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

FY-609, HSR-609

1-哌啶丙烷酸,4-(8-氟[1]苯并氧环[4,3-b]吡啶-11(5H)-伊烯)- Chemical Name: 3-[4-(8-Fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidin-1-yl]propionic acid dihydrate
CAS No. 188199-97-5, 161522-25-...
参考文献标题:Amphoteric tricyclic compounds as antihistaminic and antiallergic agents
文献作者:Ito,Y.; Kato,H.; Yasuda,S.; Kado,N.; Iwasaki,N.; Nishino,H.; Takeshita,M.(Hokuriku Seiyaku Co.,Ltd.)
参考来源:EP 0556813; JP 1994192263; US 5334594

Fosteabine sodium hydrate, Cytarabine ocfosfate, C18PCA, YNK01, Starasid

2(1H)-嘧啶酮,4-氨基-1-[5-O-[羟基(辛基氧基)phoshinyl]-b-D-阿拉伯氨脋诺基]-,钠盐(1:1) [(2R,3S,4S)-5-(4-氨基-2-氧代嘧啶-1-基)-3,4-二羟基四氢呋喃-2-基]甲基十八烷基氢磷酸酯Chemical Name: 1-beta-D-Arabinofuranosylcytosine 5'-stearyl phosphate monosod...
参考文献标题:YNK01
文献作者:Takahashi,K.; Kodama,K.
参考来源:Drugs Fut 1989,14(11),1056

新产品编号:259957

2-(2-((4-氯苯基)硫代)乙氧基)-3-甲氧基-5-((2S,5S)-5-(3,4,5-三甲氧基苯基)四氢呋喃-2-基)苯并腈 Chemical Name: (?-trans-2-[2-(4-Chlorophenylsulfanyl)ethoxy]-3-methoxy-5-[5-(3,4,5-trimethoxyphenyl)tetrahydrofuran-2-yl]benzonitril...
参考文献标题:(+-)-trans-2-[3-Methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N-hydroxyureidyl)methylphenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran (CMI-392),a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist
文献作者:Cai,X.; Scannell,R.T.; Yaeger,D.; Hussoin,M.S.; Killian,D.B.; Qian,C.; Eckman,J.; Hwang,S.B.; Libertine-Garahan,L.; Yeh,C.G.; Ip,S.H.; Shen,T.Y.
参考来源:J Med Chem 1998,41(11),1970

Atliprofen methyl ester, IDPH-8261

2-(4-噻吩-3-基-苯基)-丙酸 2-(4-(3-噻吩)苯基)丙酸甲酯Chemical Name: 2-[4-(3-Thienyl)phenyl]propionic acid methyl ester
CAS No. 108912-17-0, 108912-14-7 (free acid), 158885-09-7 (racemic free acid)
项目整合开发状态: Ph...
参考文献标题:4-(3-Thienyl)phenylalkanoic acid derivs.
文献作者:Marwah,A.; Sastry,C.V.R.; Shridhar,D.R.(Indian Drugs & Pharmaceuticals Ltd.)
参考来源:DE 3537768

MID, IV-2, PX-12

2-(仲丁基二硫基)-1H-咪唑Chemical Name: (2-Imidazolyl)(1-methylpropyl)disulfide
CAS No. 141400-58-0
项目整合开发状态: Phase I
项目研究机构: ProlX (Originator)
合成路线:The reaction of S-(2-imiazolylsulfanyl)isothio...
参考文献标题:Parallel syntheses of disulfide inhibitors of the thioredoxin redox system as potential antitumor agents
文献作者:Ulhaq,S.; Kunkel,M.; Watson,S.; Fletcher,S.; Kirkpatrick,D.L.; Powis,G.
参考来源:Anti-Cancer Drug Des 1999,14(5),421

Ipidacrine hydrochloride hydrate, Amiridine, NIK-247, Senita

2,3,5,6,7,8-六氢-1H-环戊并[b]喹啉-9-胺 2,3,5,6,7,8-六氢-9-氨基-1H-环戊烯并[b]喹啉盐酸盐盐酸伊匹达克林Chemical Name: 9-Amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta[b]quinoline hydrochloride monohydrate
CAS No. 62732-44-9 (anhyd...
参考文献标题:9-Amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta(b)quinoline monohydrate hydrochloride as stimulant of neuro-muscular transmission of smooth muscles
文献作者:(Nauchno-Issledovatelsky Institut)
参考来源:US 4550113

Delmopinol hydrochloride, Decapinol, M-1650, Decapinol

2-[3-(4-丙基庚基)吗啉-4-基]乙醇地莫匹醇Chemical Name: (?-3-(4-Propylheptyl)-4-morpholineethanol hydrochloride
CAS No. 143966-12-5 (free base), 98092-92-3 (undefined stereoch.), 79874-76-3 (undefined stereoch....
参考文献标题:New morpholino cpds.their process of preparation and medicines containing them
文献作者:(Ferrosan AB)
参考来源:BE 0888052; BE 0901496

Capsavanil, KR-25018, DA-5018(monohydrochloride)

2-[4-(2-氨基乙氧基)-3-甲氧基苯基]-N-[3-(3,4-二甲基苯基)丙基]乙酰胺盐酸盐(1:1) Chemical Name: 2-[4-(2-Aminoethoxy)-3-methoxyphenyl]-N-[3-(3,4-dimethylphenyl)propyl]acetamide
CAS No. 147497-64-1, 174661-97-3 (hydrochlorid...
参考文献标题:Novel phenylacetamide derivs.and processes for the preparation thereof
文献作者:Lee,K.S.; Choi,J.K.; Hong,M.S.; Kim,H.S.; Lim,H.J.; Ha,D.C.; Park,N.S.(Korea Research Institute of Chemical Technology)
参考来源:EP 0525360; US 5242944

SEA-0400

2-[4-[(2,5-二氟苯基)甲氧基]苯氧基]-5-乙氧基苯胺Chemical Name: 2-[4-(2,5-Difluorobenzyloxy)phenoxy]-5-ethoxyphenylamine
CAS No. 223104-29-8, 223104-09-4 (HCl)
项目整合开发状态: Preclinical
项目研究机构: Taisho (Originato...
参考文献标题:2-Phenoxyaniline derivs.
文献作者:Tomisawa,K.; Taguchi,M.; Nakanishi,M.; Ota,T.; Aibe,I.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 1031556; JP 1999193263; US 6162832; WO 9920598

Fandosentan potassium, CI-1034, PD-180988

2H-1,2-苯并噻嗪-3-羧酸泛多生坦 Chemical Name: 4-(7-Ethyl-1,3-benzodioxol-5-yl)-2-[2-(trifluoromethyl)phenyl]-2H-1,2-benzothiazine-3-carboxylic acid S,S-dioxide potassium salt
CAS No. 221246-12-4, 221241-63...
参考文献标题:Benzothiazine dioxides as endothelin antagonists
文献作者:Berryman,K.A.; Bunker,A.M.; Doherty,A.M.; Edmunds,J.J.(Pfizer Inc.)
参考来源:EP 0811001; JP 1999501013; WO 9626195