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

NO-aspirin, m-NO-ASA, NO-ASA, NCX-4016

Chemical Name: 2-Acetoxybenzoic acid 3-(nitrooxymethyl)phenyl ester
CAS No. 175033-36-0, 190442-10-5 (deleted CAS)
项目整合开发状态: Phase II
项目研究机构: NicOx (Originator)
合成路线:Alternatively,coupling...
参考文献标题:Synthesis method of nitroxymethylphenyl esters of aspirin derivs.
文献作者:Garufi,M.; Del Soldato,P.(NicOx SA)
参考来源:WO 0044705

KT-6587, CEP-751

Chemical Name: 9(S),12(R)-Epoxy-10(S)-(hydroxymethyl)-10-methoxy-9-methyl-2,3,9,10,11,12-hexahydrodiindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one
CAS No. 156177-59-2
项目整合开发状...
参考文献标题:Synthetic process development of antitumor agent KT 6587,an indolocarbazole alkaloid K 252a derivative
文献作者:Kinugawa,M.; et al.
参考来源:Org Process Res Dev 1999,3(2),131

DU-125530

Chemical Name: 2-[4-[4-(7-Chloro-2,3-dihydro-1,4-benzodioxin-5-yl)piperazin-1-yl]butyl]-1,2-benzisothiazol-3(2H)-one 1,1-dioxide
CAS No. 161612-21-1 (diHCl), 161612-00-6 (monomesylate salt)
项目整合...
参考文献标题:2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors
文献作者:Regan,J.; Bruno,J.; McGarry,D.; Poli,G.; Hanney,B.; Bower,S.; Travis,J.; Sweeney,D.; Miller,B.; Souness,J.; Djuric,S.
参考来源:Bioorg Med Chem Lett 1998,8(19),2737

新产品编号:250465

Chemical Name: (?-(2R*,5Z,10S*,16R*)-10,2,10-(Epoxymetheno)-1-benz[b]azacyclododeca-5-ene-3,7-diyne-1-carboxylic acid 4-chlorophenyl ester
CAS No. 193094-12-1
项目整合开发状态: Preclinical
项目研究机构: Sa...
参考文献标题:Structure-activity relationships of cyclic enediynes related to dynemicin A-II.Synthesis and antitumor activity of 9- and 12-substituted enediynes equipped with aryl carbamate moieties
文献作者:Unno,R.; Michishita,H.; Inagaki,H.; Suzuki,Y.; Baba,Y.; Jomori,T.; Moku,M.; Nishikawa,T.; Isobe,M.
参考来源:Bioorg Med Chem 1997,5(5),903

新产品编号:242555

Chemical Name: N,N',N'',N'''-(1,4,8,11-Tetraazacyclotetradecan-1,4,8,11-tetrayl)tetrakis(pentane-1,5-diyl)tetrakis(N-benzylcarbamic acid tert-butyl ester)
CAS No. 192518-27-7
项目整合开发状态: Biologica...
参考文献标题:Design,synthesis and structure relationships of new N,N',N'',N'''-tetrakis (omega-amino alkyl) tetraazamacrocycles
文献作者:Trabaud,C.; Dessolin,J.; Camplo,M.; Hantz,O.; Zoulim,F.; Borel,C.; Meyer,M.; Pepe,G.; Chermann,J.-C.; Kraus,J.-L.
参考来源:Antivir Chem Chemother 1998,9(1),73-84

Tecadenoson , CVT-510

Chemical Name: N6-[3(R)-Tetrahydrofuranyl]adenosine; (2R,3R,4S,5R)-2-(Hydroxymethyl)-5-[6-[tetrahydrofuran-3(R)-ylamino]-9H-purin-9-yl]tetrahydrofuran-3,4-diol
CAS No. 204512-90-3, 204512-92-5 ((S)...
参考文献标题:N6 Heterocyclic substd.adenosine derivs.
文献作者:Lum,R.T.; Pfister,J.R.; Schow,S.R.; Wick,M.M.; Nelson,M.G.; Schreiner,G.F.(CV Therapeutics,Inc.)
参考来源:EP 0920438; EP 0992510; JP 2000501426; US 5789416; WO 9808855

BIBO-3304

Chemical Name: Nalpha-(2,2-Diphenylacetyl)-D-arginine 4-(ureidomethyl)benzylamide trifluoroacetate
CAS No. 191868-14-1
项目整合开发状态: Preclinical
项目研究机构: Boehringer Ingelheim (Originator)
合成路线:...
参考文献标题:Amino acid derivs.,pharmaceutical compsns.containing these cpds.and processes for preparing them
文献作者:Engel,W.; Eberlein,W.; Rudolf,K.; Doods,H.; Wieland,H.-A.; Willim,K.-D.; Entzeroth,M.; Wienen,W.(Dr.Karl Thomae GmbH)
参考来源:DE 19544687; EP 0885186; WO 9719911

新产品编号:229899

Chemical Name: 2'-(2-O-Acetyl-beta-D-glucopyranosyloxy)-3-(benzofuran-5-yl)-6'-hydroxypropiophenone
CAS No. 190777-97-0
项目整合开发状态: Preclinical
项目研究机构: Tanabe Seiyaku (Originator)
合成路线:React...
参考文献标题:Na+-glucose cotransporter inhibitors as antidiabetics.I.Synthesis and pharmacological properties of 4'-dehydroxyphlorizin derivatives based on a new concept
文献作者:Tsujihara,K.; Hongu,M.; Saito,K.; Inamasu,M.; Arakawa,K.; Oku,A.; Matsumoto,M.
参考来源:Chem Pharm Bull 1996,44(6),1174

VA-033

Chemical Name: (13aalpha,13balpha)-8-Acetyl-13a-ethyl-2,3,5,6,13a,13b-hexahydro-1H-indolo[3,2,1-de]pyrido[3,2,1-ij][1,5]naphthyridine-12-carboxylic acid hexyl ester
CAS No. 121658-88-6
项目整合开发状态:...
参考文献标题:Vincaminic acid derivs.
文献作者:Nakatsuka,S.-I.; Hayashi,M.; Yokomori,S.; Nakashima,Y.; Hatayama,K.; Araki,H.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0307167; JP 1989156977; US 4883875

新产品编号:112831

Chemical Name: (3R,4S,5R,6R,8R,9R,10E,12E,15R)-5-[3,6-Dideoxy-4-O-(2,6-dideoxy-3-O,3-C-dimethyl-4-O-pentanoyl-alpha-L-altropyranosyl)-3-(dimethylamino)-beta-D-glucopyranosyloxy]-6-(formylmethyl)-3,9-d...
参考文献标题:16-Membered macrolide derivs.and process for producing the same
文献作者:Ajito,K.; Hara,O.; Kurihara,K.; Kikuchi,N.; Araake,M.; Shimizu,A.; Okonogi,T.; Inouye,S.; Shibahara,S.(Meiji Seika Kaisha,Ltd.)
参考来源:EP 0633266; JP 1995025894; JP 1995309889; JP 1995330791; JP 1996012696; US 5602106