CN104245700B - 二取代的苯并噻吩基-吡咯并三嗪及其作为fgfr激酶抑制剂的用途 - Google Patents
二取代的苯并噻吩基-吡咯并三嗪及其作为fgfr激酶抑制剂的用途 Download PDFInfo
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- CN104245700B CN104245700B CN201280069882.6A CN201280069882A CN104245700B CN 104245700 B CN104245700 B CN 104245700B CN 201280069882 A CN201280069882 A CN 201280069882A CN 104245700 B CN104245700 B CN 104245700B
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- 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
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical 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)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Treatment Of Liquids With Adsorbents In General (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11193841 | 2011-12-15 | ||
| EP11193841.1 | 2011-12-15 | ||
| PCT/EP2012/074977 WO2013087578A1 (en) | 2011-12-15 | 2012-12-10 | Disubstituted benzothienyl-pyrrolotriazines and their use as fgfr kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104245700A CN104245700A (zh) | 2014-12-24 |
| CN104245700B true CN104245700B (zh) | 2016-11-16 |
Family
ID=47326168
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280069882.6A Expired - Fee Related CN104245700B (zh) | 2011-12-15 | 2012-12-10 | 二取代的苯并噻吩基-吡咯并三嗪及其作为fgfr激酶抑制剂的用途 |
Country Status (42)
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10388493B2 (en) | 2011-09-16 | 2019-08-20 | Lam Research Corporation | Component of a substrate support assembly producing localized magnetic fields |
| UY34484A (es) * | 2011-12-15 | 2013-07-31 | Bayer Ip Gmbh | Benzotienilo-pirrolotriazinas disustituidas y sus usos |
| WO2015008844A1 (ja) | 2013-07-18 | 2015-01-22 | 大鵬薬品工業株式会社 | Ｆｇｆｒ阻害剤耐性癌の治療薬 |
| TR201907147T4 (tr) | 2013-07-18 | 2019-06-21 | Taiho Pharmaceutical Co Ltd | Fgfr inhibitörünün aralıklı uygulanmasına yönelik anti-tümör ilaç. |
| EP3060562B1 (en) * | 2013-10-21 | 2021-07-28 | Genosco | Substituted pyrimidine compounds and their use as syk inhibitors |
| MX2017007656A (es) * | 2014-12-11 | 2017-10-11 | Bayer Pharma AG | Uso de los inhibidores de pan fgfr y metodo para identificacion de pacientes con cancer elegibles para el tratamiento con un inhibidor de pan fgfr. |
| KR20180013851A (ko) * | 2015-03-09 | 2018-02-07 | 바이엘 파마 악티엔게젤샤프트 | 치환된 2,3-디히드로이미다조[1,2-c]퀴나졸린-함유 조합물 |
| CN109311868B (zh) | 2015-12-22 | 2022-04-01 | 尚医治疗有限责任公司 | 用于治疗癌症和炎性疾病的化合物 |
| US11883404B2 (en) | 2016-03-04 | 2024-01-30 | Taiho Pharmaceuticals Co., Ltd. | Preparation and composition for treatment of malignant tumors |
| KR102793563B1 (ko) | 2016-03-04 | 2025-04-11 | 다이호야쿠힌고교 가부시키가이샤 | 악성 종양 치료용 제제 및 조성물 |
| TWI753892B (zh) | 2016-03-28 | 2022-02-01 | 美商英塞特公司 | 作為ｔａｍ抑制劑之吡咯并三嗪化合物 |
| CN107513068A (zh) * | 2016-06-16 | 2017-12-26 | 中国科学院上海药物研究所 | 一种具有fgfr抑制活性的新型化合物及其制备和应用 |
| US10131670B2 (en) | 2016-12-16 | 2018-11-20 | Cystic Fibrosis Foundation Therapeutics, Inc. | Bicyclic heteroaryl derivatives as CFTR potentiators |
| IL271230B2 (en) | 2017-06-21 | 2024-06-01 | SHY Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| WO2019034075A1 (zh) * | 2017-08-15 | 2019-02-21 | 南京明德新药研发股份有限公司 | Fgfr和egfr抑制剂 |
| JP7341122B2 (ja) * | 2017-08-15 | 2023-09-08 | 石薬集団中奇制薬技術（石家庄）有限公司 | Ｆｇｆｒ阻害剤及びその医薬品の用途 |
| MA50655B1 (fr) | 2017-09-27 | 2021-11-30 | Incyte Corp | Sels de dérivés de pyrrolotriazine utiles en tant qu'inhibiteurs de tam |
| KR20200074128A (ko) * | 2017-10-25 | 2020-06-24 | 바이엘 파마 악티엔게젤샤프트 | 벤조티오펜-2-일 보로네이트의 제조 방법 |
| WO2019105734A1 (en) | 2017-11-28 | 2019-06-06 | Bayer Consumer Care Ag | Combinations of copanlisib |
| MY203305A (en) | 2018-03-19 | 2024-06-23 | Taiho Pharmaceutical Co Ltd | Pharmaceutical composition including sodium alkyl sulfate |
| WO2019180141A1 (en) | 2018-03-23 | 2019-09-26 | Bayer Aktiengesellschaft | Combinations of rogaratinib |
| MD3813800T2 (ro) | 2018-06-29 | 2025-10-31 | Incyte Corp | Formulări de inhibitor al AXL/MER |
| JP7407461B2 (ja) | 2018-12-19 | 2024-01-04 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ｒａｓ病、及び線維性疾患の処置のためのｒａｓスーパーファミリーと相互作用する化合物 |
| EA202192133A1 (ru) | 2019-01-31 | 2022-02-09 | Байер Акциенгезельшафт | Моногидрат гидрохлорида рогаратиниба и его твердые состояния |
| WO2020164603A1 (zh) * | 2019-02-15 | 2020-08-20 | 石药集团中奇制药技术（石家庄）有限公司 | 固体形式的fgfr抑制剂化合物及其制备方法 |
| WO2020170355A1 (ja) * | 2019-02-20 | 2020-08-27 | 大鵬薬品工業株式会社 | Ｆｇｆｒ１変異腫瘍の治療方法 |
| CN109928976A (zh) * | 2019-02-26 | 2019-06-25 | 泰州亿腾景昂药业有限公司 | 一种工业化生产eoc317的方法 |
| PH12021552862A1 (en) * | 2019-05-13 | 2022-12-19 | De Shaw Res Llc | Fgfr inhibitors and methods of use thereof |
| CN114641293B (zh) * | 2019-11-08 | 2024-05-31 | 石药集团中奇制药技术（石家庄）有限公司 | 一种fgfr抑制剂的用途 |
| CN111004234A (zh) * | 2019-11-28 | 2020-04-14 | 湖南农业大学 | 一种2-苯基咪唑并[1,2-α]吡啶类化合物的C3位卤化方法 |
| CN115697343A (zh) | 2020-03-06 | 2023-02-03 | 因赛特公司 | 包含axl/mer和pd-1/pd-l1抑制剂的组合疗法 |
| CN117402161A (zh) * | 2022-07-06 | 2024-01-16 | 上海科恩泰生物医药科技有限公司 | 一种具有fgfr抑制作用的亚砜亚胺类化合物、包含其的药物组合物及其用途 |
| TW202504611A (zh) | 2023-03-30 | 2025-02-01 | 美商銳新醫藥公司 | 用於誘導ｒａｓ ｇｔｐ水解之組合物及其用途 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
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|---|---|---|---|---|
| WO2004096806A1 (ja) * | 2003-04-30 | 2004-11-11 | Sumitomo Pharmaceuticals Co. Ltd. | 縮合イミダゾール誘導体 |
| WO2004111051A1 (de) * | 2003-06-18 | 2004-12-23 | Boehringer Ingelheim International Gmbh | Imidazopyridazinon- und imidazopyridonderivate, deren herstellung und deren verwendung als arzneimittel |
| CN101087792A (zh) * | 2004-12-22 | 2007-12-12 | 布里斯托尔-迈尔斯斯奎布公司 | 制备双环化合物的合成方法 |
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| CA2373990C (en) * | 1999-05-21 | 2007-05-08 | Bristol-Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| HUP0303363A2 (hu) | 1999-09-17 | 2004-07-28 | Abbott Gmbh & Co., Kg | Kináz-inhibitor hatású heterociklusos vegyületek alkalmazása gyógyszerkészítmények előállítására |
| ES2652440T3 (es) | 2004-04-02 | 2018-02-02 | OSI Pharmaceuticals, LLC | Inhibidores de proteína cinasa heterobicíclicos sustituidos con anillo 6,6-bicíclico |
| UY28931A1 (es) | 2004-06-03 | 2005-12-30 | Bayer Pharmaceuticals Corp | Derivados de pirrolotriazina utiles para tratar trastornos hiper-proliferativos y enfermedades asociadas con angiogenesis |
| JP5116687B2 (ja) | 2005-11-02 | 2013-01-09 | バイエル・ファルマ・アクチェンゲゼルシャフト | がんおよび他の過剰増殖性疾患の処置のためのピロロ［２，１−ｆ］［１，２，４］トリアジン−４−イルアミンＩＧＦ−１Ｒキナーゼ阻害剤 |
| KR20080078668A (ko) * | 2005-11-17 | 2008-08-27 | 오에스아이 파마슈티컬스, 인코포레이티드 | 융합된 바이사이클릭 ｍＴＯＲ 억제자 |
| US7514435B2 (en) | 2005-11-18 | 2009-04-07 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| WO2007064932A2 (en) | 2005-12-02 | 2007-06-07 | Bayer Healthcare Llc. | Pyrrolotriazine derivatives useful for treating cancer through inhibition of aurora kinase |
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| BRPI0619146A2 (pt) | 2005-12-02 | 2011-09-13 | Bayer Pharmaceuticals Corp | derivados de 4-amino-pirroltriazina substituìda úteis no tratamento de disordens e doenças hiperproliferativas associadas com angiogênesis |
| CA2635231C (en) * | 2005-12-29 | 2014-07-15 | Abbott Laboratories | Protein kinase inhibitors |
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| US8476431B2 (en) | 2008-11-03 | 2013-07-02 | Itellikine LLC | Benzoxazole kinase inhibitors and methods of use |
| JP5656976B2 (ja) | 2009-04-29 | 2015-01-21 | ローカス ファーマシューティカルズ インコーポレイテッド | ピロロトリアジン化合物 |
| UY34484A (es) * | 2011-12-15 | 2013-07-31 | Bayer Ip Gmbh | Benzotienilo-pirrolotriazinas disustituidas y sus usos |
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2012
- 2012-12-03 UY UY0001034484A patent/UY34484A/es unknown
- 2012-12-10 SI SI201230702A patent/SI2791140T1/sl unknown
- 2012-12-10 UA UAA201407930A patent/UA116768C2/uk unknown
- 2012-12-10 ES ES12798738.6T patent/ES2591203T3/es active Active
- 2012-12-10 PT PT127987386T patent/PT2791140T/pt unknown
- 2012-12-10 EP EP12798738.6A patent/EP2791140B1/en active Active
- 2012-12-10 PL PL12798738T patent/PL2791140T3/pl unknown
- 2012-12-10 BR BR112014014531-8A patent/BR112014014531B1/pt not_active IP Right Cessation
- 2012-12-10 JP JP2014546445A patent/JP6050829B2/ja not_active Expired - Fee Related
- 2012-12-10 LT LTEP12798738.6T patent/LT2791140T/lt unknown
- 2012-12-10 IN IN4310CHN2014 patent/IN2014CN04310A/en unknown
- 2012-12-10 HU HUE12798738A patent/HUE029582T2/en unknown
- 2012-12-10 ME MEP-2016-181A patent/ME02517B/me unknown
- 2012-12-10 CN CN201280069882.6A patent/CN104245700B/zh not_active Expired - Fee Related
- 2012-12-10 MX MX2014006905A patent/MX367158B/es active IP Right Grant
- 2012-12-10 PE PE2014000926A patent/PE20141855A1/es active IP Right Grant
- 2012-12-10 WO PCT/EP2012/074977 patent/WO2013087578A1/en not_active Ceased
- 2012-12-10 EA EA201400707A patent/EA029556B1/ru not_active IP Right Cessation
- 2012-12-10 CA CA2859133A patent/CA2859133C/en active Active
- 2012-12-10 RS RS20160733A patent/RS55144B1/sr unknown
- 2012-12-10 CU CU2016000039A patent/CU24426B1/es unknown
- 2012-12-10 US US14/365,424 patent/US20140336173A1/en not_active Abandoned
- 2012-12-10 AU AU2012350750A patent/AU2012350750B2/en not_active Ceased
- 2012-12-10 SG SG11201402325QA patent/SG11201402325QA/en unknown
- 2012-12-10 HR HRP20161130TT patent/HRP20161130T1/hr unknown
- 2012-12-10 DK DK12798738.6T patent/DK2791140T3/en active
- 2012-12-10 KR KR1020147019406A patent/KR102057444B1/ko not_active Expired - Fee Related
- 2012-12-10 MY MYPI2014701550A patent/MY178660A/en unknown
- 2012-12-12 JO JOP/2012/0377A patent/JO3295B1/ar active
- 2012-12-12 AR ARP120104679A patent/AR089207A1/es unknown
- 2012-12-14 US US13/715,553 patent/US9206184B2/en active Active
- 2012-12-14 TW TW101147336A patent/TWI567076B/zh not_active IP Right Cessation
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2014
- 2014-05-14 IL IL232611A patent/IL232611A/en active IP Right Grant
- 2014-06-09 CU CUP2014000065A patent/CU20140065A7/es unknown
- 2014-06-09 CO CO14123802A patent/CO7030961A2/es unknown
- 2014-06-10 DO DO2014000127A patent/DOP2014000127A/es unknown
- 2014-06-11 TN TNP2014000255A patent/TN2014000255A1/en unknown
- 2014-06-12 EC ECIEPI20144722A patent/ECSP14004722A/es unknown
- 2014-06-12 CL CL2014001547A patent/CL2014001547A1/es unknown
- 2014-06-13 PH PH12014501355A patent/PH12014501355A1/en unknown
- 2014-06-13 GT GT201400113A patent/GT201400113A/es unknown
- 2014-06-17 CR CR20140288A patent/CR20140288A/es unknown
- 2014-07-14 ZA ZA2014/05140A patent/ZA201405140B/en unknown
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2016
- 2016-08-31 CY CY20161100853T patent/CY1118112T1/el unknown
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2017
- 2017-07-17 AU AU2017206140A patent/AU2017206140A1/en not_active Abandoned
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2018
- 2018-02-20 US US15/900,725 patent/US20190016724A1/en not_active Abandoned
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2019
- 2019-06-18 AU AU2019204255A patent/AU2019204255A1/en not_active Abandoned
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2021
- 2021-11-01 US US17/516,542 patent/US20220153745A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004096806A1 (ja) * | 2003-04-30 | 2004-11-11 | Sumitomo Pharmaceuticals Co. Ltd. | 縮合イミダゾール誘導体 |
| WO2004111051A1 (de) * | 2003-06-18 | 2004-12-23 | Boehringer Ingelheim International Gmbh | Imidazopyridazinon- und imidazopyridonderivate, deren herstellung und deren verwendung als arzneimittel |
| CN101087792A (zh) * | 2004-12-22 | 2007-12-12 | 布里斯托尔-迈尔斯斯奎布公司 | 制备双环化合物的合成方法 |
Non-Patent Citations (1)
| Title |
|---|
| "新型抗糖尿病药物二肽基肽酶Ⅳ抑制剂";焦伟杰 等;《药学进展》;20081231;第32卷(第7期);第289-296页 * |
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