JP5596026B2 - チオフェン又はチアゾール誘導体及びpi3k阻害剤としてのそれらの使用 - Google Patents
チオフェン又はチアゾール誘導体及びpi3k阻害剤としてのそれらの使用 Download PDFInfo
- Publication number
- JP5596026B2 JP5596026B2 JP2011514600A JP2011514600A JP5596026B2 JP 5596026 B2 JP5596026 B2 JP 5596026B2 JP 2011514600 A JP2011514600 A JP 2011514600A JP 2011514600 A JP2011514600 A JP 2011514600A JP 5596026 B2 JP5596026 B2 JP 5596026B2
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- Japan
- Prior art keywords
- membered
- optionally substituted
- nitrogen
- sulfur
- oxygen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 0 C*CC(CO)Nc1c(C)c(*)c(C2=N***2)[s]1 Chemical compound C*CC(CO)Nc1c(C)c(*)c(C2=N***2)[s]1 0.000 description 23
- DZRKPIICYODVAO-UHFFFAOYSA-N CCOC(c([s]c(SC)c1C#N)c1I)=O Chemical compound CCOC(c([s]c(SC)c1C#N)c1I)=O DZRKPIICYODVAO-UHFFFAOYSA-N 0.000 description 1
- SYDDCXMMTMOPIS-UHFFFAOYSA-N CCS(C)c([s]c(C(N)=O)c1I)c1C#N Chemical compound CCS(C)c([s]c(C(N)=O)c1I)c1C#N SYDDCXMMTMOPIS-UHFFFAOYSA-N 0.000 description 1
- RLLYIKSEIMDBCR-UHFFFAOYSA-N CSc([s]c(C(N)=O)c1I)c1C#N Chemical compound CSc([s]c(C(N)=O)c1I)c1C#N RLLYIKSEIMDBCR-UHFFFAOYSA-N 0.000 description 1
- XQJYHEHIXVFDIS-UHFFFAOYSA-N Cc1ccc(C[Cl]=O)c(Cl)c1 Chemical compound Cc1ccc(C[Cl]=O)c(Cl)c1 XQJYHEHIXVFDIS-UHFFFAOYSA-N 0.000 description 1
- QGKBWMKHMCWYHW-UHFFFAOYSA-N N#CC(C(c(c(Cl)c1)ccc1Cl)=O)C(N1CCC2=CC2CC1)=S Chemical compound N#CC(C(c(c(Cl)c1)ccc1Cl)=O)C(N1CCC2=CC2CC1)=S QGKBWMKHMCWYHW-UHFFFAOYSA-N 0.000 description 1
- AUZPMUJGZZSMCP-UHFFFAOYSA-N N#CCC(N1CCOCC1)=O Chemical compound N#CCC(N1CCOCC1)=O AUZPMUJGZZSMCP-UHFFFAOYSA-N 0.000 description 1
- VLMZXRFDZPDWQU-UHFFFAOYSA-N N#CCC(N1CCOCC1)=S Chemical compound N#CCC(N1CCOCC1)=S VLMZXRFDZPDWQU-UHFFFAOYSA-N 0.000 description 1
- VXTYIKXKNTWGFZ-UHFFFAOYSA-N N#Cc1c(N2CCOCC2)[s]c(-c2cnc[nH]2)c1-c(ccc(Cl)c1)c1Cl Chemical compound N#Cc1c(N2CCOCC2)[s]c(-c2cnc[nH]2)c1-c(ccc(Cl)c1)c1Cl VXTYIKXKNTWGFZ-UHFFFAOYSA-N 0.000 description 1
- MXDXVJFDWBKXLK-UHFFFAOYSA-N NC(c([s]c(N1CC(CO)CCC1)c1N)c1-c(ccc(C=[IH])c1)c1Cl)=O Chemical compound NC(c([s]c(N1CC(CO)CCC1)c1N)c1-c(ccc(C=[IH])c1)c1Cl)=O MXDXVJFDWBKXLK-UHFFFAOYSA-N 0.000 description 1
- UTYCGBVJQHLJOX-UHFFFAOYSA-N Nc1c(N2CC(CO)CCC2)[s]c(-c2nnc[nH]2)c1-c(ccc(Cl)c1)c1Cl Chemical compound Nc1c(N2CC(CO)CCC2)[s]c(-c2nnc[nH]2)c1-c(ccc(Cl)c1)c1Cl UTYCGBVJQHLJOX-UHFFFAOYSA-N 0.000 description 1
- QNEGDGPAXKYZHZ-UHFFFAOYSA-N OB(c(c(Cl)c1)ccc1Cl)O Chemical compound OB(c(c(Cl)c1)ccc1Cl)O QNEGDGPAXKYZHZ-UHFFFAOYSA-N 0.000 description 1
- VLAZLCVSFAYIIL-UHFFFAOYSA-N OCC1OCCNC1 Chemical compound OCC1OCCNC1 VLAZLCVSFAYIIL-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13248408P | 2008-06-19 | 2008-06-19 | |
| US61/132,484 | 2008-06-19 | ||
| PCT/US2009/003607 WO2009154741A1 (en) | 2008-06-19 | 2009-06-17 | Thiophene or thiazole derivatives and their use as pi3k inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011524904A JP2011524904A (ja) | 2011-09-08 |
| JP2011524904A5 JP2011524904A5 (enExample) | 2012-10-18 |
| JP5596026B2 true JP5596026B2 (ja) | 2014-09-24 |
Family
ID=41010579
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011514600A Active JP5596026B2 (ja) | 2008-06-19 | 2009-06-17 | チオフェン又はチアゾール誘導体及びpi3k阻害剤としてのそれらの使用 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US8183240B2 (enExample) |
| EP (1) | EP2313399B1 (enExample) |
| JP (1) | JP5596026B2 (enExample) |
| KR (1) | KR20110018451A (enExample) |
| CN (1) | CN102066365A (enExample) |
| AU (1) | AU2009260782B2 (enExample) |
| BR (1) | BRPI0914223A2 (enExample) |
| CA (1) | CA2727069A1 (enExample) |
| CL (1) | CL2010001474A1 (enExample) |
| CO (1) | CO6331431A2 (enExample) |
| CR (1) | CR20110032A (enExample) |
| EA (1) | EA201170052A1 (enExample) |
| ES (1) | ES2491522T3 (enExample) |
| GE (1) | GEP20125650B (enExample) |
| IL (1) | IL210055A0 (enExample) |
| MA (1) | MA32468B1 (enExample) |
| MX (1) | MX2010014125A (enExample) |
| NZ (1) | NZ589844A (enExample) |
| UA (1) | UA106206C2 (enExample) |
| WO (1) | WO2009154741A1 (enExample) |
| ZA (1) | ZA201008875B (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9029411B2 (en) | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| KR20110018451A (ko) * | 2008-06-19 | 2011-02-23 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 티오펜 또는 티아졸 유도체, 그리고 pi3k 저해물질로서 이들의 용도 |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| EP2391619A1 (en) * | 2009-01-30 | 2011-12-07 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| US9062038B2 (en) | 2010-08-11 | 2015-06-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| SG10201506238SA (en) | 2010-08-11 | 2015-09-29 | Millennium Pharm Inc | Heteroaryls And Uses Thereof |
| US8859768B2 (en) | 2010-08-11 | 2014-10-14 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| JP5726635B2 (ja) | 2010-08-25 | 2015-06-03 | 株式会社Nttドコモ | マルチモードフロントエンド回路 |
| PE20141044A1 (es) | 2010-10-13 | 2014-09-07 | Millennium Pharm Inc | Heteroarilos y sus usos |
| CN102503930B (zh) * | 2011-10-28 | 2014-07-02 | 浙江大学 | 3,4,5,-三取代氨基噻吩类化合物及其制备和用途 |
| PL2790705T3 (pl) | 2011-12-15 | 2018-06-29 | Novartis Ag | Zastosowanie inhibitorów czynności lub funkcji PI3K |
| WO2013096642A1 (en) * | 2011-12-23 | 2013-06-27 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| JP6329936B2 (ja) * | 2012-03-14 | 2018-05-23 | ソーク インスティテュート フォー バイオロジカル スタディーズ | アデノウイルス腫瘍診断 |
| KR102089121B1 (ko) | 2013-03-14 | 2020-03-13 | 더 솔크 인스티튜트 포 바이올로지칼 스터디즈 | 종양살상형 아데노바이러스 조성물 |
| MX2015011899A (es) | 2013-03-15 | 2016-05-05 | Genentech Inc | Metodos para el tratamiento de cáncer y prevención de resistencia a los fármacos para el cáncer. |
| JP2017505787A (ja) * | 2014-02-14 | 2017-02-23 | ザ ユニバーシティ オブ ブリティッシュ コロンビア | 治療薬としてのヒトアンドロゲン受容体dna結合ドメイン(dbd)化合物およびそれらを使用する方法 |
| CN117384961A (zh) | 2016-02-23 | 2024-01-12 | 萨克生物研究学院 | 对病毒动力学影响最小的治疗性腺病毒中的外源基因表达 |
| AU2017222568B2 (en) | 2016-02-23 | 2020-09-10 | Salk Institute For Biological Studies | High throughput assay for measuring adenovirus replication kinetics |
| WO2018111767A1 (en) | 2016-12-12 | 2018-06-21 | Salk Institute For Biological Studies | Tumor-targeting synthetic adenoviruses and uses thereof |
| MX2020010499A (es) | 2018-04-09 | 2020-10-28 | Salk Inst For Biological Studi | Composiciones de adenovirus oncoliticas con propiedades aumentadas de replicacion. |
| JP7498199B2 (ja) * | 2019-06-28 | 2024-06-11 | ファイザー・インク | 種々の疾患を処置するために有用なbckdk阻害剤としての5-(チオフェン-2-イル)-1h-テトラゾール誘導体 |
| CN110759900B (zh) * | 2019-10-25 | 2021-07-30 | 沈阳药科大学 | 噻吩类化合物的制备方法和用途 |
| MX2022007665A (es) | 2019-12-20 | 2022-07-19 | Bayer Ag | Tiofenocarboxamidas sustituidas y sus derivados. |
| CN113527281B (zh) * | 2020-04-20 | 2023-12-22 | 昆山彭济凯丰生物科技有限公司 | 杂环化合物及其制备方法和应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DD275870A1 (de) | 1988-09-27 | 1990-02-07 | Univ Leipzig | Verfahren zur herstellung von in 5-position verschiedenartig substituierten 3-aminothiophen-4-carbonitrilen |
| CA2565965A1 (en) | 2004-05-06 | 2006-07-27 | Plexxikon, Inc. | Pde4b inhibitors and uses therefor |
| GB0508472D0 (en) * | 2005-04-26 | 2005-06-01 | Glaxo Group Ltd | Compounds |
| BRPI0710874A2 (pt) | 2006-04-26 | 2012-02-14 | Hoffmann La Roche | compostos de tienopirimidina, processos de produção dos referidos compostos, composições farmacêuticas contendo os mesmos, kit, produto, e usos dos compostos |
| CN101484452A (zh) | 2006-05-03 | 2009-07-15 | 阿斯利康(瑞典)有限公司 | 噻唑衍生物及其作为抗肿瘤药物的用途 |
| AU2007287428B2 (en) * | 2006-08-24 | 2011-08-11 | Astrazeneca Ab | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| ES2399774T3 (es) * | 2007-09-24 | 2013-04-03 | Genentech, Inc. | Compuestos de tiazolopirimidina inhibidores de PI3K y métodos de uso |
| US9029411B2 (en) * | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| KR20110018451A (ko) * | 2008-06-19 | 2011-02-23 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 티오펜 또는 티아졸 유도체, 그리고 pi3k 저해물질로서 이들의 용도 |
-
2009
- 2009-06-17 KR KR1020117001175A patent/KR20110018451A/ko not_active Ceased
- 2009-06-17 WO PCT/US2009/003607 patent/WO2009154741A1/en not_active Ceased
- 2009-06-17 UA UAA201100563A patent/UA106206C2/ru unknown
- 2009-06-17 AU AU2009260782A patent/AU2009260782B2/en not_active Ceased
- 2009-06-17 CN CN2009801230046A patent/CN102066365A/zh active Pending
- 2009-06-17 US US12/456,455 patent/US8183240B2/en active Active
- 2009-06-17 NZ NZ589844A patent/NZ589844A/xx not_active IP Right Cessation
- 2009-06-17 GE GEAP200912065A patent/GEP20125650B/en unknown
- 2009-06-17 MX MX2010014125A patent/MX2010014125A/es active IP Right Grant
- 2009-06-17 ES ES09767054.1T patent/ES2491522T3/es active Active
- 2009-06-17 EP EP09767054.1A patent/EP2313399B1/en active Active
- 2009-06-17 JP JP2011514600A patent/JP5596026B2/ja active Active
- 2009-06-17 CA CA2727069A patent/CA2727069A1/en not_active Abandoned
- 2009-06-17 EA EA201170052A patent/EA201170052A1/ru unknown
- 2009-06-17 BR BRPI0914223A patent/BRPI0914223A2/pt not_active IP Right Cessation
-
2010
- 2010-12-09 ZA ZA2010/08875A patent/ZA201008875B/en unknown
- 2010-12-16 IL IL210055A patent/IL210055A0/en unknown
- 2010-12-17 CL CL2010001474A patent/CL2010001474A1/es unknown
- 2010-12-23 CO CO10161488A patent/CO6331431A2/es active IP Right Grant
-
2011
- 2011-01-13 MA MA33511A patent/MA32468B1/fr unknown
- 2011-01-17 CR CR20110032A patent/CR20110032A/es not_active Application Discontinuation
-
2012
- 2012-04-18 US US13/449,341 patent/US8440664B2/en active Active
-
2013
- 2013-04-01 US US13/854,409 patent/US20130217689A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CA2727069A1 (en) | 2009-12-23 |
| EP2313399B1 (en) | 2014-05-28 |
| US8440664B2 (en) | 2013-05-14 |
| GEP20125650B (en) | 2012-09-25 |
| AU2009260782A1 (en) | 2009-12-23 |
| US20120202812A1 (en) | 2012-08-09 |
| US20130217689A1 (en) | 2013-08-22 |
| MA32468B1 (fr) | 2011-07-03 |
| US20100075951A1 (en) | 2010-03-25 |
| BRPI0914223A2 (pt) | 2019-09-24 |
| EP2313399A1 (en) | 2011-04-27 |
| JP2011524904A (ja) | 2011-09-08 |
| EA201170052A1 (ru) | 2011-06-30 |
| UA106206C2 (ru) | 2014-08-11 |
| NZ589844A (en) | 2012-11-30 |
| CO6331431A2 (es) | 2011-10-20 |
| IL210055A0 (en) | 2011-02-28 |
| WO2009154741A8 (en) | 2010-03-25 |
| CR20110032A (es) | 2011-03-14 |
| MX2010014125A (es) | 2011-02-24 |
| CL2010001474A1 (es) | 2011-04-29 |
| KR20110018451A (ko) | 2011-02-23 |
| CN102066365A (zh) | 2011-05-18 |
| ZA201008875B (en) | 2012-02-29 |
| US8183240B2 (en) | 2012-05-22 |
| WO2009154741A1 (en) | 2009-12-23 |
| ES2491522T3 (es) | 2014-09-08 |
| AU2009260782B2 (en) | 2014-12-11 |
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| JP5596026B2 (ja) | チオフェン又はチアゾール誘導体及びpi3k阻害剤としてのそれらの使用 | |
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| AU2013203960A1 (en) | Thiophene or thiazole derivatives and their use as PI3K inhibitors | |
| HK40087839A (zh) | 哌嗪环状脲 |
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