JP2020518582A5 - - Google Patents
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- Publication number
- JP2020518582A5 JP2020518582A5 JP2019559304A JP2019559304A JP2020518582A5 JP 2020518582 A5 JP2020518582 A5 JP 2020518582A5 JP 2019559304 A JP2019559304 A JP 2019559304A JP 2019559304 A JP2019559304 A JP 2019559304A JP 2020518582 A5 JP2020518582 A5 JP 2020518582A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline
- hydrate
- pharmaceutical composition
- succinate
- oxalate
- 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
Links
- ZDYUUBIMAGBMPY-UHFFFAOYSA-N oxalic acid;hydrate Chemical compound O.OC(=O)C(O)=O ZDYUUBIMAGBMPY-UHFFFAOYSA-N 0.000 claims description 31
- SXDQRQUWNQKZBL-UHFFFAOYSA-N butanedioic acid;hydrate Chemical compound O.OC(=O)CCC(O)=O SXDQRQUWNQKZBL-UHFFFAOYSA-N 0.000 claims description 26
- 238000000034 method Methods 0.000 claims description 19
- 239000008194 pharmaceutical composition Substances 0.000 claims description 19
- 208000023504 respiratory system disease Diseases 0.000 claims description 18
- 241000124008 Mammalia Species 0.000 claims description 14
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims description 13
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 12
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 claims description 8
- 208000029523 Interstitial Lung disease Diseases 0.000 claims description 8
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 8
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 8
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Substances C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 7
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 6
- 208000006673 asthma Diseases 0.000 claims description 6
- WJJMNDUMQPNECX-UHFFFAOYSA-N dipicolinic acid Chemical compound OC(=O)C1=CC=CC(C(O)=O)=N1 WJJMNDUMQPNECX-UHFFFAOYSA-N 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 6
- 208000030533 eye disease Diseases 0.000 claims description 6
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 6
- 239000000725 suspension Substances 0.000 claims description 6
- 239000003937 drug carrier Substances 0.000 claims description 5
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 4
- 206010006451 bronchitis Diseases 0.000 claims description 4
- 238000010438 heat treatment Methods 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims description 4
- 208000024891 symptom Diseases 0.000 claims description 4
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 4
- 201000009580 eosinophilic pneumonia Diseases 0.000 claims description 3
- 239000001384 succinic acid Substances 0.000 claims description 3
- 206010006474 Bronchopulmonary aspergillosis allergic Diseases 0.000 claims description 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 2
- 206010014561 Emphysema Diseases 0.000 claims description 2
- 206010061201 Helminthic infection Diseases 0.000 claims description 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 2
- 208000016300 Idiopathic chronic eosinophilic pneumonia Diseases 0.000 claims description 2
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 claims description 2
- 102000037984 Inhibitory immune checkpoint proteins Human genes 0.000 claims description 2
- 108091008026 Inhibitory immune checkpoint proteins Proteins 0.000 claims description 2
- 208000019693 Lung disease Diseases 0.000 claims description 2
- 206010049459 Lymphangioleiomyomatosis Diseases 0.000 claims description 2
- 206010029888 Obliterative bronchiolitis Diseases 0.000 claims description 2
- 206010067472 Organising pneumonia Diseases 0.000 claims description 2
- 206010035664 Pneumonia Diseases 0.000 claims description 2
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims description 2
- -1 Pyridine-2-yl Chemical group 0.000 claims description 2
- 206010038687 Respiratory distress Diseases 0.000 claims description 2
- 206010047115 Vasculitis Diseases 0.000 claims description 2
- 230000001154 acute effect Effects 0.000 claims description 2
- 206010069351 acute lung injury Diseases 0.000 claims description 2
- 208000006778 allergic bronchopulmonary aspergillosis Diseases 0.000 claims description 2
- 210000000621 bronchi Anatomy 0.000 claims description 2
- 201000009267 bronchiectasis Diseases 0.000 claims description 2
- 201000003848 bronchiolitis obliterans Diseases 0.000 claims description 2
- 208000023367 bronchiolitis obliterans with obstructive pulmonary disease Diseases 0.000 claims description 2
- 201000009805 cryptogenic organizing pneumonia Diseases 0.000 claims description 2
- 239000013078 crystal Substances 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 230000002538 fungal effect Effects 0.000 claims description 2
- 208000013397 idiopathic acute eosinophilic pneumonia Diseases 0.000 claims description 2
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 2
- 230000000414 obstructive effect Effects 0.000 claims description 2
- 235000006408 oxalic acid Nutrition 0.000 claims description 2
- 230000002685 pulmonary effect Effects 0.000 claims description 2
- 201000009732 pulmonary eosinophilia Diseases 0.000 claims description 2
- 201000000306 sarcoidosis Diseases 0.000 claims description 2
- 238000003756 stirring Methods 0.000 claims description 2
- PQLVXDKIJBQVDF-UHFFFAOYSA-N acetic acid;hydrate Chemical compound O.CC(O)=O PQLVXDKIJBQVDF-UHFFFAOYSA-N 0.000 claims 1
- 230000002327 eosinophilic effect Effects 0.000 claims 1
- 201000001155 extrinsic allergic alveolitis Diseases 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 208000022098 hypersensitivity pneumonitis Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- DKAGJZJALZXOOV-UHFFFAOYSA-N hydrate;hydrochloride Chemical compound O.Cl DKAGJZJALZXOOV-UHFFFAOYSA-N 0.000 description 1
- 230000009610 hypersensitivity Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762492571P | 2017-05-01 | 2017-05-01 | |
| US62/492,571 | 2017-05-01 | ||
| PCT/US2018/030144 WO2018204236A1 (en) | 2017-05-01 | 2018-04-30 | Crystalline forms of a jak inhibitor compound |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020518582A JP2020518582A (ja) | 2020-06-25 |
| JP2020518582A5 true JP2020518582A5 (enExample) | 2021-05-06 |
| JP7096268B2 JP7096268B2 (ja) | 2022-07-05 |
Family
ID=62165729
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019559304A Active JP7096268B2 (ja) | 2017-05-01 | 2018-04-30 | Ｊａｋ阻害剤化合物の結晶形態 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US10251874B2 (enExample) |
| EP (1) | EP3619208B1 (enExample) |
| JP (1) | JP7096268B2 (enExample) |
| KR (1) | KR20200003121A (enExample) |
| CN (1) | CN110603255B (enExample) |
| AU (1) | AU2018261591B2 (enExample) |
| CA (1) | CA3059790A1 (enExample) |
| MX (1) | MX389014B (enExample) |
| MY (1) | MY200348A (enExample) |
| PH (1) | PH12019502425A1 (enExample) |
| SG (1) | SG11201909376TA (enExample) |
| TW (1) | TWI808083B (enExample) |
| WO (1) | WO2018204236A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2016350816B2 (en) | 2015-11-03 | 2020-06-25 | Theravance Biopharma R&D Ip, Llc | JAK kinase inhibitor compounds for treatment of respiratory disease |
| EA037261B1 (ru) | 2017-03-09 | 2021-03-01 | ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи | Ингибиторы jak, содержащие 4-членный гетероциклический амид |
| AR111495A1 (es) | 2017-05-01 | 2019-07-17 | Theravance Biopharma R&D Ip Llc | Compuestos de imidazo-piperidina fusionada como inhibidores de jak |
| CA3059785A1 (en) | 2017-05-01 | 2018-11-08 | Theravance Biopharma R&D Ip, Llc | Methods of treatment using a jak inhibitor compound |
| ES2955717T3 (es) | 2018-09-04 | 2023-12-05 | Theravance Biopharma R&D Ip Llc | Amidas heterocíclicas de 5 a 7 elementos como inhibidores de JAK |
| CA3108848A1 (en) | 2018-09-04 | 2020-03-12 | Theravance Biopharma R&D Ip, Llc | Process for preparing jak inhibitors and intermediates thereof |
| SI3837258T1 (sl) | 2018-09-04 | 2024-09-30 | Theravance Biopharma R&D Ip, Llc | Dimetil amino azetidin amidi, ki se uporabljajo kot JAK zaviralci |
| EP3853229A1 (en) | 2018-10-29 | 2021-07-28 | Theravance Biopharma R&D IP, LLC | 2-azabicyclo hexane compound as jak inhibitor |
| TW202144343A (zh) * | 2020-03-02 | 2021-12-01 | 美商施萬生物製藥研發 Ip有限責任公司 | Jak抑制劑化合物之結晶水合物 |
| TW202304902A (zh) * | 2021-03-26 | 2023-02-01 | 美商施萬生物製藥研發 Ip有限責任公司 | Jak抑制劑化合物之二鹽酸鹽之結晶形式 |
| EP4359402A1 (en) | 2021-06-25 | 2024-05-01 | Theravance Biopharma R&D IP, LLC | Imidazolo indazole compounds as jak inhibitors |
| KR20230092805A (ko) * | 2021-12-17 | 2023-06-26 | 주식회사 대웅제약 | (2R, 3S)-2-(3-(4,5-디클로로-1H-벤조[d]이미다졸-1-일)프로필)피페리딘-3-올의 신규한 산부가염 및 결정형 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI262914B (en) | 1999-07-02 | 2006-10-01 | Agouron Pharma | Compounds and pharmaceutical compositions for inhibiting protein kinases |
| AU2004259012C1 (en) | 2003-07-23 | 2012-08-02 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
| US20050090529A1 (en) | 2003-07-31 | 2005-04-28 | Pfizer Inc | 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| US7884109B2 (en) | 2005-04-05 | 2011-02-08 | Wyeth Llc | Purine and imidazopyridine derivatives for immunosuppression |
| US8648069B2 (en) | 2007-06-08 | 2014-02-11 | Abbvie Inc. | 5-substituted indazoles as kinase inhibitors |
| JP2010111624A (ja) | 2008-11-06 | 2010-05-20 | Shionogi & Co Ltd | Ｔｔｋ阻害作用を有するインダゾール誘導体 |
| WO2010114971A1 (en) | 2009-04-03 | 2010-10-07 | Sepracor Inc. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| WO2011084486A1 (en) | 2009-12-21 | 2011-07-14 | Epitherix, Llc | 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
| US8575336B2 (en) | 2011-07-27 | 2013-11-05 | Pfizer Limited | Indazoles |
| ME02883B (me) | 2013-12-05 | 2018-04-20 | Pfizer | PIROLO[2,3-d]PIRIMIDINIL-, PIROLO[2,3-b]PIRAZINIL- I PIROLO[2,3-d] PIRIDINILAKRILAMIDI |
| CR20160525A (es) | 2014-05-14 | 2016-12-20 | Pfizer | Pirazolopiridinas y pirazolopirimidinas |
| WO2016026078A1 (en) | 2014-08-19 | 2016-02-25 | Changzhou Jiekai Pharmatech Co., Ltd. | Heterocyclic compounds as erk inhibitors |
| KR101663277B1 (ko) | 2015-03-30 | 2016-10-06 | 주식회사 녹십자 | TNIK, IKKε 및 TBK1 억제제로서의 피라졸계 유도체 및 이를 포함하는 약학적 조성물 |
| AU2016350816B2 (en) * | 2015-11-03 | 2020-06-25 | Theravance Biopharma R&D Ip, Llc | JAK kinase inhibitor compounds for treatment of respiratory disease |
| US10851097B2 (en) | 2015-11-03 | 2020-12-01 | Topivert Pharma Limited | 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors |
| PT3371185T (pt) | 2015-11-03 | 2020-12-28 | Topivert Pharma Ltd | Derivados de 4,5,6,7-tetrahidro-1h-imidazo[4,5-c]piridina e 1,4,5,6,7,8-hexahidroimidazo[4,5-d]azepina como inibidores de janus quinase |
-
2018
- 2018-04-30 KR KR1020197035428A patent/KR20200003121A/ko not_active Abandoned
- 2018-04-30 TW TW107114723A patent/TWI808083B/zh not_active IP Right Cessation
- 2018-04-30 US US15/966,452 patent/US10251874B2/en active Active
- 2018-04-30 WO PCT/US2018/030144 patent/WO2018204236A1/en not_active Ceased
- 2018-04-30 EP EP18724753.1A patent/EP3619208B1/en active Active
- 2018-04-30 CN CN201880029410.5A patent/CN110603255B/zh not_active Expired - Fee Related
- 2018-04-30 MY MYPI2019005859A patent/MY200348A/en unknown
- 2018-04-30 MX MX2019012945A patent/MX389014B/es unknown
- 2018-04-30 CA CA3059790A patent/CA3059790A1/en active Pending
- 2018-04-30 SG SG11201909376T patent/SG11201909376TA/en unknown
- 2018-04-30 JP JP2019559304A patent/JP7096268B2/ja active Active
- 2018-04-30 AU AU2018261591A patent/AU2018261591B2/en not_active Ceased
-
2019
- 2019-10-25 PH PH12019502425A patent/PH12019502425A1/en unknown