Acyclic Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/328)
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Patent number: 11161811Abstract: The present invention discloses a process for preparing a Mannich base quaternary ammonium salt high-temperature resistant corrosion inhibitor and applications thereof. The preparation process comprises the following steps: (1) dissolve an amine substance indole, benzhydrylpiperidine, diphenylethylamine, dibenzylamine or diisopropanolamine into an organic solvent, slowly add an aldehyde substance 3-(2-thienyl)benzaldehyde or cinnamaldehyde, then place in a constant-temperature water bath, stir to react at 60-80° C.Type: GrantFiled: November 20, 2018Date of Patent: November 2, 2021Assignee: SOUTHWEST PETROLEUM UNIVERSITYInventors: Dingli Wang, Yongming Li, Xiyu Chen, Youshi Jiang, Juhui Zhu
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Patent number: 9809548Abstract: Disclosed are novel polymorphic solvated and desolvated forms of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)phenyl]-benzenesulfonamide. One embodiment of the present invention is directed to a crystalline sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]benzenesulfonamide (hereinafter “Compound A-1,4-dioxane/water solvate”), wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles (°28), when measured using Cu Ku radiation, at about 4.0, 8.1, 10.1, 14.2, 16.2, 18.6, 20.3, 24.7, 25.0, and 26.5.Type: GrantFiled: October 10, 2016Date of Patent: November 7, 2017Assignee: ChemoCentryx, Inc.Inventors: Joanna Bis, David H. Igo
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Patent number: 9556112Abstract: The invention generally relates to compounds having structure I: wherein x represents alkyl, aryl or het-aryl, each of y independently represents hydrogen or halogen and z represents hydrogen or alkyl. Further, said compounds are inhibitors of MEK 1, 2 and 5. Furthermore, the invention includes methods of making said compounds, compositions including said compounds and uses for inhibiting MEK 1, 2 and 5.Type: GrantFiled: November 15, 2013Date of Patent: January 31, 2017Assignee: Duquesne University of the Holy GhostInventors: Suravi Chakrabarty, Darlene Monlish, Patrick Flaherty, Jane E. Cavanaugh, Sneha Potdar
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Patent number: 9493417Abstract: Disclosed are novel novel polymorphic solvated and desolvated forms of the sodium salt of 4-tert-butyl-N-[chloro-2-(1-oxy-pyridine-4-carbonyl)phenyl]-benzenesulfonamide. One embodiment of the present invention is directed to a crystalline sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]benzenesulfonamide (hereinafter “Compound A-1,4-dioxane/water solvate”), wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles (° 28), when measured using Cu Ku radiation, at about 4.0, 8.1, 10.1, 14.2, 16.2, 18.6, 20.3, 24.7, 25.0, and 26.5.Type: GrantFiled: August 21, 2015Date of Patent: November 15, 2016Assignee: ChemoCentryx, Inc.Inventors: Joanna Bis, David H. Igo
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Patent number: 9464054Abstract: Disclosed are novel polymorphic trihydrated forms of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]benzenesulfonamide. One embodiment of the present invention is directed to a crystalline form of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-25 phenyl]-benzenesulfonamide (hereinafter “Compound A_crystalline trihydrate form I”), wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles (°28), when measured using Cu Ka radiation, at about 4.5, 9.0, 13.6, 13.9, 15.8, 17.8, 18.2, 18.5, 19.1, 19.9, 20A, 21.2, 22.1, 22.7, 24.3, 25.0, 25.6, 26.2, 26.8, 27.3, 27.6, 28.0, 28.8, and 30.8.Type: GrantFiled: August 12, 2015Date of Patent: October 11, 2016Assignee: ChemoCentryx, Inc.Inventors: Joanna Bis, David H. Igo, Bert Ho, Deven Shah
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Publication number: 20150080351Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
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Publication number: 20140171473Abstract: Disclosed are novel novel polymorphic solvated and desolvated forms of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)phenyl]-benzenesulfonamide. One embodiment of the present invention is directed to a crystalline sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]benzenesulfonamide (hereinafter “Compound A-1,4-dioxane/water solvate”), wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles (° 28), when measured using Cu Ku radiation, at about 4.0,8.1, 10.1, 14.2, 16.2, 18.6,20.3,24.7,25.0, and 26.5.Type: ApplicationFiled: July 20, 2012Publication date: June 19, 2014Applicant: CHEMOCENTRYX, INC.Inventors: Joanna Bis, David H. Igo
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Patent number: 8748624Abstract: The present invention is directed to picolanmido-propanoic acid derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.Type: GrantFiled: May 23, 2012Date of Patent: June 10, 2014Assignee: Janssen Pharmaceutica NVInventors: Devraj Chakravarty, Kevin Kreutter, Mark Powell, Brian Shook, Fengbin Song, Guozhang Xu, Shyh-Ming Yang, Rui Zhang, Bao-Ping Zhao
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Publication number: 20140155438Abstract: Disclosed are novel polymorphic trihydrated forms of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl] benzenesulfonamide. One embodiment of the present invention is directed to a crystalline form of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-25 phenyl]-benzenesulfonamide (hereinafter “Compound A _ crystal-line trihydrate form I”), wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles (°28), when measured using Cu Ka radiation, at about 4.5, 9.0, 13.6, 13.9, 15.8, 17.8, 18.2, 18.5, 19.1, 19.9, 20A, 21.2, 22.1, 22.7, 24.3, 25.0, 25.6, 26.2, 26.8, 27.3, 27.6, 28.0, 28.8, and 30.8.Type: ApplicationFiled: July 20, 2012Publication date: June 5, 2014Applicant: CHEMOCENTRYX, INC.Inventors: Joanna Bis, David H. Igo, Bert Ho, Deven Shah
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Publication number: 20140135328Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
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Publication number: 20140107160Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: October 9, 2013Publication date: April 17, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
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Publication number: 20140088046Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.Type: ApplicationFiled: September 5, 2013Publication date: March 27, 2014Applicant: ZOETIS LLCInventors: Denis Billen, Michael Curtis, Richard Andrew Ewin, Richard M. Goodwin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Todd M. Maddux, Susan Mary Kult Sheehan, Rajendran Vairagoundar
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Publication number: 20130267492Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: March 28, 2013Publication date: October 10, 2013Applicant: ChemoCentryx, Inc.Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
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Patent number: 8497380Abstract: The present invention relates to a compound according to formula: (1); wherein X1, X2, X3, X4 and X5 independently of each other represent —CH— or N; or X3, X4 and X5 independently of each other represent —CH— or N, and X1 and X2 independently of each other represent C and form part of an additional 6-membered aromatic ring; R1 represents hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, —CH2, —C(O)NR—R?, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, aikylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent —CH— or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to methods of treating dermal disease.Type: GrantFiled: July 11, 2012Date of Patent: July 30, 2013Assignee: Leo Pharma A/SInventors: Jakob Felding, Simon Feldbæk Nielsen
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Patent number: 8466292Abstract: The present invention is directed to compounds of the general formula: as well as pharmaceutical compositions thereof. The invention is also directed to their therapeutic use as urotensin II receptor antagonists, e.g., in the treatment of cardiac, coronary, and central nervous system disorders. In particular embodiments, the invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.Type: GrantFiled: August 6, 2010Date of Patent: June 18, 2013Assignee: SanofiInventors: Jean-Michel Altenburger, Valérie Fossey, Daniel Galtier, Frédéric Petit
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Publication number: 20130059893Abstract: A novel crystalline form of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide and pharmaceutical compositions containing the same are disclosed. Processes for the preparation thereof and methods for use thereof are also disclosed.Type: ApplicationFiled: July 20, 2012Publication date: March 7, 2013Applicant: ChemoCentryx, Inc.Inventor: Andrew M.K. Pennell
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Publication number: 20130035492Abstract: Methods and processes for preparation and production of deuterated ?-diphenylurea are disclosed. Especially, a kind of deuterated ?-diphenylurea compounds which can inhibit phosphokinase and the preparation method of N-(4-chloro-3-(trifluoromethyl)phenye-N?-(4-(2-(N-d3-methylcarbamoyl)-4-pridinyloxy)phenyl)urea are disclosed. The said deuterated diphenylurea compounds can be used for treating or preventing tumors and relative diseases.Type: ApplicationFiled: March 17, 2011Publication date: February 7, 2013Applicant: SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD.Inventors: Weidong Feng, Xiaoyong Gao, Xiaojun Dai
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Publication number: 20130012716Abstract: The present invention relates to a compound according to formula: (1); wherein X1, X2, X3, X4 and X5 independently of each other represent —CH— or N; or X3, X4 and X5 independently of each other represent —CH— or N, and X1 and X2 independently of each other represent C and form part of an additional 6-membered aromatic ring; R1 represents hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, —CH2, —C(O)NR—R?, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, alkylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent —CH— or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to methods of treating dermal disease.Type: ApplicationFiled: July 11, 2012Publication date: January 10, 2013Inventors: Jakob FELDING, Simon Feldbaek Nielsen
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Publication number: 20120330007Abstract: The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.Type: ApplicationFiled: September 15, 2010Publication date: December 27, 2012Applicant: PAION UK LimitedInventors: Gary Stuart Tilbrook, Andreas Schumacher, René Emmengger
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Publication number: 20120302809Abstract: Higher molecular weight linear ?-olefins are produced by the oligomerization of ethylene using certain iron complexes of 2,6-diacylpyridinedimimines or 2,6-pyridinedicarboxaldehydedimines as catalysts. These iron complexes are more sterically hindered than those heretofore used. The resulting ?-olefins are useful as comonomers in olefin polymerizations.Type: ApplicationFiled: March 28, 2011Publication date: November 29, 2012Applicant: E.I. Dupont De Nemours and CompanyInventors: Joel David Citron, Alex Sergey Ionkin
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Publication number: 20120277423Abstract: The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3: wherein R1 is a substituted or unsubstituted aryl or heterocyclyl group, R2, R3, and R4 are hydrogen atoms, n is 2, X is halogen, R5 and R6 independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R5 and R6 are not hydrogen atoms at the same time, or R5 and R6 may be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.Type: ApplicationFiled: May 19, 2010Publication date: November 1, 2012Inventors: Katsuhiko Mikoshiba, Kozo Hamada, Akiko Terauchi, Shouichirou Ozaki, Jun-ichi Goto, Etsuko Ebisui, Akinobu Suzuki
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Patent number: 8247437Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: June 8, 2011Date of Patent: August 21, 2012Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20120107240Abstract: Embodiments of the present disclosure provide for labeled probes such as a 3-18F-fluoropicolinamide probe, methods of making labeled probes, pharmaceutical compositions including labeled probes, methods of using labeled probes, methods of diagnosing, localizing, monitoring, and/or assessing melanin related diseases, cancers, tumors, precancerous cells, and related biological events (e.g., malignant melanoma), using labeled probes, kits for diagnosing, localizing, monitoring, and/or assessing melanin related diseases, cancers, tumors, precancerous cells, and related biological events, using labeled probes, and the like.Type: ApplicationFiled: November 3, 2011Publication date: May 3, 2012Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Shuanglong Liu, Hongguang Liu, Zhen Cheng
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Publication number: 20120101097Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.Type: ApplicationFiled: March 10, 2011Publication date: April 26, 2012Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
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Publication number: 20120088782Abstract: A compound of the general formula (I): (wherein the symbols are as defined in the description), or a non-toxic salt thereof.Type: ApplicationFiled: December 19, 2011Publication date: April 12, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masahiko Terakado, Shinji Nakade, Takuya Seko, Yoshikazu Takaoka
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Publication number: 20120040997Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 31, 2008Publication date: February 16, 2012Inventor: Shoujun Chen
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Patent number: 8110579Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: GrantFiled: February 11, 2009Date of Patent: February 7, 2012Assignee: Sanofi-AventisInventors: Jean-Michel Altenburger, Valerie Fossey, Philip Janiak, Gilbert Lassalle, Frederic Petit, Jean Claude Vernieres
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Publication number: 20120022263Abstract: The present invention herein provides a 3-aminooxalylaminobenzamide derivative which is used as an insecticide or miticide. The 3-aminooxalylaminobenzamide derivative is one represented by the following general formula [1]: (R1 and R2 each represent, for instance, a C1 to C3 alkoxy group or a C1 to C3 haloalkoxy group; R3 and R4 each represent, for instance, a C1 to C8 alkyl group or a C1 to C8 haloalkyl group; R5 represents, for instance, a C1 to C5 haloalkyl group; R6 and R7 each represent, for instance, a hydrogen atom or a C1 to C5 alkyl group; Y represents, for instance, a hydrogen atom or a halogen atom; Z represents, for instance, a hydrogen atom; n is an integer ranging from 0 to 4 and m is an integer ranging from 0 to 2).Type: ApplicationFiled: February 5, 2010Publication date: January 26, 2012Applicant: AGRO-KANESHO Co., Ltd.Inventors: Shuichi Usui, Toshiki Fukuchi, Sachiko Kinoshita
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Publication number: 20120014997Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: September 26, 2011Publication date: January 19, 2012Inventors: Solomon Ungashe, J.J. Wright, Andrew Pennell, Zheng Wei, Anita Melikan
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Publication number: 20110313000Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: August 30, 2011Publication date: December 22, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20110281894Abstract: The present invention relates to a hemifumarate salt of the compound (1S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine, Form A thereof and its pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Downs syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.Type: ApplicationFiled: May 11, 2011Publication date: November 17, 2011Applicant: ASTRAZENECA ABInventors: Per-Olov Bergström, Anna Minidis, Robert Ulf Johan Stranne, Mikael Wernersson
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Patent number: 8008302Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: July 25, 2005Date of Patent: August 30, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110201610Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.Type: ApplicationFiled: March 10, 2011Publication date: August 18, 2011Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
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Patent number: 7989634Abstract: The present invention relates a compound of formula 1, and pharmaceutically acceptable salt, hydrate, solvate, or isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.Type: GrantFiled: November 12, 2004Date of Patent: August 2, 2011Assignees: LG Life Sciences Ltd., Yamanouchi Pharmaceutical Co., Ltd.Inventors: Koo Lee, Heui-Sul Park, In-Ae Ahn, Hyun-Ju Yoo, Jong-Yup Kim, Deog-Young Choi, Hyeon-Joo Yim, Kyung-Ha Chung, Dong-Sup Shim, Sang-Kyun Lee, Yutaka Kondoh, Ryoji Hirabayashi, Shugo Honda, Hidetaka Kaku, Jun-ichi Shishikura, Hiroyuki Ito, Takeshi Kurama
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Publication number: 20110152326Abstract: This invention provides a compound of the formula (I): (I) These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor, such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.Type: ApplicationFiled: March 15, 2006Publication date: June 23, 2011Inventors: Takeshi Hanazawa, Satoshi Nagayama, Kazumari Nakao, Hirotaka Tanaka
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Patent number: 7964735Abstract: Novel 3-acylaminobenzanilides of the formula (I) wherein R1 represents phenyl which may be substituted or a 5-member or 6-member heterocyclic ring group, which may be substituted, containing at least one hetero-atom selected from the group consisting of N, O, and S; R2 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl, or C1-6 haloalkylsulfonyl; R4 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; X represents halogen, C1-6 alkyl, or C1-6 haloalkyl; and n represents 0 or 1 and the compounds are used as insecticides, and a use of the new compounds as insecticides.Type: GrantFiled: July 21, 2006Date of Patent: June 21, 2011Assignee: Bayer Cropscience AGInventors: Akihiko Yanagi, Yukiyoshi Watanabe, Katsuaki Wada, Tetsuya Murata, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
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Patent number: 7932252Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.Type: GrantFiled: May 12, 2005Date of Patent: April 26, 2011Assignee: ChemoCentryx, Inc.Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
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Publication number: 20110021523Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: CHEMOCENTRYX, INC.Inventors: Solomon Ugashe, Zheng Wei, J.J. Wright, Andrew Pennell
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Publication number: 20100324093Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: August 26, 2010Publication date: December 23, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20100292252Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 31, 2008Publication date: November 18, 2010Inventor: Shoujun Chen
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Publication number: 20100273835Abstract: The invention provides compounds of general formula (I) or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are described throughout the description and claims. The compounds of the present invention are useful as inhibitors of prolyl endopeptidase (PEP, EC 3.4.21.26) and/or IL-6.Type: ApplicationFiled: July 10, 2008Publication date: October 28, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Andre J. Niestroj, Ingo Schulz
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Patent number: 7799954Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.Type: GrantFiled: November 14, 2007Date of Patent: September 21, 2010Assignee: Abraxis BioScience, LLCInventors: Chunlin Tao, Qinwei Wang, Vuong Trieu, Neil Desai, Patrick Soon-Shiong
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Publication number: 20100234364Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 10, 2007Publication date: September 16, 2010Inventors: Arindrajit Basak, Jeff Jin, Jimmie Moore, Andrew M.K. Pennell, Sreenlvas Punna, Solomon Ungashe, Zheng Wei
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Patent number: 7795441Abstract: Process for preparing imine compounds, in which a carbonyl compound is reacted with a primary amine. The imine compound obtained in this way can be reacted further with a metalalkyl and subsequently a carbonyl compound to form an imine compound.Type: GrantFiled: January 12, 2007Date of Patent: September 14, 2010Assignee: Basell Polyolefine GmbHInventor: Lars Kölling
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Patent number: 7700808Abstract: There is provided a novel process intermediate represented by the general formula (1) or (2): (where, X represents halogen atom, cyano group or the like, Y represents halogen atom, cyano group or the like, R1 represents C1-C6 haloalkyl group or C3-C8 halocycloalkyl group, R2 represents methyl group, halogen atom, cyano group or the like, m represents an integer of 1 to 5, and n represents an integer of 1 to 4).Type: GrantFiled: December 25, 2006Date of Patent: April 20, 2010Assignee: Nissan Chemical Industries, Ltd.Inventors: Takashi Mizukoshi, Yasuhiro Sakurai, Kazutaka Matoba, Manabu Yaosaka
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Publication number: 20100093707Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji NAKAMURA, Masayuki Morita, Tetsuo Yoneda, Kenji Izakura
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Publication number: 20100063045Abstract: Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof.Type: ApplicationFiled: March 28, 2008Publication date: March 11, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hasashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20100056786Abstract: The present invention relates to a novel process for preparing known fungicidally active alkylanilides from 2-alkylhaloaromatics and heterocyclylamides.Type: ApplicationFiled: July 12, 2007Publication date: March 4, 2010Applicant: Bayer CropScience AGInventor: Alexander Straub
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Publication number: 20090318473Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: ApplicationFiled: February 11, 2009Publication date: December 24, 2009Inventors: Jean-Michel Altenburger, Valerie Fossey, Gilbert Lassalle, Frederic Petit, Jean Claude Vernieres, Philip Janiak
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Publication number: 20090270616Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 7, 2009Publication date: October 29, 2009Applicant: CHEMOCENTRYX, INCInventors: Solomon Ugashe, Zheng Wei, J.J. Wright, Andrew Pennell