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1. (WO2017092083) DPP-4 INHIBITOR COMPOUND, POLYMER AND PREPARATION METHOD AND USE OF SAME
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/092083 International Application No.: PCT/CN2015/098043
Publication Date: 08.06.2017 International Filing Date: 21.12.2015
IPC:
C07D 519/00 (2006.01) ,C07D 401/14 (2006.01) ,C07D 207/16 (2006.01) ,C07D 209/52 (2006.01) ,C07D 403/14 (2006.01) ,C07K 5/062 (2006.01) ,A61K 31/4985 (2006.01) ,A61K 31/506 (2006.01) ,A61K 38/05 (2006.01) ,A61P 3/04 (2006.01) ,A61P 3/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
519
Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04
having no double bonds between ring members or between ring members and non-ring members
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
16
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
52
condensed with a ring other than six-membered
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
06
Dipeptides
062
the side chain of the first amino acid being acyclic, e.g. Gly, Ala
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
4985
Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
506
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
04
Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
05
Dipeptides
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
04
Anorexiants; Antiobesity agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
08
for glucose homeostasis
10
for hyperglycaemia, e.g. antidiabetics
Applicants:
杭州阿诺生物医药科技股份有限公司 ADLAI NORTYE BIOPHARMA CO., LTD. [CN/CN]; 中国浙江省杭州市 杭州经济技术开发区6号大街452号 No.452, 6th Street, Hangzhou Eco. & Tech. Development Zone Hangzhou, Zhejiang 310018, CN
Inventors:
张晓 ZHANG, Xiao; CN
厉保秋 LI, Baoqiu; CN
周俊 ZHOU, Jun; CN
沈柯 SHEN, Ke; CN
杨东晖 YANG, Donghui; CN
路杨 LU, Yang; CN
Agent:
北京格旭知识产权代理事务所(普通合伙) GEXU INTELLECTUAL PROPERTY LAW FIRM; 中国北京市海淀区北三环西路甲18号院2号楼(中坤广场E座)7层722-1室 Rm. 722-1, Building2 (EZone, Zhongkun Plaza), No. A18 North 3rd Ring West Road Haidian District, Beijing 100098, CN
Priority Data:
201510866369.501.12.2015CN
Title (EN) DPP-4 INHIBITOR COMPOUND, POLYMER AND PREPARATION METHOD AND USE OF SAME
(FR) COMPOSÉ INHIBITEUR DE DPP-4, POLYMÈRE, PROCÉDÉ DE PRÉPARATION ET UTILISATION
(ZH) DPP-4抑制剂化合物、聚合物及其制备方法和应用
Abstract:
(EN) Disclosed are a DPP-4 inhibitor compound, a polymer and a preparation method and use. The structure of said compound is X-R1-R2-Y, X and Y respectively being a group formed of a DPP-4 inhibitor or a DPP-4 inhibitor analogue containing an amino or imino group,, or being a group formed of a pharmaceutically acceptable salt or an optical isomer of the above mentioned DPP-4 inhibitor or DPP-4 inhibitor analogue containing an amino or imino group; and R1 and R2 respectively being a peptide chain fragment containing 1-6 natural or non-natural amino acid(s), or being a mercaptocarboxylic acid compound group or being a mercaptocarboxylic acid compound modified peptide chain fragment containing 1-6 natural or non-natural amino acid(s). Said DPP-4 inhibitor compound and polymer have an action curve of longer time and a lower clearance rate, and at the same time prolong the half-life period of the GLP-1 in vivo.
(FR) L'invention concerne un composé inhibiteur de DPP-4, un polymère, un procédé de préparation et une utilisation. La structure dudit composé est X-R1-R2-Y, dans laquelle X et Y représentent respectivement un groupe formé d'un inhibiteur de DPP-4 ou d'un analogue d'inhibiteur de DPP-4 contenant un groupe amino ou imino, ou ils représentent un groupe formé d'un sel pharmaceutiquement acceptable ou d'un isomère optique de l'inhibiteur de DPP-4 ou de l'analogue d'inhibiteur de DPP-4 susmentionnés contenant un groupe amino ou imino; et R1 et R2 représentent respectivement un fragment de chaîne peptidique contenant de 1 à 6 acides aminés naturels ou non naturels, ou ils représentent un groupe de composé acide mercaptocarboxylique ou un fragment de chaîne peptidique contenant de 1 à 6 acides aminés naturels ou non naturels modifié par un composé acide mercaptocarboxylique. Ledit composé inhibiteur de DPP-4 et le polymère ont une courbe d'action de durée plus longue et une vitesse d'élimination inférieure, et en même temps ils prolongent la période de demi-vie du GLP-1 in vivo.
(ZH) 公开了一种DPP-4抑制剂化合物、聚合物及制备方法和应用。所述化合物结构为X-R1-R2-Y,X和Y分别为含有氨基或亚氨基的DPP-4抑制剂或者DPP-4抑制剂类似物形成的基团;或者为前述含有氨基或亚氨基的DPP-4抑制剂或者DPP-4抑制剂类似物药学上可以接受的盐或光学异构体形成的基团;R1和R2分别为含有1-6个天然或非天然氨基酸的肽链片段、或者为巯基羧酸化合物基团、或者为经巯基羧酸化合物修饰的含有1-6个天然或非天然氨基酸的肽链片段。所述DPP-4抑制剂化合物和聚合物具有更长时间的作用曲线和更低的清除率,同时延长了GLP-1在体内的半衰期。
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, 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, KN, KP, KR, 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)