公开(公告)号：US4313954A

公开(公告)日：1982-02-02

申请号：US122704

申请日：1980-02-19

申请人： Hirohisa Wakatsuka ,  Masaki Hayashi ,  Yoshitaka Konishi

发明人： Hirohisa Wakatsuka ,  Masaki Hayashi ,  Yoshitaka Konishi

IPC分类号： A61K31/557 ,  A61P7/02 ,  A61P43/00 ,  C07C405/00 ,  C07D209/52 ,  A61K31/40

CPC分类号： C07C405/0041 ,  C07C405/00 ,  C07D209/52

摘要： Prostaglandin I.sub.2 analogues of the general formula ##STR1## [wherein R.sup.1 represents a hydrogen atom, an alkyl group containing from 1 to 12 carbon atoms, an aralkyl group containing from 7 to 13 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 4 carbon atoms, a phenyl group unsubstituted or substituted by at least one halogen atom, trifluoromethyl or phenyl group, or by at least one alkyl, alkoxy or alkylthio group containing from 1 to 4 carbon atoms, or represents a group --C.sub.m H.sub.2m COOR.sup.6, --C.sub.n H.sub.2n OR.sup.7 or ##STR2## in which m represents an integer of 1 to 12, n represents an integer of 2 to 12, R.sup.6, R.sup.8 and R.sup.9, which may be the same or different, each represent an alkyl group containing from 1 to 4 carbon atoms, and R.sup.7 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, R.sup.2 represents a hydrogen atom or a methyl or ethyl group, R.sup.3 represents an alkyl group containing from 1 to 4 carbon atoms, R.sup.4 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, R.sup.5 represents an alkyl group containing from 1 to 10 carbon atoms, Y represents ethylene or trans-vinylene, the hydroxy group attached to the C-11 carbon atom is in .alpha.-configuration, and the wavy line attached to the C-15 carbon atom is in .alpha.- or .beta.-configuration or a mixture thereof] and non-toxic acid addition salts thereof and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof are new compounds possessing pharmacological properties typical of the prostaglandins.

摘要翻译： 具有通式的前列腺素I2类似物[其中R1表示氢原子，含有1至12个碳原子的烷基，含有7至13个碳原子的芳烷基，含有4至7个碳原子的环烷基 未取代或被至少一个含有1至4个碳原子的烷基取代的苯基，未被取代或被至少一个卤素原子取代的苯基，三氟甲基或苯基，或至少一个含有1至4个碳原子的烷基，烷氧基或烷硫基 4个碳原子，或表示基团-C m H 2 mCOOR 6，-C n H 2n OR 7或其中m表示1至12的整数，n表示2至12的整数，R 6，R 8和R 9可以相同或不同 各自表示含有1至4个碳原子的烷基，R 7表示氢原子或含有1至4个碳原子的烷基，R 2表示氢原子或甲基或乙基，R 3表示含有 从1 至4个碳原子，R 4表示氢原子或含有1至4个碳原子的烷基，R 5表示含有1至10个碳原子的烷基，Y表示亚乙基或反式亚乙烯基， C-11碳原子为α-构型，连接至C-15碳原子的波浪线为α-或β-构型或其混合物）及其无毒的酸加成盐，当R1表示 氢原子，其无毒盐是具有典型的前列腺素的药理学性质的新化合物。

公开(公告)号：US4024174A

公开(公告)日：1977-05-17

申请号：US534509

申请日：1964-12-19

申请人： Masaki Hayashi ,  Seiji Kori ,  Hirohisa Wakatsuka ,  Yoshitaka Konishi

发明人： Masaki Hayashi ,  Seiji Kori ,  Hirohisa Wakatsuka ,  Yoshitaka Konishi

IPC分类号： C07C405/00 ,  C07D307/20 ,  C07D309/12 ,  C07C177/00

CPC分类号： C07D307/20 ,  C07C405/00 ,  C07D309/12 ,  Y10S514/825

摘要： Trans-.DELTA..sup.2 -prostaglandin compounds are disclosed of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## R.sup.1 represents an alkyl group containing from 1 to 10 carbon atoms, or an alkyl group containing from 1 to 6 carbon atoms carrying a phenyl substituent or a cycloalkyl substituent of 5 to 7 carbon atoms, R.sup.2 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, and R.sup.3.sup.' represents a hydrogen atom or an alkyl group containing from 1 to 12 carbon atoms, the double bonds in the 2- and 5-positions being in the trans- and cis-configurations respectively. These compounds are indicated in the management of conditions such as autoimmune conditions, e.g. rheumatoid arthritis.

摘要翻译： Trans-DELTA 2-前列腺素化合物公开于下列通式：其中A代表下式的基团：其中R 1表示含有1至10个碳原子的烷基，或 含有1〜6个碳原子的烷基，带有苯基取代基或5〜7个碳原子的环烷基取代基，R2表示氢原子或含1〜4个碳原子的烷基，R3'表示氢原子 或含有1至12个碳原子的烷基，2位和5位的双键分别为反式和顺式构型。 这些化合物在诸如自身免疫病症例如自身免疫病症的条件的管理中表示。 类风湿关节炎。

公开(公告)号：US4367237A

公开(公告)日：1983-01-04

申请号：US097675

申请日：1979-11-27

申请人： Hirohisa Wakatsuka ,  Katsuichi Shimoji ,  Sadahiko Iguchi ,  Yoshitaka Konishi ,  Hisashi Suga ,  Yasuyuki Miyata ,  Yoichi Iguchi ,  Hajimu Miyake ,  Masaki Hayashi

发明人： Hirohisa Wakatsuka ,  Katsuichi Shimoji ,  Sadahiko Iguchi ,  Yoshitaka Konishi ,  Hisashi Suga ,  Yasuyuki Miyata ,  Yoichi Iguchi ,  Hajimu Miyake ,  Masaki Hayashi

IPC分类号： C07C405/00 ,  C07D333/78 ,  C07D335/04 ,  A61K31/38

CPC分类号： C07C405/0033 ,  C07C405/00 ,  C07D333/78 ,  C07D335/04

摘要： Prostaglandin analogues of the general formula: ##STR1## [wherein the ring A represents: ##STR2## the ring B represents: ##STR3## (wherein R.sup.6 represents hydrogen, methyl or ethyl, and r is zero, one or two), Y represents ethylene, cis- or trans-vinylene or ethynylene, Z represents a grouping of the formula: --(CH.sub.2).sub.m --, --(CH.sub.2).sub.3 --CHR.sup.7 --, --(CH.sub.2).sub.2 --CHR.sup.7 --CH.sub.2 --, --CH.sub.2 --CHR.sup.7 --(CH.sub.2).sub.2 --, --CHR.sup.7 --(CH.sub.2).sub.3 --, or trans--(CH.sub.2).sub.2 --CH.dbd.CH-- (wherein m is 3, 4 or 5, and R.sup.7 represents methyl or ethyl), R.sup.1 represents a grouping of the formula: --COOR.sup.8, ##STR4## or --CH.sub.2 OR.sup.11 (wherein R.sup.8 represents hydrogen, alkyl, aralkyl, cycloalkyl which is unsubstituted or substituted by at least one alkyl group, or R.sup.8 represents phenyl which is unsubstituted or substituted by halogen, trifluoromethyl, alkyl, alkoxy, alkylthio or phenyl, or represents naphthyl, 2,3- or 1,3-dihydroxypropyl, 2,3- or 1,3-bisalkanoyloxypropyl, a grouping of the formula: -D.sub.1 --COOR.sup.12, ##STR5## -D.sub.2 -R.sup.15 or -D.sub.3 -R.sup.16, wherein D.sub.1 represents alkylene, D.sub.2 represents alkylene, D.sub.3 represents a single bond or alkylene, R.sup.12, R.sup.13 and R.sup.14, each represent alkyl, R.sup.15 represents hydroxy, alkoxy or alkylthio and R.sup.16 represents a heterocyclic ring, or R.sup.8 represents a grouping of the formula: ##STR6## R.sup.9 and R.sup.10, each represent hydrogen, alkyl, alkylsulphonyl, alkanoyl or ##STR7## represents a heterocyclic ring, and R.sup.11 represents hydrogen or alkanoyl, R.sup.2 represents hydrogen, methyl or ethyl, R.sup.3 represents a single bond or alkylene, R.sup.4 represents hydrogen, alkyl, alkoxy, cycloalkyl or cycloalkyloxy unsubstituted or substituted by alkyl, or represents phenyl or phenoxy unsubstituted or substituted by halogen, trifluoromethyl or alkyl with the proviso that, when R.sup.3 represents a single bond, R.sup.4 does not represent alkoxy, cycloalkyloxy or phenoxy, R.sup.5 represents hydrogen, methyl or ethyl and with the proviso that, when one of the groups R.sup.5, R.sup.6 and R.sup.7 represents methyl or ethyl the other two groups are hydrogen atoms] and cyclodextrin clathrates, non-toxic salts and non-toxic acid addition salts thereof, possess selective strong stimulatory activity on uterine contraction in female mammals.

公开(公告)号：US4399147A

公开(公告)日：1983-08-16

申请号：US872635

申请日：1978-01-26

申请人： Masaki Hayashi ,  Yoshinobu Arai ,  Yoshitaka Konishi ,  Katsuichi Shimoji ,  Shuichi Ohuchida ,  Hirohisa Wakatsuka ,  Hiroyuki Ito

发明人： Masaki Hayashi ,  Yoshinobu Arai ,  Yoshitaka Konishi ,  Katsuichi Shimoji ,  Shuichi Ohuchida ,  Hirohisa Wakatsuka ,  Hiroyuki Ito

IPC分类号： C07D307/935 ,  A61K31/34 ,  A61K31/343 ,  A61P43/00 ,  C07C405/00 ,  C07D307/937 ,  A61K31/557

CPC分类号： C07D307/937 ,  C07C405/00

摘要： Prostaglandin I.sub.2 analogues of the formula: ##STR1## [wherein X represents trans-vinylene or an ethylene group unsubstituted or substituted by a bromine atom at the C-5 position, Y represents trans-vinylene or ethylene, R.sup.1 represents hydrogen or an alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents hydrogen or methyl or ethyl, R.sup.3 represents a single bond or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4 represents hydrogen, an alkyl group containing from 1 to 8 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 8 carbon atoms, or a phenyl or phenoxy group unsubstituted or carrying at least one substituent selected from halogen atoms, the trifluoromethyl group and alkyl groups containing from 1 to 3 carbon atoms, and the wavy line attached to the carbon atoms in positions 6, 11 and 15 depicted in the formula represents .alpha.- or .beta.-configuration or mixtures thereof] are new compounds possessing pharmacological properties typical of prostaglandins, for example PGI.sub.2, and are more stable than PGI.sub.2.

摘要翻译： 前列腺素I2类似物，具有下式：其中X表示反式亚乙烯基或未被取代或被C-5位上的溴原子取代的亚乙基，Y表示反式亚乙烯基或亚乙基，R 1表示氢或烷基 含有1至12个碳原子，R 2表示氢或甲基或乙基，R 3表示单键或含有1至4个碳原子的亚烷基，R 4表示氢，含有1至8个碳原子的烷基，环烷基 含有未取代或被至少一个含有1至8个碳原子的烷基取代的4至7个碳原子的基团，或未取代或携带至少一个选自卤素原子的取代基的苯基或苯氧基，三氟甲基和含有 1至3个碳原子，并且连接在式中描述的6,11和15位的碳原子上的波浪线代表α-或β-构型或其混合物] 是具有典型的前列腺素的药理学性质的新化合物，例如PGI 2，并且比PGI2更稳定。

公开(公告)号：US4178367A

公开(公告)日：1979-12-11

申请号：US878571

申请日：1978-02-16

申请人： Hayashi Masaki ,  Yoshinobu Arai ,  Yoshitaka Konishi ,  Katsuichi Shimoji ,  Shuichi Ohuchida ,  Hiroyuki Ito ,  Hirohisa Wakatsuka

发明人： Hayashi Masaki ,  Yoshinobu Arai ,  Yoshitaka Konishi ,  Katsuichi Shimoji ,  Shuichi Ohuchida ,  Hiroyuki Ito ,  Hirohisa Wakatsuka

IPC分类号： C07C405/00 ,  C07D307/937 ,  C07F9/40 ,  A61K31/34 ,  C07D307/93

CPC分类号： C07D307/937 ,  C07C405/00 ,  C07F9/4018

摘要： Prostaglandin I.sub.2 analogues of the formula: ##STR1## (wherein Y represents trans-vinylene or ethylene, R.sup.1 represents hydrogen or an alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents hydrogen, methyl or ethyl, R.sup.3 represents a single bond, or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, each represent hydrogen or an alkyl group containing from 1 to 8 carbon atoms, n represents 3, 4, 5 or 6, the wavy line attached to the carbon atoms in positions 11 and 15 depicted in the formula represents .alpha.- or .beta.-configuration or mixtures thereof, and the double bond between C.sub.6 -C.sub.6 is Z or E) are new compounds possessing pharmacological properties typical of prostaglandins, for example PGI.sub.2.

摘要翻译： 前列腺素I2类似物具有下式：其中Y表示反式亚乙烯基或亚乙基，R 1表示氢或含有1至12个碳原子的烷基，R 2表示氢，甲基或乙基，R 3表示单键， 或含有1至4个碳原子的亚烷基，可以相同或不同的R 4，R 5和R 6各自表示氢或含有1至8个碳原子的烷基，n表示3,4,5或6 连接在式中描述的位置11和15处的碳原子的波浪线代表α-或β-构型或其混合物，并且C6-C6之间的双键是Z或E）是具有典型的药理学性质的新化合物 前列腺素，例如PGI2。

公开(公告)号：US4145555A

公开(公告)日：1979-03-20

申请号：US774828

申请日：1977-03-07

申请人： Masaki Hayashi ,  Seiji Kori ,  Yoshinobu Arai ,  Takanori Okada ,  Yoshitaka Konishi

发明人： Masaki Hayashi ,  Seiji Kori ,  Yoshinobu Arai ,  Takanori Okada ,  Yoshitaka Konishi

IPC分类号： A61K31/23 ,  A61K9/48 ,  A61K31/557 ,  A61K31/5575 ,  A61K31/70 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D309/12 ,  C08B37/00 ,  C08B37/16 ,  C07C177/00

CPC分类号： C07C405/00 ,  C07D309/12 ,  C08B37/0015

摘要： 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.

摘要翻译： 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。

公开(公告)号：US4165437A

公开(公告)日：1979-08-21

申请号：US934444

申请日：1978-08-17

申请人： Masaki Hayashi ,  Seiji Kori ,  Yoshinobu Arai ,  Takanori Okada ,  Yoshitaka Konishi

发明人： Masaki Hayashi ,  Seiji Kori ,  Yoshinobu Arai ,  Takanori Okada ,  Yoshitaka Konishi

IPC分类号： C07C405/00 ,  C07D309/12 ,  C08B37/00 ,  C07C177/00

CPC分类号： C07C405/00 ,  C07D309/12 ,  C08B37/0015

摘要： The present invention relates to prostaglandin analogues of the general formula: ##STR1## [wherein X represents cis or trans-vinylene or ethylene, R 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.

摘要翻译： 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，R表示R 1表示氢原子或含有1个直链或支链烷基的直链或支链烷基 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。

公开(公告)号：US4479966A

公开(公告)日：1984-10-30

申请号：US113502

申请日：1980-01-21

申请人： Masaki Hayashi ,  Yoshitaka Konishi ,  Yoshinobu Arai

发明人： Masaki Hayashi ,  Yoshitaka Konishi ,  Yoshinobu Arai

IPC分类号： A61K47/48 ,  C07C45/64 ,  C07C45/65 ,  C07C45/67 ,  C07C49/517 ,  C07C405/00 ,  C07D309/12 ,  C07C177/00 ,  C07C59/46

CPC分类号： B82Y5/00 ,  A61K47/48969 ,  C07C405/0083 ,  C07C45/64 ,  C07C45/65 ,  C07C45/673 ,  C07C49/517 ,  C07D309/12 ,  Y02P20/55

摘要： Prostaglandin I.sub.2 analogues of the formula: ##STR1## [wherein the symbol between the carbon atoms in positions 5 and 6 represents a single or double bond, Y represents ethylene or trans-vinylene, R.sup.1 represents hydrogen, alkyl of 1 to 12 carbon atoms, aralkyl of 7 to 12 carbon atoms, cycloalkyl of 4 to 7 carbon atoms optionally substituted by alkyl of 1 to 4 carbon atoms, phenyl optionally substituted by chlorine, trifluoromethyl, alkyl of 1 to 4 carbon atoms or phenyl, a --C.sub.m H.sub.2m COOR.sup.7 group (wherein m represents an integer of from 1 to 12 and R.sup.7 represents alkyl of 1 to 4 carbon atoms), a --C.sub.n H.sub.2n OR.sup.8 group (wherein n represents an integer of from 2 to 12 and R.sup.8 represents hydrogen or alkyl of 1 to 4 carbon atoms) or a ##STR2## group (wherein R.sup.9 and R.sup.10 each represent alkyl of 1 to 4 carbon atoms and n is as hereinbefore defined), R.sup.2 represents hydrogen or a hydroxy-protecting group, R.sup.3 represents hydrogen or a hydroxy-protecting group which is eliminated under acidic conditions, R.sup.4 represents hydrogen, methyl or ethyl, R.sup.5 represents a single bond or alkylene of 1 to 4 carbon atoms optionally substituted by a chlorine atom (provided that, when R.sup.5 is alkylene substituted by chlorine, R.sup.6 represents hydrogen or alkyl) R.sup.6 represents hydrogen, alkyl or 1 to 8 carbon atoms, cycloalkyl of 4 to 7 carbon atoms optionally substituted by alkyl of 1 to 8 carbon atoms, or phenyl or phenoxy optionally substituted by cholrine, trifluoromethyl or alkyl of 1 to 4 carbon atoms, and when represents a double bond that bond is E, Z or a mixture thereof and when, represents a single bond, the absolute configuration of C.sub.6 is R, S or a mixture thereof] and, when R.sup.2 and R.sup.3 represent hydrogen, cyclodextrin clathrates of such acids and esters and, when R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, non-toxic salts thereof and, when R.sup.1 represents ##STR3## in which n, R.sup.9 and R.sup.10 are as hereinbefore defined, non-toxic acid addition salts thereof, are new compounds, possessing prostaglandin-like activity.

公开(公告)号：US4207332A

公开(公告)日：1980-06-10

申请号：US944164

申请日：1978-09-20

申请人： Masaki Hayashi ,  Yoshinobu Arai ,  Katsuichi Shimoji ,  Yoshitaka Konishi ,  Shuichi Ohuchida ,  Shinsuke Hashimoto

发明人： Masaki Hayashi ,  Yoshinobu Arai ,  Katsuichi Shimoji ,  Yoshitaka Konishi ,  Shuichi Ohuchida ,  Shinsuke Hashimoto

IPC分类号： C07D307/935 ,  A61K31/34 ,  A61K31/343 ,  A61P43/00 ,  C07C405/00 ,  C07D307/937 ,  C07D307/93

CPC分类号： C07D307/937 ,  C07C405/00

摘要： Prostaglandin analogues of the general formula: ##STR1## [wherein Y represents ethylene or trans-vinylene, R.sup.1 represents a group --C.sub.m H.sub.2m COOR.sup.5, --C.sub.n H.sub.2n OR.sup.6 or ##STR2## (wherein R.sup.5 represents an alkyl group containing from 1 to 4 carbon atoms, R.sup.6 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, R.sup.7 and R.sup.8, which may be the same or different, each represents an alkyl group containing from 1 to 4 carbon atoms, m represents an integer of from 1 to 12 and n represents an integer of from 2 to 12), R.sup.2 represents a hydrogen atom or a methyl or ethyl group, R.sup.3 represents a single bond, or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4 represents a hydrogen atom, an alkyl group containing from 1 to 8 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms in the ring, which may be unsubstituted or substituted by at least one alkyl group containing from 1 to 8 carbon atoms, or represents a phenyl or phenoxy group which may be unsubstituted or substituted by at least one chlorine atom, trifluoromethyl group or alkyl group containing from 1 to 3 carbon atoms, the wavy line attached to the carbon atoms in positions 11 and 15 represents .alpha.- or .beta.-configuration, or mixtures thereof, and the double bond between C.sub.5 -C.sub.6 is Z] and cyclodextrin clathrates thereof, and, when R.sup.1 represents a group ##STR3## in which n, R.sup.7 and R.sup.8 are as hereinbefore defined, non-toxic acid addition salts thereof, are new compounds and possess characteristic prostaglandin-like properties.

摘要翻译： 前列腺素类似物具有以下通式：其中Y表示亚乙基或反式亚乙烯基，R1表示基团-CmH2mCOOR5，-CnH2nOR6或其中R5表示含有1至4个碳原子的烷基，R6表示 含有1至4个碳原子的氢原子或烷基，可以相同或不同的R 7和R 8各自表示含有1至4个碳原子的烷基，m表示1至12的整数，m表示1至12的整数， n表示2〜12的整数），R2表示氢原子或甲基或乙基，R3表示单键或含有1〜4个碳原子的亚烷基，R4表示氢原子，烷基 含有1至8个碳原子的环烷基，环中含有4至7个碳原子的环烷基，其可以是未取代的或被至少一个含有1至8个碳原子的烷基取代，或表示苯基或苯氧基， 可以是未取代的或未取代的 由至少一个氯原子，三氟甲基或含有1至3个碳原子的烷基取代，连接到位置11和15的碳原子的波浪线表示α或β构型，或其混合物，双键 C5-C6之间是Z]和环糊精包合物，当R1代表其中n，R7和R8如上所定义的基团“IMAGE”时，其无毒的酸加成盐是新的化合物，并且具有特征性的前列腺素 - 像属性。

公开(公告)号：US07897897B2

公开(公告)日：2011-03-01

申请号：US11934303

申请日：2007-11-02

申请人： Megumi Jyousaka ,  Yoshitaka Konishi

发明人： Megumi Jyousaka ,  Yoshitaka Konishi

IPC分类号： H05B1/02

CPC分类号： G05D23/1932 ,  H01L21/67248

摘要： In the present invention, a thermal plate of a PEB unit is divided into a plurality of thermal plate regions, and a temperature is settable for each of the thermal plate regions. A temperature correction value for adjusting the temperature within the thermal plate is settable for each of the thermal plate regions of the thermal plate. The line widths within the substrate which has been subjected to the photolithography process are measured, and an improvement in-plane tendency Za improved by change of the temperature settings is subtracted from an in-plane tendency Z of the measured line widths within the substrate to calculate an in-plane tendency Zb of the line widths within the substrate after change of temperature settings. The improvement in-plane tendency Za is calculated using the following expression. Za=−1×α×MT (α: a resist heat sensitivity, M: a calculation model, and T: temperature correction values for thermal plate regions).

摘要翻译： 在本发明中，将PEB单元的热板分割为多个热板区域，并且可以对每个热板区域设定温度。 用于调节热板内的温度的温度校正值可针对热板的每个热板区域而设定。 测量已进行了光刻处理的基板内的线宽，并从基板内的被测线宽度的面内倾向Z中减去由温度设定的变化而提高的面内倾向Za， 在温度设置更改后，计算衬底内线宽的面内倾向Zb。 使用以下表达式计算平面内倾向Za的改善。 Za = -1×α×MT（α：抗蚀剂热敏感性，M：计算模型，T：热板区域的温度校正值）。