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1. (WO2017133687) TLR7 AGONIST TRIFLUOROACETATE SALT AND CRYSTALLINE FORM B THEREOF, PREPARATION METHODS AND USES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/133687 International Application No.: PCT/CN2017/072894
Publication Date: 10.08.2017 International Filing Date: 04.02.2017
IPC:
C07D 487/04 (2006.01) ,A61K 31/519 (2006.01) ,A61P 31/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12
Antivirals
Applicants:
正大天晴药业集团股份有限公司 CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD. [CN/CN]; 中国江苏省连云港市 海州区郁州南路369号 No.369 Yuzhou South Rd., Haizhou District Lianyungang, Jiangsu 222062, CN
Inventors:
丁照中 DING, Zhaozhong; CN
孙飞 SUN, Fei; CN
胡迎虎 HU, Yinghu; CN
周义龙 ZHOU, Yilong; CN
王峥 WANG, Zheng; CN
赵锐 ZHAO, Rui; CN
杨玲 YANG, Ling; CN
Agent:
北京永新同创知识产权代理有限公司 NTD UNIVATION INTELLECTUAL PROPERTY AGENCY LTD.; 中国北京市 东城区北三环东路36号北京环球贸易中心C座10层 10th Floor, Tower C, Beijing Global Trade Center, 36 North Third Ring Road East, Dongcheng District Beijing 100013, CN
Priority Data:
201610081899.305.02.2016CN
Title (EN) TLR7 AGONIST TRIFLUOROACETATE SALT AND CRYSTALLINE FORM B THEREOF, PREPARATION METHODS AND USES
(FR) SEL DE TRIFLUOROACÉTATE D'UN AGONISTE DE TLR7, SA FORME CRISTALLINE B, SES PROCÉDÉS DE PRÉPARATION ET SES UTILISATIONS
(ZH) 一种TLR7激动剂的三氟乙酸盐、晶型B、制备方法和用途
Abstract:
(EN) The present invention relates to a trifluoroacetate salt of a TLR7 agonist 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine (formula I), crystalline form B of the trifluoroacetate salt, methods for preparing the trifluoroacetate salt and crystalline form B, and uses of the trifluoroacetate salt and crystalline form B.
(FR) La présente invention concerne un sel de trifluoroacétate d'un agoniste de TLR7, 2-butoxy-7-(4-(pyrrolidin-1-ylméthyl)benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine (formule I), la forme cristalline B du sel de trifluoroacétate, des procédés de préparation du sel de trifluoroacétate et de la forme cristalline B, et les utilisations du sel de trifluoroacétate et de la forme cristalline B.
(ZH) 本发明涉及一种TLR7激动剂2-丁氧基-7-(4-(吡咯烷-1-基甲基)苄基)-5H-吡咯并[3,2-d]嘧啶-4-胺(式I)的三氟乙酸盐、其晶型B、其制备方法和用途。
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)
Also published as:
UAa201809128AU2017214135CA3013521MYPI 2018702700SG11201806688QKR1020180104118
CN108602833EP3412674IL260981BR112018015878US20190031666IN201817032726
EA201891772ID2018/12857PH1/2018/501641