Tricyclo Ring System Having The 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/234)
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Patent number: 5990107Abstract: Fibrinogen receptor antagonist alcohol prodrugs having the structure, for example, of ##STR1## more particularly, ##STR2##Type: GrantFiled: June 26, 1997Date of Patent: November 23, 1999Assignee: Merck & Co., Inc.Inventors: Melissa S. Egbertson, George D. Hartman, William C. Lumma, John S. Wai, Steven D. Young
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Patent number: 5990106Abstract: This invention relates to bicyclic amino group-substituted pyridonecarboxylic acid derivatives of the general formulaA--Priesters thereof and salts thereof, wherein: Pri is a pyridonecarboxylic acid residue, and A is a bicyclic amino group represented by the following formula and joined to the 7-position of the pyridonecarboxylic acid or a position equivalent to the 7-position thereof. ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represents a hydrogen atom, a lower alkyl group or an amino-protecting group; R.sub.3 and R.sub.4 may be the same or different and each represents a hydrogen atom, a halogen atom, a cyano group, a hydroxyl group, an oxo group, a lower alkoxy group or a lower alkyl group; and n is an integer of 0 or 1.The above-described pyridonecarboxylic acid derivatives, esters thereof and salts thereof are useful as antibacterial agents.Type: GrantFiled: August 4, 1997Date of Patent: November 23, 1999Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Masato Sakamoto, Katsumi Chiba, Yukio Tominaga, Akira Minami
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Patent number: 5985869Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substitued benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups beign optionally replaced by O, S, SO, SO.sub.Type: GrantFiled: July 15, 1997Date of Patent: November 16, 1999Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Shinya Kora, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5945418Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: March 20, 1997Date of Patent: August 31, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy
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Patent number: 5935956Abstract: The invention relates to fused pyridazine compounds, in particular pyrido ?h!cinnoline, pyrido?h!cinnolinone, pyridocyclopenta?1,2-c!pyridazine, pyridocyclopenta?1,2-c!pyridazinone, pyridocyclohepta?1,2-c!pyridazine and pyridocyclohepta?1,2-c!pyridazinone derivatives, their use as medicaments and pharmaceutical compositions comprising them.Type: GrantFiled: September 5, 1997Date of Patent: August 10, 1999Assignee: Astra Pharmaceuticals Ltd.Inventors: John Bantick, Simon Hirst, Matthew Perry
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Patent number: 5892040Abstract: A process for preparing a compound of formula (I) or a phamaceutically-acceptable salt thereof, comprising: 1) reacting a compound. of formula (III), in which R is a straight or branched chain alkyl having from one to four carbon atoms, with an alkali metal hydroxide in an aqueous medium at a temperature of about 80.degree. to 120.degree. C. and time of about 20 to 100 hours to form a reaction product; 2) cyclizing the reaction product of step 1) with formic acid and formaldehyde to form a formiate compound; and 3) neutralizing the formiate compound of step 2) with an aqueous base.Type: GrantFiled: January 4, 1996Date of Patent: April 6, 1999Assignee: Pfizer. IncInventors: Martin Karpf, Rene Trussardi
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Patent number: 5886008Abstract: Compounds of formula (I), wherein R.sub.1 is (a), (b), (c) or (d); n is 0, 1 or 2; A, B, C and D are each independently nitrogen or carbon; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkyl-aryl, halogen (e.g. fluorine, chlorine, bromine or iodine), cyano, nitro, --(CH.sub.2).sub.m NR.sub.14 R.sub.15, --(CH.sub.2).sub.m OR.sub.9, --SR.sub.9, --SO.sub.2 NR.sub.14 R.sub.15, --(CH.sub.2).sub.m NR.sub.14 SO.sub.2 R.sub.15 --(CH.sub.2).sub.m NR.sub.14 CO.sub.2 R.sub.9, --(CH.sub.2).sub.m NR.sub.14 COR.sub.9, --(CH.sub.2).sub.m NR.sub.14 CONHR.sub.9, --CONR.sub.14 R.sub.15, or --CO.sub.2 R.sub.9 ; R.sub.2 and R.sub.3, R.sub.3 and R.sub.4, or R.sub.4 and R.sub.Type: GrantFiled: April 27, 1995Date of Patent: March 23, 1999Assignee: Pfizer Inc.Inventor: John Eugene Macor
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Patent number: 5837705Abstract: The invention relates to alpha-substituted pyridazino-quinoline compounds of the formula I: ##STR1## wherein Ring A is chosen from an ortho fused aromatic or heteroaromatic five- or six-membered ring; R.sup.1 is selected from a variety of substituents including halogen, (1-4C)alkyl and nitro; R.sup.2 is selected from a group of the formula R2', R2" or R2"' wherein R2' is --CHR.sup.3 (CH.sub.2).sub.n C(O)NR.sup.5 R.sup.6 ; R2" is --CHR.sup.3 (CH.sub.2).sub.n R.sup.4 and R2"' is --CHR.sup.3 (CH.sub.2).sub.n L wherein n is 0-6; R.sup.5 is aryl or substituted aryl; R.sup.6 is (1-6C)alkyl or hydrogen; R.sup.3 is (1-6C)alkyl, (0-6C)alkylCF.sub.3 or (0-6C)alkylCOOR'; R.sup.4 is (1-6C)alkyl, (2-6C)alkyl containing a double or triple bond, or (0-6C)alkylaryl; L is a variety of substituents including phenyl, heteroaryl and CO.sub.2 R'; R' is hydrogen or (1-4C)alkyl; Z is selected from oxo, --OH, H,H--, H, (1-6C)alkyl or (1-6C)alkylaryl; and R.sup.7 is hydrogen or --(CO)R.sup.8 wherein R.sup.Type: GrantFiled: April 1, 1996Date of Patent: November 17, 1998Assignee: Zeneca LimitedInventors: Thomas Michael Bare, James Roy Empfield, Janet Marie Forst, Keith John Herzog, Richard Bruce Sparks
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Patent number: 5792766Abstract: Disclosed are compounds of compounds of the formula: ##STR1## or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H.sub.2 or sulfurY is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups;W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; orW is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; andZ.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C-R.sub.1 whereR.sub.1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors.Type: GrantFiled: March 13, 1996Date of Patent: August 11, 1998Assignee: Neurogen CorporationInventors: Paul Chen, Alan Hutchison, Guolin Cai
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Patent number: 5786361Abstract: Compounds of the formula (I): ##STR1## are prepared by reaction of the phenylacetic acid derivatives substituted by the appropriate heterocycles, optionally in an activated form, with phenylglycinols. The compounds are suitable as active compounds in medicaments, in particular in medicaments having antiatherosclerotic activity.Type: GrantFiled: April 11, 1997Date of Patent: July 28, 1998Assignee: Bayer AktiengesellschaftInventors: Ulrich Muller, Peter Eckenberg, Rudi Grutzmann, Hilmar Bischoff, Dirk Denzer, Ulrich Nielsch
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Patent number: 5776935Abstract: Pyridyl-phtalazin diones having the following formula: ##STR1## wherein R1 and R2 are selected from the group consisting of hydrogen, halogen, and methoxy or wherein R1 and R2 together form methylenedioxy, and pharmaceutically-acceptable salts thereof, and pharmaceutical compositions containing an effective glycine.sub.B antagonistic amount thereof, are useful in combatting neurological disorders associated with excitotoxicity and malfunctioning of glutamatergic neurotransmission in a living animal, including a human, in need thereof.Type: GrantFiled: July 25, 1996Date of Patent: July 7, 1998Assignee: Merz & Co. GmbH & Co.Inventors: Wojciech Danysz, Markus Gold, Ivars Kalvinsh, Christopher Graham Raphael Parsons, Irene Piskunova, Eugene Rozhkov
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Patent number: 5763440Abstract: Compounds with fungicidal properties having formula I ##STR1## wherein W is CH.sub.3 --O--A.dbd.C(-)--CO(V)CH.sub.3 ;A is N or CH;V is O or NH;R.sub.4 and R.sub.5 are independently selected from hydrogen and substituted or unsubstituted alkyl and aryl groups and Q is substituted or unsubstituted aryl groups.Type: GrantFiled: June 7, 1996Date of Patent: June 9, 1998Assignee: Rohm and Haas CompanyInventors: Ronald Ross, Steven Howard Shaber
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Patent number: 5756501Abstract: This invention relates to novel compounds which bind to central cholinergic muscarinic M1 receptors and may be useful for treatment of diseases attributed to cholinergic insufficiency such as presenile dementia, senile dementia of the Alzheimer's type, Parkinson's disease, Down's syndrome, and dementia pugilistica. The compounds useful in this invention have the formula ##STR1## or a 6, 7, 8, 9 tetrahydro analog thereof, where R.sup.1 is selected from H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, cyano, halo, nitro, and --NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently selected from H, C.sub.1 -C.sub.6 alkyl and phenyl, optionally substituted with halo, cyano, hydroxy, nitro, amino, mono or di C.sub.1 -C.sub.6 alkylamino, phenylamino, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy;R.sup.2 is CF.sub.3 --, CF.sub.3 CH.sub.2 --, or --CH.sub.2 --X--R.sup.6 where X is oxygen or NH and R.sup.6 is C.sub.1 -C.sub.6 alkyl, phenyl-(CH.sub.2).sub.n -- or --(CH.sub.2).Type: GrantFiled: December 3, 1996Date of Patent: May 26, 1998Assignee: American Home Products CorporationInventor: Annmarie L. Sabb
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1-arylsulphonyl, arylcarbonyl and arylthiocarbonyl pyridazino derivatives and methods of preparation
Patent number: 5753655Abstract: 1-Arylsulphonyl, arylcarbonyl and arylthiocarbonyl pyridazino derivatives and processes for making said derivatives are described. The novel derivatives are non-steroidal heterocyclic compounds which act as selective progestins and/or antiprogestins having a high in-vitro affinity for either the uterine, breast or bone progestin receptor. As such, the non-steroidal heterocyclic derivatives are useful in contraception, menopause, osteoporosis or endometriosis.Type: GrantFiled: October 10, 1996Date of Patent: May 19, 1998Assignee: Ortho Pharmaceutical CorporationInventor: Donald W. Combs -
Patent number: 5753664Abstract: A novel compound of the formula:A--Z--Ar.sup.1 1'CO--Ar.sup.2wherein A is a condensed pyrimidinone or condensed pyridazinone ring; Ar.sup.1 and Ar.sup.2 are independently a ring; Z is a divalent group, or a salt thereof which have an excellent antitumor activity.Type: GrantFiled: March 13, 1996Date of Patent: May 19, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Shogo Marui, Fumio Itoh, Masuo Yamaoka, Masafumi Nakao
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Patent number: 5750690Abstract: A process for the asymmetric hydrogenation of a compound of the formula ##STR1## wherein each R, independently, is alkyl, arylmethyl, aryl, alkoxy, arylmethoxy or aryloxy or both R's, taken together, are methylene, ethylene or 1,2-phenylene and n is 1,2 or 3,or of a salt thereof to a compound of the formula ##STR2## in the form of an (S) or (R) enantiomer, wherein R and n have the significances given above, using an optically active ruthenium-diphosphine complex as catalyst, is described. The preparation of the compounds of formula II, as well as the compounds of formula II, which form a further object of the invention, are also described.Type: GrantFiled: July 26, 1996Date of Patent: May 12, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Emil Albin Broger, Yvo Crameri, Marquard Imfeld, Fran.cedilla.ois Montavon, Erich Widmer
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Patent number: 5744471Abstract: The present invention relates to compounds, pharmaceutical compositions and methods of using compounds of formula (I) in the treatment and/or prevention of certain diseases or conditions. In formula (I), A is chosen from ortho substituted aryl or heteroaryl species, X is chosen from --OH, --SH, NHR and R.sup.1 or R.sup.2 is chosen from --(CH.sub.2).sub.n L wherein L may be selected from a variety of substituents including aryl, heteroaryl and heterocyclic groups. The compounds are useful in treating and/or preventing neurological disorders associated with excitatory amino acids.Type: GrantFiled: April 17, 1996Date of Patent: April 28, 1998Assignee: Zeneca LimitedInventors: Thomas Michael Bare, Timothy Wayne Davenport, James Roy Empfield, Jeffrey Alan McKinney, Richard Bruce Sparks
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Patent number: 5739133Abstract: The present invention relates to pyridazino?4,5-b!quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino?4,5-b!quinolines as active ingredient, and methods for the treatment of neurological disorders.Type: GrantFiled: August 15, 1996Date of Patent: April 14, 1998Assignee: Zeneca LimitedInventors: Thomas Michael Bare, Richard Bruce Sparks
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Patent number: 5733910Abstract: The present invention relates to pyridazino?4,5-b!quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino?4,5-b!quinolines as active ingredient, and methods for the treatment of neurological disorders.Type: GrantFiled: August 5, 1996Date of Patent: March 31, 1998Assignee: Imperial Chemical Industries PLCInventors: Thomas Michael Bare, Richard Bruce Sparks
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Patent number: 5719282Abstract: The invention relates to new compounds derived from 1,4-bis(alkylamino)benzo?g!phthalazenes of formula (I) which are useful as anticancerous and antiparasitic agents.Type: GrantFiled: May 10, 1995Date of Patent: February 17, 1998Assignee: Consejo Superior De Investigaciones CientificasInventors: Pilar Navarro Torres, Lucrecia Campayo Perez, Jose Antonio Escario Garcia Trevijano, Ismael Alvarez Rodriguez
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Patent number: 5716956Abstract: Substituted dihydrophthalazine compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neurosychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.Type: GrantFiled: January 18, 1996Date of Patent: February 10, 1998Assignee: Bearsden Bearsden Bio, Inc.Inventor: Jeffrey C. Pelletier
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Patent number: 5696127Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 9, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lin Zhi, James P. Edwards, Christopher M. Tegley, Sarah J. West
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Patent number: 5696130Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 9, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, David T. Winn, Mark E. Goldman, Lawrence G. Hamann, Lin Zhi, Luc J. Farmer, Robert L. Davis
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Patent number: 5693640Abstract: A class of pyridazino?4,5-b!indole-1,4-dione derivatives, substituted in the 2-position by an optionally substituted phenyl moiety, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment and/or prevention of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA antagonist.Type: GrantFiled: June 6, 1995Date of Patent: December 2, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Tamara Ladduwahetty, Angus Murray MacLeod
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Patent number: 5693646Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 2, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Christopher M. Tegley, Lin Zhi, James P. Edwards, Sarah J. West
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Patent number: 5693647Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 2, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lin Zhi, Christopher M. Tegley, David T. Winn, Lawrence G. Hamann, James P. Edwards, Sarah J. West
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Patent number: 5688810Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 18, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Mark E. Goldman, Charlotte L.F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
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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
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Patent number: 5688808Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 18, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, David T. Winn, Lin Zhi, Lawrence G. Hamann, Christopher M. Tegley, Charlotte L. F. Pooley
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Patent number: 5663172Abstract: A preventive agent for platelet aggregation comprising a compound represented by the following general formula [I]: ##STR1## wherein Y is --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --, R is hydrogen or methyl, and ---------- represents a single bond or a double bond, or a pharmaceutically-compatible complex thereof as the active ingredient, is disclosed.Type: GrantFiled: April 26, 1995Date of Patent: September 2, 1997Assignee: Nippon Soda Co., Ltd.Inventors: Nobuo Mochizuki, Shuichi Souma, Takayoshi Sasaki, Yukihiro Kanaguchi, Nobuhiro Umeda
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Patent number: 5658917Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.Type: GrantFiled: April 28, 1995Date of Patent: August 19, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shigeki Fujiwara, Daisuke Machii, Haruki Takai, Hiromi Nonaka, Hiroshi Kase, Kozo Yao, Michiyo Kawakage, Hideaki Kusaka, Akira Karasawa
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Patent number: 5652239Abstract: The present invention relates to pyridazino[4,5-b]indoles, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]indoles as active ingredient, and methods for the treatment of neurological disorders.Type: GrantFiled: October 19, 1995Date of Patent: July 29, 1997Assignee: Imperial Chemical CompanyInventors: Thomas Michael Bare, James Franklin Resch, Paul Francis Jackson
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Patent number: 5648353Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.Type: GrantFiled: May 22, 1995Date of Patent: July 15, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shigeki Fujiwara, Daisuke Machii, Haruki Takai, Hiromi Nonaka, Hiroshi Kase, Kozo Yao, Michiyo Kawakage, Hideaki Kusaka, Akira Karasawa
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Patent number: 5631254Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.Type: GrantFiled: June 6, 1995Date of Patent: May 20, 1997Assignee: Rohm and Haas CompanyInventors: Enrique L. Michelotti, Anne R. Egan, Ronald Ross, Jr., Willie J. Wilson
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Patent number: 5624926Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.Type: GrantFiled: October 17, 1994Date of Patent: April 29, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shigeki Fujiwara, Daisuke Machii, Haruki Takai, Hiromi Nonaka, Hiroshi Kase, Kozo Yao, Michiyo Kawakage, Hideaki Kusaka, Akira Karasawa
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Patent number: 5622962Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase.Type: GrantFiled: May 11, 1995Date of Patent: April 22, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, Loretta A. McQuaid, Blake L. Neubauer, Vincent P. Rocco
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Patent number: 5622961Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase.Type: GrantFiled: May 11, 1995Date of Patent: April 22, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, Loretta A. McQuaid, Blake L. Neubauer, Vincent P. Rocco
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Patent number: 5609867Abstract: This invention provides novel antitumor agents having the formula: ##STR1## wherein A, B, G, W, R.sup.1, R.sup.2, R.sup.3, n, m and Z are described in the specification which have activity as anticancer agents and inhibit leukemia and solid tumor growth in a mammal.Type: GrantFiled: August 29, 1995Date of Patent: March 11, 1997Assignee: American Cyanamid CompanyInventor: Hwei-Ru Tsou
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Patent number: 5605900Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C-R.sup.11 (wherein R.Type: GrantFiled: April 28, 1995Date of Patent: February 25, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shigeki Fujiwara, Daisuke Machii, Haruki Takai, Hiromi Nonaka, Hiroshi Kase, Kozo Yao, Michiyo Kawakage, Hideaki Kusaka, Akira Karasawa
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Patent number: 5606059Abstract: This invention encompasses compounds of formula (I) and pharmaceutically acceptable non-toxic salts thereof wherein (Ia) represents (i) or (ii) where n is 0, 1, or 2: R.sub.1 and R.sub.2 are hydrogen or straight or branched chain alkyl groups; Y 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; and E is hydrogen or straight or branched alkyl groups. 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: May 12, 1995Date of Patent: February 25, 1997Assignee: Neurogen CorporationInventors: Charles Blum, Alan Hutchison
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Patent number: 5604227Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.Type: GrantFiled: April 13, 1995Date of Patent: February 18, 1997Assignee: Imperial Chemical Industries PLCInventors: Thomas M. Bare, Richard B. Sparks
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Patent number: 5599814Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.Type: GrantFiled: April 24, 1995Date of Patent: February 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Thomas M. Bare, Richard B. Sparks
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Patent number: 5597922Abstract: 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 and inducing anesthesia are disclosed by administering to an animal in need of such treatment a compound which has high binding to the glycine receptor.Type: GrantFiled: July 29, 1994Date of Patent: January 28, 1997Assignees: 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, Acea Pharmaceuticals, Inc., The Regents of the University of CaliforniaInventors: Sui X. Cai, John F. W. Keana, Eckard Weber
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Patent number: 5597823Abstract: The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a tricyclic heterocyclic ring system; which is an .alpha.-1 adrenergic antagonist and is useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 receptors and treating BPH.Type: GrantFiled: June 5, 1995Date of Patent: January 28, 1997Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, Robert J. Altenbach, Fatima Z. Basha, William A. Carroll, Irene Drizin, Steven W. Elmore, James F. Kerwin, Jr., Suzanne A. Lebold, Edmund L. Lee, Kevin B. Sippy, Karin R. Tietje, Michael D. Wendt
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Patent number: 5597918Abstract: A fused pyridazine compound of the formula ##STR1## wherein each symbol is as defined in the description. The compounds of the present invention are useful as anxiolytic agents which selectively act on anxiety because of having less side effects (e.g. muscle-relaxation, sedation or interaction with alcohol/barbiturates).Type: GrantFiled: June 2, 1995Date of Patent: January 28, 1997Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tohru Nakao, Hiroshi Tanaka, Yasuto Morimoto, Shuzo Takehara
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Patent number: 5578724Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase and their preparation is disclosed.Type: GrantFiled: September 20, 1994Date of Patent: November 26, 1996Assignee: Eli Lilly and CompanyInventors: Kevin L. Haehl, Thomas J. Kress, James P. Wepsiec
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Patent number: 5569658Abstract: The invention concerns tricyclic derivatives of the formula I ##STR1## wherein R.sup.1 and R.sup.2 together form an optionally substituted group of the formula --N.dbd.CH--NH--, --N.dbd.CH--O--, --N.dbd.CH--S--, --N.dbd.N--NH--, --NH--N.dbd.CH--, --NH--CH.dbd.CH--. --NH--CO--NH--, --NH--CO--O--, --NH--CO--S--, --NH--NH--CO--, --N.dbd.CH--CH.dbd.N--, --N.dbd.N--CH.dbd.CH--, --N.dbd.CH--N.dbd.CH--, --N.dbd.CH--CH.dbd.N--, --NH--CO--CH.dbd.CH-- or --N.dbd.CH--CO--NH--; m is 1, 2 or 3 and R.sup.3 includes hydrogen, halogeno 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: July 19, 1994Date of Patent: October 29, 1996Assignee: Zeneca LimitedInventor: Andrew J. Barker
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Patent number: 5552409Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R.sup.1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.Type: GrantFiled: March 31, 1994Date of Patent: September 3, 1996Assignee: Rohm and Haas CompanyInventors: Enrique L. Michelotti, Anne R. Egan, Ronald Ross, Jr., Willie J. Wilson
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Patent number: 5545835Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pylidinedicarboxylic acids.Type: GrantFiled: November 4, 1994Date of Patent: August 13, 1996Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Patent number: 5527921Abstract: Peroxycarboxylic ester photoinitiators derived from aromatic nitrogen containing heterocyclic carboxylic acids are described. The heterocyclic aromatic ring may contain additional nitrogen atoms, be fused with another aromatic ring system, be substituted with an additional peroxycarboxylic ester group and/or be substituted with an electron group having a Hammett sigma value greater than 0.1. The peroxycarboxylic ester photoinitiators have been found to be useful in photopolymerizable compositions and photosensitive elements.Type: GrantFiled: March 21, 1995Date of Patent: June 18, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: Jeanne E. Haubrich