专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4792570A 3- and 4-biphenyloxyaminoalkanes and related compounds as anti-inflammatory and analgetic agents 失效
标题翻译： 3-和4-联苯氧基氨基烷烃和相关化合物作为抗炎和止痛剂
公开(公告)号：US4792570A
公开(公告)日：1988-12-20
申请号：US597790
申请日：1984-04-06
申请人： Peter H. Nelson , James P. Dunn , Stefan H. Unger , Thomas R. Thieme
发明人： Peter H. Nelson , James P. Dunn , Stefan H. Unger , Thomas R. Thieme
IPC分类号： C07D295/08 , A61K31/135 , A61K31/205 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P17/00 , A61P25/04 , A61P29/00 , C07C37/055 , C07C43/205 , C07C43/225 , C07C43/23 , C07C67/00 , C07C213/00 , C07C217/18 , C07D209/48 , C07D295/092
CPC分类号： C07D209/48 , C07C309/00 , C07C37/055 , C07C41/26 , C07C41/30 , C07D295/088
摘要： Compounds useful for treating inflammation, swelling and associated pain, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-3;b is an integer of 0-2;n is an integer of 3-12;each X and each Y are independently -halo, --R.sup.1, -alkoxy, or -phenyl; andB is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or --CH.sub.2 CH.sub.2 OH; andm is an integer of 3-8.Novel compounds are those wherein n is at least 6 if both a and b are 0.
摘要翻译：用于治疗由下式表示的炎症，肿胀和相关疼痛的化合物及其药学上可接受的酸加成盐，其中：a为0-3的整数; b为0-2的整数; n为3-12的整数; 每个X和每个Y独立地是卤素，-R1， - 烷氧基或 - 苯基; 并且B选自：-NR 1 R 2，-NR 1（CH 2 CH 2 OH），其中R 1和R 2独立地为H，烷基或环烷基; R3是H，烷基或-CH2CH2OH; m为3-8的整数。如果a和b都为0，则新的化合物是其中n至少为6的化合物。

2. 发明授权

US4599331A Etianic acids as antiangiogenics 失效
标题翻译： Etianic酸作为抗血管生成剂
公开(公告)号：US4599331A
公开(公告)日：1986-07-08
申请号：US685568
申请日：1984-12-24
申请人： Alain B. Schreiber , William J. Kowalski , Stefan H. Unger
发明人： Alain B. Schreiber , William J. Kowalski , Stefan H. Unger
IPC分类号： A61K31/56
CPC分类号： A61K31/56
摘要： This invention provides a method for inhibiting angiogenesis in mammals. A pharmaceutically acceptable formulation containing a compound of the formula ##STR1## where X.sub.1 X.sub.2 and X.sub.3 are H, C1, or F and X.sub.3 must be H if the substituent of R.sub.1 is .alpha.OH;R.sup.1 is chosen from the group consisting of hydroxyl and hydrogen;R.sub.2 is chosen from the group of alkyloxy or thioalkyls wherein said alkyls have less than 5 carbon atomsR.sub.3 is H or an alkyl having less than 6 carbon atoms, is administered to the mammal having undesirable angiogenesis.The wavy line at C-16 refers to either .alpha. or .beta..
摘要翻译：本发明提供一种抑制哺乳动物血管发生的方法。含有下式化合物的药学上可接受的制剂，其中X1 X2和X3是H，C1或F和X3必须是H，如果R1的取代基是αOH; R1选自羟基和氢; R 2选自烷氧基或硫代烷基，其中所述烷基具有少于5个碳原子，R 3为H或具有少于6个碳原子的烷基，被给予具有不期望的血管发生的哺乳动物。 C-16的波浪线是指alpha或beta。

3. 发明授权

US4123550A Bicyclo[3.1.0]hexylethylaminocarbonyl-substituted heteroaryl cardiovascular agents 失效
标题翻译：双环{8 3.1.0 {9己基乙基氨基羰基取代的杂芳基心血管剂
公开(公告)号：US4123550A
公开(公告)日：1978-10-31
申请号：US846959
申请日：1977-10-31
申请人： Karl G. Untch , Stefan H. Unger , Brian Lewis
发明人： Karl G. Untch , Stefan H. Unger , Brian Lewis
IPC分类号： C07C29/14 , C07C29/17 , C07D333/38 , A01N9/00 , C07D333/24
CPC分类号： C07D333/38 , C07C29/14 , C07C29/172
摘要： 1-Alkylamino-3-([2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]thienyloxy)-2-propanols and methods for preparing these compounds are disclosed. The compounds are useful in the treatment of hypertension and abnormal heart conditions in mammals. These compounds are prepared by the treatment of the corresponding 1,2-epoxy-3-[2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]heterocyclic aryloxy)propane with an alkylamine having the desired alkyl substituent or by base or acid hydrolysis of the corresponding 2-optionally substituted-3-alkyl-5-([2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]heterocyclic aryloxymethyl)oxazolidine. These latter compounds can be prepared by condensing a halo-substituted thiophene with a 3-alkyl-5-hydroxymethyloxazolidine such substituted or unsubstituted at the 2-position or alternatively, by treating the former aminopropanol compounds of the present invention with an aldehyde having the desired substituent. These latter oxazolidine compounds are also active for treatment of hypertension and abnormal heart conditions.
摘要翻译： 1-烷基氨基-3 - （[2-（内双环[3.1.0]己基-6-基）乙基氨基羰基]十一烷氧基）-2-丙醇及其制备方法。该化合物可用于治疗哺乳动物的高血压和异常心脏病。这些化合物通过用具有所需烷基取代基的烷基胺处理相应的1,2-环氧-3- [2-（内双环[3.1.0]己基-6-基）乙基氨基羰基]杂环烯基芳氧基）丙烷来制备，或通过碱或酸水解相应的2-任选取代的-3-烷基-5 - （[2-（内双环[3.1.0]己基-6-基）乙基氨基羰基]杂环芳氧基甲基）恶唑烷。这些后一种化合物可以通过将卤代取代的噻吩与2-位取代或未取代的3-烷基-5-羟基甲基恶唑烷缩合来制备，或者通过用具有所需的醛处理本发明的前一种氨基丙醇化合物取代基。这些后者的恶唑烷化合物对于治疗高血压和异常心脏病也是有活性的。

4. 发明授权

US4064259A Thiazole cardiovascular agents 失效
标题翻译：噻唑心血管药
公开(公告)号：US4064259A
公开(公告)日：1977-12-20
申请号：US706413
申请日：1976-07-19
申请人： Belig M. Berkoz , Brian Lewis , Stefan H. Unger
发明人： Belig M. Berkoz , Brian Lewis , Stefan H. Unger
IPC分类号： C07D277/56 , A61K31/425
CPC分类号： C07D277/56
摘要： 1-Alkylamino-3-(5-alkenylaminocarbonylthiazol-2-yloxy)-2-propanol; 5-(5-alkenylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolidine and/or 2-substituted oxazolidine derivatives thereof, and methods of making such compounds. The compounds exhibit cardiovascular activity and are useful in the treatment of abnormal heart conditions in mammals. The compounds are also useful in the treatment of hypertension in mammals. The 5-(5-alkenylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolidines and derivatives are also intermediates for the 1-alkylamino-3-(5-alkenylaminocarbonylthiazol-2-yloxy)-2-propanols. The 1-alkylamino-3-(5-alkenylaminocarbonylthiazol-2-yloxy)-2-propanols can be prepared by base or acid hydrolysis of the corresponding 5-(5-alkenylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolidine or derivative; or by treatment of the corresponding 3-(5-alkenylaminocarbonylthiazol-2-yloxy)-2,3-epoxypropane with the desired alkylamine. Similarly the 5-(5-alkenylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolidine or derivative can be prepared from the corresponding 1-alkylamino-3-(5-alkenylaminocarbonylthiazol-2-yloxy)-2-propanols via treatment with an aldehyde or ketone.
摘要翻译： 1-烷基氨基-3-（5-链烯基氨基羰基噻唑-2-基氧基）-2-丙醇; 5-（5-链烯基氨基羰基噻唑-2-基氧基亚甲基）-N-烷基恶唑烷和/或其2-取代的恶唑烷衍生物及其制备方法。该化合物显示出心血管活性，并且可用于治疗哺乳动物的异常心脏病。该化合物也可用于治疗哺乳动物的高血压。 5-（5-链烯基氨基羰基噻唑-2-基氧基亚甲基）-N-烷基恶唑烷及其衍生物也是1-烷基氨基-3-（5-链烯基氨基羰基噻唑-2-基氧基）-2-丙醇的中间体。 1-烷基氨基-3-（5-链烯基氨基羰基噻唑-2-基氧基）-2-丙醇可以通过相应的5-（5-链烯基氨基羰基噻唑-2-基氧基亚甲基）-N-烷基恶唑烷或其衍生物的碱或酸水解来制备。或通过用所需的烷基胺处理相应的3-（5-链烯基氨基羰基噻唑-2-基氧基）-2,3-环氧丙烷。类似地，5-（5-链烯基氨基羰基噻唑-2-基氧基亚甲基）-N-烷基恶唑烷或衍生物可以由相应的1-烷基氨基-3-（5-链烯基氨基羰基噻唑-2-基氧基）-2-丙醇通过用醛或酮。

5. 发明授权

US4064257A Thiazole cardiovascular agents 失效
标题翻译：噻唑心血管药
公开(公告)号：US4064257A
公开(公告)日：1977-12-20
申请号：US706341
申请日：1976-07-19
申请人： Belig M. Berkoz , Brian Lewis , Stefan H. Unger
发明人： Belig M. Berkoz , Brian Lewis , Stefan H. Unger
IPC分类号： C07D277/36 , C07D277/56 , A61K31/425
CPC分类号： C07D277/36 , C07D277/56
摘要： 1-Alkylamino-3-(5-alkynylaminocarbonylthiazol-2-yloxy)-2-propanol; 5-(5-alkynylaminocarbonyl-thiazol-2-yloxymethylene)-N-alkyloxazolidine and/or 2-substituted oxazolidine derivatives thereof, and methods of making such compounds. The compounds exhibit cardiovascular activity and are useful in the treatment of abnormal heart conditions in mammals. The compounds are also useful in the treatment of hypertension in mammals. The 5-(5-alkynyl-aminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolidines and derivatives are also intermediates for the 1-alkylamino-3-(5-alkynylaminocarbonylthiazol-2-yloxy)-2-propanols. The 1-alkylamino-3-(5-alkynylaminocarbonylthiazol-2-yloxy)-2-propanols can be prepared by base or acid hydrolysis of the corresponding 5-(5-alkynylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolidine or derivative; or by treatment of the corresponding 3-(5-alkynylaminocarbonylthiazol-2-yloxy)-2,3-epoxypropane with the desired alkylamine. Similarly the 5-(5-alkynylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolidine or derivative can be prepared from the corresponding 1-alkylamino-3-(5-alkynylaminocarbonylthiazol-2-yloxy)-2-propanols via treatment with an aldehyde or ketone.
摘要翻译： 1-烷基氨基-3-（5-炔基氨基羰基噻唑-2-基氧基）-2-丙醇; 5-（5-炔基氨基羰基 - 噻唑-2-基氧基亚甲基）-N-烷基恶唑烷和/或其2-取代的恶唑烷衍生物及其制备方法。该化合物显示出心血管活性，并且可用于治疗哺乳动物的异常心脏病。该化合物也可用于治疗哺乳动物的高血压。 5-（5-炔基 - 氨基羰基噻唑-2-基氧基亚甲基）-N-烷基恶唑烷及其衍生物也是1-烷基氨基-3-（5-炔基氨基羰基噻唑-2-基氧基）-2-丙醇的中间体。 1-烷基氨基-3-（5-炔基氨基羰基噻唑-2-基氧基）-2-丙醇可以通过相应的5-（5-炔基氨基羰基噻唑-2-基氧基亚甲基）-N-烷基恶唑烷或其衍生物的碱或酸水解制备。或通过用所需的烷基胺处理相应的3-（5-炔基氨基羰基噻唑-2-基氧基）-2,3-环氧丙烷。类似地，5-（5-炔基氨基羰基噻唑-2-基氧基亚甲基）-N-烷基恶唑烷或衍生物可以由相应的1-烷基氨基-3-（5-炔基氨基羰基噻唑-2-基氧基）-2-丙醇通过用醛或酮。

6. 发明授权

US4680300A Anti-inflammatory guanidines 失效
标题翻译：抗炎胍
公开(公告)号：US4680300A
公开(公告)日：1987-07-14
申请号：US690295
申请日：1985-01-10
申请人： Peter Nelson , Stefan H. Unger
发明人： Peter Nelson , Stefan H. Unger
IPC分类号： A61K31/155 , A61K31/425 , A61K31/426 , A61K31/47 , A61P17/00 , A61P29/00 , C07C67/00 , C07C239/00 , C07C279/04 , C07C279/08 , C07D215/38 , C07D215/46 , C07D277/20 , C07D277/48 , C07C129/00
CPC分类号： C07D215/46 , C07C279/08 , C07D277/48 , C07C2101/14 , Y10S514/852
摘要： A compound having the formula ##STR1## where Ar=naphthyl, biphenyl, or quinolinyl;X=oxygen or NH;Y=2 to 8;R.sub.1 =phenyl, substituted phenyl, hydrogen, lower alkyl; andR.sub.2 is the same or different from R.sub.3 and is alkyl, cycloalkyl, phenyl, substituted phenyl, thiazolyl; andthe pharmaceutically acceptable salts thereof.Compounds of this general formula are useful as anti-inflammatories, and as anti-psoriatic agents.
摘要翻译：具有式“IMAGE”的化合物，其中Ar =萘基，联苯基或喹啉基; X =氧或NH; Y = 2〜8; R1 =苯基，取代的苯基，氢，低级烷基; 并且R 2与R 3相同或不同，并且是烷基，环烷基，苯基，取代的苯基，噻唑基; 及其药学上可接受的盐。该通式的化合物可用作抗炎剂，也可用作抗牛皮癣剂。

7. 发明授权

US4255432A 8-[2-3-Indolyl)ethyl]-1-oxa-3-,8-diazaspiro[4.5]decan-2-ones, pharmaceutical compositions thereof and methods of use thereof 失效
标题翻译： 8- [2,3-吲哚基]乙基] -1-氧杂-3-，8-二氮杂螺[4.5]癸-2-酮，其药物组合物及其使用方法
公开(公告)号：US4255432A
公开(公告)日：1981-03-10
申请号：US72867
申请日：1979-09-06
申请人： Arthur F. Kluge , Arthur M. Strosberg , Stefan H. Unger
发明人： Arthur F. Kluge , Arthur M. Strosberg , Stefan H. Unger
IPC分类号： C07D211/48 , C07D498/10 , A61K31/435 , C07D521/00
CPC分类号： C07D211/48
摘要： Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen, C.sub.1 to C.sub.6 alkyl, C.sub.6 to C.sub.12 carbocyclic aryl or aralkyl of 1 to 6 carbon atoms in the alkyl moiety and 6 to 12 carbon atoms in the carbocyclic aryl moiety;R.sup.4 and R.sup.5 are the same or different and are hydrogen or C.sub.1 to C.sub.6 alkyl; andR.sup.6 and R.sup.7 are the same or different and are hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.1 to C.sub.6 alkoxy. Methods for preparing these compounds are also disclosed. The compounds are useful as antihypertensives and as diuretics. They also function as antihistamines and as bronchodilating agents and are therefore effective in inhibiting the effects of allergic reactions. They are also of use in the treatment of migraine and in the treatment of vasospastic disorders.
摘要翻译：其中R 1，R 2和R 3相同或不同且为氢，C 1至C 6烷基，C 6至C 12碳环芳基或烷基部分具有1至6个碳原子的芳烷基和6至12个碳的式碳环芳基部分中的原子; R 4和R 5相同或不同，为氢或C 1至C 6烷基; R 6和R 7相同或不同，为氢，C 1至C 6烷基或C 1至C 6烷氧基。还公开了制备这些化合物的方法。该化合物可用作抗高血压药物和利尿剂。它们还用作抗组胺剂和作为支气管扩张剂，因此有效地抑制过敏反应的作用。它们也可用于治疗偏头痛和治疗血管痉挛性疾病。

8. 发明授权

US4177280A Bicyclo[3.1.0]hexyl-substituted carbonylaminophenoxy cardiovascular agents 失效
标题翻译：双环[3.1.0]己基取代的羰基氨基苯氧基心血管药
公开(公告)号：US4177280A
公开(公告)日：1979-12-04
申请号：US921371
申请日：1978-07-03
申请人： Karl G. Untch , Belig Berkoz , Stefan H. Unger
发明人： Karl G. Untch , Belig Berkoz , Stefan H. Unger
IPC分类号： A61K31/16 , A61K31/138 , A61K31/165 , A61K31/275 , A61P9/00 , A61P9/06 , A61P9/12 , A61P25/02 , A61P27/02 , A61P27/06 , C07C53/136 , C07C67/00 , C07C239/00 , C07C253/00 , C07C255/59 , C07C275/34 , C07D263/06 , C07D303/22 , C07C103/19 , A61K31/17 , A61K31/42 , C07C127/15
CPC分类号： C07D303/22 , C07C53/136 , C07D263/06
摘要： 1-Alkylamino-3-(4-[(endobicyclo[3.1.0]hex-6-yl)alkylure ido]-1-phenoxy)-2-propanol and substituted derivatives thereof; 1-alkylamino-3-(4-[(endobicyclo[3.1.0]hex-6-yl)-alkylcarbonylamino]-1-phenoxy)-2-propanol and substituted derivatives thereof; and 1-alkylamino-3-(4-[(endobicyclo-[3.1.0]hex-6-yl)alkoxycarbonylamino]-1-phenoxy)-2-propanol and substituted derivatives thereof as well as methods for preparing such compounds are disclosed. 5-(4-[(Endobicyclo[3.1.0]hex-6-yl)alkylureido]-1-phenoxy) methyl-3-alkyl-2-optionally substituted oxazolidine and derivatives thereof; 5-(4-[(endobicyclo[3.1.0]hex-6-yl alkylcarbonylamino]-1-phenoxy)methyl-3-alkyl-2-optionally substituted oxazolidine and derivatives thereof; and 5-(4-[(endobicyclo[3.1.0]hex-6-yl)alkoxycarbonylamino]-1-phenoxy)methyl-3-alkyl-2-optionally substituted oxazolidine and derivatives thereof and methods for preparing these compounds are also disclosed. These compounds exhibit cardiovascular activity and are useful in the treatment of abnormal heart conditions as well as hypertension in mammals. The bicyclo-2-propanols are prepared by treatment of the corresponding 1,2-epoxy-3-(4-[(endobicyclo[3.1.0]hex-6-yl)alkylureido, alkylcarbonylamino or alkoxycarbonylamino-1-phenoxypropane, with the desired alkylamine or by base or acid hydrolysis of the corresponding 5-(4-[(endobicyclo[3.1.0]-hex-6-yl)alkylureido, alkylcarbonylamino or alkoxycarbonylamino]-1-phenoxy)-methyloxazolidine. The lattercompounds are prepared from the corresponding 1-alkylamino-3-(4-[(endobicyclo[3.1.0]-hex-6-yl)alkylureido, alkylcarbonylamino or alkoxycarbonylamino]-1-phenoxy)-2-propanol by treatment with an aldehyde having the desired optional substituent.
摘要翻译： 1-烷基氨基-3-（4 - [（内双环[3.1.0]己基-6-基）烷基] -1-苯氧基）-2-丙醇及其取代衍生物; 1-烷基氨基-3-（4 - [（内双环[3.1.0]己基-6-基） - 烷基羰基氨基] -1-苯氧基）-2-丙醇及其取代衍生物; 和1-烷基氨基-3-（4 - [（内双环 - [3.1.0]己基-6-基）烷氧基羰基氨基] -1-苯氧基）-2-丙醇及其取代的衍生物以及制备这些化合物的方法。 5-（4 - [（内双环[3.1.0]己-6-基）烷基脲基] -1-苯氧基）甲基-3-烷基-2-任选取代的恶唑烷及其衍生物; 5-（4 - [（内双环[3.1.0]己-6-基烷基羰基氨基] -1-苯氧基）甲基-3-烷基-2-任选取代的恶唑烷及其衍生物;和5-（4 - [（内双环[ 3.1.0]己基-6-基）烷氧基羰基氨基] -1-苯氧基）甲基-3-烷基-2-任选取代的恶唑烷及其衍生物及其制备方法也公开了这些化合物显示心血管活性并且是有用的二环-2-丙醇通过处理相应的1,2-环氧-3-（4 - [（内双环[3.1.0]六-6-三氟甲基 - 烷基酰胺基，烷基羰基氨基或烷氧基羰基氨基-1-苯氧基丙烷与所需的烷基胺反应，或通过相应的5-（4 - [（内双环[3.1.0] - 己-6-基）烷基脲基，烷基羰基氨基或烷氧基羰基氨基 ] - 苯氧基） - 甲基恶唑烷，后者由相应的1-烷基氨基-3-（4 - [（内双环[3.1.0]己基-6-基）烷基脲基，烷基羰基氨基或烷氧基羰基氨基] -1-苯氧基）-2-丙醇，用具有所需任选取代基的醛进行处理。

9. 发明授权

US4560699A 5-(4-Vinylbenzoyl)-1,2-dihydro-3H-pyrrolo-[1,2-a]-pyrrole-1-carboxylic acids and derivatives thereof and use as analgesics and anti-inflammatories 失效
标题翻译： 5-（4-乙烯基苯甲酰基）-1,2-二氢-3H-吡咯并[1,2-a] - 吡咯-1-羧酸及其衍生物，用作镇痛药和抗炎剂
公开(公告)号：US4560699A
公开(公告)日：1985-12-24
申请号：US458243
申请日：1983-01-17
申请人： Joseph M. Muchowski , Stefan H. Unger
发明人： Joseph M. Muchowski , Stefan H. Unger
IPC分类号： A61K31/40 , A61P7/02 , A61P9/00 , A61P25/04 , A61P29/00 , C07D487/04 , C07D487/06
CPC分类号： C07D487/04
摘要： Novel 5-(4-vinyl- or 4-ethynylbenzoyl)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic alkyl esters and salts thereof, wherein R is vinyl or ethynyl, and Y is hydrogen, a lower alkyl group having from 1 to 6 carbon atoms, chloro or bromo.
摘要翻译：由式“IMAGE”表示的新型5-（4-乙烯基或4-乙炔基苯甲酰基）-1,2-二氢-3H-吡咯并[1,2-a]吡咯-1-羧酸和其药学上可接受的，有毒的烷基酯及其盐，其中R是乙烯基或乙炔基，Y是氢，具有1至6个碳原子的低级烷基，氯或溴。

10. 发明授权

US4145443A Bicyclo�3.1.0!hexylethylaminocarbonyl-substituted naphthyloxy cardiovascular agents 失效
标题翻译：双环{8 3.1.0 {9己基乙基氨基羰基取代的萘基氧基心血管剂
公开(公告)号：US4145443A
公开(公告)日：1979-03-20
申请号：US846952
申请日：1977-10-31
申请人： Karl G. Untch , Stefan H. Unger
发明人： Karl G. Untch , Stefan H. Unger
IPC分类号： C07C29/14 , C07C29/17 , C07D263/06 , C07D303/22 , C07C103/29
CPC分类号： C07D303/22 , C07C29/14 , C07C29/172 , C07D263/06
摘要： 1-Alkylamino-3-(�2-(endobicyclo�3.1.0!-hex-6-yl)ethylaminocarbonyl!naphthyloxy)-2-propanols and methods for preparing these compounds are disclosed. The compounds are useful in the treatment of hypertension and abnormal heart conditions in mammals. These compounds are prepared by the treatment of the corresponding 1,2-epoxy-3-�2-(endobicyclo�3.1.0!hex-6-yl)ethylaminocarbonyl!naphthyloxy)-propane with an alkylamine having the desired alkyl substituent or by base or acid hydrolysis of the corresponding 2-optionally substituted -3-alkyl-5-(�2-(endobicyclo�3.1.0!hex-6-yl)ethylaminocarbonyl!naphthyloxymethyl)oxazolidine. These latter compounds can be prepared by condensing a hydroxy-substituted naphthalene with a 3-alkyl-5-tosyloxymethyloxazolidine such substituted or unsubstituted at the 2-position or alternatively, by treating the former aminopropanol compounds of the present invention with an aldehyde having the desired substituent. These latter oxazolidine compounds are also active for treatment of hypertension and abnormal heart conditions.
摘要翻译： 1-烷基氨基-3 - （[2-（内双环[3.1.0] - 己-6-基）乙基氨基羰基]萘基甲氧基）-2-丙醇和制备这些化合物的方法。该化合物可用于治疗哺乳动物的高血压和异常心脏病。这些化合物是通过用具有所需烷基取代基的烷基胺处理相应的1,2-环氧-3- [2-（内双环[3.1.0]己基-6-基）乙基氨基羰基]萘基氧） - 丙烷制备的通过碱或酸水解相应的2-任选取代的-3-烷基-5 - （[2-（内双环[3.1.0]己基-6-基）乙基氨基羰基]萘基氧甲基）恶唑烷。这些后一种化合物可以通过将2-羟基取代的萘与2-位取代或未取代的3-烷基-5-甲苯磺酰氧基甲基恶唑烷缩合来制备，或者通过用具有所需的醛处理本发明的前一种氨基丙醇化合物取代基。这些后者的恶唑烷化合物对于治疗高血压和异常心脏病也是有活性的。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式