HRP20170873T1 - Monociklički derivat piridina - Google Patents
Monociklički derivat piridina Download PDFInfo
- Publication number
- HRP20170873T1 HRP20170873T1 HRP20170873TT HRP20170873T HRP20170873T1 HR P20170873 T1 HRP20170873 T1 HR P20170873T1 HR P20170873T T HRP20170873T T HR P20170873TT HR P20170873 T HRP20170873 T HR P20170873T HR P20170873 T1 HRP20170873 T1 HR P20170873T1
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- Prior art keywords
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- pharmaceutically acceptable
- acceptable salt
- compound
- alkoxy
- Prior art date
Links
- -1 Monocyclic pyridine derivative Chemical class 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000005843 halogen group Chemical group 0.000 claims 16
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 15
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 9
- 125000002393 azetidinyl group Chemical group 0.000 claims 6
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 5
- 125000006585 (C6-C10) arylene group Chemical group 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000005549 heteroarylene group Chemical group 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 1
- 208000033749 Small cell carcinoma of the bladder Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000005551 pyridylene group Chemical group 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 125000005556 thienylene group Chemical group 0.000 claims 1
- 201000007710 urinary bladder small cell neuroendocrine carcinoma Diseases 0.000 claims 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
-
- 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
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
Claims (16)
1. Spoj predstavljen sa slijedećom formulom (IA) ili njegova farmaceutski prihvatljiva sol
[image]
naznačen time da
n predstavlja 0 do 2;
A predstavlja skupinu C6-10 arilen ili skupinu C3-5 heteroarilen;
G predstavlja jednostruku vezu, kisikov atom ili -CH2-;
E predstavlja C3-5 ne-aromatski heterocikl koji sadrži dušik;
R1 predstavlja skupinu cijano, skupinu mono-C1-6 alkilamino, skupinu di-C1-6 alkilamino, skupinu C2-6 alkil proizvoljno supstituiranu s 1 do 3 halogenih atoma, skupinu C1-6 alkoksi proizvoljno supstituiranu s 1 do 3 halogenih atoma ili jednu hidroksilnu skupinu, skupinu C1-6 alkoksi C1-6 alkil proizvoljno supstituiranu s 1 do 3 halogenih atoma, ili skupinu C1-6 alkoksi C1-6 alkoksi proizvoljno supstituiranu s 1 do 3 halogenih atoma;
R2 predstavlja vodikov atom, halogeni atom, hidroksilnu skupinu, skupinu C2-6 acil proizvoljno supstituiranu s jednim supstituentom odabranim iz skupine S koja je opisana ispod, skupinu C1-6 alkil proizvoljno supstituiranu s 1 do 3 halogenih atoma, skupinu hidroksi C1-6 alkil proizvoljno supstituiranu s 1 do 3 halogenih atoma, ili C3-5 ne-aromatsku heterocikličku skupinu koja sadrži dušik;
R3 predstavlja vodikov atom, okso skupinu, skupinu C1-6 alkil proizvoljno supstituiranu s 1 do 3 halogenih atoma, ili skupinu C1-6 alkoksi proizvoljno supstituiranu s 1 do 3 halogenih atoma;
R4 predstavlja skupinu C1-6 alkil, uz uvjet da kada E predstavlja azetidinski prsten i R2 ili R3 je prisutan na dušikovom atomu u azetidinskom prstenu, R2 ili R3 ne predstavljaju vodikov atom; i
skupina S predstavlja skupinu koja sadrži hidroksilnu skupinu, skupinu mono-C1-6 alkilamino, skupinu di-C1-6 alkilamino, skupinu C1-6 alkoksi i C3-5 ne-aromatsku heterocikličku skupinu koja sadrži dušik.
2. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1, predstavljen sa slijedećom formulom (IB):
[image]
naznačen time da
n predstavlja 0 do 2;
A predstavlja skupinu C6-10 arilen ili skupinu C3-5 heteroarilen;
G predstavlja jednostruku vezu, kisikov atom ili -CH2-;
E predstavlja C3-5 ne-aromatski heterocikl koji sadrži dušik;
R1 predstavlja skupinu C1-6 alkoksi proizvoljno supstituiranu s 1 do 3 halogenih atoma ili jednom hidroksilnom skupinom, ili skupinu C1-6 alkoksi C1-6 alkoksi proizvoljno supstituiranu s 1 do 3 halogenih atoma;
R2 predstavlja vodikov atom, halogeni atom, hidroksilnu skupinu, skupinu C1-6 alkil proizvoljno supstituiranu s 1 do 3 halogenih atoma, skupinu hidroksi C1-6 alkil proizvoljno supstituiranu s 1 do 3 halogenih atoma, ili C3-5 ne-aromatsku heterocikličku skupinu koja sadrži dušik; i
R3 predstavlja vodikov atom, okso skupinu, skupinu C1-6 alkil proizvoljno supstituiranu s 1 do 3 halogenih atoma, ili skupinu C1-6 alkoksi proizvoljno supstituiranu s 1 do 3 halogenih atoma, uz uvjet da kada E predstavlja azetidinski prsten i R2 ili R3 je prisutan na dušikovom atomu na azetidinskom prstenu, R2 ili R3 ne predstavljaju vodikov atom.
3. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1 ili 2, naznačen time da A predstavlja skupinu C6-10 arilen.
4. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 3, naznačen time da G predstavlja jednostruku vezu ili kisikov atom.
5. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1 ili 2, naznačen time da
A predstavlja skupinu fenilen, skupinu tienilen skupinu, skupinu pirazolilen ili skupinu piridilen; i
E predstavlja azetidinski prsten, pirolidinski prsten, piperidinski prsten ili piperazinski prsten
ili pri čemu
A predstavlja skupinu fenilen; i
E predstavlja azetidinski prsten ili piperidinski prsten
ili pri čemu
A predstavlja skupinu fenilen; i
E predstavlja piperidinski prsten.
6. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 5, naznačen time da
n predstavlja 0; i
G predstavlja jednostruku vezu.
7. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 6, naznačen time da
R1 predstavlja skupinu C1-6 alkoksi ili skupinu C1-6 alkoksi C1-6 alkoksi;
R2 predstavlja vodikov atom, hidroksilnu skupinu, skupinu C1-6 alkil ili skupinu hidroksi C1-6 alkil; i
R3 predstavlja vodikov atom.
8. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 7, naznačen time da R1 predstavlja skupinu C1-6 alkoksi C1-6 alkoksi.
9. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1 ili 2, predstavljen sa slijedećom formulom (II):
[image]
naznačen time da R1 predstavlja skupinu C1-6 alkoksi C1-6 alkoksi; i
R2 predstavlja vodikov atom, skupinu C1-6 alkil ili skupinu hidroksi C2-6 alkil
ili predstavljen sa slijedećom formulom (III):
[image]
pri čemu
R1 predstavlja skupinu C1-6 alkoksi C1-6 alkoksi; i
R2 predstavlja skupinu C1-6 alkil ili skupinu hidroksi C2-6 alkil.
10. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1, naznačen time da spoj je
5-((2-(4-(1-etilpiperidin-4-il)benzamid)piridin-4-il)oksi)-6-metoksi-N-metil-1H-indol-1-karboksamid predstavljen sa slijedećom strukturnom formulom, ili njegova farmaceutski prihvatljiva sol:
[image]
ili
6-(2-metoksietoksi)-N-metil-5-((2-(4-(1-metilpiperidin-4-il)benzamid)piridin-4-il)oksi)-1H-indol-1-karboksamid predstavljen sa slijedećom strukturnom formulom, ili njegova farmaceutski prihvatljiva sol:
[image]
ili
6-(2-etoksietoksi)-5-((2-(4-(1-(2-hidroksietil)piperidin-4-il)benzamid)piridin-4-il)oksi)-N-metil-1H-indol-1-karboksamid predstavljen sa slijedećom strukturnom formulom, ili njegova farmaceutski prihvatljiva sol:
[image]
ili
6-(2-etoksietoksi)-5-((2-(4-(1-etilazetidin-3-il)benzamid)piridin-4-il)oksi)-N-metil-1H-indol-1-karboksamid predstavljen sa slijedećom strukturnom formulom, ili njegova farmaceutski prihvatljiva sol:
[image]
11. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1, naznačen time da spoj je
5-((2-(4-(1-(2-hidroksietil)piperidin-4-il)benzamid)piridin-4-il)oksi)-6-(2-met-oksietoksi)-N-metil-1H-indol-1-karboksamid predstavljen sa slijedećom strukturnom formulom, ili njegova farmaceutski prihvatljiva sol:
[image]
12. Farmaceutski pripravak, naznačen time da sadrži spoj ili njegovu farmaceutski prihvatljivu sol prema bilo kojem od zahtjeva 1 do 11.
13. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 11, naznačen time da je za uporabu kao terapijsko sredstvo.
14. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 11, naznačen time da je za uporabu u postupku liječenja karcinoma želuca, karcinoma ne-malih stanica pluća, karcinoma mjehura ili raka endometrija.
15. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 11, naznačen time da je za uporabu u postupku liječenja karcinoma ne-malih stanica pluća.
16. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 11, naznačen time da je za uporabu u postupku liječenja karcinoma skvamoznih stanica.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361766922P | 2013-02-20 | 2013-02-20 | |
EP14754294.8A EP2960238B1 (en) | 2013-02-20 | 2014-02-18 | Monocyclic pyridine derivative |
PCT/JP2014/053819 WO2014129477A1 (ja) | 2013-02-20 | 2014-02-18 | 単環ピリジン誘導体 |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20170873T1 true HRP20170873T1 (hr) | 2017-09-08 |
Family
ID=51351646
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20170873TT HRP20170873T1 (hr) | 2013-02-20 | 2017-06-07 | Monociklički derivat piridina |
Country Status (35)
Country | Link |
---|---|
US (1) | US8933099B2 (hr) |
EP (1) | EP2960238B1 (hr) |
JP (2) | JP5600229B1 (hr) |
KR (1) | KR102050128B1 (hr) |
CN (1) | CN105073730B (hr) |
AR (1) | AR094812A1 (hr) |
AU (1) | AU2014219811B2 (hr) |
BR (1) | BR112015019790B1 (hr) |
CA (1) | CA2901585C (hr) |
CL (1) | CL2015002311A1 (hr) |
CY (1) | CY1119220T1 (hr) |
DK (1) | DK2960238T3 (hr) |
ES (1) | ES2628495T3 (hr) |
HK (1) | HK1215949A1 (hr) |
HR (1) | HRP20170873T1 (hr) |
HU (1) | HUE032931T2 (hr) |
IL (1) | IL240623B (hr) |
JO (1) | JO3261B1 (hr) |
LT (1) | LT2960238T (hr) |
ME (1) | ME02755B (hr) |
MX (1) | MX361870B (hr) |
MY (1) | MY178760A (hr) |
NZ (1) | NZ711101A (hr) |
PE (1) | PE20151509A1 (hr) |
PH (1) | PH12015501813A1 (hr) |
PL (1) | PL2960238T3 (hr) |
PT (1) | PT2960238T (hr) |
RS (1) | RS56064B1 (hr) |
RU (1) | RU2645352C2 (hr) |
SG (1) | SG11201506488WA (hr) |
SI (1) | SI2960238T1 (hr) |
TW (4) | TWI672296B (hr) |
UA (1) | UA116794C2 (hr) |
WO (1) | WO2014129477A1 (hr) |
ZA (1) | ZA201505941B (hr) |
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KR102344105B1 (ko) * | 2014-08-18 | 2021-12-29 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 모노시클릭 피리딘 유도체의 염 및 이의 결정 |
BR112017016392B1 (pt) * | 2015-03-25 | 2023-02-23 | National Cancer Center | Agente terapêutico para câncer do ducto biliar |
WO2017104739A1 (ja) * | 2015-12-17 | 2017-06-22 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 乳がん治療剤 |
CN107098884A (zh) * | 2016-02-19 | 2017-08-29 | 中国科学院上海药物研究所 | 一类取代的氨基吡啶类化合物及其制备和用途 |
EP3694513A4 (en) * | 2017-10-12 | 2021-06-30 | Eisai R&D Management Co., Ltd. | PHARMACEUTICAL COMPOSITION WITH FGFR-SELECTIVE TYROSINKINAS INHIBITOR |
EP3777860A4 (en) | 2018-03-28 | 2021-12-15 | Eisai R&D Management Co., Ltd. | THERAPEUTIC FOR HEPATOCELLULAR CARCINOMA |
AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
US20220401436A1 (en) | 2019-11-08 | 2022-12-22 | INSERM (Institute National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
BR112022020786A2 (pt) | 2020-04-17 | 2022-11-29 | Eisai R&D Man Co Ltd | Agente terapêutico de câncer de mama |
AU2021315234A1 (en) | 2020-07-31 | 2023-01-19 | Eisai R&D Management Co., Ltd. | Therapeutic agent for breast cancer |
WO2022092085A1 (ja) | 2020-10-28 | 2022-05-05 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 腫瘍治療用医薬組成物 |
EP4361143A1 (en) | 2021-08-31 | 2024-05-01 | Eisai R&D Management Co., Ltd. | Method for producing monocyclic pyridine derivative |
CA3227445A1 (en) | 2021-08-31 | 2023-03-09 | Eisai R&D Management Co., Ltd. | Production method for synthetic intermediate of monocyclic pyridine derivative |
WO2023174400A1 (zh) * | 2022-03-18 | 2023-09-21 | 上海润石医药科技有限公司 | 一种取代的氨基六元氮杂环类化合物的盐及其晶型、制备方法和应用 |
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