Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/65)
  • Patent number: 8993617
    Abstract: The present invention directed to a method of treating multiple myeloma with the following compound: or a pharmaceutically acceptable salt thereof. The compound is a novel small molecule inhibitor of Ire1.
    Type: Grant
    Filed: November 8, 2011
    Date of Patent: March 31, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Albert C. Koong, Ioanna Papandreou
  • Patent number: 8946286
    Abstract: A novel organic amine salt or salt with quaternary ammonium ion of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid having useful properties as a drug is provided. A novel organic amine or salt with quaternary ammonium ion of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid, a method for producing the organic amine salt or the salt with quaternary ammonium ion and a platelet increasing agent.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: February 3, 2015
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Shunsuke Iwamoto, Satoshi Nakano, Mariko Ishida, Masao Yamamoto, Kazuya Takeuchi
  • Publication number: 20150024032
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 22, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
  • Patent number: 8916183
    Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Lindsey G. Fischer, Gary D. Crouse, Thomas C. Sparks, Erich W. Baum
  • Patent number: 8889732
    Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: November 18, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • Publication number: 20140303377
    Abstract: An object of the present invention is to provide insecticides having high effectiveness.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 9, 2014
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba, Atsuko Kawahara
  • Patent number: 8822467
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 2, 2014
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
  • Publication number: 20140235702
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having sulfonamido-1-hydroxynaphthalene structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Application
    Filed: October 8, 2012
    Publication date: August 21, 2014
    Inventors: Zaneta Nikolovska-Coleska, Hollis D. Showalter, Chenzhong Liao, Ramzi Mohammad, Fardokht Abulwerdi
  • Publication number: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Patent number: 8765797
    Abstract: Methods and compounds for treating cancer, dmg resistance and/or metastasis are described herein. These methods and compounds can inhibit the expression of aberrant TG2 expression and/or inhibit the binding of GTP to TG2, and thereby prevent the induction of epithelial to mesenchymal transition of cancer cells, and a stem cell-like phenotype.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: July 1, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventors: Kapil Mehta, Anupam Kumar, Jansina Fok, Shuxing Zhang
  • Publication number: 20140113941
    Abstract: This invention provides a compound having the structure wherein R1 is H, wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is wherein m is an integer from 0 to 8; R3 is an amino, alkyl, aryl, heteroaryl, diol, piperazine, morpholine, piperidine, triazole, azide or biphenyl, each with or without substitution, branched or unbranched, or and R4 is alkyl, aryl, or heteroaryl, each with or without substitution, branched or unbranched, R2 is H, CH3, or alkyl, aryl, heteroaryl, pyrrole, diazole, or triazole, each with or without substitution, branched or unbranched, or wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is and R6 is azide, methoxy, trifluoromethyl, biphenyl, substituted phenyl, substituted triazole, or alkyl, aryl or heteroaryl, with or without substitution, branched or unbranched, when R1 is H then R2 is other than H or CH3, and
    Type: Application
    Filed: March 23, 2012
    Publication date: April 24, 2014
    Applicant: The Research Foundation for The State University of New York
    Inventors: Peter Tonge, Carl Machutta, Gopal Reddy Bommineni, Kanishk Kapilashrami
  • Publication number: 20140107160
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: October 9, 2013
    Publication date: April 17, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20140088158
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
  • Publication number: 20140057953
    Abstract: The invention relates to selective, non-steroidal 17beta-hydroxysteroid dehydrogenase type 2 (l7beta-HSD2) inhibitors of formula (I), their production and use, notably for the treatment and prophylaxis of sex steroid deficient diseases like osteoporosis in men and women.
    Type: Application
    Filed: March 2, 2012
    Publication date: February 27, 2014
    Inventors: Rolf Hartmann, Sandrine Marchais-Oberwinkler, Kuiying Xu, Ruth Werth
  • Publication number: 20140051857
    Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: October 28, 2013
    Publication date: February 20, 2014
    Applicant: Nissan Chemical Industries Limited
    Inventors: Shingo OWADA, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
  • Publication number: 20140051682
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Patent number: 8652364
    Abstract: A polymer film comprising at least one compound represented by formula (I) is disclosed. A1 and A2 each independently represent a group having a Hammett's ?p value of 0.2 or more, or bond each other to form a cyclic active methylene structure; and X1 and X2 each independently represent a hydrogen atom, aryl group, hetero-cyclic group, cyano, N-alkyl- or N-aryl-carbamoyl, or alkyl- or aryl-oxycarbonyl, or bond each other to form a saturated ring in which nitrogen and carbon atoms are embedded, and the group and ring may have at least one substituent.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: February 18, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Shunya Katoh, Hiroko Kamee
  • Publication number: 20140031394
    Abstract: Provided is a novel cyclic sulfonium salt compound which is useful for the prevention or treatment of diabetes and the like. The present invention relates to a novel cyclic sulfonium salt compound represented by general formula (I) or (II), an isomer or solvate of the compound, or a pharmaceutically acceptable salt of the compound or the isomer or solvate. The present invention also relates to an ?-glucosidase inhibitor, a pharmaceutical composition for preventing or treating diabetes, and an anti-diabetes food, each of which comprises the compound represented by general formula (I) or (II) and the like.
    Type: Application
    Filed: January 31, 2012
    Publication date: January 30, 2014
    Applicants: DIABETYM CO., LTD., KINKI UNIVERSITY
    Inventors: Osamu Muraoka, Genzoh Tanabe
  • Publication number: 20140031331
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: September 19, 2013
    Publication date: January 30, 2014
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
  • Publication number: 20140024608
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Application
    Filed: March 14, 2013
    Publication date: January 23, 2014
    Applicant: METHYLGENE INC.
    Inventors: Robert Deziel, Alain Ajamian
  • Publication number: 20130345196
    Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.
    Type: Application
    Filed: May 24, 2012
    Publication date: December 26, 2013
    Inventors: Alfred L. WILLIAMS, John Scott, Li-An Yeh, Matthew Robert Redinbo
  • Publication number: 20130345235
    Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. Glucuronidase inhibitors described include phenoxy thiophene sulfonamides. Other compounds, for instance pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls, are also contemplated. Also contemplated are compositions including one or more of such compounds for use inhibiting glucuronidase and methods of using one or more of such compounds as a co-drug to be used in combination with the anticancer drug CPT-11.
    Type: Application
    Filed: March 10, 2011
    Publication date: December 26, 2013
    Applicants: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, NORTH CAROLINA CENTRAL UNIVERSITY
    Inventors: Alfred L. Williams, John Scott, Li-An Yeh, Matthew Robert Redinbo
  • Publication number: 20130324409
    Abstract: The present invention provides methods of regulating plant stress tolerance.
    Type: Application
    Filed: March 14, 2013
    Publication date: December 5, 2013
    Inventors: SEAN R. CUTLER, ANDREW DEFRIES
  • Publication number: 20130303599
    Abstract: Activation of the adaptive Ire1-XBP1 pathway has been identified in many solid tumors and hematological malignancies, including multiple myeloma (MM). What is disclosed is STF-083010, a novel small molecule inhibitor of Ire1. STF-083010 inhibited Ire1 endonuclease activity, without affecting its kinase activity, after ER stress both in vitro and in vivo. Treatment with STF-083010 showed significant anti-myeloma activity in model human MM xenografts. Similarly, STF-083010 was preferentially toxic to freshly isolated human CD138(+) MM cells when compared to other similarly isolated cell populations. The identification of this novel Ire1 inhibitor supports the hypothesis that the Ire1-XBP1 axis is a promising target for anti-cancer therapy, especially in the context of multiple myeloma.
    Type: Application
    Filed: November 8, 2011
    Publication date: November 14, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Albert C. Koong, Ioanna Papandreou
  • Patent number: 8563763
    Abstract: The present invention relates to isonitrile compounds, methods of synthesis, and uses in a variety of fields. In one aspect, the present invention includes sulfinyl methyl isonitriles and methods for their preparation. In another aspect, the present invention includes the use of sulfinyl methyl isonitriles to prepare various other isonitrile compounds and derivatives thereof. In yet another aspect, the present invention includes a relatively simple and routine synthesis of sulfinyl methyl isonitrile compounds, other isonitrile compounds and derivatives thereof.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: October 22, 2013
    Assignee: Duquesne University of the Holy Ghost
    Inventors: Fraser Ferguson Fleming, Bhaskar Reddy Pitta
  • Publication number: 20130225619
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 29, 2013
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Publication number: 20130217894
    Abstract: A novel organic amine salt or salt with quaternary ammonium ion of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid having useful properties as a drug is provided. A novel organic amine or salt with quaternary ammonium ion of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid, a method for producing the organic amine salt or the salt with quaternary ammonium ion and a platelet increasing agent.
    Type: Application
    Filed: November 1, 2011
    Publication date: August 22, 2013
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Shunsuke Iwamoto, Satoshi Nakano, Mariko Ishida, Masao Yamamoto, Kazuya Takeuchi
  • Publication number: 20130190338
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 11, 2013
    Publication date: July 25, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130183252
    Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
    Type: Application
    Filed: February 10, 2012
    Publication date: July 18, 2013
    Applicant: Senomyx, Inc.
    Inventors: Xiaodong LI, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
  • Publication number: 20130165460
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: February 20, 2013
    Publication date: June 27, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130158087
    Abstract: Methods and compounds for treating cancer, dmg resistance and/or metastasis are described herein. These methods and compounds can inhibit the expression of aberrant TG2 expression and/or inhibit the binding of GTP to TG2, and thereby prevent the induction of epithelial to mesenchymal transition of cancer cells, and a stem cell-like phenotype.
    Type: Application
    Filed: June 21, 2011
    Publication date: June 20, 2013
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Kapil Mehta, Anupam Kumar, Jansina Fok, Shuxing Zhang
  • Patent number: 8440854
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: May 14, 2013
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Melean Visnick
  • Patent number: 8440844
    Abstract: A high-yielding enantioselective synthesis of the bioactive (S)—N-(5-chlorothiophene-2-sulfonyl)-?,?-diethylalaniol (7.b.2), a Notch-1-sparing ?-secretase inhibitor metabolite (with EC50=28 nM) effective in reduction of A? production in vivo, has been realized starting from readily available 3-pentanone. The key steps of the synthesis are proline-catalyzed ?-aminooxylation and ?-amination of aldehyde; the latter contributing an overall yield of 50-75% and 90-99% enantiomeric excess.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: May 14, 2013
    Assignee: Council of Scientific & Industrial Research
    Inventors: Varun Rawat, Pandurang Vilasrao Chouthaiwale, Vilas Bhiku Chavan, Gurunath Mallappa Suryavanshi, Arumugam Sudalai
  • Publication number: 20130102609
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Application
    Filed: December 14, 2012
    Publication date: April 25, 2013
    Applicant: LIGAND PHARMACEUTICALS INC.
    Inventor: Ligand Pharmaceuticals Inc.
  • Publication number: 20130012708
    Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 10, 2013
    Applicant: Nissan Chemical Industries Limited
    Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
  • Publication number: 20120330031
    Abstract: A high-yielding enantioselective synthesis of the bioactive (S)—N-(5-chlorothiophene-2-sulfonyl)- ?,?-diethylalaniol (7.b.2), a Notch-1-sparing ?-secretase inhibitor metabolite (with EC50=28 nM) effective in reduction of A? production in vivo, has been realized starting from readily available 3-pentanone. The key steps of the synthesis are proline-catalyzed ?-aminooxylation and ?-amination of aldehyde; the latter contributing an overall yield of 50-75% and 90-99% enantiomeric excess.
    Type: Application
    Filed: October 13, 2011
    Publication date: December 27, 2012
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Varun Rawat, Pandurang Vilasrao Chouthaiwale, Vilas Bhiku Chavan, Gurunath Mallappa Suryavanshi, Arumugam Sudalai
  • Patent number: 8269023
    Abstract: An improved process for synthesis of duloxetine hydrochloride (1) having chiral purity greater than 99.9% that is characterized by the following: (i) preparation of racemic condensed compound (RS)—N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (4) by reaction of racemic hydroxy compound (2) with 1-fluoronaphthalene (3) in presence of a base such as sodamide, potassium amide or potassium bis(trimethylsilyl)amide (KHDMS) in polar aprotic solvent, (ii) optical resolution of racemic condensed compound (5a+5b) with di-benzoyl-L-tartaric acid (7, DBTA, R=H) or di-para-anisoyl-L-tartaric acid (7, DATA, R=OCH3) to obtain crude (S)—N.N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine dibenzoyl tartarate salt (8a) or (S)—N.
    Type: Grant
    Filed: March 5, 2008
    Date of Patent: September 18, 2012
    Assignee: Lupin Ltd.
    Inventors: Rajinder Singh Siyan, Sunil Kumar Vinubhai Gohel, Girij Pal Singh
  • Publication number: 20120209005
    Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: October 22, 2010
    Publication date: August 16, 2012
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • Publication number: 20120196884
    Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).
    Type: Application
    Filed: June 14, 2010
    Publication date: August 2, 2012
    Applicant: BIOTIE THERAPIES CORPORATION
    Inventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
  • Publication number: 20120149909
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Application
    Filed: December 21, 2011
    Publication date: June 14, 2012
    Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
  • Publication number: 20120142917
    Abstract: Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl4. The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.
    Type: Application
    Filed: September 6, 2011
    Publication date: June 7, 2012
    Applicants: H. Lee Moffitt Cancer Center and Research Institute, Inc., UNIVERSITY OF SOUTH FLORIDA
    Inventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
  • Publication number: 20120128640
    Abstract: An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy useful for treatment of various disorders is provided. An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells containing a compound represented by the formula (I) (wherein X, Y, Z, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof, which can expand hematopoietic stem cells and/or hematopoietic progenitor cells.
    Type: Application
    Filed: June 4, 2010
    Publication date: May 24, 2012
    Applicant: NISSAN CHEMICAL INDUSTRIES LTD.
    Inventors: Taito Nishino, Shunsuke Iwamoto, Katsuaki Miyaji
  • Publication number: 20120095219
    Abstract: The present invention refers to the preparation and purification of brinzolamide as well as to novel compounds useful in such processes.
    Type: Application
    Filed: March 12, 2010
    Publication date: April 19, 2012
    Applicant: Azad Pharmaceutical Ingredients AG
    Inventors: Arul Ramakrishnan, Anil Kumar Soni, Sujit Das Adhikari, Kommula Srinivasa Rao, Soumendu Paul, Ganta Srinivasulu
  • Publication number: 20120095012
    Abstract: The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.
    Type: Application
    Filed: December 30, 2009
    Publication date: April 19, 2012
    Applicant: Elara Pharmaceuticals GmbH
    Inventors: Jorge Alonson, Arantxa Encinas Lopez, Marcel Muelbaier, Jochen Ammenn, Bernd Wendt, Joe Lewis, Christoph Schultes, Bernd Janssen
  • Publication number: 20120064062
    Abstract: Organic compounds showing the ability to inhibit bacterial omptin proteases, specifically Yersinia pestis plasminogen activator (Pla) are disclosed. The disclosed Y. pestis plasminogen activator inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by Y. pestis.
    Type: Application
    Filed: September 13, 2011
    Publication date: March 15, 2012
    Inventors: Jon D. Goguen, Daniel Aiello, Donald T. Moir, Bing Li
  • Patent number: 8088925
    Abstract: The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.
    Type: Grant
    Filed: November 15, 2007
    Date of Patent: January 3, 2012
    Assignee: Sanofi-Aventis
    Inventors: Michael Wagner, Matthias Urmann, Volkmar Wehner, Martin Lorenz, Armin Bauer, Marc Nazare, Hans Matter
  • Publication number: 20110319416
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-E, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
    Type: Application
    Filed: January 28, 2010
    Publication date: December 29, 2011
    Applicant: EMORY UNIVERSITY
    Inventors: Stephen F. Traynelis, Dennis C. Liotta, Cara Mosley, Timothy M. Acker, Sommer Zimmerman
  • Publication number: 20110313000
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: August 30, 2011
    Publication date: December 22, 2011
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Publication number: 20110306614
    Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
    Type: Application
    Filed: August 19, 2011
    Publication date: December 15, 2011
    Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Patent number: RE45314
    Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: December 30, 2014
    Assignees: The Johns Hopkins University, Cardioxyl Pharmaceuticals, Inc.
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish