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1. 发明申请

US20140275069A1 Novel inhibitor compounds of phosphodiesterase type 10A 有权
标题翻译：新型磷酸二酯酶10A抑制剂化合物
公开(公告)号：US20140275069A1
公开(公告)日：2014-09-18
申请号：US14189961
申请日：2014-02-25
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Katja JANTOS , Michael OCHSE , Hervé GENESTE , Jayne FROGGETT , Clarissa JAKOB , Karla DRESCHER , Jürgen DINGES
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables X1 is CH or N, X2 is O or S and where R1, R2, R3, R4 and Q are as defined in the claims.The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
摘要翻译：本发明涉及式I化合物，N-氧化物，互变异构体，其前药及其药学上可接受的盐：在式I中，变量X1是CH或N，X2是O或S，并且其中R1，R2，R3 R4和Q如权利要求中所定义。式I化合物，N-氧化物，互变异构体，其前药和药学上可接受的盐是10A型磷酸二酯酶的抑制剂。因此，本发明还涉及式I化合物，N-氧化物，互变异构体，前药和其药学上可接受的盐在制备药物中的用途，因此其适用于治疗或控制医学病症选自神经障碍和精神障碍，用于改善与这种障碍相关的症状并降低这种障碍的风险。

2. 发明申请

US20180030033A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
公开(公告)号：US20180030033A1
公开(公告)日：2018-02-01
申请号：US15724410
申请日：2017-10-04
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Hervé GENESTE , Sean Colm TURNER , Michael OCHSE , Karla DRESCHER , Lawrence A. BLACK , Katja JANTOS
IPC分类号： C07D401/14 , C07D471/04 , C07D401/04 , C07D401/10 , C07D487/04
CPC分类号： C07D401/14 , C07D401/04 , C07D401/10 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Y1 and Y2 are adjacent atoms in Het1, which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het1 is a bivalent monocyclic 5- or 6-membered heteroaromatic radical, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N—Ra as ring members, or a bivalent fused bicyclic 8-, 9- or 10-membered heteroaromatic radical, having 1, 2, 3 or 4 heteroatoms or heteroatom moieties selected from O, S, N and N—Ra as ring members; Het2 is inter alia monocyclic 5- or 6-membered hetaryl, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N—R1a as ring members, Cyc is inter alia optionally substituted monocyclic 5- or 6-membered hetaryl or optionally substituted fused 8-, 9- or 10-membered bicyclic hetaryl; Ar is optionally substituted phenylene or optionally substituted bivalent 6-membered hetaryl; R is attached to a carbon atom of Het1 and inter alia—halogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C1-C6-fluoroalkyl, C1-C6-fluoroalkoxy, C3-C6-cycloalkyl etc.

3. 发明申请

US20160137668A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20160137668A1
公开(公告)日：2016-05-19
申请号：US14997997
申请日：2016-01-18
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Hervé GENESTE , Michael OCHSE , Karla DRESCHER , Sean TURNER , Berthold BEHL , Loic LAPLANCHE , Jürgen DINGES , Clarissa JAKOB , Lawrence BLACK
IPC分类号： C07D519/00 , C07D401/14 , C07D491/048 , C07D405/14 , C07D471/04 , C07D495/04 , C07D401/06
CPC分类号： C07D519/00 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Q is O or S, X1 is N or CH, X2 is N or C—R7; X3 is O, S—X4═C(R8)—, where C(R8) is bound to the carbon atom which carries R2, or —X5═C(R9)—, where X5 is bound to the carbon atom which carries R2; X4 is N or C—R9; X5 is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R1 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkylsulfanyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, the moiety Y1-Cyc1; R2 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, C2-C4-alkenyloxy, etc; A represents one of the following groups A1, A2, A3, A4 or A5: where * indicates the points of attachment to Het and to the nitrogen atom, respectively; and where R3 to R9, R3e, R3f, A′, Y1 and Cyc1 are defined in the claims.
摘要翻译：本发明涉及式I的新型化合物，其是10A型磷酸二酯酶的抑制剂及其用于制备药物的用途，因此其适用于治疗或控制选自神经障碍和精神疾病的医学病症，用于改善与这些疾病相关的症状并降低这种疾病的风险。其中Q为O或S，X1为N或CH，X2为N或C-R7; X3是O，S-X4 = C（R8） - ，其中C（R8）与携带R2的碳原子结合，或-X5 = C（R9） - ，其中X5与携带R2的碳原子结合 ; X4是N或C-R9; X5是N; Het选自任选取代的苯基，单环杂芳基和稠合双环杂芳基; R1特别选自氢，卤素，OH，C 1 -C 4 - 烷基，三甲基甲硅烷基，C 1 -C 4烷基硫烷基，C 1 -C 4 - 烷氧基-C 1 -C 4烷基，C 1 -C 4 - 烷氧基，C 1 -C 4烷氧基 - C1-C4-烷氧基，Y1-Cyc1部分; R2选自氢，卤素，OH，C 1 -C 4 - 烷基，三甲基甲硅烷基，C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 烷氧基-C 1 -C 4烷氧基， C2-C4-烯氧基等; A代表以下组A1，A2，A3，A4或A5：其中*表示分别与Het和氮原子相连的点; 并且在权利要求中定义R3至R9，R3e，R3f，A'，Y1和Cyc1。

4. 发明申请

US20140303176A1 ACYLAMINOCYCLOALKYL COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF DOPAMINE D3 RECEPTOR 有权
标题翻译：适用于治疗多巴胺D3受体调节障碍的ACYLAMINOCOCLOALKYL化合物
公开(公告)号：US20140303176A1
公开(公告)日：2014-10-09
申请号：US14213169
申请日：2014-03-14
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Andreas HAUPT , Jürgen DINGES , Liliane UNGER , Karsten WICKE , Robert VAN WATERSCHOOT , Karla DRESCHER , Ana RELO
IPC分类号： C07D295/155
CPC分类号： C07D295/155 , A61K31/496 , C07D239/42 , C07D403/04
摘要： The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. In formula I, the variables have the following meanings: m is 1 or 2, n is 1 or 2, A is selected from the group consisting of CH2, CH2CH2, CHFCH2 and CF2CH2, R1 is an oxygen containing cyclic radical selected such as C3-C6 cycloalkyl, which carries one or two oxygen containing radicals selected from the group consisting of OH, C1-C2-alkoxy, fluorinated C1-C2-alkoxy, and a carbonyl oxygen, R2 is selected from the group consisting of hydrogen, OH and fluorine, R3a is selected from the group consisting of hydrogen and methyl, R3b is selected from the group consisting of hydrogen and methyl, R4 is branched C4-C6 alkyl or branched fluorinated C4-C6 alkyl, and R5 is inter alia C1-C6 alkyl, fluorinated C1-C3 alkyl, C1-C2-alkoxy-C1-C4-alkyl, fluorinated C1-C2-alkoxy-C1-C4-alkyl, hydroxy-C1-C4-alkyl, fluorinated hydroxy-C1-C4-alkyl, oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, C3-C5 cycloalkyl, fluorinated C3-C5 cycloalkyl, etc.
摘要翻译：本发明涉及新的酰氨基环烷基化合物，特别是涉及本文所述的式I化合物及其盐和N-氧化物。该化合物具有有价值的治疗特性，特别适用于治疗对多巴胺D3受体调节作出反应的疾病。在式I中，变量具有以下含义：m为1或2，n为1或2，A选自CH 2，CH 2 CH 2，CHFCH 2和CF 2 CH 2，R 1为选自氧的环状基团，例如C 3 -C 6环烷基，其携带一个或两个选自OH，C 1 -C 2烷氧基，氟化C 1 -C 2烷氧基和羰基氧的含氧基团，R 2选自氢，OH和氟，R 3a选自氢和甲基，R 3b选自氢和甲基，R 4是支链C 4 -C 6烷基或支链氟化C 4 -C 6烷基，R 5尤其是C 1 -C 6烷基氟化C 1 -C 3烷基，C 1 -C 2烷氧基-C 1 -C 4烷基，氟化C 1 -C 2烷氧基-C 1 -C 4 - 烷基，羟基-C 1 -C 4 - 烷基，氟化羟基-C 1 -C 4烷基，氧杂环丁烷基，氟化氧杂环丁烷基，氧杂环戊烷基，氟代氧杂环戊烷基，C3-C5环烷基，氟化C3-C5环烷基等

5. 发明申请

US20140303153A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20140303153A1
公开(公告)日：2014-10-09
申请号：US14208067
申请日：2014-03-13
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Hervé GENESTE , Michael OCHSE , Karla DRESCHER , Berthold BEHL , Loic LAPLANCHE , Jürgen DINGES , Clarissa JAKOB
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q are as defined in the claims.The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
摘要翻译：本发明涉及式I化合物，N-氧化物，互变异构体，前药及其药学上可接受的盐：在式I中，变量Het，A，X，Y，Z，R1，R2，R3，R4， R5和Q如权利要求中所定义。式I化合物，N-氧化物，互变异构体，其前药和药学上可接受的盐是10A型磷酸二酯酶的抑制剂。因此，本发明还涉及式I化合物，N-氧化物，互变异构体，前药和其药学上可接受的盐在制备药物中的用途，因此其适用于治疗或控制医学病症选自神经障碍和精神障碍，用于改善与这种障碍相关的症状并降低这种障碍的风险。

6. 发明申请

US20140275104A1 ACYLAMINOCYCLOALKYL COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF DOPAMINE D3 RECEPTOR 有权
公开(公告)号：US20140275104A1
公开(公告)日：2014-09-18
申请号：US14213720
申请日：2014-03-14
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Andreas HAUPT , Jürgen DINGES , Liliane UNGER , Karsten WICKE , Robert VAN WATERSCHOOT , Karla DRESCHER , Ana RELO
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , A61K31/506 , C07D403/04
摘要： The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. In formula I, the variables have the following meanings: m is 1 or 2, n is 1 or 2, A is selected from the group consisting of CH2, CH2CH2, CHFCH2 and CF2CH2, R1 is an oxygen containing cyclic radical selected such as C3-C6 cycloalkyl, which carries one or two oxygen containing radicals selected from the group consisting of OH, C1-C2-alkoxy, fluorinated C1-C2-alkoxy, and a carbonyl oxygen, R2 is selected from the group consisting of hydrogen, OH and fluorine, R3a is selected from the group consisting of hydrogen and methyl, R3b is selected from the group consisting of hydrogen and methyl, R4 is branched C4-C6 alkyl or branched fluorinated C4-C6 alkyl, and R5 is inter alia C1-C6 alkyl, fluorinated C1-C3 alkyl, C1-C2-alkoxy-C1-C4-alkyl, fluorinated C1-C2-alkoxy-C1-C4-alkyl, hydroxy-C1-C4-alkyl, fluorinated hydroxy-C1-C4-alkyl, oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, C3-C5 cycloalkyl, fluorinated C3-C5 cycloalkyl, etc.

7. 发明申请

US20140051695A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20140051695A1
公开(公告)日：2014-02-20
申请号：US13968242
申请日：2013-08-15
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Hervé GENESTE , Michael OCHSE , Karla DRESCHER , Clarissa JAKOB
IPC分类号： C07D471/14 , C07D487/04
CPC分类号： C07D471/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims and where X is C—R6 or N, Y is C—R7 or N, where R6 and R7 are, inter alia, hydrogen, halogen, alkoxy, haloalkoxy and the like. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
摘要翻译：本发明涉及式I化合物，其N-氧化物，互变异构体，前体药物及其药学上可接受的盐，其中在式I中，变量R1，R2，R3，R4和R5如权利要求中所定义，其中X 是C-R6或N，Y是C-R7或N，其中R6和R7尤其是氢，卤素，烷氧基，卤代烷氧基等。式I化合物，N-氧化物，互变异构体，其前药和药学上可接受的盐是10A型磷酸二酯酶的抑制剂及其用于制备药物的用途，因此其适用于治疗或控制医学病症选自神经障碍和精神障碍，用于改善与这种障碍相关的症状并降低这种障碍的风险。

8. 发明申请

US20170158693A1 HEXAHYDRODIAZEPINOQUINOLINES CARRYING A CYCLIC RADICAL 审中-公开
公开(公告)号：US20170158693A1
公开(公告)日：2017-06-08
申请号：US15435553
申请日：2017-02-17
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Gisela BACKFISCH , Margaretha Henrica Maria BAKKER , Günter BLAICH , Wilfried BRAJE , Karla DRESCHER , Thomas ERHARD , Andreas HAUPT , Hannes KOOLMAN , Viktor LAKICS , Anna LINSENMEIER , Helmut MACK , Raimund PETER , Ana Lucia RELO , Xiaona ZHAO , Jincheng WANG
IPC分类号： C07D471/06
CPC分类号： C07D471/06 , C07D471/04
摘要： The present invention relates to tricyclic hexahydrodiazepinoquinolines carrying a cyclic substituent, to a method for producing them, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor, and processes for preparing such compounds and compositions.

9. 发明申请

US20160002231A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20160002231A1
公开(公告)日：2016-01-07
申请号：US14854835
申请日：2015-09-15
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Hervé GENESTE , Michael OCHSE , Karla DRESCHER , Berthold BEHL , Loic LAPLANCHE , Jürgen DINGES , Clarissa JAKOB
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q are as defined in the claims.The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
摘要翻译：本发明涉及式I化合物，N-氧化物，互变异构体，前药及其药学上可接受的盐：在式I中，变量Het，A，X，Y，Z，R1，R2，R3，R4， R5和Q如权利要求中所定义。式I化合物，N-氧化物，互变异构体，其前药和药学上可接受的盐是10A型磷酸二酯酶的抑制剂。因此，本发明还涉及式I化合物，N-氧化物，互变异构体，前药和其药学上可接受的盐在制备药物中的用途，因此其适用于治疗或控制医学病症选自神经障碍和精神障碍，用于改善与这种障碍相关的症状并降低这种障碍的风险。

10. 发明申请

US20140148461A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20140148461A1
公开(公告)日：2014-05-29
申请号：US14087680
申请日：2013-11-22
申请人： ABBVIE INC. , ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： Hervé GENESTE , Sean Colm TURNER , Michael OCHSE , Karla DRESCHER , Lawrence A. BLACK , Katja JANTOS
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D401/04 , C07D401/10 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Y1 and Y2 are adjacent atoms in Het1, which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het1 is a bivalent monocyclic 5- or 6-membered heteroaromatic radical, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N—Ra as ring members, or a bivalent fused bicyclic 8-, 9- or 10-membered heteroaromatic radical, having 1, 2, 3 or 4 heteroatoms or heteroatom moieties selected from O, S, N and N—Ra as ring members; Het2 is inter alia monocyclic 5- or 6-membered hetaryl, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N—R1a as ring members, Cyc is inter alia optionally substituted monocyclic 5- or 6-membered hetaryl or optionally substituted fused 8-, 9- or 10-membered bicyclic hetaryl; Ar is optionally substituted phenylene or optionally substituted bivalent 6-membered hetaryl; R is attached to a carbon atom of Het1 and inter alia-halogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C1-C6-fluoroalkyl, C1-C6-fluoroalkoxy, C3-C6-cycloalkyl etc.
摘要翻译：本发明涉及式I化合物及其盐等，它们是10A型磷酸二酯酶的抑制剂及其用于制备药物的用途，因此其适用于治疗或控制选自神经障碍和精神病学的医学病症疾病，用于改善与这种障碍相关的症状并降低这种障碍的风险。其中Y 1和Y 2是Het 1中的相邻原子，其独立地选自碳和氮; k为0,1,2或3; Het1是具有1,2或3个选自O，S，N和N-Ra的杂环或杂原子的二价单环5-或6-元杂芳族基，作为环成员，或二价稠合双环8-，9-或具有1,2,3或4个选自O，S，N和N-Ra的杂原子或杂原子的10元杂芳族基团作为环成员; Het2特别是具有1,2或3个选自O，S，N和N-R 1a作为环成员的杂原子部分的单环5-或6-元杂芳基，Cyc特别是任选取代的单环5-或6-元杂环，任选取代的稠合的8-，9-或10-元双环杂芳基; Ar是任选取代的亚苯基或任选取代的二价6元杂芳基; R连接到Het1的碳原子上，特别是卤素，C 1 -C 6烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 氟代烷基，C 1 -C 6 - 氟代烷氧基，C3-C6-环烷基等

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