CN102727498B - 使用吡啶并嘧啶酮PI3Kα抑制剂的治疗方法 - Google Patents
使用吡啶并嘧啶酮PI3Kα抑制剂的治疗方法 Download PDFInfo
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- CN102727498B CN102727498B CN201210032620.4A CN201210032620A CN102727498B CN 102727498 B CN102727498 B CN 102727498B CN 201210032620 A CN201210032620 A CN 201210032620A CN 102727498 B CN102727498 B CN 102727498B
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- 0 *C(c1c(N2*)nc(*)nc1*)=C(*)C2=O Chemical compound *C(c1c(N2*)nc(*)nc1*)=C(*)C2=O 0.000 description 1
- QZRNDZGOBUBXSS-UHFFFAOYSA-N CC(C)N(C(C=C1)=O)c2c1c(C)nc(S(C)(=O)=O)n2 Chemical compound CC(C)N(C(C=C1)=O)c2c1c(C)nc(S(C)(=O)=O)n2 QZRNDZGOBUBXSS-UHFFFAOYSA-N 0.000 description 1
- SLWMENIGFIJCMA-UHFFFAOYSA-N CC(C)N(C(C=C1)=O)c2c1c(C)nc(SC)n2 Chemical compound CC(C)N(C(C=C1)=O)c2c1c(C)nc(SC)n2 SLWMENIGFIJCMA-UHFFFAOYSA-N 0.000 description 1
- HXTWEUUYONZWNC-UHFFFAOYSA-N CCN(c1c(C=C2C#N)c(C)nc(N)n1)C2=O Chemical compound CCN(c1c(C=C2C#N)c(C)nc(N)n1)C2=O HXTWEUUYONZWNC-UHFFFAOYSA-N 0.000 description 1
- WHOQYWDDWMTSEV-UHFFFAOYSA-N CCN(c1c(C=C2C#N)c(C)nc(SC)n1)C2=O Chemical compound CCN(c1c(C=C2C#N)c(C)nc(SC)n1)C2=O WHOQYWDDWMTSEV-UHFFFAOYSA-N 0.000 description 1
- OEIYXFCEHMXIQJ-UHFFFAOYSA-N CCNc1c(C(OCC)=O)c(C)nc(SC)n1 Chemical compound CCNc1c(C(OCC)=O)c(C)nc(SC)n1 OEIYXFCEHMXIQJ-UHFFFAOYSA-N 0.000 description 1
- OQUIWJMZWPZRRR-UHFFFAOYSA-N CCNc1c(CO)c(C)nc(SC)n1 Chemical compound CCNc1c(CO)c(C)nc(SC)n1 OQUIWJMZWPZRRR-UHFFFAOYSA-N 0.000 description 1
- MAPPVNNJRAFIGP-UHFFFAOYSA-N CCNc1nc(C)cc(NC2CCCCC2)n1 Chemical compound CCNc1nc(C)cc(NC2CCCCC2)n1 MAPPVNNJRAFIGP-UHFFFAOYSA-N 0.000 description 1
- MHBOFFGOGSNRKL-UHFFFAOYSA-N CCNc1nc(N)nc(C)c1 Chemical compound CCNc1nc(N)nc(C)c1 MHBOFFGOGSNRKL-UHFFFAOYSA-N 0.000 description 1
- BZFQFVMNIIONKA-UHFFFAOYSA-N CCNc1nc(NC(C(Br)=C2)=O)c2c(C)n1 Chemical compound CCNc1nc(NC(C(Br)=C2)=O)c2c(C)n1 BZFQFVMNIIONKA-UHFFFAOYSA-N 0.000 description 1
- NPTGVVKPLWFPPX-UHFFFAOYSA-N Cc1cc(Cl)nc(N)n1 Chemical compound Cc1cc(Cl)nc(N)n1 NPTGVVKPLWFPPX-UHFFFAOYSA-N 0.000 description 1
- FCZIYFITALPIDD-UHFFFAOYSA-N Cc1cc(NC2CCCCC2)nc(Cl)n1 Chemical compound Cc1cc(NC2CCCCC2)nc(Cl)n1 FCZIYFITALPIDD-UHFFFAOYSA-N 0.000 description 1
- ALMBOXQFPLQVLF-UHFFFAOYSA-N Cc1nc(SC)nc(Cl)c1 Chemical compound Cc1nc(SC)nc(Cl)c1 ALMBOXQFPLQVLF-UHFFFAOYSA-N 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/28—Compounds containing heavy metals
- A61K31/282—Platinum compounds
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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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- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92289907P | 2007-04-10 | 2007-04-10 | |
| US60/922899 | 2007-04-10 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200880018725A Division CN101715345A (zh) | 2007-04-10 | 2008-04-09 | 使用吡啶并嘧啶酮PI3Kα抑制剂的治疗方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102727498A CN102727498A (zh) | 2012-10-17 |
| CN102727498B true CN102727498B (zh) | 2016-08-03 |
Family
ID=39627802
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200880018725A Pending CN101715345A (zh) | 2007-04-10 | 2008-04-09 | 使用吡啶并嘧啶酮PI3Kα抑制剂的治疗方法 |
| CN201210032620.4A Expired - Fee Related CN102727498B (zh) | 2007-04-10 | 2008-04-09 | 使用吡啶并嘧啶酮PI3Kα抑制剂的治疗方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200880018725A Pending CN101715345A (zh) | 2007-04-10 | 2008-04-09 | 使用吡啶并嘧啶酮PI3Kα抑制剂的治疗方法 |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US8513266B2 (enExample) |
| EP (1) | EP2139484B9 (enExample) |
| JP (3) | JP2010523670A (enExample) |
| KR (1) | KR101626435B1 (enExample) |
| CN (2) | CN101715345A (enExample) |
| AU (1) | AU2008236562B2 (enExample) |
| BR (1) | BRPI0810206A2 (enExample) |
| CA (1) | CA2683641C (enExample) |
| CO (1) | CO6251254A2 (enExample) |
| CR (1) | CR11100A (enExample) |
| DK (1) | DK2139484T3 (enExample) |
| DO (1) | DOP2009000243A (enExample) |
| EA (1) | EA020022B1 (enExample) |
| EC (1) | ECSP099724A (enExample) |
| ES (1) | ES2430614T3 (enExample) |
| HN (1) | HN2009003002A (enExample) |
| HR (1) | HRP20130688T1 (enExample) |
| IL (1) | IL201284A (enExample) |
| MA (1) | MA31358B1 (enExample) |
| ME (1) | ME00936B (enExample) |
| MX (1) | MX2009010930A (enExample) |
| MY (1) | MY150697A (enExample) |
| NZ (1) | NZ580110A (enExample) |
| PL (1) | PL2139484T3 (enExample) |
| PT (1) | PT2139484E (enExample) |
| RS (1) | RS52939B (enExample) |
| SI (1) | SI2139484T1 (enExample) |
| TN (1) | TN2009000400A1 (enExample) |
| UA (1) | UA100979C2 (enExample) |
| WO (1) | WO2008124161A1 (enExample) |
| ZA (1) | ZA200906764B (enExample) |
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| TW200726767A (en) * | 2005-07-04 | 2007-07-16 | Astrazeneca Ab | Chemical compounds 2 |
| JP5461012B2 (ja) * | 2005-10-07 | 2014-04-02 | エクセリクシス， インク． | ＰＩ３Ｋαのピリドピリミジノン型阻害剤 |
| CN101282948A (zh) * | 2005-10-07 | 2008-10-08 | 埃克塞里艾克西斯公司 | N-(3-氨基-喹喔啉-2-基)-磺酰胺衍生物及其作为磷脂酰肌醇3-激酶抑制剂的用途 |
| WO2008021389A2 (en) | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| US8188113B2 (en) * | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| SA08280783B1 (ar) * | 2007-01-11 | 2011-04-24 | استرازينيكا ايه بي | مشتقات بيريدوبيريميدين كمثبطات pde4 |
| DK2139484T3 (da) | 2007-04-10 | 2013-10-21 | Exelixis Inc | Fremgangsmåder til behandling af cancer ved brug af pyridopyrimidinon-inhibitorer af PI3K-alfa |
| NZ580009A (en) * | 2007-04-11 | 2012-06-29 | Exelixis Inc | Combination therapies comprising quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer |
| US8470834B2 (en) | 2008-08-20 | 2013-06-25 | Merck Sharp & Dohme Corp. | AZO-substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
| JP5674661B2 (ja) | 2008-08-20 | 2015-02-25 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | エチニル置換ピリジンおよびピリミジン誘導体ならびにそれらのウイルス感染の治療における使用 |
| AR072939A1 (es) | 2008-08-20 | 2010-09-29 | Schering Corp | Derivados de piridina y pirimidina sustituidas con etenilo y su uso en el tratamiento de infecciones virales |
| AU2009282567B2 (en) | 2008-08-20 | 2014-10-02 | Merck Sharp & Dohme Corp. | Substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
| AR080151A1 (es) | 2010-02-09 | 2012-03-14 | Exelixis Inc | Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia |
| US20130156768A1 (en) * | 2010-08-26 | 2013-06-20 | Bristol-Myers Squibb Company | Combination of anti-ctla4 antibody with braf inhibitors for the synergistic treatment of proliferative diseases |
| TWI642670B (zh) | 2010-09-14 | 2018-12-01 | 伊塞利克斯公司 | Ｐｉ３ｋ-德爾塔抑制劑以及其應用和生產方法 |
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| TW201306842A (zh) * | 2011-06-15 | 2013-02-16 | Exelixis Inc | 使用ｐｉ３ｋ／ｍｔｏｒ吡啶並嘧啶酮抑制劑及苯達莫司汀及／或利妥昔單抗治療惡性血液疾病之組合療法 |
| RU2014107713A (ru) * | 2011-07-28 | 2015-09-10 | Дженентек, Инк | Модель рака молочной железы у животных, кроме человека, с активируемым pik3ca h1047r |
| WO2013056067A1 (en) * | 2011-10-13 | 2013-04-18 | Exelixis, Inc. | Compounds for use in the treatment of basal cell carcinoma |
| CN104302294A (zh) | 2011-11-01 | 2015-01-21 | 埃克塞利希斯股份有限公司 | 用于治疗淋巴组织增生性恶性肿瘤的作为磷脂酰肌醇3-激酶抑制剂的n-(3-{[(3-{[2-氯-5-(甲氧基)苯基]氨基}喹喔啉-2-基)氨基]磺酰基}苯基)-2-甲基丙氨酰胺 |
| US9682141B2 (en) | 2011-11-11 | 2017-06-20 | Intellikine Llc | Combination of kinase inhibitors and uses thereof |
| CA2860051A1 (en) * | 2011-12-27 | 2013-07-04 | Kadmon Corporation, Llc | Methods for treatment of breast cancer nonresponsive to trastuzumab |
| US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| EP2872161B1 (en) | 2012-06-26 | 2020-12-16 | Del Mar Pharmaceuticals | Dianhydrogalactitol for use in treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations |
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| SI2882440T1 (sl) | 2012-08-07 | 2019-05-31 | Novartis Ag | Farmacevtske kombinacije, ki vsebujejo inhibitor B-RAF, inhibitor EGFR in neobvezno inhibitor PI3K-alfa |
| AU2014251038A1 (en) | 2013-04-08 | 2015-11-26 | Dennis M. Brown | Therapeutic benefit of suboptimally administered chemical compounds |
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| JP7677646B2 (ja) * | 2019-12-10 | 2025-05-15 | ザ・トラスティーズ・オブ・インディアナ・ユニバーシティー | 複製タンパク質ａ（ｒｐａ）－ｄｎａ相互作用阻害剤 |
| CN115243681B (zh) | 2019-12-30 | 2024-08-16 | 德西费拉制药有限责任公司 | 1-(4-溴-5-(1-乙基-7-(甲氨基)-2-侧氧基-1,2-二氢-1,6-萘啶-3-基)-2-氟苯基)-3-苯基脲的组合物 |
| FI4084778T3 (fi) | 2019-12-30 | 2023-12-18 | Deciphera Pharmaceuticals Llc | Amorfisia kinaasi-inhibiittoriformulaatioita ja menetelmiä niiden käyttämiseksi |
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| CN101282948A (zh) * | 2005-10-07 | 2008-10-08 | 埃克塞里艾克西斯公司 | N-(3-氨基-喹喔啉-2-基)-磺酰胺衍生物及其作为磷脂酰肌醇3-激酶抑制剂的用途 |
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| WO2008021389A2 (en) | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| ATE514695T1 (de) * | 2006-09-15 | 2011-07-15 | Pfizer Prod Inc | Pyrido(2,3-d)pyrimidinonverbindungen und ihre verwendung als pi3-inhibitoren |
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| JP2010523681A (ja) | 2007-04-11 | 2010-07-15 | エクセリクシス， インク． | 癌の治療のためのＰＩ３Ｋ−αの阻害剤としてのピリド［２，３−Ｄ］ピリミジン−７−オン化合物 |
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| EP2350070A1 (en) * | 2008-09-30 | 2011-08-03 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of pi3k and mtor |
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