Ring In A Substituent E Patents (Class 564/174)
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Patent number: 9162993Abstract: 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: GrantFiled: January 29, 2015Date of Patent: October 20, 2015Assignee: National Defense Medical CenterInventors: Deh-Ming Chang, Hsu-Shan Huang, Chia-Chung Lee, Chun-Liang Chen
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Publication number: 20140371232Abstract: 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: ApplicationFiled: December 18, 2012Publication date: December 18, 2014Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
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Publication number: 20140336378Abstract: 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: ApplicationFiled: November 29, 2012Publication date: November 13, 2014Inventor: Doo Hyun Lee
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Publication number: 20140219989Abstract: 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: ApplicationFiled: July 3, 2012Publication date: August 7, 2014Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
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Patent number: 8778939Abstract: 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: GrantFiled: September 27, 2010Date of Patent: July 15, 2014Assignee: Glaxo Group LimitedInventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
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Patent number: 8692005Abstract: 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: GrantFiled: August 15, 2012Date of Patent: April 8, 2014Assignee: Stepan CompanyInventors: Marshall J. Nepras, Franz J. Luxem, Leonard F. Zaporowski, David Eisenberg
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Publication number: 20130281444Abstract: 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: ApplicationFiled: August 9, 2012Publication date: October 24, 2013Inventors: Deh-Ming CHANG, Hsu-Shan HUNAG, Chia-Chung LEE, Chun-Liang CHEN
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Publication number: 20130281412Abstract: 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: ApplicationFiled: September 11, 2012Publication date: October 24, 2013Inventors: Deh-Ming CHANG, Hsu-Shan Huang, Chun-Liang Chen, Chia-Chung Lee
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Publication number: 20130129626Abstract: 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: ApplicationFiled: December 18, 2012Publication date: May 23, 2013Applicants: HAMMERSMITH IMANET LIMITED, GE HEALTHCARE LIMITEDInventors: GE Healthcare Limited, Hammersmith Imanet Limited
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Publication number: 20120214858Abstract: 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: ApplicationFiled: August 16, 2010Publication date: August 23, 2012Applicant: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
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Publication number: 20120184553Abstract: 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: ApplicationFiled: September 27, 2010Publication date: July 19, 2012Inventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
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Publication number: 20120165339Abstract: 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: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: 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
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Publication number: 20120046293Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: October 10, 2011Publication date: February 23, 2012Applicant: 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
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Patent number: 7968577Abstract: 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: GrantFiled: October 31, 2007Date of Patent: June 28, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
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Publication number: 20110152291Abstract: 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: ApplicationFiled: March 1, 2011Publication date: June 23, 2011Applicant: REVOTAR BIOPHARMACEUTICALS AGInventors: Ewald M. AYDT, Remo Kranich, Anke S. Busemann
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Publication number: 20110129419Abstract: 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: ApplicationFiled: December 19, 2007Publication date: June 2, 2011Applicants: GE HEALTHCARE LIMITED, HAMMERSMITH IMANET LIMITEDInventors: Anthony Eamon Storey, Julie Davis, Erik Arstad, Benedicte Guilbert, Alessandra Gaeta
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Publication number: 20110039853Abstract: 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: ApplicationFiled: February 19, 2008Publication date: February 17, 2011Inventor: Soren Ebdrup
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Publication number: 20110009447Abstract: 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: ApplicationFiled: April 24, 2001Publication date: January 13, 2011Inventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch
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Publication number: 20100152207Abstract: 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: ApplicationFiled: April 4, 2008Publication date: June 17, 2010Inventors: 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
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Publication number: 20100137377Abstract: 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: ApplicationFiled: April 9, 2008Publication date: June 3, 2010Inventors: Anders Klarskov Petersen, Soren Ebdrup
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Publication number: 20100075932Abstract: Novel salicylic anilides are chemical uncouplers useful e.g. for the treatment of obesity.Type: ApplicationFiled: November 24, 2009Publication date: March 25, 2010Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Preben Olesen, Thomas Kruse Hansen, Lise Brown Christiansen, Holger Claus Hansen
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Publication number: 20100041657Abstract: 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: ApplicationFiled: May 11, 2006Publication date: February 18, 2010Applicant: NOVO NORDICK A/SInventors: Preben Houlberg Olesen, Holger Claus Hansen, Lise Brown Christiansen, Flemming Elmelund Nielsen, Anders Klarskov Petersen
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Publication number: 20090124698Abstract: 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: ApplicationFiled: November 9, 2007Publication date: May 14, 2009Applicants: Oregon Health & Science University, The Regents of the University of CaliforniaInventors: Thomas S. Scanlan, Toru Iijima
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Publication number: 20090118338Abstract: 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: ApplicationFiled: October 10, 2008Publication date: May 7, 2009Inventors: Weichuan Caroline Chen, Paul Krenitsky, Pramod Joshi, Andreas Termin, Dean Wilson
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Publication number: 20090099147Abstract: 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: ApplicationFiled: July 9, 2008Publication date: April 16, 2009Inventors: Wolfgnag SCHWEDE, Carsten Moeller, Anja Schmidt, Ulrike Fuhrmann, Andrea Rotgeri, Thomas Kirkland
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Publication number: 20090075989Abstract: 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: ApplicationFiled: December 20, 2007Publication date: March 19, 2009Inventors: Wolfgang Schwede, Carsten Moeller, Anja Schmidt, Ulrike Fuhrmann, Andrea Rotgeri, Thomas Andrew Kirkland, Ralf Wyrwa
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Publication number: 20090005434Abstract: Novel salicylic anilides are chemical uncouplers useful e.g. for the treatment of obesity.Type: ApplicationFiled: June 27, 2008Publication date: January 1, 2009Applicant: Novo Nordisk A/SInventors: Preben Houlberg Olesen, Thomas Kruse Hansen, Lise Brown Christiansen, Holger Claus Hansen
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Publication number: 20080287493Abstract: 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: ApplicationFiled: April 24, 2008Publication date: November 20, 2008Inventors: Lars Wortmann, Bernd Menzenbach, Marcus Koppitz, Dirk Kosemund, Hans-Peter Muhn, Anna Schrey, Ronald Kuhne, Thomas Frenzel, Florian Peter Liesener
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Patent number: 7388111Abstract: 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: GrantFiled: October 18, 2006Date of Patent: June 17, 2008Assignee: Roche Palo Alto LLCInventors: Taraneh Mirzadegan, Tania Silva
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Patent number: 7223888Abstract: 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: GrantFiled: October 10, 2003Date of Patent: May 29, 2007Assignee: President and Fellows of Harvard CollegeInventors: Bryce A. Harrison, Tiffany M. Gierasch, Gregory L. Verdine, Zhangjie Shi
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Patent number: 7041702Abstract: 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: GrantFiled: October 20, 1998Date of Patent: May 9, 2006Assignee: Scion Pharmaceuticals, Inc.Inventors: Graham J. Durant, Seetharamaiyer Padmanabhan
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Patent number: 6693208Abstract: 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: GrantFiled: July 15, 2002Date of Patent: February 17, 2004Assignee: Emisphere Technologies, Inc.Inventors: David Gscheidner, Andrea Leone-Bay, Eric Wang, John J. Freeman, Doris C. O'Toole, Lynn Shields
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Patent number: 6376524Abstract: 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: GrantFiled: June 21, 2000Date of Patent: April 23, 2002Assignee: 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
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Patent number: 6326510Abstract: 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: GrantFiled: January 8, 1999Date of Patent: December 4, 2001Assignee: Centre International de Recherches DermatologiquesInventor: Jean-Michel Bernardon
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Patent number: 6310247Abstract: Novel trienoic retinoid compounds of with apoptotic activity useful for the prevention and treatment of cancer.Type: GrantFiled: December 14, 1999Date of Patent: October 30, 2001Assignee: Hoffmann-LA Roche Inc.Inventors: Adrian Wai-Hing Cheung, Stephen B. Ferguson, Louise Helen Foley, Allen John Lovey
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Patent number: 6288234Abstract: 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: GrantFiled: June 4, 1999Date of Patent: September 11, 2001Assignee: Advanced Medicine, Inc.Inventor: John H. Griffin
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Patent number: 6242609Abstract: 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: GrantFiled: April 7, 1999Date of Patent: June 5, 2001Assignee: Konica CorporationInventor: Fumio Ishii
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Patent number: 5925646Abstract: 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: GrantFiled: January 16, 1998Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
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Patent number: 5922771Abstract: 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: GrantFiled: August 19, 1996Date of Patent: July 13, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
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Patent number: 5900432Abstract: 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: GrantFiled: October 12, 1995Date of Patent: May 4, 1999Assignee: Zeneca LimitedInventors: James Roy Empfield, Cyrus John Ohnmacht, Keith Russell, Diane Amy Trainor, Paul James Warwick, Jr.
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Patent number: 5886046Abstract: 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: GrantFiled: January 19, 1996Date of Patent: March 23, 1999Assignee: The Trustees of the University of PennsylvaniaInventors: Ralph F. Hirschmann, Amos B. Smith, III, Paul Sprengeler, Wenqing Yao, Paul Anderson
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Patent number: 5750783Abstract: 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: GrantFiled: April 10, 1997Date of Patent: May 12, 1998Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Ulrich Muller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Martin Beuck
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Patent number: 5591776Abstract: 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: GrantFiled: January 10, 1995Date of Patent: January 7, 1997Assignee: Euro-Celtique, S.A.Inventors: David J. Cavalla, Lloyd J. Dolby, Mark Chasin
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Patent number: 5523457Abstract: 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: GrantFiled: June 2, 1995Date of Patent: June 4, 1996Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., Muzammil M. Mansuri, David R. Tortolani
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Patent number: 5494933Abstract: 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: GrantFiled: June 1, 1995Date of Patent: February 27, 1996Assignee: Beecham-Wuelfing GmbH & Co. KGInventor: Harald Maschler
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Patent number: 5482969Abstract: 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: GrantFiled: March 11, 1994Date of Patent: January 9, 1996Assignee: Zeneca LimitedInventors: James R. Empfield, Cyrus J. Ohnmacht, Keith Russell, Diane A. Trainor, Paul J. Warwick, Jr.
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Patent number: 5430060Abstract: 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: GrantFiled: September 15, 1993Date of Patent: July 4, 1995Assignee: Zeneca LimitedInventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
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Patent number: 5426224Abstract: 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: GrantFiled: March 18, 1993Date of Patent: June 20, 1995Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Kenneth F. Bastow
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Patent number: 5416118Abstract: 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: GrantFiled: September 28, 1993Date of Patent: May 16, 1995Assignee: Schering CorporationInventors: John W. Clader, Thomas Fevig, Wayne Vaccaro, Joel G. Berger
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Patent number: 5354767Abstract: 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: GrantFiled: December 10, 1992Date of Patent: October 11, 1994Assignee: Bio-Mega, Inc.Inventors: Paul C. Anderson, Gary W. Bantle, Grace L. Jung, Pierre Lavallee, Bruno Simoneau