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

Adatanserin hydrochloride, WAY-SEB-324, SEB-324, Wy-50324

阿达色林 Chemical Name: N-[2-[4-(2-Pyrimidinyl)piperazin-1-yl]ethyl]adamantane-1-carboxamide hydrochloride; N-[2-[4-(2-Pyrimidinyl)-1-piperazinyl]ethyl]tricyclo[3.3.1.1(3,7)]decane-1-carboxamide hydrochl...
参考文献标题:Aryl- and heteroaryl piperazinyl carboxamides having CNS activity
文献作者:Abou-Gharbia,M.A.-M.; Yardley,J.P.; Childers,W.E.Jr.(American Home Products Corp.)
参考来源:AU 8935025; EP 0343961; JP 1990015059

Anastrozole, ZD-1033, ICI-D1033, Arimidex

阿那曲唑Chemical Name: 2,2'-[5-(1H-1,2,4-Triazol-1-ylmethyl)-1,3-phenylene]bis(2-methylpropionitrile)
CAS No. 120511-73-1
项目整合开发状态: Launched-1995
项目研究机构: AstraZeneca (Originator), Cancer Researc...
参考文献标题:(Substd.aralkyl)heterocyclic cpds
文献作者:Edwards,P.N.; Large,M.W.(AstraZeneca plc)
参考来源:AU 8816911; EP 0296749; JP 1989019067; US 4935437

Triptonide

雷公藤内酯酮Chemical Name: (3bS,4aS,5aS,6aS,7aS,7bS,8aS,8bS)-6a-Isopropyl-8b-methyl-3b,4,4a,7a,7b,8b,9,10-octahydrotrisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1,6(3H,6aH)-dione
CAS No. 38647-11-9 参考文献标题:Enantioselective total synthesis of (-)-triptolide,(-)-triptonide,(+)-triptophenolide,and (+)-triptoquinomide
文献作者:Yang,D.; Ye,X.Y.; Xu,M.
参考来源:J Org Chem 2000,65(7),2208

Strontium ranelate, Ranelic acid distrontium salt, FK-481, S-12911-2, S-12911, Osseor, Protelos, Protos

雷尼酸锶 5-[二(羧甲基)氨基]-2-羧基-4-氰基-3-噻吩乙酸 Chemical Name: 2-[2-Carboxy-4-cyano-5-[N,N-di(carboxymethyl)amino]thiophen-3-yl]acetic acid distrontium salt
CAS No. 135459-87-9, 135459-90-4 (free acid)
项目整合...
参考文献标题:Bivalent metal salts of 2-N,N-di(carboxymethyl)amino,3-cyano,4-carboxymethyl,5-carboxy-thiophene-acid,process for their preparation and pharmaceutical compsns.containing them
文献作者:Wierzbicki,M.; Bonnet,J.; Brisset,M.; Tsouderos,Y.(ADIR et Cie.)
参考来源:AU 9162033; EP 0415850; FR 2651497; JP 1991169876; US 5128367

Ramelteon, TAK-375

雷美替胺 (R)-雷美替胺 N-[2-(1,6,7,8-四氢-2H-茚并[5,4-b]呋喃-8-基)乙基]-丙酰胺Chemical Name: (-)-(S)-N-[2-(2,6,7,8-Tetrahydro-1H-indeno[5,4-b]furan-8-yl)ethyl]propionamide
CAS No. 196597-26-9, 196597-27-0 (R-isomer), ...
参考文献标题:Tricyclic cpds.,their production and use
文献作者:Ohkawa,S.; Uchikawa,O.; Fukatsu,K.; Miyamoto,M.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0885210; JP 1998287665; JP 1999152281; WO 9732871

Fezolamine fumarate, Win-41528-2

非唑拉明 Chemical Name: N,N-Dimethyl-3,4-diphenyl-1H-pyrazole-1-propanamine (E)-2-butenedioate (1:1); 1-[3-(Dimethylamino)propyl]-3,4-diphenylpyrazole fumarate (1:1)
CAS No. 80410-37-3, 80410-36-2 (fr...
参考文献标题:1-Amino-lower-alkyl-3,4-diphenyl-1H-pyrazoles
文献作者:Bailey,D.M.(Sanofi-Synthabo)
参考来源:US 4182895

Fenaperone, MD-67332

非那哌隆Chemical Name: 4-[4-(4-Fluorophenyl)-4-oxobutyl]piperazine-1-carboxylic acid cyclohexyl ester
CAS No. 54063-38-6
项目整合开发状态: Not Determined
项目研究机构:
合成路线:By condensation of p-fluoro-gam...
参考文献标题:
文献作者:Fauran,C.; et al.
参考来源:DE 1907244; FR 1581468; FR M7162; GB 1186495; US 3658821

Cisplatin, DDP-H, NSC-119875, CPDC, CACP, CDDP, Cis-DDP, Platinex, Briplatin, Randa, Platinol-AQ, Platinol, Neoplatin

顺铂Chemical Name: cis-Diaminedichloroplatinum(II); (SP-4-2)-Diaminedichloroplatinum
CAS No. 15663-27-1
项目整合开发状态: Launched-1979
项目研究机构: Bristol-Myers Squibb (Originator), EORTC (Not Determined...
参考文献标题:Cisplatin
文献作者:Castar,J.; Woodman,R.J.
参考来源:Drugs Fut 1978,3(8),574

Mabuterol hydrochloride, KF-868DS, PB-868, Broncholin

马布台诺甲醇中马布特罗盐酸盐(以马布特罗计)Chemical Name: 1-[4-Amino-3-chloro-5-(trifluoromethyl)phenyl]-2-(tert-butylamino)ethanol hydrochloride
CAS No. 56795-19-8, 56341-08-3 (free base), 54240-36-7 (monoHCl)
项目...
参考文献标题:Mabuterol Hydrochloride
文献作者:Kr黦er,G.; Engelhardt,G.
参考来源:Drugs Fut 1985,10(11),913

Ruboxistaurin hydrochloride, LY-333531.HCl

鲁伯斯塔盐酸盐Chemical Name: 9(S)-(Dimethylaminomethyl)-5,6,7,9,10,11,12,17,18,19,20,21-dodecahydro-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20-dione hydrochloride 参考文献标题:Protein kinase C inhibitors
文献作者:Heath,W.F.Jr.; Jirousek,M.R.; McDonald,J.H.III; Rito,C.J.(Eli Lilly and Company)
参考来源:CA 2137203; EP 0657458; JP 1995238044; US 5624949