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

Nabutan hyrochloride(former USAN), Nabitan hydrochloride(Prop INNM, USAN), SP-106, Abbott-4056, NIB, BPP

4-哌啶丁酸[8-(1,2-二甲基庚基)-5,5-二甲基-2-炔丙基-3,4-二氢-1H-苯并吡喃o[4,3-c]吡啶-10-基]酯盐酸盐大麻坦 Chemical Name: (?-8-(3-Methyl-2-octyl)-1,3,4,5-tetrahydro-5,5-dimethyl-2-(2-propynyl)-2H-[1]benzopyrano[4,3-c]pyridin-10-yl 1-...
参考文献标题:Nabitan Hydrochloride
文献作者:Castar,J.; Paton,D.M.
参考来源:Drugs Fut 1980,5(9),439

BM-113

4-哌啶醋酸,1-[2-(二苯甲氧基)乙基]-,乙基酯Chemical Name: 1-[2-(Benzhydryloxy)ethyl]piperidine-4-acetic acid ethyl ester
CAS No. 115313-90-1, 115313-91-2 (maleate)
项目整合开发状态: Phase I
项目研究机构: Meram (Originator...
参考文献标题:Benzhydryloxyethylpiperidine derivs.,process for their preparation and pharmaceutical compsns.,in which they are present
文献作者:Buzas,A.; Merour,J.-Y.; Ollivier,R.(Laboratoires Meram SA)
参考来源:EP 0259227; US 4983614

MS-31-038

4-喹喹碱羧酰胺,N-(氨基亚氨基甲基)-8-(2-甲氧基乙氧基)-2-苯基-Chemical Name: N1-[8-(2-Methoxyethoxy)-2-phenylquinolin-4-ylcarbonyl]guanidine bis(methanesulfonate)
CAS No. 181048-36-2 (free base), 181049-21-8 (monomethane...
参考文献标题:Quinoline-4-carbonylguanidine derivates,process for producing the same and pharmaceutical compsns.containing the cpds.
文献作者:Fujiwara,J.; Mori,H.; Yamashita,H.; Kitamori,T.; Hosoya,J.; Banno,H.(Mitsui Chemicals,Inc.)
参考来源:EP 0726254; JP 1996277269; US 5627193

Torcitabine, L-dC, NV-02C

4-氨基-1-(2-脱氧-beta-L-赤式-呋喃戊糖基)-2(1H)-嘧啶酮Chemical Name: 4-Amino-1-[(2S,4R,5S)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]pyrimidin-2(1H)-one; beta-L-Deoxycytidine; 4-Amino-1-(2-deoxy-beta-L-erythro...
参考文献标题:beta-L-2'-Deoxy-nucleosides for the treatment of hepatitis B
文献作者:Bryant,M.L.; Gosselin,G.; Imbach,J.-L.(CNRS (Centre National de la Recherche Scientifique); Novirio Pharmaceuticals Ltd.)
参考来源:WO 0009531

OSI-7836, GS-7836, 4'-Thio-ara-C

4-氨基-1-(4-硫代-Β-D-阿糖腺苷)-2(氢)-嘧啶酮Chemical Name: 4'-Thio-beta-D-arabinofuranosylcytosine; 4-Amino-1-(4-thio-beta-D-arabinofuranosyl)-2(1H)-pyrimidinone; 1-(4-Thio-beta-D-arabinofuranosyl)cytosine
CAS ...
参考文献标题:4-Thio-D-arabinofuranosylpyrimidine nucleosides
文献作者:Whistler,R.L.; Doner,L.W.; Nayak,U.G.
参考来源:J Org Chem 1971,36(1),108

Tezacitabine, KW-2331, FMdC, MDL-101731

4-氨基-1-[(2R,3E,4S,5R)-3-(氟亚甲基)-4-羟基-5-(羟基甲基)四氢呋喃-2-基]嘧啶-2-酮胞苷,2'-脱氧-2'-(氟甲苯)-,单水合物,(2'E)-(9CI) Chemical Name: (E)-2'-Deoxy-2'-(fluoromethylene)cytidine
CAS No. 130306-02-4, 171176-43-5 (hydrate) 参考文献标题:Novel 2'-halomethylidene,2'-ethenylidene and 2'-ethynyl cytidine,uridine and guanosine derivs.
文献作者:McCarthy,J.R.; Edwards,M.L.; Matthews,D.P.(Merrell Pharmaceuticals,Inc.)
参考来源:EP 0372268; JP 1990178272; US 5378693

Troxacitabine, SPD-758, beta-L-OddC, BCH-4556, Troxatyl

4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮Chemical Name: (2'S,4'S)-1-[2-(Hydroxymethyl)-1,3-dioxolan-4-yl]cytosine; (2',4'S)-4-Amino-[2-(hydroxymethyl)-1,3-dioxolan-4-yl]pyrimidin-2-one; (-)-beta-L-Dio...
参考文献标题:2-Substd.-4-substd.-1,3-dioxolanes,synthesis and use thereof
文献作者:Belleau,B.; Dixit,D.; Nguyen-Ba,N.(Shire BioChem Inc.)
参考来源:EP 0337713

Batanopride hydrochloride, BMY-25801-01, BMY-25801 free base

4-氨基-5-氯-N-(2-二乙基氨基乙基)-2-(3-氧代丁烷-2-基氧基)苯甲酰胺盐酸盐巴他必利 Chemical Name: (?-4-Amino-5-chloro-N-[2-(diethylamino)ethyl]-2-(1-methyl-2-oxopropoxy)benzamide hydrochloride
CAS No. 102670-59-7, 102670-46-2 (f...
参考文献标题:Substituted benzamides.1.Potential nondopaminergic antagonists of chemotherapy-induced nausea and emesis
文献作者:Monkovic,I.; Willner,D.; Adam,M.A.; Brown,M.; Crenshaw,R.R.; Fuller,C.E.; Juby,P.F.; Luke,G.M.; Matiskella,J.A.; Montzka,T.A.
参考来源:J Med Chem 1988,31(8),1548-58

Y-36912

4-氨基-N-[1-[3-(苄磺酰)丙基]哌啶-4-甲甲基]-5-氯-2-甲氧基苯甲酰Chemical Name: 4-Amino-N-[1-[3-(benzylsulfonyl)propyl]piperidin-4-ylmethyl]-5-chloro-2-methoxybenzamide
CAS No. 213600-06-7
项目整合开发状态: Preclinical
项目...
参考文献标题:Synthesis and pharmacological evaluation of benzamides as selective 5-HT4 receptor agonists
文献作者:Baker,S.R.; et al.
参考来源:15th European Federation for Medicinal Chemistry International Symposium on Medicinal Chemistry (Sept 6 1998,Edinburgh) 1998,Abs P 270

Pymadin, Fampridine, 4-Aminopyridine, EL-970, 4-AP, Fampridine-SR, Neurelan

4-氨基吡啶Chemical Name: 4-Aminopyridine; 4-Pyridinamine
CAS No. 504-24-5
项目整合开发状态: Phase III
项目研究机构: Elan (Orphan Drug), Rush Presbyterian-St. Luke's Med. Center (Originator), Acorda (Licensee),...
参考文献标题:
文献作者:Koenig,C.; et al.
参考来源:DE 1270563