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

SAL-V-11

Chemical Name: 4-(3,4-Dichlorophenyl)-1-methylpiperidine-4-carboxylic acid ethyl ester hydrochloride
CAS No. 258500-91-3 (free base)
项目整合开发状态: Biological Testing
项目研究机构: National Institute on...
参考文献标题:Synthesis,dopamine and serotonin transporter binding affinities of novel analogues of meperidine
文献作者:Lomenzo,S.A.; Izenwasser,S.; Gerdes,R.M.; katz,J.L.; Kopajtic,T.; Trudell,M.L.
参考来源:Bioorg Med Chem Lett 1999,9(23),3273

新产品编号:144471

Chemical Name: 3-[3-[4-(N-Benzyl-N-methylaminomethyl)-4-hydroxypiperidin-1-yl]propyl]-5-(1,2,4-triazol-4-yl)-1H-indole
CAS No. 177946-34-8, 177946-35-9 (oxalate salt)
项目整合开发状态: Biological Testin...
参考文献标题:Azetidine,pyrrolidine and piperidine derivs.
文献作者:Baker,R.; Bourrain,S.; Castro Pineiro,J.L.; Chambers,M.S.; Guiblin,A.R.; Hobbs,S.C.; Jelley,R.A.; Madin,A.; Matassa,V.G.; Reeve,A.J.; Russell,M.G.N.; Showell,G.A.; Sternfeld,F.; Street,L.J.; Van Niel,M.B.(Merck Sharp & Dohme Ltd.)
参考来源:EP 0804434; JP 1998503768; US 5854268; WO 9604274

S-24718

Chemical Name: 1-[8-(Benzylamino)-3,4-dihydrospiro[2H-1,4-benzoxazine-3,1'-cyclopentan]-5-yl]-1-phenylmethanone
CAS No. 251562-03-5
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:...
参考文献标题:Novel 8-amino-1,4-benzoxazine cpds.,preparation method and pharmaceutical compsns.containing them
文献作者:Largeron,M.; Lestage,P.; Fleury,M.B.; Lockhart,B.(ADIR et Cie.)
参考来源:FR 2779144; WO 9962889

Co-134444

Chemical Name: 3alpha-Hydroxy-21-(1-imidazolyl)-3-(methoxymethyl)-5alpha-pregnan-20-one
CAS No. 256955-84-7
项目整合开发状态: Preclinical
项目研究机构: CoCensys (Originator)
合成路线:Regioselective addition...
参考文献标题:3alpha-Hydroxy-3beta methoxymethyl-21-heterocycle substd.steroids with anesthetic activity
文献作者:Hogenkamp,D.L.(CoCensys,Inc.)
参考来源:WO 0066614

Co-177843

Chemical Name: 3alpha-Hydroxy-3-(methoxymethyl)-21-(1-oxidoquinolin-6-yloxy)-5alpha-pregnan-20-one
CAS No. 256955-85-8
项目整合开发状态: Preclinical
项目研究机构: CoCensys (Originator)
合成路线:Regioselecti...
参考文献标题:3alpha-Hydroxy-3beta methoxymethyl-21-heterocycle substd.steroids with anesthetic activity
文献作者:Hogenkamp,D.L.(CoCensys,Inc.)
参考来源:WO 0066614

GW-432042

Chemical Name: S-[2-(1-Iminoethylamino)-1(R)-methylethyl]-L-cysteine
CAS No. 251325-08-3, 251325-24-3 (diHCl)
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originator)
合成路线:Alkylat...
参考文献标题:Nitric oxide synthase inhibitors
文献作者:Beswick,P.J.; Young,R.J.; Kleanthous,S.(Glaxo Group Ltd.)
参考来源:EP 1084104; WO 9962875

新产品编号:168201

Chemical Name: Pivalic acid (+)-4(R)-(methylamino)-4,5,6,7-tetrahydro-1,2-benzisoxazol-3-yloxymethyl ester hemioxalate
CAS No. 182316-77-4, 182316-76-3 (free base), 182317-67-5 (S-isomer), 182317-6...
参考文献标题:4-Aminotetrahydrobenzisoxazole or -isothiazole cpds.
文献作者:Falch,E.; Moltzen,L.S.; Schousboe,A.; Frolund,B.; Perregaard,J.K.; Krogsgaard-Larsen,P.(H.Lundbeck A/S)
参考来源:WO 9626929

新产品编号:120741

Chemical Name: 2-[4-[N-(6-Amidino-2-naphthyl)carbamoyl]phenoxy]acetic acid hydrochloride
CAS No. 170737-04-9, 259199-27-4 (free base)
项目整合开发状态: Biological Testing
项目研究机构: Mitsubishi Pharma (O...
参考文献标题:Preparation and pharmacological evaluation of novel glycoprotein (Gp) IIb/IIIa antagonists.1.The selection of naphthalene derivatives
文献作者:Ono,S.; Inoue,Y.; Yoshida,T.; Ashimori,A.; Kosaka,K.; Imada,T.; Fukaya,C.; Nakamura,N.
参考来源:Chem Pharm Bull 1999,47(12),1685

HI-443

Chemical Name: N-(5-Bromopyridin-2-yl)-N'-[2-(2-thienyl)ethyl]thiourea
CAS No. 258340-15-7
项目整合开发状态: Preclinical
项目研究机构: Parker Hughes Institute (Originator)
合成路线:Reaction of 2-amino-5-bro...
参考文献标题:Thiophene-ethyl thiourea cpds.and use
文献作者:Ventatachalam,T.K.; Uckun,F.M.(Parker Hughes Institute)
参考来源:US 6124324; WO 0078755

DPC-082

Chemical Name: (E)-4(S)-(2-Cyclopropylvinyl)-5,6-difluoro-4-(trifluoromethyl)-3,4-dihydro-1H-quinazolin-2-one
CAS No. 214287-98-6
项目整合开发状态: Phase I
项目研究机构: Bristol-Myers Squibb (Originator) 参考文献标题:4,4-Disubstd.-3,4-dihydro-2(1H)-quinazolinones useful as HIV reverse transcriptase inhibitors
文献作者:Corbett,J.W.; Ko,S.S.(DuPont Pharmaceuticals Co.)
参考来源:US 6124302; WO 9845276