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

Imexon, BM-06002

亚美克松Chemical Name: 4-Imino-1,3-diazabicyclo[3.1.0]hexan-2-one; 4-Imino-1,5-methyleneimidazolidin-2-one
CAS No. 59643-91-3
项目整合开发状态: Phase I
项目研究机构: Roche (Originator)
合成路线:By isomerization...
参考文献标题:BM-06002
文献作者:Hillier,K.; Castar,J.
参考来源:Drugs Fut 1978,3(2),95

Imipenem, Imipemide(former USAN), MK-0787, Tienam

亚胺培南(一水物) 亚胺培南 Chemical Name: [5R-[5alpha,6alpha(R*)]]-6-(1-Hydroxyethyl)-3-[[2-[(iminomethyl)amino]ethyl]thio]-7-oxo-1-azabicyclo[3.2.O]hept-2-ene-2-carboxylic acid monohydrate
CAS No. 74431-23-5...
参考文献标题:Derivatives of thienamycin and its isomers
文献作者:Christensen,B.G.; et al.(Merck & Co.,Inc.)
参考来源:DE 2652679; FR 2332012; GB 1570990; NL 7612939

Lenampicillin hydrochloride, KBT-1585, KB-1585, Takacillin, Veracillin

仑氨西林仑氨西林 Chemical Name: Ampicillin (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl ester hydrochloride; 6beta-[2(R)-Amino-2-phenylacetamido]penicillanic acid 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl ester hyd...
参考文献标题:Novel ampicillin esters and production thereof
文献作者:Sakamoto,F.; Ikeda,S.; Tsukamoto,G.; Utsumi,I.(Kanebo Pharmaceuticals,Ltd.)
参考来源:EP 0039086; EP 0039477; EP 0061206; US 4389408

Tacrolimus, Fujimycin, L-679934, FK-506, FR-900506, Protopy, Protopic, Prograf(as hydrate)

他克莫司他克莫司 Chemical Name: [3S-[3R*[E(1S*,3S*,4S*)],4S*,5R*,8S*,9E,12R*,14R*,15S*,16R*,18S*,19S*,26aR*]]-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[2-(4-hydroxy-3-met...
参考文献标题:Process for synthesis of FK-506 and tricarbonyl intermediates
文献作者:Jones,T.K.; Askin,D.; Mills,S.G.; Reamer,R.A.; Desmond,R.; Volante,R.P.; Tschaen,D.M.; Shinkai,I.(Merck & Co.,Inc.)
参考来源:EP 0378318; JP 1990233643

Taprostene sodium, CG-4203

他前列烯钠他前列烯 Chemical Name: [(5Z,13E,9alpha,15S)-2,3,4-Trinor-inter-m-phenyl-ene-6,9-epoxy-11,15-dihydroxy-15-cyclohexyl-16,17,18,19,20-pentanor]prosta-5,13-dienoic acid sodium salt; [3aR-[2Z,3aalpha,5a...
参考文献标题:CG-4203
文献作者:Castar,J.; Hillier,K.; Serradell,M.N.
参考来源:Drugs Fut 1984,9(7),494

Tacalcitol(hydrate), 1,24(R)-Dihydroxyvitamin D3, PRI-2191, TV-02, Apsor, Vellutan, Curatoderm, Bonalfa

他卡西妥他骨化醇一水物 Chemical Name: (+)-(1alpha,3beta,5Z,7E,24R)-9,10-Secocholesta-5,7,10(19)-triene-1,3,24-triol; (+)-1alpha,24R-Dihydroxyvitamin D3
CAS No. 57333-96-7, 93129-94-3 (monohydrate)
项目整合开发状...
参考文献标题:1alpha,24-Dihydroxycholecalciferol derivs.and pro
文献作者:Takeshita,T.; Hashimoto,Y.; Kawashima,H.; Ishimoto,S.; Ikekawa,N.; Morisaki,M.(Teijin Ltd.)
参考来源:DE 2526981; US 4022891

Tazobactam sodium, YP-14(comb. with piperacillin), CL-307579, CL-298741(free acid), YTR-830H, YTR-830(free acid), Tazocilline(comb. with piperacillin), Tazocin(comb. with piperacillin), Tazobac, Astat

他唑巴坦钠三唑巴坦 Chemical Name: [2S-(2alpha,3beta,5alpha)]-3-Methyl-7-oxo-3-(1H-1,2,3-triazol-1-ylmethyl)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid 4,4-dioxide sodium salt
CAS No. 89785-84-2, 8...
参考文献标题:Penicillin derivatives and process for preparation of the same
文献作者:Micetich,R.G.; et al.(Taiho Pharmaceutical Co.,Ltd.)
参考来源:EP 0097446; ES 523701; ES 538020

ABR-5050

他喹莫德Chemical Name: 4-Hydroxy-N-[4-(trifluoromethyl)phenyl]-5-methoxy-N,1-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide
CAS No. 254964-60-8
项目整合开发状态: Preclinical
项目研究机构: Active Biotech (Or...
参考文献标题:Quinoline derivs.
文献作者:Fex,T.; Bjk,A.; J鰊sson,S.; Hedlund,G.(Active Biotech AB)
参考来源:EP 1095021; JP 2002520395; WO 0003991

Talnetant, SB-223412

他奈坦(S)-3-羟基-2-苯基-4-((1-苯基丙基)氨基甲酰基)喹啉-1-鎓氯化物Chemical Name: (-)-3-Hydroxy-2-phenyl-N-[1(S)-phenylpropyl]quinoline-4-carboxamide
CAS No. 174636-32-9, 174636-33-0 ((R)-isomer), 204519-66-4 (monoHCl), 1...
参考文献标题:Discovery of a novel class of selective non-peptid
文献作者:Giardina,G.A.; Raveglia,L.F.; Grugni,M.; Sarau,H.M.; Farina,C.; Medhurst,A.D.; Graziani,D.; Schmidt,D.B.; Rigolio,R.; Luttmann,M.; Cavagnera,S.; Foley,J.J.; Vecchietti,V.; Hay,D.W.
参考来源:J Med Chem 1999,42(6),1053

Talniflumate, MSI-1995, Ba-7602-06, Lomucin, Somalgen

他尼氟酯Chemical Name: 2-[3-(Trifluoromethyl)phenylamino]-3-pyridinecarboxylic acid 1,3-dihydro-3-oxo-1-isobenzofuranyl ester
CAS No. 66898-62-2
项目整合开发状态: Launched-1982
项目研究机构: Bag?(Originator), ...
参考文献标题:Talniflumate
文献作者:Torriani,H.
参考来源:Drugs Fut 1979,4(6),448