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

新产品编号:79609

Chemical Name: (S)-4-Bromo-N-[4-[2-[2-hydroxy-3-(4-hydroxyphenoxy)propylamino]ethyl]phenyl]benzenesulfonamide
CAS No. 159182-77-1
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)
合成路...
参考文献标题:Substd.phenyl sulfonamides as selective beta3 agonists for the treatment of diabetes and obesity
文献作者:Fisher,M.H.; Mathvink,R.J.; Ok,H.O.; Parmee,E.R.; Weber,A.E.(Merck & Co.,Inc.)
参考来源:CA 2114712; EP 0611003; JP 1995010827; US 5451677; WO 9418161

PNU-173954

Chemical Name: N-[3-[4-(4-Pyridyl)phenyl]-4,5-dihydroisoxazol-5(R)-ylmethyl]acetamide
CAS No. 203633-95-8
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The asymmetric 1,3-dipolar ...
参考文献标题:Isoxazoline derivs.useful as antimicrobials
文献作者:Barbachyn,M.R.; Thomas,R.C.; Cleek,G.J.(Pharmacia & Upjohn AB)
参考来源:EP 0920421; US 5990136; WO 9807708

L-167307

Chemical Name: 4-[2-(4-Fluorophenyl)-5-[4-(methylsulfinyl)phenyl]-1H-pyrrol-3-yl]pyridine
CAS No. 188352-45-6
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)
合成路线:The condensation o...
参考文献标题:2,5-Substd.aryl pyrroles,comspns.containing suc
文献作者:De Laszlo,S.E.; Mantlo,N.B.; Ponticello,G.S.; Selnick,H.G.; Liverton,N.J.(Merck & Co.,Inc.)
参考来源:EP 0871444; JP 1999510511; WO 9705878

DNK-333, DNK-333A

Chemical Name: 5-(3,4-Dichlorophenyl)-4(R)-[N-methyl-3,5-bis(trifluoromethyl)benzamido]-N-[2-oxoperhydroazepin-3(R)-yl]-2(E)-pentenamide; N-[1(R)-(3,4-Dichlorobenzyl)-4-[hexahydro-2-oxo-1H-azepin-3(R)...
参考文献标题:Acylaminoalkenylene-amide derivs.as NK1 and NK2 antagonists
文献作者:Gerspacher,M.; Von Sprecher,A.; Mah,R.; Roggo,S.; Stutz,S.(Novartis AG)
参考来源:EP 0923550; JP 2001503387; US 6319917; WO 9807694

PPI-368

Chemical Name: (3alpha,5beta,7alpha,12alpha)-Trihydroxycholan-24-oyl-L-leucyl-L-valyl-L-phenylalanyl-L-phenylalanyl-L-alanine
CAS No. 183746-33-0
项目整合开发状态: Biological Testing
项目研究机构: Praecis ...
参考文献标题:Modulators of amyloid aggregation
文献作者:Reed,M.J.; Hundal,A.; Molineaux,S.; Chin,J.; Kelley,M.; Findeis,M.A.; Kasman,L.; Benjamin,H.; Kubasek,W.; Musso,G.; Signer,E.R.; Wakefield,J.; Lee,J.-J.; Garnick,M.B.; Gefter,M.L.(Praecis Pharmaceuticals Inc.)
参考来源:JP 1999514333; WO 9628471

LU-420627(sodium salt), BSF-420627(sodium salt), LU-302872

Chemical Name: 3-[2-(3,4-Dimethoxyphenyl)ethoxy]-2(S)-(4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid
CAS No. 204267-34-5
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:...
参考文献标题:Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2-(4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872),a novel orally active mixed ETA/ETB receptor antagonist
文献作者:Amberg,W.; Hergenr鰀er,S.; Hillen,H.; Jansen,R.; Kettschau,G.; Kling,A.; Klinge,D.; Raschack,M.; Riechers,H.; Unger,L.
参考来源:J Med Chem 1999,42(16),3026

NNC-55-0118

Chemical Name: 6-Chloro-N-isopropyl-4H-thieno[3,2-e][1,2,4]thiadiazin-3-amine 1,1-dioxide
CAS No. 194086-39-0, 292864-95-0
项目整合开发状态: Preclinical
项目研究机构: Novo Nordisk (Originator)
合成路线:The ...
参考文献标题:6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells
文献作者:Nielsen,F.E.; Bodvarsdottir,T.B.; Worsaae,A.; MacKay,P.; Stidsen,C,E.; Boonen,H.C.; Pridal,L.; Arkhammar,P.O.; Wahl,P.; Ynddal,L.; Junager,F.; Dragsted,N.; Tagmose,T.M.; Mogensen,J.P.; Koch,A.; Treppendahl,S.P.; Hansen,J.B.
参考来源:J Med Chem 2002,45(19),4171

新产品编号:359623

Chemical Name: 2-[5-[2(E)-(N,N-Diethylcarbamoyl)-1-methylvinyl]-2-(2,6-difluorobenzyloxy)phenoxy]acetic acid
CAS No. 205317-49-3
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:3'...
参考文献标题:Carboxy-substituted cinnamides: A novel series of potent,orally active LTB4 receptor antagonists
文献作者:Greenspan,P.D.; Fujimoto,R.A.; Marshall,P.J.; Raychaudhuri,A.; Lipson,K.E.; Zhou,H.; Doti,R.A.; Coppa,D.E.; Zhu,L.; Pelletier,R.; Uziel-Fusi,S.; Jackson,R.H.; Chin,M.H.; Kotyuk,B.L.; Fitt,J.J.
参考来源:J Med Chem 1999,42(1),164

FMA-122

Chemical Name: 3-Des(hexopyranosyl)-9-deoxo-9(S)-hydroxy-3-O-[2-(3-pyridyl)acetyl]erythromycin A 6-O,9-O:11-O,12-O-bis(cyclic carbonate)
CAS No. 205320-30-5
项目整合开发状态: Preclinical
项目研究机构: Tais...
参考文献标题:Erythromycin A derivs.
文献作者:Asaka,T.; Tanikawa,T.; Ishii,T.; Kashimura,M.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:WO 9813373

KN-734, CT-052923, CT-52923

Chemical Name: N-(1,3-Benzodioxol-5-ylmethyl)-4-(6,7-dimethoxyquinazolin-4-yl)piperazine-1-carbothioamide
CAS No. 205256-55-9
项目整合开发状态: Preclinical
项目研究机构: Kyowa Hakko (Originator), Millenniu...
参考文献标题:Nitrogenous heterocyclic cpds
文献作者:Matsuno,K.; Ichimura,M.; Nomoto,Y.; Fujiwara,S.; Ide,S.; Tsukuda,E.; Irie,J.; Oda,S.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0882717; WO 9814431