(20 s, 5 @ )-20-(3 @ -isopropylthiazole-5 @ -yl)-6 @ - methoxy-3 @ , 5-cyclo-5 @ -pregnan as an intermediate in the synthesis of (22 r, 23r)-3 @ -acetoxy-22,23 - isopropylidenedioxy-24-metalholic-5-ene
(57) Abstract:Use: an intermediate in the synthesis of known fotograma-brassinolide) Entity: product - (20 S. 5) -20-(3 - isopropylthiazole-5-yl) -b/3-methoxy -. 5-cyclo-5A - pregnan Output 90% BF With N N0. Reagent 27 43 2 I)-20-formyl - 6(3-methoxy -. 5-cyclo-5A - pregnan Reagent 2: reagent Wittig Reagent 3: isobutyronitrile in the presence of utility reaction Conditions: in the midst of tetrahydrofuran
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to the substituted 4-benzylaminoquinolines and their heteroanalogs of the general formula (I): P-L-G (I) wherein G means compound of the formula: G(I) wherein K means -OR(7), -NH-CH2-CH2-SO3H, -NH-CH2-CO2H wherein R(7) means hydrogen atom, CH3; R1-R6 mean independently of one another hydrogen atom, -OR(10), -R(10) being one of residues R1-R6 means a bond with L always; R(10) means hydrogen atom, (C1-C4)-alkyl; L means (C1-C15)-alkyl being one or some structural CH2-fragments can be replaced for -C≡C-, -NR(11)-, -CO-, -O- wherein R(11) means hydrogen atom; P means: or wherein A means nitrogen atom (N); B means CH; D means CH; E means CH; R16-R24 mean independently of one another hydrogen atom, F, Cl atoms, (C1-C4)-alkyl being alkyl residues can be mono- or multiple-substituted with fluorine atom, NR(25)R(26), OR(25), COR(25), COOR(25), CONR(25)R(26) being one of residues R16-R(24) means a bond with L always; R25 and R26 mean independently of one another hydrogen atom, (C1-C4)-alkyl or benzyl. Also, invention relates to their pharmaceutically acceptable salts. Also, invention relates to a method for their preparing and to a drug based on thereof for prophylaxis of supersaturation of bile with cholesterol. Invention provides preparing new compounds and a drug based on thereof that can be used for prophylaxis and treatment of patients suffering with gallstones.
EFFECT: improved preparing method, valuable medicinal properties of compounds and drugs.
10 cl, 32 ex
FIELD: organic chemistry, steroids, biology.
SUBSTANCE: invention relates to steroid compounds of the general formula (X):
wherein in fragment of the formula XA:
each bond between C6 and C7, between C7 and C8, between C8 and C9, between C8 and C14 and between C14 and C15 is a single or double bond under condition that each atom C6, C7, C8, C9, C14 and C15 is bound with adjacent C-atom by a single bond or one double bond; CR3 means -CHOH; A means methylene or ethylene group; R4 and R4' mean (C1-C4)-alkyl, hydrogen atom (H); R20 means (C1-C4)-alkyl; R23 and R23' mean in common piperidine-1-yl, morpholine-4-yl, pyrrolidine-1-yl, piperazinyl possibly substituted with -OH, benzene, pyridine, pyrimidine, phenyl, alkoxycarbonyl group, or R23 means H and R23' means substituted alkyl. These compounds can be used for stimulation of meiosis in human oocytes. In proposed compounds steroid differs specifically as nitrogen atom of amino-group is bound with C17-atom of steroid skeleton by spacer A.
EFFECT: improved methods of synthesis, valuable biological properties of compounds.
16 cl, 8 dwg, 2 tbl, 30 ex
SUBSTANCE: invention concerns (a) new compounds of the formula I: , where M is a macrolipid subunit (macrolipid group) obtained from a macrolipid inclined to accumulation in inflamed cells, S is a steroid subunit (steroid group) obtained from a steroid medicine with anti-inflammatory effect, and L is a linker molecule connecting M and S; (b) their pharmacologically acceptable salts, prodrugs and solvates; (c) methods and mediators for their obtaining; and (d) methods of their application in treatment of human and animal inflammation diseases and conditions. The claimed compounds are inhibiting many cytokines and immune mediators participating in immune reactions that cause inflammation, allergy or alloimmunity, including IL (interleukin)-1, 2, 4, 5, 6, 10, 12, GMCSF (Granulocyte Macrophage Colony Stimulating Factor), ICAM (Intercellular Adhesion Molecule) and TNF (tumour necrosis factor) - α without limitation. At that, antiinflammation steroids have immediate anti-inflammatory effect due to the link to glycocorticosteroid receptor.
EFFECT: application in treatment of human and animal inflammation diseases and conditions.
30 cl, 40 ex, 4 dwg
SUBSTANCE: description is given of thiomorpholine derivatives of steroids with general formula I . These steroids are characterised by presence of a thiomorpholine fragment, bonded to a C17 steroid skeleton through an alkylene spacer, where R4 and R4' are hydrogen and methyl, under the condition that, both R4 and R4' represent hydrogen at the same time.
EFFECT: invention can be successfully used for stimulating meiosis of human oocyte.
12 cl, 2 ex, 5 tbl, 6 dwg
SUBSTANCE: present invention relates to steroids with (11β)-[4-(aza-aryl)phenyl] substitutes which modulate progesterone receptors, or pharmaceutically acceptable salts and/or hydrated form, and/or prodrug thereof.
EFFECT: compounds exhibit combined activity profile of PR agonist and PR antagonist which makes them suitable for contraception and treating gynaecological disorders.
30 cl, 28 ex, 1 tbl
SUBSTANCE: invention describes substituted derivatives of steroids which are selective inhibitors of type I 17β-hydroxysteroid dehydrogenase 17β-HSD1 and which can also be steroid sulphatase inhibitors, as well as salts thereof, pharmaceutical agents containing said compounds. The invention also describes use of said novel substituted derivatives of steroids for treatment, especially their use in treating or preventing steroid hormone dependent diseases or disorders, such as those for which inhibition of the 17β-HSD1 and/or STS is necessary and/or for which reduction of concentration of endogenic 17β-oestradiol is necessary.
EFFECT: more effective treatment.
35 cl, 164 ex, 19 tbl
SUBSTANCE: invention relates to a novel chemical compound and specifically to N-ethylpiperazylamide of betulinic acid of formula (I): which can be used in medicine as a medicinal agent with antitumour activity.
EFFECT: high efficiency of the compounds.
1 cl, 6 ex, 3 tbl, 2 dwg
SUBSTANCE: invention relates to substituted extratriene derivatives of general formula (values of radicals are given in the claim), useful in therapy, especially for treating and/or preventing steroid hormone-dependent disorders which require inhibition of 17β-hydroxysteroid dehydrogenase (17-HSD) enzyme type 1, type 2 and/or type 3, as well as salts thereof, pharmaceutical preparations containing said compounds, as well as methods of producing said compounds.
EFFECT: improved method.
41 cl, 98 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a chemical compound, namely N-[3-oxo-lupano-28-yl]-morpholine of formula (1): possessing antitumour and antimetastatic activity and representing a corrector of hepatotoxic damages caused by a tumour process and cytostatic polychemotherapy, and may be applicable in medicine as a pharmaceutic agent for reducing manifestation of morphological liver damages accompanying oncological diseases, including as a part of the integrated antitumour therapy.
EFFECT: preparation of the chemical compound possessing antitumour and antimetastatic activity.
1 cl, 10 ex, 6 tbl, 3 dwg
SUBSTANCE: invention relates to a novel chemical compound and specifically to N-[3-oxo-lupano-28-yl]-piperidine of formula (1): having complex activity - anti-tumour, anti-metastatic, anti-inflammatory and cytoprotective activity. The compound is synthesised from dihydrobetulonic acid.
EFFECT: obtaining compounds for reducing proliferation and dissemination of malignant cells and relieving necrobiotic disorders in normal cells, arising under the influence of paraneoplastic processes and cytotoxic chemotherapy.
1 cl, 11 ex, 7 tbl, 4 dwg