Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., 1,3- And 1,4- Benzothiazines, Etc.) Patents (Class 514/224.2)
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Publication number: 20140179690Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; R is monofluoromethyl or difluoromethyl; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: ApplicationFiled: January 19, 2012Publication date: June 26, 2014Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Mamoru Takaishi, Tasuku Ishida
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Publication number: 20140171363Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.Type: ApplicationFiled: February 24, 2014Publication date: June 19, 2014Applicant: NOVARTIS AGInventors: David Weninger BARNES, Gregory Raymond BEBERNITZ, Kevin CLAIRMONT, Scott Louis COHEN, Robert Edson DAMON, II, Robert Francis DAY, Stephanie Kay DODD, Christoph GAUL, Hatice Belgin GULGEZE EFTHYMIOU, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Kai LIN, Justin Yik Ching MAO, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, SU Liansheng
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Publication number: 20140171425Abstract: The invention relates to antibacterial compounds of formula (I), wherein R1 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; R2 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy or pyrrolidin-1-yl; R3 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy, vinyl or 2-methoxycarbonyvinyl or R2 and R3 together with the two carbon atoms which bear them form a phenyl ring; R4 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; and R5 is H, (C1-C3)alkyl or cyclopropyl, or R4 and R5 form together a —CH2CH2CH2— group; A is the divalent group —CH2—, —CH2CH2—, #—CH(OH)CH2—*, #—CH2N(R6)—* and —CH2NHCH2—, wherein # indicates the point of attachment to the optionally substituted (quinazoline-2,4-dione-3-yl)methyl residue and * represents the point of attachment to the substituted (oxazolidinon-4-yl)methyl residue; R6 is H or acetyl; Y is CH or N; and Q is O or S; and salts of such compounds.Type: ApplicationFiled: August 10, 2012Publication date: June 19, 2014Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
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Publication number: 20140163016Abstract: The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.Type: ApplicationFiled: December 11, 2013Publication date: June 12, 2014Applicant: NeurAxon, Inc.Inventors: Jailall RAMNAUTH, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
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Publication number: 20140163015Abstract: The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: December 10, 2013Publication date: June 12, 2014Applicant: Pfizer Inc.Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
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Publication number: 20140148431Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: ApplicationFiled: August 24, 2012Publication date: May 29, 2014Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawsar, Sachin Bhagwat, Mohammed Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
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Publication number: 20140142092Abstract: The disclosure provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one mixed EP2/EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.Type: ApplicationFiled: November 13, 2013Publication date: May 22, 2014Applicant: Allergan, Inc.Inventors: Robert M. Burk, Wha-Bin Im
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Publication number: 20140142093Abstract: The present invention relates to antibacterial compounds of formula (I) wherein “----” is a bond or is absent, V is CH, CR6 or N; R0 is H or, if “----” is a bond, may also be alkoxy; R1 is cyano, alkyl, or ethynyl; U is CH or N when “----” is a bond, or, if “----” is absent, U is CH2, NH or NH9; R2 is H, alkylcarbonyl or CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2, wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sType: ApplicationFiled: December 4, 2013Publication date: May 22, 2014Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian HUBSCHWERLEN, Daniel RITZ, Georg RUEEDI, Jean-Philippe SURIVET, Cornelia ZUMBRUNN-ACKLIN
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Publication number: 20140142091Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C?N; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: ApplicationFiled: October 18, 2013Publication date: May 22, 2014Applicant: Eisai R&D Management Co., Ltd.Inventors: Adrian Hall, Christopher Neil Farthing, Jose Luis Castro Pineiro
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Publication number: 20140142094Abstract: This disclosure relates to compounds, methods for their preparation, pharmaceutical compositions including these compounds and methods for the treatment of cellular proliferative disorders, including, but not limited to cancer. The method includes administering to the patient a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 30, 2012Publication date: May 22, 2014Applicant: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAIInventors: M.V. Ramana Reddy, E. Premkumar Reddy
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Publication number: 20140135318Abstract: Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: May 23, 2012Publication date: May 15, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Zhen-Wei Cai, Andrew J. Tebben, Heidi L. Perez, Liping Zhang, Gretchen M. Schroeder, Donna D. Wei
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Patent number: 8716280Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.Type: GrantFiled: January 21, 2010Date of Patent: May 6, 2014Assignee: Basilea Pharmaceutica AGInventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
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Patent number: 8703721Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 12, 2011Date of Patent: April 22, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Publication number: 20140107109Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.Type: ApplicationFiled: December 18, 2013Publication date: April 17, 2014Inventors: Richard T. LEWIS, Jennifer R. ALLEN, Yuan CHENG, Deborah CHOQUETTE, Oleg EPSTEIN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Zihao HUA, Randall W. HUNGATE, Jason Brooks HUMAN, Ted JUDD, Qingyian LIU, Patricia LOPEZ, Ana Elena MINATTI, Philip OLIVIERI, Karina ROMERO, Shannon RUMFELT, Robert M. RZASA, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE, Qiufen XUE, Xiao ZHENG, Wenge ZHONG
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Publication number: 20140094454Abstract: The present invention provides compounds of Formula I: wherein A is selected from the group consisting of; R1 is H or F; R2 is H, —CH2OH, C1-C3 alkyl, R3 is H, F, or CN; R4 is H, F; or CN; and R5 is H, —CH3, or —OCH3; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 4, 2013Publication date: April 3, 2014Applicant: Eli Lilly and CompanyInventors: James Peter BECK, Steven James GREEN, Jose Eduardo LOPEZ, Brian Michael MATHES, Dustin James MERGOTT, Warren Jaye PORTER, Zoran RANKOVIC, Yuan SHI, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR.
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Patent number: 8685963Abstract: The present invention relates to compounds with activity as BACE1 and NF?B modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds.Type: GrantFiled: April 26, 2011Date of Patent: April 1, 2014Assignee: The Trustees of Columbia University in the city of New YorkInventors: Donald W. Landry, Shi Xian Deng, Gangli Gong, Yuli Xie, Yidong Liu, K. Alison Rinderspacher
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Publication number: 20140086941Abstract: The present invention relates to compounds according to Formula I: and salts thereof, wherein R1, R2, R3, R4, Ar, and n are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.Type: ApplicationFiled: November 26, 2013Publication date: March 27, 2014Applicants: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI, TEMPLE UNIVERSITY - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATIONInventors: E. Premkumar Reddy, M. V. Ramana Reddy
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Publication number: 20140080770Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 17, 2013Publication date: March 20, 2014Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi MIYAZAKI, Junko OKABE, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAI, Tetsuya YANAGIDA, Yutaka HISADA
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Publication number: 20140080788Abstract: Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R3, R4, R4a, R5a, R5b, R5c, R5d, R5e, R6a, R6b, and R6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: April 27, 2012Publication date: March 20, 2014Inventors: Jeffrey A. Robl, Jun Li, Lawrence J. Kennedy, Steven J. Walker, Haixia Wang, William N. Washburn, Saleem Ahmad, Khehyong Ngu
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Patent number: 8658639Abstract: The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is —N(R1b)—, G2 is —CO—, G3 is —C(R1c)(R1d)—, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.Type: GrantFiled: June 24, 2010Date of Patent: February 25, 2014Assignee: Dainippon Sumitomo Pharma Co., LtdInventors: Satoshi Suetsugu, Nobuhisa Fukuda, Yoshio Nakai, Takashi Takada, Yohei Ikuma, Hiroyuki Nakahira
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Publication number: 20140031346Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is CR3, and A is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: ApplicationFiled: September 30, 2013Publication date: January 30, 2014Applicant: Anadys Pharmaceuticals, Inc.Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich
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Publication number: 20140031339Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein A1, A2, L1 and B are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: July 16, 2013Publication date: January 30, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael Jason BURKE, Thomas Martin KIRRANE, JR., Chuk Chui MAN, Daniel Richard MARSHALL, Anil Kumar PADYANA, Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Roger John SNOW, Ronald John SORCEK, Hidenori TAKAHASHI, Steven John TAYLOR, Michael Robert TURNER, Erick Richard Roush YOUNG, Qiang ZHANG, Yunlong ZHANG, Renee M. ZINDELL
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Patent number: 8629270Abstract: The present invention provides compounds of Formula I: wherein A is selected from the group consisting of; R1 is H or F; R2 is H, —CH2OH, C1-C3 alkyl, R3 is H, F, or CN; R4 is H, F; or CN; and R5 is H, —CH3, or —OCH3; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 27, 2013Date of Patent: January 14, 2014Assignee: Eli Lilly and CompanyInventors: Jose Eduardo Lopez, Dustin James Mergott
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Publication number: 20140011802Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein R is hydrogen or C1-6 alkyl, optionally substituted by one to five halogen atoms; n is 0, 1, 2 or 3; Ar is phenyl or a 5- or 6-membered heteroaromatic group containing 1, 2 or 3 N atoms, which Ar is optionally substituted by one to three substituents selected from hal, hydroxyl, —CN, C1-6alkyl, C2-3alkenyl, C2-3alkynyl,C-6alkoxy, C3-6cycloalkoxy and pyrazine, where C1-6alkyl and C1-6alkoxy are optionally substituted by one to three halogen atoms; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease 1 caused by A? and typified by Alzheimer-type dementia.Type: ApplicationFiled: January 5, 2012Publication date: January 9, 2014Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Paschalis Dimopoulos, Adrian Hall, Yoichi Kita, Andrew Madin, Nicola Louise Shuker
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Patent number: 8623818Abstract: The present invention relates to compounds of general formula (I), wherein ring A, ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: GrantFiled: May 13, 2009Date of Patent: January 7, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: William J. Greenlee, Andrew Stamford, Michael W. Miller, Duane Eugene DeMong
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Patent number: 8618092Abstract: The invention relates to antibacterial compounds of formula I wherein is a bond or is absent, V is CH, CR6 or N; R0 is H or, if is a bond, may also be alkoxy; R1 is notably H or halogen; U is CH or N when is a bond, or, if is absent, U is CH2, NH or NR9; R2 is H, alkylcarbonyl or —CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2 wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 orType: GrantFiled: October 6, 2009Date of Patent: December 31, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Daniel Ritz, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20130338151Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.Type: ApplicationFiled: October 21, 2010Publication date: December 19, 2013Applicant: Fibrotech Therapeutics Pty LtdInventors: Spencer John Williams, Steven Zammit, Darren James Kelly
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Publication number: 20130338152Abstract: The present invention provides a compound the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: March 8, 2012Publication date: December 19, 2013Applicants: IRM LLC, NOVARTIS AGInventors: Bei Chen, Robin Alec Fairhurst, Songchun Jiang, Wenshuo Lu, Thomas H. Marsilje, III, Clive McCarthy, Pierre-Yves Michellys, Stefan Stutz
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Publication number: 20130338142Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided.Type: ApplicationFiled: June 14, 2013Publication date: December 19, 2013Inventors: Peter A. BLOMGREN, Kevin S. CURRIE, Randall HALCOMB, Jeffrey E. KROPF, Seung H. LEE, Jiayao LI, Jennifer R. LO, Scott A. MITCHELL, Aaron SCHMITT, Qiaoyin WU, Jin-Min XIONG, Jianjun XU, Zhongdong ZHAO, Jayaraman CHANDRASEKHAR, Eric LANSDON
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Patent number: 8598161Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein R1, R2, R3, R4, R5, and R6 are independently hydrogen, C1-C6 alkyl or C1-C6 cycloalkyl; Y and Z are independently a C6-C10-aryl group or a 5-10 membered heterocyclic group, wherein each Y and Z group can be optionally substituted with from 0-3 substituents selected from halogen, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, OH, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is either a bond or is —NHCO—; L and Z together can be absent; and m is 1, 2 or 3.Type: GrantFiled: May 23, 2012Date of Patent: December 3, 2013Assignee: Bristol-Myers Squibb CompanyInventor: Yong-Jin Wu
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Patent number: 8592408Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C?N; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: GrantFiled: November 26, 2012Date of Patent: November 26, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Adrian Hall, Christopher Neil Farthing
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Publication number: 20130303512Abstract: This disclosure is directed, in part, to a method of determining whether a subject having cancer is at risk for developing metastasis of the cancer. In one embodiment, the method comprises (a) obtaining a biological sample from the subject having cancer; (b) determining CCR5 expression level and/or expression level of at least one of CCR5 ligands in the biological sample; and (c) if the expression level of CCR5 and/or of at least one of CCR5 ligands determined in step (b) is increased compared to CCR5 expression level and/or expression level of at least one of CCR5 ligands in a control sample, then the subject is identified as likely at risk for developing metastasis of the cancer.Type: ApplicationFiled: May 14, 2013Publication date: November 14, 2013Inventor: Richard G. PESTELL
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Publication number: 20130296308Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: May 3, 2013Publication date: November 7, 2013Applicant: Pfizer Inc.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
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Publication number: 20130274251Abstract: The present invention provides compounds of formula (1) acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as anti-cancer agents for preventions and treatments of PK- and RK-related disorders, in particular cancer. (I) wherein A is H or CN; Z is S, SO or S02; X1, X2, X3, X4, X5, Y1 and Y2 are each independently selected from H, halogen, alkyl, haloalkyl and OR1; and Y3 and Y4 are each OR1, wherein each R1 is independently H, C1-C4 alkyl, acyl, —(CH2CH20)n wherein n is an integer of 1 to 20, or a functional group that gives rise to hydroxyl upon hydrolysis.Type: ApplicationFiled: December 27, 2011Publication date: October 17, 2013Applicant: NOVOTYR THERAPEUTICS LTD.Inventors: Hadas Reuveni, Alexander Levitzki
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Publication number: 20130261111Abstract: The present invention provides compounds of Formula I: wherein A is selected from the group consisting of; R1 is H or F; R2 is H, —CH2OH, C1-C3 alkyl, R3 is H, F, or CN; R4 is H, F; or CN; and R5 is H, —CH3, or —OCH3; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 27, 2013Publication date: October 3, 2013Applicant: Eli Lilly and CompanyInventors: James Peter BECK, Steven James GREEN, Jose Eduardo LOPEZ, Brian Michael MATHES, Dustin James MERGOTT, Warren Jaye PORTER, Zoran RANKOVIC, Yuan SHI, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR
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Publication number: 20130261103Abstract: Pyridazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: August 31, 2011Publication date: October 3, 2013Applicants: GENENTECH, INC., GILEAD CONNECTICUT, INC.Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
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Publication number: 20130245007Abstract: The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria. (I).Type: ApplicationFiled: November 21, 2011Publication date: September 19, 2013Applicant: ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE (EPFL)Inventors: Vadim Makarov, Stewart Cole
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Publication number: 20130231333Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: September 15, 2011Publication date: September 5, 2013Applicant: ARAGON PHARMACEUTICALS, INC.Inventors: Nicholas D. Smith, Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Andiliy G. Lai, Jackaline D. Julien, Mark R. Herbert, Celine Bonnefous, Karensa L. Douglas
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Patent number: 8524707Abstract: 3,4-diaryl-bicyclicpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: December 17, 2009Date of Patent: September 3, 2013Assignee: Nerviano Medical Sciences S.r.l.Inventors: Maurizio Pulici, Chiara Marchionni, Claudia Piutti, Fabio Gasparri
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Patent number: 8507478Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is alkoxy or halogen; U and V each independently are CH or N; is a bond or is absent; W is CH or N or, when is absent, W is CH2 or NH, with the proviso that U, V and W are not all N; A is a bond or CH2; R2 is H or, provided A is CH2, may also be OH; m and n each independently are 0 or 1; D is CH2 or a bond; G represents a phenyl group substituted once or twice in the meta and/or para position(s) by substituents selected from alkyl, (C1-C3)alkoxy and halogen, or G is a group G1 or G2 wherein Z1, Z2 and Z3 may each represent CH or N; X is N or CH and Q is O or S; it being understood that if m and n each are 0, then A is CH2; and salts of such compounds.Type: GrantFiled: October 9, 2009Date of Patent: August 13, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20130203740Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C?N; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: ApplicationFiled: November 26, 2012Publication date: August 8, 2013Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventor: Eisai R&D Management Co., Ltd.
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Publication number: 20130203741Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: ApplicationFiled: March 14, 2013Publication date: August 8, 2013Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventor: EISAI R&D MANAGEMENT CO., LTD.
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Patent number: 8492111Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 7, 2010Date of Patent: July 23, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
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Patent number: 8461154Abstract: The present invention provides arylpiperazine derivatives having Formula I which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.Type: GrantFiled: May 7, 2012Date of Patent: June 11, 2013Assignee: Reviva Pharmaceuticals, Inc.Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
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Patent number: 8461133Abstract: The invention relates to a method for preparing a soluble inclusion complex comprising one or several active substances which are hardly soluble in an aqueous medium and are included in one or several host molecules, characterised in that it comprises the following succesive stages: (a) one or several active substances are brought into contact with one or several host molecules; (b) initiation of a molecular diffusion stage by bringing a dense pressurized fluid into contact with the mixture obtained in stage (a) in a static mode in the presence of one or several diffusing agents; (c) recovery of the active substance- host molecule molecular complex thus formed; (d) initiation of a stage wherein an interaction agent is added to and mixed with the active substance host molecule molecular complex; (e) recovery of the soluble inclusion compound thus formed. The invention also relates to the soluble inclusion compound which can be obtained by said method, particularly a piroxicam-cyclodextrin-arginine compound.Type: GrantFiled: March 29, 2005Date of Patent: June 11, 2013Assignee: Pierre Fabre MedicamentInventors: Bernard Freiss, Florence Marciaçq, Hubert Lochard
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Publication number: 20130131049Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein R1, R2, R3, R4, R5, and R6 are independently hydrogen, C1-C6 alkyl or C1-C6 cycloalkyl; Y and Z are independently a C6-C10-aryl group or a 5-10 membered heterocyclic group, wherein each Y and Z group can be optionally substituted with from 0-3 substituents selected from halogen, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, OH, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is either a bond or is —NHCO—; L and Z together can be absent; and m is 1, 2 or 3.Type: ApplicationFiled: May 23, 2012Publication date: May 23, 2013Inventor: Yong-Jin Wu
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Publication number: 20130131050Abstract: The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like. The present invention relates to a compound represented by the following formula: wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: July 22, 2011Publication date: May 23, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Nobuyuki Matsunaga, Hideo Suzuki, Kouhei Asano, Hidekazu Tokuhara, Takeshi Yamamoto, Rei Okamoto
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Patent number: 8440842Abstract: The present invention relates to compounds of Formula (I) or salts thereof wherein R1, R2, R3, R4, R5, R6, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.Type: GrantFiled: June 25, 2008Date of Patent: May 14, 2013Assignee: Leibniz-Institut fuer Naturstoff-Forschung und Infektionsbiologie e.V. Hans-Knoell-InstitutInventors: Ute Moellmann, Vadim Makarov, Cole T. Stewart
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Publication number: 20130109656Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: August 15, 2012Publication date: May 2, 2013Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robinson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtli
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Patent number: 8420634Abstract: Amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,1-4H-benzothiazines and 3-amino-1,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: and the use of the products and the corresponding pharmaceutical formulations for the treatment of neurodegenerative pathologies such as cerebral ischemia, neurodegeneration induced by cranial trauma, Alzheimer's disease, Multiple Sclerosis and Amyotrophic Lateral Sclerosis.Type: GrantFiled: September 22, 2008Date of Patent: April 16, 2013Assignee: Rottapharm S.p.A.Inventors: Maurizio Anzini, Antonio Giordani, Francesco Makovec, Andrea Cappelli, Salvatore Vomero, Gianfranco Caselli, Lucio Claudio Rovati