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

PS-5

(5R,6R)-3-(2-乙酰氨基基乙基硫基)-6-乙基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸Chemical Name: trans-3-[2-(Acetamido)ethylsulfanyl]-6-ethyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
CAS No. 67007-79-8
项目整合...
参考文献标题:Asymmetric synthesis of the carbapenem antibiotic (+)-PS-5
文献作者:Shibasaki,M.; Ishida,Y.; Iwasaki,G.; Iimori,T.
参考来源:J Org Chem 1987,52(15),3488-9

Ritipenem sodium, FCE-22101

(5R,6S)-2-(氨甲酰氧基甲基)-6-[1(R)-羟基乙基]-2-戊烯-3-羧酸钠盐利替培南 Chemical Name: (5R,6S)-2-(Carbamoyloxymethyl)-6-[1(R)-hydroxyethyl]-2-penem-3-carboxylic acid sodium salt
CAS No. 84845-58-9, 84845-57-8 (free aci...
参考文献标题:FCE-22101
文献作者:Riva,F.
参考来源:Drugs Fut 1985,10(2),119

L-685458

(5S)-(叔丁氧羰基氨基)-6-苯基-(4R)-羟基-(2R)-苄基己酰)-L-亮氨酰-L-苯丙氨酰胺Chemical Name: N-[2(R)-Benzyl-5(S)-(tert-butoxycarboxamido)-4(R)-hydroxy-6-phenylhexanoyl]-L-leucyl-L-phenylalanylamide
CAS No. 292632-98-5
项目...
参考文献标题:gamma-Secretase inhibitors
文献作者:Hunt,P.A.; Harrison,T.; Castro Pineiro,J.L.; Nadin,A.J.(Merck Sharp & Dohme Ltd.)
参考来源:WO 0153255

ONO-8711

(5Z)-6-[(2R,3S)-3-[[[(4-氯-2-甲基苯基)磺酰基]氨基]甲基]双环[2.2.2]辛-2-基]-5-己烯酸Chemical Name: 6-[(2R,3S)-3-(4-Chloro-2-methylphenylsulfonamidomethyl)bicyclo[2.2.2]oct-2-yl]-5(Z)-hexenoic acid
CAS No. 216158-34-8<...
参考文献标题:Benzenesulfonamide cpds.
文献作者:Maruyama,T.; Nagao,Y.; Ohuchida,S.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 0878465; JP 1999029548; JP 2000103778

UCM-707

(5Z,8Z,11Z,14Z)-N-(3-呋喃基甲基)-5,8,11,14-二十碳四烯酰胺Chemical Name: N-(Furan-3-ylmethyl)-5(Z),8(Z),11(Z),14(Z)-icosatetraenamide
CAS No. 390824-20-1
项目整合开发状态: Preclinical
项目研究机构: Universidad Complute...
参考文献标题:Novel araquidonic acid derivs.with affinity toward the anandamide transporter
文献作者:Lopez Rodriguez,M.L.; Viso Beronda,A.; Ortega Gutierrez,S.; Latres Becker,I.; Gonzalez Rodriguez de Castro,S.; Fernandez Ruiz,J.J.; Ramos Atance,J.A.(Universidad Complutense de Madrid)
参考来源:WO 0212167

D-64131

(5-甲氧基-1H-吲哚-2-基)苯基甲酮Chemical Name: 1-(5-Methoxy-1H-indol-2-yl)-1-phenylmethanone
CAS No. 74588-78-6
项目整合开发状态: Preclinical
项目研究机构: Baxter Oncology (Originator)
合成路线:Protection of 5-methoxy...
参考文献标题:2-Acyl indol derivs.and their use as anti-tumour agents
文献作者:Burger,A.; Mahboobi,S.; Pongratz,H.; Hufsky,H.; B鰄mer,F.-D.; Beckers,T.; Klenner,T.; Baasner,S.; Frieser,M.; Hockemeyer,J.; Fiebig,H.-H.(Asta Medica AG)
参考来源:DE 10020852; WO 0182909

Compound 301029, PG-301029, 301029

(5-苯基-1,2,4-噻二唑-3-基)硫脲Chemical Name: N-(5-Phenyl-1,2,4-thiadiazol-3-yl)thiourea
CAS No. 97149-60-5
项目整合开发状态: Preclinical
项目研究机构: University of Arizona (Proprietary), Procter & Gamble (Origina...
参考文献标题:Thiadiazolyl urea or thiourea derivs.for antiviral treatment
文献作者:Camden,J.B.(The Procter & Gamble Co.)
参考来源:JP 2002540156; US 6258831; WO 0057878

Ajulemic acid, IP-751, DMH-THC-11-OIC, CT-3

(6aR,10aR)-1-羟基-6,6-二甲基-3-(2-甲基辛-2-基)-6a,7,10,10a-四氢苯并[c]色原烯-9-羧酸Chemical Name: (6aR,10aR)-3-(1,1-Dimethylheptyl)-1-hydroxy-6,6-dimethyl-6a,7,10,10a-tetrahydro-6H-benzo[c]chromene-9-carboxylic acid; (...
参考文献标题:(3R,4R)-DELTA6-Tetrahydrocannabinol-7-oic acids
文献作者:Mechoulam,R.; Burstein,S.H.
参考来源:US 5338753; WO 9401429

Sapropterin dihydrochloride, Dapropterin dihydrochloride, R-THBP, 6R-BH4, SUN-0588, Phenoptin, Biopten, Biobuden, Bipten

(6R)-5,6,7,8-四氢生物蝶呤二盐酸盐沙丙蝶呤 Chemical Name: (-)-(6R)-2-Amino-6-[(1R,2S)-1,2-dihydroxypropyl]-5,6,7,8-tetrahydro-4(3H)-pteridinone dihydrochloride; 6R-L-erythro-Tetrahydrobiopterin dihydrochloride
C...
参考文献标题:Preparation process for (6R)-tetrahydro-l-biopterin
文献作者:Sakai,H.; Kanai,T.(Shiratori; Suntory Ltd.)
参考来源:EP 0191335

FR-182024

(6R,7R)-3-(5-甲基-1,3,4-噻二唑-2-酰磺酰)-7-(2-苯乙酰胺)-3-头孢素-4-羧酸Chemical Name: (6R,7R)-3-(5-Methyl-1,3,4-thiadiazol-2-ylsulfanyl)-7-(2-phenylacetamido)-3-cephem-4-carboxylic acid
CAS No. 179034-83-4, 179035-...
参考文献标题:Cephem cpds.and pharmaceutical use thereof
文献作者:Yoshida,Y.; Sasaki,H.; Matsuda,K.; Takasugi,H.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0796263; JP 1998510258; WO 9617850