JP2015537020A5 - - Google Patents
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- JP2015537020A5 JP2015537020A5 JP2015542270A JP2015542270A JP2015537020A5 JP 2015537020 A5 JP2015537020 A5 JP 2015537020A5 JP 2015542270 A JP2015542270 A JP 2015542270A JP 2015542270 A JP2015542270 A JP 2015542270A JP 2015537020 A5 JP2015537020 A5 JP 2015537020A5
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- Prior art keywords
- alkyl
- hydrogen
- formula
- pharmaceutically acceptable
- tautomer
- Prior art date
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 10
- 150000001875 compounds Chemical class 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 239000011780 sodium chloride Substances 0.000 claims description 8
- 239000012453 solvate Substances 0.000 claims description 8
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- SDTFBAXSPXZDKC-UHFFFAOYSA-N 2-imino-1,2,3,4-tetrahydroquinazolin-4-one Chemical class C1=CC=C2C(=O)NC(N)=NC2=C1 SDTFBAXSPXZDKC-UHFFFAOYSA-N 0.000 claims description 2
- 102100006355 TLR7 Human genes 0.000 claims description 2
- 101700075266 TLR7 Proteins 0.000 claims description 2
- 102100006354 TLR8 Human genes 0.000 claims description 2
- 101700071772 TLR8 Proteins 0.000 claims description 2
- 239000000969 carrier Substances 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 239000011737 fluorine Substances 0.000 claims description 2
- YCKRFDGAMUMZLT-UHFFFAOYSA-N fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 claims description 2
- 230000000051 modifying Effects 0.000 claims description 2
- -1 -O- (C 1-3 ) -alkyl Inorganic materials 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000005842 heteroatoms Chemical group 0.000 description 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 2
- 239000000126 substance Substances 0.000 description 1
Description
本発明は、以下の態様を包含し得る。
［１］
式（Ｉ）の化合物
（式中、
Ｒ １ は次の構造
Ｒ ２ は、水素、−Ｏ−（Ｃ １〜３ ）−アルキル、ハロゲン、（Ｃ １〜３ ）−アルキル、−Ｏ−（Ｃ １〜３ ）−アルキル−Ｏ−（Ｃ １〜３ ）−アルキルまたはＣＨ ２ ＯＨであり、
Ｒ ３ は、水素、−Ｏ−（Ｃ １〜３ ）−アルキル、ハロゲン、（Ｃ １〜３ ）−アルキルまたは−Ｃ（＝Ｏ）−Ｒ ７ であり、ここでＲ ７ は、−Ｏ−（Ｃ １〜３ ）−アルキル、ＮＨ ２ 、ＮＨ（ＣＨ ３ ）、Ｎ（ＣＨ ３ ） ２ 、Ｎ（ＣＨ ３ ）（Ｃ １〜３ ）−アルキル、Ｎ（（Ｃ １〜３ ）−アルキル） ２ またはピロリジンであり、
Ｒ ４ は水素またはフッ素であり、
Ｒ ５ は、（Ｃ １〜３ ）−アルキル、（Ｃ １〜３ ）−フルオロ−アルキルまたはＣＨ ２ ＯＨであり、
Ｒ ６ は、ＮＨ ２ 、ＮＨ（ＣＨ ３ ）もしくはＮ（ＣＨ ３ ） ２ 、Ｒ ８ 、Ｒ ９ 、Ｒ １０ 、Ｒ １１ またはＲ １２ のうち１つまたは複数で任意選択的に置換された（ヘテロ）−アニリン、またはＲ ８ 、Ｒ ９ 、Ｒ １０ 、Ｒ １１ またはＲ １２ のうち１つまたは複数で任意選択的に置換された（ヘテロ）−ベンジルアミンであり、
Ｒ ８ 、Ｒ ９ 、Ｒ １０ 、Ｒ １１ およびＲ １２ は、同一であるか、または異なっており、水素、（Ｃ １〜３ ）−アルキル、−Ｏ−（Ｃ １〜３ ）−アルキルまたはハロゲンからそれぞれ独立に選択され、
かつ
Ｒ １３ は、水素、（Ｃ １〜３ ）−アルキルまたは（Ｃ １〜３ ）−フルオロ−アルキルである）
またはその薬学的に許容できる塩、互変異性体、立体異性体の形態、溶媒和物もしくは多形体。
［２］
上記［１］に記載の式（Ｉ）の化合物またはその薬学的に許容できる塩、互変異性体、立体異性体の形態、溶媒和物もしくは多形体を、１種または複数種の薬学的に許容できる賦形剤、希釈剤または担体とともに含む医薬組成物。
［３］
薬剤として使用するための、上記［１］に記載の式（Ｉ）の化合物またはその薬学的に許容できる塩、互変異性体、立体異性体の形態、溶媒和物もしくは多形体、または上記［２］に記載の医薬組成物。
［４］
ＴＬＲ７および／またはＴＬＲ８の調節が関与する障害の治療に使用するための、上記［１］に記載の式（Ｉ）の化合物またはその薬学的に許容できる塩、互変異性体、立体異性体の形態、溶媒和物もしくは多形体、または上記［２］に記載の医薬組成物。
［５］
次式を有する置換２−アミノ−４−ヒドロキシキナゾリン。
Claims (5)
- 式（Ｉ）の化合物
（式中、
Ｒ１は次の構造
のうちのいずれかであり、
Ｒ２は、水素、−Ｏ−（Ｃ１〜３）−アルキル、ハロゲン、（Ｃ１〜３）−アルキル、−Ｏ−（Ｃ１〜３）−アルキル−Ｏ−（Ｃ１〜３）−アルキルまたはＣＨ２ＯＨであり、
Ｒ３は、水素、−Ｏ−（Ｃ１〜３）−アルキル、ハロゲンまたは（Ｃ１〜３）−アルキルであり、
Ｒ４は水素またはフッ素であり、
Ｒ５は、（Ｃ１〜３）−アルキル、（Ｃ１〜３）−フルオロ−アルキルまたはＣＨ２ＯＨであり、
Ｒ ８、Ｒ９、Ｒ１０、Ｒ１１およびＲ１２は、同一であるか、または異なっており、水素、（Ｃ１〜３）−アルキル、−Ｏ−（Ｃ１〜３）−アルキルまたはハロゲンからそれぞれ独立に選択され、
かつ
Ｒ１３は、水素、（Ｃ１〜３）−アルキルまたは（Ｃ１〜３）−フルオロ−アルキルである）
またはその薬学的に許容できる塩、互変異性体、立体異性体の形態、溶媒和物もしくは多形体。 - 請求項１に記載の式（Ｉ）の化合物またはその薬学的に許容できる塩、互変異性体、立体異性体の形態、溶媒和物もしくは多形体を、１種または複数種の薬学的に許容できる賦形剤、希釈剤または担体とともに含む医薬組成物。
- 薬剤として使用するための、請求項１に記載の式（Ｉ）の化合物またはその薬学的に許容できる塩、互変異性体、立体異性体の形態、溶媒和物もしくは多形体、または請求項２に記載の医薬組成物。
- ＴＬＲ７および／またはＴＬＲ８の調節が関与する障害の治療に使用するための、請求項１に記載の式（Ｉ）の化合物またはその薬学的に許容できる塩、互変異性体、立体異性体の形態、溶媒和物もしくは多形体、または請求項２に記載の医薬組成物。
- 次式を有する置換２−アミノ−４−ヒドロキシキナゾリン。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12192970 | 2012-11-16 | ||
| EP12192970.7 | 2012-11-16 | ||
| PCT/EP2013/073901 WO2014076221A1 (en) | 2012-11-16 | 2013-11-15 | Heterocyclic substituted 2-amino-quinazoline derivatives for the treatment of viral infections |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015537020A JP2015537020A (ja) | 2015-12-24 |
| JP2015537020A5 true JP2015537020A5 (ja) | 2018-02-01 |
| JP6297055B2 JP6297055B2 (ja) | 2018-03-20 |
Family
ID=47189782
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015542270A Active JP6297055B2 (ja) | 2012-11-16 | 2013-11-15 | ウイルス感染症の治療のための複素環置換２−アミノ−キナゾリン誘導体 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US9663474B2 (ja) |
| EP (1) | EP2925729B1 (ja) |
| JP (1) | JP6297055B2 (ja) |
| KR (1) | KR102253773B1 (ja) |
| CN (1) | CN105051018B (ja) |
| AU (1) | AU2013346793B2 (ja) |
| BR (1) | BR112015011036B1 (ja) |
| CA (1) | CA2886635C (ja) |
| CL (1) | CL2015001265A1 (ja) |
| DK (1) | DK2925729T3 (ja) |
| EA (1) | EA035431B1 (ja) |
| ES (1) | ES2655843T3 (ja) |
| IL (1) | IL237864A (ja) |
| MX (1) | MX361585B (ja) |
| MY (1) | MY171115A (ja) |
| NZ (2) | NZ706226A (ja) |
| PH (1) | PH12015500983B1 (ja) |
| PL (1) | PL2925729T3 (ja) |
| SG (1) | SG11201503042QA (ja) |
| UA (1) | UA118341C2 (ja) |
| WO (1) | WO2014076221A1 (ja) |
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