CN101389622A - 用作pi-3激酶抑制剂的嘧啶衍生物 - Google Patents
用作pi-3激酶抑制剂的嘧啶衍生物 Download PDFInfo
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- CN101389622A CN101389622A CNA2007800063742A CN200780006374A CN101389622A CN 101389622 A CN101389622 A CN 101389622A CN A2007800063742 A CNA2007800063742 A CN A2007800063742A CN 200780006374 A CN200780006374 A CN 200780006374A CN 101389622 A CN101389622 A CN 101389622A
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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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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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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
- C07D401/14—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
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- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Description
化合物 | 60mg/kg | 100mg/kg |
91,于8hr | >50% | |
183,于8hr | 50-75% | |
103,于8hr | <50% | |
10,于10hr | >75% | >75% |
84,于10hr | 50-75% | |
76,于10hr | >75% | >75% |
66,于10hr | <50% |
Claims (54)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US76078906P | 2006-01-20 | 2006-01-20 | |
US60/760,789 | 2006-01-20 | ||
PCT/US2007/001708 WO2007084786A1 (en) | 2006-01-20 | 2007-01-22 | Pyrimidine derivatives used as pi-3 kinase inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101389622A true CN101389622A (zh) | 2009-03-18 |
CN101389622B CN101389622B (zh) | 2013-04-17 |
Family
ID=37951939
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2007800063742A Active CN101389622B (zh) | 2006-01-20 | 2007-01-22 | 用作pi-3激酶抑制剂的嘧啶衍生物 |
Country Status (41)
Country | Link |
---|---|
US (2) | US8217035B2 (zh) |
EP (2) | EP2261223B1 (zh) |
JP (1) | JP5161110B2 (zh) |
KR (1) | KR101353829B1 (zh) |
CN (1) | CN101389622B (zh) |
AR (2) | AR059087A1 (zh) |
AT (1) | ATE478064T1 (zh) |
AU (1) | AU2007206048B2 (zh) |
BR (1) | BRPI0707189B1 (zh) |
CA (1) | CA2636993C (zh) |
CR (1) | CR10163A (zh) |
CY (1) | CY1111091T1 (zh) |
DE (1) | DE602007008529D1 (zh) |
DK (2) | DK2261223T3 (zh) |
EA (1) | EA018083B1 (zh) |
EC (1) | ECSP088630A (zh) |
ES (2) | ES2427624T3 (zh) |
GE (1) | GEP20115147B (zh) |
GT (1) | GT200800143A (zh) |
HK (1) | HK1122031A1 (zh) |
HN (1) | HN2008001144A (zh) |
HR (2) | HRP20100603T1 (zh) |
IL (1) | IL192763A (zh) |
JO (1) | JO2660B1 (zh) |
MA (1) | MA30208B1 (zh) |
ME (2) | MEP3908A (zh) |
MY (1) | MY144233A (zh) |
NO (1) | NO342183B1 (zh) |
NZ (1) | NZ569771A (zh) |
PE (1) | PE20071322A1 (zh) |
PL (2) | PL1984350T3 (zh) |
PT (2) | PT1984350E (zh) |
RS (2) | RS51548B (zh) |
SI (2) | SI1984350T1 (zh) |
SM (1) | SMP200800048B (zh) |
SV (1) | SV2008002984A (zh) |
TN (1) | TNSN08305A1 (zh) |
TW (2) | TW201315723A (zh) |
UA (1) | UA96284C2 (zh) |
WO (1) | WO2007084786A1 (zh) |
ZA (1) | ZA200806017B (zh) |
Cited By (39)
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WO2011022928A1 (zh) * | 2009-08-27 | 2011-03-03 | 中国科学院上海药物研究所 | 喹啉类化合物、其制备方法、包含该化合物的药物组合物及该化合物的用途 |
CN102459272A (zh) * | 2009-05-27 | 2012-05-16 | 健泰科生物技术公司 | 对P110δ具有选择性的为PI3K抑制剂的二环嘧啶化合物和使用方法 |
CN102958518A (zh) * | 2009-05-15 | 2013-03-06 | 诺瓦提斯公司 | 磷脂酰肌醇3-激酶抑制剂和抗糖尿病化合物的组合 |
CN102952086A (zh) * | 2012-09-28 | 2013-03-06 | 天津科创医药中间体技术生产力促进有限公司 | 一种2-吗啉基取代嘧啶类化合物的制备方法 |
CN103140479A (zh) * | 2010-10-01 | 2013-06-05 | 诺华有限公司 | 制造嘧啶衍生物的方法 |
CN103313714A (zh) * | 2010-11-12 | 2013-09-18 | 得克萨斯州大学系统董事会 | 地塞米松组合治疗 |
CN103476765A (zh) * | 2011-02-11 | 2013-12-25 | 达娜-法勃肿瘤研究所公司 | 抑制错构瘤肿瘤细胞的方法 |
CN103483345A (zh) * | 2013-09-25 | 2014-01-01 | 中山大学 | Pi3k 激酶抑制剂、包含其的药物组合物及其应用 |
CN103764130A (zh) * | 2011-09-01 | 2014-04-30 | 诺华股份有限公司 | 用于治疗骨癌或者预防原发性癌细胞转移性播散入骨中的pi3k抑制剂 |
CN103889422A (zh) * | 2011-10-28 | 2014-06-25 | 诺华股份有限公司 | 治疗胃肠道间质瘤的方法 |
CN104144926A (zh) * | 2012-02-24 | 2014-11-12 | 诺华股份有限公司 | 噁唑烷-2-酮化合物及其作为磷脂酰肌醇-3-激酶抑制剂的用途 |
CN104151256A (zh) * | 2014-08-14 | 2014-11-19 | 西安交通大学 | 二取代苯甲酰胺类化合物及其合成方法和应用 |
CN104245693A (zh) * | 2012-12-14 | 2014-12-24 | 上海恒瑞医药有限公司 | 嘧啶类衍生物及其可药用盐、其制备方法及其在医药上的应用 |
CN104349779A (zh) * | 2012-05-16 | 2015-02-11 | 诺华股份有限公司 | Pi-3激酶抑制剂的剂量方案 |
CN104718204A (zh) * | 2012-11-12 | 2015-06-17 | 诺华股份有限公司 | 噁唑烷-2-酮-嘧啶衍生物 |
CN105001151A (zh) * | 2015-08-28 | 2015-10-28 | 苏州明锐医药科技有限公司 | 布帕尼西中间体及其制备方法 |
CN105050623A (zh) * | 2012-08-16 | 2015-11-11 | 诺华股份有限公司 | Pi3k抑制剂和c-met抑制剂的组合 |
CN105073099A (zh) * | 2013-03-06 | 2015-11-18 | 诺华股份有限公司 | 有机化合物的制剂 |
CN105228611A (zh) * | 2013-05-07 | 2016-01-06 | 诺华股份有限公司 | 用于治疗或预防头颈癌的pi3激酶抑制剂与紫杉醇的组合 |
CN105330699A (zh) * | 2014-08-13 | 2016-02-17 | 山东汇睿迪生物技术有限公司 | 一种含磷吡啶并[2,3-d]嘧啶-7-酮类化合物或其药学上可接受的盐、药物组合物及其应用 |
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