The Five-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/368)
  • Patent number: 10336745
    Abstract: A two-photon absorbing (TPA) compound is provided along with a method of making same. The TPA compound has a general structural formula: where R1 and R2 are independently selected from the group consisting of linear or branched alkyl chains having a general formula CnH2n+1, n ranges from about 6 to about 20, and ethoxylated alkyls having a general formula R3(OCH2CH2)mOCH2CH2—, where R3 is a C1 to C4 alkyl group, and where m ranges from 0 to about 3; and where Y is selected from the group consisting of H, OH, and alkoxyl groups.
    Type: Grant
    Filed: March 2, 2018
    Date of Patent: July 2, 2019
    Assignee: The United States of America as represented by the Secretery of the Air Force
    Inventors: Loon-Seng Tan, Zhenning Yu
  • Patent number: 9580414
    Abstract: The present invention relates to a novel salt of (3aR,4S,7R,7aS)-2-[((1R,2R)-2-{[4-(1,2-benzisothiazol-3-yl)-piperazin-1-yl]methyl}cyclohexyl)methyl]hexahydro-1H-4,7-methanisoindol-1,3-dione and hydrates thereof, to methods for preparing the novel salt and its hydrates. In one aspect, the present invention provides a compound which is lurasidone dihydrochloride. In another aspect, the present invention provides a process for preparation of lurasidone dihydrochloride comprising: (i) mixing lurasidone free base in an organic solvent system; (ii) subjecting step (i) mixture to acid proton source; and (iii) isolating compound of lurasidone dihydrochloride.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: February 28, 2017
    Assignee: Shasun Pharmaceuticals Limited
    Inventors: Vijayabaskar Veerappan, Srimurugan Sankareswaran, Sathish Kumar Raman Viswanathan, N. Subramanian
  • Patent number: 9388197
    Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, R5, n, m, p and X are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: July 12, 2016
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg, Simon Stamm
  • Patent number: 9040508
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: May 26, 2015
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Publication number: 20150133465
    Abstract: The invention provides compounds of formula (I): wherein R1-R3, n, and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Yongzheng Zhang, Malvika Kaul
  • Publication number: 20150126515
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Application
    Filed: January 25, 2013
    Publication date: May 7, 2015
    Applicant: PTC Therapeutics, Inc.
    Inventors: Guangming Chen, Amal Dakka, Gary Mitchell Karp, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Marla L. Weetall, Ellen Welch, Xin Zhao
  • Publication number: 20150119380
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
    Type: Application
    Filed: December 28, 2012
    Publication date: April 30, 2015
    Inventors: Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
  • Patent number: 9018213
    Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: April 28, 2015
    Assignees: Huazhong University of Science & Technology, NHWA Pharma. Corporation
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Minquan Yu, Yinli Qiu
  • Publication number: 20150105397
    Abstract: The present inventions relate to substituted piperazine derivatives of general formula (I) and to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various medical conditions related to glycine transporter-1 (GlyT1).
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christoph HOENKE, Riccardo GIOVANNINI, Uta LESSEL, Holger ROSENBROCK, Bernhard SCHMID
  • Patent number: 8999990
    Abstract: 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 act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
  • Patent number: 8999991
    Abstract: 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 act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Barbara Pio, Harry R. Chobanian
  • Patent number: 8999992
    Abstract: The invention relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: April 7, 2015
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Publication number: 20150094297
    Abstract: The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 2, 2015
    Inventors: Jacques Banville, Roger Rèmillard, Edward H. Ruediger, Daniel H. Deon, Marc Gagnon, Laurence Dubé, Julia Guy, Eldon Scott Priestley, Shoshana L. Posy, Brad D. Maxwell, Pancras C. Wong, R. Michael Lawrence, Michael M. Miller
  • Patent number: 8993575
    Abstract: The present invention belongs to the medicinal chemistry field, and specifically discloses a [1,3,4]oxadiazole derivative with the structure of general formula (I) and pharmaceutically acceptable salt thereof. The compound can be used to prepare a medicine for preventing or treating a disease of the central nervous system.
    Type: Grant
    Filed: April 1, 2012
    Date of Patent: March 31, 2015
    Assignees: Huazhong University of Science & Technology, NHWA Pharma Corporation
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Bifeng Liu, Xiaojun Feng, Song Zhao, Shicheng Liu, Minquan Yu, Yu Lan, Yinli Qiu
  • Publication number: 20150087830
    Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 26, 2015
    Inventors: Nobuyuki AE, Yuji FUJIWARA
  • Publication number: 20150080383
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 19, 2015
    Inventors: Tianle Yang, Gary Mitchell Karp, Hongyan Qi
  • Patent number: 8981095
    Abstract: The present invention relates to a process for the preparation of Lurasidone or a pharmaceutically acceptable salt thereof, a compound useful for the treatment of schizophrenia and bipolar disorder. The present invention further relates to processes for the preparation of Lurasidone intermediates, and to certain novel intermediates obtained by such processes.
    Type: Grant
    Filed: June 13, 2012
    Date of Patent: March 17, 2015
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Michael Mizhiritskii, Susanna Tchilibon, Shai Rubnov
  • Patent number: 8962607
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: February 24, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J Connolly, Christopher Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark M McDonnell, Philip M Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Publication number: 20150018339
    Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Application
    Filed: February 21, 2014
    Publication date: January 15, 2015
    Inventors: Christopher R. MCCURDY, Christophe Mesangeau, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem, Frederick T. Chin, Jacques Henri Poupaert
  • Publication number: 20150018368
    Abstract: The present invention discloses process for preparing benzisothiazol-3-yl-piperazin-1-yl-methyl-cyclo hexyl-methan-isoindol-1,3-dione and intermediates thereof.
    Type: Application
    Filed: February 12, 2013
    Publication date: January 15, 2015
    Inventors: Shri Prakash Dhar Dwivedi, Ramesh Chandra Singh, Rajendra Gokalbhai Chavda
  • Patent number: 8921551
    Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: December 30, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Nobuyuki Ae, Yuji Fujiwara
  • Patent number: 8921552
    Abstract: Compounds of general formula A useful as potential anticancer agents against human cancer cell lines and a process for the preparation thereof.
    Type: Grant
    Filed: August 2, 2013
    Date of Patent: December 30, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Adla Mallareddy, Paidakula Suresh, Rajesh V. C. R. N. C. Shetti, Harish Chandra Pal, Ajit Kumar Saxena
  • Publication number: 20140371204
    Abstract: The invention relates to compounds of Formula (I) wherein ring A, X, (R1)n, R2, R3, R4, R4?, R5, n, and p are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.
    Type: Application
    Filed: February 1, 2013
    Publication date: December 18, 2014
    Inventors: Eva Caroff, Marcel Keller, Thierry Kimmerlin, Emmanuel Meyer
  • Publication number: 20140350029
    Abstract: Dosage regimens for at least one compound chosen from Iurasidone and pharmaceutically acceptable salts, solvates, clathrates, and stereoisomers thereof are disclosed as are kits and methods for treatment and/or prevention of at least one CNS disorder such as, for example, mixed depression and bipolar disorder, and management of at least one CNS disorder, such as improving quality of life and reversing impairment in learning and memory associated with schizophrenia, comprising administering to a patient a therapeutically or prophylactically effective amount of at least one compound chosen from lurasidone and pharmaceutically acceptable salts, solvates, clathrates, and stereoisomers thereof.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 27, 2014
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventor: Antony D Loebel
  • Publication number: 20140350012
    Abstract: The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-
    Type: Application
    Filed: August 11, 2014
    Publication date: November 27, 2014
    Inventors: Jean-Pierre Andre Marc Bongartz, Lieven Meerpoel, Maria Gustaaf Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
  • Patent number: 8895558
    Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: November 25, 2014
    Assignee: Green Cross Corporation
    Inventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
  • Publication number: 20140336200
    Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Applicant: ADAMED SP. Z O.O.
    Inventors: Marcin KOŁACZKOWSKI, Piotr KOWALSKI, Jolanta Jaskowska, Monika MARCINKOWSKA, Katarzyna MITKA, Adam BUCKI, Anna WESOŁOWSKA, Maciej PAWŁOWSKI
  • Patent number: 8883833
    Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 11, 2014
    Assignee: Decode Genetics EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
  • Patent number: 8883794
    Abstract: A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1?R,2?S,3?R,4?S)-2,3-bicyclo[2,2,1]-heptanedicarboxylmide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied.
    Type: Grant
    Filed: February 18, 2014
    Date of Patent: November 11, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventor: Kazuyuki Fujihara
  • Publication number: 20140329831
    Abstract: The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.
    Type: Application
    Filed: June 3, 2014
    Publication date: November 6, 2014
    Inventors: Jin LI, Rifang Yang, Rui Song, Hui Zhu, Ning Wu, Liuhong Yun, Ruibin Su, Rusheng Zhao
  • Publication number: 20140323467
    Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Application
    Filed: May 23, 2014
    Publication date: October 30, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
  • Publication number: 20140303143
    Abstract: Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Mark E. Layton, Joseph E. Pero, Hannah Fiji, Michael J. Kelly, III, Pablo de Leon, Michael A. Rossi, Kevin F. Gilbert, Anthony J. Roecker, Zhijian Zhao, Swati I P. Mercer, Scott Wolkenberg, James Mulhearn, Lianyun Zhao, Dansu Li
  • Patent number: 8853395
    Abstract: Disclosed is a new and efficient process for the synthesis with high yields and purity of lurasidone hydrochloride, a medicament which is useful as a psychotropic substance. The process involves the preparation of lurasidone base in a reaction system not containing inorganic salts, followed by conversion of the latter to an addition salt with an organic carboxylic acid, which is finally converted to lurasidone hydrochloride.
    Type: Grant
    Filed: February 20, 2014
    Date of Patent: October 7, 2014
    Assignee: Edmond Pharma S.R.L.
    Inventors: Matteo Zacche', Fulvio Gerli, Pierandrea Gatti
  • Publication number: 20140296219
    Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.
    Type: Application
    Filed: November 14, 2013
    Publication date: October 2, 2014
    Applicant: UNIVERSITY OF MASSACHUSETTS
    Inventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
  • Publication number: 20140296225
    Abstract: 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 act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Application
    Filed: October 22, 2012
    Publication date: October 2, 2014
    Inventors: Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
  • Publication number: 20140288045
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
  • Publication number: 20140288088
    Abstract: 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 act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 25, 2014
    Inventors: Haifeng Tang, Barbara Pio, Harry R. Chobanian
  • Publication number: 20140288302
    Abstract: A pharmaceutical composition including a compound of formula (I): its pharmaceutically acceptable salt, or a solvate thereof. Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by formula: —C(R1R2)—C(?O)—NR3R4 and a group represented by formula: —R5, a broken line represents presence or absence of a bond, Z is —NR6—, ?N—, —O—, or —S—, R6 is halogen or substituted or unsubstituted alkyl, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen or substituted or unsubstituted alkyl, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.
    Type: Application
    Filed: March 18, 2014
    Publication date: September 25, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Koji MASUDA, Shiro KIDA, Kyohei HAYASHI, Manabu KATOU, Naoki YOSHIKAWA, Akira KUGIMIYA, Mado NAKAJIMA, Nobuyuki TANAKA
  • Publication number: 20140275113
    Abstract: The invention relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Patent number: 8835437
    Abstract: The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p—; C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-m
    Type: Grant
    Filed: June 5, 2008
    Date of Patent: September 16, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Pierre André Marc Bongartz, Lieven Meerpoel, Gustaaf Maria Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
  • Publication number: 20140256939
    Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 11, 2014
    Applicant: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Nobuyuki AE, Yuji FUJIWARA
  • Patent number: 8829001
    Abstract: The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: September 9, 2014
    Assignee: The Institute of Pharmacology and Toxicology Academy of Military Medical Science P.L.A. China
    Inventors: Jin Li, Rifang Yang, Rui Song, Hui Zhu, Ning Wu, Liuhong Yun, Ruibin Su, Rusheng Zhao
  • Patent number: 8822698
    Abstract: Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: September 2, 2014
    Assignees: Universite d'Aix-Marseille, Universite de Lorraine, Oreste Piccolo Studio di Consulenza Scientifica, Universitat de Barcelona, Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Flavio Maina, Rosanna Dono, Oreste Piccolo, Daniele Passarella, Francesco Colombo, Joan Bosch, Bernard Maigret, Vincent Leroux
  • Publication number: 20140243529
    Abstract: Disclosed is a new and efficient process for the synthesis with high yields and purity of lurasidone hydrochloride, a medicament which is useful as a psychotropic substance. The process involves the preparation of lurasidone base in a reaction system not containing inorganic salts, followed by conversion of the latter to an addition salt with an organic carboxylic acid, which is finally converted to lurasidone hydrochloride.
    Type: Application
    Filed: February 20, 2014
    Publication date: August 28, 2014
    Applicant: EDMOND PHARMA s.r.l.
    Inventors: Matteo ZACCHE', Fulvio GERLI, Pierandrea GATTI
  • Patent number: 8815839
    Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: August 26, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Kristen Chevalier, Jose Clemente, Scott L Dax, Chris Flores, Li Liu, Mark J Macielag, Mark McDonnell, Marina Nelen, Erica Nulton, Stephen Prouty, Matthew Todd, Sui-Po Zhang, Bin Zhu
  • Patent number: 8809530
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF recptor TrkA.
    Type: Grant
    Filed: April 18, 2014
    Date of Patent: August 19, 2014
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Publication number: 20140221653
    Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Applicant: Alkermes Pharma Ireland Limited
    Inventors: Laura Cook Blumberg, Julius F. Remenar, Orn Almarsson, Tarek A. Zeidan
  • Patent number: 8791111
    Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in Claim (1), can and be employed for the treatment of tumors.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: July 29, 2014
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
  • Patent number: 8778948
    Abstract: The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate, wherein C1 and C2 represent chiral carbon atoms, and the compound is one of the six isomers: (1RS, 2SR), (1RS, 2RS), (1R, 2S), (1S, 2S), (1R, 2R) or (1S, 2R); and R, R1, R2, R3 and Ar are as defined in the specification. The derivative is non-opioid analgesic, has good analgesic effect and relatively small side effects. The invention also relates to a composition comprising the derivative and its use.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: July 15, 2014
    Assignee: NHWA Pharma, Corporation
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Xiangping Yang, Peng Xie, Linjie Zhang, Xiangqing Xu, Yumei Wang
  • Patent number: 8772285
    Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: July 8, 2014
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Florencio Zaragoza Dorwald, Inge Thoger Christensen