CN103328442A - 可用于治疗代谢性和炎性疾病的氮杂环丁烷衍生物 - Google Patents
可用于治疗代谢性和炎性疾病的氮杂环丁烷衍生物 Download PDFInfo
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- CN103328442A CN103328442A CN2012800059625A CN201280005962A CN103328442A CN 103328442 A CN103328442 A CN 103328442A CN 2012800059625 A CN2012800059625 A CN 2012800059625A CN 201280005962 A CN201280005962 A CN 201280005962A CN 103328442 A CN103328442 A CN 103328442A
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- Prior art keywords
- methyl
- azetidine
- compound
- chloro
- alkyl
- 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 CCC(C)*(C)C([C@@](CCC(C)C)(CC1)*1C(CCN)=O)=O Chemical compound CCC(C)*(C)C([C@@](CCC(C)C)(CC1)*1C(CCN)=O)=O 0.000 description 4
- HEEGQHRLCYQJIX-UHFFFAOYSA-N CC(CC1)(C(N(CCCC(OC)=O)Cc(cc2)ccc2Cl)=O)N1C(Oc1ccc(C(F)(F)F)cc1)=O Chemical compound CC(CC1)(C(N(CCCC(OC)=O)Cc(cc2)ccc2Cl)=O)N1C(Oc1ccc(C(F)(F)F)cc1)=O HEEGQHRLCYQJIX-UHFFFAOYSA-N 0.000 description 1
- VLGJVKBHYMESGQ-UHFFFAOYSA-N CC1(C(N(CCCC(OC)=O)Cc(cc2)ccc2Cl)=O)NCC1 Chemical compound CC1(C(N(CCCC(OC)=O)Cc(cc2)ccc2Cl)=O)NCC1 VLGJVKBHYMESGQ-UHFFFAOYSA-N 0.000 description 1
- QAWFLJGZSZIZHO-UHFFFAOYSA-N COC(CCCBr)=O Chemical compound COC(CCCBr)=O QAWFLJGZSZIZHO-UHFFFAOYSA-N 0.000 description 1
- UQGOTDUTYINDJD-UHFFFAOYSA-N COC(c(cc1)cc2c1[s]cn2)=O Chemical compound COC(c(cc1)cc2c1[s]cn2)=O UQGOTDUTYINDJD-UHFFFAOYSA-N 0.000 description 1
- QOWBXWFYRXSBAS-UHFFFAOYSA-N COc1cc(OC)c(CN)cc1 Chemical compound COc1cc(OC)c(CN)cc1 QOWBXWFYRXSBAS-UHFFFAOYSA-N 0.000 description 1
- XRCLLNNZCPNEDU-UHFFFAOYSA-N COc1cc(OC)c(CNS(CCCCl)(=O)=O)cc1 Chemical compound COc1cc(OC)c(CNS(CCCCl)(=O)=O)cc1 XRCLLNNZCPNEDU-UHFFFAOYSA-N 0.000 description 1
- XRYJXFNGPZNSFR-UHFFFAOYSA-N COc1cc(OC)c(CNS(CCCNCc(cc2)ccc2Cl)(=O)=O)cc1 Chemical compound COc1cc(OC)c(CNS(CCCNCc(cc2)ccc2Cl)(=O)=O)cc1 XRYJXFNGPZNSFR-UHFFFAOYSA-N 0.000 description 1
- PINPOEWMCLFRRB-ZCFIWIBFSA-N C[C@H](c(cc1)ccc1Cl)N Chemical compound C[C@H](c(cc1)ccc1Cl)N PINPOEWMCLFRRB-ZCFIWIBFSA-N 0.000 description 1
- AIGIHDUXNLDEOO-SNVBAGLBSA-N C[C@H](c(cc1)ccc1Cl)NCCCC(OC)=O Chemical compound C[C@H](c(cc1)ccc1Cl)NCCCC(OC)=O AIGIHDUXNLDEOO-SNVBAGLBSA-N 0.000 description 1
- FYFLCWYDZJJMDE-UHFFFAOYSA-N Cc1ccccc1OC(Cl)=O Chemical compound Cc1ccccc1OC(Cl)=O FYFLCWYDZJJMDE-UHFFFAOYSA-N 0.000 description 1
- YMVFJGSXZNNUDW-UHFFFAOYSA-N NCc(cc1)ccc1Cl Chemical compound NCc(cc1)ccc1Cl YMVFJGSXZNNUDW-UHFFFAOYSA-N 0.000 description 1
- YMEMSAXFUBUVNV-UHFFFAOYSA-N O=Cc(cc1)cc2c1[s]cn2 Chemical compound O=Cc(cc1)cc2c1[s]cn2 YMEMSAXFUBUVNV-UHFFFAOYSA-N 0.000 description 1
- RBIZQDIIVYJNRS-UHFFFAOYSA-N OC(c1ccc2[s]cnc2c1)=O Chemical compound OC(c1ccc2[s]cnc2c1)=O RBIZQDIIVYJNRS-UHFFFAOYSA-N 0.000 description 1
- BAYGVMXZJBFEMB-UHFFFAOYSA-N Oc1ccc(C(F)(F)F)cc1 Chemical compound Oc1ccc(C(F)(F)F)cc1 BAYGVMXZJBFEMB-UHFFFAOYSA-N 0.000 description 1
- DFXQXFGFOLXAPO-UHFFFAOYSA-N [O-][N+](c1cc(C(O)=O)ccc1Cl)=O Chemical compound [O-][N+](c1cc(C(O)=O)ccc1Cl)=O DFXQXFGFOLXAPO-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
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- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
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- A61K31/415—1,2-Diazoles
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- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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- A61K31/425—Thiazoles
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- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- 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
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- C07D405/02—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
- C07D405/06—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 carbon chain containing only aliphatic carbon atoms
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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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- 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
- C07D409/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
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- 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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- 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
- C07D417/14—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 three or more hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161434077P | 2011-01-19 | 2011-01-19 | |
| US61/434,077 | 2011-01-19 | ||
| PCT/EP2012/050297 WO2012098033A1 (en) | 2011-01-19 | 2012-01-10 | Azetidine derivatives useful for the treatment of metabolic and inflammatory diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103328442A true CN103328442A (zh) | 2013-09-25 |
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ID=45507689
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107709337A (zh) * | 2015-07-07 | 2018-02-16 | 日本烟草产业株式会社 | 7H‑吡咯并[2,3‑d]嘧啶衍生物的制备方法和其中间体 |
| CN108863980A (zh) * | 2018-07-05 | 2018-11-23 | 浙江工业大学 | 一种合成1-(5-苯并噻唑基)乙酮的方法 |
| CN110684000A (zh) * | 2019-10-18 | 2020-01-14 | 上海皓元医药股份有限公司 | 苯并呋喃衍生物的制备方法 |
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| AU2012208693B2 (en) * | 2011-01-19 | 2015-02-26 | Galapagos Nv | Azetidine derivatives useful for the treatment of metabolic and inflammatory diseases |
| CN105916500A (zh) | 2013-11-27 | 2016-08-31 | 欧洲筛选有限公司 | 用于治疗炎性疾病的化合物、药物组合物和方法 |
| US9839644B2 (en) | 2014-09-09 | 2017-12-12 | ARKAY Therapeutics, LLC | Formulations and methods for treatment of metabolic syndrome |
| KR101656662B1 (ko) * | 2014-11-18 | 2016-09-12 | 한국생명공학연구원 | 2-옥소-1,2,3,4-테트라하이드로피리미딘-5-카르복사미드 유도체를 유효성분으로 함유하는 대사성 질환 예방 또는 치료용 약학적 조성물 |
| AU2017384317C1 (en) | 2016-12-21 | 2022-06-30 | Japan Tobacco Inc. | PROCESS FOR PREPARING 7H-PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES AND SYNTHETIC INTERMEDIATES THEREOF |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| TWI707849B (zh) | 2018-02-13 | 2020-10-21 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| KR102591947B1 (ko) | 2018-04-19 | 2023-10-25 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| EP3820572B1 (en) | 2018-07-13 | 2023-08-16 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| US11236085B2 (en) | 2018-10-24 | 2022-02-01 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
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- 2012-01-10 US US13/980,798 patent/US8759334B2/en not_active Expired - Fee Related
- 2012-01-10 CN CN2012800059625A patent/CN103328442A/zh active Pending
- 2012-01-10 RU RU2013138372/04A patent/RU2013138372A/ru not_active Application Discontinuation
- 2012-01-10 PH PH1/2013/501437A patent/PH12013501437A1/en unknown
- 2012-01-10 WO PCT/EP2012/050297 patent/WO2012098033A1/en not_active Ceased
- 2012-01-10 JP JP2013549769A patent/JP2014507414A/ja active Pending
- 2012-01-10 CA CA2824460A patent/CA2824460A1/en not_active Abandoned
- 2012-01-10 BR BR112013018286A patent/BR112013018286A2/pt not_active IP Right Cessation
- 2012-01-10 GB GB1213267.6A patent/GB2489382A/en not_active Withdrawn
- 2012-01-10 KR KR1020137020884A patent/KR20140040104A/ko not_active Withdrawn
- 2012-01-10 SG SG2013048038A patent/SG191291A1/en unknown
- 2012-01-10 EP EP12700552.8A patent/EP2665704A1/en not_active Withdrawn
- 2012-01-10 MX MX2013008257A patent/MX2013008257A/es not_active Application Discontinuation
- 2012-01-13 AR ARP120100129A patent/AR084857A1/es unknown
- 2012-01-18 TW TW101102008A patent/TW201245144A/zh unknown
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- 2013-06-27 ZA ZA2013/04822A patent/ZA201304822B/en unknown
- 2013-08-15 CO CO13194671A patent/CO6741223A2/es unknown
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- 2014-06-23 US US14/311,574 patent/US20140371198A1/en not_active Abandoned
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| CN107709337A (zh) * | 2015-07-07 | 2018-02-16 | 日本烟草产业株式会社 | 7H‑吡咯并[2,3‑d]嘧啶衍生物的制备方法和其中间体 |
| CN107709337B (zh) * | 2015-07-07 | 2021-11-16 | 日本烟草产业株式会社 | 7H-吡咯并[2,3-d]嘧啶衍生物的制备方法和其中间体 |
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Also Published As
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| CO6741223A2 (es) | 2013-08-30 |
| WO2012098033A1 (en) | 2012-07-26 |
| GB2489382A (en) | 2012-09-26 |
| KR20140040104A (ko) | 2014-04-02 |
| US20130303515A1 (en) | 2013-11-14 |
| AU2012208693A1 (en) | 2013-03-21 |
| RU2013138372A (ru) | 2015-02-27 |
| ZA201304822B (en) | 2014-03-26 |
| CA2824460A1 (en) | 2012-07-26 |
| JP2014507414A (ja) | 2014-03-27 |
| AU2012208693B2 (en) | 2015-02-26 |
| BR112013018286A2 (pt) | 2016-11-16 |
| PH12013501437A1 (en) | 2013-09-16 |
| US8759334B2 (en) | 2014-06-24 |
| GB201213267D0 (en) | 2012-09-05 |
| MX2013008257A (es) | 2013-08-12 |
| AR084857A1 (es) | 2013-06-26 |
| TW201245144A (en) | 2012-11-16 |
| EP2665704A1 (en) | 2013-11-27 |
| SG191291A1 (en) | 2013-07-31 |
| US20140371198A1 (en) | 2014-12-18 |
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