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1. (WO2019001551) CRYSTALLINE FORM OF FREE BASE OF IMIDAZO-ISOINDOLE DERIVATIVE AND PREPARATION METHOD THEREFOR
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Pub. No.: WO/2019/001551 International Application No.: PCT/CN2018/093533
Publication Date: 03.01.2019 International Filing Date: 29.06.2018
IPC:
C07D 487/04 (2006.01) ,A61P 25/24 (2006.01) ,A61K 31/454 (2006.01) ,A61P 37/06 (2006.01) ,A61P 35/00 (2006.01) ,A61P 25/22 (2006.01) ,A61P 35/02 (2006.01) ,A61P 25/00 (2006.01) ,A61P 35/04 (2006.01) ,A61P 31/18 (2006.01) ,A61P 25/28 (2006.01) ,A61P 27/12 (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
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
24
Antidepressants
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
454
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
02
Immunomodulators
06
Immunosuppressants, e.g. drugs for graft rejection
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
22
Anxiolytics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
02
specific for leukemia
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
04
specific for metastasis
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
14
for RNA viruses
18
for HIV
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27
Drugs for disorders of the senses
02
Ophthalmic agents
12
for cataracts
Applicants:
江苏恒瑞医药股份有限公司 JIANGSU HENGRUI MEDICINE CO., LTD. [CN/CN]; 中国江苏省连云港市 经济技术开发区昆仑山路7号 No. 7 Kunlunshan Road Economic and Technological Development Zone Lianyungang, Jiangsu 222047, CN
上海恒瑞医药有限公司 SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD. [CN/CN]; 中国上海市 闵行区文井路279号 No. 279 Wenjing Road, Minhang District Shanghai 200245, CN
Inventors:
曹笑立 CAO, Xiaoli; CN
尤凌峰 YOU, Lingfeng; CN
肖昌琴 XIAO, Changqin; CN
杜振兴 DU, Zhenxing; CN
王立坤 WANG, Likun; CN
Agent:
北京戈程知识产权代理有限公司 GE CHENG & CO., LTD.; 中国北京市 东城区东长安街1号东方广场东三办公楼19层 Level 19, Tower E3, The Towers, Oriental Plaza No. 1, East Chang An Avenue, Dongcheng District Beijing 100738, CN
Priority Data:
201710520144.330.06.2017CN
Title (EN) CRYSTALLINE FORM OF FREE BASE OF IMIDAZO-ISOINDOLE DERIVATIVE AND PREPARATION METHOD THEREFOR
(FR) FORME CRISTALLINE DE BASE LIBRE DE DÉRIVÉ D'IMIDAZO-ISOINDOLE ET SON PROCÉDÉ DE PRÉPARATION
(ZH) 一种咪唑并异吲哚类衍生物游离碱的晶型及其制备方法
Abstract:
(EN) Provided are a crystalline form G of a free base of an imidazo-isoindole derivative and a preparation method therefor. The chemical structure of the compound is shown in formula (I), and the chemical name thereof is (S)-2-(4-(4-(4-(6-fluoro-5H-imidazo[5,1-a] isoindole-5-yl) piperidine-1-yl) phenyl)-1H-pyrazol-1-yl) ethanol. Provided are the application of the crystalline form G of the compound in a pharmaceutical composition and the pharmaceutical use of the crystalline form G and the composition in the preparation of a medicine for treating diseases with pathological characteristics of tryptophan metabolic pathway mediated by IDO (indoleamine-pyrrole-2,3-dioxygenase). The crystalline form G of the compound has good stability, and the crystallization solvent that is used has low toxicity and residue and may be used well in clinical treatment.
(FR) L'invention concerne une forme cristalline G d'une base libre d'un dérivé d'imidazo-isoindole et son procédé de préparation. La structure chimique du composé est représentée dans la formule (I), et son nom chimique est représenté par la formule (I) (S)-2-(4- (4- (4- (6-fluoro -5 H-imidazo [5,1-a] isoindole-5-yl) pipéridine-1-yl) phényl) -1 H-pyrazol-1-yl) éthanol. L'invention concerne l'application de la forme cristalline G du composé dans une composition pharmaceutique et l'utilisation pharmaceutique de la forme cristalline G et de la composition dans la préparation d'un médicament pour le traitement de maladies avec des caractéristiques pathologiques de la voie métabolique du tryptophane médiée par IDO (indoléamine-pyrrole -2,3-dioxygénase). La forme cristalline G du composé présente une bonne stabilité, et le solvant de cristallisation qui est utilisé présente une faible toxicité et un faible résidu et peut être utilisé de manière satisfaisante dans un traitement clinique.
(ZH) 提供一种咪唑并异吲哚类衍生物游离碱的G晶型及其制备方法,所述化合物的化学结构如式(I)所示,化学名称为(S)-2-(4-(4-(4-(6-氟-5H-咪唑并[5,1-a]异吲哚-5-基)哌啶-1-基)苯基)-1H-吡唑-1-基)乙醇。提供所述化合物的G晶型在药物组合物中的应用以及所述G晶型和组合物在制备治疗具有IDO(吲哚胺-吡咯-2,3-双加氧酶)介导的色氨酸代谢途径病理学特征疾病中的药物用途。所述化合物的G晶型具备良好的稳定性,并且所用结晶溶剂低毒低残留,可更好地用于临床治疗。
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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, JO, 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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)