WO2015158204A1 - 酰胺类衍生物及其可药用盐、其制备方法及其在医药上的应用 - Google Patents
酰胺类衍生物及其可药用盐、其制备方法及其在医药上的应用 Download PDFInfo
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- WO2015158204A1 WO2015158204A1 PCT/CN2015/075531 CN2015075531W WO2015158204A1 WO 2015158204 A1 WO2015158204 A1 WO 2015158204A1 CN 2015075531 W CN2015075531 W CN 2015075531W WO 2015158204 A1 WO2015158204 A1 WO 2015158204A1
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- 0 CCCC*(CCCC(*)C(NC1=*C(CC(C)(CCC(C)(C)C2)*(C)*)C2*=B1)=O)CNC(*)=O Chemical compound CCCC*(CCCC(*)C(NC1=*C(CC(C)(CCC(C)(C)C2)*(C)*)C2*=B1)=O)CNC(*)=O 0.000 description 5
- CPODMFFOZLYDTL-UHFFFAOYSA-N CC(C)(C(NCc1cc(C(Cl)=O)c(C(F)F)nc1)=O)F Chemical compound CC(C)(C(NCc1cc(C(Cl)=O)c(C(F)F)nc1)=O)F CPODMFFOZLYDTL-UHFFFAOYSA-N 0.000 description 2
- GQFKAXSZAMNAIM-UHFFFAOYSA-N CC(C)(C(NCc1cc(C(O)=O)c(C(F)F)nc1)=O)F Chemical compound CC(C)(C(NCc1cc(C(O)=O)c(C(F)F)nc1)=O)F GQFKAXSZAMNAIM-UHFFFAOYSA-N 0.000 description 2
- MDVPHODXRFXXKQ-UHFFFAOYSA-N CC[n]1c(-c(cc2)ccc2Cl)nc2c1ccc(N)c2 Chemical compound CC[n]1c(-c(cc2)ccc2Cl)nc2c1ccc(N)c2 MDVPHODXRFXXKQ-UHFFFAOYSA-N 0.000 description 2
- FVFFBSMJPITPJY-UHFFFAOYSA-N CC[n]1c(-c(cc2)ccc2Cl)nc2c1ccc(NC(c1cc(CNC(C(C)C)=O)cnc1C(F)F)=O)c2 Chemical compound CC[n]1c(-c(cc2)ccc2Cl)nc2c1ccc(NC(c1cc(CNC(C(C)C)=O)cnc1C(F)F)=O)c2 FVFFBSMJPITPJY-UHFFFAOYSA-N 0.000 description 2
- YHSPOCHEGHGPCN-UHFFFAOYSA-N CC(C)C(NCc1cc(C(O)=O)c(C(F)F)nc1)=O Chemical compound CC(C)C(NCc1cc(C(O)=O)c(C(F)F)nc1)=O YHSPOCHEGHGPCN-UHFFFAOYSA-N 0.000 description 1
- UBSDYNGRFUAKPG-UHFFFAOYSA-N CC[n](c(-c1cc(Cl)ccc1)c1)c(cc2)c1nc2Cl Chemical compound CC[n](c(-c1cc(Cl)ccc1)c1)c(cc2)c1nc2Cl UBSDYNGRFUAKPG-UHFFFAOYSA-N 0.000 description 1
- XEOQFGZVIQXFLO-UHFFFAOYSA-N CC[n](c(-c1cc(Cl)ccc1)c1)c(cc2)c1nc2N Chemical compound CC[n](c(-c1cc(Cl)ccc1)c1)c(cc2)c1nc2N XEOQFGZVIQXFLO-UHFFFAOYSA-N 0.000 description 1
- OSNVMTSRFZDTBL-UHFFFAOYSA-N CC[n](c(-c1ccc(C(F)(F)F)cc1)c1)c(cc2)c1cc2NC(c1c(C(F)F)ncc(CNC(C(C)C)=O)c1)=O Chemical compound CC[n](c(-c1ccc(C(F)(F)F)cc1)c1)c(cc2)c1cc2NC(c1c(C(F)F)ncc(CNC(C(C)C)=O)c1)=O OSNVMTSRFZDTBL-UHFFFAOYSA-N 0.000 description 1
- DBBHVZPHBJJNSU-UHFFFAOYSA-N CC[n]1c2ccc(N=C(c3ccccc3)c3ccccc3)nc2cc1-c1cc(Cl)ccc1 Chemical compound CC[n]1c2ccc(N=C(c3ccccc3)c3ccccc3)nc2cc1-c1cc(Cl)ccc1 DBBHVZPHBJJNSU-UHFFFAOYSA-N 0.000 description 1
- DXPCSEBCKXUVMV-UHFFFAOYSA-N CC[n]1c2ccc(NC(c3c(C(F)F)ncc(CNC(C(C)(C)F)=O)c3)=O)nc2cc1-c1cccc(Cl)c1 Chemical compound CC[n]1c2ccc(NC(c3c(C(F)F)ncc(CNC(C(C)(C)F)=O)c3)=O)nc2cc1-c1cccc(Cl)c1 DXPCSEBCKXUVMV-UHFFFAOYSA-N 0.000 description 1
- OAJXKCRGMPNUPO-UHFFFAOYSA-N C[ClH]c(cc1)ccc1[IH]C Chemical compound C[ClH]c(cc1)ccc1[IH]C OAJXKCRGMPNUPO-UHFFFAOYSA-N 0.000 description 1
- MURSLIZLMVUHNV-UHFFFAOYSA-N Clc1cccc(-c2cc(nc(cc3)Cl)c3[nH]2)c1 Chemical compound Clc1cccc(-c2cc(nc(cc3)Cl)c3[nH]2)c1 MURSLIZLMVUHNV-UHFFFAOYSA-N 0.000 description 1
- FLUVCYLGGOSDAP-UHFFFAOYSA-N Nc(cc1)cc2c1[n](C1COCC1)c(-c(cc1)ccc1Cl)c2 Chemical compound Nc(cc1)cc2c1[n](C1COCC1)c(-c(cc1)ccc1Cl)c2 FLUVCYLGGOSDAP-UHFFFAOYSA-N 0.000 description 1
- IQYZYNICIBQOJB-UHFFFAOYSA-N O=Nc(cc1)cc2c1[nH]c(-c(cc1)ccc1Cl)c2 Chemical compound O=Nc(cc1)cc2c1[nH]c(-c(cc1)ccc1Cl)c2 IQYZYNICIBQOJB-UHFFFAOYSA-N 0.000 description 1
- LDJCAMUVZBTVOE-WYMLVPIESA-N [O-][N+](c1cc(C=C/C(/CC2)=C3/COCC3)c2cc1)=O Chemical compound [O-][N+](c1cc(C=C/C(/CC2)=C3/COCC3)c2cc1)=O LDJCAMUVZBTVOE-WYMLVPIESA-N 0.000 description 1
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Abstract
Description
实施例编号 | IC50(nM) |
1 | 8.26 |
5 | 21.97 |
7 | 6.02 |
8 | 3.88 |
9 | 15.64 |
10 | 11.15 |
11 | 5.14 |
13 | 7.43 |
14 | 4.59 |
15 | 23.44 |
16 | 9.31 |
17 | 2.68 |
18 | 5.15 |
19 | 8.12 |
20 | 3.54 |
21 | 8.24 |
22 | 6.69 |
23 | 4.73 |
24 | 17.22 |
25 | 11.86 |
26 | 3.38 |
27 | 4.77 |
30 | 2.99 |
31 | 2.95 |
30 | 1.73 |
31 | 4.12 |
32 | 2.24 |
33 | 5.33 |
34 | 7.75 |
35 | 4.07 |
36 | 4.19 |
37 | 6.46 |
38 | 5.43 |
39 | 3.68 |
40 | 22.44 |
41 | 25.65 |
42 | 7.21 |
43 | 15.96 |
45 | 49.39 |
46 | 2.71 |
47 | 5.72 |
48 | 3.58 |
49 | 8.29 |
54 | 47.09 |
55 | 29.78 |
56 | 7.74 |
57 | 6.75 |
58 | 8.51 |
59 | 1.18 |
实施例编号 | IC50(nM) |
11 | 210.60 |
14 | 91.18 |
18 | 152.50 |
20 | 74.73 |
32 | 16.86 |
33 | 107.60 |
35 | 39.88 |
36 | 137.30 |
37 | 141.10 |
实施例编号 | IC50(nM) |
1 | 3.55 |
4 | 26.87 |
5 | 12.40 |
6 | 68.10 |
7 | 10.44 |
8 | 19.15 |
9 | 11.85 |
10 | 12.31 |
11 | 16.30 |
13 | 16.67 |
14 | 20.46 |
15 | 33.31 |
16 | 26.18 |
17 | 12.14 |
18 | 17.19 |
19 | 42.60 |
20 | 12.57 |
21 | 57.42 |
22 | 38.80 |
23 | 49.02 |
24 | 45.65 |
25 | 47.63 |
26 | 46.05 |
27 | 13.44 |
30 | 19.17 |
31 | 32.39 |
30 | 7.18 |
31 | 17.00 |
32 | 18.83 |
33 | 12.78 |
34 | 12.21 |
35 | 31.56 |
36 | 13.22 |
37 | 22.45 |
38 | 42.85 |
39 | 30.53 |
40 | 16.87 |
43 | 58.18 |
45 | 25.91 |
46 | 24.70 |
47 | 18.93 |
48 | 14.13 |
49 | 23.97 |
52 | 55.20 |
54 | 58.53 |
56 | 27.49 |
57 | 6.22 |
58 | 2.18 |
59 | 20.52 |
Claims (18)
- 一种通式(I)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐:其中:环P选自5元杂芳基或5元杂环基;环Q选自芳基或杂芳基;A、B或Y选自-CH-或N;R1选自烷基或环烷基,其中所述的烷基或环烷基任选进一步被一个或多个选自烷基、卤素或卤代烷基的取代基所取代;R2选自卤素或卤代烷基;各个R3相同或不同,其各自独立地选自氢原子、卤素、烷氧基、氰基、硝基、烷基、环烷基、杂环基、氧代、-C(O)OR5、-OC(O)R5、-NHS(O)mR5、-C(O)R5、-NHC(O)R5、-NHC(O)OR5、-NR6R7、-OC(O)NR6R7或-C(O)NR6R7,其中所述的烷基、环烷基或杂环基任选进一步被一个或多个选自卤素、羟基、烷氧基、氰基、硝基、烷基、卤代烷基、羟烷基、环烷基、杂环基、芳基、杂芳基、-C(O)OR5、-OC(O)R5、-NHS(O)mR5、-C(O)R5、-NHC(O)R5、-NHC(O)OR5、-NR6R7、-OC(O)NR6R7或-C(O)NR6R7的取代基所取代;R4选自芳基或杂芳基,其中所述的芳基或杂芳基任选进一步被一个或多个选自卤素、烷氧基、羟基、氰基、硝基、烷基、卤代烷基、羟烷基、环烷基、杂环基、芳基、杂芳基、-C(O)OR5、-OC(O)R5、-NHS(O)mR5、-C(O)R5、-NHC(O)R5、-NHC(O)OR5、-NR6R7、-OC(O)NR6R7或-C(O)NR6R7的取代基所取代,其中所述的卤代烷基优选为三氟甲基;R5选自烷基、烯基、炔基、环烷基、杂环基、芳基或杂芳基,其中所述的烷基、环烷基、芳基或杂芳基任选进一步被一个或多个选自烷基、卤素、羟基、羟烷基、烷氧基、环烷基、杂环基、芳基、杂芳基、羧酸或羧酸酯的取代基所取代;R6或R7各自独立地选自氢原子、烷基、烷氧基、环烷基、杂环基、芳基或杂芳基,其中所述的烷基、烷氧基、环烷基、杂环基、芳基或杂芳基各自独立地任选进一步被一个或多个选自烷基、卤素、羟基、羟烷基、烷氧基、环烷基、杂环 基、芳基、杂芳基、羧酸或羧酸酯的取代基所取代;或者,R6或R7与相连接的氮原子一起形成杂环基,其中所述的杂环基内含有一个或多个N、O或S(O)m杂原子,并且所述杂环基任选进一步被一个或多个选自烷基、卤素、羟基、烷氧基、羟烷基、环烷基、杂环基、芳基、杂芳基、羧酸或羧酸酯的取代基所取代;m为0、1或2;s为0~3的整数;t为0或1。
- 根据权利要求1所述的通式(I)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐,其为通式(III)、(IV)或(V)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐:其中:X选自-CH-或N;E、G和W各自独立地选自CRa、NRb、N、O或S;Ra和Rb各自独立地选自氢原子、卤素、烷氧基、氰基、硝基、烷基、环烷基、杂环基、-C(O)OR5、-OC(O)R5、-NHS(O)mR5、-C(O)R5、-NHC(O)R5、-NHC(O)OR5、-NR6R7、-OC(O)NR6R7或-C(O)NR6R7,其中所述的烷基、环烷基或杂环基任选进一步被一个或多个选卤素、羟基、烷氧基、氰基、硝基、烷基、卤代烷基、羟烷基、环烷基、杂环基、芳基、杂芳基、-C(O)OR5、-OC(O)R5、-NHS(O)mR5、-C(O)R5、-NHC(O)R5、-NHC(O)OR5、-NR6R7、-OC(O)NR6R7或-C(O)NR6R7的取代基所取代;且A、B、Y、t、R1~R2、R4~R7的定义如权利要求1中所述。
- 根据权利要求1所述的通式(I)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐,其为通式(VI)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐:其中:X选自-CH-或N;Rb选自氢原子、卤素、烷氧基、氰基、硝基、烷基、环烷基、杂环基、-C(O)OR5、-OC(O)R5、-NHS(O)mR5、-C(O)R5、-NHC(O)R5、-NHC(O)OR5、-NR6R7、-OC(O)NR6R7或-C(O)NR6R7,其中所述的烷基、环烷基或杂环基任选进一步被一个或多个选自卤素、羟基、烷氧基、氰基、硝基、烷基、卤代烷基、羟烷基、环烷基、杂环基、芳基、杂芳基、-C(O)OR5、-OC(O)R5、-NHS(O)mR5、-C(O)R5、-NHC(O)R5、 -NHC(O)OR5、-NR6R7、-OC(O)NR6R7或-C(O)NR6R7的取代基所取代;且A、B、Y、t、R1~R2、R4~R7的定义如权利要求1中所述。
- 根据权利要求1所述的通式(I)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐,其为通式(VII)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐:其中:X选自-CH-或N;Rb选自氢原子、卤素、烷氧基、氰基、硝基、烷基、环烷基、杂环基、-C(O)OR5、-OC(O)R5、-NHS(O)mR5、-C(O)R5、-NHC(O)R5、-NHC(O)OR5、-NR6R7、-OC(O)NR6R7或-C(O)NR6R7,其中所述的烷基、环烷基或杂环基任选进一步被一个或多个选自卤素、羟基、烷氧基、氰基、硝基、烷基、卤代烷基、羟烷基、环烷基、杂环基、芳基、杂芳基、-C(O)OR5、-OC(O)R5、-NHS(O)mR5、-C(O)R5、-NHC(O)R5、-NHC(O)OR5、-NR6R7、-OC(O)NR6R7或-C(O)NR6R7的取代基所取代;R8选自卤素、烷氧基、羟基、氰基、硝基、烷基、卤代烷基、羟烷基、环烷基、杂环基、芳基、杂芳基、-C(O)OR5、-OC(O)R5、-NHS(O)mR5、-C(O)R5、-NHC(O)R5、-NHC(O)OR5、-NR6R7、-OC(O)NR6R7或-C(O)NR6R7的取代基所取代,其中所述的卤代烷基优选为三氟甲基;且A、B、Y、R1~R2、R5~R7的定义如权利要求1中所述。
- 根据权利要求1~5任一项所述的通式(I)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐,其中A、B和Y选自-CH-。
- 根据权利要求1~5任一项所述的通式(I)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐,其中A、B和Y之一为N,其余两个为-CH-。
- 一种通式(IA)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐,包括如下基团:其中:R3选自氢原子、烷基或杂环基,其中所述的烷基任选进一步被一个或多个选自烷氧基或杂环基的取代基所取代;R4选自芳基或杂芳基,其中所述的芳基或杂芳基任选进一步被一个或多个选自卤素或卤代烷基的取代基所取代,其中所述的卤代烷基优选为三氟甲基;R4优选为苯基,其中所述的苯基进一步被一个卤素或卤代烷基的取代基所取代;t为1;条件是:当通式(IA)为R3选自氢原子或烷基,其中所述的烷基任选进一步被一个或多个选自烷氧基或杂环基的取代基所取代;R4选自苯基,其中所述的苯基进一步被一个卤代烷基的取代基所取代;其中所述的卤代烷基优选为三氟甲基;或者,R3选自杂环基;R4选自为苯基,其中所述的苯基进一步被一个卤素或卤代烷基的取代基所取代。
- 一种药物组合物,所述药物组合物含有治疗有效量的根据权利要求1所述的通式(I)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式、或其可药用的盐及药学上可接受的载体、稀释剂或赋形剂。
- 根据权利要求1-10任意一项所述的通式(I)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐,或根据权利要求15所述的药物组合物在制备治疗微粒体前列腺素E合成酶-1介导的疾病的药物中的用途。
- 根据权利要求1-10任意一项所述的通式(I)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐,或根据权利要求15所述的药物组合物在制备抑制微粒体前列腺素E合成酶-1的药物中的用途。
- 根据权利要求1-10任意一项所述的通式(I)所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用盐,或根据权利要求15所述的药物组合物在制备治疗和/或预防疾病或病症的药物中的用途,所述疾病或病症选自炎症、疼痛、癌症、糖尿病和糖尿病并发症或神经变性病症,优选为炎症或疼痛,更优选为骨关节炎、类风湿性关节炎、粘液囊炎、强直性脊柱炎、或与其中任一者相关的疼痛。
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JP2016561312A JP6688445B2 (ja) | 2014-04-14 | 2015-03-31 | アミド誘導体およびそれらの薬学的に許容される塩、それらの製造方法およびそれらの医薬応用 |
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KR1020167031674A KR20160134865A (ko) | 2014-04-14 | 2015-03-31 | 아미드 유도체 및 이의 약제학적으로 허용되는 염, 이의 제조방법 및 이의 의학적 적용 |
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Also Published As
Publication number | Publication date |
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RU2681537C2 (ru) | 2019-03-07 |
EP3133068A4 (en) | 2018-02-21 |
MX2016013529A (es) | 2017-05-09 |
TWI714527B (zh) | 2021-01-01 |
CN105636951A (zh) | 2016-06-01 |
US10081629B2 (en) | 2018-09-25 |
CA2944357A1 (en) | 2015-10-22 |
CN105636951B (zh) | 2018-05-15 |
ES2838625T3 (es) | 2021-07-02 |
AU2015246577B2 (en) | 2019-10-03 |
TW201612158A (en) | 2016-04-01 |
PT3133068T (pt) | 2021-01-06 |
JP6688445B2 (ja) | 2020-04-28 |
EP3133068B1 (en) | 2020-11-25 |
KR20160134865A (ko) | 2016-11-23 |
BR112016023679A2 (pt) | 2017-08-15 |
MX368504B (es) | 2019-10-04 |
EP3133068A1 (en) | 2017-02-22 |
RU2016143333A3 (zh) | 2018-10-26 |
HUE052925T2 (hu) | 2021-05-28 |
US20170037044A1 (en) | 2017-02-09 |
AU2015246577A1 (en) | 2016-11-10 |
RU2016143333A (ru) | 2018-05-17 |
JP2017513828A (ja) | 2017-06-01 |
DK3133068T3 (da) | 2021-01-11 |
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