Ring In A Substituent E Patents (Class 564/174)
  • Patent number: 9162993
    Abstract: The present invention provides a biphenyl benzamide-derived derivatives, which structure is selected from formula I or formula II and the synthesis and the application thereof.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: October 20, 2015
    Assignee: National Defense Medical Center
    Inventors: Deh-Ming Chang, Hsu-Shan Huang, Chia-Chung Lee, Chun-Liang Chen
  • Publication number: 20140371232
    Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.
    Type: Application
    Filed: December 18, 2012
    Publication date: December 18, 2014
    Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
  • Publication number: 20140336378
    Abstract: Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventor: Doo Hyun Lee
  • Publication number: 20140219989
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 7, 2014
    Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
  • Patent number: 8778939
    Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
    Type: Grant
    Filed: September 27, 2010
    Date of Patent: July 15, 2014
    Assignee: Glaxo Group Limited
    Inventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
  • Patent number: 8692005
    Abstract: Provided are methods for decreasing the reaction time between an alkanolamine such as triethanolamine and a fatty acid alkyl ester such as, a triglyceride, a vegetable oil, a methyl ester, an ethyl ester, etc., a fatty acid, or a mixture thereof. The methods utilize a divalent zinc catalyst to facilitate and accelerate an esterification or transesterification reaction between the alkanolamine and the fatty acid, or fatty acid alkyl ester.
    Type: Grant
    Filed: August 15, 2012
    Date of Patent: April 8, 2014
    Assignee: Stepan Company
    Inventors: Marshall J. Nepras, Franz J. Luxem, Leonard F. Zaporowski, David Eisenberg
  • Publication number: 20130281412
    Abstract: The present invention provides a pharmaceutical composition of salicylanilide-derived small molecules include: (a) a compound which structure is selected from formula I or formula II: (b) a pharmaceutically acceptable salt and excipient. The present invention also provides the synthesis method of the pharmaceutical composition and the application thereof.
    Type: Application
    Filed: September 11, 2012
    Publication date: October 24, 2013
    Inventors: Deh-Ming CHANG, Hsu-Shan Huang, Chun-Liang Chen, Chia-Chung Lee
  • Publication number: 20130281444
    Abstract: The present invention provides a biphenyl benzamide-derived derivatives, which structure is selected from formula I or formula II: and the synthesis and the application thereof.
    Type: Application
    Filed: August 9, 2012
    Publication date: October 24, 2013
    Inventors: Deh-Ming CHANG, Hsu-Shan HUNAG, Chia-Chung LEE, Chun-Liang CHEN
  • Publication number: 20130129626
    Abstract: The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.
    Type: Application
    Filed: December 18, 2012
    Publication date: May 23, 2013
    Applicants: HAMMERSMITH IMANET LIMITED, GE HEALTHCARE LIMITED
    Inventors: GE Healthcare Limited, Hammersmith Imanet Limited
  • Publication number: 20120214858
    Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.
    Type: Application
    Filed: August 16, 2010
    Publication date: August 23, 2012
    Applicant: University of Virginia Patent Foundation
    Inventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
  • Publication number: 20120184553
    Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
    Type: Application
    Filed: September 27, 2010
    Publication date: July 19, 2012
    Inventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
  • Publication number: 20120165339
    Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.
    Type: Application
    Filed: December 20, 2011
    Publication date: June 28, 2012
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
  • Publication number: 20120046293
    Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: October 10, 2011
    Publication date: February 23, 2012
    Applicant: Merck Frosst Canada Ltd.
    Inventors: CHRISTOPHER I. BAYLY, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
  • Patent number: 7968577
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: June 28, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
  • Publication number: 20110152291
    Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier wherein the symbols have the following meaning —X- is e.g. and Y being e.g. or the pharmaceutically acceptable salts can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
    Type: Application
    Filed: March 1, 2011
    Publication date: June 23, 2011
    Applicant: REVOTAR BIOPHARMACEUTICALS AG
    Inventors: Ewald M. AYDT, Remo Kranich, Anke S. Busemann
  • Publication number: 20110129419
    Abstract: The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.
    Type: Application
    Filed: December 19, 2007
    Publication date: June 2, 2011
    Applicants: GE HEALTHCARE LIMITED, HAMMERSMITH IMANET LIMITED
    Inventors: Anthony Eamon Storey, Julie Davis, Erik Arstad, Benedicte Guilbert, Alessandra Gaeta
  • Publication number: 20110039853
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: February 19, 2008
    Publication date: February 17, 2011
    Inventor: Soren Ebdrup
  • Publication number: 20110009447
    Abstract: Substituted benzoic acid amides of formula (I) and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of benzoic acid amides are described.
    Type: Application
    Filed: April 24, 2001
    Publication date: January 13, 2011
    Inventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch
  • Publication number: 20100152207
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Application
    Filed: April 4, 2008
    Publication date: June 17, 2010
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
  • Publication number: 20100137377
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: April 9, 2008
    Publication date: June 3, 2010
    Inventors: Anders Klarskov Petersen, Soren Ebdrup
  • Publication number: 20100075932
    Abstract: Novel salicylic anilides are chemical uncouplers useful e.g. for the treatment of obesity.
    Type: Application
    Filed: November 24, 2009
    Publication date: March 25, 2010
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: Preben Olesen, Thomas Kruse Hansen, Lise Brown Christiansen, Holger Claus Hansen
  • Publication number: 20100041657
    Abstract: The present invention relates to compounds of formula I, in which at least one of R5, R6 and R7 is SR12, S(O)R12 or S(O)2R12 group where R12 is a C1-6haloalkyl group, that act, as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
    Type: Application
    Filed: May 11, 2006
    Publication date: February 18, 2010
    Applicant: NOVO NORDICK A/S
    Inventors: Preben Houlberg Olesen, Holger Claus Hansen, Lise Brown Christiansen, Flemming Elmelund Nielsen, Anders Klarskov Petersen
  • Publication number: 20090124698
    Abstract: The present disclosure concerns a new class of selective estrogen receptor modulators (SERMs). The disclosure also includes the identification of a previously unknown membrane associated estrogen receptor. Methods for making and using the disclosed SERMs are disclosed, including pharmaceutical formulations of the disclosed novel compounds in useful compositions.
    Type: Application
    Filed: November 9, 2007
    Publication date: May 14, 2009
    Applicants: Oregon Health & Science University, The Regents of the University of California
    Inventors: Thomas S. Scanlan, Toru Iijima
  • Publication number: 20090118338
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: October 10, 2008
    Publication date: May 7, 2009
    Inventors: Weichuan Caroline Chen, Paul Krenitsky, Pramod Joshi, Andreas Termin, Dean Wilson
  • Publication number: 20090099147
    Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula I the use of the progesterone receptor modulators for producing medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.
    Type: Application
    Filed: July 9, 2008
    Publication date: April 16, 2009
    Inventors: Wolfgnag SCHWEDE, Carsten Moeller, Anja Schmidt, Ulrike Fuhrmann, Andrea Rotgeri, Thomas Kirkland
  • Publication number: 20090075989
    Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula 1, the use of the progesterone receptor modulators for the manufacture of medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.
    Type: Application
    Filed: December 20, 2007
    Publication date: March 19, 2009
    Inventors: Wolfgang Schwede, Carsten Moeller, Anja Schmidt, Ulrike Fuhrmann, Andrea Rotgeri, Thomas Andrew Kirkland, Ralf Wyrwa
  • Publication number: 20090005434
    Abstract: Novel salicylic anilides are chemical uncouplers useful e.g. for the treatment of obesity.
    Type: Application
    Filed: June 27, 2008
    Publication date: January 1, 2009
    Applicant: Novo Nordisk A/S
    Inventors: Preben Houlberg Olesen, Thomas Kruse Hansen, Lise Brown Christiansen, Holger Claus Hansen
  • Publication number: 20080287493
    Abstract: The present invention relates to arylmethylen substituted N-acyl-Y-aminoalcohols of the general formula I in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description. The compounds according to the invention are effective FSH modulators and can be used for example for fertility regulation in men or in women.
    Type: Application
    Filed: April 24, 2008
    Publication date: November 20, 2008
    Inventors: Lars Wortmann, Bernd Menzenbach, Marcus Koppitz, Dirk Kosemund, Hans-Peter Muhn, Anna Schrey, Ronald Kuhne, Thomas Frenzel, Florian Peter Liesener
  • Patent number: 7388111
    Abstract: The present invention provides for compounds useful for treating an HIV-1 infection, or preventing an HIV-1 infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1-R4 and Ar are as herein defined.
    Type: Grant
    Filed: October 18, 2006
    Date of Patent: June 17, 2008
    Assignee: Roche Palo Alto LLC
    Inventors: Taraneh Mirzadegan, Tania Silva
  • Patent number: 7223888
    Abstract: Novel compounds and compositions including those compounds, as well as methods of using and making the compounds are herein described. The compounds are useful in therapeutic applications, including modulation of disease or disease symptoms in a subject (e.g., mammal, human, dog, cat, horse). The compounds are useful as modulators of the mu opioid receptor (MOR) through their binding affinity with that receptor.
    Type: Grant
    Filed: October 10, 2003
    Date of Patent: May 29, 2007
    Assignee: President and Fellows of Harvard College
    Inventors: Bryce A. Harrison, Tiffany M. Gierasch, Gregory L. Verdine, Zhangjie Shi
  • Patent number: 7041702
    Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: May 9, 2006
    Assignee: Scion Pharmaceuticals, Inc.
    Inventors: Graham J. Durant, Seetharamaiyer Padmanabhan
  • Patent number: 6693208
    Abstract: Amino acid derivative as carrier compounds and compositions which are useful in the delivery of active agents are provided. The active agents can be a peptide, mucopolysaccharide, carbohydrate, or lipid. Methods of administration, including oral administration, and preparation are provided as well.
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: February 17, 2004
    Assignee: Emisphere Technologies, Inc.
    Inventors: David Gscheidner, Andrea Leone-Bay, Eric Wang, John J. Freeman, Doris C. O'Toole, Lynn Shields
  • Patent number: 6376524
    Abstract: Triphenyl compounds of the formulae I, II, and VI: methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are compounds are interleukin-4 antagonists; and are useful for the treatment of asthma and allergies.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: April 23, 2002
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Kenneth J. Barr, Brian C. Cunningham, William Michael Flanagan, Wanli Lu, Brian C. Raimundo, Nathan D. Waal, Jennifer Wilkinson, Jiang Zhu, Wenjin Yang
  • Patent number: 6326510
    Abstract: The invention relates to novel biaromatic compounds having general formula I and their use in pharmaceutical compositions for use in human and veterinary medicine, in particular for treating dermatological, rheumatic, respiratory, cardiovascular, and ophthalmological disorders, and for use in cosmetic compositions.
    Type: Grant
    Filed: January 8, 1999
    Date of Patent: December 4, 2001
    Assignee: Centre International de Recherches Dermatologiques
    Inventor: Jean-Michel Bernardon
  • Patent number: 6310247
    Abstract: Novel trienoic retinoid compounds of with apoptotic activity useful for the prevention and treatment of cancer.
    Type: Grant
    Filed: December 14, 1999
    Date of Patent: October 30, 2001
    Assignee: Hoffmann-LA Roche Inc.
    Inventors: Adrian Wai-Hing Cheung, Stephen B. Ferguson, Louise Helen Foley, Allen John Lovey
  • Patent number: 6288234
    Abstract: Disclosed are multibinding compounds which inhibit microsomal triglyceride transferase protein (MTP), a protein which mediates the transfer of lipids during the assembly of lipoproteins and related biomolecules. The multibinding compounds contain from 2 to 10 ligands covalently attached to one or more linkers. The multibinding compounds of this invention are useful for lowering serum lipid, cholesterol and/or triglyceride levels, and for preventing and treating disorders associated with hyperlipemia, hyperlipidemia, hyperlipoproteinemia, hypercholestrolemia, hypertriglyceridemia and the like, such atherosclerosis.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: September 11, 2001
    Assignee: Advanced Medicine, Inc.
    Inventor: John H. Griffin
  • Patent number: 6242609
    Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.
    Type: Grant
    Filed: April 7, 1999
    Date of Patent: June 5, 2001
    Assignee: Konica Corporation
    Inventor: Fumio Ishii
  • Patent number: 5925646
    Abstract: The heterocyclic aryl-, alkyl- and cycloalkylacetamides are prepared by reacting the appropriately substituted acetic acids with amines, if appropriate in complexed form. The heterocyclic aryl-, alkyl- and cycloalkylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.
    Type: Grant
    Filed: January 16, 1998
    Date of Patent: July 20, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
  • Patent number: 5922771
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.
    Type: Grant
    Filed: August 19, 1996
    Date of Patent: July 13, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
  • Patent number: 5900432
    Abstract: Compounds of formula I: ##STR1## wherein, ring C, A--B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: October 12, 1995
    Date of Patent: May 4, 1999
    Assignee: Zeneca Limited
    Inventors: James Roy Empfield, Cyrus John Ohnmacht, Keith Russell, Diane Amy Trainor, Paul James Warwick, Jr.
  • Patent number: 5886046
    Abstract: This invention relates to chemical compounds that contain adjacent carbonyl groups, which effectively inhibit the biological, chemical, and/or physical properties of enzymes and other medicinally-significant proteins. In particular, the invention relates to dicarbonyl compounds that are capable of acting as enzyme inhibitors, including irreversible inhibitors of HIV-1 protease.
    Type: Grant
    Filed: January 19, 1996
    Date of Patent: March 23, 1999
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Ralph F. Hirschmann, Amos B. Smith, III, Paul Sprengeler, Wenqing Yao, Paul Anderson
  • Patent number: 5750783
    Abstract: Benzyloxy-substituted phenylglycinolamides are prepared by reaction of benzyloxy-substituted phenylacetic acids with phenylglycinols. The benzyloxy-substituted phenylglycinolamides are suitable as active compounds in medicaments, in particular in medicaments for the treatment of atherosclerosis.
    Type: Grant
    Filed: April 10, 1997
    Date of Patent: May 12, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Ulrich Muller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Martin Beuck
  • Patent number: 5591776
    Abstract: Rolipram-based PDE IV inhibitors containing phenyl- or benzyl-substituted moieties of the formula: ##STR1## wherein X.sub.1 and X.sub.2 may be the same or different and each is O or S;R.sub.1 is selected from the group consisting of hydrogen, saturated or unsaturated straight-chain or branched C.sub.2-12 alkyl groups, cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 10 carbon atoms in the cycloalkyl moiety;R.sub.2 =R.sub.1 or --CH.sub.3 ;R.sub.3 is hydrogen, halogen, or a saturated or unsaturated straight-chain or branched C.sub.1-12 alkyl group, a cycloalkyl or cycloalkyl-alkyl groups containing from 3 to 7 carbon atoms in the cycloalkyl moiety;Z is a linkage selected from --CH.sub.2 CONH-- or --CH.sub.2 NHCO--, andR.sub.
    Type: Grant
    Filed: January 10, 1995
    Date of Patent: January 7, 1997
    Assignee: Euro-Celtique, S.A.
    Inventors: David J. Cavalla, Lloyd J. Dolby, Mark Chasin
  • Patent number: 5523457
    Abstract: This invention relates to a retinoid mpound of formula I ##STR1## in which Y is --CO--NH--, --CR.sup.2 .dbd.CR.sup.3 --, --CO--O--, --O--CO--, --C(.dbd.S)--NH--, --C.tbd.C--, --O--CH.sub.2 --, --CH.sub.2 --O--, or --CH.sub.2 --CH.sub.2 --;A is --(CH.sub.2).sub.t -- or a bond;Q is phenyl optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen, or --CO.sub.2 R.sup.4 ;R.sup.1 is --CO.sub.2 Z, --CONHR.sup.5, C.sub.1-6 alkyl, --CH.sub.2 OH, or --CHO;R.sup.2, R.sup.3, R.sup.4, R.sup.5, and Z are independently hydrogen or C.sub.1-6 alkyl;t is one to six.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: June 4, 1996
    Assignee: Bristol-Myers Squibb Company
    Inventors: John E. Starrett, Jr., Muzammil M. Mansuri, David R. Tortolani
  • Patent number: 5494933
    Abstract: A method of treatment or prophylaxis of angina in mammals, such as humans, which comprises the administration to the sufferer of an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate of any of the foregoing: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, A and B are herein defined.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: February 27, 1996
    Assignee: Beecham-Wuelfing GmbH & Co. KG
    Inventor: Harald Maschler
  • Patent number: 5482969
    Abstract: Compounds of formula I: ##STR1## wherein, ring C, A-B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: March 11, 1994
    Date of Patent: January 9, 1996
    Assignee: Zeneca Limited
    Inventors: James R. Empfield, Cyrus J. Ohnmacht, Keith Russell, Diane A. Trainor, Paul J. Warwick, Jr.
  • Patent number: 5430060
    Abstract: The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.
    Type: Grant
    Filed: September 15, 1993
    Date of Patent: July 4, 1995
    Assignee: Zeneca Limited
    Inventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
  • Patent number: 5426224
    Abstract: A novel antiproliferative drug and methods are disclosed. The drug has the general structural formula: ##STR1## where R1=OR.sub.1 ', SR.sub.1 ', or N(R.sub.1 'R.sub.1 ").sub.2, where R.sub.1 ' and R.sub.1 " are H or lower alkyl groups, and R.sub.2 is an acylamino, or aroylamino group. The compound is useful for inhibiting cell proliferation in drug-resistant tumor cells. Also disclosed is a method of chemical converting a colchicine derivative to form an active inhibitor of DNA topisomerase II.
    Type: Grant
    Filed: March 18, 1993
    Date of Patent: June 20, 1995
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Kenneth F. Bastow
  • Patent number: 5416118
    Abstract: Novel bicyclic amides of the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl, wherein R.sup.2 is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;X, Y and Z are --CH.sub.2 --, --CH(alkyl)--, --C(alkyl).sub.2 --, --NH--, --N(alkyl)--, --O-- or --SO.sub.r, wherein r is 0, 1 or 2, and m, n and p are 0 or 1;R.sup.1 is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain --O--, --SO.sub.r, phenylene, R.sup.2 -substituted phenylene, heteroarylene or R.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: May 16, 1995
    Assignee: Schering Corporation
    Inventors: John W. Clader, Thomas Fevig, Wayne Vaccaro, Joel G. Berger
  • Patent number: 5354767
    Abstract: Disclosed herein are compounds of the formula:R.sup.1 CH.sub.2 CH(X)CH(Y)CH(Z)CHR.sup.2 C(O)NHCHR.sup.3 CH(OH)CH(OH)R.sup.4wherein R.sup.1 is a terminal unit, for example lower cycloalkyl or phenyl; R.sup.2 is, for example, an optionally substituted alkyl, cycloalkylmethyl, benzyl, 4-imidazolylmethyl, 2-thienylmethyl or 4-thiazolylmethyl; R.sup.3 is alkyl, cycloalkylmethyl or an optionally substituted benzyl; R.sup.4 is alkyl or cycloalkyl; and X and Y each is hydroxy and Z is hydrogen, or X and Z each is hydroxy and Y is hydrogen; with the provisos that (a) the carbon atom bearing R.sup.2 has the "R" configuration except when R.sup.2 is 2-thienylmethyl or 2-thiazolylmethyl, X and Y each is hydroxy and Z is hydrogen, then the carbon atom bearing R.sup.2 has the "S" configuration; (b) the carbon atoms bearing R.sup.3 and R.sup.4 each has the "S" configuration; and (c) the carbon atom located between the last-said two carbon atoms has the "R" configuration.
    Type: Grant
    Filed: December 10, 1992
    Date of Patent: October 11, 1994
    Assignee: Bio-Mega, Inc.
    Inventors: Paul C. Anderson, Gary W. Bantle, Grace L. Jung, Pierre Lavallee, Bruno Simoneau