Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 540/521)
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Patent number: 6093714Abstract: Tricyclic benzazepine compounds represented by the following formula (I) and pharmacologically acceptable salts thereof are disclosed. These compounds have antiallergic activity and are useful for treatment and prevention of bronchial asthma, eczema, hives, allergic gastrointestinal troubles, allergic rhinitis, allergic conjunctivitis, etc. wherein R represents a hydrogen atom, substituted C.sub.1-6 alkyl or a protective group and R.sup.1, R.sup.2, R.sup.3, and R.sup.4 represent a hydrogen atom, a hydroxyl group, substituted C.sub.1-4 alkyl, substituted C.sub.2-12 alkenyl, substituted C.sub.1-12 alkoxy, or substituted amino.Type: GrantFiled: June 17, 1998Date of Patent: July 25, 2000Assignee: Meiji Seika Kaisha, Ltd.Inventors: Yasuo Ohtsuka, Toshio Nishizuka, Sohjiro Shiokawa, Seiji Tsutsumi, Kenichi Fusihara, Mami Kawaguchi, Megumi Imai, Keiko Shito, Koji Tsuchiya, Takako Iwasaki, Hiroko Ogino, Takashi Shishikura
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Patent number: 6051705Abstract: The present invention relates to a substituted thiazolo[3,2-a] azepine derivative having inhibitory activity against angiotensin I converting enzyme and neutral endpeptidase and is represented by the following general formula (I): ##STR1##Type: GrantFiled: May 27, 1998Date of Patent: April 18, 2000Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Shinji Suda, Naoki Yoneda, Makoto Kotake, Masanori Mizuno, Tomohiro Matsushima, Yoshio Fukuda, Mamoru Saito, Toshiyuki Matsuoka, Hideyuki Adachi, Masayuki Namiki, Takeshi Sudo, Kazutoshi Miyake, Makoto Okita
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Patent number: 6030967Abstract: A compound of the formula: whereinQ is an optionally substituted carbon atom or N(O)p wherein p is 0 or 1;Y is an optionally substituted methylene group, S(O)q wherein q is an integer of 0 to 2, or an optionally substituted imino group;Z.sup.1 is a C.sub.1-3 alkylene group which may have an oxo group or a thioxo group and may contain etherified oxygen or sulfur within the carbon chain;Z.sup.2 is an optionally substituted C.sub.1-3 alkylene group;Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;one of R.sup.1 and R.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group;the other is a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; orR.sup.1 and R.sup.2 taken together with adjacent --c.dbd.c-- form a ring; andring A is a benzene ring which may be substituted in addition to R.sup.1 and R.Type: GrantFiled: October 30, 1997Date of Patent: February 29, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Masaki Ogino
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Patent number: 6018043Abstract: The subject invention concerns a process for preparing a compound of formula (3) ##STR1## in enantio-enriched form, comprising reducing a compound of formula (4) ##STR2## using an asymmetric enantiospecific reductant, wherein A.sup.1 .dbd.A.sup.2 .dbd.H or A.sup.1, A.sup.2 .dbd.O; B.sup.1 .dbd.B.sup.2 .dbd.H or B.sup.1, B.sup.2 .dbd.O; Z.dbd.H, C.sub.1-20 alkyl or a precursor thereof, or a removable protecting group for nitrogen, e.g, acyl or alkyloxycarbonyl; Y.dbd.H or a substituent; R.sup.1 .dbd.C.sub.1-20 alkyl; and R is an optional, additional substituent.Type: GrantFiled: February 2, 1998Date of Patent: January 25, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Ulrich Conrad Dyer, Jane Marie Paul, Raymond McCague
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Patent number: 5962448Abstract: A pyrroloazepine compound having the following formula (I): whereinthe ring P represented by ##STR1## is a pyrrole ring having the following structure: ##STR2## wherein R.sub.1 represents C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.8 cycloalkyl-alkyl, C.sub.6 -C.sub.14 aryl or C.sub.7 -C.sub.22 aralkyl, which are optionally substituted; and R.sub.2 represents H or C.sub.1 -C.sub.8 alkyl, which is optionally substituted; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z.sub.2 is not present and Z.sub.1 represents H, but, when the bond is absent, Z.sub.1 and Z.sub.2 are both H; Z.sub.1 represents H and Z.sub.2 represents a group OR.sub.3, in which R.sub.3 represents H, C.sub.1 -C.sub.8 alkyl, or C.sub.7 -C.sub.22 aralkyl, which are optionally substituted; Z.sub.1 and Z.sub.2 both represent groups SR.sub.4, in which R.sub.4 represents C.sub.1 -C.sub.8 alkyl or C.sub.7 -C.sub.22 aralkyl, which are optionally substituted; or Z.sub.1 and Z.sub.Type: GrantFiled: August 21, 1997Date of Patent: October 5, 1999Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Tetsuo Shimamoto, Kyoko Nakanishi, Norio Inomata
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Patent number: 5919778Abstract: The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1-(CH2)n-Z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R3 being hydrogen or a lower alkyl, R4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.Type: GrantFiled: May 25, 1995Date of Patent: July 6, 1999Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Masahiro Yonaga, Norio Karibe, Youichi Iimura, Satoshi Nagato, Atsushi Sasaki, Yoshiharu Yamanishi, Hiroo Ogura, Takashi Kosasa, Kumi Uchikoshi, Kiyomi Yamatsu
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Patent number: 5908841Abstract: There are disclosed compounds of the formula 1 ##STR1## wherein X is an oxygen atom or nothing and R1, R2 and R3 are as defined in the specification, useful in the prevention or treatment of HIV infection.Type: GrantFiled: August 11, 1998Date of Patent: June 1, 1999Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: John R. Proudfoot, Karl D. Hargrave
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Patent number: 5872251Abstract: The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme.Type: GrantFiled: November 10, 1997Date of Patent: February 16, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Gary A. Flynn, Thomas D. Bannister
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Patent number: 5849908Abstract: The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme.Type: GrantFiled: November 10, 1997Date of Patent: December 15, 1998Assignee: Hoechst Marion Roussel Inc.Inventors: Gary A. Flynn, Michael J. Genin, Douglas W. Beight
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Patent number: 5834609Abstract: The subject invention provides a bicyclic aminoimidazole compound, a hydroxyalkyl aminoimidazole compound, a bicyclic pyrrole compound, a hymenin compound, an aldehyde aminoimidazole compound, a ketal aminoimidazole compound, a tricyclic compound, and a tetrahydropurine compound. The subject invention also provides for processes for preparing the compounds. The bicyclic aminoimidazole compounds of the invention have anti-tumor and anti-microbial activity.Type: GrantFiled: October 6, 1995Date of Patent: November 10, 1998Assignee: The Trustees of Columbia University in the City of New YorkInventors: David A. Horne, Kenichi Yakushijin
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Patent number: 5789587Abstract: There are disclosed certain novel compounds identified as heterocyclic-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 heterocyclic-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: November 6, 1996Date of Patent: August 4, 1998Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Helmut Mrozik, William R. Schoen, Thomas L. Shih, Matthew J. Wyvratt
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Patent number: 5789403Abstract: The present invention relates to a substituted thiazolo?3,2-a!azepine derivative having inhibitory activity against angiotensin I converting enzyme and neutral endpeptidase.Type: GrantFiled: March 11, 1996Date of Patent: August 4, 1998Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Shinji Suda, Naoki Yoneda, Makoto Kotake, Masanori Mizuno, Tomohiro Matsushima, Yoshio Fukuda, Mamoru Saito, Toshiyuki Matsuoka, Hideyuki Adachi, Masayuki Namiki, Takeshi Sudo, Kazutoshi Miyake, Makoto Okita
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Patent number: 5760220Abstract: A process is described for preparing a compound of the formula I: ##STR1## or a salt thereof; wherein X is a protecting group and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1-6 alkyl or C.sub.1-6 perfluoroalkyl, R.sub.5 is hydrogen or when n is 1 R.sub.5 taken together with R.sub.3 comprises a double bond; m is 1, 2 or 3; n is 0 or 1, and p is 0, 1 or 2.Type: GrantFiled: June 4, 1996Date of Patent: June 2, 1998Assignee: American Home Products CorporationInventors: Pierre Giguere, Silvio Iera, Michel Bernatchez, Giuseppe Barreca, Graziano Castaldi, Vincenzo Cannata
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Patent number: 5750556Abstract: Compounds of Formula I are selective autoreceptor agonists useful in treating disease states involving hyperactivity of dopamine systems: ##STR1## in which X is --(CH.sub.2).sub.n --; n is 1-3; R.sub.1 is hydrogen, alkyl, hydroxyalkyl, cycloalkyl-methyl, bicyclo-alkylmethyl or --(CH.sub.2).sub.m YAr; where m is 0-4, Y is --CH.sub.2 --, and Ar is phenyl, halophenyl, alkylphenyl, dialkylphenyl or alkoxyphenyl; R.sub.2 is hydrogen or alkyl; R.sub.3 is hydrogen, halogen, alkyl, alkoxy or hydroxy; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 30, 1996Date of Patent: May 12, 1998Assignee: American Home Products CorporationInventors: Richard E. Mewshaw, Gary P. Stack
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Patent number: 5750521Abstract: The present invention relates to certain mercaptoacetylamide disulfide derivatives of Formula (I) ##STR1## useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: November 4, 1996Date of Patent: May 12, 1998Assignee: Hoechst Marion Roussel Inc.Inventors: Gary A. Flynn, Douglas W. Beight, Shujaath Mehdi, Alan M. Warshawsky, John F. French, John H. Kehne
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Patent number: 5750702Abstract: The present invention encompasses structures of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted phenyl;X is hydrogen, hydroxy or lower alkyl;T is hydrogen, halogen, hydroxy, nitro, amino or alkyl;R.sub.3 is hydrogen or an organic group;R.sub.4 is hydrogen or substituted or unsubstituted organic substituent;R.sub.5 and R.sub.6 represent organic, and inorganic substituents; andn is 1, 2, 3, or 4,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: July 16, 1996Date of Patent: May 12, 1998Assignee: Neurogen CorporationInventors: Pamela Albaugh, Alan Hutchison
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Patent number: 5734049Abstract: The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme.Type: GrantFiled: November 4, 1996Date of Patent: March 31, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Gary A. Flynn, Michael J. Genin, Douglas W. Beight
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Patent number: 5708168Abstract: Disclosed are methods of preparing azepines by a multistep synthesis including a Diels-Alder reaction. Also disclosed are methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment an azepine which has high binding to the NMDA glycine site.Type: GrantFiled: October 17, 1995Date of Patent: January 13, 1998Assignees: State of Oregon, Acting by and through The Oregon State Board of Higher Education, Acting for and on behalf of The Oregon Health Sciences University and The University of Oregon, Eugene Oregon, ACEA Pharmaceuticals, Inc.Inventors: John F. W. Keana, Anthony P. Guzikowski, Daniel F. Nogales, Sui Xiong Cai
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Patent number: 5698553Abstract: A benzylpiperidine compound of formula I ##STR1## in which R.sup.1 is H, Hal or nitro,R.sup.2 is a benzyl group, which is unsubstituted or substituted by Hal on the aromatic portion, in the 2-, 3- or 4-position of the piperidine ring, with the proviso that R.sup.2 is not in the 4-position if X is --CO--, Y and Z are --CH.sub.2 and R.sup.1 is H,R.sup.3 is H or A,X is --O--, --S--, --NH--, --CO-- or --SO.sub.2 --,Y is --CH.sub.2 --, --NH--, --O--, --S--, --NH-- or alternatively --CO-- if X is --CO-- and Z is --NH-- or --NA--,Z is --CH.sub.2 --, --C(A).sub.2-, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CO--, --NH--, --NA--, --O--, --S-- or a bond,wherein X--Y or Y--Z is not --O--, --S--S--, --NH--O--, --O--NH--, --NH--NH--, --O--S-- or --S--O,A is alkyl having 1-6 C atoms,B is O or both H and OH, i.e.Type: GrantFiled: October 30, 1995Date of Patent: December 16, 1997Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Helmut Prucher, Rudolf Gottschlich, Joachim Leibrock, Harry Schwartz
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Patent number: 5696111Abstract: This invention is concerned with novel compounds represented by structural formula I and II. ##STR1## which are antiarrhythmic agents.Type: GrantFiled: May 16, 1996Date of Patent: December 9, 1997Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Nigel Liverton, Harold G. Selnick
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Patent number: 5679670Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.Type: GrantFiled: December 15, 1994Date of Patent: October 21, 1997Assignee: Alcon Laboratories, Inc.Inventors: Thomas Robert Dean, Hwang-Hsing Chen, Jesse Albert May
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Patent number: 5679671Abstract: The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity.This amino acid derivative is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or an acyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent;m and n represent each independently an integer of 0, 1 or 2 andJ represents a cyclic group having an angiotensin I-converting enzyme inhibition activity.Type: GrantFiled: January 25, 1995Date of Patent: October 21, 1997Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Shinji Suda, Naoki Yoneda, Makoto Kotake, Kenji Hayashi, Kazutoshi Miyake, Nobuyuki Mori, Mamoru Saito, Toshiyuki Matsuoka, Masayuki Namiki, Takeshi Sudo, Shigeru Souda
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Patent number: 5663166Abstract: A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.Type: GrantFiled: May 26, 1995Date of Patent: September 2, 1997Assignee: Genentech, Inc.Inventors: Brent Blackburn, Peter Barker, Thomas Gadek, Robert McDowell, Lawrence McGee, Todd Somers, Rob Webb, Kirk Robarge
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Patent number: 5656627Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. 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 interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: March 17, 1995Date of Patent: August 12, 1997Assignee: Vertex Pharmaceuticals, Inc.Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
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Patent number: 5650408Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors.Type: GrantFiled: June 7, 1995Date of Patent: July 22, 1997Inventors: Donald S. Karanewsky, Chong-Qing Sun
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Patent number: 5641880Abstract: The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme.Type: GrantFiled: October 24, 1995Date of Patent: June 24, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gary A. Flynn, Thomas D. Bannister
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Patent number: 5637698Abstract: Compounds of the formula ##STR1## are useful as intermediates in the preparation of compounds possessing ACE and NEP inhibition activity.Type: GrantFiled: February 26, 1996Date of Patent: June 10, 1997Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5635502Abstract: The present invention relates to certain novel mercaptoacetylamide bicyclic lactam derivatives useful as inhibitors of enkephalinase and of ACE.These mercaptoacetylamide bicyclic lactam derivatives can be described by the following formula: ##STR1## wherein R is hydrogen, a C.sub.1 -C.sub.4 alkyl, an Ar--Y--group, --CH.sub.2 O--C(O)C(CH.sub.3).sub.3 or diphenylmethyl;R.sub.1 is hydrogen, acetyl, --CH.sub.2 O--C(O)C(CH.sub.3).sub.3, benzoyl or a group of the formula ##STR2## R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, --CH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 or an Ar--Y--group;A is --CH.sub.2 --, --O--, or --S--;B is --S--or --O--; andpharmaceutically acceptable salts thereof.Type: GrantFiled: April 3, 1995Date of Patent: June 3, 1997Assignee: Merrell Pharmaceuticals Inc.Inventor: Gary A. Flynn
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Patent number: 5629309Abstract: The present invention relates to certain novel 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and of ACE.Type: GrantFiled: December 14, 1995Date of Patent: May 13, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight, Alan M. Warshawsky, Shujaath Mehdi, John F. French, John H. Kehne
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Patent number: 5621099Abstract: The present invention provides hymenialdisine or its derivatives having the formula (I): ##STR1## wherein X.sup.1 is a halogen atom or a hydrogen atom and a process for production of the same. Further, synthetic intermediates are included in the invention. Hymenialdisine and its derivatives have inhibitory effects against protein kinase C and can be expected to have applications as a drug for the treatment of conditions where it is believed the activation of protein kinase C is involved.Type: GrantFiled: January 18, 1996Date of Patent: April 15, 1997Assignee: Suntory LimitedInventors: Hirokazu Annoura, Toshio Tatsuoka
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Patent number: 5606054Abstract: There are disclosed certain novel compounds identified as heterocyclic-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 heterocyclic-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: December 14, 1993Date of Patent: February 25, 1997Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Helmut Mrozik, William R. Schoen, Thomas L. Shih, Matthew J. Wyvratt
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Patent number: 5604221Abstract: The present invention relates to certain novel indane-2-mercaptoacetylamide disulfide derivatives of the formula ##STR1## useful as inhibitors of enkephalinase.Type: GrantFiled: December 12, 1995Date of Patent: February 18, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight, Alan M. Warshawsky, Shujaath Mehdi, John H. Kehne
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Patent number: 5567814Abstract: The present invention relates to certain novel 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and of ACE.Type: GrantFiled: March 2, 1995Date of Patent: October 22, 1996Assignee: Merrell Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight, Alan M. Warshawsky, Shujaath Mehdi, John F. French, John H. Kehne
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Patent number: 5563157Abstract: The present invention is new 3-(heterocyclic)-propenoic acid derivatives and pharmaceutical compositions thereof. These new 3-(heterocyclic)-propenoic acid derivatives are useful as NMDA antagonist.Type: GrantFiled: October 31, 1994Date of Patent: October 8, 1996Assignee: Hoechst Marion Roussel Inc.Inventors: Boyd L. Harrison, Philip L. Nyce, Robert A. Farr
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Patent number: 5552400Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.Type: GrantFiled: June 8, 1994Date of Patent: September 3, 1996Assignee: Sterling Winthrop Inc.Inventors: Roland E. Dolle, Prasad V. Chaturvedula, Tina M. Ross, Stanley J. Schmidt
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Patent number: 5543298Abstract: The method for assaying the SOD (super oxide dismutase) activity in liquid medium is based on the activation of self-oxidization, by SOD activity, of a reactive agent having the general formula (I) wherein either n is 1 or 2, R.sup.1 is --OR.sup.4 or --NR.sup.5 R.sup.6 ; R.sup.2 is H, --OR.sup.4, alkyl (1-6C), --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --, to form a ring by binding to the phenyl substituent, at meta with respect to R.sup.1 ; and R.sup.3 is H, alkyl (1-6C) or --OR.sup.4 (if R.sup.2 is different from --OR.sup.4); with R.sup.4 being H or alkyl (1-6C); R.sup.5 being H, alkyl (1-6C), --CH.sub.2 COOH, --C.sub.6 H.sub.5 COOH or --C.sub.6 H.sub.5 SO.sub.3 H; and R.sup.6 is H, alkyl (1-6C) or --CH.sub.2 COOH; or n is 1, R.sup.1 is --OR.sup.4, R.sup.2 is --CH.sub.2 --O--, in order to form a ring by bonding of O with the phenyl substituent, at meta with respect to R.sup.1 ; and R.sup.3 is H or --OR.sup.4.Type: GrantFiled: June 6, 1994Date of Patent: August 6, 1996Assignee: Oxis International S.A.Inventors: Jinzhu Xu, Jean-Claude Y. Yadan, Marc E. Moutet, Jean R. Chaudiere
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Patent number: 5536716Abstract: There are disclosed certain novel compounds identified as spiro piperidines and homologs 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 treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: November 3, 1993Date of Patent: July 16, 1996Assignee: Merck & Co., Inc.Inventors: Meng-Hsin Chen, David B. R. Johnston, Ravi P. Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang
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Patent number: 5532240Abstract: A condensed thiophene compound represented by general formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein ring S represents a thiophene ring; R.sup.1 represents hydrogen, halogen, alkyl, etc.; R.sup.2 represents hydrogen, alkyl, acyl, etc.; G represents --CH.sub.2 --, --CH(OH)--, --CO--, etc.; Q represents alkylene; T represents --N(Rb)(Rc) (wherein Rb, Rc represents each alkyl etc.; or alternatively Rb and Rc are combined together to form cyclic amino); D represents --CH.sub.2 -- or --S--; A and B represent each carbonyl or thiocarbonyl, or are null; and m and n represent each 0, 1 to 4, provided that m+n represents an integer of 4 or less.This compound is useful as an antipsychotic drug having a reduced extrapyramidal side effect.Type: GrantFiled: July 8, 1994Date of Patent: July 2, 1996Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tohru Nakao, Yuji Ono, Masahiro Bougauchi, Yasuto Morimoto
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2-substituted indane-2-mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ace
Patent number: 5529996Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide derivatives which are useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: March 1, 1995Date of Patent: June 25, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Gary A. Flynn -
Patent number: 5527795Abstract: The present invention relates to certain novel mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and of ACE.Type: GrantFiled: April 5, 1995Date of Patent: June 18, 1996Assignee: Merrell Pharmaceuticals Inc.Inventors: Gary A. Flynn, Philippe Bey, Alan M. Warshawsky, Douglas W. Beight, Shujaath Mehdi, Eugene L. Giroux, Timothy P. Burkholder, Edward D. Daugs, John F. French
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Patent number: 5525723Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## are useful as ACE and NEP inhibitors and those wherein A is ##STR3## are useful as ACE inhibitors. Methods of preparation and intermediates are also disclosed.Type: GrantFiled: November 18, 1993Date of Patent: June 11, 1996Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5510480Abstract: The invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein n is 0, 1, or 2, X is ##STR2## Z is H.sub.2, oxygen or sulfur, and R.sub.1, R.sub.2, R.sub.3, R.sub.4, T, W, and Y are defined variables.These compounds are highly selective agonists or inverse agonists for the GABAa brain receptors and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepinc type drugs, and enhancement of alertness.Type: GrantFiled: July 11, 1994Date of Patent: April 23, 1996Assignee: Neurogen CorporationInventor: Pamela Albaugh
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Patent number: 5504088Abstract: The cyclic amide derivative is defined by the formula (I) or a salt thereof:R.sup.1 --(CH.sub.2).sub.n --Zin which R.sup.1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R.sup.2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R.sup.3 being hydrogen or a lower alkyl, R.sup.4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R.sup.2 and R.sup.4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.Type: GrantFiled: December 13, 1993Date of Patent: April 2, 1996Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Masahiro Yonaga, Norio Karibe, Youichi Iimura, Satoshi Nagato, Atsushi Sasaki, Yoshiharu Yamanishi, Hiroo Ogura, Takashi Kosasa, Kumi Uchikoshi, Kiyomi Yamatsu
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Patent number: 5498776Abstract: This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently H, lower alkyl containing 1 to 6 carbon atoms, or perfluoroalkyl containing 1 to 6 carbon atoms; R.sup.5 is H or, when n is 1, R.sup.5 taken together with R.sup.3 comprises a double bond, n is 0 or 1, p is 0 to 2, m is 0 to 3; Ar.sup.1 is ##STR2## wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; and Ar.sup.2 is ##STR3## wherein X is ##STR4## wherein R.sup.6 is H, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereof, which compounds are useful in the treatment of hypertension and congestive heart failure.Type: GrantFiled: August 8, 1994Date of Patent: March 12, 1996Assignee: American Home Products CorporationInventors: John W. Ellingboe, Madelene Nikaido, Jehan Bagli
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Patent number: 5491141Abstract: The present invention relates to novel 2-substitited indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.Type: GrantFiled: March 1, 1995Date of Patent: February 13, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Gary A. Flynn
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Patent number: 5491143Abstract: The present invention relates to certain novel mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and of ACE.Type: GrantFiled: April 5, 1995Date of Patent: February 13, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Philippe Bey, Alan M. Warshawsky, Douglas W. Beight, Shujaath Mehdi, Eugene L. Giroux, Timothy P. Burkholder, Edward D. Daugs, John F. French
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Patent number: 5491142Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.Type: GrantFiled: March 1, 1995Date of Patent: February 13, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Gary A. Flynn
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Patent number: 5488047Abstract: The present invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar-Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -C.sub.4 alkyl; or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;A is a bond, methylene or oxygen, sulfur or NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Y-- group;R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ;R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; andn is an integer 1 to 3,which are useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: June 2, 1995Date of Patent: January 30, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Gary A. Flynn
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Patent number: 5488048Abstract: The present invention relates to novel aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: March 1, 1995Date of Patent: January 30, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Robert J. Cregge, Thomas L. Fevig, Shyam Sunder, Patrick W. Shum
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2-substituted indane-2-mercaptoacetylamide derivatives useful as inhibitors or enkephalinase and ace
Patent number: 5486513Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide derivatives which are useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: March 1, 1995Date of Patent: January 23, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Gary A. Flynn