Sulfur, -c(=x)-, Wherein X Is Chalcogen, Or Nitrogen, Other Than As Nitro Or Nitroso, Bonded Directly To The Carbocyclic Ring Of The Bicyclo Ring System Patents (Class 540/513)
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Patent number: 10513501Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.Type: GrantFiled: December 12, 2018Date of Patent: December 24, 2019Assignee: FORMA Therapeutics, Inc.Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin, Kenneth W. Bair
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Patent number: 7074783Abstract: Disclosed are compounds, which are bradykinin antagonists and are useful to treat diseases or relieve adverse symptoms associated with disease conditions in mammals mediated by bradykinin. Certain of the compounds exhibit increased potency and are expected to also exhibit an increased duration of action.Type: GrantFiled: October 9, 2003Date of Patent: July 11, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Ryan C. Holcomb, Francine S. Grant, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 6653303Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: January 6, 2003Date of Patent: November 25, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 6630475Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of ParkinsoType: GrantFiled: May 24, 2001Date of Patent: October 7, 2003Assignee: Schering CorporationInventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil
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Publication number: 20030149262Abstract: The present invention describes novel compounds of the formula:Type: ApplicationFiled: November 26, 2002Publication date: August 7, 2003Inventors: Edward H. Cheesman, Michael Sworin
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Patent number: 6558649Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: December 17, 1999Date of Patent: May 6, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Edward H. Cheesman, Michael Sworin, Milind Rajopadhye
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Patent number: 6495545Abstract: The present invention relates to compounds of general formula (I) and their preparation and use for the production of pharmaceuticals, and pharmaceuticals comprising these compounds.Type: GrantFiled: June 12, 2001Date of Patent: December 17, 2002Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Delf Schmidt, Ulf Brüggemeier, Christoph Gerdes, Beatrix Stelte-Ludwig, Jörg Keldenich, Elke Stahl
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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: 6455529Abstract: Compounds of the formula I in which R1, R2 and R3 have the stated meanings, and their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be used for the treatment of thromboses, osteoporoses, oncoses, stroke, myocardial infarct, ischemias, inflammations, arteriosclerosis and osteolytic disorders.Type: GrantFiled: May 3, 1996Date of Patent: September 24, 2002Assignee: Merck Patent Gesellschaft mit beschraenkter HaftungInventors: Joachim Gante, Hörst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
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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: 6339083Abstract: The present invention relates to compounds of the general formula (I): and their preparation and use for the production of pharmaceuticals, and pharmaceuticals comprising these compounds.Type: GrantFiled: December 14, 1998Date of Patent: January 15, 2002Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Delf Schmidt, Ulf Brueggemeier, Christoph Gerdes, Beatrix Stelte-Ludwig, Jörg Keldenich, Elke Stahl
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Patent number: 6335330Abstract: This invention provides (S)-7-[(4,4′-bipiperidin-1-yl)carbonyl]-2,3,4,5-tetrahydro-4-methyl-3-oxo-1H-1,4-benzodiazepine-2-acetic acid, hydrochloride, processes for its preparation and methods for its use.Type: GrantFiled: March 3, 1999Date of Patent: January 1, 2002Assignee: SmithKline Beecham CorporationInventor: Stephen Torey Ross
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Patent number: 6225465Abstract: A new process for preparing substituted 7-aminocarbonyl-3-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepines is disclosed.Type: GrantFiled: May 14, 1999Date of Patent: May 1, 2001Assignee: SmithKline Beecham plcInventors: Stephen K. Etridge, Timothy Charles Walsgrove, Jerome Hayes, Andrew S. Wells
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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: 6015791Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole, and triazoles, in particular those including a cycloheptane structure, that are useful as serine protease inhibitors, including inhibitors for human neutrophil elastase. Compounds of the invention are useful in treating conditions such as adult respiratory distress syndrome, septic shock, and multiple organ failure.Type: GrantFiled: December 4, 1997Date of Patent: January 18, 2000Assignee: Cortech Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 6008214Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, which are effective for inhibiting platelet aggregation and bone resorption, pharmaceutical compositions for effecting such activity, and a method for using these compounds.Type: GrantFiled: February 18, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beecham CorporationInventors: Chet Kwon, William Henry Miller
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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: 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
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Patent number: RE44205Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compType: GrantFiled: April 6, 2012Date of Patent: May 7, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil