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

FR-193879

(6R,7R)-3-[4-(氨甲酰甲基)噻唑-2-酰磺酰]-7-(2-苯乙酰胺)-3-头孢氨-4-羧酸Chemical Name: (6R,7R)-3-[4-(Carbamoylmethyl)thiazol-2-ylsulfanyl]-7-(2-phenylacetamido)-3-cephem-4-carboxylic acid
CAS No. 194928-82-0
项目整合开发状...
参考文献标题:New cephem cpds.and pharmaceutical use thereof
文献作者:Yoshida,Y.; Okuda,S.; Sasaki,H.; Matsuda,K.; Takasugi,H.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0882052; JP 2000505432; WO 9729111

FK-089

(6R,7R)-7-[[(2Z)-2-(羧甲氧基亚基)-2-(1,3-噻唑-4-基)乙酰]氨基]-8-氧基-5-硫-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸Chemical Name: (6R,7R)-7-[(Z)-2-(4-Thiazolyl)-2-(carboxymethoxyimino)acetamido]-8-oxo-5-thia-1-azabicyclo[4.2.0] oct-2-...
参考文献标题:Cephem compounds
文献作者:Takaya,T.; Takasugi,H.; Yamanaka,H.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0071891; US 4515788; US 4649136; US 4736039

Annamycin LF(lipid formulation), Annamycin, AR-522

(7S,9S)-7-[(2R,3R,4R,5R,6S)-4,5-二羟基-3-碘-6-甲基氧杂环己-2-基]氧基-6,9,11-三羟基-9-(2-羟基乙酰基)-8,10-二氢-7H-并四苯-5,12-二酮Chemical Name: 3'-Deamino-4-demethoxy-4'-epi-3'-hydroxy-2'-iododoxorubicin; (7S,9S)-4-Demethoxy-7-O...
参考文献标题:4-Demethoxy-3'-desamino-2'-haloanthracycline and pharmaceutical compsn
文献作者:Horton,D.; Priebe,W.(Ohio State University)
参考来源:US 4537882

Talampanel, IDR-53773, GYKI-53773, LY-300164, Kinampa, Ampanel

(8R)-7-乙酰基-5-(4-氨基苯基)-8,9-二氢-8-甲基-7H-1,3-二氧杂环戊烯并[4,5-H][2,3]苯并二氮杂卓Chemical Name: 7-Acetyl-5-(4-aminophenyl)-8(R)-methyl-8,9-dihydro-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine
CAS No. 161832-65-1
项...
参考文献标题:N-Acyl-2,3-benzodiazepine derivs.,pharmaceutical compsns.containing them and process for preparing same
文献作者:Andrasi,F.; Berzsenyi,P.; Botka,P.; Farkas,S.; Goldschmidt,K.; Hamori,T.; Korosi,J.; Moravcsik,I.; Tarnawa,I.(Gyogyszerkutato Intezet Kft.)
参考来源:EP 0492485; JP 1993070463; US 5519019; US 5521174; US 5536832; US 5604223; US 5639751

Sabcomeline hydrochloride, CEB-2424, BRL-55473, SB-202026A, Memric

(8R)-N-甲氧基-1-氮杂双环[2.2.2]辛烷-8-甲醛肟氰化物盐酸盐Chemical Name: (+)-2(Z)-(Methoxyimino)-2-[quinuclidin-3(R)-yl]acetonitrile hydrochloride
CAS No. 159912-58-0, 151433-83-9 ((E)-isomer free base), 151433-82-8 (...
参考文献标题:Novel cpds
文献作者:Orlek,B.S.; Bromidge,S.M.; Dabbs,S.(SmithKline Beecham plc)
参考来源:AU 9053159; EP 0392803; JP 1991007285; JP 1997188678; JP 1997188679; US 5278170

NKS-01

(8R,9S,10R,13S)-14-羟基-10,13-二甲基-2,7,8,9,11,12,15,16-八氢-1H-环戊二烯并[a]菲-3,6,17-三酮Chemical Name: 14alpha-Hydroxy-4-androstene-3,6,17-trione
CAS No. 120051-39-0
项目整合开发状态: Phase II
项目研究机构: Nippon Ka...
参考文献标题:Novel androst-4-ene-3,17-dione derivs.and process for their preparation
文献作者:Yoshihama,M.; Tamura,K.; Miyata,N.; Nakayama,S.; Nakakoshi,M.(Snow Brand Milk Products Co.,Ltd.)
参考来源:JP 1988192794; JP 1988192795; JP 1988192796; JP 1988192797; US 4975368; WO 8805781

Tosagestin, ORG-30659

(8R,9S,10R,13S,14S,17R)-17-乙炔基-17-羟基-13-甲基-11-亚甲基-2,6,7,8,9,10,12,14-八氢-1H-环戊二烯并[a]菲-3-酮Chemical Name: 17alpha-Ethynyl-17beta-hydroxy-11-methyleneestra-4,15-dien-3-one; (17alpha)-17-Hydroxy-11-methyle...
参考文献标题:Novel 11-methylene-oestr-15-enes,processes for their preparation,and pharmaceutical compsns.
文献作者:Bergink,E.W.(Akzo Nobel N.V.)
参考来源:AU 8660162; EP 0210678; ES 8802233; JP 1987030799; US 5236913

NSC-378901, IDX, I-DOX, FCE-21954, Iodo-Dox

(8S,10S)-10-(2R,4S,5S,6S)-4-氨基四氢-5-碘-6-甲基-2H-吡喃-2-基氧基-7,8,9,10-四氢-6,8,11-三羟基-8-(羟基乙酰基)-1-甲氧基-5,12-并四苯醌Chemical Name: 4'-Deoxy-4'-iododoxorubicin
CAS No. 83997-75-5
项目整合开发状态: Phase II
项目研究机构: ...
参考文献标题:4'-Iododerivatives of anthracycline glycosides
文献作者:Suarato,A.; Penco,S.; Casazza,A.M.; Arcamone,F.(Pharmacia Corp.)
参考来源:BE 0892943; DE 3214559; FR 2525225; GB 2118540; JP 58183698; US 4438105

Etiprednol dicloacetate, BNP-166, Respicort, Ethinase, Cronaze

(8S,9S,10R,11S,13S,14S)-17-(2,2-二氯乙酰基)氧基-11-羟基-10,13-二甲基-3-氧代-7,8,9,11,12,14,15,16-八氢-6H-环戊[a]菲-17-羧酸乙酯Chemical Name: (11beta,17alpha)-17-(2,2-Dichloroacetoxy)-11-hydroxy-3-oxoandrosta-1,4-diene-17-ca...
参考文献标题:Androstene derivs.
文献作者:Bodor,N.S.(Soft Drugs,Inc.)
参考来源:WO 9742214

TPI

(9CI)-5-氯-6-[(2-亚氨基-1-吡咯烷)甲基]-2,4(1H,3H)-嘧啶二酮盐酸盐替吡嘧啶杂质 Chemical Name: 5-Chloro-6-(2-iminopyrrolidin-1-ylmethyl)-1,2,3,4-tetrahydropyrimidine-2,4-dione hydrochloride; 5-Chloro-6-(2-iminopyrrolidin-1-y...
参考文献标题:Uracil derivs.,and antitumor effect potentiator and antitumor agent containing the same
文献作者:Yano,S.; Tada,Y.; Kazuno,H.; Sato,T.; Yamashita,J.; Suzuki,N.; Emura,T.; Fukushima,M.; Asao,T.(Taiho Pharmaceutical Co.,Ltd.)
参考来源:EP 0763529; US 5744475; WO 9630346