Nitrogen In The 1-position Substituent Of The Bicyclo Ring System Patents (Class 540/514)
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Patent number: 8906913Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.Type: GrantFiled: June 22, 2010Date of Patent: December 9, 2014Assignee: Panacea Biotec LimitedInventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
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Publication number: 20120165320Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.Type: ApplicationFiled: June 22, 2010Publication date: June 28, 2012Applicant: PANACEA BIOTEC LTD.Inventors: Rajseh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
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Publication number: 20110306604Abstract: Compounds of Formula (I): (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.Type: ApplicationFiled: August 14, 2009Publication date: December 15, 2011Inventors: Michael R. Wood, Ian M. Bell, June J. Kim, Harold G. Selnick, Craig A. Stump
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Publication number: 20110245492Abstract: The invention provides methods, PCR primers and sequence determination oligonucleotides for determining a human's capacity to metabolise a substrate of the CYP2C19 enzyme using genetic analysis.Type: ApplicationFiled: May 16, 2011Publication date: October 6, 2011Inventors: Brahmachari Samir KUMAR, Kukreti Ritushree, Mukerji Mitali, Martis Suparna, Fernandes Ravina, Sharma Nitin
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Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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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: 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: 6458784Abstract: Pharmaceutically active benzodiazapine compounds of formula (I) are disclosed. These compounds inhibit the vitronectin receptor and are useful for treatment of osteoporosis.Type: GrantFiled: October 5, 2000Date of Patent: October 1, 2002Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, Richard McCulloch Keenan, Chet Kwon, William Henry Miller, Irene Nijole Uzinskas
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Patent number: 6403578Abstract: This invention relates to compounds of the formulae: wherein A1 is O, S, N—R1 or CHR1; A4 is N—R4 or CHR4; R2 is a sidechain containing an acid or ester group; R1, R4 and R5 are substituents such as H, alkyl and aryl alkyl, and R6 is a sidechain containing a nitrogen group; and pharmaceutically acceptable salts thereof, which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.Type: GrantFiled: August 4, 1995Date of Patent: June 11, 2002Assignee: SmithKline Beecham CorporationInventors: William Edward Bondinell, James Francis Callahan, William Francis Huffman, Richard McCulloch Keenan, Thomas Wen-Fu Ku, Kenneth Allen Newlander, James Martin Samanen, Irene Nijole Uzinskas
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Patent number: 6117866Abstract: Certain compounds within formula (I) are inhibitors of platelet aggregation: ##STR1## wherein A.sup.1 is NH or CH.sub.2 ;R is H, C.sub.1-6 alkyl, benzyl or a carboxy protecting group;R.sup.3 is C.sub.1-6 alkyl, Ar-C.sub.0-6 alkyl, C.sub.3-7 cycloalkylC.sub.0-6 alkyl, or Het-C.sub.0-6 alkyl;R.sup.6 is 4-amidino-Ar-N(CH.sub.3)CO, [[2-(4-piperidinyl)ethyl](N-methyl)amino]carbonyl, (4,4'-bipiperidin-1-yl)carbonyl, [4-(2-aminoethyl)piperidin-1-yl]carbonyl, [[[3-(4-piperidinyl]propyl]methylamino]carbonyl, 1-[4-(4-pyridyl)piperazinyl]carbonyl, [[2-[(2-amino)pyrid-4-yl]ethyl]methylamino]carbonyl, [[2-(4-piperidinyl)ethyl]carbonyl]amino, [[2-(4-piperidinyl)ethyl]carbonyl]amino, [[2-(1-piperazinyl)ethyl]methylamino]-carbonyl, or [[(1,2,3,4-tetrahydro-7-isoquinolinyl]amino]carbonyl; andX is H, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkthio, trifluoroalkyl, N(R').sub.2, CO.sub.2 R', CON(R').sub.2, OH, F, Cl, Br or I.Type: GrantFiled: July 3, 1996Date of Patent: September 12, 2000Assignee: SmithKline Beecham CorporationInventors: William Edward Bondinell, James Martin Samanen
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Patent number: 6100254Abstract: Disclosed herein are small molecule, non-peptidyl inhibitors of protein tyrosine kinases, and methods for their use. The instant inhibitors are based on a 1,4-benzodiazepin-2-one nucleus. Methods are provided for inhibition of specific protein tyrosine kinases, for example pp60.sup.c-src. Methods are further provided for the use of these inhibitors in situations where the inhibition of a protein tyrosine kinase is indicated, for example, in the treatment of certain diseases in mammals, including humans.Type: GrantFiled: October 10, 1997Date of Patent: August 8, 2000Assignees: Board of Regents, The University of Texas System, The Regents of the University of CaliforniaInventors: Raymond J. A. Budde, Jonathan A. Ellman, Victor A. Levin, Gary E. Gallick, Robert A. Newman
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Patent number: 5843941Abstract: Benzodiazepine derivatives represented by the structure below are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases foe which inhibition of the ras farnesyl:protein transferase as indicated.Type: GrantFiled: September 26, 1994Date of Patent: December 1, 1998Assignees: Genentech, Inc., Board of Regents University of TexasInventors: James C. Marsters, Jr., Michael S. Brown, Craig W. Crowley, Joseph L. Goldstein, Guy L. James, Robert S. McDowell, David Oare, Thomas E. Rawson, Mark Reynolds, Todd C. Somers
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Patent number: 5662911Abstract: Benzodiazepine protein conjugates of the formula I ##STR1## wherein R1 is hydrogen, a methyl group or R, R2 is hydrogen, a hydroxyl or an OR group, with R1 or R2 containing an R group,R3 is a halogen, NO2 or NH2,X is hydrogen or a halogen,wherein R is a group of the formula II, wherein Z is a macromolecular immunogen reactive carrier substance and n is 2 or 3.The benzodiazepine protein conjugates are used as immunogens to obtain antibodies to benzodiazepines.The invention also relates to an immunoassay for the detection of benzodiazepines where the so generated antibodies are used.Type: GrantFiled: January 24, 1996Date of Patent: September 2, 1997Assignee: Boehringer Mannheim GmbHInventors: Erasmus Huber, Christian Klein, Hans-Peter Josel, Bruno Zink
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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: 5013836Abstract: The difficulty of methylating a hindered piperidinyl, piperazinyl, or diazepinyl group with an Eschweiler-Clarke ("E-C") procedure without using a large molar excess (more than double) of formaldehyde is surprisingly found to be non-existent in the case of a diazacycloalkan-2-one group with a hindered N.sup.4 - or N.sup.5 -atom of its NH group which is to be methylated. The N.sup.4 - or N.sup.5 -atom of a polysubstituted diazacycloalkan-2-one group ("DCA") is substantially stoichiometrically converted even when a conventional E-C procedure is starved of HCHO, that is, with a much smaller molar excess of formaldehyde than deemed necessary. The effective molar ratio of NH groups: HCHO in the starved E-C process is in the range from 1:1 to 1:1.5, in the presence of enough formic acid to function both as reactant and solvent not only for a DCA-containing complex amine ("starting amine") to be methylated, but also for the methylated amine (product).Type: GrantFiled: November 21, 1989Date of Patent: May 7, 1991Assignee: The B. F. Goodrich CompanyInventor: John T. Lai
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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
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Patent number: 4656026Abstract: An improved imaging technique involving nuclear magnetic resonance. Known drug or neurotransmitter receptor ligands are covalently bound to magnetic resonance image enhancing spin label compounds, such as sterically hindered free radical nitroxide compounds, with the resulting adduct being administered to a patient, and thereafter when the ligand is bound to specific receptor sites in the soft tissue such as the brain, regional tissue area is assessed with nuclear magnetic resonance, allowing diagnostic discrimination.Type: GrantFiled: December 10, 1984Date of Patent: April 7, 1987Assignee: University of Iowa Research FoundationInventors: Jeffrey A. Coffman, Charles F. Barfknecht