专利号:EP-1641812-B1 优先权日:2003-06-30 标题 :PURE d-(17alpha)-13-ETHYL-17-HYDROXY-18,19-DINORPREGN-4-ENE-20-YNE-3-ONE-3E- AND -3Z-OXIME ISOMERS, AS WELL AS PROCESS FOR THE SYNTHESIS OF THE MIXTURE OF ISOMERS AND THE PURE ISOMERS 发明人:TUBA ZOLTAN; MAHO SANDOR; KESERU GYOERGY; KOZMA JOZSEF; HORVATH JANOS; BALOGH GABOR 权利人:RICHTER GEDEON NYRT 摘要:The invention relates to the pure d-(17alpha)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-Â20-yne-3-one-3E-oxime isomer of formula (IA), the pure d-(17alpha)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yne-3-one-3Z-oxime isomer of formula (IB), which are of gestagen activity, as well as the process for the synthesis of the mixture of the above isomers and the pure isomers. The invention also relates to the pharmaceutical compositions - and the process for their synthesis - which contain either the pure isomer of formula (IA) or the pure isomer of formula (IB) as active ingredient as such or in combination with other active ingredients (for example an oestrogen agent) together with pharmaceutical auxiliary materials commonly used in practice.
专利号:US-6448413-B1 优先权日:1999-06-10 标题:Process for the synthesis of a-nor-seco compounds with sterane skeleton 发明人:SANTA CSABA; TUBA ZOLTAN; MAHO SANDOR; SZELES JANOS; BALOGH GABOR; BRLIK JANOS; TRISCHLER FERENC; SZILAGYI GABRIELLA; BAKCSI ERIKA 权利人:RICHTER GEDEON VEGYESZET 摘要:The invention relates to a new process for the synthesis of 17β-hydroxy-17α-methyl-1,3-seco-2-nor-5α-androstane-3-acid derivatives of formula (I) n wherein the meaning of Z is carboxyl or formyl group and n to the new secoindoxylidene carboxylic acid derivatives of formula (II) n wherein R 1 and R 2 independently are C 1 -C 4 alkyl or alkoxy group, hydrogen or halogen atom—which are intermediates for preparing the compounds of formula (I). n The 17β-hydroxy-17α-methyl-1,3-seco-2-nor-5α-androstane-3-acid derivatives of formula (I) are intermediates in the synthesis of oxandrolon (17β-hydroxy-17α-methyl-2-oxa-5α-androstane-3-one), which is used as anabolic in therapy.
专利号:US-9676814-B2 优先权日:2013-10-01 标题:Industrial process for the synthesis of ulipristal acetate and its 4′-acetyl analogue 发明人:Mahó Sándor; SÃ?NTA CSABA; Csörgei János; Horváth János; ARANYI ANTAL; BÉNI ZOLTÃ?N 权利人:RICHTER GEDEON NYRT 摘要:The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxolan-2-yl group) as starting material, as well as to the intermediate of the process.
专利号:US-8557979-B2 优先权日:2004-06-10 标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation 发明人:CHOI WOO-BAEG; KOWALIK EWA 权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC 摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.
专利号:WO-2004101594-A1 优先权日:2003-05-14 标题 :New mono-and bismethylene-steroid derivatives and process for their synthesis 发明人:TUBA ZOLTAN; DANCSI LAJOSNE; FRANCSICSNE CZINEGE ERZSEBET; FALKAY GYOERGY; ZUPKO ISTVAN; MARKI ARPAD; MOLNAR CSABA; CSOERGEI JANOS; DUKATNE ABROK VILMA; BALOGH GABOR; MAK MARIANNA 权利人:RICHTER GEDEON VEGYESZET; TUBA ZOLTAN; DANCSI LAJOSNE; FRANCSICSNE CZINEGE ERZSEBET; FALKAY GYOERGY; ZUPKO ISTVAN; MARKI ARPAD; MOLNAR CSABA; CSOERGEI JANOS; DUKATNE ABROK VILMA; BALOGH GABOR; MAK MARIANNA 摘要:The invention relates to new mono- and bismethylene-steroid derivatives of general formula (I) - wherein Z represents two hydrogen atoms or an oxo group; X and Y independently of each other represent either two hydrogen atoms of a CH2= group, with the restriction that at least one of them is CH2= group and if the meaning of Z is oxo group Y represents two hydrogen atoms, R represents a C1-C4 alkyl group, as well as the pharmaceutical compositions containing the above compounds as active ingredients, and the processes for the synthesis of active ingredients and pharmaceutical compositions. The invention also relates to the methods of treatments with these compounds, which means administering to a mammal to be treated with progestogen - including human - effective amount/amounts of the active ingredients of the present invention as such or as medicament. The mono- and bismethylene-steroid derivatives of the general formula (I) have progestogen effect. They can be used as active ingredients of contraceptive medicaments as such or in combination with an estrogen component. Furthermore, they can be used in the treatment of endometriosis and in the substitution therapy of estrogen as gestagen agent beside the estrogen component. The mono- and bismethylene-steroid derivatives of the general formula (I) of the present invention can be synthesized by reacting a compound of the general formula (II), - wherein the meaning of Z, X and Y is as described for the compounds of formula (I) - with an acid anhydride of the general formula (R-CO)2O or with an acid chloride of the general formula R-CO-Cl - wherein R represents a C1-C4 alkyl group - in the presence of a strong acid.
专利号:US-10933051-B2 优先权日:2017-06-09 标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections 发明人:CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN 权利人:FOB SYNTHESIS INC 摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
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