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

FT-005, S-22954

Chemical Name: 2-(4,5-Dihydro-1H-imidazol-2-yl)-4-methyl-3,4-dihydro-2H-1,4-benzoxazine
CAS No. 96988-34-0, 97002-49-8 (diHCl)
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:The c...
参考文献标题:Synthesis of 2-(2-imidazolinyl) substituted 2,3-dihydro-4H-1,4-benzothiazine and 3,4-dihydro-2H-1,4-benzoxazines
文献作者:Buttler,R.C.M.; et al.
参考来源:J Heterocycl Chem 1985,22(1),177

NSC-712392, LB-42908

Chemical Name: 1-[1-[1-(1,3-Benzodioxol-5-ylmethyl)-1H-imidazol-5-ylmethyl]-4-(1-naphthyl)-1H-pyrrol-3-yl]-1-(4-methyl-1-piperazinyl)methanone; 1-[1-[1-(1,3-Benzodioxol-5-ylmethyl)-1H-imidazol-5-ylmet...
参考文献标题:Imidazole derivs.having an inhibitory activity for farnesyl transferase and process for preparation thereof
文献作者:Lee,J.H.; Yoo,J.K.; Koh,J.S.; Choi,T.S.; Shin,Y.S.; Kim,K.H.; Jung,W.H.; Kim,J.H.; Lee,S.H.; Ahn,I.A.; Ro,S.G.; Lee,H.I.; Kim,H.S.; Chung,H.H.; Jeong,S.W.; Kwak,T.H.(LG Chem Ltd.)
参考来源:WO 9928315

PD-172803

Chemical Name: 8-Isopropyl-2-[4-(4-methyl-1-piperazinyl)phenylamino]pyrido[2,3-d]pyrimidin-7(8H)-one
CAS No. 211245-21-5
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:Treat...
参考文献标题:Pyrido[2,3-d]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
文献作者:Dobrusin,E.M.; Fattacy,A.; Boschelli,D.H.; Fry,D.W.; Wu,Z.; Doherty,A.M.; Kallmeyer,S.T.; Barvian,M.R.(Pfizer Inc.)
参考来源:WO 9833798

S-31214

Chemical Name: 1(R)-[1-[N-(2-Phenylethyl)carbamoyl]cyclopentylcarboxamido]-4-guanidinobutylboronic acid hydrochloride
CAS No. 196209-64-0 (free base), 196209-65-1 (monobenzenesulfonate salt)
项目整...
参考文献标题:Cpds.derived from boronic acid
文献作者:Gloanec,P.; Portevin,B.; Lila,C.; Rupin,A.; de Nanteuil,G.; Simonet,S.; Verbeuren,T.(ADIR et Cie.)
参考来源:EP 0792883; FR 2745288; US 5814622

BILN-303-SE

Chemical Name: Acetyl-L-aspartyl-D-glutamyl-L-(2-cyclohexyl)glycyl-L-valyl-4(R)-(2-naphthylmethoxy)-L-prolyl-L-norvaline
CAS No. 220425-58-1
项目整合开发状态: Biological Testing
项目研究机构: Boehringer In...
参考文献标题:Hepatitis C inhibitor peptides
文献作者:Rancourt,J.; Tsantrizos,Y.; Simoneau,B.; Wernic,D.; Poupart,M.-A.; Llinas-Brunet,M.(Boehringer Ingelheim (Canada) Ltd.)
参考来源:EP 1003775; WO 9907733

S-31922

Chemical Name: 5-Amino-1(R)-[1-[N-(2-phenylethyl)carbamoyl]cyclopentylcarboxamido]pentylboronic acid
CAS No. 196209-59-3 (monoHCl)
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:C...
参考文献标题:Cpds.derived from boronic acid
文献作者:Gloanec,P.; Portevin,B.; Lila,C.; Rupin,A.; de Nanteuil,G.; Simonet,S.; Verbeuren,T.(ADIR et Cie.)
参考来源:EP 0792883; FR 2745288; US 5814622

SanOrg-123781, SR-123781A

Chemical Name: Methyl O-2,3,4,6-tetra-O-sulfo-alpha-D-glucopyranosyl-(1--4)-O-2,3,6-tri-O-sulfo-alpha-D-glucopyranosyl-(1--4)-O-2,3,6-tri-O-sulfo-beta-D-glucopyranosyl-(1--4)-O-2,3-di-O-methyl-6-O-sul...
参考文献标题:Synthetic polysaccharides,their method of production and pharmaceutical compsns.containing same
文献作者:Petitou,M.; Herbert,J.-M.; Duchaussoy,P.; Basten,J.; Dreef-Tromp,C.; Driguez,P.-A.; Van Boeckel,C.(Akzo Nobel N.V.; Sanofi-Synthabo)
参考来源:EP 1049721; FR 2773804; US 6528497; WO 9936443

RPR-200765A

Chemical Name: trans-1-[2-[4-(4-Fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-5-methyl-1,3-dioxan-5-yl]-1-(4-morpholinyl)methanone methanesulfonate
CAS No. 218162-38-0, 218158-45-3 (free base), 2...
参考文献标题:Imidazolyl-cyclic acetals
文献作者:Halley,F.; Porter,B.; Bamborough,P.L.; Lewis,R.A.; Ratcliffe,A.J.; Wallace,P.A.; McLay,I.M.; McKenna,J.M.; Lythgoe,D.J.; Collis,A.J.(Rh鬾e-Poulenc Rorer Ltd.)
参考来源:EP 0988301; WO 9856788

新产品编号:539971

Chemical Name: (3bR,4aS)-6-[3-(2-Methoxy-5-pyrimidinyl)-2(E)-propenoyl]-2-methyl-8-oxo-1,4,4a,5,6,8-hexahydrocyclopropa[c]pyrrolo[3,2-e]indole-3-carboxylic acid methyl ester
CAS No. 221549-90-2
...
参考文献标题:New water-soluble duocarmycin derivatives: Synthesis and antitumor activity of A-ring pyrrole compounds bearing beta-heteroarylacryloyl groups
文献作者:Amishiro,N.; Nagamura,S.; Kobayashi,E.; Gomi,K.; Saito,H.
参考来源:J Med Chem 1999,42(4),669

新产品编号:405501

Chemical Name: 1-[4-(2-Pyridinyl)piperazin-1-ylsulfonyl]piperidine-2(R)-carbohydroxamic acid
CAS No. 210915-22-3 (undefined isomer)
项目整合开发状态: Biological Testing
项目研究机构: Agouron (Originator), ...
参考文献标题:Novel sulfamides and sulfonamide inhibitors of matrix metalloproteases
文献作者:Mitchell,L.J.Jr.; Burke,B.; Dagostino,E.; et al.
参考来源:218th ACS Natl Meet (Aug 22 1999,New Orleans) 1999,Abst MEDI 76