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公开(公告)号:US4954628A
公开(公告)日:1990-09-04
申请号:US317769
申请日:1989-03-02
Applicant: Gabor Besenyei , Sandor Nemeth , Laszlo Simandi , Maria Belak , Maria Szabo , Jozsef Dukai , Lajos Nagy , Elemer Tomordi , Csaba Soptei , Erzsebet E. Dioszegine
Inventor: Gabor Besenyei , Sandor Nemeth , Laszlo Simandi , Maria Belak , Maria Szabo , Jozsef Dukai , Lajos Nagy , Elemer Tomordi , Csaba Soptei , Erzsebet E. Dioszegine
IPC: C07D251/16 , B01J27/13 , B01J31/16 , C07B61/00 , C07C311/60 , C07D213/75 , C07D239/42 , C07D251/18 , C07D251/22 , C07D251/46 , C07D333/34 , C07D521/00
CPC classification number: C07D521/00 , C07C311/60
Abstract: The invention relates to a process for preparing sulphonyl-ureas of the general formula (I) ##STR1## wherein Ar.sub.1 represents a phenyl, naphthyl or thienyl group, the derivatives thereof substituted by C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, (halo)alkoxycarbonyl, (halo)alkyloxy, nitro, cyano groups as well as by halogen atoms,Ar.sub.2 represents a phenyl, pyridyl, pirimidinyl or triazinyl group and the derivatives thereof substituted by C.sub.1-4 (halo)alkyl, C.sub.1-4 (halo)alkyloxy, amino, O-acyl, O-arylsulphonyl, O-(substituted carbamoyl) groups as well as by halogen atoms.According to the invention N-halogen aryl sulphonamidate is reacted in the presence of a carbonylating catalyst, carbon monoxide and an aromatic amine, optionally in the presence of a phase transfer catalyst, or N-halogen aryl sulphonamidate is reacted with carbon monoxide in the presence of a carbonylating catalyst, and optionally in the presence of a phase transfer catalyst, then the obtained reaction mixture is further reacted with an aromatic amine or an N-halogen-arylamine-alkali metal salt is reacted with aryl-sulphonamid in the presence of a carbonylating catalyst, carbon monoxide and optionally in the presence of a phase transfer catalyst or an amine, amine dihalogenid, aryl sulphonamid are reacted in the presence of a carbonylating catalyst and carbon monoxide and the obtained reaction mixture is worked up in a known manner.The thus prepared sulphonyl-ureas are biologically active compounds, which are used in the pharmaceutical industry and for regulating plant growth.
Abstract translation: 本发明涉及一种制备通式(I)的磺酰脲的方法,其中Ar 1表示苯基,萘基或噻吩基,其衍生物被C 1-4烷基,C 1-4卤代烷基, (卤代)烷氧基羰基,(卤代)烷氧基,硝基,氰基以及卤素原子,Ar 2表示苯基,吡啶基,吡啶基或三嗪基,其衍生物被C 1-4(卤代)烷基, 卤代)烷氧基,氨基,O-酰基,O-芳基磺酰基,O-(取代的氨基甲酰基)基团以及卤素原子。 根据本发明,N-卤素芳基磺酰胺酸酯在羰基化催化剂,一氧化碳和芳族胺的存在下,任选地在相转移催化剂存在下反应,或N-卤素芳基磺酰胺盐与一氧化碳在存在下反应 的羰基化催化剂,并且任选地在相转移催化剂存在下,然后将所得反应混合物进一步与芳族胺反应或N-卤素 - 芳基胺 - 碱金属盐在芳基 - 磺酰胺存在下与 羰基化催化剂,一氧化碳和任选在相转移催化剂或胺,胺二卤代芳基磺酰胺存在下,在羰基化催化剂和一氧化碳的存在下反应,并将所得反应混合物以已知方式处理。 如此制备的磺酰脲是生物活性化合物,其用于制药工业和调节植物生长。
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公开(公告)号:US5218117A
公开(公告)日:1993-06-08
申请号:US951448
申请日:1992-09-25
Applicant: Kalman Takacs , Iloma Kiss nee Ajzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter Szekely Kormoczy , Maria Szabo , Judit Szeredy , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
Inventor: Kalman Takacs , Iloma Kiss nee Ajzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter Szekely Kormoczy , Maria Szabo , Judit Szeredy , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
IPC: C07D217/16
CPC classification number: C07D217/16
Abstract: The invention relates to novel compounds of the general formula (I), ##STR1## The compounds of the invention antagonize the effects of constrictive mediators, e.g. histamine, acetylcholine or serotonin; they show an antiallergic action and possess an antiinflammatory effect. Thus, these compounds can therapeutically be used as bronchodilators as well as antiallergic or antiinflammatory drugs, particularly in the treatment of bronchial asthma.
Abstract translation: 本发明涉及通式(I)的新化合物,(I)本发明的化合物拮抗收缩性介质的作用,例如, 组胺,乙酰胆碱或5-羟色胺; 它们显示抗过敏作用并具有抗炎作用。 因此,这些化合物可以治疗性地用作支气管扩张剂以及抗过敏药或抗炎药,特别是用于治疗支气管哮喘。
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公开(公告)号:US5179089A
公开(公告)日:1993-01-12
申请号:US792255
申请日:1991-11-14
Applicant: Kalman Takacs , Iloma Kiss neAjzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter S. Kormoczy , Maria Szabo , Judit Szeredy nee Varga , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
Inventor: Kalman Takacs , Iloma Kiss neAjzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter S. Kormoczy , Maria Szabo , Judit Szeredy nee Varga , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
IPC: A61K31/47 , A61K31/33 , A61K31/472 , A61K31/4725 , A61P11/08 , A61P29/00 , A61P37/08 , C07D217/12 , C07D217/16 , C07D217/26
CPC classification number: C07D217/16
Abstract: The invention relates to novel compounds of the general formula (I), ##STR1## wherein R means hydrogen or a straight or branched chain C.sub.1-6 alkoxy group;R.sup.1 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group;R.sup.2 represents hydrogen or a straight or branched chain C.sub.1-6 alkyl group;R.sup.3 means hydrogen, a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group;R.sup.4 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group; orR.sup.3 and R.sup.4 together with the nitrogen atom, to which they are attached form a 4 to 8-membered cyclic group of formula ##STR2## optionally substituted by one or two straight or branched chain C.sub.1-4 alkoxy and/or one or two straight or branched chain C.sub.1-4 alkyl group(s), where optionally an oxygen or sulfur atom or an N-R.sup.5 group may be substituted for a ring carbon atom, where R.sup.5 means hydrogen or a straight or branched chain C.sub.1-6 aliphatic alkyl group, the 4- to 8-membered cycle optionally being condensed with a benzene ring;R.sup.6 stands for hydrogen or a C.sub.1-10 acyl group and the salts and hydrates thereof as well as pharmaceutical compositions containing these compounds.The compounds of the invention antagonize the effects of constrictive mediators, e.g. histamine, acetylcholine or serotonin; they show an antiallergic action and possess an antiinflammatory effect. Thus, these compounds can therapeutically be used as bronchodilators as well as antiallergic or antiinflammatory drugs, particularly in the treatment of bronchial asthma.
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