项目整合精选

聚焦新型临床类新产品的整合与转化. 在创新药研发领域，传统的“单一产品、单打独斗”模式正在被一种更系统化的“项目整合”思维所取代。项目整合的核心，在于将散落在研发早期、中期的创新资产，通过资金、临床资源、产业生态等多维度要素的有机组合，实现从“科学发现”到“临床价值”，再到“商业成功”的跨越。研发与商业的战略整合：从“资产思维”到“组合思维”它要求我们超越单个分子的视野，拥抱一个由技术创新、临床需求、资本支持和商业洞察共同构成的复杂网络。在这个网络中，成功的标准不再是单一的“获批上市”，而是能否通过高效的整合，将科学上的突破，转化为临床上真正可及、商业上可持续、能够惠及患者的解决方案。近年来，药物发现已从传统的小分子化药拓展至更多元的分子类型，这些新型API在项目整合中呈现出独特的开发范式，项目整合的核心挑战在于递送系统的设计与肝外靶向能力的突破。
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项目整合精选

Cloturin, VUFB-15686

S-(7H-嘌呤-6-基)(2-氯乙基氨基)硫代甲酸酯Chemical Name: N-(2-Chloroethyl)thiocarbamic acid 6-purinyl ester; 6-[N-(2-Chloroethyl)carbamoyl]thiopurine; (2-Chloroethyl)carbamothioic acid S-1H-purin-6-yl ester
CAS N...
参考文献标题:6-Purinyl N-(2-chloroethyl)carbamate and thiocarbamate,a process for their preparation and use thereof.CS 249576
文献作者:Cerny,A.; Krepelka,J.I.; Melka,M.; Molko,M.; Pokorn? S.; Reichov? R.; Kejhov? I.; Beitov? M.; Grimov? J.(SPOFA - United Pharmaceutical Works)
参考来源:EP 0186454; JP 1986186382; US 4720497

SCH-79797

SCH 79797二盐酸盐Chemical Name: N3-Cyclopropyl-7-(4-isopropylbenzyl)-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine
CAS No. 245520-69-8
项目整合开发状态: Biological Testing
项目研究机构: Schering-Plough (Originator)...
参考文献标题:Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists
文献作者:Ahn,H.-S.; Arik,L.; Boykow,G.; Burnett,D.A.; Caplen,M.A.; Czarniecki,M.; Domalski,M.S.; Foster,C.; Manna,M.; Stamford,A.W.; Wu,Y.
参考来源:Bioorg Med Chem Lett 1999,9(14),2073

SK&F-89976A

SKF89976A盐酸盐 1-(4,4-二苯基-3-丁烯-1-基)-3-哌啶羧酸 Chemical Name: N-(4,4-Diphenyl-3-butenyl)nipecotic acid hydrochloride; 4-(3-Carboxypiperidine)-1,1-diphenyl-1-butene hydrochloride; 1-(4,4-Diphenyl-3-butenyl)-...
参考文献标题:SK&F-89976-A
文献作者:Lcher,W.
参考来源:Drugs Fut 1986,11(1),36

Lintitript, SR-27897

SR 27897(Lintitript),竞争性非肽CCK 1受体拮抗剂Chemical Name: 1-(Carboxymethyl)-N-[4-(2-chlorophenyl)thiazol-2-yl]indole-2-carboxamide; 2-[[N-[4-(2-Chlorophenyl)-2-thiazolyl]amino]carbonyl]-1H-indole-1-acetic ac...
参考文献标题:Heterocyclic derivs.of acylaminothiazole,their preparation and pharmaceutical compsns.containing them
文献作者:Bras,J.-P.; Frehel,D.; Gully,D.; Valette,G.(Sanofi-Synthabo )
参考来源:EP 0432040; FR 2655344; FR 2661677; JP 1991279374; JP 1998130147; US 5189049

ENMD-0995, S-3APG

S-泊马度胺杂质泊马度胺 Chemical Name: (-)-4-Amino-2-[2,6-dioxopiperidin-3(S)-yl]-1,2-dihydroisoindole-1,3-dione
CAS No. 202271-89-4, 19171-19-8 (undefined isomer)
项目整合开发状态: Phase I
项目研究机构: Children's ...
参考文献标题:Substd.2-(2,6-dioxopiperidin-3-yl)-phthalimides and 1-oxoisoindolines and method of reducing TNFalpha levels
文献作者:Stirling,D.I.; Chen,R.S.-C.; Muller,G.W.(Celgene Corp.)
参考来源:EP 0925294; EP 0984955; US 5635517; WO 9803502; WO 9854170

BMS-247615, TAS-103

TAS-103二盐酸盐 6-[[2-(二甲基氨基)乙基]氨基]-3-羟基-7H-茚并[2,1-C]喹啉-7-酮 Chemical Name: 6-[2-(Dimethylamino)ethylamino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one dihydrochloride
CAS No. 174634-09-4, 174634-08-3 (fre...
参考文献标题:Novel fused indan deriv.and pharmaceutically acceptable salt
文献作者:Okazaki,S.; Asao,T.; Wakida,M.; Ishida,K.; Washinosu,M.; Utsugi,T.; Yamada,Y.(Taiho Pharmaceutical Co.,Ltd.)
参考来源:EP 0713870; US 5710162; US 5733918; WO 9532187

TOP-53

TOP-53双盐酸盐 2’-O-没食子酰基金丝桃甙 Chemical Name: [5R-(5alpha,5abeta,8aalpha,9beta)]-9-[2-[N-[2-(Dimethylamino)ethyl]-N-methylamino]ethyl]-5-(4-hydroxy-3,5-dimethoxyphenyl)-5,5a,6,8,8a,9-hexahydrofuro[3',4':6,...
参考文献标题:4-Desoxy-4-epipodophyllotoxin deriv.or pharmaceutically aceptable salt thereof
文献作者:Terada,T.; Fujimoto,K.; Nomura,M.; Yamashita,J.; Takeda,S.; Kobunai,T.; Yamaguchi,H.; Wierzba,K.(Taiho Pharmaceutical Co.,Ltd.)
参考来源:EP 0522173; JP 1993503298; WO 9212982

Y-27632

Y-27632二盐酸盐Chemical Name: (+)-trans-4-[1(R)-Aminoethyl]-N-(4-pyridyl)cyclohexane-1-carboxamide
CAS No. 146986-50-7, 138381-45-0 (undefined isomer, diHCl salt)
项目整合开发状态: Preclinical
项目研究机构: Mi...
参考文献标题:Trans-4-amino(alkyl)-1-pyridylcarbamoylcyclohexane cpds.and pharmaceutical use thereof
文献作者:Muro,T.; Seki,T.; Abe,M.; Inui,J.; Sato,H.(Mitsubishi Pharma Corp.)
参考来源:EP 0370498; JP 1990509475; US 4997834; WO 9005723

YM-90K, YM-900(free base)

YM 90K盐酸盐 2,3-喹诺沙林地酮,1,4-二氢-6-(1H-吡达唑-1-基)-7-硝基- Chemical Name: 6-(1-Imidazolyl)-7-nitroquinoxaline-2,3-(1H,4H)-dione monohydrochloride
CAS No. 154164-30-4, 143151-35-3 (free base), 157971-78-3 (YM...
参考文献标题:Imidazolylquinoxaline-2,3-diones: Novel and potent antagonists of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) excitatory amino acid receptor
文献作者:Sakamoto,S.; Ohmori,J.; Shimizu-Sasamata,M.; et al.
参考来源:12th Int Symp Med Chem (Sept 13-17,Basel) 1992,Abst P-022.A.

SU-11654

Z)-5-(5-氟-2-氧代-2,3-二氢-1H-吲哚-3-亚基甲基)-2,4-二甲基-N-[2-(1-吡咯烷基)乙基]-1H-吡咯-3-甲酰胺Chemical Name: (Z)-5-(5-Fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidenemethyl)-2,4-dimethyl-N-[2-(1-pyrrolidinyl)ethyl]-1H-pyrrole-3...
参考文献标题:Pyrrole substd.2-indolinone protein kinase inhibitors
文献作者:Wei,C.C.; Miller,T.; Tang,P.C.; Nematalla,A.S.; Li,X.; Liang,C.; Shirazian,S.; Su,L.; Vojkovsky,T.(Sugen,Inc.)
参考来源:EP 1255752; US 2002156292; US 6573293; WO 0160814