JP2017527578A5 - - Google Patents
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- JP2017527578A5 JP2017527578A5 JP2017513450A JP2017513450A JP2017527578A5 JP 2017527578 A5 JP2017527578 A5 JP 2017527578A5 JP 2017513450 A JP2017513450 A JP 2017513450A JP 2017513450 A JP2017513450 A JP 2017513450A JP 2017527578 A5 JP2017527578 A5 JP 2017527578A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- irritable bowel
- bowel syndrome
- 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.)
- Granted
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- 150000003839 salts Chemical class 0.000 claims 8
- 239000011780 sodium chloride Substances 0.000 claims 8
- 102100006051 RET Human genes 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- -1 2- (dimethylamino) ethyl Chemical group 0.000 claims 4
- 208000002551 Irritable Bowel Syndrome Diseases 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 230000001404 mediated Effects 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 206010010774 Constipation Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 101700001630 RET Proteins 0.000 claims 2
- DLFVBJFMPXGRIB-UHFFFAOYSA-N acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 2
- 208000004998 Abdominal Pain Diseases 0.000 claims 1
- 229940009098 Aspartate Drugs 0.000 claims 1
- CKLJMWTZIZZHCS-UHFFFAOYSA-N DL-aspartic acid Chemical compound OC(=O)C(N)CC(O)=O CKLJMWTZIZZHCS-UHFFFAOYSA-N 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N HCl Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- QIAFMBKCNZACKA-UHFFFAOYSA-M N-benzoylglycinate Chemical compound [O-]C(=O)CNC(=O)C1=CC=CC=C1 QIAFMBKCNZACKA-UHFFFAOYSA-M 0.000 claims 1
- 102000030951 Phosphotransferases Human genes 0.000 claims 1
- 108091000081 Phosphotransferases Proteins 0.000 claims 1
- 206010036772 Proctalgia Diseases 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K [O-]P([O-])([O-])=O Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000000117 functional diarrhea Diseases 0.000 claims 1
- 150000003840 hydrochlorides Chemical class 0.000 claims 1
- 230000002757 inflammatory Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
Claims (12)
- 塩酸塩、アスパラギン酸塩、馬尿酸塩およびリン酸塩からなる群から選択される、請求項1に記載の化合物の薬学的に許容可能な塩。
- 塩酸塩である、請求項1に記載の化合物の薬学的に許容可能な塩。
- 結晶形である、請求項4に記載の薬学的に許容可能な塩。
- 前記結晶形が、CuKα放射線を用いて測定した際に、約8.3,8.4,10.7,11.3,15.5,16.0,20.0,20.4,20.8,22.6,23.2,23.3,23.6,24.6,24.9,25.3,25.9,26.9,27.3,27.4,28.1および28.2度 2θからなる群から選択される、少なくとも3つの回折角を含んでなるX線粉末回折(XRPD)パターンによって特徴付けられる、請求項5に記載の薬学的に許容可能な塩。
- 前記結晶形が、CuKα放射線を用いて測定した際に、約16.0,20.0,22.6,23.3および26.9度 2θの回折角を含んでなるX線粉末回折(XRPD)パターンによって特徴付けられる、請求項5に記載の薬学的に許容可能な塩。
- 請求項1〜7のいずれか一項に記載の化合物または薬学的に許容可能な塩および薬学的に許容可能な賦形剤を含んでなる医薬組成物。
- RET(Rearranged during Transfection)キナーゼにより媒介される疾患の治療のための薬剤の製造における、請求項1〜7のいずれか一項に記載の化合物または薬学的に許容可能な塩の使用。
- RETキナーゼにより媒介される前記疾患が、過敏性腸症候群、過敏性腸症候群に関連する疼痛、機能性便秘、機能性下痢、慢性特発性便秘、機能性腹痛症候群、機能性肛門直腸痛および炎症性腸疾患からなる群から選択される、請求項9に記載の使用。
- RETキナーゼにより媒介される前記疾患が、過敏性腸症候群である、請求項9に記載の使用。
- RETキナーゼにより媒介される前記疾患が、過敏性腸症候群に関連する疼痛である、請求項9に記載の使用。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNPCT/CN2014/086197 | 2014-09-10 | ||
CN2014086197 | 2014-09-10 | ||
CNPCT/CN2015/086995 | 2015-08-14 | ||
CN2015086995 | 2015-08-14 | ||
PCT/IB2015/056905 WO2016038552A1 (en) | 2014-09-10 | 2015-09-09 | Pyridone derivatives as rearranged during transfection (ret) kinase inhibitors |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2019102776A Division JP6728447B2 (ja) | 2014-09-10 | 2019-05-31 | Ret(rearranged during transfection)キナーゼ阻害剤としてのピリジン誘導体 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2017527578A JP2017527578A (ja) | 2017-09-21 |
JP2017527578A5 true JP2017527578A5 (ja) | 2018-10-25 |
JP6538154B2 JP6538154B2 (ja) | 2019-07-03 |
Family
ID=54186249
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2017513450A Expired - Fee Related JP6538154B2 (ja) | 2014-09-10 | 2015-09-09 | Ret(rearranged during transfection)キナーゼ阻害剤としてのピリジン誘導体 |
JP2019102776A Expired - Fee Related JP6728447B2 (ja) | 2014-09-10 | 2019-05-31 | Ret(rearranged during transfection)キナーゼ阻害剤としてのピリジン誘導体 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2019102776A Expired - Fee Related JP6728447B2 (ja) | 2014-09-10 | 2019-05-31 | Ret(rearranged during transfection)キナーゼ阻害剤としてのピリジン誘導体 |
Country Status (35)
Country | Link |
---|---|
US (4) | US9918974B2 (ja) |
EP (2) | EP3517526B1 (ja) |
JP (2) | JP6538154B2 (ja) |
KR (1) | KR20170045350A (ja) |
CN (1) | CN107074768B (ja) |
AU (1) | AU2015313841B2 (ja) |
BR (1) | BR112017004900A2 (ja) |
CA (1) | CA2960768A1 (ja) |
CL (1) | CL2017000588A1 (ja) |
CO (1) | CO2017002273A2 (ja) |
CR (1) | CR20170093A (ja) |
CY (1) | CY1121661T1 (ja) |
DK (1) | DK3191450T3 (ja) |
DO (1) | DOP2017000059A (ja) |
EA (1) | EA033544B1 (ja) |
ES (2) | ES2816453T3 (ja) |
HR (1) | HRP20190815T1 (ja) |
HU (1) | HUE044604T2 (ja) |
IL (1) | IL250908B (ja) |
LT (1) | LT3191450T (ja) |
MA (1) | MA40581A (ja) |
ME (1) | ME03432B (ja) |
MX (1) | MX2017003114A (ja) |
MY (1) | MY181913A (ja) |
PE (1) | PE20170705A1 (ja) |
PH (1) | PH12017500425B1 (ja) |
PL (1) | PL3191450T3 (ja) |
PT (1) | PT3191450T (ja) |
RS (1) | RS58813B1 (ja) |
SG (1) | SG11201701694QA (ja) |
SI (1) | SI3191450T1 (ja) |
TW (1) | TWI683807B (ja) |
UA (1) | UA122213C2 (ja) |
UY (1) | UY36293A (ja) |
WO (1) | WO2016038552A1 (ja) |
Families Citing this family (23)
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EP3521291A1 (en) | 2010-05-20 | 2019-08-07 | Array Biopharma, Inc. | Macrocyclic compounds as trk kinase inhibitors |
CR20170094A (es) | 2014-09-10 | 2017-05-08 | Glaxosmithkline Ip Dev Ltd | Nuevos compuestos como inhibidores de reorganizado durante la transfección (ret) |
EP3517526B1 (en) | 2014-09-10 | 2020-08-19 | GlaxoSmithKline Intellectual Property Development Limited | Pyridinones as rearranged during transfection (ret) inhibitors |
US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
RS61485B1 (sr) | 2015-07-16 | 2021-03-31 | Array Biopharma Inc | Supstituisana pirazolo [1,5-a] piridinska jedinjenja kao inhibitori ret kinaze |
SG11201803653QA (en) | 2015-11-02 | 2018-05-30 | Blueprint Medicines Corp | Inhibitors of ret |
TW201738228A (zh) | 2016-03-17 | 2017-11-01 | 藍圖醫藥公司 | Ret之抑制劑 |
US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
JP2018052878A (ja) * | 2016-09-29 | 2018-04-05 | 第一三共株式会社 | ピリジン化合物 |
TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
CA3049136C (en) | 2017-01-18 | 2022-06-14 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
US20210290620A1 (en) | 2017-05-15 | 2021-09-23 | Blueprint Medicines Corporation | Combinations of RET Inhibitors and mTORC1 Inhibitors and Uses Thereof for the Treatment of Cancer Mediated by Aberrant RET Activity |
TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
JP7061195B2 (ja) | 2018-01-18 | 2022-04-27 | アレイ バイオファーマ インコーポレイテッド | RETキナーゼ阻害剤としての置換ピラゾロ[3,4-d]ピリミジン化合物 |
CA3087354C (en) | 2018-01-18 | 2023-01-03 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
CA3096043A1 (en) | 2018-04-03 | 2019-10-10 | Blueprint Medicines Corporation | Ret inhibitor for use in treating cancer having a ret alteration |
EP3849986B1 (en) | 2018-09-10 | 2022-06-08 | Array Biopharma, Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
WO2022017524A1 (zh) * | 2020-07-23 | 2022-01-27 | 深圳晶泰科技有限公司 | 吡啶酮类化合物及其制备方法和应用 |
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US8937071B2 (en) | 2013-03-15 | 2015-01-20 | Glaxosmithkline Intellectual Property Development Limited | Compounds as rearranged during transfection (RET) inhibitors |
PL2970191T3 (pl) | 2013-03-15 | 2017-07-31 | Glaxosmithkline Intellectual Property Development Limited | Pochodne pirydyny jako inhibitory kinazy przebudowanej podczas transfekcji (RET) |
EP3517526B1 (en) | 2014-09-10 | 2020-08-19 | GlaxoSmithKline Intellectual Property Development Limited | Pyridinones as rearranged during transfection (ret) inhibitors |
CR20170094A (es) | 2014-09-10 | 2017-05-08 | Glaxosmithkline Ip Dev Ltd | Nuevos compuestos como inhibidores de reorganizado durante la transfección (ret) |
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2015
- 2015-09-09 EP EP19160650.8A patent/EP3517526B1/en active Active
- 2015-09-09 AU AU2015313841A patent/AU2015313841B2/en not_active Ceased
- 2015-09-09 BR BR112017004900A patent/BR112017004900A2/pt not_active IP Right Cessation
- 2015-09-09 WO PCT/IB2015/056905 patent/WO2016038552A1/en active Application Filing
- 2015-09-09 CR CR20170093A patent/CR20170093A/es unknown
- 2015-09-09 ES ES19160650T patent/ES2816453T3/es active Active
- 2015-09-09 US US15/509,613 patent/US9918974B2/en not_active Expired - Fee Related
- 2015-09-09 CA CA2960768A patent/CA2960768A1/en not_active Abandoned
- 2015-09-09 ES ES15767599T patent/ES2725704T3/es active Active
- 2015-09-09 ME MEP-2019-136A patent/ME03432B/me unknown
- 2015-09-09 PE PE2017000417A patent/PE20170705A1/es unknown
- 2015-09-09 LT LTEP15767599.2T patent/LT3191450T/lt unknown
- 2015-09-09 MA MA040581A patent/MA40581A/fr unknown
- 2015-09-09 SI SI201530720T patent/SI3191450T1/sl unknown
- 2015-09-09 DK DK15767599.2T patent/DK3191450T3/da active
- 2015-09-09 PT PT15767599T patent/PT3191450T/pt unknown
- 2015-09-09 SG SG11201701694QA patent/SG11201701694QA/en unknown
- 2015-09-09 KR KR1020177009237A patent/KR20170045350A/ko not_active Application Discontinuation
- 2015-09-09 JP JP2017513450A patent/JP6538154B2/ja not_active Expired - Fee Related
- 2015-09-09 RS RS20190559A patent/RS58813B1/sr unknown
- 2015-09-09 CN CN201580058320.5A patent/CN107074768B/zh not_active Expired - Fee Related
- 2015-09-09 UA UAA201703478A patent/UA122213C2/uk unknown
- 2015-09-09 EP EP15767599.2A patent/EP3191450B1/en active Active
- 2015-09-09 PL PL15767599T patent/PL3191450T3/pl unknown
- 2015-09-09 EA EA201790546A patent/EA033544B1/ru not_active IP Right Cessation
- 2015-09-09 MX MX2017003114A patent/MX2017003114A/es active IP Right Grant
- 2015-09-09 HU HUE15767599 patent/HUE044604T2/hu unknown
- 2015-09-09 MY MYPI2017700782A patent/MY181913A/en unknown
- 2015-09-10 TW TW104129876A patent/TWI683807B/zh not_active IP Right Cessation
- 2015-09-10 UY UY0001036293A patent/UY36293A/es unknown
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2017
- 2017-03-02 IL IL250908A patent/IL250908B/en active IP Right Grant
- 2017-03-07 DO DO2017000059A patent/DOP2017000059A/es unknown
- 2017-03-07 PH PH12017500425A patent/PH12017500425B1/en unknown
- 2017-03-07 CO CONC2017/0002273A patent/CO2017002273A2/es unknown
- 2017-03-09 CL CL2017000588A patent/CL2017000588A1/es unknown
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2018
- 2018-01-23 US US15/877,524 patent/US10111866B2/en not_active Expired - Fee Related
- 2018-09-28 US US16/145,271 patent/US10292975B2/en not_active Expired - Fee Related
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2019
- 2019-04-05 US US16/376,858 patent/US10709695B2/en active Active
- 2019-05-02 HR HRP20190815TT patent/HRP20190815T1/hr unknown
- 2019-05-09 CY CY20191100502T patent/CY1121661T1/el unknown
- 2019-05-31 JP JP2019102776A patent/JP6728447B2/ja not_active Expired - Fee Related
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