| 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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