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1. 发明申请

WO1994025459A1 HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：杂环衍生物
公开(公告)号：WO1994025459A1
公开(公告)日：1994-11-10
申请号：PCT/GB1994000910
申请日：1994-04-28
申请人： ZENECA LIMITED , BROWN, George, Robert , WHITTAMORE, Paul, Robert, Owen , BRITTAIN, David, Robert
发明人： ZENECA LIMITED
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Compounds of formula (I) wherein R is hydrogen or hydroxy; R is hydrogen; or R and R are joined together so that CR -CR is a double bond; X is selected from -CH2CH2-, -CH=CH-, -CC-, -CH2O-, -OCH2-, CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -CH2S(O)n- and -S(O)nCH2- (wherein n is 0, 1 or 2); Ar is phenyl which bears one or more substituents independently selected from the groups (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-6C)alkoxy, (1-6C)alkoxycarbonyl, (1-6C)alkoxycarbonyl(1-6C)alkyl, (1-6C)alkoxy(1-6C)alkyl, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, carbamoyl, (1-6C) alkylcarbamoyl, di-[(1-6C)alkyl]carbamoyl, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oximes, (1-6C)alkylthio, (1-6C)alkylsulphinyl and (1-6C)alkylsulphonyl when substituted by one or more groups selected from (1-6C)alkoxycarbonyl, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oxime derivatives, (1-6C)alkanoylamino, (1-6C)alkanoyloxy, (1-6C)alkanoyloxy(1-6C)alkyl, carbamoyl, N-(1-6C)alkylcarbamoyl, N,N-di[(1-6C)alkyl]carbamoyl, amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, (1-6C)alkoxy, (2-6C)alkenyloxy, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, halogeno(1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, phenyl, phenoxy, cyano, nitro, hydroxy and carboxy; and wherein Ar may bear further substituents; and their pharmaceutically acceptable salts inhibit squalene synthese and are hence useful in lowering cholesterol levels in blood plasma. Processes for preparing compounds of formula (I) are also referred to as well as pharmaceutical compositions containing them and their use in medicine.
摘要翻译：式（I）的化合物，其中R 1是氢或羟基; R 2是氢; 或R 1和R 2连接在一起，使得CR 1 -CR 2是双键; X选自-CH 2 CH 2 - ， - CH = CH - ， - C - ， - CH 2 O - ， - OCH 2 - ，CH 2 NH-，-NHCH 2 - ， - CH 2 CO-，-COCH 2 - ， - CH 2 S（O） S（O）n CH 2 - （其中n为0,1或2）; Ar是含有一个或多个独立地选自（1-6C）烷基，（2-6C）烯基，（2-6C）炔基，（1-6C）烷氧基，（1-6C）烷氧羰基，（1-6C）（1-6C）烷基，（1-6C）烷氧基（1-6C）烷基，（1-6C）烷基氨基，二 - [（1-6C）烷基]氨基，氨基甲酰基，（1-6C ）烷基氨基甲酰基，二 - [（1-6C）烷基]氨基甲酰基，（1-6C）烷酰基和肟衍生物和所述肟的（1-6C）烷基醚，（1-6C）烷硫基，（1-6C ）（1-6C）烷氧基羰基，（1-6C）烷酰基及其肟衍生物和所述肟衍生物的O-（1-6C）烷基醚取代的（1-6C）烷基磺酰基，（1-6C）烷酰氨基，（1-6C）烷酰氧基，（1-6C）烷酰氧基（1-6C）烷基，氨基甲酰基，N-（1-6C）烷基氨基甲酰基，N，N-二[（1-6C）氨基，（1-6C）烷基氨基，二 - [（1-6C）烷基]氨基，（1-6C）烷氧基，（2-6C）烯氧基，（1-6C）烷硫基，（1-6C）烷基亚磺酰基，（1-6C）烷基磺酰基，卤代（1-6C）烷基，（2-6C）烯基，（2-6C）炔基，苯基，苯氧基，氰基，硝基，羟基和羧基; 并且其中Ar可以带有其它取代基; 其药学上可接受的盐抑制角鲨烯合成物，因此可用于降低血浆中的胆固醇水平。制备式（I）化合物的方法也被称为含有它们的药物组合物及其在医药中的用途。

2. 发明申请

WO0005224A3 HETEROCYCLIC DERIVATIVES AND THEIR USE AS INTEGRIN INHIBITOR 审中-公开
标题翻译：杂环衍生物及其作为整合抑制剂的用途
公开(公告)号：WO0005224A3
公开(公告)日：2001-08-09
申请号：PCT/GB9902342
申请日：1999-07-20
申请人： ASTRAZENECA AB , BRITTAIN DAVID ROBERT , JOHNSTONE CRAIG , DAVIES GARETH MORSE , LARGE MICHAEL STEWART
发明人： BRITTAIN DAVID ROBERT , JOHNSTONE CRAIG , DAVIES GARETH MORSE , LARGE MICHAEL STEWART
IPC分类号： C07D277/82 , A61K31/423 , A61K31/428 , A61K31/4427 , A61P1/00 , A61P3/10 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/14 , A61P29/00 , A61P37/06 , A61P43/00 , C07D263/58 , C07D413/04 , C07D413/12
CPC分类号： C07D263/58 , C07D413/04
摘要： Compound of formula (I) wherein: A is a bicyclic heteroaryl, optionally substituted with one or more substituents; B is linker group connecting group A to group D and comprising a 3 or 4 atom linker where each atom is independently selected from carbon, oxygen, nitrogen and sulphur and is optionally subsituted with one or more C1-6 alkyl groups or two of such adjacent alkyl substituents may form a ring; C is aryl or a mono or bicyclic heteroaryl, each of which can be optionally substituted; D is an aryl or heteroaryl, both of which are optionally substituted R is hydrogen, C1-5 alkyl, C1-3 alkanoyl or C1-3 alkoxycarbonyl; R to R are each independently selected from hydrogen, C1-6 alkyl, aryl and heteroaryl containing up to 2 heteroatoms chosen from oxygen, sulphur and nitrogen, the aryl and heteroaryl optionally substituted with C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-4 alkoxy, C1-4 alkanoyl, C1-6 alkylamino, C1-4alkylC1-6alkyoxyl, C1-6alkylaminoC1-6alkyl, nitro, cyano, halogeno, trifluoromethyl, hydroxy, (CH2)pOH where p is 1 or 2, -CO2R , and -CONR R , where R and R are independently selected from hydrogen and C1-6 alkyl or two of R to R can be taken together to form a 3 to 7 membered ring; R is an acidic functional group; r and s are each independently 0 or 1 with the proviso that r and s cannot both be 0; or a pharmaceutically acceptable salt or in vivo hydrolysable derivative thereof.
摘要翻译：式（I）化合物其中：A是任选被一个或多个取代基取代的双环杂芳基; B是连接基团A与D组并且包含3或4个原子连接体的连接基团，其中每个原子独立地选自碳，氧，氮和硫，并且任选被一个或多个C 1-6烷基取代或两个相邻的烷基取代基可以形成环; C是芳基或单或双环杂芳基，其各自可任选被取代; D是芳基或杂芳基，它们都是任选取代的R 1是氢，C 1-5烷基，C 1-3烷酰基或C 1-3烷氧基羰基; R 2至R 5各自独立地选自氢，C 1-6烷基，芳基和含有至多2个选自氧，硫和氮的杂原子的杂芳基，芳基和杂芳基任选被C 1-6烷基，C 2 C6链烯基，C2-6炔基，C1-4烷氧基，C1-4烷酰基，C1-6烷基氨基，C1-4烷基C1-6烷氧基，C1-6烷基氨基C1-6烷基，硝基，氰基，卤代，三氟甲基，羟基，（CH2）其中p为1或2，-CO 2 R a和-CONR a R b，其中R a和R b独立地选自氢和C 1-6烷基或R 2中的两个 > R 5可以一起形成3至7元环; R 6是酸性官能团; r和s各自独立地为0或1，条件是r和s不能都是0; 或其药学上可接受的盐或体内可水解的衍生物。

3. 发明申请

WO0005223A3 HETEROCYCLIC DERIVATIVES AND THEIR USE AS INTEGRIN INHIBITORS 审中-公开
标题翻译：杂环衍生物及其作为整合抑制剂的用途
公开(公告)号：WO0005223A3
公开(公告)日：2001-07-12
申请号：PCT/GB9902330
申请日：1999-07-20
申请人： ASTRAZENECA AB , BRITTAIN DAVID ROBERT , JOHNSTONE CRAIG , DAVIES GARETH MORSE , LARGE MICHAEL STEWART
发明人： BRITTAIN DAVID ROBERT , JOHNSTONE CRAIG , DAVIES GARETH MORSE , LARGE MICHAEL STEWART
IPC分类号： A61K31/423 , A61K31/428 , A61K31/4439 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/00 , A61P37/06 , C04B41/45 , C04B41/81 , C07D263/58 , C07D277/82 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/4184 , C07D235/30
CPC分类号： C07D263/58 , C04B41/009 , C04B41/4572 , C04B41/81 , C07D277/82 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C04B41/5022 , C04B41/53 , C04B33/00
摘要： Compound of formula (I) wherein: A is a bicyclic heteroaryl, optionally substituted with one or more substituents; B is aryl or a mono or bicyclic heteroaryl, each of which can be optionally subsituted with one or more subsituents; Z is -X(CR R )aCO, -NH, -CO or the group X-(CH2)bCONH (CH2)cNH where X is oxygen, sulphur, amino, alkylamino or a direct bond, R and R are independently hydrogen or C1-4 alkyl, a is an integer from 1 to 4, b is 1 or 2 and c is from 2 to 5, and; W is -NHCH(R )CO- or OC(R )CHNH where R is -CH2CH(CH3)2-CH2CH2S(CH3) or CH2CH2S(O2)(CH3); q is 0 or 1 and when q is 0 Z is linked to the group W by the formation of an amide bond between Z and Y, and when q is 1 Z is linked to the group W by the formation of an amide bond between Z and W and W is linked to the group Y by the formation of an amide bond between W and Y; Y is a fragment derived from the C-terminus of a compound which inhibits the interaction between the integrin alpha IIb beta 3 and its ligand fibrinogen; R is hydrogen, C1-5alkyl, C1-3 alkanoyl or C1-3 alkoxycarbonyl; or a pharmaceutically acceptable salt or in vivo hydrolysable derivative thereof.
摘要翻译：式（I）的化合物，其中：A是任选被一个或多个取代基取代的二环杂芳基; B是芳基或单或双环杂芳基，其各自可以任选地被一个或多个取代基取代; Z是-X（CR a R b）aCO，-NH，-CO或基团X（CH 2）b CONH（CH 2）c NH，其中X是氧，硫，氨基，烷基氨基或直接键，R α和R b独立地为氢或C 1-4烷基，a为1至4的整数，b为1或2，c为2至5。 W是-NHCH（R）CO-或OC（R））CHNH，其中R 0是-CH 2 CH（CH 3）2 -CH 2 CH 2 S（CH 3）或CH 2 CH 2 S（O 2）（CH 3）; q为0或1，当q为0时，通过在Z和Y之间形成酰胺键将Z连接于基团W，当q为1时，Z通过在Z W和W通过在W和Y之间形成酰胺键与基团Y连接; Y是衍生自抑制整合素αIIbβ3与其配体纤维蛋白原之间相互作用的化合物的C末端的片段; R 1是氢，C 1-5烷基，C 1-3烷酰基或C 1-3烷氧基羰基; 或其药学上可接受的盐或体内可水解的衍生物。

4. 发明申请

WO9924398A3 UREA DERIVATIVES AND THEIR USE AS INTEGRIN INHIBITORS 审中-公开
标题翻译：尿素衍生物及其作为INTEGRIN抑制剂的用途
公开(公告)号：WO9924398A3
公开(公告)日：1999-08-05
申请号：PCT/GB9803334
申请日：1998-11-09
申请人： ZENECA LTD , BRITTAIN DAVID ROBERT , JOHNSTONE CRAIG
发明人： BRITTAIN DAVID ROBERT , JOHNSTONE CRAIG
IPC分类号： C07D317/58 , A61K31/22 , A61K31/357 , A61K31/36 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , C07C275/34 , C07D317/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07K5/06 , A61K31/195 , A61K31/41 , C07C317/50 , C07C323/60 , C07D317/60 , C07K5/02
CPC分类号： C07D405/12 , C07C275/34 , C07D317/12 , C07D407/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (II) where R is in the para or meta position and is (A); R and R are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6alkylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, -CO2R and -CONR R , where R and R are independently selected from hydrogen or C1-6alkyl, or R and R together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R is C1-4alkyl; R is selected from hydrogen and C1-4alkyl; R is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R is halogeno; R is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halogeno, and trifluoromethyl; R is aryl, heteroaryl, a bicyclic heteroaryl ring system linked to the nitrogen via a ring carbon or a 9 or 10 membered bicyclic ring system linked to the nitrogen via a ring carbon and each ring is optionally substituted with up to two substituents, which may be the same or different, and are selected from C1-6alkyl, C1-4alkoxy, C1-4alkylthio, C1-6alkylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, hydroxy, -CO2H, -(CH2)pOH where p is 1 or 2, cyano, halogeno, and trifluoromethyl; R and R are each independently selected from hydrogen and C1-4alkyl or R and R together with the nitrogen to which they are attached form a dihydroindolyl, or a dihidroquinolinyl group; R is selected from carboxyl, tetrazolyl, alkyl sulphonylcarbamyl, sulfo and sulfino; Y is oxygen, sulphur or sulfonyl; m is 0 or 1; and n is 0 or an integer from 1 to 4 with the proviso that when m and n cannot both be 0 and when m is 1, n is 0; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. The compounds inhibit the interaction of vascular cell-adhesion molecule-1 and fibronectin with integrin very late antigen 4 ( alpha 4 beta 1). They have therapeutic applications such as in multiple sclerosis, rheumatoid arthritis, asthma, coronary artery disease and psoriasis.
摘要翻译：其中R 1为对位或间位且为（A）的式（II）化合物; R 2和R 3各自独立地选自氢，硝基，C 1-6烷基，C 3-6环烷基，C 2-6烯基，C 2-6炔基，C 1-4烷氧基，C 1-6烷基氨基，C 1-6二烷基氨基，C 1-6烷基C 1- 4-烷氧基，C 1-6烷基氨基C 1-6烷基，氨基，氰基，卤代，三氟甲基，-CO 2 R 12和-CONR 12 R 13，其中R 12和R 13独立地选自氢或C1- 6烷基或R 2和R 3与它们所连接的苯基一起形成9或10元双环体系; R 4是C 1-4烷基; R 5选自氢和C 1-4烷基; R 6选自C 1-6烷基，C 1-4烷基（C 4-6）环烷基，C 1-6烷基（C 1-6）烷氧基，C 1-6烷基S（C 1-6）烷基，C 1-4烷基磺酰基（C 1-4）烷基 ; （B）其中q是1至6的整数，R 14是卤素; R 7选自C 1-6烷基，C 1-8烷氧基羰基，C 2-6烯基，1,3-苯并间二氧杂环戊烯-5-基和芳基，各自任选被一个或多个选自C 1-4烷氧基，C 1-6烷基，氰基，卤代和三氟甲基; R 8是芳基，杂芳基，通过环碳与氮连接的双环杂芳基环系统，或通过环碳与氮连接的9或10元双环系统，并且每个环任选被至多两个取代基取代，其可以相同或不同，并且选自C 1-6烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-6烷基C 1-4烷氧基，C 1-6烷基氨基C 1-6烷基，羟基，-CO 2 H， - （CH 2）p OH，其中p为 1或2，氰基，卤代和三氟甲基; R 9和R 10各自独立地选自氢和C 1-4烷基或R 8和R 9与它们所连接的氮一起形成二氢吲哚基或二杀喹啉基; R 11选自羧基，四唑基，烷基磺酰基氨基甲酰基，磺基和亚磺酰基; Y是氧，硫或磺酰基; m为0或1; 并且n为0或1至4的整数，条件是当m和n不能均为0时，当m为1时，n为0; 或其药学上可接受的盐或体内可水解的酯。该化合物抑制血管细胞粘附分子-1和纤连蛋白与整合素非常晚的抗原4（α4β1）的相互作用。它们具有治疗应用，例如多发性硬化，类风湿性关节炎，哮喘，冠状动脉疾病和牛皮癣。

5. 发明申请

WO1995035295A1 QUINUCLIDINE DERIVATIVES AS SQUALENE SYNTHASE INHIBITORS 审中-公开
标题翻译：喹啉衍生物作为平均合成酶抑制剂
公开(公告)号：WO1995035295A1
公开(公告)日：1995-12-28
申请号：PCT/GB1995001362
申请日：1995-06-12
申请人： ZENECA LIMITED , BROWN, George, Robert , WHITTAMORE, Paul, Robert, Owen , BRITTAIN, David, Robert
发明人： ZENECA LIMITED
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Compounds of formula (I) wherein R is hydrogen or hydroxy; R is hydrogen; or R and R are joined together so that CR -CR is a double bond; X is selected from -CH2CH2-, -CH = CH-, -C = C-, -CH2O-, -CH2NH-, -NHCH2-, -CH2CO-, -COOH2-, -CH2S(O)n- and -S(O)nCH2- (wherein n is 0,1 or 2); Ar is phenyl which bears one or more substituents independently selected from the groups alkyl, alkenyl, alkynyl, alkoxy, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxyalkyl, alkylamino, di-[alkyl]amino, carbamoyle, alkylcarbamoyl, di-[alkyl]carbamoyl, alkanoyl and oxime derivatives thereof and 0-alkyl ethers of said oximes, alkylthio, alkylsulphinyl and alkylsulphonyl when substituted by one or more groups selected from heterocyclyl, heterocyclyloxy and heterocyclyloxycarbonyl; or Ar is phenyl which bears one or more heterocyclyloxy groups; and wherein Ar and/or a phenyl or heterocyclyl moiety in any of said groups mentioned above may further be substituted; and their pharmaceutically acceptable salts inhibits squalene synthase and are hence useful in lowering cholesterol levels in blood plasma. Processes for preparing compounds of formula (I) are also referred to as well as pharmaceutical compositions containing them and their use in medicine.
摘要翻译：式（I）的化合物，其中R 1是氢或羟基; R 2是氢; 或R 1和R 2连接在一起，使得CR 1 -CR 2是双键; X选自-CH 2 CH 2 - ， - CH = CH - ， - C = C - ， - CH 2 O - ， - CH 2 NH - ， - NHCH 2 - ， - CH 2 CO-，-COOH 2 - ， - CH 2 S（O）（O）nCH 2 - （其中n为0,1或2）; Ar是具有一个或多个独立地选自烷基，烯基，炔基，烷氧基，烷氧基羰基，烷氧基羰基烷基，烷氧基烷基，烷基氨基，二 - [烷基]氨基，氨基甲酰基，烷基氨基甲酰基，二 - （烷基）氨基甲酰基，烷酰基和当被一个或多个选自杂环基，杂环氧基和杂环氧基羰基的基团取代时，所述肟，烷硫基，烷基亚磺酰基和烷基磺酰基的O-烷基醚; 或Ar是含有一个或多个杂环氧基的苯基; 并且其中Ar和/或上述任何一个基团中的苯基或杂环基部分可以进一步被取代; 其药学上可接受的盐抑制角鲨烯合酶，因此可用于降低血浆中的胆固醇水平。制备式（I）化合物的方法也被称为含有它们的药物组合物及其在医药中的用途。

6. 发明申请

WO1994005660A1 QUINUCLIDINE DERIVATIVES AS SQUALENE SYNTHASE INHIBITORS 审中-公开
标题翻译：喹啉衍生物作为平均合成酶抑制剂
公开(公告)号：WO1994005660A1
公开(公告)日：1994-03-17
申请号：PCT/GB1993001802
申请日：1993-08-24
申请人： ZENECA LIMITED , BROWN, George, Robert , MALLION, Keith, Blakeney , WHITTAMORE, Paul, Robert, Owen , BRITTAIN, David, Robert
发明人： ZENECA LIMITED
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts in which R is hydrogen or hydroxy; R is hydrogen; or R and R are joined together so that CR -CR is a double bond; X is selected from -CH2CH2-, -CH=CH-, -C=C-, -CH2O-, -CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -CH2S- and -SCH2-; Ar is a phenylene moiety; Ar is a heteroaryl moiety; and wherein one or both of Ar and Ar may optionally bear one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogeno-alkyl, carboxyalkyl and alkanoylamino; provided that when R is hydroxy, X is not selected from -NHCH2- and -SCH2-; are inhibitors of squalene synthase and hence useful in treating medical conditions in which a lowering of cholesterol is beneficial, such as hypercholesterolemia and atherosclerosis. Processes for preparing these derivatives, pharmaceutical compositions containing them are also described together with their use in medicine.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中R 1是氢或羟基; R 2是氢; 或R 1和R 2连接在一起，使得CR 1 -CR 2是双键; X选自-CH 2 CH 2 - ， - CH = CH - ， - C = C - ， - CH 2 O - ， - CH 2 NH - ， - NHCH 2 - ， - CH 2 CO-，-COCH 2 - ， - CH 2 S-和-SCH 2 - Ar 1是亚苯基; Ar 2是杂芳基部分; 并且其中Ar 1和Ar 2中的一个或两个可任选地具有一个或多个独立地选自卤素，羟基，氨基，硝基，氰基，羧基，氨基甲酰基，烷基，烯基，炔基，烷氧基，烷基氨基，二 - 烷基氨基，N-烷基氨基甲酰基，二-N，N-烷基氨基甲酰基，烷氧基羰基，烷硫基，烷基亚磺酰基，烷基磺酰基，卤代 - 烷基，羧基烷基和烷酰基氨基; 条件是当R 1是羟基时，X不选自-NHCH 2 - 和-SCH 2 - ; 是角鲨烯合酶的抑制剂，因此可用于治疗胆固醇降低有益的医学病症，例如高胆固醇血症和动脉粥样硬化。制备这些衍生物的方法，含有它们的药物组合物也与其在医药中的用途一起被描述。

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