专利号:EP-1363951-B1 优先权日:2000-12-07 标 题 :Polynuclear complex fe(iii) with pullulan oligomers, process of its obtaining, and pharmaceutical preparations on the basis of the complex 发明人:ILIC LJUBOMIR; RISTIC SUZANA; CAKIC MILORAD; NIKOLIC GORAN; STANKOVIC SLOBODAN 权利人:AD ZDRAVLJE FARMACEUTSKO HEMIJ 摘要:A polynuclear complex of pullulan oligomers of formula (I): wherein n = (100-8200), obtained by process of synthesis of soluble pullulan with insoluble iron (III)-hydroxyde of formula (II): wherein n=(900). The process of synthesis is characterized by technical simplicity and economy. In accordance with suggested process, first of all, preparation of pullulan for synthesis, including its characterization (determination of RG, Mw, Mn, [θ]) is carried out, and subsequently its hydrogenation is carried out in order to eliminate reducing groups, iron(III)-hydroxyde gel is prepared, and synthesis of the complex can start. Obtained complex is afterwards prepared for pharmacological use and it is subjected to the subsequent physical and chemical processes of purification. The preparation obtained in such a way is used for prevention and treatment of syderopenic anemia in human and veterinay medicine.
专利号:US-2008045726-A1 优先权日:2004-05-10 标题 :Spirolactams and Their Synthesis 发明人:NOHEDA MARIN PEDRO; BERNABE PAJARES MANUEL; MAROTO QUINTANA SERGIO; TABARES CANTERO NURIA 权利人:ESTEVE LABOR DR 摘要:New spirolactams of formula (I) having a cycloexadienone moiety which are highly stable due to pi interactions between the W group and the dienone moiety. They are useful as UV absorbers and as intermediates for the synthesis of active biomolecules.
专利号:EP-1476441-B1 优先权日:2002-01-23 标题 :A method of eliminating sulfone analog in the synthesis of pyridine-benzimidazole sulfoxides 发明人:UENSAL SERAFETTIN 权利人:ULKAR KIMYA SANAYII VE TICARET 摘要:Process for the preparation of pyridine-benzimidazole sulfinyl compounds such as Omeprazole, Lansoprozole and Pantoprozole of general formula (I), wherein the ring A may optionally be substituted, R1 is hydrogen or an N-protecting group, each of R2, R3 and R4 represent (1) a hydrogen atom, (2) alkyl group which may be substituted with halogen atom(s) or (3) an alkoxy group which may be optionally substituted with halogen atom(s) or alkoxy; or its salt. Sulphone analogs of the corresponding compounds as impurity are formed during oxidation of the precursor thioether of the compèound of formula (I). A process is provided for the elimination of sulphone analogs in contaminated products. The purification process comprises treatment of semi-pure benzimidazole derivatives with solid K2CO3 in alcohol medium at elevated temperatures.
专利号:US-2009198084-A1 优先权日:2006-05-02 标题:Process for the deprotection of protected amines 发明人:ALSTERS PAULUS LAMBERTUS; VERKADE JORGE MERIJN MATHIEU; QUAEDFLIEG PETER JAN LEONARD MARIO; RUTJES FLORIS PETRUS JOHANNES 权利人:ALSTERS PAULUS LAMBERTUS; VERKADE JORGE MERIJN MATHIEU; QUAEDFLIEG PETER JAN LEONARD MARIO; RUTJES FLORIS PETRUS JOHANNES 摘要:The present invention relates to a process for the deprotection of protected amine compounds, wherein the protected amine compound is contacted with an electrophilic oxidating agent that is optionally formed in situ, said electrophilic oxidating agent being selected from the group of I 2 , Br 2 , Cl 2 and compounds comprising a halogen atom having a formal oxidation state of 1+, 3+, 5+ or 7+, provided that the electrophilic oxidating agent is not iodobenzene diacetate. The process can be conveniently employed in the synthesis of 1,3-amino alcohols, β-amino acids and heterocyclic compounds, in particular β-amino acids.
专利号:US-2012095211-A1 优先权日:2010-09-22 标 题 :Substituted proline inhibitors of hepatitis c virus replication 发明人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D 权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC 摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.
专利号:US-8030496-B2 优先权日:2005-02-17 标 题:Intermediate compound for synthesis of viridiofungin a derivative 发明人:KATO TATSUYA; KIMURA NOBUAKI; MIZUTANI AKEMI; MAKINO TOSHIHIKO; KAWASAKI KENICHI; FUKUDA HIROSHI; KOMIYAMA SUSUMU; TSUKUDA TAKUO 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:A method whereby a compound having HCV replication inhibitory activity and desired optical activity can be synthesized selectively and at high yield in a small number of steps by using a compound having a specific chiral auxiliary as a starting compound is provided. n A compound represented by the formula (1-8): n n n n n n n n n n n n wherein Y represents a group represented by the following formula: n n n n n n n n n n n n n n n n Q represents a protected carbonyl group; D represents —(CH 2 ) m —R′, etc.; and n represents an integer of 0 to 10.