Acyclic Nitrogen Bonded Directly To The Hetero Ring Patents (Class 540/509)
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Patent number: 7205293Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, 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 is involved.Type: GrantFiled: March 10, 2004Date of Patent: April 17, 2007Assignee: Merck & Co., Inc.Inventors: Ian M. Bell, Samuel L. Graham, Theresa M. Williams, Craig A. Stump
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Patent number: 7196079Abstract: The present invention is directed to compounds of Formula I: (where variables R1, R2, R3, R6, R7, G, J, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, 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 is involved.Type: GrantFiled: June 24, 2004Date of Patent: March 27, 2007Assignee: Merck & Co, Inc.Inventors: Christopher S. Burgey, Craig A. Stump, Theresa M. Williams
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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: 7115598Abstract: The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.Type: GrantFiled: April 21, 2004Date of Patent: October 3, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Tianbao Lu, Karen L. Milkiewicz, Pierre Raboisson, Maxwell David Cummings, Raul R. Calvo, Daniel J. Parks, Louis V. Lafrance, III, Juan Jose Marugan Sanchez, Joan Gushue, Kristi Leonard
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Patent number: 7105509Abstract: A novel class of 1,4- and 1,5-benzodiazepines of formula (I) is disclosed.Type: GrantFiled: May 21, 2001Date of Patent: September 12, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Ian Churcher, Alexander Richard Guiblin, Timothy Harrison, Sonia Kerrard, Andrew Madin, Alan John Nadin, Andrew Pate Owens, Timothy Jason Sparey, Martin Richard Teall, Susannah Williams
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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: 6995155Abstract: 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: GrantFiled: August 8, 2001Date of Patent: February 7, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Ian Churcher, Alan John Nadin, Andrew Pate Owens
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Patent number: 6960576Abstract: 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: November 4, 2002Date of Patent: November 1, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Richard E. Olson, Hong Liu, Lorin A. Thompson
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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: 6825191Abstract: The present invention provides benzodiazepine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of inhibiting activated blood-coagulation factor X. These compounds are usable as agents for treating various diseases concerned with the activated blood-coagulation factor X.Type: GrantFiled: March 27, 2003Date of Patent: November 30, 2004Assignee: Ajinomoto Co., Inc.Inventors: Tadakiyo Nakagawa, Munetaka Tokumasu, Kazumi Tashiro, Mitsuo Takahashi, Takashi Kayahara, Shunji Takehana, Yuki Kajigaya, Kaoru Yoshida, Kuniya Sakurai
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Patent number: 6759404Abstract: Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein.Type: GrantFiled: April 3, 2001Date of Patent: July 6, 2004Inventors: Richard E. Olson, Michael G. Yang
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Patent number: 6756511Abstract: Gamma-secretase inhibitors, useful in the treatment or prevention of Alzheimer's disease, are disclosed. The preferred compounds have, as the central portion of the molecule, the structure (a) and are di-astereoisomers of known protease inhibitors.Type: GrantFiled: July 18, 2002Date of Patent: June 29, 2004Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Timothy Harrison, Peter Alan Hunt, Alan John Nadin
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Patent number: 6713476Abstract: 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&bgr;-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 &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: April 3, 2001Date of Patent: March 30, 2004Assignee: Dupont Pharmaceuticals CompanyInventors: Michael G Yang, Hong Liu
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Patent number: 6632812Abstract: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-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 &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: April 11, 2001Date of Patent: October 14, 2003Assignee: Dupont Pharmaceuticals CompanyInventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
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Patent number: 6569851Abstract: 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 that include 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: June 22, 1999Date of Patent: May 27, 2003Assignees: Elan Pharmaceutials, Inc., Eli Lilly & CompanyInventors: Richard C. Thompson, Stephen Wilkie, Douglas R. Stack, Eldon E. VanMeter, Qing Shi, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
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Patent number: 6552041Abstract: The present invention relates to cyclized amide derivatives of formula (I) These cyclized amide derivatives are useful for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: GrantFiled: January 3, 2002Date of Patent: April 22, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Lauffer, Michael Mullican, Brian Ledford
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Patent number: 6509333Abstract: 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&bgr;-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 &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: June 1, 2001Date of Patent: January 21, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard E. Olson
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Patent number: 6503901Abstract: 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&bgr;-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 &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: October 7, 2000Date of Patent: January 7, 2003Assignee: Bristol Myers Squibb Pharma CompanyInventors: Lorin Andrew Thompson, Amy Qi Han
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Patent number: 6503902Abstract: 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&bgr;-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 &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: March 14, 2001Date of Patent: January 7, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Richard Eric Olson, Hong Liu, Lorin Andrew Thompson, III
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Publication number: 20020183313Abstract: Benzodiazepine derivatives of the formula: 1Type: ApplicationFiled: March 20, 2002Publication date: December 5, 2002Applicant: Fujisawa Pharmaceutical Co., Ltd.Inventors: Yoshinari Sato, Seiichiro Tabuchi, Hitoshi Mitsui, Ikuyo Katsumi, Naoko Yamamoto
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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: 6333321Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: August 11, 1998Date of Patent: December 25, 2001Assignee: COR Therapeutics, Inc.Inventor: Robert Scarborough
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Patent number: 6329365Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme (“ICE”). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.Type: GrantFiled: June 4, 1999Date of Patent: December 11, 2001Assignee: Vertex Pharmaceuticals, Inc.Inventors: Julian M. C. Golec, David J. Lauffer, David J. Livingston, Michael D. Mullican, Mark A. Murcko, Philip L. Nyce, Andrea L. C. Robidoux, Marion W. Wannamaker
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Patent number: 6291452Abstract: Benzodiazepine derivatives of the formula: wherein R2 is alkyl or cycloalkyl-alkyl when R4 is hydrogen, or R2 is a variety of specified groups when R4 is alkyl, halogen or dialkylamino, are useful as cholecystokinin antagonists.Type: GrantFiled: April 30, 1999Date of Patent: September 18, 2001Assignees: Fujisawa Pharmacetical Co., Ltd., Nippon Shokubai Co., Ltd.Inventors: Yoshinari Sato, Seiichiro Tabuchi, Hitoshi Mitsui, Ikuyo Katsumi, Naoko Yamamoto
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Patent number: 6232308Abstract: The present invention relates to benzazepine derivatives and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.Type: GrantFiled: February 2, 2000Date of Patent: May 15, 2001Assignee: Merck & Co., Inc.Inventor: Ben C. Askew
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Patent number: 6214823Abstract: This invention is concerned with novel compounds represented by structural formula I which are useful in the treatment of arrhythmia.Type: GrantFiled: October 6, 1998Date of Patent: April 10, 2001Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, David A. Claremon, Harold G. Selnick
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Patent number: 6121258Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: August 26, 1997Date of Patent: September 19, 2000Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
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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: 5998407Abstract: The present invention is directed to substituted benozdiazepine compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: October 1, 1998Date of Patent: December 7, 1999Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, John S. Wai, Neville J. Anthony
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Patent number: 5962451Abstract: A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein (a) R.sup.1 is --CH.sub.2 CHOH(CH.sub.2).sub.a R.sup.4 or a ketone group --CH.sub.2 CO(CH.sub.2).sub.a R.sup.5 in which a is 0 or 1 and R.sup.4 and R.sup.5 are selected from alkyl and cycloalkyl groups and saturated heterocyclic groups optionally substituted at a hetero-atom; (b) R.sup.2 and R.sup.3 are independently selected from aromatic carbocyclic and heterocylic residues; and (c) W and X are selected independently from halogen and hydrogen atoms and alkyl and alkoxy groups. These compounds are gastrin and/or CCK-B receptor antagonists.Type: GrantFiled: June 6, 1997Date of Patent: October 5, 1999Assignees: Ferring BV, Yamanouchi Pharmaceutical Co. Ltd.Inventors: Hamish Ryder, Graeme Semple, David Alan Kendrick, Michael Szelke, Masato Satoh, Mitsuaki Ohta, Keiji Miyata, Akito Nishida
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Patent number: 5852010Abstract: The present invention is directed to substituted benozdiazepine compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: March 25, 1997Date of Patent: December 22, 1998Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, Neville J. Anthony, John S. Wai
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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: 5795887Abstract: A method of inducing a Cholescystokinin-A receptor agonist response in a mammal by administering a compound of formula (I), ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3-6 cycloalkyl, phenyl, or substituted phenyl; R.sup.2 is C.sub.3-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 alkenyl, benzyl, phenylC.sub.1-3 alkyl or substituted phenyl; or NR.sup.1 R.sup.2 together form 1,2,3,4-tetrahydroquinoline or benzazepine mono-, di-, or trisubstituted independently with C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen substituents; n is an integer selected from the grouping consisting of 0,1,2 or 3; p is the integer 0 or 1; q is the integer 0 or 1; r is the integer 0 or 1, provided that when q is 0 then r is 0; R.sup.3, R.sup.4, R.sup.5 and R.sup.8 are selected from a variety of substituents; X is nitrogen, nitroso or R.sup.Type: GrantFiled: October 11, 1996Date of Patent: August 18, 1998Assignee: Glaxo Wellcome Inc.Inventors: Christopher Joseph Aquino, Milana Dezube, Ronald George Sherrill, Elizabeth Ellen Sugg, Jerzy Ryszard Szewczyk, Timothy Mark Willson
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Patent number: 5770731Abstract: A prodrug of the general formula FTLi-(PRT)m, where m is an integer from 1 to 5; FTLi is a ras inhibitor such as a farnesyltransferase inhibitor compound, such as Ia, Ib, Ic; and PRT represents m protecting groups or a precursor thereof, such as compound XVI, which are capable of being cleaved from the ras inhibitor by the action of a enzyme.Type: GrantFiled: April 19, 1996Date of Patent: June 23, 1998Assignee: Cancer Research Campaign Technology LimitedInventors: Caroline Joy Springer, Richard Marais
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Patent number: 5763437Abstract: Benzodiazepine derivatives of formula (I) wherein R.sup.1 is aryl which may have one or more suitable substituent(s), R.sup.2 is C.sub.3 -C.sub.8 cycloalkyl which may have one or more suitable substituent(s), A is lower alkylene, R.sup.3 is a heterocyclic group selected from the group consisting of tetrahydrofuryl, dioxolanyl, filryl, thienyl, isoxazolyl, pyridyl, benzimidazolyl, benzotiazolyl, benzoxazolyl, benzopyrany, quinolyl, isoquinolyl, tetrahydroisoquinolyl, benzothienyl and benzofuryl, each of which may have one or more suitable substituent(s), or a pharmaceutically acceptable salt thereof, which are useful as a medicament.Type: GrantFiled: January 29, 1997Date of Patent: June 9, 1998Assignees: Fujisawa Pharmaceutical Co., Ltd., Nippon Shokubai Co., Ltd.Inventors: Yoshinari Sato, Kazuo Sakane, Seiichiro Tabuchi, Hitoshi Mitsui, Ikuyo Katsumi, Yuichi Satoh
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Patent number: 5753650Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer, which compound has the structure; ##STR1## or a pharmaceutically acceptable salt or disulfide thereof and wherein the variables are as defined in the specification.Type: GrantFiled: November 6, 1996Date of Patent: May 19, 1998Assignee: Merck & Co., Inc.Inventors: John S. Wai, J. Christopher Culberson, Samuel L. Graham
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Patent number: 5728829Abstract: A benzodiazepine derivative of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein: (a) R.sup.4 is an alkyl, cycloalkyl or aryl group.(b) R.sup.10 is chosen from halo, OH, CH.sub.3, OCH.sub.3, NR.sup.11 R.sup.12, NO.sub.2, NHCHO, CO.sub.2 H and CN, and R.sup.11 and R.sup.12 are independently selected from H and alkyl (C.sub.1 -C.sub.5) or together NR.sup.11 R.sup.12 form a cyclic structure II, ##STR2## wherein a is 1-6; and (c) R.sup.2 is an aromatic 5- or 6-membered, substituted or unsubstituted heterocycle containing at least two heteroatoms of which at least one is nitrogen.These compounds are gastrin and/or CCK-B receptor antagonists.Type: GrantFiled: May 2, 1996Date of Patent: March 17, 1998Assignees: Ferring-Research Limited, Yamanouchi Pharmaceutical Co. Ltd.Inventors: Graeme Semple, Hamish Ryder, Michael Szelke, Masato Satoh, Mitsuaki Ohta, Keiji Miyata, Akito Nishida, Masato Ishii
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Patent number: 5719143Abstract: The invention relates to the compounds of formula (I) ##STR1## in which R.sub.I, R.sub.II, X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are as defined in claim 1.Type: GrantFiled: February 14, 1995Date of Patent: February 17, 1998Assignee: SanofiInventors: Alain Badorc, Pierre Despeyroux, Daniele Gully, Paul de Cointet, Daniel Frehel, Jean-Pierre Maffrand
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Patent number: 5696110Type: GrantFiled: September 5, 1995Date of Patent: December 9, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Sylvie Bourrain, Stephen Robert Fletcher, Victor Giulio Matassa, Graham Andrew Showell
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Patent number: 5688943Abstract: This invention relates to benzodiazepine derivatives which are useful as drugs exhibiting antagonism at the gastrin and/or CCK-B receptor, and to their production.Type: GrantFiled: September 14, 1994Date of Patent: November 18, 1997Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hamish Ryder, Graeme Semple, David Alan Kendrick, Michael Szelke, Masato Satoh, Mitsuaki Ohta, Keiji Miyata, Akito Nishida
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Patent number: 5658901Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## where X and Y are independently hydrogen, chloro, fluoro, bromo, iodo, or trifluoromethyl and n is 0, 1 or 2;R is hydrogen, fluoro, chloro, bromo, iodo, or trifluoromethyl, methyl, or methoxy; andthe racemates, mixtures of enantiomers, individual diastereomers or individual enantiomers with all isomeric forms and pharmaceutically acceptable salts, hydrates or crystal forms thereof, which are antiarrhythmic agents.Type: GrantFiled: August 17, 1995Date of Patent: August 19, 1997Assignee: Merck & Co., Inc.Inventors: David A. Claremon, Nigel Liverton, Harold G. Selnick
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Patent number: 5637585Abstract: This invention provides the form B crystal of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazep in-3-yl]-3-(3-tolyl)urea which is produced by recrystallizing the compound from a mixed solvent of at least 1 volume of water and 5 volumes of an alcohol. The form B crystals have excellent filtration property and flowability, so that they can be handled markedly easily at the time of filtration for their large scale production or when they are made into pharmaceutical preparations and therefore are useful in view of their industrial production.Type: GrantFiled: December 21, 1995Date of Patent: June 10, 1997Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Makoto Nakamura, Kouichi Watanabe
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Patent number: 5633251Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## where R.sup.1 is ##STR2## X and Y are independently hydrogen, fluoro, chloro, bromo, iodo, or trifluoromethyl;n is 0, 1 or 2; andR.sup.2 is hydrogen, fluoro, chloro, bromo, iodo, or trifluoromethyl, methyl, or methoxy;as the racemates, mixtures of enantiomers, individual diastereomers or individual enantiomers, and pharmaceutically acceptable crystal forms, salts, or hydrates thereof.Type: GrantFiled: August 17, 1995Date of Patent: May 27, 1997Assignee: Merck & Co., Inc.Inventors: David A. Claremon, Nigel Liverton, Harold G. Selnick
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Patent number: 5631251Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## Z is C.sub.0-6 alkyl; and R.sup.1 is phenyl or mono or disubstituted phenyl, where the substitutents are Cl, and CF.sub.3,or pharmaceutically acceptable salts, hydrates and crystal forms thereof which are useful in the treatment of arrhythmia.Type: GrantFiled: June 7, 1995Date of Patent: May 20, 1997Assignee: Merck & Co., Inc.Inventors: John Butcher, David A. Claremon, Nigel Liverton, Harold G. Selnick
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Patent number: 5618812Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents H, optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 is NHR.sup.12 or (CH.sub.2).sub.s R.sup.13 where 5 is 0, 1 or 2; R.sup.3 represents C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 and R.sup.5 are H, C.sub.1-12 alkyl optionally substituted by NR.sup.9 R.sup.9' or an azacyclic or azabicyclic group, optionally substituted C.sub.4-9 cycloalkyl, C.sub.4-9 cycloalkyl C.sub.1-4 alkyl, aryl, arylC.sub.1-6 alkyl or azacyclic or azabicyclic groups, or R.sup.4 and R.sup.5 together form the residue of an optionally substituted azacyclic or azabicyclic ring system; x is 0, 1, 2 or 3; R.sup.12 is optionally substituted phenyl or pyridyl; R.sup.13 represents a group (A) wherein R.sup.14 is H or C.sub.1-6 alkyl; R.sup.15 is H, C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; and the dotted line is an optional covalent bond; are CCK and/or gastrin antagonists useful in therapy.Type: GrantFiled: January 26, 1995Date of Patent: April 8, 1997Assignee: Merck Sharp & Dohme, Ltd.Inventors: Jose L. Castro Pineiro, William R. Carling, Mark S. Chambers, Stephen R. Fletcher, Sarah C. Hobbs, Victor G. Matassa, Kevin W. Moore, Graham A. Showell, Michael G. Russell
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Patent number: 5597915Abstract: Compounds of Formula (I), and salts and prodrugs thereof wherein: R.sup.1 is H, certain optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 represents a group (a) wherein X is O, S or NR.sup.8 where R.sup.8 is H or C.sub.1-4 alkyl; one of Z and Y is C.dbd.O and the other is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-4 alkyl; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 is C.sub.3-10 cycloalkyl; n is 0, 1, 2 or 3, and are CCK and/or gastrin antagonists, which compounds and compositions thereof are useful in therapy.Type: GrantFiled: September 15, 1994Date of Patent: January 28, 1997Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark S. Chambers, Stephen R. Fletcher, Victor G. Matassa, Mark G. Bock
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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: 5563136Abstract: This invention relates to compounds having formula (I), ##STR1## wherein R.sub.1 is a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, nitro, hydroxy or cyano radical; R.sub.2 is an alkyl radical or a chain --CH(R.sub.5)--CO--R.sub.6 ; R.sub.3 is (a) a phenyl radical substituted by one or a plurality of substituents selected amongst the radicals -alk-SO.sub.3 H, -alk-PO.sub.3 H.sub.2, --CH.dbd.NOH, --CH--NO-alk-COOX, --S-alk-COOX, --SO-alk-COOX, --SO.sub.2 -alk-COOX, --CH.dbd.CH--COOX, -alk-CO--NHOH, --C(.dbd.NOH)--COOX, -alk-N(OH)--CO-alk,-alk-SO.sub.2 H, --CH.dbd.CH--SO.sub.3 H, --C(COOX).dbd.N--O-alk-COOX, tetrazolyalkyle or a group having a formula (I) or (b) a ring having the formula (A) ##STR2## wherein R.sub.9 is a radical .dbd.NOX, .dbd.NO-alk-COOX, .dbd.CH--COOX, -alk-COOX, -alk-SO.sub.2 H or -alk-S).sub.3 H, R.sub.10 is an oxygen or sulfur atom or a methylene or alkylimino radical and R.sub.11 is a methylene or ethylene radical, R.sub.Type: GrantFiled: April 6, 1994Date of Patent: October 8, 1996Assignee: Rhone-Poulenc Rorer S.A.Inventors: Marc Capet, Claude Cotrel, Marie-Christine Dubroeuco, Claude Guyon, Jean-Paul Martin
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Patent number: 5556969Abstract: Compounds of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or specified optionally substituted alkyl, R.sup.2 is specified optionally substituted phenyl or pyridyl, x is 0, 1, 2 or 3, R.sup.3 is a specified alkyl, halo or amino and R.sup.4 is specified cycoalkyl or bicycloalkyl; and salts and prodrugs thereof, are useful as antagonists of cholecystokin and gastrin receptors.Type: GrantFiled: June 29, 1995Date of Patent: September 17, 1996Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark S. Chambers, Stephen R. Fletcher