JP2015529681A5 - - Google Patents
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- JP2015529681A5 JP2015529681A5 JP2015532068A JP2015532068A JP2015529681A5 JP 2015529681 A5 JP2015529681 A5 JP 2015529681A5 JP 2015532068 A JP2015532068 A JP 2015532068A JP 2015532068 A JP2015532068 A JP 2015532068A JP 2015529681 A5 JP2015529681 A5 JP 2015529681A5
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- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- hydrate
- compound
- salt
- 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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- 239000011780 sodium chloride Substances 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 18
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- -1 2-((4- (benzo [d] thiazol-5-ylamino) -6- (tert-butylsulfonyl) quinazolin-7-yl) oxy) ethyl Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 206010009900 Colitis ulcerative Diseases 0.000 claims 3
- 206010011401 Crohn's disease Diseases 0.000 claims 3
- 201000006704 ulcerative colitis Diseases 0.000 claims 3
- 208000009766 Blau syndrome Diseases 0.000 claims 2
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 2
- 206010021972 Inflammatory bowel disease Diseases 0.000 claims 2
- LMLSTUCUPVCKEU-UHFFFAOYSA-N O.O.O.O.O.O.[Ca] Chemical compound O.O.O.O.O.O.[Ca] LMLSTUCUPVCKEU-UHFFFAOYSA-N 0.000 claims 2
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 2
- 206010046851 Uveitis Diseases 0.000 claims 2
- 159000000007 calcium salts Chemical group 0.000 claims 2
- 239000000546 pharmaceutic aid Substances 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 201000000306 sarcoidosis Diseases 0.000 claims 2
- 206010069351 Acute lung injury Diseases 0.000 claims 1
- 206010003246 Arthritis Diseases 0.000 claims 1
- 208000006673 Asthma Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N HCl Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 208000006897 Interstitial Lung Disease Diseases 0.000 claims 1
- 206010053219 Non-alcoholic steatohepatitis Diseases 0.000 claims 1
- 102100014280 RIPK2 Human genes 0.000 claims 1
- 101700084307 RIPK2 Proteins 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000001072 Type 2 Diabetes Mellitus Diseases 0.000 claims 1
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims 1
- 201000004624 dermatitis Diseases 0.000 claims 1
- 231100000406 dermatitis Toxicity 0.000 claims 1
- 235000019700 dicalcium phosphate Nutrition 0.000 claims 1
- 230000000302 ischemic Effects 0.000 claims 1
- 230000001404 mediated Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 210000000056 organs Anatomy 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 201000003774 sarcomatosis Diseases 0.000 claims 1
- 159000000000 sodium salts Chemical group 0.000 claims 1
- 201000010874 syndrome Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 150000004684 trihydrates Chemical class 0.000 claims 1
Claims (17)
- リン酸二水素2−((4−(ベンゾ[d]チアゾール−5−イルアミノ)−6−(tert−ブチルスルホニル)キナゾリン−7−イル)オキシ)エチルである、請求項1に記載の化合物、またはその薬学的に許容可能な塩、またはその水和物。
- 前記化合物の薬学的に許容可能な塩である、請求項1に記載の化合物、またはその薬学的に許容可能な塩、またはその水和物。
- 薬学的に許容可能な塩がナトリウム塩である、請求項3に記載の化合物、またはその薬学的に許容可能な塩、またはその水和物。
- 薬学的に許容可能な塩が塩酸塩である、請求項3に記載の化合物、またはその薬学的に許容可能な塩、またはその水和物。
- リン酸二水素2−((4−(ベンゾ[d]チアゾール−5−イルアミノ)−6−(tert−ブチルスルホニル)キナゾリン−7−イル)オキシ)エチル塩酸塩一水和物である、請求項1に記載の化合物、またはその薬学的に許容可能な塩、またはその水和物。
- 図2のPXRDを備えた結晶性のリン酸二水素2−((4−(ベンゾ[d]チアゾール−5−イルアミノ)−6−(tert−ブチルスルホニル)キナゾリン−7−イル)オキシ)エチル塩酸塩一水和物である、請求項1に記載の化合物、またはその薬学的に許容可能な塩、またはその水和物。
- 薬学的に許容可能な塩がカルシウム塩である、請求項3に記載の化合物、またはその薬学的に許容可能な塩、またはその水和物。
- 前記化合物のカルシウム塩の水和物である、請求項1に記載の化合物、またはその薬学的に許容可能な塩、またはその水和物。
- 前記化合物のヘミカルシウム塩の水和物である、請求項1に記載の化合物、またはその薬学的に許容可能な塩、またはその水和物。
- 図1のPXRDを備えた結晶性のリン酸水素カルシウム(I)2−((4−(ベンゾ[d]チアゾール−5−イルアミノ)−6−(tert−ブチルスルホニル)キナゾリン−7−イル)オキシ)エチル三水和物である、請求項11に記載の化合物のヘミカルシウム塩の三水和物。
- 請求項1に記載の化合物、またはその薬学上許容可能な塩、またはその水和物と、薬学的に許容可能な賦形剤とを含んでなる医薬組成物。
- 請求項11に記載の化合物のヘミカルシウム塩の三水和物と、薬学的に許容可能な賦形剤とを含んでなる医薬組成物。
- RIP2キナーゼにより媒介される疾患を治療するための、請求項13または14に記載の医薬組成物であって、該疾患が、ブドウ膜炎、皮膚炎、急性肺傷害、2型真性糖尿病、関節炎、関節リウマチ、潰瘍性大腸炎、クローン病、早期発症炎症性腸疾患、腸管外炎症性腸疾患、臓器移植における虚血性再潅流傷害の予防、非アルコール性脂肪性肝炎、自己免疫性肝炎、喘息、全身性紅斑性狼瘡、多発性硬化症、類肉腫症、ブラウ症候群/早期発症類肉腫症、ウェゲナー肉芽腫症、および間質性肺疾患から選択される、医薬組成物。
- 前記疾患が、ブドウ膜炎、ブラウ症候群、早期発症類肉腫症、潰瘍性大腸炎、クローン病、ウェゲナー肉芽腫症および類肉腫症から選択される、請求項13または14に記載の医薬組成物。
- 前記疾患が、クローン病、潰瘍性大腸炎、ブラウ症候群、または関節リウマチである、請求項13または14に記載の医薬組成物。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261700422P | 2012-09-13 | 2012-09-13 | |
US61/700,422 | 2012-09-13 | ||
US201361767387P | 2013-02-21 | 2013-02-21 | |
US61/767,387 | 2013-02-21 | ||
PCT/US2013/059619 WO2014043446A1 (en) | 2012-09-13 | 2013-09-13 | Prodrugs of amino quinazoline kinase inhibitor |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2015529681A JP2015529681A (ja) | 2015-10-08 |
JP2015529681A5 true JP2015529681A5 (ja) | 2016-10-20 |
JP6246813B2 JP6246813B2 (ja) | 2017-12-13 |
Family
ID=50278703
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015532068A Expired - Fee Related JP6246813B2 (ja) | 2012-09-13 | 2013-09-13 | アミノキナゾリンキナーゼ阻害剤のプロドラッグ |
Country Status (33)
Country | Link |
---|---|
US (3) | US9586953B2 (ja) |
EP (2) | EP3323819B1 (ja) |
JP (1) | JP6246813B2 (ja) |
KR (1) | KR102101527B1 (ja) |
CN (1) | CN104619327B (ja) |
AR (1) | AR092529A1 (ja) |
AU (1) | AU2013315396B2 (ja) |
BR (1) | BR112015005694A2 (ja) |
CA (1) | CA2886467C (ja) |
CL (1) | CL2015000614A1 (ja) |
CR (1) | CR20150132A (ja) |
CY (1) | CY1120236T1 (ja) |
DK (1) | DK2895174T3 (ja) |
DO (1) | DOP2015000060A (ja) |
EA (1) | EA028146B1 (ja) |
ES (1) | ES2663237T3 (ja) |
HK (2) | HK1212223A1 (ja) |
HR (1) | HRP20180411T1 (ja) |
HU (1) | HUE036347T2 (ja) |
IL (1) | IL237263B (ja) |
LT (1) | LT2895174T (ja) |
ME (1) | ME02985B (ja) |
MX (1) | MX371356B (ja) |
NZ (1) | NZ628452A (ja) |
PE (1) | PE20150635A1 (ja) |
PH (1) | PH12015500363A1 (ja) |
PL (1) | PL2895174T3 (ja) |
PT (1) | PT2895174T (ja) |
RS (1) | RS57144B1 (ja) |
SG (1) | SG11201501139RA (ja) |
SI (1) | SI2895174T1 (ja) |
TW (1) | TWI592417B (ja) |
WO (1) | WO2014043446A1 (ja) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2680844B1 (en) | 2011-03-04 | 2016-10-19 | GlaxoSmithKline Intellectual Property Development Limited | Amino-quinolines as kinase inhibitors |
TWI547494B (zh) | 2011-08-18 | 2016-09-01 | 葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之胺基喹唑啉類 |
TWI592417B (zh) | 2012-09-13 | 2017-07-21 | 葛蘭素史克智慧財產發展有限公司 | 胺基喹唑啉激酶抑制劑之前藥 |
TW201425307A (zh) | 2012-09-13 | 2014-07-01 | Glaxosmithkline Llc | 作為激酶抑制劑之胺基-喹啉類 |
RU2662810C2 (ru) | 2013-02-21 | 2018-07-31 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Хиназолины в качестве ингибиторов киназы |
GB201506872D0 (en) * | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
RU2748260C2 (ru) * | 2016-04-04 | 2021-05-21 | Кемосентрикс, Инк. | РАСТВОРИМЫЕ С5аR АНТАГОНИСТЫ |
WO2018052772A1 (en) | 2016-09-15 | 2018-03-22 | Boehringer Ingelheim International Gmbh | Heteroaryl carboxamide compounds as inhibitors of ripk2 |
WO2020043122A1 (zh) * | 2018-08-28 | 2020-03-05 | 南京明德新药研发有限公司 | 作为rip2激酶抑制剂的喹唑啉类衍生物 |
WO2020094613A1 (en) | 2018-11-06 | 2020-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Nod2 inhibitors for the treatment of hereditary periodic fevers |
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US20130053375A1 (en) | 2010-05-07 | 2013-02-28 | Glaxo Group Limited | Amino-quinolines as kinase inhibitors |
UY33549A (es) | 2010-08-10 | 2012-01-31 | Glaxo Group Ltd | Quinolil aminas como agentes inhibidores de las quinasas |
US8609672B2 (en) | 2010-08-27 | 2013-12-17 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
ES2590778T3 (es) | 2011-02-28 | 2016-11-23 | Calitor Sciences, Llc | Compuestos de quinolina sustituida |
EP2680844B1 (en) | 2011-03-04 | 2016-10-19 | GlaxoSmithKline Intellectual Property Development Limited | Amino-quinolines as kinase inhibitors |
TWI547494B (zh) | 2011-08-18 | 2016-09-01 | 葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之胺基喹唑啉類 |
TW201425307A (zh) | 2012-09-13 | 2014-07-01 | Glaxosmithkline Llc | 作為激酶抑制劑之胺基-喹啉類 |
TWI592417B (zh) | 2012-09-13 | 2017-07-21 | 葛蘭素史克智慧財產發展有限公司 | 胺基喹唑啉激酶抑制劑之前藥 |
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