Nitrogen, Other Than As Nitro Or Nitroso, Attached Indirectly To The Quinoline Ring System By Nonionic Bonding Patents (Class 546/176)
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Patent number: 5807866Abstract: A process for producing a compound of the formu5la ##STR1## comprising the step of reacting a compound of the formula ##STR2## with a compound of the formula ##STR3## to form a compound of the formula ##STR4## wherein R.sup.2a is selected from the groups recited above for R.sup.2, or R.sup.2a --X-- is a protected hydroxyl group, and Z is a group of formula --Y--R.sub.5 recited above, or a group that can be converted into a group of said formula --Y--R.sup.5. Intermediates of formula IV and composition containing substantially optically pure enantiomers of Formula (I) are included within the scope of the invention.Type: GrantFiled: November 19, 1996Date of Patent: September 15, 1998Assignees: The University of East Anglia, Eli Lilly and CompanyInventors: Nicholas James Bach, Stephen Richard Baker, Jeremy Gilmore, Russell Andrew Lewthwaite, Alexander McKillop, Jason Scott Sawyer, George Richard Stephenson, Michael William John Urquhart
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Patent number: 5795889Abstract: This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.Type: GrantFiled: February 9, 1995Date of Patent: August 18, 1998Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
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Patent number: 5795900Abstract: Compounds having the formula: ##STR1## wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH.dbd.N--O--A--COM, (c) CH.sub.2 --O--N.dbd.A--COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.6, (c) --NR.sup.7 R.sup.8, (d)--NR.sup.6 SO.sub.2 R.sup.Type: GrantFiled: September 17, 1996Date of Patent: August 18, 1998Assignee: Abbott LaboratoriesInventors: Clint D. Brooks, Pramila Bhatia, Teodozyj Kolasa, Andrew O. Stewart, David E. Gunn, Richard A. Craig
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Patent number: 5776932Abstract: 1,3,5-trisubstituted indazole derivatives of the formula ##STR1## wherein R1 is H, (b) a C.sub.1-6 straight or branched, substituted or unsubstituted alkyl residue, (c) a C.sub.3-7 cycloalkyl residue, (d) an unsustituted or substituted phenyl, naphthyl, anthranyl, or fluorenyl residue, (e) a quinolin-2-ylmethoxy, or pyridin-2-ylmethoxy residue; X is O, or a --NH, --NH--(C.dbd.O)--NH--, --NH--(C.dbd.O)--O--, --NH--(C.dbd.O)--, or --NH--CH.sub.2 --(C.dbd.O)-- residue; Y is O, or S; R.sub.2 is H; Z is a SO, SO.sub.2, --(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --O--, --O--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--, --(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--NH--, --NH--(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CHOH--, --CHOH--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CH.dbd.CH--, or --CH.dbd.CH--(CH.sub.2).sub.Type: GrantFiled: March 20, 1997Date of Patent: July 7, 1998Assignee: Arzneimittelwerk Dresden G.m.b.H.Inventors: Rudolf Schindler, Ilona Fleischhauer, Istvan Szelenyi
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Patent number: 5770614Abstract: A novel 2-(substituted phenyl)-2-alkoxyiino-N-alkylacetamide compounds having a wide fungicidal spectrum and especially an excellent activity of controlling Pseudocercosporella herpotrichoides; and a composition containing the compound for controlling Pseudocercosporella herpotrichoides.Type: GrantFiled: November 12, 1996Date of Patent: June 23, 1998Assignee: Shionogi & Co., Ltd.Inventors: Akira Murabayashi, Akira Takase, Hideyuki Takenaka, Michio Masuko
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Patent number: 5763638Abstract: A process for the preparation of nitriles of formula ##STR1## wherein X is CH or N, and R.sub.1 and R.sub.2 are each independently of the other hydrogen, chloro, bromo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, CN, phenyl, phenoxy, dimethylamino, piperidyl, morpholinyl or pyrrolidyl, or R.sub.1 and R.sub.2 together form a fused benzene ring, by reacting an aldehyde of formula ##STR2## with hydroxylaminosulfate in the presence of a tertiary amine base of formula ##STR3## wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen, methyl or ethyl, R.sub.5 is branched C.sub.3 -C.sub.5 alkyl or phenyl, and R.sub.6 and R.sub.7 are methyl or ethyl,in the temperature range from 100.degree. to 160.degree. C., while distilling the released water of reaction off concomittantly at a pressure in the range of 0.02 to 1.5 bar, with subsequent removal of the ammonium salts, and isolating the nitrile so obtained by customary methods.Type: GrantFiled: February 4, 1997Date of Patent: June 9, 1998Assignee: Ciba Specialty Chemicals CorporationInventor: Richard Breitschuh
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Patent number: 5760018Abstract: The present invention is directed to certain compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, A.sup.1, A.sup.2, X, m and n are defined herein. The compounds of this invention are tachykinin receptor antagonists and are of particular use in the treatment of pain, inflammation, migraine and emesis.Type: GrantFiled: July 11, 1996Date of Patent: June 2, 1998Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Richard Thomas Lewis, Angus Murray MacLeod, Graeme Irvine Stevenson
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Patent number: 5756769Abstract: A method for producing a propargylamine compound represented by the general formula (I): ##STR1## which comprises reacting a propargyl compound represented by the general formula (II): ##STR2## with an aromatic aldehyde represented by the general formula (III):ArCHO (III)and ammonia to obtain an imine compound represented by the general formula (IV): ##STR3## and hydrolyzing the resultant imine compound. It is to provide a method for producing a propargylamine compound from a propargyl compound by a simple operation without using a special facility, using ammonia as a reaction reagent, without producing a dipropatygylamine compound and a tripropargylamine compound as by-products.Type: GrantFiled: May 30, 1997Date of Patent: May 26, 1998Assignee: Sumitomo Chemical Company, Ltd.Inventors: Shinzo Seko, Akihiko Nakamura, Motoo Hazama
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Patent number: 5756518Abstract: This invention relates to a phenylene derivative represented by the following formula (1) or a salt thereof and also to a medicine containing it as an effective ingredient. ##STR1## wherein R.sup.1 represents H or halogen; A represents --CH.dbd.CH--, --CH.dbd.N--, --N(R.sup.2)--, --O-- or --S--; W represents --CH.dbd.CH-- or --CH.sub.2 O--; X represents --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 N(R.sup.3)--, --CH.dbd.N--, --COO-- or --CONH--; Y represents ##STR2## B.sup.1 represents --C(R.sup.7)(R.sup.8)(CH.sub.2).sub.l --, --S(O).sub.m (CH.sub.2).sub.n -- or --CH.dbd.C(R.sup.9)--; B.sup.2 represents --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --; Z.sup.1 and Z.sup.2 each represents O or S; etc. The phenylene derivative or salt thereof has antileukotrienic action and antihistaminic action and is useful as a medicine such as an asthma preventive or curative.Type: GrantFiled: March 26, 1997Date of Patent: May 26, 1998Assignee: Kowa Co., Ltd.Inventors: Henk Timmerman, Mingqiang Zhang, Kazuhiro Onogi, Masahiro Tamura, Tsutomu Toma, Yasushi Wada
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Patent number: 5753652Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.Type: GrantFiled: April 4, 1995Date of Patent: May 19, 1998Assignee: Novartis CorporationInventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
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Patent number: 5747505Abstract: The heterocyclic aryl-, alkyl- and cycloalklacetamides are prepared by reacting the appropriately substituted acetic acids with amines, if appropriate in complexed form. The heterocyclic aryl-, alkyl- and cycloalkylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.Type: GrantFiled: September 20, 1996Date of Patent: May 5, 1998Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
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Patent number: 5747420Abstract: Novel herbicidal tetrazolinone derivatives of the formula ##STR1## and intermediates therefor of the formula ##STR2## wherein R.sup.1 is alkyl substituted by halogen, andR.sup.2 and R.sup.3 each independently is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or substituted phenyl, orR.sup.2 and R.sup.3 together with the N-atom to which they are attached, which may form a 5- or 6-membered heterocyclic ring.Type: GrantFiled: November 3, 1995Date of Patent: May 5, 1998Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Seishi Ito, Kazuhiro Ukawa, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
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Patent number: 5734058Abstract: New intercalating cyanine dyes are provided in which the benzothiazole portion of the cyanine dye has been modified to produce dyes with improved properties for labelling nucleic acids. The fluorescent cyanine dyes have a positively charged substituent attached to the positively charged nitrogen on the benzothiazole portion of the cyanine dye.Type: GrantFiled: November 9, 1995Date of Patent: March 31, 1998Assignee: Biometric Imaging, Inc.Inventor: Linda G. Lee
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Patent number: 5731315Abstract: The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: December 6, 1996Date of Patent: March 24, 1998Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: William R. Ewing, Michael R. Becker, Yong Mi Choi-Sledeski, Heinz W. Pauls, Daniel G. McGarry, Roderick S. Davis, Alfred P. Spada
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Patent number: 5728715Abstract: 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: October 30, 1996Date of Patent: March 17, 1998Assignee: Rohm and Haas CompanyInventors: Enrique Luis Michelotti, Anne Ritchie Egan, Ronald Ross, Jr., Willie Joe Wilson
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Patent number: 5721255Abstract: The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula ##STR1## wherein W, R.sup.1, R.sup.2, R.sup.3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: February 15, 1995Date of Patent: February 24, 1998Assignee: Pfizer Inc.Inventors: Harry R. Howard, Masami Nakane, Masaya Ikunaka, Kunio Satake, Terry J. Rosen, John A. Lowe, III, Brian T. O'Neill, Fumitaka Ito
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Patent number: 5719163Abstract: A class of substituted oxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R is selected from alkyl, hydroxyalkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl optionally substituted at a substitutable position by carboxy, alkyl, alkoxy and halo, aralkyl optionally substituted at a substitutable position on the aryl radical by carboxy, alkyl, alkoxy and halo, aryloxyalkyl optionally substituted at a substitutable position on the aryl radical with halo, carboxy, alkyl and alkoxy, aralkoxyalkyl optionally substituted at a substitutable position by alkyl, carboxy, alkoxy and halo, heteroaryloxyalkyl optionally substituted at a substitutable position with halo, carboxy, alkyl and alkoxy, alkoxycarbonylalkyl, carboxyalkyl and aminocarbonylalkyl; wherein R.sup.Type: GrantFiled: October 27, 1995Date of Patent: February 17, 1998Assignee: G.D. Searle & Co.Inventors: Bryan H. Norman, Len F. Lee, Jaime L. Masferrer, John J. Talley
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Patent number: 5716967Abstract: This invention relates to isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDE.sub.IV). The isoxazoline compounds are useful in inhibiting PDE.sub.IV and in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease, psoriasis, allergic rhinitis, dermatitis, shock, atopic dermatitis, rheumatoid arthritis and osteoarthritis. This invention also relates to pharmaceutical compositions useful therefor.Type: GrantFiled: May 15, 1996Date of Patent: February 10, 1998Assignee: Pfizer Inc.Inventor: Edward Fox Kleinman
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Patent number: 5716989Abstract: The invention relates to bicyclo?3.3.0!octane compounds of formula I, ##STR1## wherein the variable are defined in this specification, as well as their enantiomers, and their salts with physiologically compatible bases. .alpha.-, .beta.-, or .tau.-Cyclodextrin clathrates of the compounds and the compounds encapsulated with liposomes are also included. The invention is further directed to processes for production of the compounds and their pharmaceutical use.Type: GrantFiled: November 27, 1991Date of Patent: February 10, 1998Assignee: Schering AktiengesellschaftInventors: Ulrich Klar, Hartmut Rehwinkel, Helmut Vorbruggen, Karl Heinz Thierauch, Peter Verhallen
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Patent number: 5714488Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein W is selected from the group consisting of optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are one or more groups independently selected from hydrogen, alkyl, halolalkyl, alkoxy, and halogen; Z is selected from the group consisting of N--OH, N--O--A--COM, CH--COM, and CH--CH.dbd.N--0--A--COM wherein A is selected from the group consisting of alkylene, alkenylene, cycloalkylene, and optionally substituted alkylphenyl wherein the alkyl portion is of one to six carbon atoms, and M is selected from the group consisting of a pharmaceutically acceptable, metabolically clearable group, --OR.sup.3, and --NR.sup.4 R.sup.Type: GrantFiled: September 17, 1996Date of Patent: February 3, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Pramila Bhatia, Teodozyj Kolasa
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Patent number: 5710164Abstract: Disclosed herein are compounds of the formula: ##STR1## where Ar.sub.1 and Ar.sub.2 are, independently, pyridinyl, quinolinyl, 1,4-benzodioxanyl, dihydro-1,4-benzodioxanyl, pyrrolyl, azaindolyl or carbazolyl, or a pharmaceutically acceptable salt thereof, which are useful as inhibitors of smooth muscle cell proliferation.Type: GrantFiled: June 6, 1995Date of Patent: January 20, 1998Assignee: American Home Products CorporationInventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski
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Patent number: 5703071Abstract: The present invention provides novel tropolone derivatives of the formula I ##STR1## wherein R.sub.10 is a substituted or unsubstituted piperazinyl or benzothiazolidinyl group, and pharamaceutical compositions thereof. These compounds are useful for the prevention and treatment of ischemic diseases, including cerebrovascular diseases and cardiovascular diseases.Type: GrantFiled: May 18, 1995Date of Patent: December 30, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Noriie Itoh, Mineo Kunihara, Hiroshi Kushida, William W. McWhorter, Syunji Nomura, Kazunori Ozawa, Mikio Taniguchi, Kazuo Tsuzuki
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Patent number: 5695684Abstract: A mesomorphic compound represented by a formula (I) containing a quinoline-2,6-diyl skeleton is suitable as a component for a liquid crystal composition providing improved response characteristics and a high contrast. A liquid crystal device is constituted by disposing the liquid crystal composition between a pair of electrode plates. The liquid crystal device may preferably be used as a display panel constituting a liquid crystal apparatus providing good display characteristics.Type: GrantFiled: March 27, 1995Date of Patent: December 9, 1997Assignee: Canon Kabushiki KaishaInventors: Yoko Kosaka, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura
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Patent number: 5686480Abstract: A class of fused tricyclic heteroaromatic compounds of formula (I), or a salt thereof or a prodrug thereof containing a fused pyrazole ring are ligands for dopamine receptor subtypes within the body and are therefore of use in the treatment and/or prevention of disorders of the dopamine system, such as schizophrenia.Type: GrantFiled: March 1, 1996Date of Patent: November 11, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Ian James Collins, Paul David Leeson, Michael Rowley
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Patent number: 5677451Abstract: Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are alkyl groups having 2 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N-R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is phenyl or pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub. 2OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR11OR.sub.10 O, where R.sub.5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.Type: GrantFiled: June 6, 1995Date of Patent: October 14, 1997Assignee: AllerganInventor: Roshantha A. S. Chandraratna
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Patent number: 5670526Abstract: 1,3,4-oxadiazole compounds are disclosed. The subject compounds suppress immune function and have hepatoprotection activity.Type: GrantFiled: December 21, 1995Date of Patent: September 23, 1997Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Dharmpal S. Dodd, Takao Nishi
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Patent number: 5670511Abstract: Indolepiperidine derivatives of the formula I ##STR1## and their physiologically acceptable salts exhibit action on the central nervous system, in particular dopamine-agonistic or dopamine-antagonistic action.Type: GrantFiled: January 16, 1996Date of Patent: September 23, 1997Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Joachim Marz, Hartmut Greiner, Christoph Seyfried, Gerd Bartoszyk
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Patent number: 5668150Abstract: Compounds having the formula ##STR1## wherein W and Y are independently selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, and optionally substituted naphthyl with the proviso that W and Y are not simultaneously the same substituent; R.sup.1 and R.sup.2 are independently hydrogen, alkyl, haloalkyl, alkoxy, or halogen; R.sup.3 is hydrogen or alkyl; X is absent or is alkylene, alkenylene, or alkynylene; and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.4 wherein R.sup.4 is hydrogen or alkyl; and (c) --NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from hydrogen, alkyl, hydroxy and alkoxy are disclosed. These compounds inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states.Type: GrantFiled: July 26, 1996Date of Patent: September 16, 1997Assignee: Abbott LaboratoriesInventors: Clint D.W. Brooks, Teodozyj Kolasa, David E. Gunn
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Patent number: 5663349Abstract: Novel processes are disclosed for the preparation and resolution of substituted piperidines of the formula ##STR1## wherein R.sup.1 and R.sup.2 are defined as below, and related compounds, as well as novel intermediates used in such processes.Type: GrantFiled: July 12, 1994Date of Patent: September 2, 1997Assignee: Pfizer IncInventors: Terry J. Rosen, Dennis M. Godek, Sally Gut, Lewin Wint
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5658904Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: June 6, 1995Date of Patent: August 19, 1997Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5659065Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or heteroaromatic radical, a hydroxy group that is aliphatically, araliphatically or heteroarylaliphatically etherified or protected by a hydroxy-protecting group, or an aliphatically etherified mercapto group, andR.sub.2 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical, orR.sub.1 and R.sub.2 together form a divalent aliphatic radical,R.sub.3 is free or aliphatically, araliphatically or aromatically esterified carboxy, formyl or hydroxymethyl,R.sub.4 is hydrogen, an aliphatic or araliphatic radical or an amino-protecting group, andR.sub.5 is hydrogen or an aliphatic radical,and the salts thereof can be used as intermediates in the preparation of medicinal active ingredients.Type: GrantFiled: April 4, 1995Date of Patent: August 19, 1997Assignee: Novartis CorporationInventor: Richard Goschke
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Patent number: 5650514Abstract: The present invention relates to 3-substituted quinoline-5-carboxylic acid derivatives and processes for their preparation.Type: GrantFiled: July 17, 1995Date of Patent: July 22, 1997Assignee: Bayer AktiengesellschaftInventors: Jurgen Stoltefuss, Michael Negele, Karl-Heinz Wahl, Jan-Bernd Lenfers, Samir Samaan
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Patent number: 5646144Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalized carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Ciba-Geigy CorporationInventors: Walter Schilling, Silvio Ofner, Siem J. Veenstra
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Patent number: 5633371Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: September 15, 1995Date of Patent: May 27, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
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Patent number: 5633380Abstract: The invention is substituted quinoline intermediates useful in the synthesis of the herbicide 2-(4-isopropyl-4-methyl 5-oxo 2-imidazolidinyl)-5-methoxymethylnicotinic acid and a process for preparing the herbicide intermediate 3-methoxymethyl-7- or 8-hydroxyquinoline.Type: GrantFiled: June 5, 1995Date of Patent: May 27, 1997Assignee: American Cyanamid CompanyInventor: Wen-Xue Wu
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Patent number: 5620988Abstract: Substituted tetrahydropyridines and hydroxypiperidines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: June 6, 1995Date of Patent: April 15, 1997Assignee: Warner-Lambert CompanyInventors: Shelly Glase, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
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Patent number: 5620989Abstract: The present invention is directed to compounds of the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.Type: GrantFiled: April 13, 1995Date of Patent: April 15, 1997Assignee: Merck Sharp & Dohme LimitedInventors: Timothy Harrison, Angus M. MacLeod, Graeme I. Stevenson, Brian J. Williams
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Patent number: 5612356Abstract: A heterocycle-containing carbonic acid derivative represented by the following general formula (I): ##STR1## or a physiologically acceptable salt thereof which exhibits an excellent preventive and therapeutic effect against various diseases, and an intermediate which is useful for the production of the heterocycle-containing carbonic acid derivative.Type: GrantFiled: April 25, 1995Date of Patent: March 18, 1997Assignee: Eisai Co., Ltd.Inventors: Hiroyuki Yoshimura, Mitsuo Nagai, Shigeki Hibi, Koichi Kikuchi, Ieharu Hishinuma, Junichi Nagakawa, Makoto Asada, Norimasa Miyamoto, Takayuki Hida, Aichi Ogasawara, Isao Yamatsu
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Patent number: 5605896Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.Type: GrantFiled: August 31, 1994Date of Patent: February 25, 1997Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 5597834Abstract: This invention concerns compounds having the Z-configuration of formula: ##STR1## or salts thereof, wherein R represents an optionally substituted aryl or heteroaryl radical, R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, carboxy, hydroxy (C.sub.1 -C.sub.6)alkyl, halogen, halo(C.sub.1 -C.sub.6)alkyl, carboxy(C.sub.1 -C.sub.6)alkyl, optionally substituted aryl or heteroaryl or optionally substituted aralkyl or heteroarylalkyl; n represents O, 1 or 2; R.sup.4 and R.sup.5 each independently represent hydrogen or a substituent selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl or R.sup.4 and R.sup.5 are geminal C.sub.1 -C.sub.6 alkyl substituents and R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl which possess antiinflammatory activity.Type: GrantFiled: December 1, 1994Date of Patent: January 28, 1997Assignee: American Home Products CorporationInventors: Roger Crossley, Albert Opalko
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Patent number: 5591752Abstract: This invention relates to a compound (a quinoline derivative) represented by the formula (I): ##STR1## The quinoline derivative of this invention has a strong leukotriene antagonistic action and is extremely useful as an antiallergic medicine and an anti-inflammatory medicine.Type: GrantFiled: August 16, 1995Date of Patent: January 7, 1997Assignee: Ube Industries, Ltd.Inventors: Tomio Kimura, Yoshio Kaku, Takashi Ikuta, Hiroshi Fujiwara, Hitoshi Ueno, Eiji Okanari
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Patent number: 5589484Abstract: The present invention is concerned with novel quinoline derivatives having anti-Helicobacter activity of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, the stereochemically isomeric forms thereof, the quaternized forms thereof and the N-oxides thereof, wherein --A-- represents a bivalent radical of formula--N.dbd.CH--CH.dbd.CH-- (a),--CH.dbd.N--CH.dbd.CH-- (b),--N.dbd.N--CH.dbd.CH-- (c),--N.dbd.CH--N.dbd.CH-- (d),--N.dbd.CH--CH.dbd.N-- (e),--CH.dbd.N--N.dbd.CH-- (f),--N.dbd.N--N.dbd.CH-- (g),--N.dbd.N--CH.dbd.N-- (h),or--CH.dbd.CH--CH.dbd.CH-- (i);R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently represent hydrogen, halo, hydroxy, C.sub.1-4 alkyloxy, C.sub.1-4 alkyl, trifluoromethyl, amino, mono- or di(C.sub.Type: GrantFiled: April 4, 1995Date of Patent: December 31, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Marc G. Venet, J er ome E. G. Guillemont, Daniel F. J. Vernier, Frank C. Odds
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Patent number: 5587482Abstract: The present invention is directed to a dye suitable for spectral sensitization of a photographic element. Specifically, the dye is a compound having the structure: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each independently represents H; halogen; alkyl of 1-6 carbons; aryl of 6-24 carbons; alkoxy of 1-6 carbons; carbonyl; or sulfonate; or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 taken together represent the atoms necessary to complete a six-membered carbocylic ring;R.sup.5 represents hydrogen, alkyl of 1-6 carbons or aryl of 6-24 carbons;R.sup.6, R.sup.7, and R.sup.8 independently represent alkyl 1-6 carbons; aryl of 6-24 carbons; or any pair of R.sup.6, R.sup.7 and R.sup.8 taken together represent a five- or six-member heterocyclic ring;X represents O, S, CH.dbd.CH, Se, Te or N--R.sup.10 ;Y represents O, S, or N--R.sup.9 ;Z represents O, S or Se;R.sup.9 represents alkyl of 1-6 carbons; or an aryl of 6-24 carbons;R.sup.Type: GrantFiled: March 7, 1996Date of Patent: December 24, 1996Assignee: Sterling Diagnostic Imaging, Inc.Inventors: Dietrich M. Fabricius, Ralf H. Harms, James J. Welter
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Patent number: 5569763Abstract: Hydrazone compound useful as an excellent organic nonlinear optical material and a highly sensitive coloring chelation agent, represented by the following formula (1): ##STR1## wherein Ar is a substituted or an non-substituted 2-imidazolyl group, a 4-imidazolyl group, 3-pyrazolyl group, 3-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 2-quinolyl, 1-isoquinolyl, 3-isoquinolyl, 1-phthalazinyl, 2-quinazolinyl, 2-benzimidazolyl, 2-benzothiazolyl, or 2-thiazolyl group,R.sup.1 is a nitro group, cyano group or trifluoromethyl group,R.sup.2 is a nitro group, cyano group, trifluoromethyl group or a halogen atom, or a substituted or an non-substituted alkyl group,R.sup.3 is a hydrogen atom, andn is an integer from 0 to 3.Type: GrantFiled: March 10, 1995Date of Patent: October 29, 1996Assignee: Kabushiki Kaisha ToshibaInventor: Yoshiaki Kawamonzen
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Patent number: 5565473Abstract: Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: February 23, 1995Date of Patent: October 15, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Michel L. Belley, Serge Leger, Marc Labelle, Patrick Roy, Yi B. Xiang, Daniel Guay
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Patent number: 5563037Abstract: A highly sensitive homogeneous assay allows for quantitative detection of amplified nucleic acids. This detection is achieved during or after amplification with a high affinity fluorescent dye which is from the class of unsymmetrical cyanine dyes having at least two positive charges and a binding constant (K.sub.b) within the range of from about 1.times.10.sup.4 to about 5.times.10.sup.5 (molar.sup.-1). The reagents used for the assay can be contained in a kit designed for amplification such as by polymerase chain reaction.Type: GrantFiled: December 21, 1995Date of Patent: October 8, 1996Assignee: Johnson & Johnson Clinical Diagnostics, Inc.Inventors: John W. H. Sutherland, David R. Patterson
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Patent number: 5545651Abstract: Novel substituted imidazoles of Formula (I), which are useful as angiotensin II antagonists, are disclosed: ##STR1##Type: GrantFiled: November 28, 1994Date of Patent: August 13, 1996Assignee: The DuPont Merck Pharmaceutical CompanyInventors: John J. V. Duncia, Carol L. Ensinger, Richard E. Olson, Mimi L. Quan, Joseph B. Santella, III, Mary K. Vanatten
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Patent number: 5541199Abstract: Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3,or 4; m is one of the integers 0 or 1; R is ##STR2## or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.Type: GrantFiled: June 2, 1995Date of Patent: July 30, 1996Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5541197Abstract: Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.Type: GrantFiled: March 21, 1995Date of Patent: July 30, 1996Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Elizabeth M. Naylor, Ann E. Weber
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Patent number: 5532243Abstract: There are provided nitrogen-containing bicyclic compounds, pharmaceutical compositions containing these compounds and methods of using these compounds to treat physiological or drug-induced psychosis or diskinesia in a mammal.Type: GrantFiled: February 14, 1992Date of Patent: July 2, 1996Assignee: The DuPont Merck Pharmaceutical CompanyInventor: Paul J. Gilligan