Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 548/171)
  • Publication number: 20150045401
    Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.
    Type: Application
    Filed: March 15, 2013
    Publication date: February 12, 2015
    Inventors: Garry Robert Smith, Allen B. Reitz, Mark McDonnell, Suzie Chen, Matthew Douglas Vera, Benjamin Eric Blass, Jeffrey Claude Pelletier, Venkata Naga Velvadapu, Jay Edward Wrobel
  • Publication number: 20150031685
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 29, 2015
    Applicant: Dr. Reeddy's Laboratories Ltd.
    Inventors: Pradip Kumar Sasmal, Chintakunta Vamseekrishna, Vijay Potluri, Ashok Tehim, Yonghua Gai, Hang Zhang
  • Patent number: 8940900
    Abstract: Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.
    Type: Grant
    Filed: February 25, 2008
    Date of Patent: January 27, 2015
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Kasim A. Mookhtiar, Debnath Bhuniya, Bhavesh Dave, Gobind S. Kapkoti, Sujay Basu, Anita Chugh, Siddhartha De, Venkata P. Palle
  • Publication number: 20130040999
    Abstract: The present invention provides novel compounds of Chemical Formula I, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, a preparation thereof and a composition for the alleviation, prevention or treatment of osteoporosis, comprising thereof in an effective amount, and a method for alleviating, preventing or treating osteoporosis.
    Type: Application
    Filed: June 14, 2012
    Publication date: February 14, 2013
    Applicant: Ewha University-Industry Collaboration Foundation
    Inventors: Hea-Young PARKCHOO, Kyung-Eun Doh, Mijung Yim, Jung-Min Lee
  • Publication number: 20130005701
    Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
    Type: Application
    Filed: January 27, 2012
    Publication date: January 3, 2013
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Röhrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
  • Publication number: 20120329775
    Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: June 4, 2012
    Publication date: December 27, 2012
    Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
  • Publication number: 20120330009
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: July 16, 2012
    Publication date: December 27, 2012
    Inventors: Weiwen Ying, David James, Shijie Zhang, Teresa Przewloka, Junghyun Chae, Dinesh U. Chimmanamada, Chi-Wan Lee, Elena Kostik, Howard P. Ng, Kevin Foley, Zhenjian Du, James Barsoum
  • Patent number: 8299266
    Abstract: A process for making aziridinyl epothilone compounds according to formula G, starting from a compound according formula C where R1, R2, R3, R4, R5, R6, R12, R13, Z1 and Z2 in formulae (G) and (C) are as defined herein. The aziridinyl epothilone compounds of formula (G) are useful for the treatment of cancer.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: October 30, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Luca Parlanti, Jurong Yu
  • Publication number: 20120129893
    Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
    Type: Application
    Filed: January 12, 2012
    Publication date: May 24, 2012
    Inventors: Jacques DUMAS, Uday Khire, Timothy B. Lowinger, Holger Paulsen, Bernd Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, Holia Hatoum-Mokdad, Jeffrey Johnson, Wendy Lee, Aniko Redman, Robert Sibley, Joel Renick
  • Publication number: 20120122889
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (I)-(I), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: December 23, 2009
    Publication date: May 17, 2012
    Applicant: President and Fellows of Harvard College
    Inventors: Junying Yuan, Emily S. Hsu
  • 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
  • Patent number: 8044078
    Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: October 25, 2011
    Assignee: Sanofi-Aventis
    Inventors: Agnes Pappne Behr, Zoltan Kapui, Peter Aranyi, Sandor Batori, Veronika Bartane Bodor, Lajos T. Nagy, Mihalyne Santa, legal representative, Marton Varga, Endre Mikus, Katalin Urban-Szabo, Judit Vargane Szeredi, Tibor Szabo, Edit Susan, Marianna Kovacs
  • Publication number: 20110251200
    Abstract: The invention provides to a family of aryl guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.
    Type: Application
    Filed: September 11, 2009
    Publication date: October 13, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Gary D. Glick, Peter Toogood, Gina Ney
  • Publication number: 20110212467
    Abstract: Evidence demonstrating that elevated expression of dUTPase protects breast cancer cells from the expansion of the intracellular uracil pool, translating to reduced growth inhibition following treatment with 5-FU is provided. The implementation of in silica drug development techniques to identify and develop small molecule inhibitors of dUTPase are reported. As 5-FU and the oral 5-FU pro-drug capecitabine remain central agents in the treatment of a variety of malignancies, the clinical utility of a small molecule inhibitor to dUTPase represents a viable strategy to improve the clinical efficacy of these mainstay chemotherapeutic agents.
    Type: Application
    Filed: August 27, 2009
    Publication date: September 1, 2011
    Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Robert D. Ladner, Nouri Neamati
  • Patent number: 7960369
    Abstract: The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.
    Type: Grant
    Filed: November 6, 2003
    Date of Patent: June 14, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kohji Fukatsu, Shinobu Sasaki, Shuji Hinuma, Yasuaki Ito, Nobuhiro Suzuki, Masataka Harada, Tsuneo Yasuma
  • Publication number: 20110053910
    Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
    Type: Application
    Filed: July 3, 2006
    Publication date: March 3, 2011
    Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
  • Publication number: 20110009448
    Abstract: A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.
    Type: Application
    Filed: July 23, 2010
    Publication date: January 13, 2011
    Inventors: Nigel Vicker, Su Xiangdong, Dharshini Ganeshapillai, Atul Purohit, Michael John Reed, Barry Victor Lloyd Potter
  • Publication number: 20100286118
    Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: May 6, 2010
    Publication date: November 11, 2010
    Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
  • Publication number: 20100267689
    Abstract: The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Application
    Filed: April 15, 2010
    Publication date: October 21, 2010
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui
  • Publication number: 20100256130
    Abstract: The present invention relates to morpholinyl, and pyrrolidinyl analogs, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
    Type: Application
    Filed: May 19, 2010
    Publication date: October 7, 2010
    Inventors: Krista B. Goodman, Michael J. Neeb, Clark A. Sehon, Andrew Q. Viet, Gren Z. Wang
  • Publication number: 20100240656
    Abstract: The invention provides novel compounds of formula (I) wherein: one of the a, b, c or d members is a nitrogen atom and the remaining members are carbon atoms; and R3 is a radical selected from the group consisting of: —S—R14 and —CH2—R15. The compounds of formula (I) are useful for treating diseases mediated by a heat shock protein 90 (Hsp 90).
    Type: Application
    Filed: July 9, 2008
    Publication date: September 23, 2010
    Applicant: ORYZON GENOMICS, S.A.
    Inventors: Marc Martinell Pedemonte, Isabel Navarro Muñoz, Montserrat Soler López, David Mormeneo Julián, Malgorzata Rosol, Amadeo Llebaria Soldevila, Juan Aymami Bofarull
  • Publication number: 20100137274
    Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
    Type: Application
    Filed: June 30, 2009
    Publication date: June 3, 2010
    Applicant: Bayer Schering Pharma AG
    Inventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
  • Publication number: 20100130737
    Abstract: The present invention provides a GPR receptor function regulator comprising the compound represented by the formula: [wherein ring A is an optionally substituted isocyclic or heterocyclic ring, P is a bond or spacer, ring D is an optionally substituted monocyclic aromatic ring which may be condensed with a 5- to 7-membered ring, V is a bond or the group represented by the formula —CR14?CR15— or —N?CR16— (wherein R14, R15 and R16 each represents a hydrogen atom or optionally substituted hydrocarbon group), Q is a bond or spacer, and W is a carboxyl or a group biologically equivalent to a carboxyl] or its salt or a prodrug thereof.
    Type: Application
    Filed: February 17, 2006
    Publication date: May 27, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Fumio Itoh, Eiji Kimura, Yumi Imai, Masaaki Mori, Yoshio Aramaki, Yasuhisa Kohara, Tsukasa Sugo, Yoji Hayase, Hiromi Kobayashi, Kazuhiro Ogi
  • Patent number: 7723366
    Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to the use of compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, the invention relates to the use of compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the following formulae: (I) and (II) Wherein Y, C, R1, R2, R6, and R7 are defined herein.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: May 25, 2010
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Thomas Arrhenius, Jie Fei Cheng, Mark E. Wilson, Rossy Serafimov, Masahiro Nishimoto, David Mark Wallace, Sovouthy Tith, Steve Joel Brown, Charles Stanford Harmon, Gary D. Lopaschuk, Jason R. Dyck
  • Patent number: 7709511
    Abstract: The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4, R5, R6, R7, R7a, R7b, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: May 4, 2010
    Assignee: AstraZeneca AB
    Inventors: Roger Bonnert, Alice Flaherty, Garry Pairaudeau, Michael Stocks
  • Publication number: 20100022491
    Abstract: The present invention provides compounds of formula (I) (A chemical formula should be inserted here—please see paper copy enclosed herewith) wherein Ra, Rb, R1, R2, R3, R4, R5, R6 and R29 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: December 19, 2007
    Publication date: January 28, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Stephen Connolly, Alexander Humphries, Premji Meghani
  • Patent number: 7625889
    Abstract: The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: December 1, 2009
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Paul Robert Eastwood, Hazel Hunt, David Mark Fink, Helen Katherine Smith, Richard Simon Todd
  • Publication number: 20090239917
    Abstract: Compounds of formula (I): wherein: R1 represents a (C3-C8)cycloalkyl group, R2 represents a group of formula (II) as defined in the description, X represents an oxygen atom or an N—OR? group wherein R? represents a hydrogen atom, a linear or branched (C1-C6)alkyl group, an aryl group or an aryl-(C1-C6)alkyl group in which the alkyl moiety may be linear or branched. Medicinal products containing the same which are useful as hypoglycaemic and hypolipaemic agents.
    Type: Application
    Filed: March 5, 2007
    Publication date: September 24, 2009
    Applicant: Les Laboratoires Servier
    Inventors: Aurelie Hurtevent, Jean-Martial L'Helgoual'ch, Pascal Carato, Nicolas Lebegue, Veronique Leclerc, Morgan Le Naour, Pascal Berthelot, Catherine Dacquet, Alain Ktorza, Daniel-Henri Caignard
  • Publication number: 20090203753
    Abstract: The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4?, R5?, R6, R7, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: August 28, 2006
    Publication date: August 13, 2009
    Applicant: AstraZeneca AB
    Inventors: Andrew Bailey, Roger Bonnert, Alice Flaherty, Garry Pairaudeau, Michael Stocks
  • Publication number: 20090143229
    Abstract: Synthesis and herbicidal activity of novel 1-(2-substituted benzo[d]thiazol-5-yl)-1H-1,2,4-triazol-5(4H)-one derivatives. Using a dose of 300 gai./h, the compounds of the invention possess significant herbicidal activity for Echinochloa crusgalli, Digiatria sanguinalis, Setaria viridis, Brassica juncea, Amaranthus retroflexus and Chenopodium album.
    Type: Application
    Filed: December 2, 2008
    Publication date: June 4, 2009
    Inventors: Guangfu YANG, Yanping LUO, Zuming LIU
  • Publication number: 20080300275
    Abstract: The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4, R5, R6, R7, R7a, R7b, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: August 3, 2006
    Publication date: December 4, 2008
    Applicant: ASTRAZENECA AB
    Inventors: Roger Bonnert, Alice Flaherty, Garry Pairaudeau, Michael Stocks
  • Publication number: 20080280961
    Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.
    Type: Application
    Filed: March 19, 2008
    Publication date: November 13, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Agnes PAPPNE BEHR, Zoltan KAPUI, Peter ARANYI, Sandor BATORI, Veronika BARTANE BODOR, Lajos T. NAGY, Mihalyne Santa, Marton VARGA, Endre MIKUS, Katalin URBAN-SZABO, Judit VARGANE SZEREDI, Tibor SZABO, Edit SUSAN, Marianna KOVACS
  • Publication number: 20080269265
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: June 25, 2008
    Publication date: October 30, 2008
    Inventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, Bernd Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, David Gunn, Martha Rodriguez, Ming Wang, Tiffany Turner, Catherine Brennan
  • Publication number: 20080207698
    Abstract: The present invention provides compounds of formula (I) wherein Ra, Rb, R1, R2, R3, R4, R5, R6 and R29 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: December 19, 2007
    Publication date: August 28, 2008
    Inventors: Stephen Connolly, Alexander Humphries, Premji Meghani
  • Publication number: 20080161358
    Abstract: The present invention provides previous methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.
    Type: Application
    Filed: October 2, 2007
    Publication date: July 3, 2008
    Inventors: Mark D. Kafka, Mark E. Wilson, Anna Russell, Gary D. Lopaschuk, Jason R. Dyck
  • Publication number: 20080161370
    Abstract: The invention relates to benzothiazol-2-one derivatives of general formula (I) with the meanings indicated in the description, the pharmaceutically usable salts thereof, and the use thereof as medicinal substances.
    Type: Application
    Filed: December 5, 2007
    Publication date: July 3, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard Zoller, Stefan Petry, Gunter Muller, Hubert Heuer, Norbert Tennagels
  • Patent number: 7125863
    Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.
    Type: Grant
    Filed: April 26, 2001
    Date of Patent: October 24, 2006
    Assignee: Ferring BV
    Inventors: David Michael Evans, Gary Robert William Pitt
  • Patent number: 6825223
    Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: wherein Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or an oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NR6—; R4 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: November 30, 2004
    Assignee: Kowa Company, Ltd.
    Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Souhei Tanabe, Masami Shiratsuchi
  • Patent number: 6713477
    Abstract: A hydroxamic acid derivative represented by formula (1) or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which has a matrix metalo-proteinase inhibitor.
    Type: Grant
    Filed: November 9, 2001
    Date of Patent: March 30, 2004
    Assignee: Sumitomo Pharmaceuticals Company, Limited
    Inventors: Gerard Robert Scarlato, Sara Sabina Hadida Ruah, Tamiki Nishimura, Masashi Nakatsuka, Fumio Samizo, Yumiko Kamikawa, Hitoshi Houtigai
  • Publication number: 20040029935
    Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
    Type: Application
    Filed: October 28, 2002
    Publication date: February 12, 2004
    Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
  • Patent number: 6603044
    Abstract: The present invention provides a phthalamide derivative of the formula (I): wherein A1 is (substituted) C1-C8 alkylene, (substituted) C3-C8 alkenylene, (substituted) C3-C8 alkynylene, etc., R1 is H, (halo) C3-C6 cycloalkyl, (substituted) phenyl, (substituted) heterocycle, —A2—R4, etc., R2 and R3 are H, C3-C6 cycloalkyl, —A2—R4, etc., A2 is —C(═O)—, —C(═S)— or —C(═NR5)—, R4 is H, alkyl, (substituted) phenyl, (substituted) heterocycle, etc., X and Y are halogen, cyano, nitro, (halo) C1-C6 alkyl, (halo) C1-C6 alkoxy, etc., l is 0-4, m is 0-5, n is 0-2; and an agrohorticultural insecticide containing said compound as active ingredient and exhibiting an excellent insecticidal effect.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: August 5, 2003
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Masanori Tohnishi, Hayami Nakao, Eiji Kohno, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka, Hideo Kanno
  • Patent number: 6596738
    Abstract: Heterocyclic compounds of the following formula: wherein B is  [wherein R1 is hydrogen or lower alkyl; R2 is hydrogen or lower alkyl; and X is hydrogen or hydroxy protective group], lower alkanoyl or hydroxyimino(lower)alkyl A is lower alkylene; W is heterocyclic or carbocyclic group, each of which may have one or more substituent(s); Z is heterocyclic group selected from the group consisting of imidazolyl, triazolyl,imidazopyridyl and adenyl, each of which may have one or more substituent(s); or a salt thereof, provided that when W is aryl which may have one or more substituent(s), then (i) Z is triazolyl, imidazopyridyl or adenyl, each of which may have one or more substituent(s); (ii) Z is imidazolyl which may have one or more substituent(s) and B is lower alkanoyl or hydroxyimino(lower)alkyl; or (iii) Z is imidazolyl which may have one or more substituent(s) and R1 and R2 are both lower alkyl.
    Type: Grant
    Filed: September 7, 2001
    Date of Patent: July 22, 2003
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Tadashi Terasaka, Nobuo Seki, Kiyoshi Tsuji, Isao Nakanishi, Takayoshi Kinoshita, Katsuya Nakamura
  • Patent number: 6569855
    Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 25, 2001
    Date of Patent: May 27, 2003
    Assignee: The Procter & Gamble Company
    Inventors: Michael George Natchus, Biswanath De, Stanislaw Pikul, Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Menyan Cheng
  • Patent number: 6518292
    Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably,  and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: February 11, 2003
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, James J. Li, Jun Li, Stephen G. Swartz
  • Patent number: 6472414
    Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X,  are as defined herein.
    Type: Grant
    Filed: May 18, 1999
    Date of Patent: October 29, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
  • Patent number: 6417219
    Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: July 9, 2002
    Assignee: The Proctor & Gamble Company
    Inventors: Michael George Natchus, Biswanath De, Stanislaw Pikul, Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Menyan Cheng
  • Patent number: 6362208
    Abstract: The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula: represents a divalent residue of benzene with a substituent(s), heterocycle-condensed benzene which may or may not have a substituent, pyridine which may or may not have a substituent, cyclohexane or naphthalene or Ar represents an aryl group which may or may not have a substituent; X represents —NH—, oxygen atom or sulfur atom; Y represents —NR4—, oxygen atom, sulfur atom, sulfoxide or sulfone; Z represents single bond or —NR5—; R4 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; R5 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; and n represents an integer of 0 to 15.
    Type: Grant
    Filed: December 6, 1999
    Date of Patent: March 26, 2002
    Assignee: Kowa Company, Ltd.
    Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Mitsuteru Hirata, Chiyoka Ozaki
  • Patent number: 6362138
    Abstract: This invention relates to compounds which are suitable as ash-free antiwear additives and antioxidants, to lubricant compositions comprising said compounds as well as to their use. are particularly preferred. In the preferred compounds I′, R2 is isooctyloxycarbonylmethyl, R3 is isooctyloxycarbonylmethylthiomethyl and R4 is hydrogen; or R2 is tert-nonyl and R3 is tert-nonylthiomethyl and R4 is hydrogen; or R2 is isooctyloxycarbonylmethyl, R3 is hydrogen and R4 is isooctyloxycarbonylmethylthiomethyl; or R2 is tert-nonyl, R3 is hydrogen and R4 I is tert-nonylthiomethyl.
    Type: Grant
    Filed: September 15, 2000
    Date of Patent: March 26, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Hugo Camenzind, Samuel Evans, Alfred Dratva, Peter Hänggi
  • Patent number: 6204278
    Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: where Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NH6—; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.
    Type: Grant
    Filed: May 19, 1997
    Date of Patent: March 20, 2001
    Assignee: Kowa Company, Ltd.
    Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Souhei Tanabe, Masami Shiratsuchi
  • Patent number: RE37303
    Abstract: A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as in the specification having antagonist properties to histamine H3-receptors.
    Type: Grant
    Filed: April 6, 2000
    Date of Patent: July 31, 2001
    Assignees: Institut National del la Sante et de la Recherche Medicale, Societe Civile Bioprojet
    Inventors: Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Jeanne-Marie Lecomte, Charon R. Ganellin, Abdellatif Fkyerat, Wasyl Tertiuk, Walter Schunack, Ralph Lipp, Holger Stark, Katja Purand