JP2017537954A5 - - Google Patents
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- Publication number
- JP2017537954A5 JP2017537954A5 JP2017532034A JP2017532034A JP2017537954A5 JP 2017537954 A5 JP2017537954 A5 JP 2017537954A5 JP 2017532034 A JP2017532034 A JP 2017532034A JP 2017532034 A JP2017532034 A JP 2017532034A JP 2017537954 A5 JP2017537954 A5 JP 2017537954A5
- Authority
- JP
- Japan
- Prior art keywords
- weight
- pharmaceutical composition
- disorder
- methylcyclohexylamino
- butylamino
- 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
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 40
- 150000003839 salts Chemical class 0.000 claims description 34
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 28
- 208000035475 disorder Diseases 0.000 claims description 25
- 239000008194 pharmaceutical composition Substances 0.000 claims description 23
- QBBRJRLJWXRSHQ-CKYFFXLPSA-N 2-(tert-butylamino)-4-[[(1r,3r,4r)-3-hydroxy-4-methylcyclohexyl]amino]pyrimidine-5-carboxamide Chemical compound C1[C@@H](O)[C@H](C)CC[C@H]1NC1=NC(NC(C)(C)C)=NC=C1C(N)=O QBBRJRLJWXRSHQ-CKYFFXLPSA-N 0.000 claims description 16
- 201000010099 disease Diseases 0.000 claims description 15
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 14
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 14
- 229930195725 Mannitol Natural products 0.000 claims description 14
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 14
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 14
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 14
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 14
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 14
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 14
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 14
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 14
- 235000019359 magnesium stearate Nutrition 0.000 claims description 14
- 239000000594 mannitol Substances 0.000 claims description 14
- 235000010355 mannitol Nutrition 0.000 claims description 14
- 239000002207 metabolite Substances 0.000 claims description 14
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 14
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 14
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 14
- 239000007787 solid Substances 0.000 claims description 14
- 239000012453 solvate Substances 0.000 claims description 14
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 10
- 206010039710 Scleroderma Diseases 0.000 claims description 8
- 150000004677 hydrates Chemical class 0.000 claims description 8
- 208000029523 Interstitial Lung disease Diseases 0.000 claims description 7
- 206010025135 lupus erythematosus Diseases 0.000 claims description 7
- 201000009594 Systemic Scleroderma Diseases 0.000 claims description 6
- 206010042953 Systemic sclerosis Diseases 0.000 claims description 6
- 208000001145 Metabolic Syndrome Diseases 0.000 claims description 5
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims description 5
- 206010012601 diabetes mellitus Diseases 0.000 claims description 5
- 230000037361 pathway Effects 0.000 claims description 5
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 4
- 230000001684 chronic effect Effects 0.000 claims description 4
- 208000017169 kidney disease Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 239000000203 mixture Substances 0.000 claims description 3
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 2
- ORZMSMCZBZARKY-UHFFFAOYSA-N 1,3,2$l^{6}-benzodioxathiole 2,2-dioxide Chemical compound C1=CC=C2OS(=O)(=O)OC2=C1 ORZMSMCZBZARKY-UHFFFAOYSA-N 0.000 claims description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 2
- JVTAAEKCZFNVCJ-REOHCLBHSA-N L-lactic acid Chemical compound C[C@H](O)C(O)=O JVTAAEKCZFNVCJ-REOHCLBHSA-N 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-L L-tartrate(2-) Chemical compound [O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O FEWJPZIEWOKRBE-JCYAYHJZSA-L 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical class OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 2
- 229940116871 l-lactate Drugs 0.000 claims description 2
- LRPCLTPZMUIPFK-UHFFFAOYSA-N methane;sulfuric acid Chemical compound C.OS(O)(=O)=O LRPCLTPZMUIPFK-UHFFFAOYSA-N 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 2
- 239000010452 phosphate Substances 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 229940086735 succinate Drugs 0.000 claims description 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000002054 transplantation Methods 0.000 claims 2
- 206010063209 Chronic allograft nephropathy Diseases 0.000 description 3
- 201000001200 Crouzon syndrome-acanthosis nigricans syndrome Diseases 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- 230000009885 systemic effect Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462092537P | 2014-12-16 | 2014-12-16 | |
| US62/092,537 | 2014-12-16 | ||
| US201562196044P | 2015-07-23 | 2015-07-23 | |
| US62/196,044 | 2015-07-23 | ||
| PCT/US2015/065774 WO2016100310A1 (en) | 2014-12-16 | 2015-12-15 | Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020089532A Division JP7022172B2 (ja) | 2014-12-16 | 2020-05-22 | ２－（ｔｅｒｔ－ブチルアミノ）－４－（（１Ｒ，３Ｒ，４Ｒ）－３－ヒドロキシ－４－メチルシクロヘキシルアミノ）－ピリミジン－５－カルボキサミドの製剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017537954A JP2017537954A (ja) | 2017-12-21 |
| JP2017537954A5 true JP2017537954A5 (enExample) | 2019-01-24 |
| JP6762940B2 JP6762940B2 (ja) | 2020-09-30 |
Family
ID=56110500
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017532034A Active JP6762940B2 (ja) | 2014-12-16 | 2015-12-15 | ２−（ｔｅｒｔ−ブチルアミノ）−４−（（１Ｒ，３Ｒ，４Ｒ）−３−ヒドロキシ−４−メチルシクロヘキシルアミノ）−ピリミジン−５−カルボキサミドの製剤 |
| JP2020089532A Active JP7022172B2 (ja) | 2014-12-16 | 2020-05-22 | ２－（ｔｅｒｔ－ブチルアミノ）－４－（（１Ｒ，３Ｒ，４Ｒ）－３－ヒドロキシ－４－メチルシクロヘキシルアミノ）－ピリミジン－５－カルボキサミドの製剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020089532A Active JP7022172B2 (ja) | 2014-12-16 | 2020-05-22 | ２－（ｔｅｒｔ－ブチルアミノ）－４－（（１Ｒ，３Ｒ，４Ｒ）－３－ヒドロキシ－４－メチルシクロヘキシルアミノ）－ピリミジン－５－カルボキサミドの製剤 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US9796685B2 (enExample) |
| EP (2) | EP3233809B1 (enExample) |
| JP (2) | JP6762940B2 (enExample) |
| KR (1) | KR102606253B1 (enExample) |
| CN (2) | CN107108524A (enExample) |
| AU (2) | AU2015362728B2 (enExample) |
| BR (1) | BR112017012795A2 (enExample) |
| CA (2) | CA3210612C (enExample) |
| CL (1) | CL2017001545A1 (enExample) |
| CO (1) | CO2017006087A2 (enExample) |
| EA (1) | EA033530B1 (enExample) |
| EC (1) | ECSP17038150A (enExample) |
| ES (2) | ES2972295T3 (enExample) |
| IL (1) | IL252900B (enExample) |
| MX (2) | MX382253B (enExample) |
| NZ (1) | NZ732793A (enExample) |
| SA (1) | SA517381749B1 (enExample) |
| SG (2) | SG11201704827UA (enExample) |
| WO (1) | WO2016100310A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20240097T1 (hr) | 2011-04-22 | 2024-03-29 | Signal Pharmaceuticals, Llc | Supstituirani diaminokarboksamid i diaminokarbonitril pirimidini, njihovi pripravci i postupci liječenja s njima |
| NZ715903A (en) | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
| WO2016100310A1 (en) | 2014-12-16 | 2016-06-23 | Signal Pharmaceuticals, Llc | Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide |
| EP3233808B1 (en) * | 2014-12-16 | 2021-07-14 | Signal Pharmaceuticals, LLC | Medical uses comprising methods for measurement of inhibition of c-jun n-terminal kinase in skin |
| CA2975260C (en) | 2015-01-29 | 2024-05-21 | Signal Pharmaceuticals Llc | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
| ES2994877T3 (en) | 2015-07-24 | 2025-02-03 | Celgene Corp | Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein |
| DK3358347T3 (da) * | 2015-09-30 | 2020-11-30 | Univ Tohoku | Markør til bestemmelse af diabetisk nefropati |
| AU2019280822A1 (en) | 2018-06-06 | 2021-01-07 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the S1P1 receptor |
| KR20200043618A (ko) * | 2018-10-18 | 2020-04-28 | 주식회사유한양행 | 아미노피리미딘 유도체 또는 이의 염을 포함하는 경구투여용 약학 조성물 |
| KR20210029989A (ko) | 2019-09-09 | 2021-03-17 | 김경민 | 야구경기 데이터 기록 서버 및 야구경기 기록데이터 분석방법 |
| CN112574123B (zh) * | 2019-09-30 | 2024-06-11 | 武汉朗来科技发展有限公司 | Jnk抑制剂、其药物组合物和用途 |
| TW202434251A (zh) | 2022-11-04 | 2024-09-01 | 美商必治妥美雅史谷比公司 | 治療癌症之療法 |
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| DE69933680T2 (de) | 1998-08-29 | 2007-08-23 | Astrazeneca Ab | Pyrimidine verbindungen |
| AU5107900A (en) | 1999-06-09 | 2000-12-28 | Yamanouchi Pharmaceutical Co., Ltd. | Novel heterocyclic carboxamide derivatives |
| AU5108000A (en) | 1999-06-10 | 2001-01-02 | Yamanouchi Pharmaceutical Co., Ltd. | Novel nitrogen-contaiing heterocyclic derivatives or salts thereof |
| HK1045507A1 (zh) * | 1999-08-12 | 2002-11-29 | Vertex Pharmaceuticals Incorporated | C-jun n-末端激酶(jnk)及其他蛋白质激酶的抑制物 |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| AU2003220968A1 (en) | 2002-03-28 | 2003-10-13 | Kyowa Hakko Kogyo Co., Ltd. | Anti-inflammatory agent |
| EP1518855B1 (en) | 2002-06-28 | 2011-10-26 | Astellas Pharma Inc. | Diaminopyrimidinecarboxa mide derivative |
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| HRP20240097T1 (hr) * | 2011-04-22 | 2024-03-29 | Signal Pharmaceuticals, Llc | Supstituirani diaminokarboksamid i diaminokarbonitril pirimidini, njihovi pripravci i postupci liječenja s njima |
| NZ715903A (en) | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
| WO2016100310A1 (en) * | 2014-12-16 | 2016-06-23 | Signal Pharmaceuticals, Llc | Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide |
| EP3233808B1 (en) | 2014-12-16 | 2021-07-14 | Signal Pharmaceuticals, LLC | Medical uses comprising methods for measurement of inhibition of c-jun n-terminal kinase in skin |
-
2015
- 2015-12-15 WO PCT/US2015/065774 patent/WO2016100310A1/en not_active Ceased
- 2015-12-15 CN CN201580068532.1A patent/CN107108524A/zh active Pending
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