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    Radiolabeled angiotensin converting enzyme inhibitors for radiolabeling mammalian organ sites
    3.
    发明授权
    Radiolabeled angiotensin converting enzyme inhibitors for radiolabeling mammalian organ sites 失效
    用于放射性标记哺乳动物器官部位的放射性标记的血管紧张素转换酶抑制剂

    公开(公告)号：US4574079A

    公开(公告)日：1986-03-04

    申请号：US498736

    申请日：1983-05-27

    Applicant: Haralambos P. Gavras ,  James W. Ryan ,  Alfred Chung

    Inventor： Haralambos P. Gavras ,  James W. Ryan ,  Alfred Chung

    IPC: A61K51/04 ,  C07K5/02 ,  A61K43/00 ,  A61K49/00 ,  A61K49/02

    CPC classification number: C07K5/0222 ,  A61K51/047 ,  A61K2123/00

    Abstract: Radiolabeled angiotensin converting enzyme inhibitors having the general formula: ##STR1## wherein X is a radiolabeling substituent, preferably a radiolabeling halogen substituent such as .sup.123 I, .sup.125 I, .sup.131 I, .sup.75 Br or .sup.77 Br,Y is hydroxy, alkoxy containing from 1 to 6 carbon atoms, phenoxy, benzyloxy, or amino,R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen, an ester moiety hydrolyzable under mammalian in vivo conditions, such as alkyl of 1 or 2 carbon atoms, phenyl or benzyl, or an ionically bonded anion of a physiologically acceptable non-toxic salt, andm is an integer of from 1 to 6, are useful as in vivo radioimaging compounds for mammalian sites.

    Abstract translation: 放射性标记的具有以下通式的血管紧张素转换酶抑制剂：其中X是放射性标记取代基，优选放射性标记的卤素取代基如123I，125I，131I，75Br或77Br，Y是羟基，含有1至6个碳原子的烷氧基， 苯氧基，苄氧基或氨基，R 1是氢或甲基，R 2是氢，在哺乳动物体内条件下可水解的酯部分，例如1或2个碳原子的烷基，苯基或苄基，或生理上可接受的离子键合阴离子 无毒盐，m为1〜6的整数，可用作哺乳动物部位的体内放射成像化合物。

    Tagged pyroglu-L-Phe-L-Arg derivatives, substrates and assays for kallikrein
    6.
    发明授权
    Tagged pyroglu-L-Phe-L-Arg derivatives, substrates and assays for kallikrein 失效
    标记的pyroglu-L-Phe-L-Arg衍生物，激肽释放酶的底物和测定法

    公开(公告)号：US4448715A

    公开(公告)日：1984-05-15

    申请号：US317412

    申请日：1981-11-02

    Applicant: James W. Ryan ,  Alfred Chung

    Inventor： James W. Ryan ,  Alfred Chung

    IPC: C07K5/065 ,  C07K5/097 ,  C12Q1/37 ,  C07C103/52 ,  C12Q1/56

    CPC classification number: C12Q1/37 ,  C07K5/06078 ,  C07K5/0821 ,  C07K5/0825

    Abstract: Novel compositions of matter of the general formulaA--L--Phe--L--Arg--Yare described, in which A is lower alkanoyl, pyroglutamyl, substituted with --OH or halogen, and cyclo lower alkanoyls; Y is --OH or a known tag with either radioactive, fluorogenic, chromogenic or chemiluminescent properties.The compounds of the invention are useful as novel substrates for plasma kallikrein.A new method of performing the assay for plasma kallikrein is also described.

    Abstract translation: 描述了通式为A-L-Phe-L-Arg-Y的物质的新型组合物，其中A为低级烷酰基，焦谷氨酰基，被-OH或卤素取代，环状低级烷酰基; Y是-OH或具有放射性，荧光，显色或化学发光性质的已知标签。 本发明的化合物可用作血浆激肽释放酶的新型底物。 还描述了进行血浆激肽释放酶测定的新方法。

    Substrates for angiotensin converting enzyme
    7.
    发明授权
    Substrates for angiotensin converting enzyme 失效
    血管紧张素转换酶底物

    公开(公告)号：US4251628A

    公开(公告)日：1981-02-17

    申请号：US886511

    申请日：1978-03-14

    Applicant: James W. Ryan ,  Alfred Chung

    Inventor： James W. Ryan ,  Alfred Chung

    IPC: C07K5/083 ,  C12Q1/37 ,  C12Q1/36

    CPC classification number: C12Q1/37 ,  C07K5/0806

    Abstract: A method is disclosed for quantitative measurement of angiotensin converting enzyme activity in biological material. The method exploits certain acylated tripeptide substrates. The enzyme-catalyzed hydrolysis of the substrates results in the formation of a dipeptide reaction product and a remnant product. The substrate is radioactively labeled exclusively in that portion destined to become the remnant product. Preferably, the substrate prior to hydrolysis is essentially insoluble in an aprotic organic solvent, but the remnant hydrolysis product is essentially quantitatively extractible by the organic solvent. At the termination of the enzyme-catalyzed hydrolysis, the labeled remnant product is separated from the reaction mixture, and the radioactivity is counted in a suitable apparatus.

    Abstract translation: 公开了用于定量测量生物材料中血管紧张素转换酶活性的方法。 该方法利用某些酰化三肽底物。 底物的酶催化水解导致二肽反应产物和剩余产物的形成。 衬底被放射性地标记在注定成为剩余产品的部分中。 优选地，水解前的底物基本上不溶于非质子有机溶剂，但是残留的水解产物基本上是可由有机溶剂提取的。 在酶催化水解终止时，从反应混合物中分离出标记的剩余产物，并在合适的装置中计数放射性。

    Orally effective anti-hypertensive agents
    8.
    发明授权
    Orally effective anti-hypertensive agents 失效
    口服有效的抗高血压药

    公开(公告)号：US4745124A

    公开(公告)日：1988-05-17

    申请号：US515474

    申请日：1983-07-20

    Applicant: James W. Ryan ,  Alfred Chung

    Inventor： James W. Ryan ,  Alfred Chung

    IPC: A61K38/00 ,  C07D207/16 ,  C07D207/22 ,  C07D207/50 ,  C07K5/068 ,  C07K5/078 ,  A61K31/40 ,  A61K31/41 ,  C07D207/00 ,  C07D211/72

    CPC classification number: C07K5/06173 ,  C07D207/16 ,  C07D207/22 ,  C07D207/50 ,  C07K5/06086 ,  A61K38/00

    Abstract: Novel thiolester compounds are disclosed which are orally effective angiotensin converting enzyme inhibitors useful in the treatment of mammalian hypertension. They have the formula,R.sub.1 -A.sub.1 -S-Z,wherein Z denotes -B-A.sub.2, R.sub.1 is H or an acyl group, A.sub.1 is a carboxylic acid containing at least one amino or imino -N-, A.sub.2 is a carboxylic acid containing at least one amino or imino -N- or a lower alkyl ester or amide thereof, B is a 2-4 carbon backbone chain in mercapto linkage to S which includes a carbonyl or sulfonyl group joined in carboxamido or sulfonamido linkage, respectively, to A.sub.2.Preferably A.sub.2 includes a 4-6 membered C-N ring or a 5 membered ring of one N, one S and 3 C atoms.

    Abstract translation: 公开了新颖的硫醇酯化合物，其是可用于治疗哺乳动物高血压的口服有效的血管紧张素转换酶抑制剂。 它们具有式R1-A1-SZ，其中Z表示-B-A2，R1是H或酰基，A1是含有至少一个氨基或亚氨基-N-的羧酸，A2是含有 至少一个氨基或亚氨基-N-或其低级烷基酯或酰胺，B是与S巯基连接的2-4碳主链，其包括分别连接到甲酰氨基或亚磺酰氨基键的羰基或磺酰基。 优选地，A2包括一个N，一个S和3个C原子的4-6元C-N环或5元环。

    Anti-hypertensive agents
    10.
    发明授权
    Anti-hypertensive agents 失效
    抗高血压药

    公开(公告)号：US4692437A

    公开(公告)日：1987-09-08

    申请号：US156749

    申请日：1980-06-05

    Applicant: James W. Ryan ,  Alfred Chung

    Inventor： James W. Ryan ,  Alfred Chung

    IPC: A61K38/55 ,  A61K20060101 ,  A61K31/40 ,  A61K31/401 ,  A61K31/405 ,  A61K38/00 ,  A61P9/12 ,  A61P43/00 ,  C07C20060101 ,  C07C67/00 ,  C07C325/00 ,  C07C327/20 ,  C07D207/16 ,  C07D207/22 ,  C07D207/50 ,  C07D403/12 ,  C07K1/113 ,  C07K5/06 ,  C07K5/068 ,  C07K5/078 ,  C07K5/08 ,  C07K14/81 ,  A61K31/425 ,  C07D207/00 ,  C07D277/04

    CPC classification number: C07D207/16 ,  C07D207/22 ,  C07D207/50 ,  C07K5/06086 ,  C07K5/06173 ,  A61K38/00 ,  Y10S930/12

    Abstract: Inhibitors of angiotensin converting enzyme which are physiologically acceptable salts of compounds which have the formula: ##STR1## wherein R is hydrogen, formyl, acetyl, propanoyl, butanoyl, phenylacetyl, phenylpropanoyl, benzoyl, cyclopentanecarbonyl, tert-butyloxycarbonyl, cyclopentanecarbonyl-L-lysyl, pyro-L-glutamyl-L-lysyl, L-lysyl, L-arginyl or pyro-L-glutamyl;A is phenylalanyl, glycyl, alanyl, tryptophyl, tyrosyl, isoleucyl, leucyl, histidyl, or valyl, the .alpha.-amino group thereof being in amide linkage with R;R.sub.1 is hydrogen or methyl;R.sub.2 is L-proline, L-3,4-dehydroproline, D,L-3,4-dehydroproline, L-3-hydroxyproline, L-4-hydroxyproline, L-thiazolidine-4-carboxylic acid, or L-5-oxo-proline, the imino group thereof being in imide linkage with the adjacent ##STR2## and, n is 0 or 1, such that when n is O, R.sub.1 is methyl are disclosed as useful anti-hypertensive agents.

    Abstract translation: 其中R为氢，甲酰基，乙酰基，丙酰基，丁酰基，苯乙酰基，苯基丙酰基，苯甲酰基，环戊烷羰基，叔丁氧基羰基，环戊烷羰基-L-赖氨酰基的化合物的生理上可接受的盐的血管紧张素转换酶抑制剂 ，pyro-L-谷氨酰-L-赖氨酰，L-赖氨酰，L-精氨酰或焦-L-谷氨酰; A是与R的酰胺键合的苯丙氨酰基，甘氨酰基，丙氨酰基，色氨酸，酪氨酰基，异亮氨酰基，亮氨酰基，组氨酰基或缬氨酰基; R1是氢或甲基; R2是L-脯氨酸，L-3,4-脱氢脯氨酸，D，L-3,4-脱氢脯氨酸，L-3-羟脯氨酸，L-4-羟基脯氨酸，L-噻唑烷-4-羧酸或L-5- 氧基 - 脯氨酸，其亚氨基与相邻的“IMAGE”具有酰亚胺键，并且n为0或1，使得当n为O时，R 1为甲基作为有用的抗高血压剂公开。

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