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1. 发明授权

US4650800A Substituted pyrimidin-2-ones, the salts thereof, pharmaceutical compositions containing them and a method therefor 失效
标题翻译：取代的嘧啶-2-酮，其盐，含有它们的药物组合物及其方法
公开(公告)号：US4650800A
公开(公告)日：1987-03-17
申请号：US496093
申请日：1983-05-19
申请人： Gordon H. Phillipps , Christopher Williamson , Ian P. Steeples , Brian M. Bain , Raymond A. Borella
发明人： Gordon H. Phillipps , Christopher Williamson , Ian P. Steeples , Brian M. Bain , Raymond A. Borella
IPC分类号： A61K31/505 , A61P35/00 , A61P35/02 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
CPC分类号： C07D409/06 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/06
摘要： Compounds of the general formula: ##STR1## wherein X represents a halogen atom or a trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group and Het represents an optionally substituted C-attached 5-7 membered aromatic heterocyclic ring which ring contains one or more heteroatoms selected from O, N and S and optionally carries a fused ring and where an acidic or basic group is present, the salts thereof have been found to possess excellent metaphase arresting ability and are of use in combating abnormal cell proliferation. Thus a knowledge of the cell division cycles of the normal and abnormal cells enables a cytotoxic drug to be administered while the abnormal cells are in a phase susceptible to attack and while the normal cells are in a non-susceptible phase.The compounds of the invention are prepared by alkylation, deprotection of a protected keto group, oxidation or electrophilic halogenation.
摘要翻译：通式的化合物：其中X表示卤素原子或三氟甲基; R1表示氢原子或低级烷基，Het表示任选取代的C连接的5-7元芳族杂环，该环含有一个或多个选自O，N和S的杂原子，并且任选地带有稠环，并且其中酸性或碱性基团，其盐被发现具有优异的中期阻滞能力，并且可用于对抗异常细胞增殖。因此，正常和异常细胞的细胞分裂周期的知识使得能够施用细胞毒性药物，同时异常细胞处于易受攻击的阶段，而正常细胞处于非易感相。本发明的化合物是通过烷基化，保护的酮基的脱保护，氧化或亲电卤化来制备的。

2. 发明授权

US4335121A Androstane carbothioates 失效
标题翻译：雄甾烷硫代磷酸酯
公开(公告)号：US4335121A
公开(公告)日：1982-06-15
申请号：US234113
申请日：1981-02-13
申请人： Gordon H. Phillipps , Brian M. Bain , Ian P. Steeples , Christopher Williamson
发明人： Gordon H. Phillipps , Brian M. Bain , Ian P. Steeples , Christopher Williamson
IPC分类号： A61K31/56 , A61K31/58 , A61P29/00 , C07J3/00 , C07J31/00 , C07J41/00 , C07J71/00 , C07J7/00
CPC分类号： C07J71/0031 , C07J3/005 , C07J31/006 , C07J41/0038 , C07J71/001 , C07J71/0015
摘要： Compounds of the formula ##STR1## wherein R.sup.1 represents a fluoro-, chloro- or bromo-methyl group or a 2'-fluoroethyl group, R.sup.2 represents a group COR.sup.6 where R.sup.6 is a C.sub.1-3 alkyl group or OR.sup.2 and R.sup.3 together form a 16.alpha.,17.alpha.-isopropylidenedioxy group; R.sup.3 represents a hydrogen atom, a methyl group (which may be in either the .alpha.- or .beta.-configuration) or a methylene group; R.sup.4 represents a hydrogen, chlorine or fluorine atom; R.sup.5 represents a hydrogen or fluorine atom and symbol represents a single or double bond have good anti-inflammatory activity, particularly on topical applications.The compounds of formula I are prepared by esterification, halogenation, reduction, deprotection and reaction at a 9,11-double bond to form a 9.alpha.-halo-11.beta.-hydroxy grouping.Pharmaceutical compositions containing the compounds of formula I and methods for the use of the compounds are described and claimed.
摘要翻译：式（I）的化合物其中R 1表示氟，氯或溴甲基或2'-氟乙基，R 2表示基团COR 6，其中R 6是C 1-3烷基或OR 2和R 3 一起形成16α，17α-异亚丙基二氧基; R 3表示氢原子，甲基（其可以是α或β构型）或亚甲基; R4表示氢，氯或氟原子; R5表示氢或氟原子，符号表示单键或双键具有良好的抗炎活性，特别是局部应用。式I的化合物通过在9,11-双键进行酯化，卤化，还原，脱保护和反应来制备，以形成9α-卤代-11β-羟基。描述并要求保护含有式I化合物的药物组合物和使用该化合物的方法。

3. 发明授权

US4650610A Androstane carbothioic acids 失效
标题翻译：雄甾烷硫代酸
公开(公告)号：US4650610A
公开(公告)日：1987-03-17
申请号：US753428
申请日：1985-07-10
申请人： Gordon H. Phillipps , Brian M. Bain , Stuart B. Laing
发明人： Gordon H. Phillipps , Brian M. Bain , Stuart B. Laing
IPC分类号： C07J3/00 , C07J31/00 , C07J41/00 , C07J71/00
CPC分类号： C07J31/006 , C07J3/005 , C07J41/0038 , C07J71/001 , C07J71/0015 , C07J71/0031
摘要： Androstane carbothioic acids of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a hydroxy group in the .alpha.-configuration, a methyl group which may be in either the .alpha.- or .beta.-configuration, or a methylene group;R.sup.2 represents a hydroxy or protected hydroxy group in either the .alpha.- or .beta.-configuration or an oxo group;R.sup.3 represents a hydrogen, bromine, chlorine or fluorine atom; or R.sup.2 and R.sup.3 together represent a carbon-carbon bond or an epoxy group in the .beta.-configuration;R.sup.4 represents a hydrogen or fluorine atom; and the symbol represents a single or double bond and the salts thereof are useful as intermediates in the preparation of anti-inflammatory androstane 17.beta.-carbothioate esters.The compounds of formula I are prepared by reaction of a reactive derivative of a 17.beta.-carboxylic acid corresponding to the compound of formula I with hydrogen sulphide or a sulphide or hydrosulphide salt.
摘要翻译：具有下式的雄甾烷硫代酸：其中R 1表示氢原子，α-构型中的羟基，可以是α或β-构型的甲基或亚甲基; R2表示α或β构型或氧代基中的羟基或被保护的羟基; R3表示氢，溴，氯或氟原子; 或R 2和R 3一起表示β-构型中的碳 - 碳键或环氧基; R4表示氢或氟原子; 符号表示单键或双键，其盐可用作制备抗炎雄激素17β-硫代磷酸酯的中间体。通式Ⅰ的化合物是通过将对应于式I化合物的17β-羧酸的活性衍生物与硫化氢或硫化物或硫化氢盐反应来制备的。

4. 发明授权

US4093721A Pharmaceutical compositions of 6.alpha.,9.alpha.-difluoro-androst-4-ene-17.beta.-carboxylates and derivatives thereof 失效
标题翻译： 6 {60,9 {60-氟 - 雄甾-4-烯-17 {62-羧酸盐及其衍生物
公开(公告)号：US4093721A
公开(公告)日：1978-06-06
申请号：US757325
申请日：1977-01-06
申请人： Gordon H. Phillipps , Brian M. Bain
发明人： Gordon H. Phillipps , Brian M. Bain
IPC分类号： C07J3/00 , A61K31/56
CPC分类号： C07J3/005
摘要： The specification describes anti-inflammatory steroids having the following formula ##STR1## wherein X represents a hydrogen or fluorine atom, R' represents a methyl, ethyl, n-propyl or iso-propyl group, R" represents a methyl, chloromethyl, fluoromethyl, bromomethyl or 2-fluoroethyl group and represents a single or double bond. The specification describes processes for preparing such compounds as well as pharmaceutical compositions containing the compounds.
摘要翻译：该说明书描述了具有下式的抗炎类固醇：其中X代表氢或氟原子，R'代表甲基，乙基，正丙基或异丙基，R“表示甲基，氯甲基，氟甲基，溴甲基或2-氟乙基，并且表示单键或双键。该说明书描述了制备这些化合物的方法以及含有这些化合物的药物组合物。

5. 发明授权

US4578221A Androstane carbothioic acids 失效
公开(公告)号：US4578221A
公开(公告)日：1986-03-25
申请号：US513396
申请日：1983-07-14
申请人： Gordon H. Phillipps , Brian M. Bain , Stuart B. Laing
发明人： Gordon H. Phillipps , Brian M. Bain , Stuart B. Laing
IPC分类号： C07J3/00 , C07J31/00 , C07J41/00 , C07J71/00
CPC分类号： C07J31/006 , C07J3/005 , C07J41/0038 , C07J71/001 , C07J71/0015 , C07J71/0031
摘要： Androstane carbothioic acids of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a hydroxy group in the .alpha.-configuration, a methyl group which may be in either the .alpha.- or .beta.-configuration, or a methylene group;R.sup.2 represents a hydroxy or protected hydroxy group in either the .alpha.- or .beta.-configuration or an oxo group;R.sup.3 represents a hydrogen, bromine, chlorine or fluorine atom; or R.sup.2 and R.sup.3 together represent a carbon-carbon bond or an epoxy group in the .beta.-configuration;R.sup.4 represents a hydrogen or fluorine atom; and the symbol represents a single or double bond and the salts thereof are useful as intermediates in the preparation of anti-inflammatory androstane 17.beta.-carbothioate esters.The compounds of formula I are prepared by reaction of a reactive derivative of a 17.beta.-carboxylic acid corresponding to the compound of formula I with hydrogen sulphide or a sulphide or hydrosulphide salt.

6. 发明授权

US3981894A Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US3981894A
公开(公告)日：1976-09-21
申请号：US608982
申请日：1975-08-29
申请人： Gordon H. Phillipps , Brian M. Bain , John C. Clark
发明人： Gordon H. Phillipps , Brian M. Bain , John C. Clark
IPC分类号： C07J3/00
CPC分类号： C07J3/005
摘要： The specification describes new anti-inflammatory steroids having the formula ##SPC1##Wherein R.sup.1 represents a C.sub.1-4 alkyl or halo- C.sub.1-4 alkyl group, R.sup.2 represents a methyl, ethyl, n-propyl or iso-propyl group (an ethyl group being especially preferred), X represents a hydrogen, chlorine or fluorine atom and -- represents a single or double bond.The specification describes processes for the preparation of such compounds as well as pharmaceutical compositions containing these compounds.
摘要翻译：该说明书描述了具有下式的新的抗炎类固醇：其中R1表示C1-4烷基或卤代-C1-4烷基，R2表示甲基，乙基，正丙基或异丙基（特别优选的是乙基），X表示氢，氯或氟原子， - 表示单键或双键。

7. 发明授权

US4192871A Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US4192871A
公开(公告)日：1980-03-11
申请号：US907915
申请日：1978-05-22
申请人： Gordon H. Phillipps , Peter J. May , Barry E. Ayres
发明人： Gordon H. Phillipps , Peter J. May , Barry E. Ayres
IPC分类号： C07J3/00 , C07J5/00 , C07J7/00 , C07J13/00 , C07J17/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J63/00 , C07J71/00
CPC分类号： C07J13/005 , C07J17/00 , C07J3/005 , C07J31/006 , C07J41/0088 , C07J41/0094 , C07J43/003 , C07J5/0015 , C07J63/00 , C07J7/003 , C07J71/001
摘要： Pregnanes and androstanes are described which essentially possess a 3.alpha.-hydroxy group, a 5.alpha.-hydrogen atom or a 4.5- or 5,6-double bond, a 17.alpha.-hydrogen atom and an 11.beta.-aminoester group. Other optional substituents or double bonds may be present. The compounds have anaesthetic activity.
摘要翻译：描述了基本上具有3α-羟基，5α-氢原子或4.5-或5,6-双键，17α-氢原子和11β-氨基酯基团的孕烷和雄甾烷基。可以存在其它任选的取代基或双键。该化合物具有麻醉活性。

8. 发明授权

US4835158A Isoquinoline derivatives 失效
标题翻译：异喹啉衍生物
公开(公告)号：US4835158A
公开(公告)日：1989-05-30
申请号：US120654
申请日：1987-11-16
申请人： Gordon H. Phillipps , Stanley F. Dyke , Esme J. Bailey , Peter D. Howes , David I. C. Scopes
发明人： Gordon H. Phillipps , Stanley F. Dyke , Esme J. Bailey , Peter D. Howes , David I. C. Scopes
IPC分类号： C07D471/04 , C07D471/14
CPC分类号： C07D471/04 , C07D471/14
摘要： Pharmaceutical compositions for combatting cancer comprising a compound of formula (I) ##STR1## (wherein R.sup.1 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl group;R.sup.2 represents a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group;R.sup.3 represents a hydrogen atom, or (when R.sup.2 is other than a hydrogen atom) optionally a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group, or R.sup.2 and R.sup.3 together represent a methylenedioxy group;R.sup.4 represents a hydrogen or halogen atom or a C.sub.1-3 alkyl group or a phenyl group optionally substituted by a halogen atom or a hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group; and the ring A represents a group of formula ##STR2## where R.sup.5 and R.sup.6 each represent a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group,R.sup.7 and R.sup.8 each represents a hydrogen atom or a methyl group, and one of X, X.sup.1, X.sup.2 and X.sup.3 represents a nitrogen atom and the others represent --CH-- groups; with the proviso that where Arepresents a group of formula (i) at least one of R.sup.1 to R.sup.6 represents other than a hydrogen atom) together with at least one pharmaceutical carrier or excipient.
摘要翻译：包括式（I）化合物（I）（其中R1表示氢原子或C1-4烷基，C2-4烯基或C2-4炔基; R2表示氢原子或羟基，C 1-4烷氧基或C 2-4烷酰氧基; R 3表示氢原子，或（当R 2不是氢原子时）任选的羟基，C 1-4烷氧基或C 2-4烷酰氧基，或R 2和R 3 一起代表亚甲二氧基; R4代表氢或卤原子或C1-3烷基或任选被卤素原子或羟基，C1-4烷基，C1-4烷氧基或C1-4烷酰氧基取代的苯基; 并且环A表示式为“IMAGE”的基团，其中R 5和R 6各自表示氢原子或羟基，C 1-4烷氧基或C 1-4烷酰氧基，R 7和R 8各自表示氢原子或甲基， X，X 1，X 2和X 3中的一个表示氮原子，其余的表示-CH-基团;条件是其中A代表（i）R 1至R 6中的至少一个表示除氢原子以外的基团）以及至少一种药物载体或赋形剂。

9. 发明授权

US4515786A 11.alpha.-Amino-androstanes 失效
标题翻译： 11α-氨基 - 雄甾烷
公开(公告)号：US4515786A
公开(公告)日：1985-05-07
申请号：US509667
申请日：1983-06-30
申请人： Gordon H. Phillipps , David C. Humber , George B. Ewan , Barry A. Coomber
发明人： Gordon H. Phillipps , David C. Humber , George B. Ewan , Barry A. Coomber
IPC分类号： A61K31/56 , A61P9/06 , C07J41/00 , C07J63/00 , C07J3/00
CPC分类号： C07J63/008 , C07J41/0005 , C07J41/0011
摘要： R.sup.3 is a C.sub.1-6 alkyl group or a C.sub.3-7 cycloalkyl group; andR.sup.4 is a group --OR.sup.5 or --OCOR.sup.6 whereR.sup.5 is an optionally substituted alkyl or alkenyl group which may contain up to 6 carbon atoms, an optionally substituted C.sub.3-7 cycloalkyl group, a phenyl group or a carbon-attached 5-7 membered heterocyclic ring in which the hetero-atom is selected from nitrogen, oxygen and sulphur, andR.sup.6 is a hydrogen atom or a group R.sup.5 as defined above;provided that when the compounds contain a 5.beta.-hydrogen atom, R.sup.2 is a hydrogen atom and salts thereof, which compounds have activity as antidysthythmic agents.
摘要翻译：（I）其中R1是C1-8烷基或C3-7环烷基; R2是氢原子，C1-6烷氧基或C2-5烷酰氧基; R3是C1-6烷基或C3-7环烷基; 并且R 4是基团-OR 5或-OCOR 6，其中R 5是可以含有至多6个碳原子的任选取代的烷基或烯基，任选取代的C 3-7环烷基，苯基或连接碳的5-7元杂环选自氮，氧和硫，R6是氢原子或如上定义的基团R5; 条件是当化合物含有5个β-氢原子时，R2是氢原子及其盐，该化合物具有作为抗心律失常药的作用。

10. 发明授权

US4451405A 11.alpha.-Amino-3.beta.-hydroxy-androstanes 失效
标题翻译： 11α-氨基-3β-羟基 - 雄甾烷
公开(公告)号：US4451405A
公开(公告)日：1984-05-29
申请号：US447190
申请日：1982-12-06
申请人： Gordon H. Phillipps , David C. Humber , David B. Ewan , Barry A. Coomber
发明人： Gordon H. Phillipps , David C. Humber , David B. Ewan , Barry A. Coomber
IPC分类号： A61K31/56 , A61P9/06 , A61P9/10 , C07J41/00 , C07J63/00
CPC分类号： C07J41/0005 , C07J41/0011 , C07J63/008
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group, and R.sup.2 is a C.sub.1-6 alkyl group or a C.sub.3-6 cycloalkyl group and the D-homo analogues thereof having the group --CO.sub.2 R.sup.2 (wherein R.sup.2 is as defined above) at the 17.alpha..beta.-position, and acid addition salts thereof have activity as antidysthythmic agents and may be applicable for the treatment of dysrthymias in humans or animals. The compounds may be provided in the form of compositions in admixture with pharmaceutical carriers and excipients and may be prepared by a variety of processes known for producing steroids of this type. The invention also provides intermediates for the preparation of the compounds of formula (I) wherein R.sup.2 and/or R.sup.1 are replaced with hydrogen atoms, and processes for the preparation of such intermediates.
摘要翻译：式（I）的化合物，其中R 1为C 1-8烷基或C 3-7环烷基，R 2为C 1-6烷基或C 3-6环烷基，且其D同系物为在17αβ位具有-CO 2 R 2基团（其中R 2如上定义），其酸加成盐具有作为抗心律不齐剂的活性，并且可用于治疗人或动物中的dysrthymias。化合物可以以与药物载体和赋形剂混合的组合物的形式提供，并且可以通过已知用于生产这种类固醇的各种方法制备。本发明还提供制备其中R 2和/或R 1被氢原子代替的式（I）化合物的中间体，以及制备这种中间体的方法。

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