其它产品项目整合

项目整合的本质是一项集合成方法学、反应工程学与过程分析技术于一体的系统工程。其核心逻辑可以概括为以下几点：源头优选：利用如N-硝胺化学等底层方法学突破，从分子层面颠覆传统高成本、高污染路线。过程强化：依托连续流技术，攻克有机金属试剂应用、光化学反应放大等“不可能”任务，实现高危工艺的本质安全。系统集成：整合“反应-淬灭-分离”全流程，利用微流控与在线分析技术，消除批次间的差异，实现药品制造的连续化与智能化。当前，中间体工艺研发正在经历从“经验驱动”向“数据驱动”的转变。AI辅助路线设计、自动化高通量筛选与连续制造平台的结合，将使得“分子结构与最优工艺路径”之间的映射关系逐渐清晰。未来的竞争优势，将属于那些能够将底层化学创新与先进工程技术进行无缝整合的研发体系。
备注: 根据相关法律法规, 本站点不显示有法律约束管制的产品, 如有遗漏, 请自行鉴别,或提交我们及时更新撤除.
如有产品相关项目调研推广服务, 请致函联系我们

客户展示

其它产品项目整合

TPMPA CAS Registry Number: 182485-36-5 (1,2,5,6-四氢吡啶-4-基)甲基磷酸

CAS Name: Methyl (1,2,3,6-tetrahydro-4-pyridinyl)phosphinic acid
Additional Names: (1,2,5,6-tetrahydropyridine-4-yl)methylphosphinic acid
Percent Composition: C 44.72%, H 7.51%, N 8.69%, O 1...
Literature References: Selective antagonist for GABAc receptors. Prepn: Y. Murata et al., Bioorg. Med. Chem. Lett. 6, 2073 (1996); R. Miledi et al., US 5627169 (1997 to Univ. California). Design and in vitro pharmacology: D. Ragozzino et al., Mol. Pharmacol. 50, 1024 (1996). Specificity vs human receptors and alternate synthesis: M. Chebib et al., Eur. J. Pharmacol. 357, 227 (1998). Use as antagonist: A. Rozzo et al., Neuroscience 90, 1085 (1999).

Formestane CAS Registry Number: 566-48-3 4-雄烯-4-醇-3,17-二酮

CAS Name: 4-Hydroxyandrost-4-ene-3,17-dione
Additional Names: 4-OHATrademarks: Lentaron (Novartis)
Percent Composition: C 75.46%, H 8.67%, O 15.87%
Literature References: Selective aromatase inhibitor. Prepn: R. D. Burnett, D. N. Kirk, J. Chem. Soc. Perkin Trans. 1 1973, 1830; J. Mann, B. Pietrzak, ibid. 1983, 2681; P. G. Ciattini et al., Synth. Commun. 22, 1949 (1992). Aromatase inhibition and effect on estrogen-dependent processes in vivo: A. M. H. Brodie et al., Endocrinology 100, 1684 (1977). Radioimmunoassay in plasma: J. Khubieh et al., J. Steroid Biochem. 35, 377 (1990). GC determn in plasma and urine: P. H. Degen, W. Schneider, J. Chromatogr. 565, 67 (1991). Pharmacokinetics and endocrine effects in breast cancer patients: M. Dowsett et al., Eur. J. Cancer 28, 415 (1992). Clinical evaluation in breast cancer: R. C. Coombes, J. Steroid Biochem. Mol. Biol. 43, 145 (1992).

Talinolol CAS Registry Number: 57460-41-0 他林洛尔

CAS Name: N-Cyclohexyl-N'-[4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]phenyl]urea
Additional Names: 1-(4-cyclohexylureidophenoxy)-2-hydroxy-3-tert-butylaminopropane; (±)-1-[p-[3-(ter...
Literature References: Selective b1-adrenergic blocker structurally related to practolol, q.v. Prepn: R. Eckardt et al., DE 2153024 (1972 to Arzneimittelwerke VEB), C.A. 77, 61639b (1972); idem et al., Pharmazie 30, 633 (1975). Series of articles on pharmacology, toxicology: ibid. 638-683. Acute toxicity: K. Femmer et al., ibid. 642. Clinical pharmacokinetics and bioavailability: B. Trausch et al., Biopharm. Drug Dispos. 16, 403 (1995). Review of clinical experience: I. Assmann, Curr. Med. Res. Opin. 13, 325-342 (1995).

Formoterol CAS Registry Number: 73573-87-2 福莫特罗

CAS Name: rel-N-[2-Hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]phenyl]formamide
Additional Names: 3-formylamino-4-hydroxy-a-[N-[1-methyl-2-(p-methoxyphenyl)...
Literature References: Selective b2-adrenergic receptor agonist. Mixture of R,R (-) and S,S (+) enantiomers. Prepn: M. Murakami et al., DE 2305092; eidem, US 3994974 (1973, 1976 both to Yamanouchi); K. Murase et al., Chem. Pharm. Bull. 25, 1368 (1977). Absolute configuration and activity of isomers: eidem, ibid. 26, 1123 (1978). Toxicity studies: T. Yoshida et al., Pharmacometrics 26, 811 (1983). HPLC determn in plasma: J. Campestrini et al., J. Chromatogr. B 704, 221 (1997). Review of pharmacology: G. P. Anderson, Life Sci. 52, 2145-2160 (1993); and clinical efficacy: R. A. Bartow, R. N. Brogden, Drugs 55, 303-322 (1998).

Ivabradine CAS Registry Number: 155974-00-8 伊伐雷定

CAS Name: 3-[3-[[[(7S)-3,4-Dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one
Additional Names: 7,8-dimethoxy-3-[3-[[...
Literature References: Selective bradycardic agent with direct effect on the pacemaker If current of the sinoatrial node. Prepn: J.-L. Peglion et al., EP 534859; eidem, US 5296482 (1993, 1994 both to ADIR). In vitro electrophysiological effects: C. Thollon et al,. Br. J. Pharmacol. 112, 37 (1994). LC-MS determn in plasma: M. François-Bouchard et al., J. Chromatogr. B 745, 261 (2000). Clinical pharmacokinetics: I. Ragueneau et al., Clin. Pharmacol. Ther. 64, 192 (1998). Clinical trial in stable angina: J. S. Borer et al., Circulation 107, 817 (2003). Series of articles on pharmacology and clinical experience: Eur. Heart J. Suppl. 5, Suppl. G, G26-G56 (2003). Review of mechanism of action: D. DiFrancesco, J. A. Camm, Drugs 64, 1757-1765 (2004).

Valdecoxib CAS Registry Number: 181695-72-7 伐地考昔

CAS Name: 4-(5-Methyl-3-phenyl-4-isoxazolyl)benzenesulfonamideTrademarks: Bextra (Pharmacia Upjohn)
Percent Composition: C 61.13%, H 4.49%, N 8.91%, O 15.27%, S 10.20%
Literature References: Selective cyclooxygenase-2 (COX-2) inhibitor. Active metabolite of parecoxib, q.v. Prepn: J. J. Talley et al., WO 9625405 (1996 to Searle); eidem, US 5633272 (1997); and activity: eidem, J. Med. Chem. 43, 775 (2000). Chromatographic determn of purity: D. A. Roston et al., J. Pharm. Biomed. Anal. 26, 339 (2001). Gastrointestinal tolerability study: G. M. Eisen et al., Aliment. Pharmacol. Ther. 21, 591 (2005). Clinical trial in hip arthroplasty: F. Camu et al., Am. J. Ther. 9, 43 (2002). Clinical comparison with oxycodone/acetominophen in dental pain: S. E. Daniels et al., J. Am. Dent. Assoc. 133, 611 (2002). Clinical trial in migraine: D. Kudrow et al., Headache 45, 1151 (2005). Review of clinical experience: M. Goldman, S. Schutzer, Formulary 37, 68-77 (2002); of clinical efficacy and safety: G. P. Joshi, Expert Rev. Neurother. 5, 11-24 (2005).

Etoricoxib CAS Registry Number: 202409-33-4 依托考昔

CAS Name: 5-Chloro-6'-methyl-3-[4-(methylsulfonyl)phenyl]-2,3'-bipyridine
Additional Names: 5-chloro-3-(4-methylsulfonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridineTrademarks: Arcoxia (Merck Co.)<...
Literature References: Selective cyclooxygenase-2 (COX-2) inhibitor. Prepn: D. Dube et al., WO 9803484; eidem, US 5861419 (1998, 1999 both to Merck Frosst); R. W. Friesen et al., Bioorg. Med. Chem. Lett. 8, 2777 (1998). Practical synthesis: I. W. Davies et al., J. Org. Chem. 65, 8415 (2000). HPLC determn in urine and plasma: C. Z. Matthews et al., J. Chromatogr. B 751, 237 (2001). Pharmacology: D. Riendeau et al., J. Pharmacol. Exp. Ther. 296, 558 (2001); A. Dallob et al., J. Clin. Pharmacol. 43, 573 (2003). Clinical comparison with indomethacin in acute gouty arthritis: H. R. Schumacher, Jr. et al., Br. Med. J. 324, 1488 (2002). Clinical trial in rheumatoid arthritis: A. K. Matsumoto et al., J. Rheumatol. 29, 1623 (2002); in osteoarthritis: S. P. Curtis et al., BMC Musculoskel. Disord. 6, 58 (2005); in ankylosing spondylitis: D. van der Heijde et al., Arthritis Rheum. 52, 1205 (2005). Gastrointestinal safety profile in inflammatory bowel diseases: Y. El Miedany et al., Am. J. Gastroenterol. 101, 311 (2006). Review of pharmacology and clinical development: P. Patrignani et al., Expert Opin. Pharmacother. 4, 265-284 (2003).

Celecoxib CAS Registry Number: 169590-42-5 塞来昔布

CAS Name: 4-[5-(4-Methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamideTrademarks: Celebrex (Pfizer); Onsenal (Pfizer)
Percent Composition: C 53.54%, H 3.70%, F 14.94%, N 11.02%,...
Literature References: Selective cyclooxygenase-2 (COX-2) inhibitor. Prepn: J. J. Talley et al., WO 9515316; eidem, US 5466823 (both 1995 to Searle); T. D. Penning et al., J. Med. Chem. 40, 1347 (1997). Clinical pharmacology: P. E. Lipsky, P. C. Isakson, J. Rheumatol. 24, Suppl. 49, 9 (1997). Clinical trials in arthritis: L. S. Simon et al., Arthritis Rheum. 41, 1591 (1998). Evaluation of risk of gastrointestinal toxicity in patients with arthritis: F. E. Silverstein et al., J. Am. Med. Assoc. 284, 1247 (2000). Clinical trial in familial adenomatous polyposis: G. Steinbach et al., N. Engl. J. Med. 342, 1946 (2000).

Deracoxib CAS Registry Number: 169590-41-4 地拉考昔

CAS Name: 4-[3-(Difluoromethyl)-5-(3-fluoro-4-methoxyphenyl)-1H-pyrazol-1-yl]benzenesulfonamideTrademarks: Deramaxx (Novartis)
Percent Composition: C 51.38%, H 3.55%, F 14.34%, N 10.57%, O 12.0...
Literature References: Selective cyclooxygenase-2 (COX-2) inhibitor. Prepn: J. J. Talley et al., WO 9515316; M. J. Graneto, US 5521207 (1995, 1996 both to Searle); T. D. Penning et al., J. Med. Chem. 40, 1347 (1997). Structure activity study: G. R. Desiraju et al., Molecules 5, 945 (2000). Effect in experimental synovitis in dogs: D. L. Millis et al, Vet. Ther. 3, 453 (2002); HPLC determn in plasma: S. K. Cox et al., J. Chromatogr. B 819, 181 (2005).

Lumiracoxib CAS Registry Number: 220991-20-8 罗美昔布

CAS Name: 2-[(2-Chloro-6-fluorophenyl)amino]-5-methylbenzeneacetic acid
Additional Names: 5-methyl-2-(2'-chloro-6'-fluoroanilino)phenylacetic acidTrademarks: Prexige (Novartis)
Percent Compo...
Literature References: Selective cyclooxygenase-2 (COX-2) inhibitor. Prepn: R. A. Fujimoto et al., WO 9911605; eidem, US 6310099 (1999, 2001 both to Novartis). Clinical evaluation of gastroduodenal tolerability: C. Rordorf et al., Aliment. Pharmacol. Ther. 18, 533 (2003). Clinical experience in dysmenorrhea: M. Bitner et al., Int. J. Clin. Pract. 58, 340 (2004); in rheumatoid arthritis: P. Geusens et al. ibid. 1033; in tension headache: E. Packman et al., Headache 45, 1163 (2005). Review of clinical pharmacology: C. M. Rordorf et al., Clin. Pharmacokinet. 44, 1247-1266 (2005); of clinical experience in osteoarthritis: F. Berenbaum et al., J. Int. Med. Res. 33, 21-41 (2005); in osteoarthritis, rheumatoid arthritis, and dental pain: T. J. Schnitzer et al., Curr. Med. Res. Opin. 21, 151-161 (2005).