JP2019104748A5 - - Google Patents
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- JP2019104748A5 JP2019104748A5 JP2019034652A JP2019034652A JP2019104748A5 JP 2019104748 A5 JP2019104748 A5 JP 2019104748A5 JP 2019034652 A JP2019034652 A JP 2019034652A JP 2019034652 A JP2019034652 A JP 2019034652A JP 2019104748 A5 JP2019104748 A5 JP 2019104748A5
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- Prior art keywords
- alkyl
- salt
- compound
- deuterium
- cycloalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 125000000217 alkyl group Chemical group 0.000 claims 34
- 150000003839 salts Chemical class 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 15
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 8
- 229910052805 deuterium Inorganic materials 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- -1 chloro, bromo, methyl Chemical group 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- AVFZOVWCLRSYKC-UHFFFAOYSA-N 1-methylpyrrolidine Chemical group CN1CCCC1 AVFZOVWCLRSYKC-UHFFFAOYSA-N 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- AHVYPIQETPWLSZ-UHFFFAOYSA-N N-methyl-pyrrolidine Chemical group CN1CC=CC1 AHVYPIQETPWLSZ-UHFFFAOYSA-N 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
Claims (19)
- 次の式:
各RAおよびREは独立に、H、重水素、フルオロ、クロロ、ブロモ、メチル、エチル、プロピル、イソプロピル、メトキシ、エトキシ、イソプロポキシ、−CN、または−CF3であり;
RBは−SH、−OH、または
Alkは場合により置換されていてよいアルキル基であり、PGは保護基である)
であり;
RCはH、重水素、C1〜6アルキル、C3〜6シクロアルキル、C6〜10アリール、−C(O)ORa’、−C(O)NRa’Rb’、−NRa’Rb’、−SRa’、−S(O)Ra’、−S(O)NRa’、−S(O)2Ra’、−S(O)2NRa’または−ORa’であり;
RDはH、重水素、C1〜6アルキル、C2〜6アルケニル、C2〜6アルキニル、C3〜6シクロアルキル、3〜7員ヘテロシクロアルキル、C6〜10アリールまたは単環式もしくは二環式ヘテロアリールであり;ここで、C1〜6アルキル、C2〜6アルケニル、C2〜6アルキニル、C3〜6シクロアルキル、3〜7員ヘテロシクロアルキル、C6〜10アリールまたは単環式もしくは二環式ヘテロアリールにおける各水素原子は独立に、場合により、重水素、ハロゲン、C1〜6アルキル、C1〜6ハロアルキルまたは−ORa’により置換されていてよく;
各Ra’は独立に、C1〜6アルキル、C2〜6アルケニル、C2〜6アルキニル、C3〜6シクロアルキル、3〜7員ヘテロシクロアルキル、C6〜10アリールおよびヘテロアリールから成る群から選択され;
各Rb’は独立に、H、重水素、C1〜6アルキル、C2〜6アルケニル、C2〜6アルキニル、C3〜6シクロアルキル、3〜7員ヘテロシクロアルキル、C6〜10アリールおよびヘテロアリールから成る群から選択される〕
の化合物またはその塩。 - RBが−OHである、請求項1に記載の化合物またはその塩。
- RBが
- PGがBoc基である、請求項3に記載の化合物またはその塩。
- Alkが場合により置換されていてよいエチルまたは場合により置換されていてよいプロピルである、請求項3に記載の化合物またはその塩。
- Alk上の任意の置換基が重水素、C1〜6アルキル、C3〜6シクロアルキル、C6−10アリール、−C(O)ORa’、−C(O)NRa’Rb’、−NRa’Rb’、−SRa’、−S(O)Ra’、−S(O)NRa’、−S(O)2Ra’、−S(O)2NRa’または−ORa’であり、ここで、C1〜6アルキル、C3〜6シクロアルキルおよびC6〜10アリールにおける各水素原子は独立に、場合により、重水素、ハロゲン、−OC1〜4アルキル、−NH(C1〜4アルキル)、−N(C1〜4アルキル)2、NHC(O)C1〜4アルキル、−N(C1〜4アルキル)C(O)C1〜4アルキル、−NHC(O)NHC1〜4アルキル、−N(C1〜4アルキル)C(O)NHC1〜4アルキル、NHC(O)N(C1〜4アルキル)2、−N(C1〜4アルキル)C(O)N(C1〜4アルキル)2、−NHC(O)OC1〜4アルキル、−N(C1〜4アルキル)C(O)OC1〜4アルキル、−CO2C1〜4アルキル、−CONH(C1〜4アルキル)、−CON(C1〜4アルキル)2、−SC1〜4アルキル、−S(O)C1〜4アルキル、−S(O)2C1〜4アルキル、−S(O)NH(C1〜4アルキル)、−S(O)2NH(C1〜4アルキル)、−S(O)N(C1〜4アルキル)2、−S(O)2N(C1〜4アルキル)2、C3〜6シクロアルキルまたは3〜7員ヘテロシクロアルキルにより置換されていてよい、請求項5に記載の化合物またはその塩。
- 各RAおよびREが独立に、H、重水素、フルオロ、クロロまたはブロモである、請求項1に記載の化合物またはその塩。
- RAがフルオロ、クロロまたはブロモである、請求項7に記載の化合物またはその塩。
- RAがフルオロである、請求項8に記載の化合物またはその塩。
- REがHである、請求項7に記載の化合物またはその塩。
- RDがHである、請求項1に記載の化合物またはその塩。
- RDがメチル、エチル、シクロプロピル、n−プロピル、イソプロピル、N−メチルピロリジン、2−エタノール、または2−イソプロパノールである、請求項1に記載の化合物またはその塩。
- RCがC1〜6アルキルである、請求項1に記載の化合物またはその塩。
- RCがメチルである、請求項13に記載の化合物またはその塩。
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- 式
- 式
- 式
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201461931506P | 2014-01-24 | 2014-01-24 | |
US61/931,506 | 2014-01-24 | ||
US201462049326P | 2014-09-11 | 2014-09-11 | |
US62/049,326 | 2014-09-11 | ||
US201562106301P | 2015-01-22 | 2015-01-22 | |
US62/106,301 | 2015-01-22 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016566857A Division JP6490713B2 (ja) | 2014-01-24 | 2015-01-23 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
Related Child Applications (1)
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JP2021001588A Division JP2021063121A (ja) | 2014-01-24 | 2021-01-07 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
Publications (2)
Publication Number | Publication Date |
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JP2019104748A JP2019104748A (ja) | 2019-06-27 |
JP2019104748A5 true JP2019104748A5 (ja) | 2019-08-08 |
Family
ID=53682127
Family Applications (5)
Application Number | Title | Priority Date | Filing Date |
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JP2016566857A Active JP6490713B2 (ja) | 2014-01-24 | 2015-01-23 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
JP2019034652A Withdrawn JP2019104748A (ja) | 2014-01-24 | 2019-02-27 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
JP2021001588A Pending JP2021063121A (ja) | 2014-01-24 | 2021-01-07 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
JP2022110613A Active JP7356546B2 (ja) | 2014-01-24 | 2022-07-08 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
JP2023158350A Pending JP2023179539A (ja) | 2014-01-24 | 2023-09-22 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
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JP2016566857A Active JP6490713B2 (ja) | 2014-01-24 | 2015-01-23 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
Family Applications After (3)
Application Number | Title | Priority Date | Filing Date |
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JP2021001588A Pending JP2021063121A (ja) | 2014-01-24 | 2021-01-07 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
JP2022110613A Active JP7356546B2 (ja) | 2014-01-24 | 2022-07-08 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
JP2023158350A Pending JP2023179539A (ja) | 2014-01-24 | 2023-09-22 | タンパク質キナーゼのモジュレータとしてのジアリール大環状化合物 |
Country Status (32)
Country | Link |
---|---|
US (6) | US9714258B2 (ja) |
EP (6) | EP3097107B1 (ja) |
JP (5) | JP6490713B2 (ja) |
KR (1) | KR102402179B1 (ja) |
CN (3) | CN106170289B (ja) |
AP (1) | AP2016009383A0 (ja) |
AU (2) | AU2015209239B2 (ja) |
CA (1) | CA2936079C (ja) |
CL (1) | CL2016001876A1 (ja) |
CY (1) | CY1121850T1 (ja) |
DK (3) | DK3572416T3 (ja) |
EA (2) | EA201892241A1 (ja) |
ES (3) | ES2933350T3 (ja) |
FI (1) | FI3636649T3 (ja) |
HK (1) | HK1231407A1 (ja) |
HR (3) | HRP20221518T1 (ja) |
HU (3) | HUE066590T2 (ja) |
IL (2) | IL246860B (ja) |
LT (3) | LT3097107T (ja) |
MX (2) | MX2016009588A (ja) |
MY (1) | MY193524A (ja) |
NZ (2) | NZ761094A (ja) |
PE (1) | PE20160931A1 (ja) |
PH (1) | PH12016501463A1 (ja) |
PL (3) | PL3097107T3 (ja) |
PT (3) | PT3636649T (ja) |
RS (3) | RS65417B1 (ja) |
SG (2) | SG11201605929RA (ja) |
SI (3) | SI3097107T1 (ja) |
UA (1) | UA121206C2 (ja) |
WO (1) | WO2015112806A2 (ja) |
ZA (2) | ZA201604654B (ja) |
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