序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
101 Substituted azolone derivatives US491960 1995-07-18 US5650411A 1997-07-22 Jan Heeres; Joseph Hector Mostmans; Luc Alfons Leo Van Der Eycken; Frank Christopher Odds; Raymond Antoine Stokbroekx; Marcel Jozef Maria Van der Aa
The use for the manufacture of a medicament for treating Helicobacter-related diseases of a compound of formula ##STR1## a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, whereinX and Y each independently are CH or N;R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl;R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy;Z is C.dbd.O or CHOH; andAr is phenyl optionally substituted with up to three substituents selected from hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, halo, trifluoromethyl, triC.sub.1-4 alkylsilyloxy, nitro, amino and cyano or pyridinyl substituted with hydroxy or C.sub.1-4 alkyloxy; and--A-- is a radical of formula ##STR2##
102 Fungicidal 2-imidazolin-5-ones and 2-imidazoline-5-thiones US462849 1995-06-05 US5637729A 1997-06-10 Guy Lacroix; Raymond Peignier; Regis Pepin
Fungicidal 2-imidazolin-5-ones and 2-imidazoline-5-thiones, processes for their preparation, fungicidal compositions containing them and methods of using them to treat or prevent fungal disease in crops.
103 Acyl derivatives of azolones US448082 1995-05-23 US5637592A 1997-06-10 Jan Heeres; Raymond A. Stokbroekx; Joseph H. Mostmans; Louis J. E. Van der Veken
The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifiuoromethyl, trifiuoromethyloxy or difluoromethyloxy; R.sup.6 is hydrogen; or R.sup.6 is phenyl optionally substituted with halo; pyridinyl; furanyl; thienyl; 3-chloro-benzo[b]thien-2-yl; trifiuoromethyl; C.sub.1-4 alkyloxycarbonyl; dihalophenylcyclopropanyl; C.sub.3-6 cycloalkyl; adamantyl; C.sub.2-6 alkenyl optionally substituted with halophenyl; or C.sub.1-4 alkyl optionally substituted with halo, phenyl, halophenyl, dihalophenyl, phenyloxy, piperidinyl, pyrrolidinyl, piperazinyl, C.sub.1-4 alkylpiperazinyl, C.sub.1-4 alkylcarbonylpiperazinyl, C.sub.1-4 alkyloxycarbonylpiperazinyl, phthalimino, amino, mono- or di(C.sub.1-20)alkylamino or C.sub.3-6 cycloalkylamino; Z is C.dbd.O or CHOH; and ##STR2## is a radical of formula ##STR3## Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a medicine.
104 Fused benzeneoxyacetic acid derivatives which have PGI.sub.2 receptor agonist activity US334395 1994-11-03 US5589496A 1996-12-31 Nobuyuki Hamanaka; Kanji Takahashi; Hidekado Tokumoto
A fused benzeneoxyacetic acid derivative of the formula (I): ##STR1## where the substituents are defined in the specification and salts thereof possess an agonistic on PGI.sub.2 receptor, so it is useful for prevention and/or treatment of thrombosis, arteriosclerosis, inchemic heart diseases, gastric alcer and hypertension.
105 Methods for preparing n-substituted heterocyclic derivatives US269101 1994-06-30 US5559233A 1996-09-24 Claude Bernhart; Jean-Claude Breliere; Jacques Clement; Dino Nisato; Pierre Perreault; Claude Muneaux; Yvette Muneaux
The invention relates to processes for preparing N-substituted heterocyclic compounds of formula (I) ##STR1##
106 Cyclic urea derivatives and pharmaceutical compositions containing these compounds US144909 1993-10-28 US5478942A 1995-12-26 Frank Himmelsbach; Helmut Pieper; Volkhard Austel; Guenter Linz; Thomas Mueller; Johannes Weisenberger; Wolfgang Eisert
The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.
107 Process for the production of 2-substituted 5-chlorimidazole-4-carbaldehydes US208955 1994-03-11 US5442075A 1995-08-15 Gareth Griffiths; Rene Imwinkelried; Jacques Gosteli
A process for the production of 2-substituted 5-chlorimidazole-4-carbaldehydes of the general formula: ##STR1## wherein R is hydrogen, an alkyl group, and alkenyl group, a cycloalkyl group, a benzyl group, a phenyl group or an aryl group. These compounds form important intermediate products for the production of antihypertensive pharmaceutical agents or herbicidal compounds.
108 2-(1-substituted-2-imidazolin-2-yl)benzoic and nicotinic acids and a method for their preparation US009160 1993-01-26 US5354727A 1994-10-11 Michael A. Guaciaro
2-(1-Substituted-2-imidazolin-2-yl)benzoic and nicotinic acids, and derivatives thereof, which are effective in the control of undesirable plant species are described, Also described are a method for the herbicidal use of the compounds and a method for their preparation.
109 N-substituted heterocyclic derivatives US79866 1993-06-23 US5352788A 1994-10-04 Claude Bernhart; Jean-Claude Breliere; Jacques Clement; Dino Nisato; Pierre Perreault; Claude Muneaux; Yvette Muneaux
The invention relates to processes for preparing N-substituted heterocyclic compounds of formula (I) ##STR1## wherein the substituents are as described in the specification, and to intermediates. The compounds are useful for antagonizing angiotensin II.
110 Functionalized imidazolinone haptens and protein conjugates thereof useful in assays for the detection of imidazolinone herbicides US23231 1993-02-25 US5342771A 1994-08-30 Rosie B. Wong; Zareen Ahmed; Milon W. Bullock
This invention provides enzyme conjugates, antigens, antibodies and diagnostic test kits used in an enzyme-linked immunosorbent assay method for determining the presence and concentration of imidazolinone compounds.
111 Imidazoles for the treatment of atherosclerosis US940372 1992-09-03 US5318984A 1994-06-07 Jeffrey T. Billheimer; Peter J. Gillies; C. Anne Higley; Thomas P. Maduskuie, Jr.; Ruth R. Wexler
Disclosed are compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are selected independently from H, C.sub.1 -C.sub.8 unbranched alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 araalkyl, 2-, 3- or 4-pyridinyl, 2-thienyl, 2-furanyl, phenyl optionally substituted with 1 to 3 groups selected from F, Cl, Br, OH, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, CH.sub.3 S(O).sub.r, NO.sub.2, CF.sub.3, or NR.sup.7 R.sup.8 ; or ##STR2## where L is O, O(CH.sub.2).sub.m+1 O, or (CH.sub.2).sub.m where m is 0-4; R.sup.3 is H, C.sub.1 -C.sub.6 alkyl, allyl, benzyl, or phenyl optionally substituted with F, Cl, CH.sub.3, CH.sub.3 O, or CF.sub.3 ;R.sup.4 is straight chain C.sub.1 -C.sub.8 alkyl optionally substituted with F; C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; C.sub.3 --C.sub.6 alkenyl or alkynyl, C.sub.1 -C.sub.3 perfluoroalkyl, phenyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.1 -C.sub.4 alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8 or NCOR.sup.7 ; pentafluorophenyl, benzyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, pyrimidinyl, or biphenyl;R.sup.5 is H, C.sub.1 -C.sub.6 alkyl, or benzyl;R.sup.6 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.8 alkenyl or alkynyl, phenyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; pentafluorophenyl, benzyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ;R.sup.7 and R.sup.8 are selected independently from H or C.sub.1 -C.sub.4 alkyl;X is S(O).sub.r, O, NR.sup.5, CH.sub.2 ;A is C.sub.2 -C.sub.10 alkyl, C.sub.3 -C.sub.10 branched alkyl, C.sub.3 -C.sub.10 alkenyl, or C.sub.3 -C.sub.10 alkynyl;Y is O, S, H.sub.2, or NH;Z is NHR.sup.4, OR.sup.4, or R.sup.4 ;r is 0-2,or a pharmaceutically acceptable salt thereof and their use as antihypercholesterolemic agents or antiatherosclerotic agents.
112 Benzenesulfonyl carboxamide compounds intermediate compounds and method of preparation thereof and use of said compounds and intermediate compounds as herbicidal agents US856262 1992-03-23 US5252539A 1993-10-12 Sergio I. Alvarado; Alvin D. Crews, Jr.; Peter J. Wepplo; Robert F. Doehner, Jr.; Thomas E. Brady; David M. Gange; Desiree L. Little
There are provided novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl-2-imidazolin-5-one compounds, novel intermediates and methods for the preparation of said compounds, and a method for controlling a variety of annual and perennial plant species utilizing novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl 2-imidazolin-5-one compounds.
113 N-substituted imidazol-2-one compounds for treatment of circulatory disorders US828546 1992-01-28 US5238952A 1993-08-24 David B. Reitz; Robert E. Manning
A class of N-substituted imidazol-2-one compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R.sup.0 is selected from hydrido, methyl, fluoro, chloro, monofluoromethyl, difluoromethyl, trifluoromethyl, formyl, carboxyl and dimethoxymethyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.8, R.sup.10 and R.sup.11 is hydrido; with the proviso that at least one of R.sup.5 and R.sup.9 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3 OH, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
114 Heterocyclic acetylenic amines having central nervous system activity US923107 1992-07-30 US5225567A 1993-07-06 Malcolm W. Moon; Richard F. Heier
Heterocyclic acetylenic amine compounds having the following structural formula ##STR1## where X is ##STR2## having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of the parasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.
115 Acyl amidine and acyl, guanidine substituted biphenyl derivatives US735398 1991-07-24 US5177097A 1993-01-05 Michael A. Poss
Novel compounds are disclosed having the formula ##STR1## and wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
116 Angiotensin II receptor blocking imidazoles US279194 1988-12-06 US5138069A 1992-08-11 David J. Carini; John J. V. Duncia; Pancras C. B. Wong
Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.
117 Treatment of congestive heart failure with angiotensin 11 receptor blocking imidazoles US435869 1989-11-13 US5128355A 1992-07-07 David J. Carini; John J. V. Duncia
Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.
118 Benzenesulfonyl carboxamide compounds and intermediate compounds US611626 1990-11-13 US5120854A 1992-06-09 Sergio I. Alvarado; Alvin D. Crews, Jr.; Peter J. Wepplo; Robert F. Doehner, Jr.; Thomas E. Brady; David M. Gange; Desiree L. Little
There are provided novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl-2-imidazolin-5-one compounds, novel intermediates and methods for the preparation of said compounds, and a method for controlling a variety of annual and perennial plant species utilizing novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl 2-imidazolin-5-one compounds.
119 Phenoxyalkyl-substituted heteroaromatics and a method for controlling pests US379956 1989-07-14 US5013847A 1991-05-07 Joachim Leyendecker; Hans-Juergen Neubauer; Uwe Kardorff; Christoph Kuenast; Wolfgang Krieg; Peter Hofmeister
Phenoxyalkyl-substituted heteroaromatics of the formulae Ia and Ib ##STR1## where the substituents have the following meanings: R.sup.1 C.sub.1 -C.sub.12 -alkyl, C.sub.2 -C.sub.12 -alkenyl, C.sub.2 -C.sub.12 -alkynyl, C.sub.1 -C.sub.12 -haloalkyl, C.sub.2 -C.sub.12 -haloalkenyl, C.sub.2 -C.sub.12 -haloalkynyl, C.sub.3 -C.sub.12 -alkoxyalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.4 -C.sub.12 -cycloalkylalkyl, C.sub.3 -C.sub.8 -halocycloalkyl, C.sub.4 -C.sub.12 -halocycloalkylalkyl, C.sub.4 -C.sub.12 -cycloalkylhaloalkyl or C.sub.4 -C.sub.12 -halocycloalkylhaloalkyl;Z hydrogen, halogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.3 -C.sub.10 -cycloalkyl, nitro or cyano in the case of Ia and hydrogen, halogen, or C.sub.1 -C.sub.4 -alkyl in the case of Ib;X O, S, SO.sub.2 ;Q.sub.a substituted or unsubstituted azole;Q.sub.b substituted or unsubstituted heteroaromatic;methods of manufacturing compounds Ia and Ib, and their use for combating pests.
120 Phenylsulfonyl 2-imidazolin-5-one compounds US417400 1989-10-05 US4992094A 1991-02-12 Sergio I. Alvarado; Alvin D. Crews, Jr.; Peter J. Wepplo; Robert F. Doehner, Jr.; Thomas E. Brady; David M. Gange; Desiree L. Little
There are provided novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl-2-imidazolin-5-one compounds, novel intermediates and methods for the preparation of said compounds, and a method for controlling a variety of annual and perennial plant species utilizing novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl 2-imidazolin-5-one compounds.
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