Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 540/490)
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Patent number: 6486315Abstract: Mercaptoalkanoylamino lactam acids are recrystallized by treatment with an agent that minimizes the formation of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite.Type: GrantFiled: November 16, 2001Date of Patent: November 26, 2002Assignee: Bristol-Myers Squibb Co.Inventors: David R. Kronenthal, Rajendra P. Deshpande, James Simpson
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Patent number: 6458827Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.Type: GrantFiled: July 20, 2001Date of Patent: October 1, 2002Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski
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Publication number: 20020137928Abstract: A pyrrolesulfonamide compound having the following 1Type: ApplicationFiled: August 28, 2001Publication date: September 26, 2002Applicant: SUNTORY LIMITEDInventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 6455522Abstract: The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic sulfonamide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.Type: GrantFiled: February 10, 1999Date of Patent: September 24, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jingwu Duan, Lihua Chen, Robert J. Cherney, Carl P. Decicco, Matthew E. Voss
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Patent number: 6423840Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; 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: January 31, 2001Date of Patent: July 23, 2002Assignee: 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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Publication number: 20020072514Abstract: The present invention relates to compounds of formula I, 1Type: ApplicationFiled: October 25, 2001Publication date: June 13, 2002Applicant: Hoechst AktiengesellschaftInventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
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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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Publication number: 20020055499Abstract: Compounds of the formula (I) are disclosed which are dual fibrinogen receptor and vitronectin receptor antagonists and are useful in the treatment of atherosclerosis, in the prevention of restenosis and in the prevention of tumor metastasis and tumor growth: 1Type: ApplicationFiled: December 12, 2001Publication date: May 9, 2002Inventors: Dirk Heerding, James Martin Samanen
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Publication number: 20020049194Abstract: A benzoheterocyclic derivative of the following formula [1]: 1Type: ApplicationFiled: June 6, 2001Publication date: April 25, 2002Inventors: Hidenori Ogawa, Kazumi Kondo, Hiroshi Yamashita, Keizo Kan, Takayuki Matsuzaki, Tomoichi Shinohara, Yoshihisa Tanada, Muneaki Kurimura, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 6353099Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: August 17, 2000Date of Patent: March 5, 2002Assignee: Merck & Co., Inc.Inventors: Stephen E. DeLaszlo, William K. Hagmann, Theodore M. Kamenecka
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Patent number: 6352982Abstract: The present invention provides a compound of the formula: wherein ring A is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; ring B is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; Z is an optionally substituted cyclic group or linear hydrocarbon group; R1 is a hydrogen atom, an optionally substituted hydrocarbon group or heterocyclic ring; R2 is an optionally substituted amino group; D is a bond or an optionally substituted divalent hydrocarbon group; E is a bond, —CON(Ra)—, —N(Ra)CO—, —N(Rb)CON(Rc)—, —N(Rd)COO—, —N(Re)SO2—, —COO—, —N(Rf)—, —O—, —S— —SO—, —SO2—, (in which Ra, Rb, Rc, Rd, Re and Rf are respectively a hydrogen atom or an optionally substituted hydrocarbon group); G is a bond or an optionally divalent substituted hydrocarbon group; L is a divalent group; ringType: GrantFiled: October 14, 1999Date of Patent: March 5, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroshi Mabuchi, Nobuhiro Suzuki, Takashi Miki
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Publication number: 20020019386Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:Type: ApplicationFiled: August 27, 2001Publication date: February 14, 2002Applicant: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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Patent number: 6340752Abstract: Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite. Such agents are also employed in the recrystallization and reprocessing of the mercaptoalkanoylamino lactam acids.Type: GrantFiled: December 9, 1998Date of Patent: January 22, 2002Assignee: Bristol-Myers Squibb Co.Inventors: David R. Kronenthal, Theodor Denzel, Bang-Chi Chen, James H. Simpson, Rajendra P. Deshpande
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Publication number: 20010039272Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R1 represents hydrogen atom or a C1-6 alkyl group; R2 and R3 independently represent a hydrogen atom or a C1-6 alkyl group, or R2 and R3 may combine together to represent a 5- or 6-membered cycloalkyl group; R4 represents, for example, a hydrogen atom or a C1-6 alkyl group; R5 represents, for example, a hydrogen atom or a C1-6 alkyl group; R6 represents a hydrogen atom or a C-1-6 alkyl group; X represents —NR7—, —O—, —CHR7— or —S— in which R7 represents, for example, a hydrogen atom or a C1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.Type: ApplicationFiled: April 20, 2001Publication date: November 8, 2001Inventor: Koichi Shudo
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Patent number: 6248882Abstract: The glycinamide of the formula is reacted with the dioxolane of the formula wherein L is a leaving group such as iodo, bromo, alkylsulfonyloxy, or arylsulfonyloxy to give the dioxolane of the formula Treating the dioxolane of formula III under aqueous refluxing conditions followed by exchanging the dioxolane acetal with a dimethoxy acetal and introduction of the methyl ester gives (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester which is an intermediate in the preparation of the dual inhibitor [4S-[4&agr;(R*),7&agr;, 10a&bgr;]]-)octahydro-4-[(2-mercapto-1-oxo-3-phenylpropy)-amino]-5-oxo-7H-pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid. Also disclosed are storage stable salts of (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester.Type: GrantFiled: October 12, 2000Date of Patent: June 19, 2001Assignee: Bristol-Myers Squibb Co.Inventors: Jollie D. Godfrey, Jr., David R. Kronenthal, Mark D. Schwinden, Sushil K. Srivastava, Keith Ramig, John J. Venit, Paul A. Jass, Saibaba Racha, John L. Dillon, Jr., Nachimuthu Soundararajan, Gerald L. Powers, Atul S. Kotnis
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Patent number: 6207663Abstract: Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: October 5, 1999Date of Patent: March 27, 2001Assignees: Hoechst Atkiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel LeFrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 6204261Abstract: The present invention relates to pyradazino[1,2-a][1,2]diazepine-1-carboxamide compounds of formula: which compounds are inhibitors of interleukin-1beta converting enzyme.Type: GrantFiled: December 6, 1996Date of Patent: March 20, 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: 6162913Abstract: N-protected-L-homocysteine disulfide of the formula ##STR1## or an activated form thereof is reacted with (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester to give the disulfide intermediate of the formula ##STR2## Cleavage of the disulfide bond followed by acid catalyzed cyclization produces the N-protected lactam of formula III which is useful for preparing the pharmaceutically active compound omapatrilat.Type: GrantFiled: July 8, 1999Date of Patent: December 19, 2000Assignee: Bristol-Myers Squibb Co.Inventors: Jerome L. Moniot, Sushil K. Srivastava, William J. Winter, John J. Venit, Shankar Swaminathan, Keith Ramig, Paul A. Jass, Mark D. Schwinden, John L. Dillon, Jr., Saibaba Racha, James Simpson, Chien-Kuang Chen, Shawn K. Pack
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Patent number: 6147071Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.CC<, --CO--N< or --CS--N< as the partial structure --X . . . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.Type: GrantFiled: June 1, 1998Date of Patent: November 14, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura
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Patent number: 6140320Abstract: The present invention relates to benzoxazepinones of formula I: ##STR1## or stereoisomeric forms or 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: September 1, 1998Date of Patent: October 31, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Anthony J. Cocuzza, James D. Rodgers
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Patent number: 6114522Abstract: A process for producing 4-substituted-3-halogeno-1,4-benzoxazepin derivative or the salt thereof comprising: deprotonizing a benzoxazepine derivative having the formula (II): ##STR1## with a base; and then, reacting the deprotonized product with a phosphate halide to produce an intermediate having the formula (IV): ##STR2## and then, reacting the resultant intermediate (IV) with a reagent selected from (i) a complex of a phosphine with chlorine or bromine, (ii) a phosphine and a chlorine gas or liquid bromine, (iii) a phosphine and tetrachloromethane or tetrabromomethane, or (iv) a halogenated phosphite ester to produce a 4-substituted-3-halogeno-1,4-benzoxazepine derivative having the formula (I) ##STR3## wherein X indicates a chlorine atom or a bromine atom, or its salt.Type: GrantFiled: November 24, 1999Date of Patent: September 5, 2000Assignee: Suntory LimitedInventors: Kastuhide Kamei, Noriko Maeda, Toshio Tatsuoka
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Patent number: 6110909Abstract: This invention provides new benzoxazepine compounds represented by the formula: ##STR1## [wherein R stands for a lower alkyl group optionally substituted with a hydroxyl group, X stands for an optionally substituted carbamoyl group or an optionally substituted heterocyclic group having a deprotonatable hydrogen atom, R.sub.1 stands for a lower alkyl group and W stands for a halogen atom] having activities of lowering chlesterol-level and lowering trigluceride-level, and being useful for prophylaxis and therapy of hyperlipidemia.Type: GrantFiled: March 12, 1998Date of Patent: August 29, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hidefumi Yukimasa, Yasuo Sugiyama, Ryuichi Tozawa
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Patent number: 6096884Abstract: A method of production of 2,4'-dipyridyl derivatives by a cross coupling reaction of a 2-halopyridine derivative and a 4-halopyridine using a nickel complex catalyst and a method of separation of a 2,4'-dipyridyl derivative from a mixture of dipyridyl isomers containing a 2,2'-dipyridyl derivative, 2,4'-dipyridyl derivative, and 4,4'-dipyridyl by using a dilute aqueous copper sulfate solution to insolubilize and remove the 2,2'-dipyridyl derivative and 4,4'-dipyridyl are disclosed.Type: GrantFiled: January 21, 1999Date of Patent: August 1, 2000Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Katsuhide Kamei
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Patent number: 6069114Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).Type: GrantFiled: February 25, 1997Date of Patent: May 30, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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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: 5965553Abstract: This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, Alzheimer's agents or anti-acne agents.Type: GrantFiled: June 12, 1997Date of Patent: October 12, 1999Assignee: Pfizer Inc.Inventors: Andrew S. Bell, Ernest S. Hamanaka, Cheryl M. Hayward, Douglas A. Scully, Blanda Stammen
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Patent number: 5770594Abstract: This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents and antiatheroscierosis agents.Type: GrantFiled: June 17, 1997Date of Patent: June 23, 1998Assignee: Pfizer Inc.Inventors: Ernest S. Hamanaka, Cheryl M. Hayward, Joel M. Hawkins
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Patent number: 5726306Abstract: N-containing, condensed heterocyclic compounds and salts thereof are disclosed which are useful for inhibiting squalene synthetase and fungal growth, and which are useful for treating or preventing hyperlipidemia. Also disclosed is a method for producing these compounds.Type: GrantFiled: November 9, 1994Date of Patent: March 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Hidefumi Yukimasa, Ryuichi Tozawa, Masakuni Kori, Kazuaki Kitano, Yasuo Sugiyama
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Patent number: 5698691Abstract: Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula ##STR1## wherein R.sub.1 is hydrogen or an optionally substituted hydrocarbon group; R.sub.2 is hydrogen, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic ring group; X' is a substituent comprising an optionally esterified carboxyl group, an optionally substituted carbamoyl group, an optionally substituted hydroxyl group, an optionally substituted amino group or an optionally substituted heterocyclic radical having a protonizable hydrogen; Ring A is an optionally substituted benzene ring or an optionally substituted aromatic heterocyclic ring; Ring J' is a 7- to 8-membered heterocyclic ring containing at most three ring constituting hetero atoms; D is C or N; the Ring J' optionally having, besides R.sub.1, R.sub.Type: GrantFiled: September 26, 1994Date of Patent: December 16, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Hidefumi Yukimasa, Ryuichi Tozawa, Yasuo Sugiyama, Masakuni Kori
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Patent number: 5677298Abstract: Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula (I) ##STR1## wherein R.sub.1 stands for H or an optionally substituted hydrocarbon group; R.sub.2 and R.sub.3 independently stand for H, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic group; Z stands for a carbon chain containing a double bond or --Z'--C(OH)-- (Z' stands for a bond or a straight-chain or branched alkylene chain); the symbol .........Type: GrantFiled: August 13, 1996Date of Patent: October 14, 1997Assignee: Takeda Chemical IndustriesInventors: Hidefumi Yukimasa, Masakuni Kori, Ryuichi Tozawa, Yasuo Sugiyama
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Patent number: 5674863Abstract: 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: October 7, 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: 5674865Abstract: 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: October 7, 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: 5672599Abstract: Compounds of the formula ##STR1## wherein X is O or S--(O).sub.t ; n is one; m is zero or one; Y is CH.sub.2, O, or S--(O).sub.t provided that Y is O or S--(O).sub.t only when m is one; and A is ##STR2## are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors. Also disclosed are methods of preparation and intermediates.Type: GrantFiled: November 22, 1995Date of Patent: September 30, 1997Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5654294Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.Type: GrantFiled: June 19, 1996Date of Patent: August 5, 1997Assignee: Bristol-Myers SquibbInventor: Jeffrey A. Robl
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Patent number: 5646276Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents.Type: GrantFiled: June 19, 1996Date of Patent: July 8, 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: 5627278Abstract: A process for preparing compounds of the formula ##STR1## wherein X is O or S; n is one or two; m is zero or one; Y is CH.sub.2, O, or S provided that Y is O or S only when m is one; and A is ##STR2## is disclosed. Also disclosed are processes for preparing the corresponding amino intermediates.Type: GrantFiled: January 4, 1996Date of Patent: May 6, 1997Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5545735Abstract: 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 4, 1993Date of Patent: August 13, 1996Assignee: Merck & Co., Inc.Inventors: Richard J. Bochis, Paul J. Hodges, William R. Schoen, Matthew J. Wyvratt, Jr.
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Patent number: 5508272Abstract: Compounds of the formula ##STR1## wherein X is O or S--(O).sub.t ; n is one or two; m is zero or one; Y is CH.sub.2, O, or S--(O).sub.t provided that Y is O or S--(O).sub.t only when m is one; and A is ##STR2## are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors. Also disclosed are methods of preparation and intermediates.Type: GrantFiled: May 5, 1994Date of Patent: April 16, 1996Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
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Patent number: 5496943Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.Type: GrantFiled: March 13, 1992Date of Patent: March 5, 1996Assignee: Nippon Paint Co., Ltd.Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
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Patent number: 5416066Abstract: An object of the invention is to provide compounds having a myocardial KD (Kinetic cell death)-inhibiting effect without being accompanied by a cardiodepressant effect.A 1,4-benzothiazepine derivative represented by the following Formula [I]: ##STR1## wherein each of substituent groups is defined as follows: R represents H or a C.sub.1 -C.sub.3 lower alkoxy group; X represents O or H.sub.2 ; n represents 1 or 2; R.sup.1 represents H, a substituted phenyl group wherein the substituent group is OH or a C.sub.1 -C.sub.3 lower alkoxy group, ##STR2## a C.sub.1 -C.sub.3 lower alkoxy group, ##STR3## wherein R.sup.2 represents a C.sub.1 -C.sub.3 acyl group, and ph represents a phenyl group, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 25, 1993Date of Patent: May 16, 1995Assignee: Kirin Brewery Co., Ltd.Inventors: Noboru Kaneko, Tatsushi Oosawa, Teruyuki Sakai, Hideo Oota
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Patent number: 5317017Abstract: There are disclosed certain compounds identified as N-biphenyl-3-amido substituted benzolactams 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 benzolactams as the active ingredient thereof are also disclosed.Type: GrantFiled: September 30, 1992Date of Patent: May 31, 1994Assignee: Merck & Co., Inc.Inventors: Hyun O. Ok, William R. Schoen, Matthew Wyvratt
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Patent number: 5312625Abstract: A therapeutically effective antipsychotic preparation comprising a fused cyclic compound for the treatment of diseases involving the serotonergic pathway having the formula (I) or salts thereof: ##STR1## wherein both of A and B are carbonyl groups, or one represents a methylene group and the other a carbonyl group, Z represents a sulfur atom, or a nitrogen atom which may be substituted, or a methylene group, R represents an aromatic or heterocylcic group, which may be substituted, X represents a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.5 lower alkyl group, a C.sub.1 -C.sub.5 lower alkoxy group, a C.sub.7 -C.sub.9 arylalkoxy group, a C.sub.1 -C.sub.5 lower acyloxy group, a C.sub.7 -C.sub.10 arylcarbonyloxy group, a hydroxy group, a nitro group or an ester group, and n is an integer of 2 to 10.Type: GrantFiled: May 11, 1993Date of Patent: May 17, 1994Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Kayoko Nomura
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Patent number: 5276025Abstract: Compounds of general formula: ##STR1## are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and related disorders such as glaucoma.Type: GrantFiled: September 9, 1992Date of Patent: January 4, 1994Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Jacob M. Hoffman, Jr., James H. Jones, Clarence S. Rooney, Anthony M. Smith
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Patent number: 5250680Abstract: An amino-acid ester compound can be cyclized into a cyclic amido-carbonyl compound by contacting the amino-acid ester compound in a liquid medium with a heterogeneous acidic ion-exchange substance. For example, 2-hydroxy-3-(2-aminophenylthio)-3-(4-methoxyphenyl)propionic acid, methyl ester, threo form, can be cyclized in an aqueous mixture into cis-2-(4-methoxyphenyl)-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one by employing a sulfonated polystyrene-divinylbenzene ion-exchange resin in its acid form, e.g., Dowex.RTM. 50X4-400. at yields exceeding 85 percent of theory, and the product can be used to make diltiazem hydrochloride.Type: GrantFiled: September 2, 1992Date of Patent: October 5, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Daniel E. Martin
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Patent number: 5250679Abstract: 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: April 10, 1992Date of Patent: October 5, 1993Assignee: Genentech, Inc.Inventors: Brent Blackburn, Robert McDowell, Thomas Gadek, Peter Barker, Lawrence McGee, Rob Webb
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Patent number: 5158947Abstract: A condensed heterocyclic compound having the formula (I): ##STR1## wherein A and B are both carbonyl groups of one thereof represents a methylene group and the other represents a carbonyl group; Z represents an oxygen atom, a sulfur atom, a substituted or unsubstituted nitrogen atom, or a methylene group; n is an integer of 2 to 6; and R represents a group having the following formula: ##STR2## wherein R.sup.1 represents a hydrogen atom or a hydroxyl group; R.sup.2 represents a substituted or unsubstituted phenyl or 2-pyridyl group or salts thereof.The compounds according to the present invention exhibit a strong affinity to the .sigma.-receptor and are useful as psychopharmaceuticals.Type: GrantFiled: June 18, 1991Date of Patent: October 27, 1992Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Kayoko Nomura, Makoto Shibata, Masanori Kawai
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Patent number: 5149823Abstract: A novel class of sulfonamoyl-substituted 1,6-diaza[4.4]spirodilactams, having a sulfonamoyl substituent on the hydrocarbyl group attached to each spiro ring nitrogen atom, is useful for the preparation of polymers, including polyamides and as latent curing agents for epoxy resins.Type: GrantFiled: August 9, 1990Date of Patent: September 22, 1992Assignee: Shell Oil CompanyInventor: Pen-Chung Wang
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Patent number: 5141930Abstract: A fused thiophene compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof. In the above formula, one of E.sup.1, E.sup.2 and E.sup.3 is sulfur atom and other two of them are C--R.sup.1 and C--R.sup.2 respectively. R.sup.1 and R.sup.2 are the same or different and each is hydrogen, halogen, nitro, amino, cyano, hydroxyl, formyl, alkyl, alkoxy, haloalkyl, arylalkyl, acyl, alkoxyalkyl, acyloxyalkyl, hydroxyalkyl, acyloxyalkanoyl, alkoxyalkanoyl, hydroxyalkanoyl, aryloxyalkanoyl, haloalkanoyl, alkylthio, alkylsulfinyl, alkylsulfonyl, arylthio, arylsulfinyl, arylsulfonyl, hydroxysulfonyl, halosulfonyl, sulfamoyl, substituted sulfamoyl, carboxyl, acylamino, alkoxycharbonyl, carbamoyl, substituted carbamoyl or substituted amino. D is --CH.sub.2 -- or --S(O).sub.m -- (m is 0, 1 or 2). Q is straight or branched chain alkylene. T is primary amino, secondary amino or tertiary amino.Type: GrantFiled: July 8, 1991Date of Patent: August 25, 1992Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tohru Nakao, Hiroshi Tanaka, Hirotake Yamato, Takeshi Akagi, Shuzo Takehara
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Patent number: 5075302Abstract: Mercaptoacyl aminolactam inhibitors of endopeptidases of the formula ##STR1## wherein Y is -(CHR.sup.5).sub.n (CR.sup.3 R.sup.4)- or -(CR.sup.3 R.sup.4).sub.p X(CR.sup.3 R.sup.4).sub.q -,wherein two substituents selected from the group consisting of R.sup.3, R.sup.4 and R.sup.5, can form a benzene, cyclopentane or cyclohexane ring;X is -O-, -S-, -SO- or -SO.sub.2 -;Q is hydrogen or R.sup.6 CO-;m is 1 or 2;n is 1, 2, 3 or 4;p is 1 or 2;q is 2 or 3;R.sup.1 is lower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen, lower alkyl, hydroxylower alkyl, lower alkoxylower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, lower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.5 is hydrogen, lower alkyl, aryllower alkyl, heteroaryllower alkyl, hydroxy, lower alkoxy, mercapto, or lower alkylthio; and R.sup.Type: GrantFiled: March 9, 1990Date of Patent: December 24, 1991Assignee: Schering CorporationInventor: Bernard R. Neustadt