JP2016520131A5 - - Google Patents
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- JP2016520131A5 JP2016520131A5 JP2016516830A JP2016516830A JP2016520131A5 JP 2016520131 A5 JP2016520131 A5 JP 2016520131A5 JP 2016516830 A JP2016516830 A JP 2016516830A JP 2016516830 A JP2016516830 A JP 2016516830A JP 2016520131 A5 JP2016520131 A5 JP 2016520131A5
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- Prior art keywords
- optionally substituted
- compound according
- alkyl
- heteroaryl
- compound
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims 15
- -1 substituted Chemical class 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000005842 heteroatoms Chemical group 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- KDDQRKBRJSGMQE-UHFFFAOYSA-N 4-thiazolyl Chemical group [C]1=CSC=N1 KDDQRKBRJSGMQE-UHFFFAOYSA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- CWDWFSXUQODZGW-UHFFFAOYSA-N 5-thiazolyl Chemical group [C]1=CN=CS1 CWDWFSXUQODZGW-UHFFFAOYSA-N 0.000 claims 1
- 102100004328 BRAF Human genes 0.000 claims 1
- 101700004551 BRAF Proteins 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 201000011231 colorectal cancer Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 1
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 229920000728 polyester Polymers 0.000 claims 1
- 150000003230 pyrimidines Chemical class 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 0 Cc(c(C**)c1F)ccc1N(*)S(*)(=O)=O Chemical compound Cc(c(C**)c1F)ccc1N(*)S(*)(=O)=O 0.000 description 2
Claims (15)
- 式(Ia)または(Ib):
Yは、-N(R1)(R2)または-C(R8)(R9)(R10)であり;
R1およびR2は、各々独立して、適宜置換されているアルキル、適宜置換されているアリール、適宜置換されているヘテロアリール、適宜置換されているシクロアルキルであるか;あるいはR1およびR2は、それらが結合している窒素原子と一緒になって、環の構成要素としてO、NまたはSより選択される0〜1個の更なるヘテロ原子を有する適宜置換されている5または6員のヘテロシクロアルキルを形成し;
R8、R9およびR10は、各々独立してH、適宜置換されているC1-6アルキル、適宜置換されているC1-6ハロアルキル、適宜置換されているC1-6ハロアルコキシ、適宜置換されているC3-8シクロアルキル、適宜置換されているアリール、適宜置換されているヘテロシクロアルキル、適宜置換されているヘテロアリールであるか;あるいはR8、R9およびR10基のうちのいずれか2個は、それらが結合している炭素原子と一緒になって、環の構成要素としてN、OまたはSより選択される0〜2個のヘテロ原子を有する3〜8員の適宜置換されている非芳香環を形成し;ただし各々について、R8、R9およびR10基のうちの少なくとも2個は、同時に水素でなく;
R3は、HまたはC1-6アルキルであり;
R4は、ハロゲン、水素、C1-2アルキル、C1-2ハロアルキル、CN、C1-2ハロアルコキシまたはC1-2アルコキシであり;
Lは、結合、-C(O)-、-C(S)-、-C(O)NH-、-NHC(O)-または適宜置換されている-C(=CH2)-であり、ここで、該-C(=CH2)-基中の同一メチレン炭素に結合する2個の置換基は適宜一緒になって、O、NもしくはSより選択される0〜4個のヘテロ原子を有する適宜置換されている5または6員環を形成し、ここで、該NおよびSは適宜酸化され;
Zは、適宜置換されている5員のヘテロアリール、適宜置換されている6員のヘテロアリールまたは適宜置換されている二環式ヘテロアリールであり、ただし、R4がフェニル環上の-L-Z置換基に対してオルト位で結合するとき、Zは、適宜置換されている式:
の骨格以外であり、ここで、波線は分子の残りへの結合位を示し、
そして該化合物は、4-[[(1S)-1-シクロプロピルエチル]アミノ]-5-[3-[[エチル(メチル)スルファモイル]アミノ]-2-フルオロ-ベンゾイル]-7H-ピロロ[2,3-d]ピリミジンではない]
で示される化合物、またはその医薬的に許容される塩、溶媒和物、互変異性体もしくは異性体。 - Yが-N(R1)(R2)である、請求項1に記載の化合物。
- Gが、-NH2または-NH[CH2CH(CH3)NHC(O)OCH3]で置換されているヘテロアリールである、請求項4に記載の化合物。
- Yが-N(R1)(R2)であり、R1およびR2が、各々独立して、適宜置換されているC1-6アルキルである、請求項1〜5のいずれか1つに記載の化合物。
- Yが、1-ピペラジニル、1-ピロリジニル、2-オキソ-1-ピロリジニル、3-オキソ-1-ピロリジニル、1-ピペリジニル、4-モルホリノまたは4-チオモルホリノであり、これらの各々が適宜置換されている、請求項1〜6のいずれか1つに記載の化合物。
- Lが、結合、-C(O)-または-NHC(O)-である、請求項1〜7のいずれか1つに記載の化合物。
- R3がHである、請求項1〜8のいずれか1つに記載の化合物。
- R4が、H、F、Cl、CH3、-CH2CH3、-OCH3、-CF3、-CHF2、-CH2F、CN、-OCF3、-OCHF2または-OCH2Fである、請求項1〜9のいずれか1つに記載の化合物。
- 請求項1〜11のいずれか1つに記載の化合物、および医薬的に許容される担体、希釈剤または賦形剤を含む、医薬組成物。
- 別の治療薬をさらに含む、請求項12に記載の医薬組成物。
- 有効量の請求項1〜11のいずれか1つに記載の化合物を含む、BRAF V600 変異を有する対象を処置するための医薬組成物。
- 有効量の請求項1〜11のいずれか1つに記載の化合物を含む、転移黒色腫、甲状腺癌、結腸直腸癌、肺癌または卵巣癌を患っている対象を処置するための医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361829190P | 2013-05-30 | 2013-05-30 | |
US61/829,190 | 2013-05-30 | ||
PCT/US2014/040076 WO2014194127A1 (en) | 2013-05-30 | 2014-05-29 | Compounds for kinase modulation, and indications therefor |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2016520131A JP2016520131A (ja) | 2016-07-11 |
JP2016520131A5 true JP2016520131A5 (ja) | 2017-07-06 |
Family
ID=51023140
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016516830A Pending JP2016520131A (ja) | 2013-05-30 | 2014-05-29 | キナーゼ調節のための化合物、およびその適応 |
Country Status (18)
Country | Link |
---|---|
US (2) | US9873700B2 (ja) |
EP (1) | EP3004060B1 (ja) |
JP (1) | JP2016520131A (ja) |
KR (1) | KR20160013028A (ja) |
CN (1) | CN105228983A (ja) |
AR (1) | AR096450A1 (ja) |
AU (1) | AU2014274093B2 (ja) |
BR (1) | BR112015028845A2 (ja) |
CA (1) | CA2912568A1 (ja) |
HK (1) | HK1219732A1 (ja) |
IL (1) | IL242587A0 (ja) |
MX (1) | MX2015015966A (ja) |
PH (1) | PH12015502610A1 (ja) |
RU (1) | RU2015149937A (ja) |
SG (1) | SG11201509338QA (ja) |
TW (1) | TW201533028A (ja) |
UY (1) | UY35596A (ja) |
WO (1) | WO2014194127A1 (ja) |
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- 2014-05-29 KR KR1020157033201A patent/KR20160013028A/ko not_active Application Discontinuation
- 2014-05-29 TW TW103118934A patent/TW201533028A/zh unknown
- 2014-05-29 US US14/290,786 patent/US9873700B2/en active Active
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- 2014-05-29 JP JP2016516830A patent/JP2016520131A/ja active Pending
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- 2014-05-29 WO PCT/US2014/040076 patent/WO2014194127A1/en active Application Filing
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