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

PD-166866

FGFR1酪氨酸激酶抑制剂(PD-166866)Chemical Name: N-[2-Amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(tert-butyl)urea
CAS No. 192705-79-6
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Orig...
参考文献标题:Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors
文献作者:Hamby,J.M.; Connolly,C.J.C.; Schroeder,M.C.; Winters,R.T.; Showalter,H.D.; Panek,R.L.; Major,T.C.; Olsewski,B.; Ryan,M.J.; Dahring,T.K.; Lu,G.H.; Keiser,J.A.; Amar,A.M.; Shen,C.; Kraker,A.J.; Slintak,V.; Nelson,J.M.; Fry,D.W.; et al.
参考来源:J Med Chem 1997,40(15),2296

GW-627368X

GW627368X抑制剂Chemical Name: N-[2-[4-(4,9-Diethoxy-1-oxo-2,3-dihydro-1H-benzo[f]isoindol-2-yl)phenyl]acetyl]benzenesulfonamide; 2-[4-(4,9-Diethoxy-1-oxo-2,3-dihydro-1H-benzo[f]isoindol-2-yl)phenyl]-N-(p...
参考文献标题:Benzo(f)isoindol derivs.and their use as EP4 receptor ligands
文献作者:Frye,S.V.; Giblin,G.M.P.; Roomans,S.(GlaxoSmithKline plc)
参考来源:WO 0250033

HA-1004

HA-1004二盐酸盐Chemical Name: N-(2-Guanidinoethyl)-5-isoquinolinesulfonamide hydrochloride
CAS No. 91742-10-8
项目整合开发状态: Phase II
项目研究机构: Asahi Kasei (Originator), Mie University (Originator)
合...
参考文献标题:HA-1004
文献作者:Koch,H.; Castar,J.
参考来源:Drugs Fut 1985,10(10),815

ICI-199441

ICI-199,441盐酸盐Chemical Name: 2-(3,4-Dichlorophenyl)-N-methyl-N-[1(S)-phenyl-2-(1-pyrrolidinyl)ethyl]acetamide
CAS No. 115199-84-3
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路...
参考文献标题:2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted-ethyl]-acetamides: The use of conformational analysis in the development of a novel series of potent opioid kappa agonists
文献作者:Costello,G.F.; et al.
参考来源:J Med Chem 1991,34(1),181-9

KNK-437

KNK437(热激蛋白抑制剂I)Chemical Name: 3-[(E)-1,3-Benzodioxol-5-ylmethylene]-2-oxopyrrolidine-1-carbaldehyde
CAS No. 218924-25-5
项目整合开发状态: Preclinical
项目研究机构: Kaneka (Originator)
合成路线:Condensation...
参考文献标题:Heat shock factor activity inhibitors
文献作者:Fuse,Y.; Kitahara,M.; Yamamoto,K.; Yokota,S.; Morikawa,S.(Kaneka Corp.)
参考来源:EP 0995745; WO 9900382

TAX-109, 109881, XRP-9881, RPR-109881A

Larotaxel水合物莱龙泰素 Chemical Name: (2aR,3aR,4aR,6R,9S,11S,12S,12aR,12bS)-6,12b-Diacetoxy-9-[3(S)-(tert-butoxycarbonylamino)-2(R)-hydroxy-3-phenylpropionyloxy]-12-benzoyloxy-11-hydroxy-8,13,13-trimethyl-...
参考文献标题:7,8-Cyclopropataxones
文献作者:Chen,S.-H.; Farina,V.(Bristol-Myers Squibb Co.)
参考来源:CA 2099211; EP 0577083; JP 1994179665; JP 1994179666; JP 2001199974; US 5254580

XP-280(as besilate), XV-459

L-丙氨酸,3-[[2-[(5R)-3-[4-(氨基酰氨基甲基)苯基]-4,5-二氢-5-异氧基]氨基]-N-(丁氧羰基)-Chemical Name: 3-[3-(4-Amidinophenyl)-4,5-dihydroisoxazol-5(R)-ylacetamido]-2(S)-(butoxycarbonylamino)propionic acid; 3-[2-[3-(4-Amidinoph...
参考文献标题:Novel isoxazoline and isoxazole fibrinogen receptor antagonists
文献作者:Wityak,J.; Xue,C.-B.; Sielecki-Dzurdz,T.M.; Olson,R.E.; Degrado,W.F.; Cain,G.A.(DuPont Pharmaceuticals Co.)
参考来源:EP 0730590; EP 0832076; JP 1997505590; JP 1999504651; US 5849736; WO 9514683; WO 9638426

L-738167

L-丙氨酸,N-[(4-甲基苯基)磺酰]-3-[[[[5,6,7,8-四氢-4-氧基-5-[2-(4-哌啶基)乙基]-4H-吡拉唑[1,5-a][1,4]二氮俬-2-酰基]氨基]-Chemical Name: 2(S)-(4-Methylphenylsulfonamido)-3-[4-oxo-5-[2-(piperidin-4-yl)ethyl]-5,6,7,8-tetrahydro-4H-pyr...
参考文献标题:Synthesis of a C-11-labelled nitrated 1,4-dihydroquinoxaline-2,3-dione,the NMDA glycine receptor antagonist ACEA 1021 (Licostinel)
文献作者:Thorell,J.O.; et al.
参考来源:J Label Compd Radiopharm 1998,41(4),345-353

ZD-0892

L-丙烯酰胺,N-(4-甲氧基苯甲酰)-L-戊酸-N-[(1S)-3,3,3-三氟-1-(1-甲基乙基)-2-氧丙基]-Chemical Name: (4-Methoxybenzoyl-L-valyl-L-prolyl-L-valyl)trifluoromethane; N-(4-Methoxybenzoyl)-L-valyl-N-[3,3,3-trifluoro-1(S)-isopropyl-2...
参考文献标题:Diastereomeric pure trifluoromethyl ketone peptide
文献作者:Pegg,S.J.; Sependa,G.J.; Davies,E.P.; Veale,C.A.(AstraZeneca plc)
参考来源:EP 0743953; JP 1997508902; US 5739157; US 6037363; WO 9521855

RX-77368

L-焦谷氨酰-L-组氨酰-3,3-二甲基脯氨酰胺Chemical Name: L-Pyroglutamyl-L-Histidyl-L-3,3-dimethylprolinamide; 5-Oxo-L-prolyl-L-histidyl-3,3-dimethyl-L-prolinamide
CAS No. 76820-40-1
项目整合开发状态: Phase III
项目研究机构:...
参考文献标题:RX-77,368
文献作者:Castar,J.; Blancafort,P.; Serradell,M.N.
参考来源:Drugs Fut 1982,7(3),167