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1. 发明申请

WO2016071293A2 PHARMACEUTICAL COMPOUND 审中-公开
标题翻译：药用化合物
公开(公告)号：WO2016071293A2
公开(公告)日：2016-05-12
申请号：PCT/EP2015075486
申请日：2015-11-02
申请人： IOMET PHARMA LTD
发明人： COWLEY PHILLIP , WISE ALAN
IPC分类号： A61K31/4985
CPC分类号： A61K31/4985 , A61K31/416 , A61K31/438 , A61K31/439 , A61K31/445 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/499 , A61K31/4995 , C07D231/56 , C07D261/20 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D498/04 , C07D498/08 , C07D498/10
摘要： Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises formula (I) wherein X1, and X2 may be the same or different and each is independently selected from C, N, O and S; X3, X4, X5, and X6 may be the same or different and each is independently selected from C and N; each bond represented by a dotted line may be present or absent, provided that at least one such bond is present; R1, R2, R3, R4, R5 and R6 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R1, R2, R3, R4, R5 and R6 groups present is such that the respective valencies of X1, X2, X3, X4, X5, and X6 are maintained; and wherein at least one of R5 and R6 comprises a group Y, wherein Y is a group having a formula selected from (II), (III), (IV), (V), (VI), (VII) wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group; R31 and R32 may be the same or different and are selected from H and a substituted or unsubstituted organic group; each R34 may be the same or different and is selected from H and a substituted or unsubstituted organic group; R35 is selected from a substituted or unsubstituted alcohol group or ether group; each R36 may be the same or different and is selected from H and a substituted or unsubstituted organic group; X7 may be selected from C and N; X8, X9, X10, X11, X12, X13, X14, X15 and X16 may be the same or different and each is independently selected from C, N, O and S; each bond represented by a dotted line may be present or absent; and each R313 may be the same or different and is selected from H and a substituted or unsubstituted organic group.
摘要翻译：提供了用于药物的色氨酸-2,3-双加氧酶（TDO）和/或吲哚胺-2,3-双加氧酶（IDO）抑制剂化合物，该化合物包含式（I），其中X 1和X 2可以相同或各自独立地选自C，N，O和S; X3，X4，X5和X6可以相同或不同，并且各自独立地选自C和N; 由虚线表示的每个键可以存在或不存在，条件是存在至少一个这样的键; R 1，R 2，R 3，R 4，R 5和R 6可以存在或不存在，并且可以相同或不同，并且各自独立地选自H和取代或未取代的有机基团，条件是R 1，R 2，R 3，R 4 存在的R 5和R 6基团使得保持X 1，X 2，X 3，X 4，X 5和X 6的各自的价数; 并且其中R 5和R 6中的至少一个包含基团Y，其中Y是具有选自（II），（III），（IV），（V），（VI），（VII）的式的基团，其中L可以存在或不存在，并且可以是取代或未取代的有机连接基团; R 31和R 32可以相同或不同，并且选自H和取代或未取代的有机基团; 每个R 34可以相同或不同，并且选自H和取代或未取代的有机基团; R35选自取代或未取代的醇基或醚基; 每个R 36可以相同或不同，并且选自H和取代或未取代的有机基团; X7可以选自C和N; X 8，X 9，X 10，X 11，X 12，X 13，X 14，X 15和X 16可以相同或不同，并且各自独立地选自C，N，O和S; 由虚线表示的每个键可以存在或不存在; 并且每个R 13可以相同或不同，并且选自H和取代或未取代的有机基团。

2. 发明申请

WO2016071283A1 INHIBITORS OF TRYPTOPHAN-2,3-DIOXYGENASE OR INDOLEAMINE-2,3-DIOXYGENASE 审中-公开
标题翻译：赤霉素-2,3-二氧基或吲哚胺-2,3-二氧化物的抑制剂
公开(公告)号：WO2016071283A1
公开(公告)日：2016-05-12
申请号：PCT/EP2015/075471
申请日：2015-11-02
申请人： IOMET PHARMA LTD
发明人： COWLEY, Phillip , WISE, Alan
IPC分类号： A61K31/472 , A61K31/4725 , A61K31/502 , A61P15/18 , A61P25/28 , A61P31/04 , A61P35/00
CPC分类号： C07D237/28 , A61K31/472 , A61K31/4725 , A61K31/502 , A61K45/06 , C07D217/02 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Provided is a compound for use in medicine for inhibiting tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO), which compound comprises formula (I) wherein X 1 , X 2 , and X 7 , may be the same or different and each is independently selected from C and N; X 3 , X 4 , X 5 , and X 6 may be the same or different and each is independently selected from C, N, O and S wherein when X 3 is N it has a double bond and wherein when X 6 is N it has a double bond; the dotted line is a bond which may be present or absent; R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R 2 , R 3 , R 4 and R 6 comprises a group Y; and provided that the number of R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 groups present is such that the respective valencies of X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , and X 7 are maintained; and wherein Y is a group having a formula selected from (II), (III), (IV), (V) wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group, and R 31 and R 32 may be the same or different and are selected from H and a substituted or unsubstituted organic group, X 8 is selected from C and N, and each R 313 may be the same or different and is selected from H and a substituted or unsubstituted organic group.
摘要翻译：提供了用于抑制色氨酸-2,3-双加氧酶（TDO）和/或吲哚胺-2,3-双加氧酶（IDO）的药物中的化合物，该化合物包含式（I），其中X 1，X 2和X 7可以相同或不同，各自独立地选自C和N; X 3，X 4，X 5和X 6可以相同或不同，并且各自独立地选自C，N，O和S，其中当X 3为N时，其具有双键，并且其中当X 6为N时，其具有双键; 虚线是可能存在或不存在的债券; R 1，R 2，R 3，R 4，R 5，R 6和R 7可以存在或不存在，并且可以相同或不同，并且各自独立地选自H和取代或未取代的有机基团，条件是R 2，R 3，，R4和R6包含基团Y; 并且条件是存在的R 1，R 2，R 3，R 4，R 5，R 6和R 7基团的数目使得保持X1，X2，X3，X4，X5，X6和X7的各自的价数; 并且其中Y是具有选自（II），（III），（IV），（V））的式的基团，其中L可以存在或不存在，并且可以是取代或未取代的有机连接基团，并且R 31和R 32可以相同或不同，并且选自H和取代或未取代的有机基团，X 8选自C和N，并且每个R 13可以相同或不同，并且选自H和取代或未取代的有机基团。

3. 发明申请

WO2017007700A1 PHARMACEUTICAL COMPOUND 审中-公开
标题翻译：药用化合物
公开(公告)号：WO2017007700A1
公开(公告)日：2017-01-12
申请号：PCT/US2016/040604
申请日：2016-07-01
申请人： IOMET PHARMA LTD. , MERCK SHARP & DOHME CORP. , COWLEY, Phillip, M. , WISE, Alan , BROWN, Thomas, J. , MCGOWAN, Meredeth, A. , ZHOU, Hua , HAN, Yongxin
发明人： COWLEY, Phillip, M. , WISE, Alan , BROWN, Thomas, J. , MCGOWAN, Meredeth, A. , ZHOU, Hua , HAN, Yongxin
IPC分类号： A61K31/496 , C07D403/06 , A61K31/422
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4523 , A61K31/4545 , A61K31/496 , A61K45/06 , C07D403/06
摘要： Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the general formula (I) detailed within.
摘要翻译：提供用于医药的色氨酸-2,3-双加氧酶（TDO）和/或吲哚胺-2,3-双加氧酶（IDO）抑制剂化合物，该化合物包含在其中详述的通式（I）。

4. 发明申请

WO2015150097A1 INDOLE DERIVATIVES FOR USE IN MEDICINE 审中-公开
标题翻译：用于医学的单独使用的衍生物
公开(公告)号：WO2015150097A1
公开(公告)日：2015-10-08
申请号：PCT/EP2015/055823
申请日：2015-03-19
申请人： IOMET PHARMA LTD
发明人： COWLEY, Philip , WISE, Alan
IPC分类号： A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/407 , A61K31/4184 , A61K31/4188 , A61K31/423 , A61K31/424 , A61P31/00 , A61P25/00 , A61P35/00 , A61P37/00 , A61P43/00 , A61K31/4355 , A61K31/437
CPC分类号： C07D209/42 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/407 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4196 , A61K31/422 , A61K31/423 , A61K31/424 , A61K31/4245 , A61K31/427 , A61K31/4355 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/475 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K45/06 , C07D263/58 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X 1 , X 2 , X 3 , X 4 , and X 5 may be the same or different and each is independently selected from C, N and O; each atom having a dotted line may independently have a double bond or a single bond, provided that valencies at each atom are maintained; each R 1 , R 2 , R 3 , R 4 , R 5 , and R 7 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X 1 , X 2 , X 3 , X 4 , and X 5 are maintained; one or two R 6 groups may be present and are selected from H and a substituted or unsubstituted organic group, provided that the number of R 6 groups present is such that the valency of the carbon atom to which they are attached is maintained, and provided that at least one R 6 is an organic group comprising an atom double-bonded to an oxygen atom (preferably a carbonyl group or a sulphonyl group) at an α-, β-, or γ-position to the carbon atom to which the R 6 is attached and in which the atom double-bonded to an oxygen atom is also bonded to a hetero-atom.
摘要翻译：提供了一种用于医药的色氨酸-2,3-双加氧酶（TDO）和/或吲哚胺-2,3-双加氧酶（IDO）抑制剂化合物，该化合物包括下式：其中X1，X2，X3，X4和 X 5可以相同或不同，各自独立地选自C，N和O; 具有虚线的每个原子可以独立地具有双键或单键，条件是保持每个原子的价态; 每个R 1，R 2，R 3，R 4，R 5和R 7可以存在或不存在，并且可以相同或不同，并且选自H和取代或未取代的有机基团，条件是存在的R基团的数目使得维持X1，X2，X3，X4和X5的化合价; 可以存在一个或两个R 6基团并且选自H和取代或未取代的有机基团，条件是存在的R 6基团的数目使得它们所连接的碳原子的化合价保持，并且条件是在至少一个R 6是包含在与R 6连接的碳原子上的α-，β-或γ-位上与氧原子（优选为羰基或磺酰基）双键键合的原子的有机基团，其中与氧原子双键键合的原子也键合到杂原子上。

5. 发明申请

WO2014195228A8 SCREENING METHOD FOR A GLUT9 INHIBITOR 审中-公开
标题翻译： GLUT9抑制剂的筛选方法
公开(公告)号：WO2014195228A8
公开(公告)日：2015-03-12
申请号：PCT/EP2014061212
申请日：2014-05-29
申请人： IOMET PHARMA LTD
发明人： WISE ALAN , MHYRE ANDREW JAMES
IPC分类号： G01N33/53 , G01N33/557 , G01N33/566 , G01N33/68
CPC分类号： G01N33/5308 , G01N33/557 , G01N33/566 , G01N33/6893 , G01N2800/347
摘要： Provided is a method for screening for a GLUT9 inhibitor, which method comprises: (a) contacting a receptor having a GLUT9 function with a test compound; (b) measuring the kinetics of transport of a species across the receptor, which species is one whose transport is facilitated by GLUT9; and (c) determining whether the test compound is a GLUT9 inhibitor from the kinetics measurements taken in step (b).
摘要翻译：提供了一种筛选GLUT9抑制剂的方法，该方法包括：（a）使具有GLUT9功能的受体与测试化合物接触; （b）测量物种在受体上的运输动力学，哪种物种是通过GLUT9促进其转运的物质; 和（c）从步骤（b）中进行的动力学测量确定测试化合物是否为GLUT9抑制剂。

6. 发明申请

WO2017189386A1 NOVEL SUBSTITUTED IMIDAZOPYRIDINE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND/OR TRYPTOPHAN-2,3-DIOXYGENASE 审中-公开
标题翻译：作为吲哚胺2,3-二氧化酶和/或胰蛋白胨-2,3-二氧化酶抑制剂的新型取代的咪唑并吡啶化合物
公开(公告)号：WO2017189386A1
公开(公告)日：2017-11-02
申请号：PCT/US2017/029042
申请日：2017-04-24
申请人： IOMET PHARMA LTD. , MERCK SHARP & DOHME CORP. , COWLEY, Phillip, M. , MCGOWAN, Meredeth Ann , BROWN, Thomas, J. , HAN, Yongxin , LIU, Kun , PU, Qinglin , WISE, Alan , ZHANG, Hongjun , ZHOU, Hua
发明人： COWLEY, Phillip, M. , MCGOWAN, Meredeth Ann , BROWN, Thomas, J. , HAN, Yongxin , LIU, Kun , PU, Qinglin , WISE, Alan , ZHANG, Hongjun , ZHOU, Hua
IPC分类号： A61P35/00 , C07D401/10
摘要： Disclosed herein are substituted imidazopyridine compounds of formula (I) which are inhibitors of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan-2,3-dioxygenase (TDO) enzymes: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder.
摘要翻译：本文公开了作为吲哚胺2,3-双加氧酶（IDO）和/或色氨酸-2,3-双加氧酶（TDO）酶抑制剂的式（I）的取代咪唑并吡啶化合物：（I）。本文还公开了化合物在潜在治疗或预防IDO-和/或TDO-相关疾病或病症中的用途。本文还公开了包含这些化合物的组合物。本文进一步公开了组合物在潜在治疗或预防IDO-和/或TDO-相关疾病或病症中的用途。

7. 发明申请

WO2016026772A1 PHARMACEUTICAL COMPOUND 审中-公开
标题翻译：药用化合物
公开(公告)号：WO2016026772A1
公开(公告)日：2016-02-25
申请号：PCT/EP2015/068700
申请日：2015-08-13
申请人： IOMET PHARMA LTD
发明人： COWLEY, Philip , WISE, Alan
IPC分类号： A61K31/415 , A61K31/4164 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/433 , A61K31/44 , A61P35/00 , A61P15/00 , A61P25/00 , A61P31/00
CPC分类号： C07D413/12 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/454 , C07D233/88 , C07D257/06 , C07D261/14 , C07D261/16 , C07D413/04
摘要： Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein X 1 is selected from C and N; X 3 and X 5 may be the same or different and each is independently selected from C, N, O and S; Y is selected from N and O; Z is selected from C, N and O; each bond represented by a dotted line may independently be a double bond or a single bond, provided that valencies at each ring atom are maintained and provided that the ring Q contains at least one double bond and provided that the atom N has a double bond; R 3 and R 5 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R 3 groups present is such that the valency of X 3 is maintained, and the number of R 5 groups present is such that the valency of X 5 is maintained; each R 11 and R 12 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R 11 and R 12 groups present is such that the valency of Z is maintained; R 21 is selected from H and a substituted or unsubstituted organic group; R 22 may be present or absent and is selected from H and a substituted or unsubstituted organic group; and Cy is a cyclic organic group.
摘要翻译：提供了一种用于医药的色氨酸-2,3-双加氧酶（TDO）和/或吲哚胺-2,3-双加氧酶（IDO）抑制剂化合物，该化合物包含下式（I）：其中X1选自C和 N; X 3和X 5可以相同或不同，并且各自独立地选自C，N，O和S; Y选自N和O; Z选自C，N和O; 由虚线表示的每个键可以独立地为双键或单键，条件是每个环原子的价数保持并且环Q包含至少一个双键并且条件是原子N具有双键; R 3和R 5可以存在或不存在，并且可以相同或不同，并且各自独立地选自H和取代或未取代的有机基团，条件是存在的R 3基团的数目使得维持X3的化合价，并且存在的R5基团的数目是维持X5的化合价; 每个R 11和R 12可以存在或不存在，并且可以相同或不同，并且各自独立地选自H和取代或未取代的有机基团，条件是存在的R 11和R 12基团的数目使得保持Z的化合价 ; R 21选自H和取代或未取代的有机基团; R 22可以存在或不存在，并且选自H和取代或未取代的有机基团; Cy是环状有机基团。

8. 发明申请

WO2014187922A1 SLC2A TRANSPORTER INHIBITORS 审中-公开
标题翻译： SLC2A输送机抑制剂
公开(公告)号：WO2014187922A1
公开(公告)日：2014-11-27
申请号：PCT/EP2014/060586
申请日：2014-05-22
申请人： IOMET PHARMA LTD.
发明人： COWLEY, Phillip Martin , WISE, Alan , BROWN, Thomas James , ISHERWOOD, Matthew , CHAKRABARTI, Anjan
IPC分类号： C07D471/04 , C07D487/04 , C07D519/00 , A61K31/437 , A61K31/4985 , A61P35/00 , A61P37/00 , A61P29/00 , A61P25/00 , A61P3/00
CPC分类号： A61K31/496 , A61K31/4985 , A61K31/5377 , A61K45/06 , C07D471/04 , C07D487/04 , C07D519/00 , G01N33/502 , G01N2333/705 , G01N2500/04 , G01N2500/10 , Y02A50/385 , Y02A50/414 , Y02A50/423
摘要： Provided is a SLC2A class I transporter inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein A and Z may be the same or different and are each independently selected from C, N, O and S; each X may be the same or different and is independently selected from C, N, O and S; R 1 and R 5 may be present or absent and may be the same or different and are each selected from H and a substituted or unsubstituted organic group; Z completes a ring with each X, each ring comprising from 3 to 8 ring atoms including the X, A, and Z, each ring atom being independently selected from C, N, O and S, and each ring atom being unsubstituted or independently substituted with H or a substituted or unsubstituted organic group; and wherein the bonds between all of the atoms in the rings including the X, A, and Z may independently be single bonds or double bonds, provided that when X or a ring atom is O or S the bonds to X are single bonds.
摘要翻译：本发明提供了用于医药的SLC2A I类转运蛋白抑制剂化合物，该化合物包含下式（I）：其中A和Z可以相同或不同，并且各自独立地选自C，N，O和S; 每个X可以相同或不同，并且独立地选自C，N，O和S; R 1和R 5可以存在或不存在，可以相同或不同，并且各自选自H和取代或未取代的有机基团; Z与每个X完成一个环，每个环包含3至8个环原子，包括X，A和Z，每个环原子独立地选自C，N，O和S，每个环原子是未取代或独立取代的与H或取代或未取代的有机基团; 并且其中包括X，A和Z的环中的所有原子之间的键可以独立地为单键或双键，条件是当X或环原子为O或S时，与X的键为单键。

9. 发明申请

WO2021126725A1 NOVEL SUBSTITUTED 1,3,8-TRIAZASPIRO[4,5]DECANE-2,4-DIONE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) AND/OR TRYPTOPHAN 2,3-DIOXYGENASE (TDO) INHIBITORS 审中-公开
公开(公告)号：WO2021126725A1
公开(公告)日：2021-06-24
申请号：PCT/US2020/064750
申请日：2020-12-14
申请人： MERCK SHARP & DOHME CORP. , IOMET PHARMA LTD. , HAN, Yongxin , DENG, Yongqi , BENNETT, David, Jonathan , COWLEY, Phillip, M. , WISE, Alan
发明人： HAN, Yongxin , DENG, Yongqi , BENNETT, David, Jonathan , COWLEY, Phillip, M. , WISE, Alan
IPC分类号： A61K31/416 , A61K31/435 , A61K31/438
摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder.

10. 发明申请

WO2017048612A1 PHARMACEUTICAL COMPOUND 审中-公开
标题翻译：药用化合物
公开(公告)号：WO2017048612A1
公开(公告)日：2017-03-23
申请号：PCT/US2016/051221
申请日：2016-09-12
申请人： IOMET PHARMA LTD. , MERCK SHARP & DOHME CORP. , COWLEY, Phillip, M. , HAN, Yongxin
发明人： COWLEY, Phillip, M. , HAN, Yongxin
IPC分类号： A61K31/404 , C07D209/30
CPC分类号： A61K31/404 , C07D209/30 , C07D403/12 , A61K2300/00
摘要： Provided is a compound having formula (I): wherein R 2 is selected from -C 1 , -Br and -CN; R 1 and R 4 are independently selected from H and -F; R 631 , R 632 , R 641 and R 642 are independently selected from -H, -F and substituted or unsubstituted C 1 -C 3 alkyl groups; and R 651 and R 652 are independently selected from H and substituted or unsubstituted C 1 -C 3 alkyl groups and substituted or unsubstituted phenyl groups; and wherein at least one of R 631 , R 632 , R 641 , R 642 and R 652 is not -H, or wherein when all of R 631 , R 632 , R 641 , R 642 and R 652 are -H, R 651 is not Me or Et.
摘要翻译：提供具有式（I）的化合物：其中R 2选自-C 1，-Br和-CN; R1和R4独立地选自H和-F; R631，R632，R641和R642独立地选自-H，-F和取代或未取代的C1-C3烷基; R 651和R 652独立地选自H和取代或未取代的C 1 -C 3烷基和取代或未取代的苯基; 并且其中R631，R632，R641，R642和R652中的至少一个不是-H，或者当R631，R632，R641，R642和R652都是-H时，R651不是Me或Et。

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