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1.发明授权1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl]-.alpha.,.alpha.-diarylpyrrolidine, piperidine and homopiperidineacetamides and acetonitriles 失效1 - [（氨基烷基和氨基烷基氨基）羰基和硫代羰基]-α，α-二芳基吡咯烷，哌啶和高哌啶乙酰胺和乙腈
公开(公告)号：US4594343A
公开(公告)日：1986-06-10
申请号：US662583
申请日：1984-10-19
IPC分类号： C07D211/36 , A61K31/4427 , A61K31/445 , A61K31/451 , A61K31/55 , A61P9/06 , C07D207/08 , C07D211/34 , C07D211/42 , C07D211/46 , C07D211/94 , C07D211/96 , C07D223/04 , C07D401/06 , C07D223/06 , A61K31/40 , C07D207/06 , C07D211/08
CPC分类号： C07D207/08 , C07D211/34 , C07D211/42 , C07D223/04 , Y10S514/821
摘要： Novel 1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl]-.alpha.,.alpha.-diaryl-pyrrolidine, piperidine and homopiperidineacetamides and acetonitriles having the formula: ##STR1## wherein; n is zero, one or two;X is oxygen or sulfur;Z is ##STR2## p is 0 to 5 inclusive with the proviso that when Z is ##STR3## p is at least one; Y is aminocarbonyl or cyano;Ar.sup.1 and Ar.sup.2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl;R is hydrogen or loweralkyl;R.sup.1, R.sup.2 and R.sup.3 are hydrogen, cycloalkyl, loweralkyl, phenyl, substituted phenyl, phenylloweralkyl, and R.sup.2 and R.sup.3 taken with the adjacent nitrogen may form a heterocyclic residue, and diastereoisomers when possible and pharmaceutical salts; and the method and pharmaceutical compositions for treating cardiac arrhythmias therewith are disclosed.
摘要翻译： 新颖的1 - [（氨基烷基和氨基烷基氨基）羰基和硫代羰基]-α，α-二芳基 - 吡咯烷，哌啶和高哌啶乙酰胺和具有下式的乙腈：其中; n为零，一或二; X是氧或硫; Z是
p为0至5，其条件是当Z为 p至少为1时; Y是氨基羰基或氰基; Ar1和Ar2是2,3或4-吡啶基，苯基或取代的苯基; R是氢或低级烷基; R 1，R 2和R 3是氢，环烷基，低级烷基，苯基，取代的苯基，苯基低级烷基，与相邻的氮取代的R 2和R 3可以形成杂环残基，当可能时可以形成非对映异构体和药用盐; 并公开了用于治疗心律失常的方法和药物组合物。 -
2.发明授权1-(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl)-.alpha.,.alpha . 失效1-（氨基烷基和氨基烷基氨基）羰基和硫代羰基）-α，α二芳基吡咯烷，哌啶和高哌啶乙酰胺和乙腈
公开(公告)号：US4812451A
公开(公告)日：1989-03-14
申请号：US845148
申请日：1986-03-27
IPC分类号： C07D207/08 , C07D211/34 , C07D211/42 , C07D223/04 , A61K31/445
CPC分类号： C07D207/08 , C07D211/34 , C07D211/42 , C07D223/04
摘要： Novel 1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl-.alpha.,.alpha.-diaryl-pyrrolidine, piperidine and homopiperidineacetamides and acetonitriles having the formula: ##STR1## wherein; n is zero, one or two;X is oxygen or sulfur;Z is ##STR2## 10 or --(CH.sub.2); p is 0 to 5 inclusive with the proviso that when Z is ##STR3## p is at least one; Y is aminocarbonyl or cyano;Ar.sup.1 and Ar.sup.2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl;R is hydrogen or loweralkyl;R.sup.1, R.sup.2 and R.sup.3 are hydrogen, cycloalkyl, loweralkyl, phenyl, substituted phenyl, phenylloweralkyl, and R.sup.2 and R.sup.3 taken with the adjacent nitrogen may form a heterocyclic residue, and diastereoisomers when possible and pharmaceutical salts; and the method and pharmaceutical compositions for treating cardiac arrhythmias therewith are disclosed.
摘要翻译： 新颖的1- [（氨基烷基和氨基烷基氨基）羰基和硫代羰基-α，α-二芳基 - 吡咯烷，哌啶和高哌啶乙酰胺和具有下式的丙酮：其中; n为零，一或二; X是氧或硫; Z为10或 - （CH2）; p为0至5，其条件是当Z为至少1时; Y是氨基羰基或氰基; Ar1和Ar2是2,3或4-吡啶基，苯基或取代的苯基; R是氢或低级烷基; R 1，R 2和R 3是氢，环烷基，低级烷基，苯基，取代的苯基，苯基低级烷基，与相邻的氮取代的R 2和R 3可以形成杂环残基，当可能时可以形成非对映异构体和药用盐; 并公开了用于治疗心律失常的方法和药物组合物。
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3.发明授权1-((aminoalkyl and aminoalkylamino) carbonyl and thiocarbonyl)-.alpha.,.alpha.-diarylpyrrolidine, piperidine and homopiperidineacetamides and acetonitriles 失效1 - （（氨基烷基和氨基烷基氨基）羰基和硫代羰基）-α，α-二芳基吡咯烷，哌啶和高哌啶乙酰胺和乙腈
公开(公告)号：US4812452A
公开(公告)日：1989-03-14
申请号：US845170
申请日：1986-03-27
IPC分类号： C07D207/08 , C07D211/34 , C07D211/42 , C07D223/04 , A61K31/445
CPC分类号： C07D207/08 , C07D211/34 , C07D211/42 , C07D223/04
摘要： Novel 1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl]-.alpha.,.alpha.-diaryl-pyrrolidine, piperidine and homopiperidineacetamides and acetonitriles having the formula: ##STR1## wherein; n is zero, one or two;X is oxygen or sulfur;Z is ##STR2## or --(CH.sub.2); p is 0 to 5 inclusive with the proviso that when Z is ##STR3## p is at least one; Y is aminocarbonyl or cyano;Ar.sup.1 and Ar.sup.2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl;R is hydrogen or loweralkyl;R.sup.1, R.sup.2 and R.sup.3 are hydrogen, cycloalkyl, loweralkyl, phenyl, substituted phenyl, phenylloweralkyl, and R.sup.2 and R.sup.3 taken with the adjacent nitrogen may form a heterocyclic residue, and diastereoisomers when possible and pharmaceutical salts; and the method and pharmaceutical compositions for treating cardiac arrhythmias therewith are disclosed.
摘要翻译： 新颖的1 - [（氨基烷基和氨基烷基氨基）羰基和硫代羰基]-α，α-二芳基 - 吡咯烷，哌啶和高哌啶乙酰胺和具有下式的乙腈：其中; n为零，一或二; X是氧或硫; Z是
或 - （CH2）; p为0至5，其条件是当Z为至少1时; Y是氨基羰基或氰基; Ar1和Ar2是2,3或4-吡啶基，苯基或取代的苯基; R是氢或低级烷基; R 1，R 2和R 3是氢，环烷基，低级烷基，苯基，取代的苯基，苯基低级烷基，与相邻的氮取代的R 2和R 3可以形成杂环残基，当可能时可以形成非对映异构体和药用盐; 并公开了用于治疗心律失常的方法和药物组合物。 -
4.发明授权1-((aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl)-alpha, alpha-diarylpyrrolidine, piperidine and homopiperidineacetamides and acetonitriles 失效1 - （（氨基烷基和氨基烷基氨基）羰基和硫代羰基）-α，α-二芳基吡咯烷，哌啶和高哌啶乙酰胺和乙腈
公开(公告)号：US4810703A
公开(公告)日：1989-03-07
申请号：US882743
申请日：1986-07-07
IPC分类号： C07D207/08 , C07D211/34 , C07D211/42 , C07D223/04 , A61K31/445
CPC分类号： C07D207/08 , C07D211/34 , C07D211/42 , C07D223/04
摘要： Novel 1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl-.alpha.,.alpha.-diaryl-pyrrolidine, piperidine and homopiperidineacetamides and acetonitriles having the formula: ##STR1## wherein; n is zero, one or two;X is oxygen or sulfur;Z is ##STR2## or --(CH.sub.2); p is 0 to 5 inclusive with the proviso that when Z is ##STR3## p is at least one; Y is aminocarbonyl or cyano;Ar.sup.1 and Ar.sup.2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl;R is hydrogen or loweralkyl;R.sup.1, R.sup.2 and R.sup.3 are hydrogen, cycloalkyl, loweralkyl, phenyl, substituted phenyl, phenylloweralkyl, and R.sup.2 and R.sup.3 taken with the adjacent nitrogen may form a heterocyclic residue, and diastereoisomers when possible and pharmaceutical salts; and the method and pharmaceutical compositions for treating cardiac arrhythmias therewith are disclosed.
摘要翻译： 新颖的1- [（氨基烷基和氨基烷基氨基）羰基和硫代羰基-α，α-二芳基 - 吡咯烷，哌啶和高哌啶乙酰胺和具有下式的丙酮：其中; n为零，一或二; X是氧或硫; Z是
或 - （CH2）; p为0至5，其条件是当Z为至少1时; Y是氨基羰基或氰基; Ar1和Ar2是2,3或4-吡啶基，苯基或取代的苯基; R是氢或低级烷基; R 1，R 2和R 3是氢，环烷基，低级烷基，苯基，取代的苯基，苯基低级烷基，与相邻的氮取代的R 2和R 3可以形成杂环残基，当可能时可以形成非对映异构体和药用盐; 并公开了用于治疗心律失常的方法和药物组合物。 -
5.发明授权N-aminoalkyl-S-aryl-S-alkyl (or substituted alkyl) sulfoximines as antiarrhythmic agents 失效N-氨基烷基-S-芳基-S-烷基（或取代的烷基）亚磺酰亚胺作为抗心律不齐药
公开(公告)号：US5140026A
公开(公告)日：1992-08-18
申请号：US697825
申请日：1991-05-09
IPC分类号： C07C381/10 , C07D295/13 , C07D333/34 , C07D521/00
CPC分类号： C07D295/13 , C07C381/10 , C07D231/12 , C07D233/56 , C07D249/08 , C07D333/34
摘要： Compounds of this invention are represented by the formula: ##STR1## wherein Z is a C.sub.1 -C.sub.6 alkylene group and R is an alkyl or substituted alkyl group. Class III antiarrhythmic activity is determined in vitro using an electrophysiological test where prolongation of the action potential duration is an indication of activity.
摘要翻译： 本发明的化合物由下式表示：其中Z是C1-C6亚烷基，R是烷基或取代的烷基。 使用电生理测试在体外测定III类抗心律失常活性，其中动作电位持续时间的延长是活动的指示。
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公开(公告)号：US5187189A
公开(公告)日：1993-02-16
申请号：US643364
申请日：1991-01-22
IPC分类号： C07C381/10 , C07D295/088
CPC分类号： C07D295/088 , C07C381/10
摘要： This invention discloses novel sulfoximines having the formula: ##STR1## where Z is C.sub.1 -C.sub.6 alkylene and Y is alkyl, arylalkyl, acyl, carbamoyl, sulfonyl or alkoxycarbonyl. The invention compounds are useful in the treatment of Class II arrhythmia.
摘要翻译： 本发明公开了具有下式的新型磺酰亚胺：其中Z为C1-C6亚烷基，Y为烷基，芳基烷基，酰基，氨基甲酰基，磺酰基或烷氧基羰基。 本发明化合物可用于治疗II级心律失常。
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7.发明授权Aryloxymethyl derivatives of nitrogenous heterocyclic methanols and ethers thereof 失效含氮杂环甲醇的芳氧基甲基衍生物及其醚
公开(公告)号：US4835164A
公开(公告)日：1989-05-30
申请号：US16779
申请日：1987-02-20
IPC分类号： A61K31/40 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/443 , A61K31/445 , A61K31/451 , A61K31/55 , A61P9/06 , A61P9/12 , C07D207/08 , C07D211/22 , C07D213/30 , C07D223/04 , C07D405/12 , C07D498/04
CPC分类号： C07D207/08 , C07D211/22 , C07D213/30 , C07D223/04
摘要： Novel heterocyclicmethanols are disclosed having the formula: ##STR1## wherein Z is pyrrolidinyl, piperidinyl, homopiperidinyl or pyridinyl; R.sup.1 is hydrogen, loweralkyl or carbethoxymethyl;R.sup.2 is hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl;R.sup.3 is 1 or 2-naphthalenyl, 2,3-dihydroinden-4 or 5-yl, phenyl or phenyl substituted by loweralkyl, loweralkoxy, halogen, trifluoromethyl, phenyl, methylenedioxy, nitro, amino, loweralkylamino, diloweralkylamino, loweracylamino;the 1-position of 2-pyrrolidinyl, 2-piperidinyl or 2-homopiperidinyl may be substituted by an R.sup.4 loweralkyl group, or R.sup.1 may form methylene or --CH.sub.2 -C(O)-bridges with R.sup.4 ;the pharmaceutically acceptable salts and diastereomers thereof, which compounds have antiarrhythmic and/or hypotensive activity in animals.
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公开(公告)号：US4558155A
公开(公告)日：1985-12-10
申请号：US670795
申请日：1984-11-13
IPC分类号： C07C43/225 , C07C275/14 , C07C335/08 , C07D209/48 , C07D295/13 , C07C157/09
CPC分类号： C07D209/48 , C07C275/14 , C07C335/08 , C07C43/225 , C07D295/13
摘要： N-(Aryloxyalkyl)-N'-(aminoalkyl)ureas and thioureas having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen, loweralkyl, cycloalkyl, phenyl or phenyllower alkyl, and R.sup.3 and R.sup.4 are hydrogen, loweralkyl, phenyl and phenylalkyl or R.sup.3 and R.sup.4 taken together with the adjacent nitrogen form a heterocyclic residue are disclosed in a method of suppressing cardiac arrhythmias.
摘要翻译： 具有下式的N-（芳氧基烷基）-N' - （氨基烷基）脲和硫脲其中R1和R2是氢，低级烷基，环烷基，苯基或苯基低级烷基，R3和R4是氢，低级烷基，苯基和苯基烷基 或R 3和R 4与相邻的氮一起形成杂环残基，在抑制心律失常的方法中公开。
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公开(公告)号：US6071862A
公开(公告)日：2000-06-06
申请号：US329433
申请日：1999-06-10
IPC分类号： C10M159/12
CPC分类号： C10M159/12 , C10M2205/00 , C10M2205/02 , C10M2205/026 , C10M2205/04 , C10M2207/10 , C10M2207/129 , C10M2207/34 , C10M2209/084 , C10M2209/086 , C10M2215/04 , C10M2215/042 , C10M2215/22 , C10M2215/221 , C10M2215/225 , C10M2215/226 , C10M2215/26 , C10M2215/30 , C10M2217/046 , C10M2217/06 , C10M2227/00 , C10N2240/10 , C10N2240/101 , C10N2240/104 , C10N2240/106
摘要： A composition, comprising from about 20% to about 80% by weight of a diluent, prepared by reacting a mixture comprising(A) an esterified carboxy-containing interpolymer, said interpolymer being derived from at least two monomers, (i) one of said monomers being at least one of an aliphatic olefin containing from 2 to about 30 carbon atoms and a vinyl aromatic monomer and (ii) the other of said monomers being at least one alpha, beta-unsaturated acylating agent, and having, before esterification, M.sub.n determined by gel permeation chromatography ranging from about 8,000 to about 350,000, wherein from about 80% to about 99% of the carboxylic groups of said intelpolymer are esterified, wherein from about 80 to about 100% of the ester groups contain from 8 to about 23 carbon atoms and from 0 to about 20% of the ester groups contain from 2 to 7 carbon atoms, and(B) a hydrocarbyl substituted carboxylic acid or functional derivative thereof wherein the hydrocarbyl group comprises from about 10 to about 400 carbon atoms, with(C) an amine having an average of more than 1 condensable N--H groups, wherein from about 0 to about 95% of the diluent is present during the reacting and the product obtained from said reacting is further combined with additional diluent such that the total diluent comprises from about 20% to about 80% by weight of the total weight of the composition. Depending upon the relative amounts of reactant (A) and (B) used, a composition which acts primarily as a viscosity improver with dispersant properties (DVM) or primarily as a dispersant with viscosity improving properties (VMD)may be prepared or compositions with properties intermediate between these.
摘要翻译： 一种组合物，其包含约20％至约80％重量的稀释剂，其通过使包含（A）含酯化羧基的互聚物，所述互聚物衍生自至少两种单体的混合物，（i）所述 单体是含有2至约30个碳原子的脂族烯烃和乙烯基芳族单体中的至少一种，和（ii）所述单体中的另一种是至少一种α，β-不饱和酰化剂，并且在酯化前具有+ E，ovs M + EE n通过约8,000至约350,000的凝胶渗透色谱测定，其中约80％至约99％的所述智力聚合物的羧基被酯化，其中约80至约100％的酯 基团含有8至约23个碳原子，0至约20％的酯基含有2至7个碳原子，和（B）烃基取代的羧酸或其官能衍生物，其中烃基包括 （C）具有平均多于1个可冷凝NH基团的胺，其中在反应期间存在约0至约95％的稀释剂，并且从所述反应获得的产物为 进一步与额外的稀释剂组合，使得总稀释剂占组合物总重量的约20重量％至约80重量％。 取决于所用的反应物（A）和（B）的相对量，可以制备主要作为粘度改进剂的分散剂性能（DVM）或主要作为具有粘度改进性能（VMD）的分散剂的组合物或具有性质的组合物 这些之间的中间。
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10.发明授权4-substituted-3-1H-imidazol-1-,2,5-thiadiazoles as antiarrhythmic agents 失效4-取代的3-1H-咪唑-1-基，2,5-噻二唑作为抗心律失常药
公开(公告)号：US5051420A
公开(公告)日：1991-09-24
申请号：US664306
申请日：1991-03-04
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D417/14
摘要： Invention compounds of the formula: ##STR1## wherein Z is ##STR2## are novel. Compounds of the above formula have shown antiarrhythmic activity in an electrophysiological assay.
摘要翻译： 下式的发明化合物：其中Z是
是新颖的。 上述式的化合物在电生理测定中显示出抗心律失常活性。
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