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

RWJ-38063

Chemical Name: N-[2-[4-(2-Isopropoxyphenyl)piperazin-1-yl]ethyl]-2-(2-oxopiperidin-1-yl)acetamide
CAS No. 216252-56-1, 216252-58-3 (citrate (1:1))
项目整合开发状态: Preclinical
项目研究机构: Ortho-McNeil (...
参考文献标题:Arylsubstd.piperazines useful in the treatment of benign prostatic hyperplasia
文献作者:Mulcahy,L.; Pulito,V.; Villani,F.; Li,X.; Murray,W.; Maryanoff,C.; Jolliffe,L.; Reitz,A.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:EP 0984777; US 6071915; WO 9851298

新产品编号:489347

Chemical Name: (6S,8aS)-N-[1(S)-(1-Carbamimidoylpiperidin-4-yl)-2-oxo-2-(2-thiazolyl)ethyl]-4-oxo-2-(3-phenylpropionyl)octahydropyrrolo[1,2-a]pyrazine-6-carboxamide
CAS No. 219832-87-8
项目整合开发状态:...
参考文献标题:Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications
文献作者:Plummer,J.S.; Berryman,K.A.; Cai,C.; Cody,W.L.; DiMaio,J.; Doherty,A.M.; Edmunds,J.J.; He,J.X.; Holland,D.R.; Levesque,S.; Kent,D.R.; Narasimhan,L.S.; Rubin,J.R.; Rapundalo,S.T.; Siddiqui,M.A.; Susser,A.J.; St-Denis,Y.; Winocour,P.D.
参考来源:Bioorg Med Chem Lett 1998,8(23),3409

SM-256

Chemical Name: 3-[1-[3-(1H-Imidazol-2-ylamino)propyl]-1H-indazol-5-ylcarboxamido]-2(S)-[2,4,6-(trimethyl)phenylsulfonamido]propionic acid
CAS No. 192944-48-2
项目整合开发状态: Preclinical
项目研究机构: Bri...
参考文献标题:Disubstituted indazolines as potent antagonists of the integrin alphavbeta3
文献作者:Batt,D.G.; Petraitis,J.J.; Houghton,G.C.; Modi,D.P.; Cain,G.A.; Corjay,M.H.; Mousa,S.A.; Bouchard,P.J.; Forsythe,M.S.; Harlow,P.P.; Barbera,F.A.; Spitz,S.M.; Wexler,R.R.; Jadhav,P.K.
参考来源:J Med Chem 2000,43(1),41

NIP-530

Chemical Name: N'-[3,5-Bis(trifluoromethyl)benzyl]-N-[3-[N-[1-(4-fluorobenzyl)benzimidazol-2-yl]-N-methylamino]propyl]-N-methylurea hydrochloride
CAS No. 215583-22-5
项目整合开发状态: Preclinical
项目研...
参考文献标题:Benzimidazole deriv.
文献作者:Kamikawaji,Y.; Tanikawa,K.; Yamamoto,A.; Hirotsuka,M.; Iwama,T.; Fujita,Y.(Nissan Chemical Industry,Ltd.)
参考来源:EP 0980359; JP 1999315071; US 6114369; WO 9850368

SNAP-5540

Chemical Name: (-)-1-[3-[2,6-Dimethyl-5-(methycarbamoyl)-4-(4-nitrophenyl)-1,4-dihydropyridin-3-ylcarboxamido]propyl]-4-phenylpiperidine-4-carboxylic acid methyl ester
CAS No. 166808-20-4 (undefine...
参考文献标题:Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia
文献作者:Nagarathnam,D.; Wetzel,J.M.; Miao,S.W.; Marzabadi,M.R.; Chiu,G.; Wong,W.C.; Hong,X.; Fang,J.; Forray,C.; Branchek,T.A.; Heydorn,W.E.; Chang,R.S.; Broten,T.; Schorn,T.W.; Gluchowski,C.
参考来源:J Med Chem 1998,41(26),5320

RC-527, CRX-527

Chemical Name: N-[3(R)-(Decanoyloxy)tetradecanoyl]-O3-[2-[3(R)-(decanoyloxy)tetradecanamido]-3-O-[3(R)-(decanoyloxy)tetradecanoyl]-2-deoxy-4-O-phosphono-beta-D-glucopyranosyl]-L-serine triethylammoniu...
参考文献标题:Aminoalkyl glucosamine phosphate cpds.and their use as adjuvants and immunoeffectors
文献作者:Johnson,D.A.; Sowell,C.G.(Corixa Corp.)
参考来源:EP 0983286; US 6113918; WO 9850399

新产品编号:505167

Chemical Name: 2-Methylpropionic acid 2-(2-amino-6-fluoro-9H-purin-9-ylmethoxy)ethyl ester
CAS No. 220150-71-0
项目整合开发状态: Preclinical
项目研究机构: SK Chemicals (Originator)
合成路线:Treatment of the...
参考文献标题:Synthesis and evaluation of 2-amino-6-fluoro-9-(2-hydroxyethoxymethyl)purine esters as potential prodrugs of acyclovir
文献作者:Kim,D.-K.; Lee,N.; Im,G.J.; Kim,H.T.; Kim,K.H.
参考来源:Bioorg Med Chem 1998,6(12),2525

新产品编号:910159

Chemical Name: 5-Methoxy-1-phenyl-1H-benzimidazole
CAS No. 38205-85-5
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:The reaction of 2-chloro-5-methoxynitrobenzene (I) with ...
参考文献标题:Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor
文献作者:Palmer,B.D.; Smaill,J.B.; Boyd,M.; Boschelli,D.H.; Doherty,A.M.; Hamby,J.M.; Khatana,S.S.; Kramer,J.B.; Kraker,A.J.; Panek,R.L.; Lu,G.H.; Dahring,T.K.; Winters,R.T.; Showalter,H.D.; Denny,W.A.
参考来源:J Med Chem 1998,41(27),5457

DQ-113, D61-1113

Chemical Name: 5-Amino-7-[3(R)-(1-aminocyclopropyl)-4(S)-fluoropyrrolidin-1-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-8-methyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
CAS No. 190954-07-5, 1...
参考文献标题:Substd.aminocycloalkylpyrrolidine derivs.
文献作者:Takemura,M.; Kimura,Y.; Takahashi,H.; Kimura,K.; Miyauchi,S.; Ohki,H.(Daiichi Pharmaceutical Co.,Ltd.)
参考来源:EP 0911328; WO 9719072

Fluodipine

Chemical Name: 2,6-Dimethyl-4-(9-oxo-9H-fluoren-4-yl)-1,4-dihydropyridine-3,5-dicarboxylic acid bis(2-propenyl) diester
CAS No. 145695-42-7
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi...
参考文献标题:Fluorenone and benzophenone 1,4-dihydropyridine derivatives with cardiodepressant activity
文献作者:Valenti,P.; Brudiesi,R.; Rampa,A.; Chiarini,A.
参考来源:Arzneim-Forsch Drug Res 1992,42(11),1284