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

SDZ-64412

5-[4-[2-(3,4,5-三甲氧基苯基)乙基]苯基]-2,3-二氢咪唑并[2,1-a]异喹啉盐酸盐Chemical Name: 5-[4-[2-(3,4,5-Trimethoxyphenyl)ethyl]phenyl]-2,3-dihydroimidazo[2,1-a]isoquinoline hydrochloride
CAS No. 115622-31-6
项目整合开发状态: ...
参考文献标题:5-ARYL-2,3-DIHYDROIMIDAZO[2,1-a]ISOQUINOLINES: PLATELET-ACTIVATING FACTOR (PAF) RECEPTOR ANTAGONISTS
文献作者:Houlihan,W.J.
参考来源:Drugs Fut 1990,15(4),355

A-176120

5-[N-(2-乙氧基苯甲基)-N-[3-(4-甲基苯氧基)苯甲基]氨基甲酰]-1,2,4-苯三羧酸Chemical Name: 5-[N-(2-Ethoxybenzyl)-N-[3-(4-methylphenoxy)benzyl]carbamoyl]-1,2,4-benzenetricarboxylic acid
CAS No. 185049-54-1
项目整合开发状态: Precl...
参考文献标题:Benzene,pyridine,naphthalene or benzophenone derivs.as inhibitors of squalene synthetase and protein farnesyltransferase
文献作者:Sullivan,G.M.; Rosenberg,S.H.; Prasad,R.N.; O'Connor,S.J.; Donner,B.G.; Fakhoury,S.A.; Fung,K.L.; Stout,D.M.; Rockway,T.W.; Baker,W.R.; Shen,W.; Garvey,D.S.(Abbott Laboratories Inc.)
参考来源:WO 9634851

Gastrazole, JB-95008

5-[N-[5-[N-(环甲基)氨甲酰]-1H-苯并咪唑-6-酰羰基]-2-氟-L-苯基醛胺基]异邻苯二甲酸Chemical Name: 5-[N-[5-[N-(Cycloheptylmethyl)carbamoyl]-1H-benzimidazol-6-ylcarbonyl]-2-fluoro-L-phenylalanylamino]isophthalic acid
CAS No. 174...
参考文献标题:Gastrin and CCK receptor ligands
文献作者:Kalindjian,S.B.; Steel,K.I.M.; Pether,M.J.; Davies,J.M.R.; Low,C.M.R.; Hudson,M.L.; Buck,I.M.; McDonald,I.M.; Dunstone,D.J.; Tozer,M.J.(James Black Foundation Ltd.)
参考来源:EP 0720601; EP 0763026; GB 2290539; JP 1997502430; JP 1998504525; US 5795907; US 5912260; US 5919829; WO 9504720; WO 9532949

FO-152

5'-O-(L-valyl)-5-氟尿苷盐酸Chemical Name: 5'-O-L-Valyl-5-fluorouridine hydrochloride; 5-Fluoro-1-beta-D-(5'-O-L-valyl)ribofuranosyluracil hydrochloride
CAS No. 80667-13-6, 84998-30-1 (free base, mono-p-...
参考文献标题:Nucleoside derivs.,their preparation and their us
文献作者:Endo,T.; Sakai,K.; Chou,K.; Inamoto,Y.; Teshigawara,H.(Fuji Yakuhin Kogyo Co.,Ltd.)
参考来源:FR 2470774; US 4340728

Dimoxaprost, HR-260, Hoe-260

5-七烯酸,7-[(1R,2R,3R)-2-[(1E,3R)-5-乙氧基-3-羟基-4,4-二甲基-1-戊烯-1-盐]-3-羟基-5-氧环戊基]-,(5Z)-Chemical Name: 7-[(1RS,2RS,3RS)-2-[5-Ethoxy-3(R)-hydroxy-4,4-dimethyl-1(E)-pentenyl]-3-hydroxy-5-oxocyclopentyl]-5(Z)-hep...
参考文献标题:Dimoxaprost
文献作者:Beck,G.
参考来源:Drugs Fut 1987,12(12),1101

Ono-3708

5-七烯酸,7-[(1S,2S,3S,5R)-3-[[(2R)-2-环戊基-2-羟基乙酰]氨基]-6,6-二甲基双环[3.1.1]庚基-2-基]-,(5Z)-Chemical Name: 9alpha,11alpha-(Dimethylmethano)-13-aza-14-oxo-15beta-hydroxy-15-cyclopentyl-16,17,18,19,20-pentanor-11a-c...
参考文献标题:13-Aza-14-oxo-TXA2 analogues
文献作者:Kawasaki,A.; Miyake,H.; Okegawa,T.(Ono Pharmaceutical Co.,Ltd.)
参考来源:AU 8543495; EP 0171146; ES 8704880; ES 8705370; JP 1989151545; US 4792550

Eniluracil, GW-776, 5-EU, 776C85

5-乙炔基尿嘧啶Chemical Name: 5-Ethynyluracil; 5-Ethynyl-2,4(1H,3H)-pyrimidinedione
CAS No. 59989-18-3
项目整合开发状态: Phase III
项目研究机构: GlaxoSmithKline (Originator)
合成路线:This compound has been obtaine...
参考文献标题:Enzyme inactivators
文献作者:Spector,T.; Porter,D.J.T.; Rahim,S.G.(Glaxo Wellcome plc)
参考来源:EP 0539442; EP 0711555; JP 1994502619; JP 2000297076; WO 9201452

TA-606

5-乙酰-2-丙基-3-[2'-(1H-四唑-5-基)双苯-4-甲基]-4,5,6,7-四氢亚咪唑[4,5-c]吡啶-4-羧酸 3-戊基氧碳酰氧基甲酯盐酸Chemical Name: 5-Acetyl-2-propyl-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-4,5,6,7-tetrahydroimidazo[4,5-c]pyridine-4-ca...
参考文献标题:Imidazopyridine derivs.and process for preparing the same
文献作者:Sekine,Y.; Kawanishi,E.; Narita,H.; Hashimoto,Y.; Mizobe,M.(Tanabe Seiyaku Co.,Ltd.)
参考来源:CA 2146802; EP 0682023; JP 1996003162; US 5753672

KDI-792, FR-121070, FK-070

5-己基酸,6-[(2S,4R)-4-[[[(4-氯苯基)磺酰]氨基]-1-(3-吡啶甲基)-2-吡咯利二基]-盐酸盐(1:1),(5Z)-Chemical Name: 6-[4(R)-(4-Chlorophenylsulfonamido)-1-(3-pyridylmethyl)pyrrolidin-2(S)-yl]-5(Z)-hexenoic acid monohydrochloride; (2...
参考文献标题:Pyrrolidine derivs
文献作者:Setoi,H.; Sawada,A.; Tanaka,H.; Hashimoto,M.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:AU 8943753; EP 0367130; JP 1990152960; US 5130323; US 5264453; US 5514701

GCC-AP0341

5-氨基-3-(4-氯苯基)-N-甲基-1,2,4-三唑-1-硫代甲酰胺Chemical Name: 5-Amino-3-(4-chlorophenyl)-N-methyl-1,2,4-triazole-1-carbothioamide
CAS No. 168893-29-6
项目整合开发状态: Preclinical
项目研究机构: Mitsubishi Pharma (Ori...
参考文献标题:Triazole derivs.and pharmaceutical use thereof
文献作者:Akahoshi,F.; Okada,T.; Takeda,S.; Naito,Y.; Fukaya,C.; Kuwahara,S.; Kajii,M.; Nishimura,H.; Sugiura,M.(Welfide Corporation)
参考来源:EP 0710654; JP 1995082270; JP 1995097321; JP 1995101942; US 5750545; WO 9503286