The Chalcogen Double Bonded Directly To The Hetero Ring Is Sulfur Patents (Class 540/505)
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Publication number: 20130102774Abstract: A process for transforming a group >C?O (I) in a compound into a group >C?S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2 C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2 C5H5N.Type: ApplicationFiled: February 3, 2012Publication date: April 25, 2013Applicant: VIRONOVA ABInventors: Birgitta Pettersson, Vedran Hasimbegovic, Per H Svensson, Jan Bergman
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Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7250410Abstract: The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis intermediates.Type: GrantFiled: June 7, 2002Date of Patent: July 31, 2007Assignee: Via Pharmaceuticals, Inc.Inventors: Jean-Jacques Bourguignon, Yan Lagouge, Claire Lugnier, Eveline Klotz, Jean-Paul Macher, Pierre Raboisson, Dominique Schultz
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Patent number: 7160880Abstract: The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy.Type: GrantFiled: May 12, 2000Date of Patent: January 9, 2007Assignee: CeNeS LimitedInventors: Paul L Feldman, David Kendall Jung, Istvan Kaldor, Gregory J. Pacofsky, Jeffrey A. Stafford, Jeffrey H. Tidwell
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Patent number: 7067512Abstract: The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.Type: GrantFiled: November 13, 2002Date of Patent: June 27, 2006Inventors: Tianbao Lu, Louis V Lafrance, III, Daniel J Parks, Karen L Milkiewicz, Raul R Calvo, Maxwell D Cummings, Alexander J Kim, Bruce L Grasberger, Theodore E Carver, Jr.
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Patent number: 7053084Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: February 17, 2000Date of Patent: May 30, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Richard E. Olson
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Patent number: 6916805Abstract: This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable compositions comprising the compounds, their salts or prodrugs, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: January 4, 2002Date of Patent: July 12, 2005Assignee: Warner-Lambert Company LLCInventors: Danette Andrea Dudley, Jeremy John Edmunds
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Patent number: 6900222Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is aType: GrantFiled: May 23, 2000Date of Patent: May 31, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 6838558Abstract: Disclosed are novel pyrazolobenzodiazepines having the formula These compounds are useful in the preparation of the pyrazolobenzodiazepines of formula I, which are useful in the treatment and control of solid tumors.Type: GrantFiled: April 15, 2002Date of Patent: January 4, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Qingjie Ding, Jin-Jun Liu, Giacomo Pizzolato, Chung-Chen Wei, Peter Michael Wovkulich
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Publication number: 20040152888Abstract: The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis intermediates.Type: ApplicationFiled: November 26, 2003Publication date: August 5, 2004Inventors: Jean-Jacques Bourguignon, Yan Lagouge, Claire Lugnier, Eveline Klotz, Jean-Paul Macher, Pierre Raboisson, Dominique Schultz
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Publication number: 20040024203Abstract: Compounds of formula (I) are disclosed. The compounds inhibit the action of gamma secretase, and hence find use in the treatment and prevention of Alzheimer's disease.Type: ApplicationFiled: April 11, 2003Publication date: February 5, 2004Inventors: Ian Churcher, Alan John Nadin, Andrew Pate Owens
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Patent number: 6686350Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: January 25, 1999Date of Patent: February 3, 2004Assignee: Biogen, Inc.Inventors: Zhongli Zheng, Carol L. Ensinger, Steven P. Adams
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Publication number: 20030109518Abstract: The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.Type: ApplicationFiled: November 13, 2002Publication date: June 12, 2003Inventors: Tianbao Lu, Louis V. Lafrance, Daniel J. Parks, Karen L. Milkiewicz, Raul R. Calvo, Maxwell D. Cummings, Alexander J. Kim, Bruce L. Grasberger, Theodore E. Carver
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Patent number: 6462037Abstract: The present invention relates to 1,4-benzodiazepin-2-ones of Formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: May 25, 2000Date of Patent: October 8, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James D. Rodgers, Barry L. Johnson, Haisheng Wang
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Patent number: 6392044Abstract: Cis-R-dioxo-benzylpyrrolopiperidine is racemized in a particularly advantageous manner by treating it with a substoichiometric amount of base, preferably at temperatures below about 40° C.Type: GrantFiled: June 30, 2000Date of Patent: May 21, 2002Assignee: Bayer AktiengesellschaftInventors: Herbert Diehl, Georg Martin, Wilfried Jaworek, Andreas Krebs, Joachim Westen
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Patent number: 5580979Abstract: The present invention makes available novel compounds represented by the general formula ##STR1## wherein Y represents a phosphate analog. Which compounds are useful for inhibiting an interaction between a protein containing an SH2 domain and a phophotyrosine-containing polypeptide.Type: GrantFiled: March 15, 1994Date of Patent: December 3, 1996Assignee: Trustees of Tufts UniversityInventor: William W. Bachovchin
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Patent number: 5324726Abstract: Benzodiazepine analogs of the formula: ##STR1## wherein: R.sup.3 is ##STR2## --NH(CH.sub.2).sub.2 --.sub.3 NHCOR.sup.7, ##STR3## or --X.sup.11 NR.sup.18 SO.sub.2 (CH.sub.2).sub.q R.sup.7 ; R.sup.7 is O,S,HH, or NR.sup.15 with the proviso that X.sup.7 can be NR.sup.15 only when R.sup.1 is not H.are disclosed which are antagonists of gastrin and cholecystokinin (CCK) with enhanced aqueous solubility and have properties useful in the treatment of disorders of gastric secretion, appetite regulation, gastrointestinal motility, pancreatic secretion, and dopaminergic function, as well as in treatment producing potentiation of morphine and other opiate analgesics.Type: GrantFiled: October 29, 1992Date of Patent: June 28, 1994Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Ben E. Evans, Roger M. Freidinger
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Patent number: 5175159Abstract: Compounds of Formula I are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for stoppage of labor prepatory to Caesarean delivery.Type: GrantFiled: December 28, 1990Date of Patent: December 29, 1992Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Ben E. Evans, Roger M. Freidinger
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Patent number: 4929269Abstract: Compounds of the formula ##STR1## and salts thereof, W and W, being independently O and S, A being a nitrogen-containing heterocyclic ring system, E being O, S(O)m or NR.sub.3 where m is 0-2, R.sub.1, R.sub.2 and R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 alkenyl or alkynyl and E.sub.1 being hydrogen, halogen or one of a variety of organic substituents.The compounds are effective herbicides.Type: GrantFiled: October 19, 1988Date of Patent: May 29, 1990Assignee: ICI Australia Operations Proprietary LimitedInventors: Keith G. Watson, Peter Drygala, Stephen Bell
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Patent number: 4820834Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).Type: GrantFiled: March 16, 1987Date of Patent: April 11, 1989Assignee: Merck & Co., Inc.Inventors: Ben E. Evans, Roger M. Freidinger, Mark G. Bock