CN106536522A - 用于治疗银屑病的杂环化合物 - Google Patents
用于治疗银屑病的杂环化合物 Download PDFInfo
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- CN106536522A CN106536522A CN201580000843.4A CN201580000843A CN106536522A CN 106536522 A CN106536522 A CN 106536522A CN 201580000843 A CN201580000843 A CN 201580000843A CN 106536522 A CN106536522 A CN 106536522A
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- Prior art keywords
- bases
- pyrazine
- alkyl
- amino
- chlorphenyls
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- FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 description 1
- 235000012141 vanillin Nutrition 0.000 description 1
- 230000004862 vasculogenesis Effects 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
化合物 | HaCaT细胞IC50(μg/ml) |
5号化合物 | 544 |
顺铂 | 1.41 |
化合物编号 | 测试结果 |
2 | 阳性 |
3 | 阳性 |
5 | 阳性 |
6 | 阳性 |
7 | 阳性 |
8 | 阳性 |
9 | 阳性 |
10 | 阳性 |
11 | 阳性 |
12 | 阳性 |
13 | 阳性 |
16 | 阳性 |
17 | 阳性 |
19 | 阳性 |
20 | 阳性 |
Claims (21)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/CN2015/080718 WO2016192064A1 (en) | 2015-06-03 | 2015-06-03 | Heterocyclic compounds for treating psoriasis |
Publications (2)
Publication Number | Publication Date |
---|---|
CN106536522A true CN106536522A (zh) | 2017-03-22 |
CN106536522B CN106536522B (zh) | 2020-08-28 |
Family
ID=57439977
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201580000843.4A Active CN106536522B (zh) | 2015-06-03 | 2015-06-03 | 用于治疗银屑病的杂环化合物 |
Country Status (6)
Country | Link |
---|---|
US (1) | US10238657B2 (zh) |
EP (1) | EP3303335B1 (zh) |
CN (1) | CN106536522B (zh) |
AU (1) | AU2015396809B2 (zh) |
CA (1) | CA2987963C (zh) |
WO (1) | WO2016192064A1 (zh) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
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TN2018000119A1 (en) | 2015-11-09 | 2019-10-04 | Astrazeneca Ab | Dihydroimidazopyrazinone derivatives useful in the treatment of cancer |
CN112574207B (zh) * | 2019-09-30 | 2023-04-11 | 南京药石科技股份有限公司 | Erk1/2蛋白激酶抑制剂及其用途 |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
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CN1976919A (zh) * | 2004-05-14 | 2007-06-06 | 沃泰克斯药物股份有限公司 | 作为erk蛋白激酶抑制剂的吡咯化合物、它们的合成和中间体 |
CN101326188A (zh) * | 2005-10-14 | 2008-12-17 | 西克拉塞尔有限公司 | 嘧啶-4-基-3,4-二氢-2h-吡咯并[1,2a]吡嗪-1-酮化合物 |
WO2013050448A1 (en) * | 2011-10-07 | 2013-04-11 | Nerviano Medical Sciences S.R.L. | 4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS |
WO2013130660A1 (en) * | 2012-02-28 | 2013-09-06 | Amgen Inc. | Amides as pim inhibitors |
WO2014149164A1 (en) * | 2013-03-15 | 2014-09-25 | Celgene Avilomics Research, Inc. | Mk2 inhibitors and uses thereof |
CN104507926A (zh) * | 2012-03-01 | 2015-04-08 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2016026078A1 (en) * | 2014-08-19 | 2016-02-25 | Changzhou Jiekai Pharmatech Co., Ltd. | Heterocyclic compounds as erk inhibitors |
WO2016162325A1 (en) * | 2015-04-07 | 2016-10-13 | Astrazeneca Ab | Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1 (2h)-one derivatives as kinase inhibitors |
-
2015
- 2015-06-03 WO PCT/CN2015/080718 patent/WO2016192064A1/en active Application Filing
- 2015-06-03 US US15/578,934 patent/US10238657B2/en active Active
- 2015-06-03 CA CA2987963A patent/CA2987963C/en active Active
- 2015-06-03 AU AU2015396809A patent/AU2015396809B2/en active Active
- 2015-06-03 EP EP15893720.1A patent/EP3303335B1/en active Active
- 2015-06-03 CN CN201580000843.4A patent/CN106536522B/zh active Active
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1976919A (zh) * | 2004-05-14 | 2007-06-06 | 沃泰克斯药物股份有限公司 | 作为erk蛋白激酶抑制剂的吡咯化合物、它们的合成和中间体 |
CN101326188A (zh) * | 2005-10-14 | 2008-12-17 | 西克拉塞尔有限公司 | 嘧啶-4-基-3,4-二氢-2h-吡咯并[1,2a]吡嗪-1-酮化合物 |
WO2013050448A1 (en) * | 2011-10-07 | 2013-04-11 | Nerviano Medical Sciences S.R.L. | 4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS |
WO2013130660A1 (en) * | 2012-02-28 | 2013-09-06 | Amgen Inc. | Amides as pim inhibitors |
CN104507926A (zh) * | 2012-03-01 | 2015-04-08 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
WO2014149164A1 (en) * | 2013-03-15 | 2014-09-25 | Celgene Avilomics Research, Inc. | Mk2 inhibitors and uses thereof |
Also Published As
Publication number | Publication date |
---|---|
EP3303335B1 (en) | 2021-07-28 |
WO2016192064A1 (en) | 2016-12-08 |
EP3303335A1 (en) | 2018-04-11 |
CA2987963C (en) | 2023-01-24 |
CN106536522B (zh) | 2020-08-28 |
US20180169096A1 (en) | 2018-06-21 |
US10238657B2 (en) | 2019-03-26 |
AU2015396809B2 (en) | 2019-07-11 |
EP3303335A4 (en) | 2019-02-27 |
AU2015396809A1 (en) | 2018-01-18 |
CA2987963A1 (en) | 2016-12-08 |
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