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    Glycine derivative monosodium salt tetrahydrate
    1.
    发明授权
    Glycine derivative monosodium salt tetrahydrate 失效
    甘氨酸衍生物单钠盐四水合物

    公开(公告)号：US5359121A

    公开(公告)日：1994-10-25

    申请号：US182366

    申请日：1994-01-18

    申请人： Katsuhiro Imaki ,  Hirohisa Wakatsuka

    发明人： Katsuhiro Imaki ,  Hirohisa Wakatsuka

    IPC分类号： C07C311/29 ,  C07C311/15

    CPC分类号： C07C311/29

    摘要： N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetrahydrate of the formula (I): ##STR1## is non-hygroscopic, homogeneous and stable compound, and has an inhibitory effect on elastase. Accordingly, the compound may be useful for the treatment and/or prevention of diseases induced by the abnormal enhancing of degradation of elastin, collagen fiber and/or proteoglican by the action of elastase, e.g., pulmonary emphysema, atherosclerosis, rheumatoid arthritis, etc.

    摘要翻译： 式（I）的N- [对 - （对 - 新戊酰氧基苯磺酰基氨基）苯甲酰基]甘氨酸四钠水合物：（I）是不吸湿，均相和稳定的化合物，对弹性蛋白酶具有抑制作用。 因此，该化合物可用于治疗和/或预防由弹性蛋白酶（例如肺气肿，动脉粥样硬化，类风湿性关节炎等）的弹性蛋白，胶原纤维和/或蛋白多糖的异常增强引起的疾病的治疗和/或预防。

    6-keto-prostaglandin E.sub.1 derivatives
    4.
    发明授权
    6-keto-prostaglandin E.sub.1 derivatives 失效
    6-酮前列腺素E1衍生物

    公开(公告)号：US4783480A

    公开(公告)日：1988-11-08

    申请号：US7657

    申请日：1987-01-28

    申请人： Hirohisa Wakatsuka ,  Tadao Okegawa ,  Yoshinobu Arai

    发明人： Hirohisa Wakatsuka ,  Tadao Okegawa ,  Yoshinobu Arai

    IPC分类号： A61K31/557 ,  A61K31/5575 ,  A61P1/16 ,  A61P7/02 ,  A61P9/12 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C08B37/00 ,  C07C177/00

    CPC分类号： C07C405/0041 ,  C08B37/0015

    摘要： A 6-keto-prostaglandin E.sub.1 derivative of the formula: ##STR1## (wherein R.sup.1 represents an amino acid or amino alcohol residue, R.sup.2 represents a single bond or an alkylene group of from 1 to 4 carbon atoms, R.sup.3 represents (i) an alkyl group of from 1 to 8 carbon atoms, (ii) a cycloalkyl group of from 4 to 7 carbon atoms, which may be unsubstituted or substituted by at least one alkyl group of from 1 to 8 carbon atoms or (iii) a phenyl or phenoxy group, which may be unsubstituted or substituted by chlorine, trifluoromethyl or alkyl of from 1 to 3 carbon atoms, provided that when R.sup.2 represents a single bond R.sup.3 does not represent phenoxy)cyclodextrin clathrates thereof and non-toxic salts thereof possess selective cytoprotective activity.

    摘要翻译： 下式的6-酮前列腺素E1衍生物：其中R1表示氨基酸或氨基醇残基，R2表示单键或1〜4个碳原子的亚烷基，R3表示（ i）1至8个碳原子的烷基，（ii）4至7个碳原子的环烷基，其可以是未被取代的或被至少一个1至8个碳原子的烷基取代，或（iii） 苯基或苯氧基，其可以是未取代的或被氯，三氟甲基或具有1至3个碳原子的烷基取代，条件是当R 2表示单键时，R3不表示苯氧基）环糊精包合物和其无毒盐具有 选择性细胞保护活性。

    Trans-.DELTA..sup.2 -prostaglandin D derivatives, process for their preparation and compositions containing them
    5.
    发明授权
    Trans-.DELTA..sup.2 -prostaglandin D derivatives, process for their preparation and compositions containing them 失效
    转DELTA 2-前列腺素D衍生物，其制备方法和含有它们的组合物

    公开(公告)号：US4562204A

    公开(公告)日：1985-12-31

    申请号：US508560

    申请日：1983-06-28

    申请人： Hirohisa Wakatsuka ,  Takashi Yamato ,  Shinsuke Hashimoto

    发明人： Hirohisa Wakatsuka ,  Takashi Yamato ,  Shinsuke Hashimoto

    IPC分类号： A61K31/557 ,  A61K31/5575 ,  A61P35/00 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C08B37/00 ,  C07C177/00

    CPC分类号： C08B37/0015 ,  C07C405/00 ,  C07C405/0033 ,  Y10S514/908

    摘要： Trans-.DELTA..sup.2 -prostaglandin D derivatives of the formula: ##STR1## wherein [A] is a group of the formula: ##STR2## X is ethylene or cis-vinylene, C.sub.13 -C.sub.14 -C.sub.15 is: (i) a group of the formula: ##STR3## when [A] is a group of the formula (II) or (III), or (ii) a group of the formula: ##STR4## when [A] is a group of the formula (IV), R is hydrogen or alkyl, R.sup.1 is a single bond or alkylene, R.sup.2 is alkyl, cycloalkyl, phenyl or phenoxy, the double bonds between C.sub.2 -C.sub.3 and between C.sub.13 -C.sub.14 are both E, the double bond between C.sub.9 -C.sub.10 is Z and the double bonds between C.sub.12 -C.sub.13 and between C.sub.14 -C.sub.15 are E, Z or a mixture thereof, provided that when R.sup.1 is a single bond, R.sup.2 does not represent a substituted or unsubstituted phenoxy group, and cyclodextrin clathrates and non-toxic salts thereof, possess anti-tumor activity.

    摘要翻译： （I）其中[A]是下式的基团：X是亚乙基或顺式 - 亚乙烯基，C13-C14-C15是：（i）具有下式的组合的转DELTA 2-前列腺素D衍生物： 当[A]是式（II）或（III）的基团时，或（ⅱ）下式的组：当[A]为[IMAGE]（Ⅵ）时， 是式（IV）的基团，R是氢或烷基，R 1是单键或亚烷基，R 2是烷基，环烷基，苯基或苯氧基，C 2 -C 3和C 13 -C 14之间的双键都是E， C9-C10之间的双键为Z，C12-C13和C14-C15之间的双键为E，Z或其混合物，条件是当R1为单键时，R2不表示取代或未取代的苯氧基 和环糊精包合物及其无毒盐具有抗肿瘤活性。

    6,9-Nitrilo-prostaglandin analogues
    6.
    发明授权
    6,9-Nitrilo-prostaglandin analogues 失效
    6,9-Nitrilo-prostaglandin类似物

    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。

    Trans-.DELTA..sup.2 -prostaglandins
    7.
    发明授权
    Trans-.DELTA..sup.2 -prostaglandins 失效
    Trans- {66 {hu 2 {b-前列腺素

    公开(公告)号：US3931296A

    公开(公告)日：1976-01-06

    申请号：US427403

    申请日：1973-12-21

    申请人： Masaki Hayashi ,  Hirohisa Wakatsuka ,  Seiji Kori

    发明人： Masaki Hayashi ,  Hirohisa Wakatsuka ,  Seiji Kori

    IPC分类号： C07C405/00 ,  C07D307/935 ,  C07D309/12 ,  C07F9/40 ,  C07F9/54 ,  C07C61/38 ,  C07C69/74

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07C405/0025 ,  C07D309/12 ,  C07F9/4006 ,  C07F9/5407 ,  Y10S514/927

    摘要： New process for the preparation of trans-.DELTA..sup.2 -prostaglandins of the formula ##SPC1##(wherein A represents a grouping of the PGE, PGF or PGA type, X represents --CH.sub.2 CH.sub.2 -- or trans --CH=CH--, R.sub.1 represents an alkyl radical of 1 to 10 carbon atoms or an alkyl radical of 1 to 6 carbon atoms carrying a phenyl substituent or a cycloalkyl substituent of 5 to 7 carbon atoms, R.sub.2 represents a hydrogen atom or an alkyl radical of 1 to 4 carbon atoms) and alkyl esters thereof having 1 to 10 carbon atoms in the chain, which comprises reacting a cyclopentane derivative of the formula: ##SPC2##(where R.sub.3 represents a 2-tetrahydropyranyl group unsubstituted or substituted by at least one alkyl radical, or a 1-ethoxyethyl group) with an alkyl phosphonate of the general formula: ##EQU1## (wherein R.sub.4 represents a methyl or ethyl radical, and R.sub.5 represents an alkyl radical of 1 to 10 carbon atoms), optionally hydrolyzing the resulting trans-.DELTA..sup.2 -prostaglandin ester of the general formula: ##SPC3##To the corresponding acid, optionally converting the 9.alpha.-hydroxy radical in the ester or acid product to an oxo group, and hydrolyzing the tetrahydropyranyloxy or ethoxyethoxy groups in the resulting trans-.DELTA..sup.2 -prostaglandin compound of the formula: ##SPC4##(wherein R.sub.6 represents a hydrogen atom or an alkyl radical of 1 to 10 carbon atoms, Z represents ##EQU2## or C=O) to hydroxy radicals to obtain a trans-.DELTA..sup.2 -PGF or trans-.DELTA..sup.2 -PGE compound of the formula: ##SPC5##And, if desired, converting the PGE alicyclic ring (Z represents C=O) into that of a PGA compound.The trans-.DELTA..sup.2 -prostaglandin products, which are new compounds except for trans-.DELTA..sup.2 -PGE.sub.1, possess typical pharmacological properties of the `natural` prostaglandins.

    摘要翻译： 用于制备下式的转DELTA 2-前列腺素的新方法（WHEREIN A代表PGE，PGF或PGA类型的一组，X表示-CH 2 CH 2 - 或反-CH = CH-，R 1表示1的烷基 至10个碳原子或1至6个碳原子的烷基，带有苯基取代基或5至7个碳原子的环烷基取代基，R2表示氢原子或1至4个碳原子的烷基）及其烷基酯，其具有 1至10个碳原子的链，其包括使下式的环戊烷衍生物：

    Prostacyclin analogues
    8.
    发明授权
    Prostacyclin analogues 失效

    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.

    Prostaglandin I.sub.2 analogues
    9.
    发明授权
    Prostaglandin I.sub.2 analogues 失效
    前列腺素I2类似物

    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。

    Tranes-delta 2-prostaglandins
    10.
    发明授权
    Tranes-delta 2-prostaglandins 失效

    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。