CN104177338B - 一类布鲁顿激酶抑制剂 - Google Patents
一类布鲁顿激酶抑制剂 Download PDFInfo
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- CN104177338B CN104177338B CN201310192167.8A CN201310192167A CN104177338B CN 104177338 B CN104177338 B CN 104177338B CN 201310192167 A CN201310192167 A CN 201310192167A CN 104177338 B CN104177338 B CN 104177338B
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- UGJYTOMOCDGLRS-UHFFFAOYSA-N tert-butyl 4-(6-aminopyridin-3-yl)piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1C1=CC=C(N)N=C1 UGJYTOMOCDGLRS-UHFFFAOYSA-N 0.000 description 1
- CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 description 1
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- RBNBDIMXFJYDLQ-UHFFFAOYSA-N thieno[3,2-d]pyrimidine Chemical compound C1=NC=C2SC=CC2=N1 RBNBDIMXFJYDLQ-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- 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
- C07D401/14—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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
RN486 | 化合物1 | 化合物2 |
66.3nM | 18.73nM | 19.97nM |
RN486 | 化合物1 | 化合物2 |
37.6nM | 8.4nM | 23.0nM |
对照组 | RN486 | 化合物1 |
0.268 | 0.015 | 0.001 |
Score | 表现 |
0 | 正常 |
1 | 踝关节或腕关节有轻微的红斑、肿胀,或仅个别指头明显表现红肿 |
2 | 踝关节或腕关节有中度的红斑、肿胀 |
3 | 整个足掌,包括指头,有严重红斑、肿胀 |
4 | 肢体有非常严重的炎症表现,并累及多个关节 |
Claims (4)
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CN201310192167.8A CN104177338B (zh) | 2013-05-22 | 2013-05-22 | 一类布鲁顿激酶抑制剂 |
PCT/CN2014/077570 WO2014187262A1 (zh) | 2013-05-22 | 2014-05-15 | 一类布鲁顿激酶抑制剂 |
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CN201310192167.8A CN104177338B (zh) | 2013-05-22 | 2013-05-22 | 一类布鲁顿激酶抑制剂 |
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CN104177338A CN104177338A (zh) | 2014-12-03 |
CN104177338B true CN104177338B (zh) | 2018-04-03 |
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WO (1) | WO2014187262A1 (zh) |
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CN105837576B (zh) | 2015-01-14 | 2019-03-26 | 湖北生物医药产业技术研究院有限公司 | Btk抑制剂 |
MA46995A (fr) | 2016-12-03 | 2019-10-09 | Acerta Pharma Bv | Méthodes et compositions pour l'utilisation de lymphocytes t thérapeutiques en association avec des inhibiteurs de kinase |
CN108658976B (zh) * | 2017-03-31 | 2021-02-19 | 南京科技职业学院 | 一类新型吡唑并[4,3-c]吡啶-4(5)-酮布鲁顿激酶抑制剂 |
EP3886854A4 (en) | 2018-11-30 | 2022-07-06 | Nuvation Bio Inc. | PYRROLE AND PYRAZOLE COMPOUNDS AND METHODS OF USE THERE |
CN110283171A (zh) * | 2019-07-17 | 2019-09-27 | 鼎泰(南京)临床医学研究有限公司 | 一类含有吡啶并嘧啶-4-胺类结构的化合物、药物组合物以及其应用 |
WO2022140246A1 (en) | 2020-12-21 | 2022-06-30 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
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PE20080839A1 (es) * | 2006-09-11 | 2008-08-23 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas |
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CN102341383A (zh) * | 2009-03-02 | 2012-02-01 | 霍夫曼-拉罗奇有限公司 | 布鲁顿酪氨酸激酶的抑制剂 |
WO2012020008A1 (en) * | 2010-08-12 | 2012-02-16 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
WO2013024078A1 (en) * | 2011-08-17 | 2013-02-21 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
WO2013067264A1 (en) * | 2011-11-03 | 2013-05-10 | Genentech, Inc. | 8-fluorophthalazin-1 (2h) - one compounds as inhibitors of btk activity |
CN104619696A (zh) * | 2012-09-13 | 2015-05-13 | 弗·哈夫曼-拉罗切有限公司 | 布鲁顿氏酪氨酸激酶抑制剂 |
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