The Bicyclo Ring System Is 1,5-benzodiazepine (including Hydrogenated) Patents (Class 540/517)
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Patent number: 6258948Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-IB converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. 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 IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention.Type: GrantFiled: September 21, 1999Date of Patent: July 10, 2001Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
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Patent number: 6239131Abstract: 1,5-Benzodiazepine derivatives represented by formula (I), salts thereof, and medicines containing the same as the active ingredient: The compounds exhibit excellent gastrin and/or CCK-B receptor antagonism and are useful as remedies for gastric ulcer and gastrointestinal movement disorder.Type: GrantFiled: June 8, 1999Date of Patent: May 29, 2001Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Katsuo Shinozaki, Tomoyuki Yoneta, Masakazu Murata, Naoyoshi Miura, Kiyoto Maeda
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Patent number: 5985869Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substitued benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups beign optionally replaced by O, S, SO, SO.sub.Type: GrantFiled: July 15, 1997Date of Patent: November 16, 1999Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Shinya Kora, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5834463Abstract: Compounds represented by the formula: ##STR1## wherein ring A is benzene; Ar is aromatic group; R.sup.1, R.sup.2 and R.sup.3 each stands for H, acyl, hydrocarbon or heterocyclic, or R.sup.2 and R.sup.3, taken together, may form non-aromatic cyclic hydrocarbon; X is methylene or carbonyl; ......... is single bond or double bond; when ......... is single bond, Y is --NR.sup.4 -- (R.sup.4 is H, acyl, hydrocarbon or heterocyclic), when ......... is double bond, Y is N; n is 1-3, provided that, X is carbonyl and, at the same time, R.sup.2 and R.sup.3, taken together, form non-aromatic cyclic hydrocarbon, ......... is double bond or R.sup.4 is a heterocyclic or --Z(CH.sub.2).sub.m --W (Z is methylene or carbonyl, W is optionally substituted amino, and m denotes 0-5), or salts thereof have an excellent GnRH receptor antagonistic action and/or an action of improving sleep disturbances.Type: GrantFiled: June 26, 1995Date of Patent: November 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Nobuhiro Fujii, Koichi Kato, Masaomi Miyamoto
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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: 5726171Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.Type: GrantFiled: March 13, 1996Date of Patent: March 10, 1998Inventors: David A. Claremon, Nigel Liverton, Garry R. Smith, Harold G. Selnick
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Patent number: 5691332Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.Type: GrantFiled: August 19, 1996Date of Patent: November 25, 1997Assignee: Merck & Co., Inc.Inventors: David A. Claremon, Roger M. Freidinger, Nigel Liverton, Harold G. Selnick, Garry R. Smith
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Patent number: 5677299Abstract: Novel benzoheterocyclic compound of the formula (1): ##STR1## and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist or oxytocin antagonist.Type: GrantFiled: June 6, 1995Date of Patent: October 14, 1997Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Hidenori Ogawa, Kazumi Kondo, Hiroshi Yamashita, Keizo Kan, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5569654Abstract: Compounds of general formula (I) ##STR1## and physiologically acceptable salts thereof; wherein R.sub.1 represents CH.sub.2 CONR.sub.5 R.sub.6 or CH.sub.2 COR.sub.7 ;R.sub.2 represents a phenyl group optionally substituted by 1 or 2 substituents selected from halogen, alkyl, nitro, cyano, trifluoromethyl, trifluoromethoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, amino, substituted amino, hydroxy, alkoxy, methylenedioxy, alkoxycarbonyl, oxazolyl or oxadiazolyl;A represents a C.sub.1-4 straight or branched alkylene chain;R.sub.3 and R.sub.4 independently represent hydrogen or C.sub.1-4 alkyl or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form a saturated 5-7 membered heterocyclic ring, which ring may contain an additional heteroatom selected from oxygen, sulphur or nitrogen;R.sub.5 represents hydrogen or C.sub.1-4 alkyl;R.sub.6 represents C.sub.1-4 alkyl or phenyl, optionally substituted by halogen, or R.sub.5 and R.sub.Type: GrantFiled: June 5, 1995Date of Patent: October 29, 1996Assignee: Glaxo Group LimitedInventors: Duncan R. Armour, Philip C. Box, Pritom Shah
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Patent number: 5521170Abstract: Compounds having the structure below ##STR1## and pharmaceutically acceptable salts thereof exhibit vasopressin antagonistic activity, vasodilating activity, hypotensive activity, activity for inhibiting saccharide release in the liver, activity for inhibiting growth of mesagium cells, water diuretic activity, platelet agglutination inhibitory activity, oxytocin antagonistic activity and the like, and are useful in treating or preventing hypertension, heart failure, renal insufficiency, edema, ascites, vasopressin parasecretion syndrome, hepatocirrhosis, hyponatremia, hypokalemia, diabetic or circulation disorder, oxytocin related diseases and the like.Type: GrantFiled: March 31, 1994Date of Patent: May 28, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Keiji Hemmi, Hirokazu Tanaka
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Patent number: 5434261Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: July 26, 1993Date of Patent: July 18, 1995Assignee: Merck & Co., Inc.Inventors: William R. Schoen, Matthew J. Wyvratt, Jr.
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Patent number: 5430144Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: July 26, 1993Date of Patent: July 4, 1995Assignee: Merck & Co., Inc.Inventors: William R. Schoen, Matthew J. Wyvratt, Jr., Paul J. Hodges
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Patent number: 5374721Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: October 14, 1992Date of Patent: December 20, 1994Assignee: Merck & Co., Inc.Inventors: William R. Schoen, Matthew J. Wyvratt
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Patent number: 5216148Abstract: Described herein are compounds of the formula ##STR1## wherein R.sup.1 signifies hydrogen, lower-alkyl or a cation;R.sup.2 signifies hydrogen, lower-alkyl, lower-alkoxy or halogen;M signifies --CONH-- or --NHCO--;X and Y are each independently selected from the group consisting of >CR.sup.3 R.sup.4 and --CONR.sup.5 --;Z signifies >CR.sup.6 R.sup.7 ;R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are each independently selected from the group consisting of hydrogen and lower-alkyl;R.sup.5 signifies alkyl; andn signifies 0, 1 or 2;provided that at least one of X or Y is --CONR.sup.5 -- which is bonded to the phenyl ring via the N atom.These compounds are useful in the treatment and prophylaxis of neoplasms, dermatoses and aging of the skin.Type: GrantFiled: February 27, 1992Date of Patent: June 1, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
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Patent number: 5055464Abstract: Benzolactam compounds of the general formula ##STR1## or isomers thereof as well as salts thereof inclusive of hydrates and/or solvates forms thereof, and benzolactam compounds of the general formula ##STR2## wherein each of the symbols is as defined in the specification. The compound (I) exhibit antiamnesic activity, and are useful as brain function-improving drugs. The compounds (a) and (b) are useful as an intermediate for said compounds (I). Futher, the compound (a) show diuretic or antiulcer activity, and are useful as a diuretic or antiulcer agent.Type: GrantFiled: January 25, 1990Date of Patent: October 8, 1991Assignee: Yoshitomi Pharmaceutical Industries Ltd.Inventors: Shu Murakami, Tsuguo Ikebe, Ichiro Hakamada, Koretake Anami
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Patent number: 5008263Abstract: Platelet activating factor antagonists of formula (I), (II) or (III): ##STR1## where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or isothiazole,X is O, S or NHY is 1,4 phenylene or a group of formula ##STR2## R.sup.1 is H or optionally substituted C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 are H or C.sub.1 -C.sub.4 alkyl,B is an optionally fused 5- or 6-membered ring containing nitrogen atoms,Het is an optionally substituted 5-membered heterocyclic ring containing nitrogen or a pyridine ring, the ring optionally being fused to benzene or nitrogen-containing heterocyclic ring.Type: GrantFiled: March 20, 1990Date of Patent: April 16, 1991Assignee: Pfizer Inc.Inventors: Kelvin Cooper, Michael J. Fray
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Patent number: 4764512Abstract: This invention relates to substituted benzodiazinone-pyridone compounds and their use as cardiotonic agents including methods for increasing cardiac contractility, pharmaceutical compositions including the same and methods for the preparation thereof.Type: GrantFiled: August 27, 1986Date of Patent: August 16, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Bruce F. Molino, Henry F. Campbell, Donald E. Kuhla, William L. Studt
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Patent number: 4666913Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of hydroxy and aminothiazolyl-benzodiazinone compounds and pharmaceutical compositions including the same.Type: GrantFiled: November 22, 1985Date of Patent: May 19, 1987Assignee: William H. Rorer, Inc.Inventors: Donald E. Kubla, Henry F. Campbell, William L. Studt, Bruce F. Molino, Thomas J. Tucker