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公开(公告)号：US4186204A
公开(公告)日：1980-01-29
申请号：US8649
申请日：1979-02-01
IPC分类号： C07D231/38 , C07D231/40 , C07D233/88 , C07D249/06 , C07D249/14 , C07D257/06 , A61K31/41 , C07D257/04
CPC分类号： C07D231/38 , C07D231/40 , C07D233/88 , C07D249/06 , C07D249/14 , C07D257/06 , Y10S514/826
摘要： Acylamino tetrazolyl compounds having anti-allergic activity, methods of making the compounds and pharmaceutical formulations containing the compounds.
摘要翻译： 具有抗过敏活性的酰氨基四唑基化合物，制备该化合物的方法和含有该化合物的药物制剂。
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公开(公告)号：US4166123A
公开(公告)日：1979-08-28
申请号：US691742
申请日：1976-06-01
IPC分类号： C07D247/02 , C07D231/12 , C07D231/38 , C07D231/40 , C07D233/88 , C07D249/02 , C07D249/06 , C07D249/14 , C07D257/04 , C07D257/06 , A61K31/415 , C07D231/50
CPC分类号： C07D231/38 , C07D231/40 , C07D233/88 , C07D249/06 , C07D249/14 , C07D257/06 , Y10S514/826
摘要： Acylamino pyrazolyl compounds of the formula: ##STR1## wherein Ar represents an optionally substituted pyrazolyl group, the acylamino group --NR.sup.1 COR.sup.2 being attached to a carbon atom of the pyrazolyl ring, which have anti-allergic activity, methods of making the compounds and pharmaceutical formulations containing the compounds.
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公开(公告)号：US4513005A
公开(公告)日：1985-04-23
申请号：US386570
申请日：1982-06-09
IPC分类号： C07B45/04 , C07C317/46 , C07C323/22 , C07C323/56 , C07C323/58 , C07D303/40 , C07D303/42 , C07D307/38 , C07D309/12 , C07D309/30 , C07D313/04 , C07F9/53 , C07K5/06 , C07C149/20 , A61K31/23 , A61K31/335
CPC分类号： C07D307/38 , C07B45/04 , C07C317/46 , C07C323/22 , C07C323/56 , C07C323/58 , C07D303/40 , C07D303/42 , C07D309/12 , C07D309/30 , C07D313/04 , C07F9/5304 , C07F9/5325 , C07K5/06034
摘要： There are described pharmacologically active compounds, useful in the treatment of allergic/inflammatory disorders involving SRS-A as causal mediator and which, in free acid form, are of formula I, ##STR1## in which R.sub.1 is (i) an aliphatic, saturated or unsaturated hydrocarbyl radical of up to 20 carbon atoms, unsubstituted or substituted by at least one substituent selected from halogen, hydroxy, C.sub.3-6 alkoxy, C.sub.3-6 cycloalkyl, aryl or heteroaryl, the cycloalkyl, aryl or heteroaryl being unsubstituted or substituted by at least one substituent selected from hydroxy, halogen and alkyl, alkenyl or alkynyl of up to 10 carbon atoms,(ii) cycloalkyl of 3 to 8 carbon atoms unsubstituted or substituted by alkyl, alkenyl or alkynyl of up to 16 carbon atoms, or(iii) aryl or heteroaryl, unsubstituted or substituted by hydroxyl, C.sub.1-4 alkoxy, halogen or alkyl, alkenyl or alkynyl of up to 16 carbon atoms; and R.sub.2 is(i) alkyl, cycloalkyl or alkenyl of up to 10 carbon atoms, unsubstituted or substituted by one or more substituents selected from aryl, cycloalkyl, halogen, hydroxy, NHR.sub.3 and COX, where R.sub.3 is H, C.sub.1-4 alkyl, aryl or an amino acid residue or COX, and X is OH, C.sub.1-4 alkyl, NH.sub.2 or an amino acid residue, or(ii) aryl or heteroaryl, unsubstituted or substituted by one or more substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 acyl, halogen, hydroxy, carboxy, nitro, trihalomethyl, phenyl, C.sub.1-4 acylamino and NHR.sub.4, where R.sub.4 is hydrogen or C.sub.1-4 alkyl; and Y is --S--, --SO-- or --SO.sub.2 --,with the proviso that when --YR.sub.2 is glutathionyl, cysteinyl or cysteinylglycinyl, then R.sub.1 is other than an unsubstituted alkatetraenyl or alkapentaenyl radical of 12 to 16 carbon atoms.
摘要翻译： 描述了用于治疗涉及SRS-A作为因果介质的过敏性/炎症性疾病，其游离酸形式为式I的化学活性化合物，其中R 1是（i）脂族， 至少20个碳原子的饱和或不饱和烃基，未被取代或被至少一个选自卤素，羟基，C 3-6烷氧基，C 3-6环烷基，芳基或杂芳基的取代基取代，环烷基，芳基或杂芳基是未取代或取代的 至少一个选自羟基，卤素和至多10个碳原子的烷基，烯基或炔基的取代基，（ii）未被取代或被至多16个碳原子的烷基，烯基或炔基取代的3至8个碳原子的环烷基，或 （iii）未被取代或被羟基，C 1-4烷氧基，卤素或至多16个碳原子的烷基，链烯基或炔基取代的芳基或杂芳基; 并且R 2是（i）至少10个碳原子的烷基，环烷基或链烯基，未被取代或被一个或多个选自芳基，环烷基，卤素，羟基，NHR 3和COX的取代基取代，其中R 3是H，C 1-4烷基， 芳基或氨基酸残基或COX，X为OH，C 1-4烷基，NH 2或氨基酸残基，或（ii）未被取代或被一个或多个选自C 1-4烷基，C 1 -4-烷氧基，C 2-5酰基，卤素，羟基，羧基，硝基，三卤甲基，苯基，C 1-4酰基氨基和NHR 4，其中R 4是氢或C 1-4烷基; 并且Y是-S-，-SO-或-SO 2 - ，条件是当-YR 2是谷胱甘肽基，半胱氨酰基或半胱氨酰甘氨酰基时，则R 1不同于未被取代的具有12至16个碳原子的烷基四烯基或烷基五烯基。
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公开(公告)号：USRE32196E
公开(公告)日：1986-07-01
申请号：US379793
申请日：1982-05-19
IPC分类号： C07D307/88 , A61K31/34 , A61K31/343 , A61P11/00 , C07C45/63 , C07C65/40 , C07D257/04 , C07D307/83 , C07D307/92 , C07D317/30 , C07D405/10
CPC分类号： C07D257/04 , C07C45/63 , C07C65/40 , C07D307/83 , C07D307/92 , C07D317/30
摘要： Substituted aurones of formula (I): ##STR1## wherein R.sup.1, R.sup.2 R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and can each represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.3-8 cycloalkyl, optionally substituted phenyl, C.sub.1-6 haloalkyl, amido, amino, cyano, hydroxy, nitro, C.sub.2-4 alkenyl, carboxyl, tetrazol-5-yl and --CH.dbd.CHCOOH; orwherein R.sup.1 and R.sup.2 taken together can represent a group of formula --CH.dbd.CH--CH.dbd.CH-- provided that at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is carboxyl, tetrazol-5-yl or --CH.dbd.CHCOOH;or a pharmaceutically-acceptable salt or ester thereof, are effective in the prophylactic chemotherapy of allergic conditions such as bronchial asthma.
摘要翻译： AURONE DERIVAT IVES式（I）的取代的噢：其中R 1，R 2，R 3，R 4，R 5和R 6相同或不同并且各自表示氢，卤素，C 1-6烷基，C 1-6 烷氧基，C 3-8环烷基，任选取代的苯基，C 1-6卤代烷基，酰氨基，氨基，氰基，羟基，硝基，C 2-4烯基，羧基，四唑-5-基和-CH_CHCOOH; 或者其中R 1和R 2一起可以表示式-CH-CH-CH-CH-基团，条件是R 17，R 3，R 4，R 5和R 6中的至少一个是羧基，四唑-5-基或-CH = CICOOH; 或其药学上可接受的盐或酯在过敏性疾病例如支气管哮喘的预防性化学疗法中是有效的。
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公开(公告)号：US4241073A
公开(公告)日：1980-12-23
申请号：US39075
申请日：1979-05-14
IPC分类号： A61K31/415 , A61K31/4166 , A61P3/06 , A61P11/06 , A61P37/00 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/78 , C07D233/96 , C07D405/06 , C07D409/06
CPC分类号： C07D233/96 , C07D233/74 , C07D233/76 , C07D233/78 , Y10S514/826
摘要： Novel hydantoin compounds are described of the formula (I): ##STR1## wherein Ar is phenyl optionally substituted by up to three radicals selected from the group comprising C.sub.1-6 alkoxy, halogen, 1,3-dioxol-2-yl, hydroxy C.sub.1-4 alkoxy C.sub.1-4 alkyl, phenyl, hydroxyl, nitrile, C.sub.1-4 haloalkyl, C.sub.1-4 alkyl, C.sub.2-4 alkenyloxy, C.sub.1-4 alkoxycarbonyl or phenoxy optionally substituted by C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy or halogen;or is thiophene optionally substituted by phenyl or by one or two C.sub.1-4 alkyl groups;R.sup.1 and R.sup.2 are independently hydrogen or taken together represent a chemical bond;R.sup.3 is hydrogen, C.sub.1-6 alkyl or C.sub.2-4 alkenyl; andR.sup.4 is C.sub.1-6 alkyl, C.sub.2-4 alkenyl, phenyl or benzyl;provided that R.sup.3 cannot be hydrogen when Ar is unsubstituted phenyl and R.sup.4 is n-butyl. The compounds are useful in the treatment of immediate hypersensitivity diseases including asthma.
摘要翻译： 描述了式（I）的新型乙内酰脲化合物：其中Ar是任选被至多三个选自下列的基团取代的苯基：C 1-6烷氧基，卤素，1,3-二氧杂环戊烯-2-基 ，羟基C 1-4烷氧基C 1-4烷基，苯基，羟基，腈，C 1-4卤代烷基，C 1-4烷基，C 2-4链烯氧基，C 1-4烷氧基羰基或任选被C 1-4卤代烷基取代的苯氧基，C 1-4烷氧基 或卤素; 或任选被苯基或被一个或两个C 1-4烷基取代的噻吩; R1和R2独立地为氢或一起代表化学键; R3是氢，C1-6烷基或C2-4链烯基; R4为C1-6烷基，C2-4烯基，苯基或苄基; 条件是当Ar为未取代的苯基且R 4为正丁基时，R 3不能为氢。 该化合物可用于治疗包括哮喘在内的立即超敏反应疾病。
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公开(公告)号：US4532257A
公开(公告)日：1985-07-30
申请号：US556473
申请日：1983-11-30
IPC分类号： C07D307/83 , A61K31/34
CPC分类号： C07D307/83
摘要： There are described compounds of the formula ##STR1## in which either R.sup.1 and R.sup.2 are both hydrogen or R.sup.1 is carboxyl and R.sup.2 is hydrogen, C.sub.3-4 alkenyl or C.sub.1-4 alkyl, and R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, nitro, hydroxyl, carboxyl, carboxyC.sub.1-2 alkoxy, C.sub.3-4 alkenyl, C.sub.1-4 alkyl, C.sub.3-4 alkenyloxy, C.sub.1-4 alkoxy or the group ##STR2## where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl; and salts and esters thereof. The compounds are indicated for use in the treatment of immediate sensitivity reactions and inflammatory diseases.
摘要翻译： 描述了式“IMAGE”的化合物，其中R1和R2都是氢或R1是羧基，R2是氢，C3-4链烯基或C1-4烷基，R3，R4和R5各自是氢，硝基，羟基， 羧基，羧基C 1-2烷氧基，C 3-4烯基，C 1-4烷基，C 3-4烯氧基，C 1-4烷氧基或基团，其中R 6和R 7各自为氢或C 1-4烷基; 及其盐和酯。 该化合物用于治疗立即敏感反应和炎性疾病。
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公开(公告)号：US4293563A
公开(公告)日：1981-10-06
申请号：US148633
申请日：1980-05-12
IPC分类号： A61K31/415 , A61K31/4166 , A61P3/06 , A61P11/06 , A61P37/00 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/78 , C07D233/96 , C07D405/06 , C07D409/06
CPC分类号： C07D233/96 , C07D233/74 , C07D233/76 , C07D233/78 , Y10S514/826
摘要： Novel hydantoin compounds are described of the formula (I): ##STR1## wherein Ar is phenyl optionally substituted by up to three radicals selected from the group comprising C.sub.1-6 alkoxy, halogen, 1,3-dioxol-2-yl, hydroxy C.sub.1-4 alkoxy C.sub.1-4 alkyl, phenyl, hydroxyl, nitrile, C.sub.1-4 haloalkyl, C.sub.1-4 alkyl, C.sub.2-4 alkenyloxy, C.sub.1-4 alkoxycarbonyl or phenoxy optionally substituted by C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy or halogen;or is thiophene optionally substituted by phenyl or by one or two C.sub.1-4 alkyl groups;R.sup.1 and R.sup.2 are independently hydrogen or taken together represent a chemical bond;R.sup.3 is hydrogen, C.sub.1-6 alkyl or C.sub.2-4 alkenyl; andR.sup.4 is C.sub.1-6 alkyl, C.sub.2-4 alkenyl, phenyl or benzyl;provided that R.sup.3 cannot be hydrogen when Ar is unsubstituted phenyl and R.sup.4 is n-butyl. The compounds are useful in the treatment of immediate hypersensitivity diseases including asthma.
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公开(公告)号：US4259340A
公开(公告)日：1981-03-31
申请号：US71515
申请日：1979-08-31
IPC分类号： C07C45/63 , C07C65/40 , C07D257/04 , C07D307/83 , C07D307/92 , C07D317/30 , C07D405/02 , C07D405/10
CPC分类号： C07D257/04 , C07C45/63 , C07C65/40 , C07D307/83 , C07D307/92 , C07D317/30 , Y10S514/826
摘要： Substituted aurones of formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and can each represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.3-8 cycloalkyl, optionally substituted phenyl, C.sub.1-6 haloalkyl, amido, amino, cyano, hydroxy, nitro, C.sub.2-4 alkenyl, carboxyl, tetrazol-5-yl and --CH.dbd.CHCOOH; orwherein R.sup.1 and R.sup.2 taken together can represent a group of formula --CH.dbd.CH--CH.dbd.CH-- provided that at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is carboxyl, tetrazol-5-yl or --CH.dbd.CHCOOH;or a pharmaceutically-acceptable salt or ester thereof, are effective in the prophylactic chemotherapy of allergic conditions such as bronchial asthma.
摘要翻译： 取代的式（I）的噢：其中R 1，R 2，R 3，R 4，R 5和R 6相同或不同，各自表示氢，卤素，C 1-6烷基，C 1-6烷氧基，C 3 -8环烷基，任选取代的苯基，C 1-6卤代烷基，酰氨基，氨基，氰基，羟基，硝基，C 2-4烯基，羧基，四唑-5-基和-CH = CHCOOH; 或者其中R 1和R 2一起可以表示式-CH = CH-CH = CH-的基团，条件是R 1，R 2，R 3，R 4，R 5和R 6中的至少一个是羧基，四唑-5-基或-CH = CHCOOH; 或其药学上可接受的盐或酯在过敏性疾病例如支气管哮喘的预防性化学疗法中是有效的。
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9.发明授权Treating immediate hypersensitivity conditions with 3,5-disubstituted hydantoin derivatives 失效用3,5-二取代的乙内酰脲衍生物治疗立即超敏反应
公开(公告)号：US4230716A
公开(公告)日：1980-10-28
申请号：US39077
申请日：1979-05-14
IPC分类号： C07D233/74 , C07D233/76 , C07D233/78 , A61K31/415
CPC分类号： C07D233/76 , C07D233/74 , C07D233/78
摘要： Hydantoin compounds are described of the formula (I) : ##STR1## wherein R.sup.1 is phenyl, C.sub.1-4 hydroxyalkyl or carboxy C.sub.1-4 alkyl and wherein R.sub.2 is C.sub.1-6 alkyl. The compounds are useful in the prophylactic treatment of immediate hypersensitivity diseases including asthma.
摘要翻译： 乙内酰脲化合物描述为式（I）：其中R 1是苯基，C 1-4羟基烷基或羧基C 1-4烷基，其中R 2是C 1-6烷基。 该化合物可用于预防性治疗包括哮喘在内的立即超敏反应疾病。
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10.发明授权
公开(公告)号：US4230709A
公开(公告)日：1980-10-28
申请号：US39074
申请日：1979-05-14
IPC分类号： C07D233/74 , C07D233/96 , C07D235/02 , C07D487/04 , A61K31/445 , A61K31/415 , C07D233/58 , C07D471/04
CPC分类号： C07D235/02 , C07D233/74 , C07D233/96 , C07D487/04 , Y10S514/826
摘要： Pharmaceutical formulations are described, which comprise a hydantoin of formula (I): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl, R.sup.2 is hydrogen or C.sub.1-4 alkyl; or R.sup.1 and R.sup.2 taken together either represent a C.sub.4-6 alkylene group or a group of formula: ##STR2## where R.sup.5 and R.sup.6 independently represent hydrogen or C.sub.1-4 alkyl;R.sup.3 is C.sub.1-6 alkyl or benzyl;R.sup.4 is hydrogen or C.sub.1-6 alkyl;provided that R.sup.2 and R.sup.4 cannot both be hydrogen;or R.sup.1 and R.sup.4 taken together represent a C.sub.2-4 alkylene group;associated with a pharmaceutically-acceptable carrier therefor. The compounds, some of which are novel, are useful in the treatment of immediate hypersensitivity diseases such as asthma.
摘要翻译： 描述了药物制剂，其包含式（I）的乙内酰脲：其中R 1是C 1-4烷基，R 2是氢或C 1-4烷基; 或者R 1和R 2一起表示C4-6亚烷基或下式的基团：其中R5和R6独立地表示氢或C1-4烷基; R3是C1-6烷基或苄基; R4是氢或C1-6烷基; 条件是R2和R4不能都是氢; 或者R 1和R 4一起代表C 2-4亚烷基; 与其药学上可接受的载体相关联。 这些化合物，其中一些是新的，可用于治疗立即超敏反应性疾病如哮喘。
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