Plural Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 546/197)
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Patent number: 11498896Abstract: The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.Type: GrantFiled: March 20, 2020Date of Patent: November 15, 2022Assignees: The Broad Institute, Inc., Massachusetts Institute of TechnologyInventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Edward Scolnick, Michelle Palmer, Luka Dordevic, Michael C. Lewis, Jennifer Q. Pan, Yan-Ling Zhang, Qihong Xu
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Patent number: 11299482Abstract: The present invention provides a salt and crystal form of a modified andrographolide compound and a preparation method and pharmaceutical use thereof.Type: GrantFiled: May 24, 2018Date of Patent: April 12, 2022Assignees: Medshine Discovery, Inc., Heilongjiang Zhenbaodao Pharmaceutical Co, LTDInventors: Jianhua Xia, Zhigan Jiang, Haiying He, Jing Wang
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Patent number: 10829466Abstract: A stilbene derivative, which is a compound of the following general formula I or general formula II, or an acceptable salt formed by the compound of the general formula I or the general formula II and an inorganic or organic acid; wherein, in the general formula I or the general formula II, the atom represented by X is a hydrogen atom or a halogen atom; the substituent represented by R is C1-C6 alkyl, 1-6-membered heteroalkyl, C2-C4 alkenyl, C2-C4 alkynyl, C3-C6 cycloalkyl, substituted C3-C6 cycloalkyl, 3-6-membered heterocycloalkyl, substituted 3-6-membered heterocycloalkyl, 5-18-membered aryl, substituted 5-18-membered aryl, 5-18-membered heteroaryl, or substituted 5-18-membered heteroaryl.Type: GrantFiled: October 26, 2016Date of Patent: November 10, 2020Assignee: BEIJING INSTITUTE OF TECHNOLOGYInventors: Jianhua Liang, Hong Qing, Si Wu, Sisi Liu, Nuomin Li, Liang Yang
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Patent number: 10717720Abstract: The present disclosure discloses a modified compound of andrographolide, and particularly discloses a compound shown in formula (I) and (II) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 22, 2016Date of Patent: July 21, 2020Assignees: Heilongjiang Zhenbaodao Pharmaceutical Co., Ltd., Medshine Discovery Inc.Inventors: Haiying He, Zhigan Jiang, Jianhua Xia, Jing Wang, Lixia Han, Lihong Lan, Hui Zhou, Kunmin Lai, Shuhui Chen
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Patent number: 9777002Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.Type: GrantFiled: November 22, 2013Date of Patent: October 3, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Shawn P. Walsh, Brian Cato, Jessica L. Frie, Dooseop Kim, Alexander Pasternak, Zhi-Cai Shi
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Patent number: 9315483Abstract: The present invention provides a convenient and efficient process for the synthesis of d2-benzo[d][1,3]dioxoles.Type: GrantFiled: July 24, 2014Date of Patent: April 19, 2016Assignee: Concert Pharmaceuticals, Inc.Inventors: Andrew D. Jones, Robert E. Zelle, I. Robert Silverman
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Publication number: 20150133444Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.Type: ApplicationFiled: November 10, 2014Publication date: May 14, 2015Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
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Publication number: 20150105354Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLCInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
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Publication number: 20150094304Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: December 11, 2014Publication date: April 2, 2015Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
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Publication number: 20150080364Abstract: Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.Type: ApplicationFiled: March 15, 2013Publication date: March 19, 2015Applicants: Abide Therapeutics, Inc., The Scripps Research InsitituteInventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Dong-Hui Wang, Olivia Weber, Benjamin F. Cravatt, Micah J. Niphakis, Armand Cognetta, Jae Won Chang
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Publication number: 20150057278Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein Cy1, Cy2, n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.Type: ApplicationFiled: September 10, 2012Publication date: February 26, 2015Inventors: Dan Littman, Jun R. Huh, Ruili Huang, Wenwei Huang, Erika E. Englund
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Publication number: 20150031725Abstract: Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases.Type: ApplicationFiled: October 2, 2014Publication date: January 29, 2015Inventors: Richard J. Pietras, Michael E. Jung, Diana C. Marquez-Garban, Gang Deng
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Publication number: 20150025070Abstract: The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.Type: ApplicationFiled: July 13, 2012Publication date: January 22, 2015Applicant: Novartis AGInventors: Atwood Kim Cheung, Donovan Noel Chin, Jianmei Fan, Karen Marie Miller-Moslin, Michael David Shultz, Troy D. Smith, Ronald Charles Tomlinson, Bakary-Barry Toure, Michael Scott Visser
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Publication number: 20150018335Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: January 7, 2013Publication date: January 15, 2015Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
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Patent number: 8912199Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: October 21, 2013Date of Patent: December 16, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Publication number: 20140336387Abstract: The present invention provides a convenient and efficient process for the synthesis of d2-benzo[d][1,3]dioxoles.Type: ApplicationFiled: July 24, 2014Publication date: November 13, 2014Applicant: CONCERT PHARMACEUTICALS, INC.Inventors: Andrew D. Jones, Robert E. Zelle, I. Robert Silverman
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Patent number: 8865741Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.Type: GrantFiled: February 18, 2012Date of Patent: October 21, 2014Assignee: Asana Biosciences, LLCInventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
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Publication number: 20140309418Abstract: Gambogenic acid derivatives having a structure shown as Formula (I) or (II), salts, preparation method and application thereof in the treatment of tumor. Compared with gambogenic acid, the gambogenic acid derivatives exhibit more potent anti-tumor activities.Type: ApplicationFiled: September 28, 2012Publication date: October 16, 2014Inventors: Wantao Chen, Xu Wang, Zhiyuan Zhang, Chenping Zhang, Li Mao, Ping Zhang, Qin Xu, Ming Yan, Jianjun Zhang, Jinsong Pan, Yan Lv, Rongxin Deng, Weiliu Qiu
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Patent number: 8846947Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: July 2, 2009Date of Patent: September 30, 2014Assignee: GlaxoSmithKline LLCInventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Publication number: 20140288081Abstract: Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Giovanni Cianchetta, Janeta Popovici-Muller, Robert Zahler, Sheldon Cao, Xiaolei Wang, Zhixiong Ye
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Publication number: 20140256935Abstract: The present invention relates to naphthopyran compounds that include at least one compound represented by the following Formulas (I), (II), and (III): With reference to Formulas (I), (II), and (III), there is the proviso that: (i) at least one R1 is a group L; and/or (ii) B and/or B? is substituted with at least one group L. The group L can be described as a lengthening group. The present invention also relates to photochromic-dichroic naphthopyran compounds and photochromic-dichroic articles containing such compounds.Type: ApplicationFiled: March 11, 2013Publication date: September 11, 2014Applicant: Transitions Optical, Inc.Inventors: Darrin R. Dabideen, Meng He, Anil Kumar
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Patent number: 8822498Abstract: The present invention provides a convenient and efficient process for the synthesis of d2-benzo[d][1,3]dioxoles.Type: GrantFiled: September 12, 2008Date of Patent: September 2, 2014Assignee: Concert Pharmaceuticals, Inc.Inventors: Andrew D. Jones, Robert E. Zelle, I. Robert Silverman
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Patent number: 8809536Abstract: Compounds of formula I wherein X, Z, R1-R4, and m are as defined in the claims, exhibit alpha2C antagonistic activity, and are thus useful as alpha2C antagonists. Methods for the treatment of diseases and conditions of the peripheric system and the central nervous system are also disclosed.Type: GrantFiled: February 27, 2014Date of Patent: August 19, 2014Assignee: Orion CorporationInventors: David Din Belle, Patrik Holm, Arto Karljalainen, Arto Tolvanen, Gerd Wohlfahrt, Petteri Rummakko
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Patent number: 8791275Abstract: Psoralen compounds of Formula (I): wherein (N+ Aryl) is a member selected from the group consisting of nitrogen containing aromatic heterocycles of formulae (i)-(iii): wherein Z is a group of formula: wherein R is C1-C30 hydrocarbyl, which may be linear, branched or cyclic and contains from 1 to 15 carbon-carbon double bonds, which may be conjugated or unconjugated with one another or may include an aryl ring, and may contain one or more substituents; R1 is hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, alkene-aryl, alkene-heteroaryl, alkene-heterocyclyl, alkene-cycloalkyl, fused cycloalkylaryl, fused cycloalkylheteroaryl, fused heterocyclylaryl, fused heterocyclyheteroaryl, alkylene-fused cycloalkylaryl, alkylene-fused cycloalkylheteroaryl, alkylene-fused heterocyclylaryl, alkylene-fused heterocyclyheteroaryl; n is an integer from 1 to 8 and X is a pharmaceutically acceptable counter ion; and their use in methods for the treatment of a cell proliferatType: GrantFiled: January 11, 2013Date of Patent: July 29, 2014Assignees: Duke University, Immunolight, LLCInventors: Eric Toone, David Gooden, Tuan Vo-Dinh, Frederic A. Bourke, Jr.
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Patent number: 8772318Abstract: This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.Type: GrantFiled: November 10, 2009Date of Patent: July 8, 2014Assignee: The Scripps Research InstituteInventors: Benjamin F. Cravatt, Jonathan Z. Long, Weiwei Li, Daniel K. Nomura
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Publication number: 20140187581Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.Type: ApplicationFiled: January 5, 2012Publication date: July 3, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Suresh Yarlagadda, Srinivasa Rao Ravella, Anil Karbhari Shinde, Ramasastri Kamphampati, Praveen Kumar Roayapalley, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Sriramachandra Murthy Patnala, Jyothsna Ravula, Venkateswarlu Jasti
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Publication number: 20140179926Abstract: Compounds of formula I wherein X, Z, R1-R4, and m are as defined in the claims, exhibit alpha2C antagonistic activity, and are thus useful as alpha2C antagonists. Methods for the treatment of diseases and conditions of the peripheric system and the central nervous system are also disclosed.Type: ApplicationFiled: February 27, 2014Publication date: June 26, 2014Applicant: ORION CORPORATIONInventors: David DIN BELLE, Patrik HOLM, Arto KARLJALAINEN, Arto TOLVANEN, Gerd WOHLFAHRT, Petteri RUMMAKKO
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Patent number: 8759520Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterized by abnormal cell growth and/or dysregulated apoptosis.Type: GrantFiled: December 8, 2009Date of Patent: June 24, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotey, Smantha Jayne Bamford
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Publication number: 20140135310Abstract: Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with 5- or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; p, r independently represent 0 or 1; x, z independently represent 1 or 2; n is 2 or 3; and enancjomers, pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.Type: ApplicationFiled: June 29, 2012Publication date: May 15, 2014Applicant: Adamed Sp. z o.o.Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Maciej Pawlowski, Andrzej Krukowski, Rafal Rusiecki, Agata Magdalena Siwek, Malgorzata Anna Wolak
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Publication number: 20140121242Abstract: The present invention relates to substituted cinnamamide derivatives, the method for preparing thereof and the use thereof. Each of said derivatives has a structure of formula (I). The method for preparing the substituted cinnamamides and their derivatives of the present invention is also disclosed. Substituted piperonal derivatives are selected as starting materials to prepare the substituted cinnamamide derivatives of the present invention by Wittig reaction and acid-amine condensation reaction. Further, a use of the present compounds in preventing and treating depressive-type mental diseases is disclosed.Type: ApplicationFiled: June 26, 2012Publication date: May 1, 2014Applicant: TASLY PHARMACEUTICAL GROUP CO., LTD.Inventors: Xiaohui Ma, Yuanpeng Jin, Min Han, Shuiping Zhou, Wangyi Zhou, Xuejun Luo, Guocheng Wang, Lulu Yan, Lanlan Zhang, Yonghong Zhu
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Publication number: 20140094493Abstract: A compound of Formula (I), and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein R1 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4alkyl, C1-4alkoxy, CONH2 (optionally mono- or di-substituted by C1-4alkyl) and SO2NH2, R2 is independently selected from C1-6allkyl substituted by R3 wherein the C1-6alkyl chain optionally comprises one or two heteroatoms select from O; R3 is selected from aryl, C3-6cycloalkyl, C3-6heterocyclyl and C3-6heteroaryl, wherein the heterocyclyl and heteroaryl rings are nitrogen containing; and wherein R3 is optonally substituted by one or more groups selected from R1; n1 is zero or an integer from 1 to 2; n2 is an integer from 1 to 2; and the sum of n1 and 2 is less than or equal to 2; R5 is selected from any group defined for R1 and R2; R6a and R6b are independently selected from H or C1-4alkyl; R7 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4alType: ApplicationFiled: February 6, 2012Publication date: April 3, 2014Inventors: Jillian G. Baker, Peter M. Fischer, Christophe Fromont, Sheila M. Gardiner, Stephen J. Hill, Gopal Jadhav, Barrie Kellam, Shailesh Mistry, Jeanette Woolard
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Patent number: 8686028Abstract: The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substitutedType: GrantFiled: May 14, 2009Date of Patent: April 1, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Atul Goel, Amit Kumar, Sumit Chaurasia, Divya Singh, Abnish Kumar Gautam, Rashmi Pandey, Ritu Trivedi, Man Mohan Singh, Naibedya Chattopadhyay, Lakshmi Manickavasagam, Girish Kumar Jain, Anil Kumar Dwivedi
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Publication number: 20140080826Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: September 25, 2013Publication date: March 20, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: SARA SABINA HADIDA RUAH, Peter Diederik Jan Grootenhuis, Frederick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason Mc Cartney, Mehdi Numa, Xiaoqing Yang
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Publication number: 20140073669Abstract: Provided are 4?-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: November 18, 2013Publication date: March 13, 2014Inventors: Alexander L. RUCHELMAN, George W. Muller, Hon-Wah Man, Roger Shen-Chu Chen
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Patent number: 8648071Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.Type: GrantFiled: June 26, 2009Date of Patent: February 11, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Joseph Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
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Publication number: 20140018342Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.Type: ApplicationFiled: April 4, 2012Publication date: January 16, 2014Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
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Publication number: 20140011996Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).Type: ApplicationFiled: August 29, 2013Publication date: January 9, 2014Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Lingyun Zhang, Nagasree Chakka, MIchael Edward Grimwood, Jason Tan, Yuanxi Zhou
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Publication number: 20130345195Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. 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: August 23, 2013Publication date: December 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Michael J. BURKE, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Anil Kumar PADYANA, Lana Louise SMITH KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, QIANG ZHANG, Qing ZHANG
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Patent number: 8614232Abstract: An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.Type: GrantFiled: September 14, 2012Date of Patent: December 24, 2013Assignee: Novartis AGInventors: Dierk Wieckhusen, Alexandra Glausch, Markus Ahlheim
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Publication number: 20130323203Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: August 2, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman Belmont, Philip Anthony Morganelli, William J. Watkins
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Patent number: 8598357Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: February 27, 2012Date of Patent: December 3, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8598181Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: July 2, 2010Date of Patent: December 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Publication number: 20130296366Abstract: The present invention relates to novel isomers of a metabolite of Iloperidone, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.Type: ApplicationFiled: October 26, 2012Publication date: November 7, 2013Inventors: Dominique Grimler, Hans O. Kalkman, Hequn Yin
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Patent number: 8541453Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: May 20, 2011Date of Patent: September 24, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Publication number: 20130244996Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. 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: March 5, 2013Publication date: September 19, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael J. BURKE, Suresh R. KAPADIA, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Hossein RAZAVI, Sonia RODRIGUEZ, Anjan SAHA, Robert SIBLEY, Lana Louise SMITH-KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, Jiang-Ping WU, Erick Richard Roush YOUNG, Qiang ZHANG, Qing ZHANG, Renee M. ZINDELL
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Patent number: 8513285Abstract: There are disclosed racemic or enantiomerically enriched 3- or 4-substituted piperidine compounds represented by the following structural formula (I): or any of their isomers, or pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions containing the subject compounds. The subject compounds are useful for the treatment of diseases of the central nervous system, particularly depression, anxiety and pain disorder.Type: GrantFiled: January 19, 2012Date of Patent: August 20, 2013Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Ki-Ho Lee, Chun-Eung Park, Kyung-Hyan Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu
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Publication number: 20130196973Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. 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: March 13, 2012Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
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Patent number: 8492549Abstract: Compounds of formula I wherein X, Z, R1-R4, and m are as defined in the claims, exhibit alpha2C antagonistic activity, and are thus useful as alpha2C antagonists. Methods for the treatment of diseases and conditions of the peripheric system and the central nervous system are also disclosed.Type: GrantFiled: July 18, 2008Date of Patent: July 23, 2013Assignee: Orion CorporationInventors: David Din Belle, Patrik Holm, Arto Karljalainen, Arto Tolvanen, Gerd Wohlfahrt, Petteri Rummakko
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Patent number: 8492407Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: May 17, 2012Date of Patent: July 23, 2013Assignee: Theravance, Inc.Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
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Publication number: 20130178471Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: February 28, 2013Publication date: July 11, 2013Applicant: Vextex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated