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

GR-215864X, GW-215864X

Chemical Name: 6alpha,9alpha-Difluoro-11beta-hydroxy-16alpha-methyl-3-oxo-17alpha-(propionyloxy)androsta-1,4-diene-17beta-carbothioic acid S-[2-oxotetrahydrofuran-3(R)-yl] ester
CAS No. 192056-79-4...
参考文献标题:Lactone derivs.of 17beta-carboxy,carbothio and amide androstane derivs.
文献作者:Biggadike,K.; Procopiou,P.A.(Glaxo Wellcome plc)
参考来源:JP 1999501675; US 6197761; WO 9724365

GW-5950X

Chemical Name: 2(R)-Benzyl-5-[3(R),5(R)-dibenzyl-2-oxopyrrolidin-1-yl]-4(S)-hydroxy-N-[2(R)-hydroxyindan-1(S)-yl]pentanamide
CAS No. 240127-97-3 (undefined stereoch.)
项目整合开发状态: Preclinical
项目...
参考文献标题:Aspartyl protease inhibitors
文献作者:Tung,R.D.; Salituro,F.G.; Deininger,D.D.; Bhisetti,G.R.; Baker,C.T.; Spaltenstein,A.; Kazmierski,W.M.; Andrews,C.W.III (Vertex Pharmaceuticals Inc.)
参考来源:JP 2000501111; US 5945413; WO 9727180

新产品编号:274195

Chemical Name: 9-Fluoro-5-methyl-1-oxo-N-[2-(4-pyridyl)ethyl]-6,7-dihydro-1H,5H-benzo[ij]quinolizine-2-carboxamide hydrochloride
CAS No. 195191-82-3
项目整合开发状态: Preclinical
项目研究机构: Celltech (Or...
参考文献标题:Synthesis and evaluation of a novel series of phosphodiesterase IV inhibitors.A potential treatment for asthma
文献作者:Beasley,S.C.; Cooper,N.; Gowers,L.; Gregory,J.P.; Haughan,A.F.; Hellewell,P.G.; Macari,D.; Miotla,J.; Montana,J.G.; Morgan,T.; Naylor,R.; Runcie,K.A.; Tuladhar,B.; Warneck,J.B.
参考来源:Bioorg Med Chem Lett 1998,8(19),2629

S-18841

Chemical Name: 3-Hydroxyimidazolidin-4-one
CAS No. 192565-05-2
项目整合开发状态: Preclinical
项目研究机构: ADIR (Originator)
合成路线:Ethyl glycinate (I) was converted to the 2-aminoacetohydroxamic acid (II...
参考文献标题:4-Imidazolidinone cpds.
文献作者:Cordi,A.; Lacoste,J.-M.; Millan,M.; Audinot,V.(ADIR et Cie.)
参考来源:EP 0780379; US 5677325

CL-191983, OCA-983

Chemical Name: (1R,5S,6S)-6-[1(R)-Hydroxyethyl]-1-methyl-2-[2(R)-(L-valylaminomethyl)tetrahydrofuran-3(R)-ylsulfanyl]-1-carba-2-penem-3-carboxylic acid
CAS No. 161856-02-6
项目整合开发状态: Preclinical<...
参考文献标题:Novel 2-thiosubstd.carbapenems
文献作者:Lin,Y.-I.; Bitha,P.; Sakya,S.; Strohmeyer,T.W.; Bush,K.(American Cyanamid Co.)
参考来源:CA 2118961; EP 0617036; JP 1994321948; US 5602118

G-20000, L-39

Chemical Name: 17-(5-Isoxazolyl)androsta-4,16-dien-3-one
CAS No. 196711-63-4
项目整合开发状态: Preclinical
项目研究机构: University of Maryland (Originator), Genta (Licensee)
合成路线:Claisen condensation o...
参考文献标题:17-Imidazolyl,pyrazolyl,and isoxazolyl androstene derivatives,novel steroidal inhibitors of human cytochrome C17,20-lyase (P45017alpha)
文献作者:Ling,Y.; Li,J.S.; Liu,Y.; Kato,K.; Klus,G.T.; Brodie,A.
参考来源:J Med Chem 1997,40(20),3297

KF-22678

Chemical Name: [alpha(R),2R,7Z,9E,12R,13E,17R(R),20S]-alpha-Hydroxy-alpha,2,14-trimethyl-11,19-dioxo-12-[tetrahydropyran-2(R)-yloxy]-4,20-dithia-1,21-diazatricyclo[15.2.1.1(3,6)]heneicosa-3(21),5,7,9,...
参考文献标题:DC107 derivs.
文献作者:Kanda,Y.; Saitoh,Y.; Saito,H.; Ashizawa,T.; Sugiyama,K.; Gomi,K.; Kakita,S.; Takahashi,Y.; Murakata,C.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0786462; US 5733924; WO 9700260

新产品编号:283687

Chemical Name: 5-(4-Aminophenyl)-8,9-dihydro-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-8-one
CAS No. 197368-49-3
项目整合开发状态: Preclinical
项目研究机构: Acea (Originator)
合成路线:Esterification of 3,4-(m...
参考文献标题:Substd.2,3-benzodiazepin-4-ones and the use thereof
文献作者:Xia,H.; Field,G.; Lan,N.C.; Wang,Y.(Acea Pharmaceuticals)
参考来源:EP 1021418; JP 2000506890; US 5891871; WO 9734878

HMR-3787

Chemical Name: 11-Deoxy-3-des(hexopyranosyloxy)-2-fluoro-11-[4-(3H-imidazo[4,5-b]pyridin-3-yl)butylamino]-6-O-methyl-3-oxoerythromycin A 11-N,12-O-cyclic carbamate
CAS No. 193752-39-5
项目整合开发状态: ...
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

XV-454

Chemical Name: 3-[2-[3-(4-Amidinophenyl)-4,5-dihydroisoxazol-5(R)-yl]acetamido]-2(S)-(3-methylphenylsulfonamido)propionic acid; 3-[2-[3-(4-Amidinophenyl)-4,5-dihydroisoxazol-5(R)-yl]acetamido]-N-(3-me...
参考文献标题:Novel isoxazoline and isoxazole fibrinogen receptor antagonists
文献作者:Wityak,J.; Xue,C.-B.; Sielecki-Dzurdz,T.M.; Olson,R.E.; Degrado,W.F.; Cain,G.A.(DuPont Pharmaceuticals Co.)
参考来源:EP 0730590; EP 0832076; JP 1997505590; JP 1999504651; US 5849736; WO 9514683; WO 9638426