CN107531633A - 5‑芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途 - Google Patents
5‑芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途 Download PDFInfo
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- CN107531633A CN107531633A CN201680021804.7A CN201680021804A CN107531633A CN 107531633 A CN107531633 A CN 107531633A CN 201680021804 A CN201680021804 A CN 201680021804A CN 107531633 A CN107531633 A CN 107531633A
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- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
Abstract
Description
编号 | LogP | CLogP | tPSA |
ZD001 | 4.18 | 3.99516 | 41.46 |
ZD002 | 3.04 | 2.2036 | 41.9 |
ZD003 | 3.32 | 2.7626 | 41.9 |
ZD004 | 4.93 | 4.33516 | 41.46 |
ZD005 | 4.19 | 2.18697 | 60.63 |
ZD006 | 4.25 | 4.97516 | 53.49 |
ZD007 | 3.23 | 1.755 | 41.9 |
ZD008 | 3.51 | 2.314 | 41.9 |
ZD009 | 4.77 | 4.5316 | 41.46 |
ZD010 | 4.65 | 4.162 | 65.25 |
ZD011 | 5.22 | 5.08 | 32.67 |
ZD012 | 4.9 | 4.561 | 32.67 |
ZD013 | 3.28 | 3.462 | 53.82 |
ZD014 | 4.61 | 4.131 | 41.46 |
ZD015 | 5.54 | 5.4648 | 41.46 |
ZD017 | 4.77 | 4.5316 | 41.46 |
ZD019 | 4.65 | 4.162 | 65.25 |
ZD036 | 4.58 | 4.14516 | 41.46 |
ZD037 | 5.33 | 4.48516 | 41.46 |
ZD038 | 3.76 | 3.99516 | 41.46 |
ZD039 | 3.76 | 3.99516 | 41.46 |
ZD040 | 4.51 | 4.3506 | 41.46 |
ZD041 | 5.26 | 4.6906 | 41.46 |
ZD042 | 2.69 | 2.92556 | 53.82 |
ZD043 | 3.44 | 3.26556 | 53.82 |
ZD044 | 4.06 | 3.62556 | 65.25 |
ZD045 | 4.81 | 3.96556 | 65.25 |
ZD046 | 4.31 | 4.4396 | 32.67 |
ZD047 | 5.06 | 4.7796 | 32.67 |
ZD048 | 4.63 | 4.9586 | 32.67 |
ZD049 | 5.37 | 5.2986 | 32.67 |
ZD050 | 2.57 | 2.05432 | 66.18 |
ZD051 | 3.31 | 3.03768 | 53.82 |
ZD052 | 4.19 | 3.64034 | 45.03 |
ZD053 | 4.06 | 3.37768 | 53.82 |
ZD054 | 4.34 | 3.52768 | 53.82 |
ZD055 | 1.82 | 1.71432 | 66.18 |
ZD056 | 3.44 | 3.30034 | 45.03 |
ZD057 | 4.77 | 4.0656 | 41.46 |
ZD058 | 3.31 | 3.0588 | 77.61 |
ZD059 | 4.2 | 3.25848 | 53.82 |
ZD060 | 5.69 | 4.38996 | 41.46 |
ZD061 | 4.81 | 4.26516 | 65.25 |
ZD062 | 4.93 | 4.1695 | 56.46 |
ZD063 | 5.82 | 5.5763 | 32.67 |
ZD064 | 4.93 | 3.73516 | 41.46 |
ZD065 | 4.93 | 4.33516 | 41.46 |
ZD066 | 5.09 | 4.45246 | 41.46 |
ZD067 | 5.09 | 3.92246 | 41.46 |
ZD068 | 5.33 | 4.90516 | 41.46 |
ZD069 | 5.69 | 5.26836 | 41.46 |
ZD070 | 4.65 | 4.03934 | 50.69 |
ZD071 | 4.15 | 3.26556 | 53.82 |
ZD072 | 3.44 | 3.26556 | 53.82 |
ZD073 | 4.06 | 3.47806 | 53.82 |
ZD074 | 4.34 | 4.04806 | 53.82 |
ZD075 | 5.26 | 4.5646 | 41.46 |
ZD076 | 2.76 | 2.76656 | 53.82 |
ZD077 | 3.66 | 2.95897 | 53.82 |
ZD078 | 3.93 | 3.52897 | 53.82 |
ZD079 | 4.34 | 3.76528 | 53.82 |
ZD080 | 3.39 | 3.42456 | 53.82 |
ZD081 | 3.31 | 3.15256 | 53.82 |
ZD082 | 3.59 | 3.72256 | 53.82 |
ZD083 | 4.03 | 3.95556 | 53.82 |
ZD084 | 3.15 | 2.75356 | 77.61 |
ZD085 | 1.67 | 1.96856 | 66.18 |
ZD086 | 2.58 | 2.46756 | 66.18 |
ZD087 | 4.07 | 3.53716 | 53.82 |
ZD088 | 4.2 | 3.9816 | 45.03 |
ZD089 | 2.07 | 2.37056 | 63.05 |
ZD090 | 3.56 | 3.44016 | 50.69 |
ZD091 | 3.69 | 3.8846 | 41.9 |
ZD092 | 4.44 | 4.4536 | 41.9 |
ZD093 | 2.82 | 2.93956 | 63.05 |
ZD094 | 4.31 | 4.00916 | 50.69 |
MPEP | 3.77 | 3.782 | 12.36 |
CTEP | 5.7 | 5.70617 | 37.19 |
编号 | mGluR5IC<sub>50</sub> | mGluR1 IC<sub>50</sub> | mGluR5/mGluR1 |
ZD001 | 13.9nM | >100μM | >7194 |
ZD004 | 11nM | >100μM | >9091 |
ZD012 | 14.4nM | >100μM | >6944 |
ZD013 | 14.2nM | >100μM | >7042 |
ZD014 | 14.8nM | >100μM | >6757 |
ZD016 | 29.2nM | >100μM | >3425 |
ZD036 | 20.29nM | >100μM | >4929 |
ZD037 | 7.312nM | >100μM | >13676 |
ZD042 | 19.4nM | >100μM | >5155 |
ZD043 | 5.601nM | >100μM | >17854 |
ZD046 | 15.15nM | >100μM | >6601 |
ZD047 | 6.647nM | >100μM | >15044 |
ZD049 | 37.99nM | >100μM | >2632 |
JNJ16259685 | —— | 91.23nM | —— |
Claims (10)
- 一种具有如下通式I所示结构的5-芳香炔基取代的苯甲酰胺类化合物,及其外消旋体、R-异构体、S-异构体、可药用盐或它们混合物:X为CH或N;R1选自下组:氢、卤素、C1-C6烷基、卤素取代的C1-C6烷基、氰基;R2和R3各自独立地选自下组:氢、取代或未取代的苯基、取代或未取代的3-7元杂芳基、取代或未取代的5-7元芳香基-亚甲基、3-7元杂环基-亚甲基,各个杂环基各自独立地含有1~4个选自氧、硫和氮中的杂原子;且所述的R2和R3不同时为氢;或者R2和R3与所连接的N原子共同构成选自下组的基团:取代或未取代的5-20元螺杂环、或者取代或未取代的4-20元并杂环;其中,所述的取代指基团上的一个或多个氢原子被选自下组的取代基取代:卤素、C1-C6烷基、卤素取代的C1-C6烷基、C1-C6烷氧基、C1-C6烷氧基羰基、卤素取代的C1-C6烷氧基、C2-C6烯基、C2-C6炔基、C3-C8环烷基、氰基、硝基、氨基、羟基、羟甲基、羧基、巯基、磺酰基、C6-C10芳基、和3-12元杂环基;其中,所述的螺杂环、并杂环或杂环基各自独立地含有1~4个选自氧、硫和氮中的杂原子;环选自下组:取代或未取代的5~6元芳香杂环、取代或未取代的6-20元芳杂稠环,其中取代基为1、2、3或4个选自下组的取代基:卤素、C1-C6烷基、卤素取代的C1-C6烷基、C1-C6烷氧基、卤素取代的C1-C6烷氧基、C3-C8环烷基、C3-C8卤代环烷基、氰基、硝基、氨基、胺基(较佳地C1-C6胺基)、羟基、羟甲基、羧基、巯基、磺酰基、C6-C10芳基和3-12元杂环基,其中,所述芳香杂环、芳杂稠环或杂环基各自独立地含有1~4个选自氧、硫和氮中的杂原子;且当R1为H时,环为取代或未取代的5元芳香杂环;所述的卤素为F、Cl、Br或I。
- 如权利要求1所述的化合物,其特征在于,所述的R2和R3各自独立地选自下组:氢、取代或未取代的苯基、取代或未取代的3-7元杂芳基、取代或未取代的5-7元芳香基-亚甲基、3-7元杂环基-亚甲基,各个杂环基各自独立地含有1~4个选自氧、硫和氮中的杂原子;R2和R3不同时为氢;或者R2和R3与所连接的N原子共同构成选自下组的基团:取代或未取代的螺杂环、或者取代或未取代的并杂环;其中,所述的取代指基团上的一个或多个氢原子被选自下组的取代基取代:卤素、C1-C6烷基、C1-C6烷氧基、卤素取代的C1-C6烷氧基、氰基、硝基、氨基、羟基、羟甲基、羧基、巯基、磺酰基、三氟甲基。
- 如权利要求1所述的化合物,其特征在于,所述的环选自下组: 其中R4、R5、R6、R7、R8分别代表杂环上的1-4个取代基,且各个取代基各自独立地选自下组:卤素、C1-C6烷基、卤素取代的C1-C6烷基、C1-C6烷氧基、氰基、硝基、氨基、羟基。
- 如权利要求1所述的化合物,其特征在于,所述的R2选自下组:取代或未取代的苯基、取代或未取代的吡啶基、取代或未取代的吡嗪基;其中,所述的取代指基团上的氢原子被选自下组的取代基取代:卤素、C1-C6烷基、卤素取代的C1-C6烷基、C1-C6烷氧基、氰基、硝基、氨基、羟基;R3为H;或所述的R2和R3与相连的N原子共同构成取代或未取代的选自下组的基团:其中R9、R10、R11、R12、R13分别代表环上任意位置的1-4个取代基,且各个取代基各自独立地选自下组:卤素、C1-C6烷基、卤素取代的C1-C6烷基、C1-C6烷氧基、氰基、硝基、氨基、羟基。
- 如权利要求1所述的化合物,其特征在于,所述的选自下组:取代或未取代的吡啶基、取代或未取代的噻唑基,取代或未取代的异噁唑基、取代或未取代的嘧啶基、或取代或未取代的吲唑基;其中,所述的取代基为:卤素、C1-C6烷基、卤素取代的C1-C6烷基、C1-C6烷氧基、氰基、硝基、氨基、羟基。
- 如权利要求1所述的化合物,其特征在于,所述的化合物选自下组:
- 一种药物组合物,其特征在于,包含(a)治疗有效量的式I所示的5-芳香炔基取代的苯甲酰胺类化合物、或其药学上可接受的盐、外消旋体、R-异构体、S-异构体,或其组合;和(b)药学上可接受的载体。
- 一种mGluR5负性变构调节剂,其特征在于,包含选自上述通式I所示的5-芳香炔基取代的苯甲酰胺类化合物、其可药用的盐、外消旋体、R-异构体、S-异构体,或其组合。
- 如权利要求8所述的负性变构调节剂,其特征在于,所述的mGluR5负性变构调节剂选择性地抑制mGluR5。
- 如权利要求1所述的式I化合物、或其药学上可接受的盐、其外消旋体、R-异构体、S-异构体或它们的混合物在制备用于治疗与mGluR5(代谢型谷氨酸受体第五亚型)相关的疾病的药物中的用途。
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KR102117453B1 (ko) | 2020-06-01 |
EP3284738B1 (en) | 2020-11-25 |
EP3284738A1 (en) | 2018-02-21 |
JP6795517B2 (ja) | 2020-12-02 |
AU2016248388B2 (en) | 2019-06-06 |
EP3284738A4 (en) | 2018-09-12 |
US10618900B2 (en) | 2020-04-14 |
CA2988861C (en) | 2021-09-28 |
RU2017139564A3 (zh) | 2019-05-15 |
RU2017139564A (ru) | 2019-05-15 |
ES2864800T3 (es) | 2021-10-14 |
CA2988861A1 (en) | 2016-10-20 |
US20180194767A1 (en) | 2018-07-12 |
JP2018514524A (ja) | 2018-06-07 |
CN106146391A (zh) | 2016-11-23 |
EA201700504A1 (ru) | 2018-10-31 |
AU2016248388A1 (en) | 2017-12-07 |
WO2016165658A1 (zh) | 2016-10-20 |
CN107531633B (zh) | 2020-11-06 |
KR20170137197A (ko) | 2017-12-12 |
EA039234B1 (ru) | 2021-12-21 |
RU2695371C2 (ru) | 2019-07-23 |
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