, R2b R3, R4a, R4b, ring A, and dashed line are described in this specification, its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: December 8, 2010Publication date: September 27, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Kousuke Anan, Yukio Tada, Akihiro Hori, Moriyasu Masui
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Publication number: 20120238557Abstract: The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-? proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3, R4, R5, X, L1, L2, A, ring B and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: November 12, 2010Publication date: September 20, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Kousuke Anan
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Patent number: 8173642Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.Type: GrantFiled: October 23, 2006Date of Patent: May 8, 2012Assignee: Shionogi & Co., Ltd.Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuji Koriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
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Patent number: 8168630Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.Type: GrantFiled: April 23, 2008Date of Patent: May 1, 2012Assignee: Shionogi & Co., Ltd.Inventors: Yuusuke Tamura, Shinji Suzuki, Yukio Tada, Shuji Yonezawa, Chiaki Fujikoshi, Sae Matsumoto, Yuuji Kooriyama, Tatsuhiko Ueno
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Publication number: 20120022249Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: September 23, 2011Publication date: January 26, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Naotake KOBAYASHI, Kazuo UEDA, Naohiro ITOH, Shinji SUZUKI, Gaku SAKAGUCHI, Akira KATO, Akira YUKIMASA, Akihiro HORI, Yuji KORIYAMA, Hidekazu HARAGUCHI, Ken YASUI, Yasuhiko KANDA
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Publication number: 20120016116Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Naotake KOBAYASHI, Kazuo UEDA, Naohiro ITOH, Shinji SUZUKI, Gaku SAKAGUCHI, Akira KATO, Akira YUKIMASA, Akihiro HORI, Yuji KORIYAMA, Hidekazu HARAGUCHI, Ken YASUI, Yasuhiko KANDA
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Patent number: 8080605Abstract: Polymer-filler coupling compounds with the formula B-A-Sx—N are claimed. In these compounds, B is an azaheterocyclic oxygen or sulfur containing moiety, or an allyltin moiety; Sx is a polysulfide, where x is between 2 and about 10; A is a linking atom or group that forms a bridge between B and Sx; and N is a blocking group. Sx can be a disulfide. N can be a conventional blocking group or other group such as -A-B. Methods for using the polymer-filler coupling compounds to modify polymers containing unsaturated carbon-carbon bonds and promote filler dispersion are also claimed. Additionally, vulcanizable rubber compositions containing the polymer-filler coupling compounds and methods for making vulcanized rubber compositions using the polymer-filler coupling compounds are also claimed.Type: GrantFiled: December 28, 2006Date of Patent: December 20, 2011Assignee: Bridgestone CorporationInventors: Yasuo Fukushima, William L. Hergenrother, Russell W. Koch
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Patent number: 8063205Abstract: The present invention is a method for producing a 2-oxazoline analogue or a 1,3-oxazine analogue represented by the following general formula (3) by reacting a 1,2-aminoalcohol compound or a 1,2-aminothiol compound with an ?,?-dihaloamine compound. (In the formula, n represents 0 or 1, and R represents an oxygen atom or a sulfur atom. R1, R2 and R3 each represents an atom or a group shown in Group 1 to Group 3, and R0 represents an atom or a group shown in Group 2 or Group 3. Two or more of R1, R2 and R3 may be bonded to each other to form a ring.Type: GrantFiled: August 30, 2006Date of Patent: November 22, 2011Assignees: National University Corporation Hokkaido University, Mitsubishi Gas Chemical Company, Inc.Inventors: Shoji Hara, Tsuyoshi Fukuhara, Toshio Hidaka
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Patent number: 8022018Abstract: Corrosion of metallic tubulars in an oil, gas or geothermal well may be inhibited by introducing into the well a dithiazine or dithiazine of the formula: wherein R is selected from the group consisting of a C1 to C12 saturated or unsaturated hydrocarbyl group or a C1 to C10 ?-hydroxy saturated or unsaturated hydrocarbyl group; R1 is selected from the group consisting of a C1-C24 straight chain or branched alkyl group or a C1-C24 arylalkyl; R2 is selected from the group consisting of X-R4-X, R4 being a C1-C6 alkyl group; and X is chlorine, bromine or iodine. The dithiazine may he isolated from a whole spent fluid formed by reaction of hydrogen sulfide and a triazine. Alternately, the whole spent fluid containing the dithiazine may be introduced into the well. The dithiazines of formulae (II) and (III) are quaternized derivatives of the dithiazine of formula (I).Type: GrantFiled: August 24, 2010Date of Patent: September 20, 2011Assignee: Baker Hughes IncorporatedInventor: Grahame Nigel Taylor
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Patent number: 8022017Abstract: Corrosion of metallic tubulars in an oil, gas or geothermal well may be inhibited by introducing into the well a dithiazine of the formula: wherein R is selected from the group consisting of a C1 to C10 saturated or unsaturated hydrocarbyl group or a C1 to C10 ?-hydroxy saturated or unsaturated hydrocarbyl group. The dithiazine may be isolated from a whole spent fluid formed by reaction of hydrogen sulfide and a triazine. Alternately, the whole spent fluid containing the dithiazine may be introduced into the well. In addition, the dithiazine or whole spent fluid may be formulated with at least one component selected from alkyl, alkylaryl or arylamine quaternary salts; mono or polycyclic aromatic amine salts; imidazoline derivative or a quaternary salt thereof; a mono-, di- or trialkyl or alkylaryl phosphate ester; or a monomeric or oligomeric fatty acid.Type: GrantFiled: December 21, 2009Date of Patent: September 20, 2011Assignee: Baker Hughes IncorporatedInventor: Grahame Nigel Taylor
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Patent number: 7947675Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.Type: GrantFiled: February 16, 2006Date of Patent: May 24, 2011Assignee: Merck Patent GmbHInventors: Bruno Roux, Isabelle Berard
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Publication number: 20100120754Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor.Type: ApplicationFiled: May 6, 2009Publication date: May 13, 2010Inventors: Peter Oettgen, Alan Rigby, Towia Libermann
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Publication number: 20090234116Abstract: The present invention relates to compositions of matter that are ionic liquids, the compositions comprising any of eleven cations combined with any of three fluorinated sulfonated anions. Compositions of the invention should be useful as solvents and, perhaps, as catalysts for many reactions, including aromatic electrophilic substitution, nitration, acylation, esterification, etherification, oligomerization, transesterification, isomerization and hydration.Type: ApplicationFiled: May 27, 2009Publication date: September 17, 2009Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Mark Andrew Harmer, Christopher P. Junk, Jemma Vickery
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Patent number: 7524874Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: August 1, 2005Date of Patent: April 28, 2009Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Vassil I. Ognyanov, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Liping H. Pettus, Hui-Ling Wang, Xianghong Wang, Premilla Arasasingham
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Publication number: 20090082560Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: October 23, 2006Publication date: March 26, 2009Applicant: Shionogi & Co., Ltd.Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuji Koriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
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Patent number: 7459450Abstract: The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: April 28, 2005Date of Patent: December 2, 2008Assignee: Schering CorporationInventors: Zhaoning Zhu, Zhong-Yue Sun, Yuanzan C. Ye, Deborra E. Mullins, Brian McKittrick, Andrew Stamford, William J. Greenlee
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Patent number: 7420053Abstract: The present invention relates to 2-imino-1,3-thiazine derivatives, in specific, 2-imino-1,3-thiazine derivatives having a selective antagonistic activity or agonistic activity to a cannabinoid type 2 receptor and their pharmaceutical use.Type: GrantFiled: November 29, 2006Date of Patent: September 2, 2008Assignee: Shionogi & Co., Ltd.Inventors: Koji Hanasaki, Takami Murashi, Hiroyuki Kai
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Patent number: 7335672Abstract: Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenType: GrantFiled: September 13, 2005Date of Patent: February 26, 2008Assignee: Amgen Inc.Inventors: Mark H. Norman, Liping H. Pettus, Xianghong Wang, Jiawang Zhu
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Patent number: 7332511Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: August 1, 2005Date of Patent: February 19, 2008Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Hui-Ling Wang, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Celia Dominguez, James Richard Falsey, Christopher Hulme, Jodie Katon, Thomas Nixey, Vassil I. Ognyanov, Liping H. Pettus, Robert Michael Rzasa
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Patent number: 7259163Abstract: Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.Type: GrantFiled: October 30, 2002Date of Patent: August 21, 2007Assignee: Glaxo Group LimitedInventors: Gianpaolo Bravi, Rossella Guidetti, David Haigh, Charles David Hartley, Peter David Howes, Deborah Lynette Jackson, Victoria Lucy Helen Lovegrove, Pritom Shah, Martin John Slater, Katrina Jane Wareing
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Patent number: 7244725Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and RC are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.Type: GrantFiled: September 10, 2003Date of Patent: July 17, 2007Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn CompanyInventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth TenBrink
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Patent number: 7183275Abstract: The present invention relates to 2-imino-1,3-thiazine derivatives, in specific, 2-imino-1,3-thiazine derivatives having a selective antagonistic activity or agonistic activity to a cannabinoid type 2 receptor and their pharmaceutical use.Type: GrantFiled: October 26, 2004Date of Patent: February 27, 2007Assignee: Shionogi Co., Ltd.Inventors: Koji Hanasaki, Takami Murashi, Hiroyuki Kai
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Patent number: 7166609Abstract: Pyrimidine-4,6-dicarboxylic acid diamides of the formula I are suitable for selectively inhibiting collagenase (MMP 13). The pyrimidine-4,6-dicarboxylic acid diamides can therefore be used for treating degenerative joint diseases.Type: GrantFiled: November 3, 2003Date of Patent: January 23, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Otmar Klingler, Reinhard Kirsch, Joerg Habermann, Klaus-Ulrich Weithmann, Christian Engel, Bernard Pirard
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Patent number: 7038039Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.Type: GrantFiled: February 13, 2001Date of Patent: May 2, 2006Assignee: Mitsui Chemicals, Inc.Inventors: Hironori Komatsu, Hirokazu Awano, Nobuyuki Fukazawa, Kiyoshi Ito, Ichirou Ikeda, Tadashi Araki, Takeshi Nakamura, Tamotsu Asano, Junya Fujiwara, Tomoyuki Ando, Katsutoshi Tsuchiya, Kyoko Maruyama, Hideki Umetani, Takahiro Yamauchi, Hitoki Miyake
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Patent number: 6908937Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integers from 3 to 10, n represents 0, 1 or 2, Het represents the groups where R1 represents hydrogen; mercapto; optionally halogen-substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl or alkenyl; optionally substituted aryl; or optionally substituted heterocyclyl, Y represents oxygen or sulphur, and R2 represents hydrogen, alkyl or optionally substituted aryl, and to processes for their preparation and to their use as pesticides.Type: GrantFiled: July 2, 2001Date of Patent: June 21, 2005Assignee: Bayer Cropscience AGInventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
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Patent number: 6841668Abstract: Sterically hindered N-substituted aryloxyamines are prepared by the Keggin polyoxometalate or the transition metal substituted polyoxometalate (TMS-POM) catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitoxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.Type: GrantFiled: April 4, 2003Date of Patent: January 11, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Deborah Judd, Sai P. Shum, Stephen D. Pastor
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Patent number: 6818640Abstract: It is found out that compounds represented by general formula (I) bind selectively to cannabinoid 2 receptor (CB2R) and thus exhibit CB2R antagonism or CB2R agonis wherein R1 represents optionally substituted alkylene; R2 represents hydrogen, alkyl, a group represented by the formula —C(═R5)—R6 (wherein R5 represents O or S; and R6 represents alkyl, alkoxy, alkylthio, etc.) or a group represented by the formula SO2R7 (wherein R7 represents allyl, etc.); m is an integer of from 0 to 2; and A represents optionally substituted aryl, etc.Type: GrantFiled: February 26, 2002Date of Patent: November 16, 2004Assignee: Shionogi & Co., Ltd.Inventors: Koji Hanasaki, Takami Murashi, Hiroyuki Kai
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Publication number: 20040192910Abstract: Compounds of Formula I (I) wherein the substituents are as defined in claim 1, and the agrochemically tolerable salts and all stereoisomers and tautomers of the compounds of formula I, are suitable for use as herbicides.Type: ApplicationFiled: February 26, 2004Publication date: September 30, 2004Inventors: Christoph Luthy, Andrew Edmunds
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Publication number: 20040063934Abstract: The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the &agr;v&bgr;3 integrin receptor, their use, and pharmaceutical preparations comprising these compounds.Type: ApplicationFiled: September 8, 2003Publication date: April 1, 2004Inventors: Herve Geneste, Andreas Kling, Udo Lange, Werner Seitz, Claudia Isabella Graef, Thomas Subkoski, Wilfried Hornberger, Arnulf Lauterbach
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Patent number: 6699898Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines.Type: GrantFiled: May 23, 2002Date of Patent: March 2, 2004Assignee: Pharmacia COrporation Global Patent DepartmentInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030207869Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1Type: ApplicationFiled: May 6, 2003Publication date: November 6, 2003Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
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Publication number: 20030158184Abstract: The invention provides methods for treating female sexual dysfunctions by administering to a female individual a therapeutically effective amount of at least one compound that donates, transfers or release nitrogen monoxide, that induces the production of endogenous endothelium-derived relaxing factor, that stimulates endogenous synthesis of nitrogen monoxide, or that is a substrate for nitric oxide synthase. The methods may further comprise administering a therapeutically effective amount of a phosphodiesterase inhibitor and/or a nitrosated and/or nitrosylated phosphodiesterase inhibitor.Type: ApplicationFiled: December 21, 2001Publication date: August 21, 2003Inventors: David S. Garvey, Inigo Saenz de Tejada
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Publication number: 20030134848Abstract: There is provided heterocyclic compounds of the following formula (I): 1Type: ApplicationFiled: November 21, 2001Publication date: July 17, 2003Inventors: Masahiro Imoto, Tatsuya Iwanami, Minako Akabane, Yoshihiro Tani
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Publication number: 20030129081Abstract: The novel and known thiazines and thiazoles of the formula (I) 1Type: ApplicationFiled: June 24, 2002Publication date: July 10, 2003Inventors: Rainer Bruns, Hermann Uhr, Martin Kugler, Peter Wachtler, Oliver Kretschik
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Publication number: 20030130271Abstract: The invention provides compounds of formula 1Type: ApplicationFiled: August 27, 2002Publication date: July 10, 2003Applicant: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
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Patent number: 6579982Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: August 9, 2000Date of Patent: June 17, 2003Assignee: Pfizer Inc.Inventor: Julian Blagg
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Publication number: 20030100755Abstract: A compound of the formula: 1Type: ApplicationFiled: October 25, 2002Publication date: May 29, 2003Inventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Patent number: 6534492Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I and salts thereof, where A=oxygen or sulfur; X1=H, halogen, C1-C4-alkyl; X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl; X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl; R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl, or R1+R2 together with the atom to which they are attached form 3- to 7-membered heterocyclic ring; Q is selected from Q1 to Q40 as defined in the description. Use: As herbicides; for the desiccation/defoliation of plants.Type: GrantFiled: May 4, 2001Date of Patent: March 18, 2003Assignee: BASF AktiengesellschaftInventors: Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi
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Publication number: 20020193314Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.Type: ApplicationFiled: May 7, 2002Publication date: December 19, 2002Inventors: Hironori Komatsu, Hirokazu Awano, Nobuyuki Fukazawa, Kiyoshi Ito, Ichirou Ikeda, Tadashi Araki, Takeshi Nakamura, Tamotsu Asano, Junya Fujiwara, Tomoyuki Ando, Katsutoshi Tsuchiya, Kyoko Maruyama, Hideki Umetani, Takahiro Yamauchi, Hitoki Miyake
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Patent number: 6469000Abstract: Disclosed are compounds which are inhibitors of metalloproteases having the following structure: where Ar, W, X, Y, Z, R1 and R2 have the meanings described in the specification and optical isomers, diastereomers, and enantiomers thereof or a pharmaceutically-acceptable salt, or biohydrolyzable amides, esters, or imides thereof. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by unwanted metalloprotease activity using these compounds or pharmaceutical compositions.Type: GrantFiled: August 29, 2000Date of Patent: October 22, 2002Assignee: The Procter & Gamble Co.Inventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
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Patent number: 6451830Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines.Type: GrantFiled: November 14, 2001Date of Patent: September 17, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel