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

Z-321

Chemical Name: 1-[N-(2-Indanylacetyl)-4-thia-L-prolyl]pyrrolidine; 1-[3-(2-Indanylacetyl)thiazolidin-4(R)-ylcarbonyl]pyrrolidine
CAS No. 130849-58-0
项目整合开发状态: Phase I
项目研究机构: Zeria (Originato...
参考文献标题:Condensed benzene deriv.
文献作者:Aotsuka,T.; Torizuka,M.; Soeda,M.; Ogura,K.; Tanaka,Y.; Kato,H.; Nakata,N.; Miura,N.; Morita,H.(Zeria Pharmaceutical Co.,Ltd.)
参考来源:AU 8945914; EP 0372484; JP 1990262557; US 5028604

KF-15570

Chemical Name: 5-Butyl-1-methyl-4,5-dihydro-1H-imidazo[4,5-c]quinolin-4-one
CAS No. 133305-92-7
项目整合开发状态: Preclinical
项目研究机构: Kyowa Hakko (Originator)
合成路线:KF15570 is prepared as follows:1...
参考文献标题:Imidazoquinoline derivs
文献作者:Suzuki,F.; Kuroda,T.; Nakazato,Y.; Manabe,H.; Ohmori,K.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0386722; JP 1991264585; US 4994468

TA-510

Chemical Name: (?-8alpha-(3,4-Dimethoxyphenyl)-4,4aalpha,5,7,7aalpha,8-hexahydrobenzo[1,2-b:4,5-c']difuran-4,7-dione
CAS No. 133118-88-4 (diastereomer), 133163-96-9 (diastereomer)
项目整合开发状态: Clin...
参考文献标题:Biphenyl derivs.
文献作者:Iwasaki,T.; Sugiura,M.; Matsuoka,Y.; Matsumoto,M.; Kitamura,K.(Tanabe Seiyaku Co.,Ltd.)
参考来源:EP 0386778; JP 1990235884; US 5066669

RP-66681

Chemical Name: (+)-N-[3-[alpha-[(Z)-1-Methyl-4-piperidinyloxyimino]benzyl]phenyl]-3alpha-(3-pyridyl)-1H,3H-pyrrolo[1,2-c]thiazole-7-carboxamide
CAS No. 132710-24-8
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:RP 66681B,a water-soluble pyrrolothiazole derivative with potent and selective PAF receptor antagonist properties
文献作者:Floch,A.; Soler,F.; Cavero,I.; Lav? D.; Robaut,C.
参考来源:Drugs Fut 1992,17(3),207

RP-64406

Chemical Name: 3-[2-(Methylsulfinyl)ethyl]-6-(trifluoromethoxy)benzothiazolin-2-imine; 2-Imino-3-[2-(methylsulfinyl)ethyl]-6-(trifluoromethoxy)benzothiazoline
CAS No. 130569-53-8 (monoHCl)
项目整合开...
参考文献标题:Riluzole series.Synthesis and in vivo "antiglutamate" activity of 6-substituted-2-benzothiazolamines and 3-substituted-2-imino-benzothiazolines
文献作者:Jimonet,P.; Audiau,F.; Barreau,M.; Blanchard,J.C.; Boireau,A.; Bour,Y.; Coleno,M.A.; Doble,A.; Doerflinger,G.; Huu,C.D.; Donat,M.H.; Duchesne,J.M.; Ganil,P.; Gueremy,C.; Honor,E.; Just,B.; Kerphirique,R.; Gontier,S.; et al.
参考来源:J Med Chem 1999,42(15),2828

YM-264

Chemical Name: 1-(3-Methyl-3-phenylbutyl)-4-[2-(3-pyridyl)thiazolidin-4(R)-ylcarbonyl]piperazine fumarate
CAS No. 126911-71-5 (free base)
项目整合开发状态: Phase II
项目研究机构: Yamanouchi (Originator) 参考文献标题:Saturated heterocyclic carboxamide derivs.
文献作者:Mase,T.; Hara,H.; Nagaoka,H.; Takahasi,T.; Suzuki,T.; Tomioka,K.; Yamada,T.(Yamanouchi Pharmaceutical Co.,Ltd.)
参考来源:AU 8812080; EP 0279681; JP 1988208582; US 4987132

DuP-860

Chemical Name: 3-(2-Chlorophenyl)-2-(4-chlorophenyl)-1-(1H-1,2,4-triazol-1-yl)-3-buten-2-ol methanesulfonate; alpha-(4-Chlorophenyl)-alpha-[1-(2-chlorophenyl)ethenyl]-1H-1,2,4-triazole-1-ethanol metha...
参考文献标题:Antifungal carbinols
文献作者:Cuomo,J.; Greenberg,R.S.; Olson,R.E.(DuPont Pharmaceuticals Co.)
参考来源:EP 0251086; JP 1988060975

PD-123319

Chemical Name: 1-[4-(Dimethylamino)-3-methylbenzyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6(S)-carboxylic acid
CAS No. 114785-14-7 (racemate), 114785-90-9 (R-isomer)
项目...
参考文献标题:4,5,6,7-Tetrahydro-1H-imidazo[4,5-c]pyridine derivs.and analogs having antihypertensive activity
文献作者:Blankley,C.J.; Hodges,J.C.; Kiely,J.S.; Klutchko,S.R.(Pfizer Inc.)
参考来源:EP 0245637; JP 1987240683; JP 1996208652; US 4812462; US 4816463

Ioxipride, NCQ-298

Chemical Name: (-)-(S)-N-(1-Ethyl-2-pyrrolidinylmethyl)-2-hydroxy-3-iodo-5,6-dimethoxybenzamide
CAS No. 124929-10-8 ([123I]-labeled), 124929-13-1 ([125I]-labeled)
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Potential antipsychotic agents.5.Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds
文献作者:H鰃berg,T.; et al.
参考来源:J Med Chem 1990,331155-63

Ibrolipim, OPF-009, NO-1886

Chemical Name: N-(4-Bromo-2-cyanophenyl)-4-(diethoxyphosphorylmethyl)benzamide; 4-[N-(4-Bromo-2-cyanophenyl)carbamoyl]benzylphosphonic acid diethyl ester
CAS No. 133208-93-2
项目整合开发状态: Phase II 参考文献标题:Carboxamide derivs
文献作者:Tsutsumi,K.; Uesaka,E.; Shinomiya,K.; Tsuda,Y.; Shoji,Y.; Shima,A.(Otsuka Pharmaceutical Co.,Ltd.)
参考来源:AU 9056011; EP 0402033; JP 1991068592