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    • 51. 发明授权
    • 9,11-Methano-13-aza-11a-carbathrombanoic acid analogues
    • US4389413A
    • 1983-06-21
    • US285723
    • 1981-07-22
    • Nobuyuki HamanakaShinsuke HashimotoMasaki Hayashi
    • Nobuyuki HamanakaShinsuke HashimotoMasaki Hayashi
    • C07C33/14C07C405/00C07D309/12A61K31/557C07C101/14
    • C07C33/14C07C405/0091C07D309/12Y10S514/826
    • The 9,11-methano-13-aza-11a-carbathrombanoic acid analogues of the general formula: ##STR1## [wherein A represents ##STR2## (in which m is an integer of 1 to 6, the double bond between the carbon atoms in positions 5 and 6 in (iv) is in cis or trans-configuration or a mixture thereof and the phenylene group in (iv) represents o-, m- or p-phenylene), R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group of 1 to 12 carbon atoms, two R.sup.2 both represent hydrogen atoms or methyl groups, R.sup.3 represents a hydrogen atom or a hydroxy group, R.sup.4 represents a single bond or a straight- or branched-chain alkylene group of 1 to 5 carbon atoms, R.sup.5 represents(i) a straight- or branched-chain alkyl, alkoxy or alkylthio group of 1 to 8 carbon atoms,(ii) a cycloalkyl or cycloalkyloxy group of 4 to 7 carbon atoms being unsubstituted or substituted by at least one straight- or branched-chain alkyl group of 1 to 8 carbon atoms or ##STR3## in which Z represents a single bond, an oxygen atom or a sulfur atom and R.sup.6 may occupy any of the free positions on the phenyl ring and represents a hydrogen atom, a halogen atom, a hydroxy group, a straight- or branched-chain alkyl or alkoxy group of 1 to 5 carbon atoms, a trihalomethyl group, an amino group or a mono- or dialkyl-amino group of 1 to 5 carbon atoms)and the wavy line attached to the carbon atom in position 15 represents .alpha.- or .beta.-configuration or a mixture thereof, provided that, when R.sup.3 represents a hydroxy group and R.sup.4 represents a single bond, R.sup.5 does not represent an alkoxy group, an alkylthio group, a cycloalkyloxy group, a phenoxy group and a phenylthio group],and cyclodextrin clathrates thereof, and when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, possess strong inhibitory activities on platelet aggregation and on aorta contraction, and are useful for prevention and treatment of diseases which are induced by thromboxane A.sub.2.
    • 53. 发明授权
    • .DELTA..sup.3 -Prostaglandin analogs
    • {66 {HU 3 {B-前列腺素类似物
    • US4145555A
    • 1979-03-20
    • US774828
    • 1977-03-07
    • Masaki HayashiSeiji KoriYoshinobu AraiTakanori OkadaYoshitaka Konishi
    • Masaki HayashiSeiji KoriYoshinobu AraiTakanori OkadaYoshitaka Konishi
    • A61K31/23A61K9/48A61K31/557A61K31/5575A61K31/70A61P43/00C07C67/00C07C401/00C07C405/00C07D309/12C08B37/00C08B37/16C07C177/00
    • C07C405/00C07D309/12C08B37/0015
    • The present invention relates to prostaglandin analogues of the general formula: ##STR1## �wherein X represents cis or trans-vinylene or ethylene, Z represents ##STR2## R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents a hydrogen atom or a methyl group, R.sup.3 represents a straight- or branched-chain alkylene group containing from 1 to 7 carbon atoms and R.sup.4 represents a cycloalkyl group containing from 5 to 7 carbon atoms, a grouping of the formula: ##STR3## (wherein R.sup.5 and R.sup.6, which may be the same or different, each represent a hydrogen atom or halogen atom, a trifluoromethyl group or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms), or a grouping of the formula: ##STR4## (wherein R.sup.5 and R.sup.6 are as hereinbefore defined), or R.sup.3 and R.sup.4 together represent a straight- or branched-chain alkyl group containing from 1 to 10 carbon atoms, and (1) the double bond between C.sub.3 -C.sub.4 is trans or cis, or trans and cis, when X is cis-vinylene or ethylene, and (2) the double bond between C.sub.3 -C.sub.4 is trans, when X is trans-vinylene, and the double bond between C.sub.13 -C.sub.14 is trans! and cyclodextrin clathrates of such acids and esters, and when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, which exhibit characteristic prostaglandin-like activities.
    • 本发明涉及以下通式的前列腺素类似物:其中X表示顺式或反式亚乙烯基或亚乙基,Z表示R 1表示氢原子或含有1个或更多个的直链或支链烷基 至12个碳原子,R 2表示氢原子或甲基,R 3表示含有1至7个碳原子的直链或支链亚烷基,R 4表示含有5至7个碳原子的环烷基, 式(其中R5和R6可以相同或不同,分别表示氢原子或卤原子,三氟甲基或含有1至4个碳原子的直链或支链烷基) ,或下式的分组:其中R 5和R 6如上所定义,或者R 3和R 4一起表示含有1至10个碳原子的直链或支链烷基,和(1) C3-C4之间的双键是反式或顺式,或 反式和顺式,当X为顺式 - 亚乙烯基或亚乙基时,和(2)当X为反式亚乙烯基时,C 3 -C 4之间的双键为反式,C13-C14之间的双键为反式]和环糊精包合物 酸和酯,当R1代表氢原子时,其无毒性盐显示出特征性的前列腺素样活性。