The Diazine Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/115)
-
Patent number: 5710138Abstract: Compounds of formula I ##STR1## are described, in which substituents R.sup.1 -R.sup.4 have the meanings mentioned in the application as well as their production and use in pharmaceutical agents.Type: GrantFiled: January 22, 1996Date of Patent: January 20, 1998Assignee: Schering AktiengesellschaftInventors: Peter Holscher, Lechoslaw Turski
-
Patent number: 5698560Abstract: The present invention relates to imidazoquinazoline derivatives represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, lower alkenyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted heteroaryl, R.sup.2 and R.sup.3 represent independently hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted heteroaryl, or R.sup.2 and R.sup.3 are combined to represent a heterocyclic group containing a nitrogen atom, R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl, X represents O or S, Y represents a single bond or O, n represents 0, 1, 2, or 3, and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 23, 1996Date of Patent: December 16, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yasuo Onoda, Shin-ichi Sasaki, Daisuke Machii, Haruki Takai, Tetsuji Ohno, Koji Yamada, Michio Ichimura, Hiroshi Kase
-
Patent number: 5696260Abstract: Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable non-toxic salts thereof wherein: R.sub.9 and Y are substituents as defined herein; andR.sub.a and R.sub.b independently represent halogen, hydroxy, amino, mono or dialkylamino where each alkyl is straight or branched chain alkyl having 1-6 carbon atoms, straight or branched chain lower alkyl having 1-6 chain atoms, or straight or branched chain lower alkoxy having 1-6 carbon atoms, where R.sub.a and R.sub.b each appear at most only once on the phenyl ringwhich compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.Type: GrantFiled: June 20, 1995Date of Patent: December 9, 1997Assignee: Neurogen CorporationInventors: Kenneth Shaw, Alan Hutchison
-
Patent number: 5688803Abstract: Compounds of general formula (Ia), (Ib) and (II), wherein R.sup.1 and R.sup.2 each independently signify hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R.sup.3 R.sup.4 NS(O).sub.2 -- and R.sup.3 and R.sup.4 signify lower alkyl, and R.sup.2 can additionally signify morpholino or thiomorpholino, a 5- or 6-membered heterocycle with 1-3N atoms optionally substituted by lower alkyl, hydroxy, amino or the group --CH.sub.2 NHCH.sub.3, a bicyclic heterocycle with 1-3N atoms or a group --NR.sup.5 R.sup.6 or --OR.sup.5 in which R.sup.5 and R.sup.6 can be the same or different and signify hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl, and X in formula (II) signifies --CH.dbd.CH--, --CH.dbd.N--, --NH--, --CO-- or --O--, as well as pharmaceutically usable salts of compounds of general formula (Ia), (Ib) and (II).Type: GrantFiled: November 15, 1996Date of Patent: November 18, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buttelmann, Thierry Godel, Laurence Gross, Marie-Paule Heitz Neidhart, Claus Riemer, Rene Wyler
-
Patent number: 5668282Abstract: The invention discloses imidazo[1,5-a]quinoxalines (I) ##STR1## which do not contain an endocyclic carbonyl group that are useful as anxiolytic and sedative/hypnotic agents.Type: GrantFiled: June 6, 1995Date of Patent: September 16, 1997Assignee: Pharmacia & Upjohn CompanyInventor: Ruth E. TenBrink
-
Patent number: 5661147Abstract: The present invention relates to imidazoquinazoline derivatives represented by the general formula (I): ##STR1## or pharmacologically acceptable salts thereof. The compounds of the present invention have strong and selective cGMP-specific PDE inhibitory activity and are useful for treating or ameliorating cardiovascular diseases such as thrombosis, angina pectoris, hypertension, arterial sclerosis and the like, as well as asthma and the like.Type: GrantFiled: April 26, 1995Date of Patent: August 26, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Daisuke Machii, Kenji Matsuno, Iwao Kinoshita, Yuji Nomoto, Haruki Takai, Tetsuji Ohno, Ken Nagashima, Tomoko Ishikawa, Koji Yamada, Michio Ichimura, Hiroshi Kase
-
Patent number: 5650410Abstract: This invention provides an anti-inflammatory agent, particularly an agent for treating arthritis, containing a quinoline or quinazoline derivative or a salt thereof ##STR1## wherein Y is a nitrogen atom or C--G in which G is an optionally esterified carboxyl group;R.sup.1 and R.sup.2 are each independently a hydrogen atom, optionally substituted hydrocarbon group or optionally substituted heterocyclic group, or R.sup.1 and R.sup.2 are linked together to form a saturated ring;each of the ring A and ring B may optionally be substituted;n is an integer of 1 to 4; andk is 0 or 1.This invention also provides a novel quinoline or quinazoline derivative having anti-inflammatory activity.Type: GrantFiled: April 17, 1995Date of Patent: July 22, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Haruhiko Makino, Atsuo Baba
-
Patent number: 5646146Abstract: The present invention relates to 9H-indeno[1,2-b]pyrazin-3(4H)-ones and 9H-indeno[1,2-b]pyrazine-2,3(1H,4H)-diones or tautomeric forms thereof which are useful in treating neurological and psychiatric diseases based on the antagonism of the glycine binding site on the NMDA receptor complex.Type: GrantFiled: May 25, 1995Date of Patent: July 8, 1997Assignee: Novo Nordisk A/SInventors: Peter Faarup, Palle Jakobsen, Anker Steen J.o slashed.rgensen, Henrik Klitgaard
-
Patent number: 5633248Abstract: A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.Type: GrantFiled: November 21, 1995Date of Patent: May 27, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
-
Patent number: 5625063Abstract: The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## and W, X, A, B, C, D, E, R.sub.3, R.sub.4 are variables. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, over-dose with benzodiaziepine drugs, and enhancement of memory.Type: GrantFiled: March 14, 1996Date of Patent: April 29, 1997Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Alan Hutchison, Pamela Albaugh
-
Patent number: 5616582Abstract: The invention concerns quinazoline derivatives of the formula I ##STR1## wherein m is 1, 2 or 3 and each R.sup.1 includes hydroxy, amino, carboxy, carbamoyl, ureido, (1-4C)alkoxycarbonyl, N-(1-4C)alkylcarbamoyl, N,N-di-[(1-4C)alkyl]carbamoyl, hydroxyamino, (1-4C)alkoxyamino, (2-4C)alkanoyloxyamino, trifluoromethoxy, (1-4C)alkyl, (1-4C)alkoxy and (1-3C)alkylenedioxy;n is 1 or 2 and each R.sup.2 includes hydrogen, hydroxy, halogeno, trifluoromethyl, amino, nitro, cyano and (1-4C)alkyl; or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them; and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of cancer.Type: GrantFiled: June 15, 1995Date of Patent: April 1, 1997Assignee: Zeneca LimitedInventor: Andrew J. Barker
-
Patent number: 5614530Abstract: Substituted N-arylmethyl and heterocyclylmethyl-1H-pyrazolo[3,4-b]quinolin-4-amines, pharmaceutical compositions containing them and methods for a) effecting c-GMP-phosphodiesterase inhibition, b) treating heart failure and/or hypertension, c) reversing or reducing nitrate-induced tolerance and d) treating angina pectoris, congestive heart disease and myocardial infarction utilizing them.Type: GrantFiled: March 10, 1995Date of Patent: March 25, 1997Assignee: Sterling Winthrop Inc.Inventors: Virendra Kumar, John A. Dority, Jr.
-
Patent number: 5614516Abstract: The invention relates to new 12-amino-pyridazino-[4',5':3,4]-pyrrolo[2,1-a]isoquinolines of general formula (I) ##STR1## wherein --NR.sub.1 R.sub.2 represents an amino or substituted amino group, and acid addition salts thereof. The new active substances have potential use in pharmaceutical compositions for treating cardiac insufficiency and cerebral metabolic disorders.Type: GrantFiled: February 7, 1995Date of Patent: March 25, 1997Assignee: Boehringer Ingelheim GmbHInventors: Walter L osel, Otto Roos, Gerd Schorrenberg, Helmut Ensinger, Richard Reichl
-
Patent number: 5602252Abstract: This invention relates to novel tricyclic pteridinones, their aza analogs and their pharmaceutically acceptable salts. Further encompassed by the invention is a novel process for the production of the tricyclic pteridinones and their aza analogs. The compounds of the invention exhibit cardiovascular properties, particularly mixed vasodilation and selective venous and arterial dilation. Pharmaceutical compositions are proposed for the compounds.Type: GrantFiled: February 8, 1994Date of Patent: February 11, 1997Assignee: Berlex Laboratories, Inc.Inventor: David D. Davey
-
Patent number: 5599812Abstract: The present invention relates to a compound selected from these of formula (I): ##STR1## in which A and R.sub.1 are as defined in the description, and medicinal product containing the same which is useful for treating a disorder linked to the 5-HT.sub.3 receptors.Type: GrantFiled: April 29, 1994Date of Patent: February 4, 1997Assignee: Adir Et CompagnieInventors: Sylvain Rault, Jean-Charles Lancelot, Herv e Prunier, Max Robba, Philippe Delagrange, Pierre Renard, G erard Adam
-
Patent number: 5574038Abstract: The invention discloses imidazo[1,5-a]quinoxalines (I) ##STR1## which do not contain an endocyclic carbonyl group that are useful as anxiolytic and sedative/hypnotic agents.Type: GrantFiled: June 6, 1995Date of Patent: November 12, 1996Assignee: The Upjohn CompanyInventor: E. Jon Jacobsen
-
Patent number: 5541324Abstract: An invention relating to Imidazo[1,5-a]quinoxalines (I) ##STR1## which do not contain an endocyclic carbonyl group and which are useful as anxiolytic and sedative/hypnotic agents.Type: GrantFiled: December 13, 1993Date of Patent: July 30, 1996Assignee: The Upjohn CompanyInventors: Ruth E. TenBrink, E. Jon Jacobsen, Ronald B. Gammill
-
Patent number: 5532236Abstract: The present invention relates to [1,2,4]triazolo[4,3-a quinoxaline derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.2 is a 5- or 6-membered nitrogen-containing heterocyclic ring which is optionally substituted with one, two or three substituents, wherein each substituent is independently phenyl or C.sub.1-6 -alkyl, or one of R.sup.1 and R.sup.2 is a fused ring system comprising a 5- or 6-membered nitrogen-containing heterocyclic ring and a benzene, pyridine, pyrimidine or pyrazine ring, wherein the fused ring system is optionally substituted with phenyl or C.sub.1-6 -alkyl; and the other of R.sup.1 and R.sup.2 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, halogen, NO.sub.2, NH.sub.2, CN, CF.sub.3, COC.sub.1-6 -alkyl or SO.sub.2 NR'R", wherein R' and R" are independently hydrogen or C.sub.1-6 -alkyl; and X is O or S; and pharmaceutically acceptable salts thereof.Type: GrantFiled: May 3, 1994Date of Patent: July 2, 1996Assignee: Novo Nordisk A/SInventors: Poul Jacobsen, Flemming E. Nielsen, Lone Jeppesen
-
Patent number: 5492909Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 are a hydrogen atom, a lower alkyl group or a 5- to 7-membered cyclic group formed together with the adjacent --C.dbd.C--; X is an oxygen atom, a sulfur atom or a methylene group; Y is an optionally substituted methylene group, a divalent 3- to 7-membered homo- or heterocyclic group; R.sup.6 and R.sup.7 are a hydrogen atom, a lower alkyl group, a cycloalkyl group, an aryl group, or a nitrogen-containing heterocyclic group formed together With the adjacent nitrogen atom; m is an integer of 0 to 4; and n is an integer of 0 to 4, or a salt thereof. Said compound has an excellent anti-PAF activity, antiallergic action, etc., thus is useful as an antiasthmatic agent.Type: GrantFiled: April 12, 1994Date of Patent: February 20, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Masahiro Kajino, Yasuko Ashida
-
Patent number: 5486516Abstract: Pesticidal compounds of the formula (1) ##STR1## R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, or phenyl optionally substituted with halo, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, halo (C.sub.1 -C.sub.4) alkyl, or halo (C.sub.1 -C.sub.4) alkoxy;R.sup.2 is H, (C.sub.1 -C.sub.4) alkyl, nitro, halo; orR.sup.1 and R.sup.2 combine to form --(CH.sub.2).sub.4 --;R.sup.3 is H, (C.sub.1 -C.sub.4) alkyl, halo (C.sub.1 -C.sub.4) alkyl, phenyl, or substituted phenyl;X is O, S, NR.sup.4, or CR.sup.5 R.sup.6 ; andY is a bond or an alkylene chain one to six carbon atoms long; andZ is(a) (C.sub.3 -C.sub.8) cycloalkyl or cycloalkenyl, optionally substituted with (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, halo (C.sub.1 -C.sub.4) alkyl, halo (C.sub.1 -C.sub.4) alkoxy, halo, hydroxy or (C.sub.1 -C.sub.Type: GrantFiled: December 10, 1993Date of Patent: January 23, 1996Assignee: DowElancoInventors: Ronnie G. Edie, Ronald E. Hackler, Eriks V. Krumkalns
-
Patent number: 5482939Abstract: Novel compound represented by the formula: ##STR1## wherein R.sup.1 stands for H, an optionally substituted lower alkyl group or a halogen; R.sup.2 and R.sup.3 respectively stands for a hydrogen or an optionally substituted lower alkyl group, or R.sup.2 and R.sup.3 may, taken together with the adjacent --C.dbd.C-- group, form a 5- to 7-membered ring; X stands for O, SO or SO.sub.2 ; Y stands for a group of the formula: ##STR2## (R.sup.4 and R.sup.5 respectively stand for H or an optionally substituted lower alkyl group) or a divalent group derived from an optionally substituted 3- to 7-membered homocyclic or heterocyclic ring; R.sup.6 and R.sup.7 each stands for H, an optionally substituted lower alkyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R.sup.6 and R.sup.Type: GrantFiled: September 16, 1994Date of Patent: January 9, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Yasuhiko Kawano, Yasuko Ashida
-
Patent number: 5478825Abstract: The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR.sup.3, whereinp is 0, 1, or 2, andR.sup.3 is alkyl, alkenyl, or phenyl-, which may have halogen or nitro substituents, or phenyl optionally substituted;or NR.sup.4 R.sup.5 whereinR.sup.4 and R.sup.5 are hydrogen, alkyl, alkenyl, phenyl-alkyl, or di-alkyl-amino-alkyl;R.sup.1 and R.sup.2 are hydrogen or alkyl, ortogether form a group (CH.sub.2)n--Y--(CH.sub.2)m, wherein Y is CH.sub.2, or NR.sup.6, wherein R.sup.6 is phenyl-alkyl,n and m are 0 or 1 to 5;Z is NR.sup.7 R.sup.8, whereinR.sup.7 and R.sup.8 each are hydrogen, alkenyl, cycloalkyl, adamantayl, or phenyl-alkyl, which may have one or more substituents ortogether form a group of (CH.sub.2)j--W--(CH.sub.2)k, wherein j and k each are 1 to 3, and W is oxygen, CH.sub.2, CHOH, or NR.sup.10 , wherein R.sup.10 is hydrogen, alkoxycarbonyl, or alkyl, which latter may be substituted.or SR.sup.9, whereinR.sup.Type: GrantFiled: June 15, 1994Date of Patent: December 26, 1995Assignee: Egis GyogyszergyarInventors: Jozsef Reiter, Gabor Berecz, Gizella Zsila, Lujza Pet cz, Gabor Gigler, Marton Fekete, Maria Szecsey nee Heged s, Enik Szirt nee Kiszelly, Ludmila Rohacs nee Zamkovaja, Frigyes Gorgenyi, Margit Csorg
-
Patent number: 5463054Abstract: The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## and X represents hydrogen, halogen, or hydroxy;W represents an aryl group unsubstituted or substituted with various organic and inorganic substituents;A, B, C, D, and E represent carbon or nitrogen substituted with hydogen or varous organic and inorganic substituents; andR.sub.3, and R.sub.4 are variables representing various organic and inorganic substituents.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.Type: GrantFiled: July 1, 1994Date of Patent: October 31, 1995Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Alan Hutchison
-
Patent number: 5457105Abstract: The invention concerns quinazoline derivatives of the formula I ##STR1## wherein m is 1, 2 or 3 and each R.sup.1 includes hydroxy, amino, carboxy, carbamoyl, ureido, (1-4C)alkoxycarbonyl, N-(1-4C)alkylcarbamoyl, N,N-di-[(1-4C)alkyl]carbamoyl, hydroxyamino, (1-4C)alkoxyamino, (2-4C)alkanoyloxyamino, trifluoromethoxy, (1-4C)alkyl, (1-4C)alkoxy and (1-3C)alkylenedioxy;n is 1 or 2 and each R.sup.2 includes hydrogen, hydroxy, halogeno, trifluoromethyl, amino, nitro, cyano and (1-4C)alkyl;or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them; and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of cancer.Type: GrantFiled: August 2, 1994Date of Patent: October 10, 1995Assignee: Zeneca LimitedInventor: Andrew J. Barker
-
Patent number: 5436240Abstract: Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, alkenyl, or alkynyl, C.sub.3-10 cycloalkyl, or R.sub.1 and R.sub.2 are joined to form a C.sub.3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C.sub.1-6 alkyl, halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO.sub.2, N, CH, CH.sub.2, CHCH.sub.3, C=O, C=S, C-SCH.sub.3, C=NH, C-NH.sub.2, C-NHCH.sub.3, CNHCOOCH.sub.3, or C-NHCN. B is CH.sub.2, CH, C=O, N, NH or N-CH.sub.3 ; n is 0 or 1; and D is CH, CH.sub.2, C=O, 0, N, NH or N-CH.sub.3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.Type: GrantFiled: October 6, 1993Date of Patent: July 25, 1995Assignee: The Upjohn CompanyInventors: Malcolm W. Moon, Richard F. Heier, Jeanette K. Morris
-
Patent number: 5428161Abstract: 3,7-Diamo phenazine dye having at least one electron-withdrawing substituent on at least one of the groups attached to the amine groups at the 3- and 7-positions, provided that the algebraic sum of the para position Hammett sigma (.rho..sub.p) values for the groups attached to the nitrogen atoms of the amine groups at the 3- and 7-positions is more positive khan about -0.6. The group containing the electron-withdrawing substituent can be selected from(1) a substituted alkyl group, and(2) a substituted aryl group.Type: GrantFiled: December 14, 1990Date of Patent: June 27, 1995Assignee: Minnesota Mining and Manufacturing CompanyInventors: Alan G. Miller, Balchunis: Robert J.
-
Patent number: 5426186Abstract: This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: n is 0, 1, or 2, X is ##STR2## and R.sub.1, R.sub.2, R.sub.3, W and Y are variables These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.Type: GrantFiled: March 3, 1993Date of Patent: June 20, 1995Assignee: Neurogen CorporationInventors: Kenneth Shaw, Alan Hutchison
-
Patent number: 5420275Abstract: An assay method which comprises utilizing chemiluminescence of a pyridopyridazine compound of the formula ##STR1## wherein R.sub.1 is a hydrocarbon group or a heterocyclic group each of which may be substituted and R.sub.2 is hydroxy group, thiol group, amino group or a monosubstituted amino group, and when R.sub.2 is a monosubstituted amino group, R.sub.2 may be taken together with R.sub.1 to form the ring; R.sub.3 is hydrogen atom, a hydroxy group which may be substituted, an amino group which may be substituted, a thiol group which may be substituted, a halogen atom, a heterocyclic group, nitro group, cyano group, carboxyl group which may be esterified or amidated, azido group, sulfo group or an organic sulfonyl group, provided that when R.sub.1 is an aliphalic group, R.sub.3 is not hydrogen atom; and X is oxygen atom or sulfur atom/or a salt thereof; and a novel compound of the formula (I) wherein the symbols are as defined above with proviso that R.sub.3 is hydrogen atom, R.sub.Type: GrantFiled: November 2, 1993Date of Patent: May 30, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirotomo Masuya, Yoshio Aramaki
-
Patent number: 5405847Abstract: Novel compounds of the formula ##STR1## where the phenyl ring can also contain a nitrogen atom instead of a CH group, R.sub.1 is C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.3 -C.sub.6 -alkynyloxy, C.sub.2 -C.sub.6 -alkanoyloxy, benzoyloxy, morpholinocarbonyloxy, C.sub.1 -C.sub.6 -alkyloxycarbonyloxy, C.sub.1 -C.sub.6 -alkylaminocarbonyloxy, C.sub.1 -C.sub.6 -dialkylaminocarbonyloxy or the group -Alk-A, where Alk represents C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -hydroxyalkyl or C.sub.3 -C.sub.6 -cycloalkyl and the symbol A represents hydrogen or other substituents.R.sub.2, R.sub.3 and R.sub.4 represent various substituents, where R.sub.1 may also be hydrogen, when R.sub.2 is the group ##STR2## and R.sub.5 represents phenyl, C.sub.1 -C.sub.4 -alkoxyphenyl or diphenylmethyl and R.sub.3 and R.sub.4 are hydrogen and their salts. The compounds provide anti-allergic, anti-asthmatic, anxiolytic and hypotensive effects.Type: GrantFiled: August 24, 1993Date of Patent: April 11, 1995Assignee: Asta Medica AktiengesellschaftInventors: Hans-Reinhold Dieter, Jurgen Engel, Karl-Heinz Klingler, Bernhard Kutscher, Stefan Szelenyi, Ute Achterath-Tuckermann, Jurgen Schmidt, Peter Metzenauer
-
Patent number: 5399553Abstract: A tricyclic compound represented by the general formula (1) and salts thereof are disclosed. ##STR1## A method for producing the tricyclic compound and salts thereof, and an antimicrobial agent containing the tricyclic compound and salts thereof as an active ingredient are also disclosed.Type: GrantFiled: June 16, 1993Date of Patent: March 21, 1995Assignees: Wakunaga Seiyaku Kabushiki Kaisha, Fujisawa Pharmaceutical Company, Ltd.Inventors: Masaharu Yokomoto, Akira Yazaki, Norihiro Hayashi, Shunso Hatono, Satoshi Inoue, Yasuhiro Kuramoto
-
Patent number: 5393755Abstract: Novel polycylic guanine derivatives of the formula: ##STR1## wherein J is oxygen or sulfur, R.sup.1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy;R.sup.2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino, monoalkyl amino or dialkylamino, or --(CH.sub.2).sub.m TCOR.sup.20 wherein m is an integer from 1 to 6, T is oxygen or --NH-- and R.sup.20 is hydrogen, aryl, heteroaryl, alkyl or alkyl substituted with aryl or heteroaryl;R.sup.3 is hydrogen, halo, trifluoromethyl, alkoxy, alkylthio, alkyl, cycloalkyl, aryl, aminosulfonyl, amino, monoalkylamino, dialkylamino, hydroxyalkylamino, aminoalkylamino, carboxy, alkoxycarbonyl or aminocarbonyl or alkyl substituted with awl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino;R.sup.a, R.sup.b, R.sup.c, and R.sup.d are defined in the specification; and n is zero or one.The compounds of formulas (I) and (I') are useful as antihypertensive, muscle relaxant and bronchodilating agents.Type: GrantFiled: December 14, 1992Date of Patent: February 28, 1995Assignee: Schering CorporationInventors: Bernard R. Neustadt, Neil A. Lindo, Brian A. Mc Kittrick
-
Patent number: 5380718Abstract: Arthropodicidal tetrahydropyridazines of Formulae I and II, ##STR1## wherein Q,X,X.sup.1 Y, and G are as defined in the text, compositions containing them and their use in the control of arthropods.Type: GrantFiled: November 12, 1992Date of Patent: January 10, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventors: Charles R. Harrison, George P. Lahm, Thomas M. Stevenson
-
Patent number: 5371080Abstract: Imidazoquinazoline compounds having the formula ##STR1## wherein Q is ##STR2## --COOR.sup.8 or --CN; wherein R.sup.1 is H, alkyl, unsubstituted or substituted cycloalkyl, alkoxy, alkoxyalkyl or CF.sub.3 ; R.sup.8 is alkyl; R.sup.2 and R.sup.3 independently are H, alkyl optionally substituted, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonylalkyl, formylalkyl, or an acetal thereof, or R.sup.2 and R.sup.3 together with the N-atom form a 4-6 membered monocyclic amino group in which ring system one or more of the carbon atoms may be exchanged with N, O or S, sulphinyl, sulphonyl or carbonyl or an acetal thereof, each of these ring systems optionally being substituted; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently are H, OH, halogen, CF.sub.3, NO.sub.2, NH.sub.2, CN, alkyl, alkenyl, alkynyl, alkoxy, alkoxyalkyl or alkoxycarbonyl.Type: GrantFiled: December 15, 1992Date of Patent: December 6, 1994Assignee: Novo Nordisk A/SInventors: Holger C. Hansen, Marit Kristiansen
-
Patent number: 5369104Abstract: Novel compound represented by the formula: ##STR1## wherein X stands for a methine (i.e. the group --CH.dbd.) group or a nitrogen atom; R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, or, taken together, may form a 5- to 7-membered ring combined with the adjacent --C.dbd.C--; R.sup.4 and R.sup.5 respectively stands for a hydrogen atom or an optionally substituted lower alkyl group or, taken together, form a 3- to 7-membered homo- or heterocyclic ring combined with the adjacent carbon atom; A stands for an optionally substituted amino group; m and n denote 1 to 4, respectively, or salts thereof which has an antiallergic, antiinflammatory and anti-PAF activity and is useful as an antiasthmatic agent.Type: GrantFiled: December 28, 1992Date of Patent: November 29, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Yasuhiko Kawano, Yasuko Ashida
-
Patent number: 5326868Abstract: The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## and X represents hydrogen, halogen, or hydroxy;W represents an aryl group unsubstituted or substituted with various organic and inorganic substituents;A, B, C, D, and E represent carbon or nitrogen substituted with hydrogen or various organic and inorganic substituents; andR.sub.3, and R.sub.4 are variables representing various organic and inorganic substituents..These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.Type: GrantFiled: August 12, 1993Date of Patent: July 5, 1994Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Alan Hutchison
-
Patent number: 5318968Abstract: A compound of the formula, ##STR1## or its pharmaceutically acceptable salt, and its preparation process and pharmaceutical compositions characterized by containing these compounds as effective ingredients.These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic affections, congestive heart failure, hypertension, asthma, immediate type allergy diseases and the like.Type: GrantFiled: December 21, 1992Date of Patent: June 7, 1994Assignee: Nissan Chemical Industries Ltd.Inventors: Keizo Tanikawa, Akira Saito, Takashi Matsumoto, Ryozo Sakoda, Nobutomo Tsuruzoe, Ken-ichi Shikada
-
Patent number: 5314883Abstract: A compound of the formula: ##STR1## or its pharmaceutically acceptable salt and pharmaceutical compositions containing these compounds as effective ingredients. These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic afflictions, congestive heart failure, hypertension, asthma, immediate-type allergy diseases and the like.Type: GrantFiled: December 21, 1992Date of Patent: May 24, 1994Assignee: Nissan Chemical Industries Ltd.Inventors: Keizo Tanikawa, Akira Saito, Takashi Matsumoto, Ryozo Sakoda, Nobutomo Tsuruzoe, Ken-ichi Shikada
-
Patent number: 5308842Abstract: Conformationally constrained tricyclic derivatives of the thienodiazocine and thienothiadiazocine classes of compounds and ring homologs thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.Type: GrantFiled: May 10, 1993Date of Patent: May 3, 1994Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
-
Patent number: 5306819Abstract: The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## where W represents an aromatic group substituted with various organic and inorganic substituents;X, Y are hydrogen, halogen, hydroxy or amino with the proviso that at least X or Y is hydroxy;A, B C, and D, represent nitrogen or a carbon atom substituted with various organic and inorganic substituents;E represents oxygen, sulfur or substituted nitrogen;R.sub.3, R.sub.4, R.sub.12, and R.sub.13 are variables representing various organic and inorganic substituents; andn is 0, 1, or 2.Type: GrantFiled: August 27, 1992Date of Patent: April 26, 1994Assignee: Neurogen CorporationInventors: Pamela Albaugh, Alan Hutchison, Charles Blum
-
Patent number: 5286860Abstract: This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## represents: ##STR3## where n is 0, 1, or 2; R.sub.1 and R.sub.2 are hydrogen or straight or branched chain alkyl groups;Y represents various organic and inorganic substituents;W represents an aromatic group substituted with various organic and inorganic substituents;A is CH or N;B is a substituted or unsubstituted carbon or N; andE is hydrogen or straight or branched alkyl groupsThese compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.Type: GrantFiled: November 12, 1992Date of Patent: February 15, 1994Assignee: Neurogen CorporationInventors: Charles Blum, Alan Hutchison
-
Patent number: 5283248Abstract: The present invention relates to novel substituted pyrimidobenzimidazole derivatives of the formula ##STR1## wherein the substituents are as described in the specification, and pharmaceutically acceptable salts thereof.The products have an inhibitory action on the DNA-gyrase activity in bacteria. They can accordingly be used for the prevention or control of bacterial infections.Type: GrantFiled: June 25, 1992Date of Patent: February 1, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Christian Hubschwerlen, Ivan Kompis, Jean-Luc Specklin
-
Patent number: 5276028Abstract: The heterocyclic compounds having the general formula I ##STR1## wherein R.sup.3 is ##STR2## wherein R' is H, C.sub.1-6 -alkyl or C.sub.3-7 -cycloalkyl; --B-- is --C(R").dbd.N-- or --N.dbd.C(R")-- wherein R" is a cyclic amine or --NR"'R"", wherein R"' and R"" independently are H,C.sub.1-6 -alkoxy, C.sub.3-7 -cycloalkyl or C.sub.1-6 -alkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics and in improving the cognitive function of the brain of mammals.Type: GrantFiled: September 22, 1992Date of Patent: January 4, 1994Assignee: Nordisk A/SInventor: Holger C. Hansen
-
Patent number: 5266698Abstract: The present invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: where X represents hydrogen of lower alkyl;W represents an aryl group unsubstituted or substituted with various organic and inorganic substitutents; ##STR2## where A, B, C, D, and E represent carbon or nitrogen substituted with hydrogen or various organic and inorganic substituents; andn is 0, 1, or 2, Y, R.sub.3, R.sub.4, R.sub.12, and R.sub.13 are various organic and inorganic substituents.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.Type: GrantFiled: April 30, 1992Date of Patent: November 30, 1993Assignee: Neurogen CorporationInventors: Kenneth Shaw, Alan Hutchison
-
Patent number: 5254685Abstract: A tricyclic compound represented by the general formula (1) and salts thereof. ##STR1## A method for producing the tricyclic compound and salts thereof, and an antimicrobial agent containing the tricyclic compound and salts thereof as an active ingredient are also disclosed.Type: GrantFiled: August 7, 1991Date of Patent: October 19, 1993Assignees: Wakunaga Seiyaku Kabushiki Kaisha, Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaharu Yokomoto, Akira Yazaki, Norihiro Hayashi, Shunso Hatono, Satoshi Inoue, Yasuhiro Kuramoto
-
Patent number: 5212310Abstract: The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## and W, X, A, B, C, D, E, R.sub.3, R.sub.4 are variables. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.Type: GrantFiled: December 19, 1991Date of Patent: May 18, 1993Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Alan Hutchison, Pamela Albaugh
-
Patent number: 5210118Abstract: The present invention relates to a novel method for stabilizing synthetic thermoplastic materials against thermal degradation, which comprises incorporating in said materials one or more compounds of the formula (I) ##STR1## in which R.sub.1 is unsubstituted or substituted phenyl, n is e.g. 1, 2 or 3, and, when n is 1, R.sub.2 is e.g. --COR.sub.3, --COOR.sub.4 or --CO-N(R.sub.5)R.sub.6 in which R.sub.3 is e.g. C.sub.4 -C.sub.17 alkyl, R.sub.4 is e.g. C.sub.4 -C.sub.18 alkyl, cyclohexyl or t-butylcyclohexyl, R.sub.5 and R.sub.6 which can be identical or different are e.g. C.sub.2 -C.sub.8 alkyl or cyclohexyl, and, when n is 2, R.sub.2 is e.g. --CO--R.sub.10 --OC, --COO-R.sub.11 --OOC-- or --CONH--R.sub.12 --NHCO- in which R.sub.10 is e.g. C.sub.2 -C.sub.8 alkylene, R.sub.11 is e.g. C.sub.4 -C.sub.6 alkylene and R.sub.12 is e.g. C.sub.4 -C.sub.6 alkylene, and, when n is 3, R.sub.2 is e.g. benzenetricarbonyl.Several compounds of the formula (I) are new.Type: GrantFiled: June 10, 1991Date of Patent: May 11, 1993Assignee: Ciba-Geigy CorporationInventor: Roberto Scrima
-
Patent number: 5185446Abstract: This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein n is 0,1 or 2 and X is --N.dbd.C--R.sub.9 or NR.sub.10 --C.dbd.Twhere R.sub.1, R.sub.2, R.sub.3, and R.sub.9 and R.sub.10 and X, Y, W and T are variables.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdoes with benzodiazepine type drugs, and enhancement of alertness.Type: GrantFiled: September 4, 1990Date of Patent: February 9, 1993Assignee: Neurogen CorporationInventors: Kenneth Shaw, Alan J. Hutchison
-
Patent number: 5166344Abstract: This invention relates to novel imidazoquinoxalinones and their aza analogs and to a process for their preparation. The compounds of this invention have been found to have inodilatory, vasodilatory, venodilatory and other pharmacologic effects.Type: GrantFiled: September 19, 1991Date of Patent: November 24, 1992Assignee: Berlex Laboratories, Inc.Inventor: David D. Davey
-
Patent number: 5166203Abstract: Novel quinolinecarboxylic acid derivatives of the formula: ##STR1## wherein Z is ##STR2## or ##STR3## in which R.sup.1 is hydrogen atom, a halogen atom, hydroxy or a lower alkyloxy; R.sup.2 is a halogen atom, hydroxy or a lower alkyloxy; R.sup.3 is a lower alkyl; and R.sup.4 is hydroxy or a di(lower alkyl)amino, and a pharmaceutically acceptable salt thereof, which have excellent antibacterial activities and are useful as an antibacterial agent, a pharmaceutical composition containing the same, and process for preparing the same.Type: GrantFiled: May 12, 1991Date of Patent: November 24, 1992Assignee: Kanebo, Ltd.Inventors: Hirosata Kondo, Masahiro Taguchi, Yoshikazu Jinbo, Yoshimasa Inoue, Yasuo Kotera, Fumio Sakamoto
-
Patent number: 5164496Abstract: Compounds of the formula ##STR1## in which R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 have the following meaningsR.sup.1 and R.sup.2 designate optionally substituted aryl, or an optionally substituted heterocyclic radical which contain 1 or 2 five-, six- or seven-membered rings at least one of which contains 1, 2 or 3 hetero atoms from the series comprising O, N and S which has a C.dbd.C in conjugation with the C.dbd.C bond in the five-membered ring of III,X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 designate O, S, NR.sup.5, or X.sup.1 and Y.sup.1 or X.sup.2 and Y.sup.2 in each case form parts of a fused-on heterocyclic five-membered or six-membered ring,processes for their preparation and their use as dyestuffs and pigments.Type: GrantFiled: July 26, 1991Date of Patent: November 17, 1992Assignee: Bayer AktiengesellschaftInventor: Hans Hochstetter