CN104487441B - 有用于治疗癌症和自身免疫性疾病的可逆的共价吡咯并嘧啶或吡唑并嘧啶 - Google Patents
有用于治疗癌症和自身免疫性疾病的可逆的共价吡咯并嘧啶或吡唑并嘧啶 Download PDFInfo
- Publication number
- CN104487441B CN104487441B CN201380031739.2A CN201380031739A CN104487441B CN 104487441 B CN104487441 B CN 104487441B CN 201380031739 A CN201380031739 A CN 201380031739A CN 104487441 B CN104487441 B CN 104487441B
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- Prior art keywords
- amino
- carbonyl
- pyrimidin
- pyrazolo
- methyl
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- 0 C**1CN(*C)CCC1 Chemical compound C**1CN(*C)CCC1 0.000 description 4
- WQOHEWKWIJOAHQ-UHFFFAOYSA-N Cc(c(F)c1)ccc1OC Chemical compound Cc(c(F)c1)ccc1OC WQOHEWKWIJOAHQ-UHFFFAOYSA-N 0.000 description 1
- HWXKECVQNNJJPE-CVUKOHAISA-N Nc1c(c(-c(cc2)ccc2Oc2cc(F)cc(F)c2)n[n]2C[C@@H](CCC3)N3C(/C(/C#N)=C\C3CC3)=O)c2ncn1 Chemical compound Nc1c(c(-c(cc2)ccc2Oc2cc(F)cc(F)c2)n[n]2C[C@@H](CCC3)N3C(/C(/C#N)=C\C3CC3)=O)c2ncn1 HWXKECVQNNJJPE-CVUKOHAISA-N 0.000 description 1
- IGMIXYFOMCNIBW-XLEPWJDSSA-N Nc1c(c(-c(ccc(Oc2ccccc2)c2)c2F)n[n]2C[C@@H](CCC3)N3C(/C(/C#N)=C\NC3CC3)=O)c2ncn1 Chemical compound Nc1c(c(-c(ccc(Oc2ccccc2)c2)c2F)n[n]2C[C@@H](CCC3)N3C(/C(/C#N)=C\NC3CC3)=O)c2ncn1 IGMIXYFOMCNIBW-XLEPWJDSSA-N 0.000 description 1
Classifications
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Reproductive Health (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Otolaryngology (AREA)
- Gastroenterology & Hepatology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261661203P | 2012-06-18 | 2012-06-18 | |
| US61/661,203 | 2012-06-18 | ||
| PCT/US2013/045266 WO2013191965A1 (en) | 2012-06-18 | 2013-06-11 | Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment cancer and autoimmune diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104487441A CN104487441A (zh) | 2015-04-01 |
| CN104487441B true CN104487441B (zh) | 2018-06-01 |
Family
ID=48692669
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380031739.2A Active CN104487441B (zh) | 2012-06-18 | 2013-06-11 | 有用于治疗癌症和自身免疫性疾病的可逆的共价吡咯并嘧啶或吡唑并嘧啶 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20160045503A1 (enExample) |
| EP (1) | EP2861599B1 (enExample) |
| JP (1) | JP6189945B2 (enExample) |
| KR (1) | KR102150432B1 (enExample) |
| CN (1) | CN104487441B (enExample) |
| AU (1) | AU2013277582B2 (enExample) |
| CA (1) | CA2874461C (enExample) |
| DK (1) | DK2861599T3 (enExample) |
| ES (1) | ES2776175T3 (enExample) |
| MX (1) | MX368112B (enExample) |
| WO (1) | WO2013191965A1 (enExample) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9376438B2 (en) | 2011-05-17 | 2016-06-28 | Principia Biopharma, Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
| PL2710005T3 (pl) | 2011-05-17 | 2017-07-31 | Principia Biopharma Inc. | Inhibitory kinazy tyrozynowej |
| AU2012283775A1 (en) | 2011-07-13 | 2014-01-23 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
| US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
| CA3218491A1 (en) | 2012-06-04 | 2013-12-12 | Pharmacyclics Llc | Crystalline forms of a bruton's tyrosine kinase inhibitor |
| WO2014036016A1 (en) * | 2012-08-31 | 2014-03-06 | Principia Biopharma Inc. | Benzimidazole derivatives as itk inhibitors |
| SMT201900344T1 (it) | 2012-09-10 | 2019-07-11 | Principia Biopharma Inc | Composti di pirazolopirimidina come inibitori di chinasi |
| JP2015537033A (ja) * | 2012-11-15 | 2015-12-24 | ファーマサイクリックス,インク. | キナーゼ阻害剤としてのピロロピリミジン化合物 |
| US8957080B2 (en) | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| US9624224B2 (en) | 2013-09-30 | 2017-04-18 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
| KR20220027271A (ko) | 2014-02-21 | 2022-03-07 | 프린시피아 바이오파마, 인코퍼레이티드 | Btk 억제제의 염 및 고체 형태 |
| WO2015136398A1 (en) | 2014-03-12 | 2015-09-17 | Novartis Ag | Combination comprising a btk inhibitor and an akt inhibitor |
| CN105017256A (zh) | 2014-04-29 | 2015-11-04 | 浙江导明医药科技有限公司 | 多氟化合物作为布鲁顿酪氨酸激酶抑制剂 |
| GB201410430D0 (en) | 2014-06-11 | 2014-07-23 | Redx Pharma Ltd | Compounds |
| WO2016019233A1 (en) | 2014-08-01 | 2016-02-04 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| MX2017001671A (es) | 2014-08-07 | 2017-07-04 | Pharmacyclics Llc | Formulaciones novedosas de un inhibidor de la tirosina cinasa de bruton. |
| US10196397B2 (en) | 2014-11-19 | 2019-02-05 | Sun Pharmaceutical Industries Limited | Process for the preparation of ibrutinib |
| CA2970723C (en) | 2014-12-18 | 2023-09-05 | Principia Biopharma Inc. | Treatment of pemphigus |
| HUE061809T2 (hu) * | 2014-12-24 | 2023-08-28 | Principia Biopharma Inc | Készítmények csípõbél-éhbél szakaszba történõ hatóanyag beadáshoz |
| IL252913B (en) * | 2014-12-24 | 2022-06-01 | Principia Biopharma Inc | Dose of site-specific btk inhibitor |
| IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of bruton's tyrosine kinase inhibitor |
| US9717745B2 (en) | 2015-03-19 | 2017-08-01 | Zhejiang DTRM Biopharma Co. Ltd. | Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases |
| CN106146508A (zh) * | 2015-03-19 | 2016-11-23 | 浙江导明医药科技有限公司 | 优化的联合用药及其治疗癌症和自身免疫疾病的用途 |
| CN106146511A (zh) * | 2015-04-03 | 2016-11-23 | 安润医药科技(苏州)有限公司 | 吡唑并嘧啶衍生物、制备方法、药物组合物及用途 |
| WO2016154998A1 (zh) * | 2015-04-03 | 2016-10-06 | 安润医药科技(苏州)有限公司 | 吡唑并嘧啶衍生物、制备方法、药物组合物及用途 |
| KR20240070721A (ko) * | 2015-06-03 | 2024-05-21 | 프린시피아 바이오파마, 인코퍼레이티드 | 티로신 키나제 억제제 |
| MA42242A (fr) * | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc | Inhibiteurs de la tyrosine kinase |
| EP3334430B1 (en) | 2015-08-13 | 2025-02-26 | San Diego State University Research Foundation | Atropisomerism for increased kinase inhibitor selectivity |
| HK1258779A1 (zh) | 2015-09-16 | 2019-11-22 | Loxo Oncology Inc. | 用於治療癌症的作為btk抑制劑的吡唑並嘧啶衍生物 |
| MA55064A (fr) | 2015-12-16 | 2021-09-29 | Loxo Oncology Inc | Composés utilisés comme inhibiteurs de kinase |
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| JP6189945B2 (ja) | 2017-08-30 |
| DK2861599T3 (da) | 2020-03-02 |
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| HK1209103A1 (en) | 2016-03-24 |
| CA2874461A1 (en) | 2013-12-27 |
| KR20150023752A (ko) | 2015-03-05 |
| MX2014015346A (es) | 2015-03-05 |
| MX368112B (es) | 2019-09-18 |
| AU2013277582B2 (en) | 2017-11-30 |
| EP2861599B1 (en) | 2019-12-18 |
| CA2874461C (en) | 2021-10-12 |
| JP2015519401A (ja) | 2015-07-09 |
| KR102150432B1 (ko) | 2020-09-01 |
| AU2013277582A1 (en) | 2015-01-22 |
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