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1. 发明申请

WO1998006705A1 SUBSTITUTED PYRIMIDINE DERIVATIVES AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：取代的吡嗪衍生物及其药物用途
公开(公告)号：WO1998006705A1
公开(公告)日：1998-02-19
申请号：PCT/GB1997002029
申请日：1997-07-25
申请人： ZENECA LIMITED , BROWN, George, Robert , NEWCOMBE, Nicholas, John , STOKES, Elaine, Sophie, Elizabeth , WATERSON, David
发明人： ZENECA LIMITED
IPC分类号： C07D239/42
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14 , C07D413/14
摘要： This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.
摘要翻译：本发明涉及可用于抑制氧化 - 角鲨烯环化酶，其制备方法和含有它们的药物组合物的杂环衍生物。本发明还涉及能够抑制胆固醇生物合成并因此降低血浆中胆固醇水平的杂环衍生物。本发明还涉及在诸如高胆固醇血症和动脉粥样硬化的疾病和医学病症中使用这种杂环衍生物的方法。

2. 发明申请

WO1997006802A1 USE OF OXIDO-SQUALENE CYCLASE INHIBITORS TO LOWER BLOOD CHOLESTEROL 审中-公开
标题翻译：氧化环磷酰胺抑制剂降低胆固醇的用途
公开(公告)号：WO1997006802A1
公开(公告)日：1997-02-27
申请号：PCT/GB1996001985
申请日：1996-08-14
申请人： ZENECA LIMITED , BROWN, George, Robert , STOKES, Elaine, Sophie, Elisabeth , WATERSON, David , WOOD, Robin
发明人： ZENECA LIMITED
IPC分类号： A61K31/495
CPC分类号： C07D401/04 , A61K31/496 , A61K31/506 , C07D401/14 , C07D409/14 , C07D413/14
摘要： A compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein G, T , T and T are selected from CH and N; provided that T and T are not both CH; A is selected from a direct bond and (1-4C)alkylene; X is selected from oxy, thio, sulphinyl, sulphonyl, carbonyl, carbonylamino, N-di-(1-6C)alkylcarbonylamino, sulphonamido, methylene, (1-4C)alkylmethylene and di-(1-6C)alkylmethylene, and when T is CH, X may also be selected from aminosulphonyl and oxycarbonyl; and Q is selected from (5-7C)cycloalkyl, a heterocyclic moiety containing up to 4 heteroatoms selected from nitrogen, oxygen and sulphur; phenyl, naphthyl, phenyl(1-4C)alkyl and phenyl(2-6C)alkenyl; for the manufacture of a medicament for treating diseases or medical conditions in which an inhibition of oxido-squalene cyclase is desirable.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中G，T 1，T 2和T 3选自CH和N; 条件是T 2和T 3不都是CH; A选自直接键和（1-4C）亚烷基; X选自氧基，硫基，亚磺酰基，磺酰基，羰基，羰基氨基，N-二（1-6C）烷基羰基氨基，磺酰氨基，亚甲基，（1-4C）烷基亚甲基和二 - （1-6C）烷基亚甲基，当T <2>是CH，X也可以选自氨基磺酰基和氧羰基; 并且Q选自（5-7C）环烷基，含有至多4个选自氮，氧和硫的杂原子的杂环部分; 苯基，萘基，苯基（1-4C）烷基和苯基（2-6C）烯基; 用于制备治疗需要抑制氧化 - 角鲨烯环化酶的疾病或医学病症的药物。

3. 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。

4. 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。

5. 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。

6. 发明申请

WO1993021184A1 BIPHENYLYLQUINUCLIDINE DERIVATIVES AS SQUALENE SYNTHASE INHIBITORS 审中-公开
标题翻译：联苯胺衍生物作为平均合成酶抑制剂
公开(公告)号：WO1993021184A1
公开(公告)日：1993-10-28
申请号：PCT/GB1993000754
申请日：1993-04-08
申请人： HARRISON, Alison +hf , ZENECA LIMITED , BROWN, George, Robert , MALLION, Keith, Blakeney
发明人： HARRISON, Alison +hf , ZENECA LIMITED , HARRISON, Peter, John +di
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Biphenylylquinuclidine derivatives of Formula (I): Q-Ar -Ar , in which Q is of Formula (Ia) or (Ib), in which R and R are independently selected from hydrogen, alkyl, halogeno and hydroxy; or R and R when taken together define an oxo group; Xb is selected from -CH2-, =CH- and -CH(OH); Xa is selected from -CH2-, =CH-, CO, -O-, and -S(O)n (wherein n = 0, 1 or 2); Ar is a phenylene moiety; Ar is phenyl; and wherein one or both of Ar and Ar is optionally unsubstituted or substituted by one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-carbamoyl, N,N-di-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogeno-alkyl, alkanoyl and alkanoylamino; and their pharmaceutically acceptable salts are inhibitors of squalene synthase and hence useful in treating diseases and medical conditions in which a lowering of cholosterol is desirable. The use of these derivatives in medicine is disclosed together with novel compounds, processes for their preparation and pharmaceutical composition containing them.
摘要翻译：式（I）的联苯亚基奎宁环衍生物：Q-Ar 1 -Ar 2，其中Q为式（Ia）或（Ib），其中R 1和R 2独立地选自氢，烷基，卤代和羟基; 或R 1和R 2一起定义氧代基团; Xb选自-CH 2 - ，= CH-和-CH（OH）; Xa选自-CH 2 - ，= CH-，CO，-O-和-S（O）n（其中n = 0,1或2）; Ar 1是亚苯基; Ar 2是苯基; 并且其中Ar 1和Ar 2之一或两者任选未被取代或被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-氨基甲酰基，N，N-二烷基氨基甲酰基，烷氧基羰基，烷硫基，烷基亚磺酰基，烷基磺酰基，卤代 - 烷基，烷酰基和烷酰基氨基; 其药学上可接受的盐是角鲨烯合酶的抑制剂，因此可用于治疗需要降低胆甾醇的疾病和医学病症。这些衍生物在药物中的使用与新化合物，其制备方法和含有它们的药物组合物一起公开。

7. 发明申请

WO1993020807A1 AMINES AS INHIBITORS OF SQUALENE SYNTHASE 审中-公开
标题翻译：作为平均合成酶的抑制剂的氨基酸
公开(公告)号：WO1993020807A1
公开(公告)日：1993-10-28
申请号：PCT/GB1993000742
申请日：1993-04-08
申请人： HARRISON, Alison +hf , ZENECA LIMITED , BROWN, George, Robert , EAKIN, Murdoch, Allan , MALLION, Keith, Blakeney
发明人： HARRISON, Alison +hf , ZENECA LIMITED , HARRISON, Peter, John +di
IPC分类号： A61K31/135
CPC分类号： C07D295/088 , A61K31/135 , C07C217/18 , C07C217/20 , C07C217/22 , C07C233/25 , C07C235/34 , C07C251/48 , C07C255/54 , C07C275/34 , C07C311/29 , C07C317/22 , C07C323/20 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , Y10S514/824
摘要： Compounds of formula (I), and their pharmaceutically acceptable salts, in which R and R are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR R is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthase and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中R 1和R 2是氢，烷基，环烷基，环烷基烷基，苯基烷基或烯基; 或NR 1 R 2是杂环基; A是任选被烷基取代的三亚甲基，苯环任选被取代基如卤代，烯基，氨基，氰基，脲基，烷基，氨基甲酰基烷基，烷酰基氨基，烷氧基羰基，N-烷基 - 烷酰基氨基，烷酰基及其胺取代; 是角鲨烯合酶的抑制剂，因此可用于治疗胆固醇降低的疾病。除了在医药中使用这些化合物之外，还提及了新化合物，其制备方法和药物组合物。

8. 发明申请

WO1997028128A1 HETEROCYCLIC COMPOUNDS USEFUL AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：杂环化合物作为药物代用品有用
公开(公告)号：WO1997028128A1
公开(公告)日：1997-08-07
申请号：PCT/GB1997000282
申请日：1997-01-31
申请人： ZENECA LIMITED , BROWN, George, Robert , STOKES, Elaine, Sophie, Elizabeth , WATERSON, David , WOOD, Robin , WATKINS, William, John , NEWCOMBE, Nicholas, John , CUMMING, John, Graham
发明人： ZENECA LIMITED
IPC分类号： C07D213/74
CPC分类号： C07D239/42 , C07D213/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： Compounds of formula (I) in which all variables are defined in the description and their salts inhibit the enzyme oxido squalene cyclase and are useful in treating hypercholesterolemia and also as anti-fungal agents. Processes for their preparation are also described together with their use in medicine.
摘要翻译：其中所有变量在说明书中定义的式（I）化合物及其盐抑制酶氧化角鲨烯环化酶，并且可用于治疗高胆固醇血症，也可用作抗真菌剂。还描述了其制备方法及其在医学中的应用。

9. 发明申请

WO1994014804A1 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：WO1994014804A1
公开(公告)日：1994-07-07
申请号：PCT/GB1993002616
申请日：1993-12-21
申请人： ZENECA LIMITED , BROWN, George, 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-, -CC-, -CH2O-, -OCH2-, -CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -CH = N-, -N = CH-, -O-, -NH-, -CO-, -CH2-, -CH2S-, -SCH2- and -S- (wherein the sulphur atom in the latter three groups may optionally bear one or two oxygen atoms); Ar is a phenylene moiety; Ar is a heterocyclic 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, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-6C)alkoxy, (1-6C)alkylamino, di-[(1-6C)alkyl]amino N-(1-6C)alkylcarbamoyl, di-N,N-[(1-6C)alkyl]carbamoyl, (1-6C)alkoxycarbonyl, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, halogeno (1-6C)alkyl, (1-6C)alkanoylamino, ureido, N'-(1-6C)alkylureido, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oxime derivatives; are inhibitors of squalene synthase and hence useful in treating medical conditions in which a lowering of cholesterol is beneficial. Processes 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 - ， - CH 2 O - ， - OCH 2 - ， - CH 2 NH-， - NHCH 2 - ， - CH 2 CO-， - COCH 2 - ， - CH = = CH-， - O - ， - NH - ， - CO-， - CH 2 - ， - CH 2 S - ， - CH 2 - 和-S-（其中后三个基团中的硫原子可以任选地带有一个或两个氧原子） ; Ar 1是亚苯基; Ar 2是杂环部分; 并且其中Ar 1和Ar 2中的一个或两个可以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，（1-6C）烷基，（2-6C））（2-6C）炔基，（1-6C）烷氧基，（1-6C）烷基氨基，二 - [（1-6C）烷基]氨基N-（1-6C）烷基氨基甲酰基，二-N，（1-6C）烷基]氨基甲酰基，（1-6C）烷氧基羰基，（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，（1-6C ）烷基酰氨基，脲基，N' - （1-6C）烷基脲基，（1-6C）烷酰基和肟衍生物和所述肟衍生物的O-（1-6C）烷基醚; 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。制备这些衍生物的方法，含有它们的药物组合物也与其在药物中的用途一起被描述。

10. 发明申请

WO1994014803A1 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：WO1994014803A1
公开(公告)日：1994-07-07
申请号：PCT/GB1993002614
申请日：1993-12-21
申请人： ZENECA LIMITED , BROWN, George, Robert , MALLION, Keith, Blakeney
发明人： ZENECA LIMITED
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Compounds of formula (I) 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; Ar is a phenylene moiety and Ar is a heterocyclic moiety; or Ar is a heterocyclic moiety and Ar is a phenyl 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, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-6C)alkoxy, (1-6C)alkylamino, di-[(1-6C)alkyl]amino N-(1-6C)alkylcarbamoyl, di-N,N-[(1-6C)alkyl]carbamoyl, (1-6C)alkoxycarbonyl, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, halogeno (1-6C)alkyl, (1-6C)alkanoylamino, ureido, N'-(1-6C)alkylureido, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oxime derivatives; provided that Ar is not a 6-membered heteroaryl moiety containing one or two nitrogen atoms; when Ar and Ar are both hydrogen, Ar is not an oxadiazole moiety; and their pharmaceutically acceptable salts are inhibitors of squalene synthase and hence useful in treating medical conditions in which a lowering of cholesterol is beneficial. Processes preparing these derivatives, pharmaceutical compositions containing them are also described together with 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; Ar 1是亚苯基部分，Ar 2是杂环部分; 或Ar 1是杂环部分，Ar 2是苯基部分; 并且其中Ar 1和Ar 2中的一个或两个可以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，（1-6C）烷基，（2-6C））（2-6C）炔基，（1-6C）烷氧基，（1-6C）烷基氨基，二 - [（1-6C）烷基]氨基N-（1-6C）烷基氨基甲酰基，二-N，（1-6C）烷基]氨基甲酰基，（1-6C）烷氧基羰基，（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，（1-6C ）烷基酰氨基，脲基，N' - （1-6C）烷基脲基，（1-6C）烷酰基和肟衍生物和所述肟衍生物的O-（1-6C）烷基醚; 条件是Ar 2不是含有一个或两个氮原子的6元杂芳基部分; 当Ar 1和Ar 2都是氢时，Ar 2不是恶二唑部分; 其药学上可接受的盐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。制备这些衍生物的方法，含有它们的药物组合物也与其在药物中的用途一起被描述。

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