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

Ro-64-5781

Chemical Name: 3-[5-(2,4-Diaminopyrimidin-5-ylmethyl)-2,3-dimethoxyphenyl]-1-[1(R)-(2-methylpyrimidin-5-yl)-1,2-dihydrophthalazin-2-yl]-2(E)-propen-1-one
CAS No. 212959-84-7 (undefined isomer)
项...
参考文献标题:Anti-MRSA dihydrofolate reductase inhibitors: Synthesis and SAR
文献作者:Guerry,P.; Locher,H.H.; Hubschwerlen,C.; Wyss,P.C.; Jolidon,S.; Hartman,P.G.; Stalder,H.; Specklin,J.L.
参考来源:39th Intersci Conf Antimicrob Agents Chemother (Sept 26 1999,San Francisco) 1999,Abst F1800

S-33004((+)-enantiomer), S-32647(racemate), S-33005

Chemical Name: (-)-1-[7-(Dimethylaminomethyl)-4-methoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]cyclohexanol hydrochloride
CAS No. 242473-12-7, 242473-11-6 ((+)-enantiomer), 242473-60-5 (free base), 242...
参考文献标题:Benzocyclobutan cpds.,their process for preparation and pharmaceutical compsns.containing them
文献作者:Brocco,M.; Harmange,J.-C.; Peglion,J.-L.; Dessinges,A.; Newman-Tancredi,A.; Millan,M.(ADIR et Cie.)
参考来源:CA 2264372; EP 0940386; FR 2775687; JP 1999310557; US 6107345

S-787

Chemical Name: 3(S)-(3,5-Dichloro-2-hydroxyphenyl)-3-[2-[3-hydroxy-5-(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-ylamino)benzamido]acetamido]propionic acid ; N-[3-Hydroxy-5-(5-hydroxy-1,4,5,6-tetrahydrop...
参考文献标题:Meta-guanidine,urea,thiourea or azacyclic amino benzoic acid derivs.as integrin antagonists
文献作者:Ruminski,P.G.; Clare,M.; Collins,P.W.; Desai,B.N.; Lindmark,R.J.; Rico,J.G.; Rogers,T.E.; Russell,M.A.(Pharmacia Corp.)
参考来源:EP 0850221; JP 1999510814; US 6013651; WO 9708145

HMR-3562

Chemical Name: 11-Deoxy-3-des(hexopyranosyloxy)-2-fluoro-11-[4-[4-(3-pyridinyl)-1H-imidazol-1-yl]butylamino]-6-O-methyl-3-oxoerythromycin A 11-N,12-O-cyclic carbamate
CAS No. 193752-41-9
项目整合开发状...
参考文献标题:Erythromycin derivs.,their production and their use as medicaments
文献作者:Agouridas,C.; Bretin,F.; Chantot,J.-F.(Aventis Pharma SA)
参考来源:EP 0799833; JP 1997176182; US 5747467

FMA-199

Chemical Name: 11-Deoxy-3-des(cladinosyl)-11-[2-[N-methyl-N-(3-pyridylmethyl)amino]ethylamino]-3-O-(2-pyridylacetyl)-6-O-methylerythromycin A 11-N,12-O-cyclic carbamate
CAS No. 208455-50-9
项目整合开...
参考文献标题:Erythromycin A derivs.
文献作者:Ishii,T.; Tanikawa,T.; Matsuura,A.; Sugimoto,T.; Asaka,T.; Kashimura,M.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0945459; WO 9823628

PGE-9262932

Chemical Name: 7-[3(R)-[1(S)-Aminoethyl]pyrrolidin-1-yl]-1-cyclopropyl-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
CAS No. 221221-18-7, 221239-01-6 (HCl)
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Antimicrobial quinolones,their compsns.and uses
文献作者:Hu,X.E.; Gray,J.L.; Almstead,J.-I.K.; Ledoussal,B.(The Procter & Gamble Co.)
参考来源:EP 1015445; WO 9914214

PNU-176665

Chemical Name: N-[3-[3-Fluoro-4-(1,3,4-thiadiazol-2-yl)phenyl]-2-oxooxazolidin-5(S)-ylmethyl]acetamide
CAS No. 220009-87-0
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Diazotizat...
参考文献标题:Thiadiazolyl and oxadiazolyl phenyl oxazolidinone antibacterial agents
文献作者:Gadwood,R.C.; Thomasco,L.M.; Anderson,D.J.(Pharmacia Corp.)
参考来源:EP 0994874; WO 9902525

新产品编号:492511

Chemical Name: N-[3-[4-[5-(2-Cyanoethyl)-1,3,4-thiadiazol-2-yl]-3-fluorophenyl]-2-oxooxazolidin-5(S)-ylmethyl]acetamide
CAS No. 220009-98-3
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator) 参考文献标题:Thiadiazolyl and oxadiazolyl phenyl oxazolidinone antibacterial agents
文献作者:Gadwood,R.C.; Thomasco,L.M.; Anderson,D.J.(Pharmacia Corp.)
参考来源:EP 0994874; WO 9902525

新产品编号:611161

Chemical Name: N-[3-(4-Methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)-2-oxooxazolidin-5(S)-ylmethyl]acetamide
CAS No. 233773-46-1
项目整合开发状态: Preclinical
项目研究机构: Bayer (Originator)
合成路线:Be...
参考文献标题:Novel bicyclene-substd.oxazolidinones
文献作者:Endermann,R.; H鋌ich,D.; Ruppelt,M.; Raddatz,S.; Rosentreter,U.; Riedl,B.; Bartel,S.; Wild,H.; Stolle,A.; Guarnieri,W.; Kroll,H.-P.(Bayer AG)
参考来源:DE 19802239; WO 9937641

DF-1601A

Chemical Name: 5-(tert-Butoxycarbonylamino)-2-carboxy-2-(tetrahydropyran-4-yloxy)pentanoic acid lithium salt; 2-[3-(tert-Butoxycarbonylamino)propyl]-2-(tetrahydropyran-4-yloxy)propanedioic acid lithiu...
参考文献标题:Geminal carboxylic acids and esters thereof pharmaceutical formulations containing them useful in the treatment of bone dysmetabolism
文献作者:Fiorentino,S.; Allegretti,M.; Mantovanini,M.; Clavenna,G.; Caselli,G.; Gandolfi,C.A.(Domp?Farmaceutici SpA)
参考来源:EP 0792878; US 5908863