JP2019034943A5 - - Google Patents
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- JP2019034943A5 JP2019034943A5 JP2018177094A JP2018177094A JP2019034943A5 JP 2019034943 A5 JP2019034943 A5 JP 2019034943A5 JP 2018177094 A JP2018177094 A JP 2018177094A JP 2018177094 A JP2018177094 A JP 2018177094A JP 2019034943 A5 JP2019034943 A5 JP 2019034943A5
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- 150000001875 compounds Chemical class 0.000 claims 25
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 7
- -1 pyridin-2-one-yl Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000001246 bromo group Chemical group Br* 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 4
- 208000002672 Hepatitis B Diseases 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 241000700721 Hepatitis B virus Species 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 206010073071 Hepatocellular carcinoma Diseases 0.000 claims 1
- 230000019552 anatomical structure morphogenesis Effects 0.000 claims 1
- 125000004429 atoms Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 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
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000004044 liver cirrhosis Diseases 0.000 claims 1
- 201000009673 liver disease Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([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
- 230000001575 pathological Effects 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 0 *NC(c(cc(cc1)S(N*)=O)c1F)=O Chemical compound *NC(c(cc(cc1)S(N*)=O)c1F)=O 0.000 description 2
Claims (25)
- 式(I)の化合物、またはその鏡像異性体、ジアステレオ異性体、水和物もしくは溶媒和物:
(式中:
Aが、S(=O)2およびC(=O)から成る群から選択され;
R1が、メチル、エチル、n−プロピル、イソプロピル、n−ブチル、tert−ブチル、
から成る群より選択され;かつ
R2がHであるか、または
R1およびR2が、
が、
から成る群から選択されるように選択され、
R3が、置換されたアリール、および置換されていてもよいヘテロアリールから成る群から選択され、R3における該ヘテロアリールは、ピリジニル、ピリジン−2−オン−イルおよびピリミジニルから成る群から選択され;
R4が、水素およびC1〜6直鎖アルキルから成る群から選択され;
R5が、Hであり;
R6がHであり、かつR8がFであるか、またはR6がFであり、かつR8が、Hであり;
R7が、水素、ハロゲン、置換されていてもよいC1〜6直鎖アルキル、置換されていてもよいC1〜6分岐鎖アルキル、OR9、シアノおよびN(R9)2から成る群から選択され;
R9が、各存在において、独立して、水素、置換されていてもよいC1〜6直鎖アルキル、置換されていてもよいC1〜6分岐鎖アルキル、置換されていてもよいC3〜7シクロアルキル、置換されていてもよいベンジル、および置換されていてもよいヘテロシクリルから成る群から選択され;
ここで、前記置換された各基は、独立して、C1〜6アルキル、C1〜6ハロアルキル、C2〜8アルケニル、C2〜8アルキニル、C3〜14シクロアルキル、−F、−Cl、−Br、−I、−CN、−NO2、−OR14、−SR14、−N(R14)2、−NR14C(=O)R14、−S(=O)2R14、−S(=O)2OR14、−S(=O)2N(R14)2、−C(=O)R14、−C(=O)OR14、−C(=O)N(R14)2、ヘテロシクリル、フェニル、ピリジニル、ピリジン−2−オン−イルおよびピリミジニルから成る群から選択される少なくとも1つの置換基で置換されており、
該R14は、各存在において、独立して、水素、C1〜6アルキル、C1〜6ハロアルキル、C2〜8アルケニル、C2〜8アルキニル、およびC3〜6シクロアルキルから成る群から選択されるか、または2つのR14単位が、それらが結合している原子と一緒になって、置換されていてもよい3〜7員の炭素環基、または置換されていてもよい3〜7員の複素環基を形成し;
但し、
AがSO2であり;かつR3が置換されていてもよいフェニルである場合、R1またはR2は、個々にもしくは一緒になった時のいずれかで、ヒドロキシル基を含まない。 - AがS(=O)2である、請求項1記載の化合物。
- AがC(=O)である、請求項1記載の化合物。
- R4が、水素である、請求項1〜3のいずれか一項記載の化合物。
- R3が、置換されたフェニル、置換されていてもよいピリジン−2−オン−イル、および置換されていてもよいピリジルから成る群から選択される、請求項1〜4のいずれか一項記載の化合物。
- R3が、少なくとも1つのハロまたはC1〜6アルキルで置換されている、請求項1〜4のいずれか一項記載の化合物。
- R3が、少なくとも1つのハロで置換されている、請求項1〜4のいずれか一項記載の化合物。
- R7が、HまたはFである、請求項1〜9のいずれか一項記載の化合物。
- R7およびR8が、各々、Hである、請求項1〜11のいずれか一項記載の化合物。
- −N(R1)(R2)部分が、ヒドロキシルを含まない、請求項1記載の化合物。
- 請求項1〜19のいずれか一項記載の少なくとも1つの化合物、および薬学的に許容される賦形剤を含む、医薬組成物。
- 対象におけるB型肝炎ウイルス感染症を治療または予防するための医薬組成物であって、有効な量の請求項1〜19のいずれか一項記載の少なくとも1つの化合物、またはその鏡像異性体、ジアステレオマー、薬学的に許容される塩、水和物もしくは溶媒和物を含む、医薬組成物。
- 肝硬変または肝細胞がんを含む、肝疾患に関連する病態を管理または改善する、請求項21記載の医薬組成物。
- B型肝炎ウイルス感染症を治療または予防する少なくとも1つの追加の治療薬をさらに含む、請求項21記載の医薬組成物。
- 対象におけるB型肝炎ウイルスの複製およびB型肝炎ウイルスの形態形成から成る群より選択される少なくとも1つを抑制するための医薬組成物であって、有効な量の請求項1〜19のいずれか一項記載の少なくとも1つの化合物、またはその鏡像異性体、ジアステレオマー、薬学的に許容される塩、水和物もしくは溶媒和物を含む、医薬組成物。
- B型肝炎ウイルス感染症を治療または予防する少なくとも1つの追加の治療薬をさらに含む、請求項24記載の医薬組成物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261746552P | 2012-12-27 | 2012-12-27 | |
US61/746,552 | 2012-12-27 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015550788A Division JP6409001B2 (ja) | 2012-12-27 | 2013-12-27 | Hbv感染に対する新規抗ウイルス剤 |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2019034943A JP2019034943A (ja) | 2019-03-07 |
JP2019034943A5 true JP2019034943A5 (ja) | 2019-06-06 |
Family
ID=51022201
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015550788A Expired - Fee Related JP6409001B2 (ja) | 2012-12-27 | 2013-12-27 | Hbv感染に対する新規抗ウイルス剤 |
JP2018177094A Pending JP2019034943A (ja) | 2012-12-27 | 2018-09-21 | Hbv感染に対する新規抗ウイルス剤 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015550788A Expired - Fee Related JP6409001B2 (ja) | 2012-12-27 | 2013-12-27 | Hbv感染に対する新規抗ウイルス剤 |
Country Status (15)
Country | Link |
---|---|
US (2) | US9938236B2 (ja) |
EP (1) | EP2938338A4 (ja) |
JP (2) | JP6409001B2 (ja) |
KR (1) | KR101942151B1 (ja) |
CN (1) | CN105209031A (ja) |
AU (2) | AU2013370300B2 (ja) |
BR (1) | BR112015015584A2 (ja) |
CA (1) | CA2896554C (ja) |
EA (1) | EA201591220A1 (ja) |
HK (1) | HK1217649A1 (ja) |
IL (2) | IL239397B (ja) |
MX (1) | MX2015008471A (ja) |
PH (1) | PH12015501473A1 (ja) |
SG (2) | SG10201803698UA (ja) |
WO (1) | WO2014106019A2 (ja) |
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