ПРОИЗВОДНЫЕ ГИПЕРФОРИНА, ИХ ПРИМЕНЕНИЕ И СОДЕРЖАЩИЕ ИХ СОСТАВЫ

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention describes derivatives of hyperforin and adhyperforin of the formula (I): wherein R represents methyl or ethyl; R 2 represents hydrogen atom, lithium or dicyclohexyl ammonium cation, direct or branched (C 2 -C 5 )-acyl residue wherein alternatively: (a) R 1 represents 3-methylbut-1-yl, and oxo groups are in 1- and 10-positions; (b) R 2 represents 3-methyl-2-butene-1-yl, and hydroxy groups are in 1- and 10-positions; (c) R 1 represents 3-methylbut-1-yl, and hydroxy groups are in 1- and 10-positions. Compounds are used in preparing drugs for using in treatment of depression and Alzheimer's disease. Also, invention describes a pharmaceutical composition possessing anti-depressant effect. EFFECT: valuable medicinal properties of substances and pharmaceutical composition. 8 cl, 2 tbl, 6 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 320 636 (13) C2 (51) ÌÏÊ C07C C07C C07C A61K A61P 49/733 49/743 69/013 31/122 25/28 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2004131210/04, 18.04.2003 (72) Àâòîð(û): ÁÎÌÁÀÐÄÅËËÈ Ýöèî (IT), ÌÎÐÀÖÖÎÍÈ Ïàîëî (IT), ÐÈÂÀ Àíòîíåëëà (IT), ÔÓÄÇÀÒÈ Íèêîëà (IT) (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 18.04.2003 (73) Ïàòåíòîîáëàäàòåëü(è): ÈÍÄÅÍÀ Ñ.Ï.À. (IT) (43) Äàòà ïóáëèêàöèè çà âêè: 10.04.2005 R U (30) Êîíâåíöèîííûé ïðèîðèòåò: 23.04.2002 IT MI2002A000872 (45) Îïóáëèêîâàíî: 27.03.2008 Áþë. ¹ 9 2 3 2 0 6 3 6 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: WO 9964388 A1, 16.12.1999. WO 9941220 A1, 19.08.1999. (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 21.10.2004 2 3 2 0 6 3 6 R U (87) Ïóáëèêàöè PCT: WO 03/091194 (06.11.2003) C 2 C 2 (86) Çà âêà PCT: EP 03/04100 (18.04.2003) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Å.Å.Íàçèíîé, ðåã. ¹ 517 (54) ...

АНАЛОГИ ВИТАМИНА D, СОЕДИНЕНИЯ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Описываются новые аналоги витамина D общей формулы I, где значения R1, R2, R3, R4, R5, R'2, R'3, R'4, R'5, X, У, У' указаны в п.1 формулы, которые проявляют селективную активность в отношении клеточных функций. Описывается способ их получения и фармацевтическая композиция на основе соединений формулы I. 10 с. и 14 з.п. ф-лы, 5 ил., 3 табл.

1,2-1,4-Additions-Reaktionsschritt, der zu Diphenylacetylenen führt.

Glyoxyl-Cyclohexendione.

Verfahren zur Herstellung von Dicyclohexylaethanverbindungen

BICYCLOOCTANE COMPOUNDS, THEIR PRODUCTION, COMPOSITIONS CONTAINING THEM AND THEIR PHARMACEUTICAL USE

BITTER SUBSTANCES AND THEIR PREPARATION

... 1351524 Bitter substances WHITE TOMKINS Ltd 17 May 1972 [18 May 1971] 15660/71 Heading C2C A bitter substance is produced by treating #- acids with an alkali metal hypohalite under alkaline conditions in a polar solvent. The bitter substance is believed to have the formula where R is alkyl and X is halogen. The bitter substance may be treated with a weakly alkaline potassium salt to give the potassium salt of the bitter reaction product.

CYCLOPENTANE DERIVATIVES

... 1365173 2-Hydroxycyclopentaneacetic acid -lactones IMPERIAL CHEMICAL INDUSTRIES Ltd 10 Jan 1973 [4 Feb 1972] 5353/72 Heading C2C [Also in Division C3] The invention comprises 2-hydroxycyclopentaneacetic acid -lactones of the Formula XXIII: whereinX is ethylene or trans-vinylene; Z is Cl, Br or I; and R3 is C 1-10 alkyl, C 4-10 alkenyl, -A1.O.R4, -A2.R5 or -A3.A4.R6, wherein A1 is C 1-9 alkylene or C 5-7 cycloalkyl, provided that A1 and R4 together contain not more than 10 carbon atoms; A2 is C 2-3 alkylene, optionally bearing 1 or 2 C 1-4 alkyl substituents, R5 is aryl optionally substituted by halogen, NO 2 , C 1-3 alkyl, C 1-3 alkoxy, C 1-3 haloalkyl or di-(C 1-3 alkyl) amino; A3 is C 1-3 alkylene optionally bearing 1 or 2 C 1-3 alkyl substituents, A4 is O, S, SO or C 1-4 alkylimino; and R6 is aryl, benzyl or furfuryl optionally substituted by ...

Pesticidal oximes

A compound of formula I I in which formula: Ra represents hydrogen or a C1-C6 alkyl group, and Rc represents a C1-C6 alkyl group; Rb represents a phenyl group, optionally substituted by a C1-C6 alkyl group or halogen, a group of formula -CH=CRdRe in which Rd and Re, which may be identical or different represent hydrogen or C1-C6 alkyl groups or a group of formula -CH=NORf in which Rf represents hydrogen or a C1-C6 alkyl group and RCOO represents a residue of an acid RCO2H, which acid, or an ester-forming derivative of which acid, on reaction with alpha -cyano-3-phenoxybenzyl alcohol or an ester forming derivative thereof, gives rise to an alpha -cyano-3-phenoxybenzyl ester having pesticidal properties.

PROCESS FOR THE SYNTHESIS OF 3-KETO-CYCLOPENTENE-5-OXY DERIVATIVES HAVING INSECTICIDE ACTIVITY

PESTICIDES

CYCLOPENTENE DERIVATIVES

... 1310685 Cyclopentene derivatives M E VANDEWALLE 16 Nov 1970 [24 Nov 1969] 57302/69 Heading C2C Compounds of the formula where R1 is a primary aliphatic or aryl-substituted aliphatic group having a terminal methylene group and R2 is a C 1-5 alkyl group, are prepared by reacting compounds of the formula and HC(OR2) 3 in the presence of an acid catalyst, heating to evaporate HCOOR2 and recovering the compound of Formula I from the residue. The invention further comprises compounds of Formula I other than those wherein R1 is methyl, ethyl or 3-methylbutyl. The compounds may be reduced to compounds of the formula or reacted with an organometallic compound in which the group R3 is attached to a metal atom and hydrolysed to yield compounds of the formula where R3 is a saturated, unsaturated or aromatic hydrocarbon radical.

PROSTAGLANDIN ANALOGUES

PROSTACYCLIN DERIVATIVES THEIR USE AND PREPARATION

Preparation of carvone

Process for the preparation of carvone by heating 1-methyl-1-hydroxy -4-isopropenylcyclohexan-2- one at a temperature between 150 and 350 DEG C. The starting material may be obtained by reacting d-limonene with nitrosylsulphuric acid, hydrolysing the limonene nitrosulphate obtained to form 1-methyl-1-hydroxy-2-hydroxy- imino-4-isopropenyl-cyclohexane, and converting the latter compound into 1-methyl-1-hydroxy- 4-isopropenyl-cyclohexan-2-one.

PROCESS FOR THE STEREOSELECTIVE PREPARATION OF A PYRAZOLE CARBOXAMIDE

Process for the stereoselective preparation of a pyrazole carboxamide

Process for the stereoselective preparation of a pyrazole carboxamide

PROCEDURE FOR THE PRODUCTION OF NEW BICYCLOOCTANDERIVATEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN BICYCLOOCTANDERIVATEN

8 (NIEDERALKYL) BICYCLO (4.2.0>OCTANDERIVATE WITH VALUABLE THERAPEUTIC CHARACTERISTICS.

GLYOXYL CYCLOHEXENDIONE ONE.

(3.2.0) BICYCLOHEPTANON MORE OXIMAETHER, THE VALUABLE THERAPEUTIC CHARACTERISTICS POSSESSIONS.

NEW STRUCTURAL VITAMIN D OF DERIVATIVES

NEW STRUCTURAL VITAMIN D OF DERIVATIVES

PROSTAGLANDIN DERIVATIVES

Compositions comprising and processes for producing inorganic salts of hop acids

Compounds useful in the therapy of Alzheimer's disease and formulations containing them

Novel structural analogues of vitamin d

Ketone compounds and compositions for cholesterol management and related uses

PROCESS FOR THE MANUFACTURE OF HUMOLONES

NOVEL BICYCLIC CANNABINOID AGONISTS FOR THE CANNABINOID RECEPTOR

Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy.

4-Hydroxy-2-Cyclopentenone Derivative and Carcinostatic and Osteogenesis Promoter Containing the Same

PROCEDURE FOR THE PRODUCTION OF OXOCYCLOPENTENEN.

PROSTACYCLINDERIVATE, THEIR PRODUCTION AND THIS PROSTACYCLINDERIVATE ABSTENTION PHARMACEUTICAL PREPARATIONS.

NOVEL METHOD FOR THE SYNTHESIS OF THE 3 KETO 5 HYDROXY-CYCLOPENTEN.

BICYCLO (OF 3,3,0) OCTAN DERIVATIVES.

PROSTAGLANDIN ANALOGS, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.

СПОСОБ ПОЛУЧЕНИЯ АМИДОВ ПИРАЗОЛКАРБОНОВОЙ КИСЛОТЫ

The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methanonaphthalen-5-yl)amide.

ПРОИЗВОДНЫЕ ПОЛИГИДРОКСИФЕНОЛА, СОДЕРЖАЩИЕ ИХ ЛЕКАРСТВЕННЫЕ КОМПОЗИЦИИ И ПРИМЕНЕНИЕ УКАЗАННЫХ ВЕЩЕСТВ ДЛЯ ПРОФИЛАКТИКИ И ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ КОСТЕЙ И ХРЯЩЕЙ

DERIVATIVES OF POLYHYDRO KSIFENOLA, CONTAINING THEREOF MEDICINAL COMPOSITION AND USE OF SAID SUBSTANCES FOR PROPHYLAXIS AND TREATMENT OF DISEASES BONES AND CARTILAGES

METHOD OF PYRAZOLE CARBOXYLIC ACID AMIDES PREPARATION

СТАБИЛЬНЫЙ ЭКСТРАКТ ЗВЕРОБОЯ, СПОСОБ ЕГО ПРИГОТОВЛЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ СОСТАВЫ НА ЕГО ОСНОВЕ

Norditerpenoid compound as well as preparation method and application thereof

Cyclopentanone derivs. - useful in perfume and toilet prepn.s

CYCLOPENTANE DERIVATIVES

PROCESS FOR the PREPARATION Of HUMULONES

PROCESS OF SYNTHESIS OF DERIVED FROM 3-CETO-CYCLOPENTENE-5-OXY

AROMATIZING SUBSTANCES

ANTI-ANDROGENIC CYCLO AND BICYCLO ALKENES

Compounds having formulae (i), (ii) and (iii), where R is H, alkyl of 1 to 6 carbons, or CO-R2 where R2 is alkyl of 1 to 6 carbons; R1 is H, CH3, or (CH2)m-CH3; n is an integer having the values of 2 to 10, m is an integer having the values of 1 to 6, have anti-androgen activity on secondary androgen receptor sites. The compounds are useful for treating mammals, including humans afflicted with acne, male pattern baldness, adhesions and keloids. The compounds are also effective for treating other diseases or conditions which are related to androgen receptors, such as undesirable formation of breast capsules in females after breast augmentation surgery, osteoarthritis and symptoms of Alzheimer's disease. The compounds also have inhibitory effect on the metabolism of certain microorganisms and fungi of the kind, the metabolism of which is normally known to be controllable by antiandrogen compounds.

HYPERFORIN DERIVATIVES, THE USE THEREOF AND FORMULATIONS CONTAINING THEM

The use of the reduction products of hyperforin and adhyperforin, pharmaceutically acceptable salts or esters thereof, in the pharmaceutical and/or nutritional field, in particular in the treatment of depression and Alzheimer's disease.

Vitamin D3 Flourinated Analogs

Compounds of the formula см. иллюстрацию в PDF-документе wherein R is hydrogen, hydroxy, or fluorine, and X is H2 are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of cancer, such as, leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.

Anti-tumor halo bicyclo alkanones

Potent tumor inhibitors are prepared which are compounds of the formula: wherein Q is CO, CH(OH) or C(OH)CH3, M1 is halogen, M2 is halogen or hydrogen, c is one or two p is 0 or 1, and one of X and X' is H and the other is hydroxy-C2-9alkyl, methoxy-C2-9-alkyl, ethoxy-C2-9-alkyl, oxo-C2-9-alkyl, formyl-C2-9-alkyl, carboxy-C2-9-alkyl or (C1-2-alkyl)oxycarbonyl-C2-9-alkyl.

Process and intermediates for the synthesis of the enantiomers of bicyclo(4.2.0)oct-2-en-7-one and derivatives and for the synthesis of bicyclo(4.2.0)octane derivatives

2,4,4-Trimethyl-cyclohex-2-en-1-on derivatives and their preparation as perfumes

Process for the preparation of the compounds of the formulae Ia and Ib wherein A. 2,4,4-trimethylcyclohex-2-en-1-one oxime of the formula IIb (IIb) is treated with a strong aqueous acid at from 30 DEG to 80 DEG C., preferably 40 DEG to 70 DEG C., B. the resulting ketone of the formula IIIb (IIIb) is oxidized in a conventional manner, and C. if desired, the resulting compound Ib is isomerized in a conventional manner. Compounds of the formula A (A) where R is one of the following radicals: -CH(OH)-CH2-CH=CH2 (IIIb), -CH(OH)-CH3 (IIIc), -CH2OH (IIId), -CH(OH)-CH=CH2 (IIIe), -CH(OCOCH3)-CH3 (IIIf), -CH2-OCOCH3 (IIIg), -CO-CH2-CH=CH2 (Ib), -CO-CH3 (Ic) and -CO-CH=CH2 (Ie). The compounds IIIb to IIIg, Ib, Ic and Ie are useful scents and aromas, and furthermore may become important intermediates for novel carotenoids. They can be prepared in a relatively simple manner from compounds which are very readily available.

Antiviral compositions derived from marine sponge epipolasis reiswigi and their methods of use

Bicyclooctanes, processes for producing them and pharmaceutical compositions containing them

The invention concerns a bicyclooctane derivative of the formula, wherein A is optionally present and is C1-4 alkylene, R1 is hydrogen or C1-4 alkyl, R2 is hydrogen or C4-7 alkyl, R3 is hydrogen or C1-4 alkyl, X is optionally present and is ethylene or vinylene and R4 and R5 are each, independently of one another, hydrogen or a hydroxy-protecting group; or a non- toxic salt. Such compounds wherein each of R4 and R5 is hydrogen are useful for prevention of thrombosis.

KETO-BICYCLOOCTANES

RADIATION-SENSITIVE FILM

ANTI-ANDROGENS CYCLO AND BICYCLOALKENE

JOHANNISKRAUT TROCKENEXTRAKT, PROCEDURE FOR ITS PRODUCTION AND ITS USE

FLUORIDATED SIMILAR ONE of VITAMIN D3

HYPERFORINDERIVATE, YOUR USE AS WELL AS THESE CONTAINING PREPARATIONS

IMPROVED PROCEDURE FOR THE PRODUCTION OF KAROTENE AND KAROTENOIDEN FROM ALGAE AND CYANOBAKTERIEN

CYCLO-ALIPHATIC CURE COMPOSITIONS.

CHOLECALCIFEROLDERIVATE AND A PROCEDURE FOR THEIR PRODUCTION.

(4.2.0>-BICYCLOOCTANDERIVATE, PROCEDURE FOR YOUR PRODUCTION AND IT ABSTENTION PHARMACEUTICAL COMPOSITIONS.

ANTI-EOP READING TABLES MEANS ON BASIS OF NOT OR ONLY SLIGHT IRRITATING AND/OR ATTAINING A DOCTORATE DITERPENALKOHOLEN AND DERIVATIVES OF IT AND THEIR PRODUCTION.

1,2-1,4-ADDITIONS-REAKTIONSSCHRITT, WHICH LEADS TO DIPHENYLACETYLENEN.

Hyperforin halogenated derivatives, the use thereof and formulations containing them

CYCLOALIPHATIC PHARMACEUTICAL COMPOUNDS

3.2.0 BICYCLOHEPTANONE OXIME ETHERS

Isohumulone compound clathrate and composition containing the same

An isohumulone compound clathrate in which an isohumulone compound is encapsulated in -cyclodextrin (CD). There is provided an isohumulone compound clathrate that can be obtained by mixing together an isohumulone compound, -cyclodextrin (CD) and an aqueous solvent in a ratio of isohumulone compound : CD : aqueous solvent = 1 : 5 to 25 : 20 to 112.5 (provided that CD : aqueous solvent = 1 : 4 to 9).

Process for the stereoselective preparation of a pyrazole carboxamide

The present invention relates to a process for the enantioselective preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid ((1S,4R)-9-dichloromethylene-1,2,3,4- tetrahydro-1,4-methano-naphthalen-5-yl)-amide of formula Ib.

KETONE COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

NOVEL CYCLOPENTENEDIONE ANTIFUNGAL COMPOUNDS AND METHODS FOR THEIR USE

Novel compounds and methods useful in the control, treatment, and prevention of fungal activity.

KETONE COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

(3.2.0)BICYCLOHEPTANONE OXIME ETHERS WITH VALUABLE THERAPEUTIC PROPERTIES

Compounds useful in treating cardiovascular disorders are the carboxylic acids depicted in formulas (1) and (2) (1) (2) as well as their pharmaceutically acceptable, non-toxic salts and esters, wherein: n is an integer from one to four; R1 is hydroxy; R2 is hydrogen; or R1 and R2 together are an oxo group; R3 is wherein A is -CH2-CH2-; trans-CH=CH-; -C?C-; and R4 is linear or branched alkyl of one to twelve carbons, preferably 1-10 carbons and most preferrably 3-8 carbons, cycloalkyl of three to eight carbons; phenyl optionally substituted with one or two identical substituents selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, trifluoromethyl, and halo; or optionally substituted phenylalkyl.

PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES

The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide.

CERTAIN GLYOXYL-CYCLOHEXENDIONES

ABSTRACT CERTAIN GLYOXYL-CYCLOHEXENDIONES Compounds of formula I

STABLE EXTRACT JOHN S, METHOD OF ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS BASED ON IT

PROCESS OF PRODUCING PYRAZOLE CARBOXYLIC ACID AMIDES

ПОХІДНІ ПОЛІГІДРОКСИФЕНОЛУ, ЛІКАРСЬКІ КОМПОЗИЦІІ ТА СПОСІБ ПРОФІЛАКТИКИ ТА ЛІКУВАННЯ ЗАХВОРЮВАНЬ КІСТОК І ХРЯЩІВ

Похідні полигідроксифенолу загальної формули (I) і його хінонові похідні: (I), де: R1 - алкіл, необов'язково заміщений бензил, або необов'язково заміщений арил; R2 - водень, алкіл, алкеніл, необов'язково заміщений бензил; R3 - водень, алкіл, алкеніл, необов'язково заміщений бензил, гідроксил, алкоксі, алкенілоксі або необов'язково заміщений бензилоксі; R4 - водень, алкіл, алкеніл, необов'язково заміщений бензил або гідроксил; R5 і R6 - кожен незалежно водень, алкіл, алкеніл, необов'язково заміщений бензил. Сполуки (I) мають сильну активність приборкання кісткової резорбції і корисні як засоби профілактики і лікування захворювань хрящів і кісток.

Compounds useful in the therapy of alzheimer's disease and formulations containing them

METHOD OF PREPARATION OF DERIVED From OXOCYCLOPENTENE AND NEW PRODUCTS THUS OBTAINED

Method of preparation of hydroxyalcoyl-1 trialcoyl-3, 3,4, cyclohexenes-1 and products obtained

NEW COMPOSE, COMPOSITIONS INCLUDING/UNDERSTANDING THEM AND THEIR USE POURFAVORISER EXFOLIATION

CYCLOPENTANE DERIVATIVES

METHOD OF PREPARATION OF DERIVED From OXOCYCLOPENTENE AND NEW PRODUCTS THUS OBTAINED

UN PROCEDE DE PREPARATION D'OXOCYCLOPENTENES AYANT LA FORMULE: (CF DESSIN DANS BOPI) OU R EST L'HYDROGENE, UN GROUPE ALKYLE INFERIEUR OU ALKENYLE INFERIEUR, ET R EST L'HYDROGENE, UN GROUPE ALKYLE INFERIEUR, ALKENYLE INFERIEUR, ALKYNYLE INFERIEUR, ARYLE SUBSTITUE OU NON SUBSTITUE, ARALKYLE INFERIEUR, THIENYLE OU CYCLOALKYLE, CONSISTE A SOUMETTRE UN FURANECARBINOL AYANT LA FORMULE: (CF DESSIN DANS BOPI) OU R EST TEL QUE DEFINI CI-DESSUS ET R EST L'HYDROGENE, UN GROUPE ALKYLE INFERIEUR, ALKENYLE INFERIEUR, ALKYNYLE INFERIEUR, ARYLE SUBSTITUE OU NON SUBSTITUE, ARALKYLE INFERIEUR, THIENYLE OU CYCLOALKYLE, A UNE TRANSPOSITION, A SOUMETTRE L'HYDROXYCYCLOPENTENONE RESULTANTE A UNE HYDROGENATION ET A SOUMETTRE L'HYDROCYCLOPENTANONE RESULTANTE A LA DESHYDRATATION. A PROCESS FOR THE PREPARATION OF OXOCYCLOPENTENES HAVING THE FORMULA: (DRAWING CF IN BOPI) WHERE R IS HYDROGEN, A LOWER ALKYL GROUP OR LOWER ALKENYL, AND R IS HYDROGEN, A LOWER ALKYNYL GROUP, LOWER ALKYNYL, LOWER ALKYURY, ALKENYL GROUP SUBSTITUTES OR NON-SUBSTITUTE ARYL, LOWER ARALKYL, THIENYL OR CYCLOALKYL, CONSISTS OF SUBMITTING A FURANECARBINOL HAVING THE FORMULA: (CF DRAWING IN BOPI) OR R IS AS DEFINED ABOVE AND R IS AN INFURANECARBINOL, HAVING THE FORMULA: (CF DRAWING IN BOPI) OR R IS AS DEFINED ABOVE AND R IS AN INFINITE ALKENDURIE, GROUP ALKENDURIE LOWER, LOWER ALKYNYL, SUBSTITUTED OR NON-SUBSTITUTED ARYL, LOWER ARALKYL, THIENYL OR CYCLOALKYL, TO TRANSPOSITION, SUBJECT THE RESULTANT HYDROXYCYCLOPENTENONE TO HYDROGENATION AND RESULTANATION OF HYDROGENATION AND UNDROCYCLYTRANATION OF HYDROCYCLOPENTENONE AND RESANCYCLYTRANATION OF THE HUMANITY.

PROCEDE DE SYNTHESE DE DERIVES DU 3-CETO-CYCLOPENTENE-5-OXY

POUR EFFECTUER LA SYNTHESE DE COMPOSES REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) RHYDROGENE OU GROUPE ALKYLERGROUPE ALKYLERHYDROGENE OU GROUPE BENZOYLEON PROCEDE A LA PHOTOISOMERATION DU PRODUIT: (CF DESSIN DANS BOPI) RGROUPE ALKYLERREN UN COMPOSE CIS CORRESPONDANT ET ON CYCLISE CE DERNIER DANS DES SOLVANTS A UNE TEMPERATURE COMPRISE ENTRE 20 ET 100C. UTILISATION : PREPARATION D'UN INSECTICIDE.

COMPOSES POLYENIQUES UTILES COMME COLORANTS

La présente invention concerne des composés chimiques nouveaux. Il s'agit de composés polyéniques de formule ...

NOVEL CYCLOPENTENE DERIVATIVES

NOUVELLES 15-DESOXY-16-HYDROXY-16-(1-PROPYNYL), 15-DESOXY-16-HYDROXY-16-ETHYNYL ET 16-(ETHYNYL SUBSTITUE)PROSTAGLANDINES ET PROCEDES DE LEUR PREPARATION

L'INVENTION CONCERNE DE NOUVELLES 15-DESOXY-16-HYDROXY-16-(1-PROPYNYL), 15-DESOXY-16-HYDROXY-16-ETHYNYL ET 16-(ETHYNYL SUBSTITUE) PROSTAGLANDINES ET DES PROCEDES DE LEUR PREPARATION. LES NOUVEAUX COMPOSES DE L'INVENTION APPARTIENNENT AUX SERIES E, F, D ET A DES PROSTAGLANDINES ET PORTENT SUR LE CARBONE METHYLENIQUE TERMINAL DE LA CHAINE A UN SUBSTITUANT CHOISI PARMI LES RADICAUX: (CF DESSIN DANS BOPI) OU R REPRESENTE UN ATOME D'HYDROGENE OU UN RADICAL ALKYLE EN C-C; R REPRESENTE UN RADICAL ALKYLE EN C-C, DI-C-C-ALKYLAMINO, PHENYLE OU PHENYLE SUBSTITUE PAR UN OU PLUSIEURS SUBSTITUANTS CHOISIS PARMI UN RADICAL ALKYLE EN C-C, OR, SR, F OU CL, OU R REPRESENTE UN RADICAL ALKYLE; DES PROCEDES DE PREPARATION DE CES COMPOSES SONT EGALEMENT DECRITS. LES COMPOSES DE L'INVENTION SONT DES MEDICAMENTS PRESENTANT DE FACON AMELIOREE LES PROPRIETES GENERALES DES PROSTAGLANDINES.

NEWS 15-DESOXY-16-HYDROXY-16- (1-PROPYNYL), 15-DESOXY-16-HYDROXY-16-ETHYNYL AND 16 (ETHYNYL SUBSTITUTES) PROSTAGLANDINS AND PROCEEDED OF THEIR PREPARATION

NEW DERIVATIVES Of HUMULONES

Methods and compositions for heavy metal detoxification

Compositions and methods for enhancing heavy metal detoxification are described. The compositions and methods described provide enhanced activity of key detoxification systems including that the induction of phase II detoxification enzymes, such as glutathione S-transferases (GSTs), and NADPH quinone reductase (NQO1) activity.

Cosmetic Composition Comprising Vetiver Root Extract

A cosmetic composition is provided, which comprises a carrier and a Vetiver root extract, in particular an extract from exhausted Vetiver root. This composition provides a stimulation of sebum production, stimulation of sebum antimicrobial, lipids production, activation of adipocytes volume increase, skin hydration, skin tonicity booster, skin fatigue reduction, perilabial wrinkles reduction, skin replumping, and fragrance long-lastingness enhancement. 1. A cosmetic composition comprising a carrier and at least one active cosmetic ingredient , wherein the at least one active cosmetic ingredient comprises a Vetiver root extract.2. The cosmetic composition according to claim 1 , wherein the cosmetic composition is a skin care composition.3. The cosmetic composition according to claim 1 , wherein the at least one active cosmetic ingredient comprises an aqueous extract of Vetiver root.4. The cosmetic composition according to claim 1 , wherein the at least one active cosmetic ingredient comprises an extract of exhausted Vetiver root.5. A method of preparing an active cosmetic ingredient claim 1 , comprising the step of: extracting Vetiver root.6. The method according to claim 5 , comprising the steps of:(i) providing exhausted Vetiver root; and(ii) extracting the exhausted Vetiver root.7. The method according to claim 5 , wherein the extraction is performed using water.8. (canceled)9. A method of stimulating the sebum production claim 1 , of stimulating sebum antimicrobials claim 1 , of stimulating the lipids production claim 1 , of activating the adipocytes volume increase claim 1 , of improving the skin hydration claim 1 , of boosting the skin tonicity claim 1 , of reducing skin fatigue claim 1 , of reducing perilabial wrinkles claim 1 , of replumping skin claim 1 , and/or of enhancing fragrance long-lastingness claim 1 , the method comprising the step of: applying the cosmetic composition of to human skin. The present invention relates to cosmetic compositions ...

Preparation of Ambrox from Labdanes of Dysoxylum hongkongense, and the Preparation of New Diterpenoids from Dysoxylum hongkongense

The present invention discloses eight new diterpenoids, i.e. Dysongensins A to H, extracted from the leaves and twigs of Dysoxylum hongkongense , wherein AMBROX® which is applicable in the perfume industry is prepared from Dysongensin A via a series of chemical reactions, and the cytotoxicity of Dysongensins A to H against human cancer cell lines and their antiviral and anti-inflammatory activities are determined. Therefore, in the present invention, AMBROX® prepared from Dysongensin A is a new idea for application as an odorous compound in the perfume industry, and the novel diterpenoids can be prepared as a pharmaceutical compositions and/or a drug having antiviral, anti-inflammatory and/or anti-cancer activities.

Synthetic Route To Anhydroryanodol, Ryanodol And Structural Analogues

This disclosure is related to methods for producing anhydroryanodol, ryanodol, or analogues thereof and novel compounds prepared thereby. This application is a divisional of U.S. patent application Ser. No. 15/381,595, filed Dec. 16, 2016, which claims the priority of U.S. Provisional Patent Application No. 62/269,760, filed Dec. 18, 2015, both applications of which are incorporated by reference.This invention was made with government support under Grant No. DGE1144469 awarded by the National Science Foundation and Grant RGM097582-01 awarded by the national Institute of General Medical Sciences. The government has certain rights in invention.This disclosure is related to methods for producing anhydroryanodol, ryanodol, and analogues thereof.Terpenes are a large and structurally diverse family of natural products that range from simple hydrocarbons associated with flavors and fragrances, to complex, highly oxidized polycyclic molecules such as the anti-malarial drug artemisinin, and the anticancer compounds ingenol and taxol. Although terpenes are isolated from natural sources, it can be challenging to translate their biological activity into a practical application. In some cases, the hurdle is low natural abundance; other times, it is the difficulty encountered by chemists seeking to precisely edit a terpene's molecular structure in order to improve its drug-like properties or interrogate its role in modulating disease pathways. The development of concise chemical syntheses of terpenes can transform the ability to use these molecules and their synthetic derivatives as biological probes or as lead compounds for the development of new medicines. Furthermore, these scientific efforts often innovate chemical reactivity or synthetic design concepts.The natural product ryanodine (1) and its hydrolysis product ryanodol (2) are among the most highly oxidized and synthetically challenging diterpenoids reported to date.Isolated from the tropical shrub Ryania speciosa Vahl in ...

15-Oxospiramilactone Derivatives, Preparation Method and Uses Thereof

The invention relates to a derivative of 15-oxospiramilacton, particularly to a compound of Formula I or II, or an isomer, a solvate or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the compound as pharmaceutically active ingredient, a method for preparing the same, and use thereof in manufacture of an anti-tumor agent. The derivative of 15-oxospiramilactone of the invention have an activity against multiple tumor cell lines, and the anti-tumor activity is positively correlated to an activity inhibiting the Wnt signaling pathway.

ANTICANCER AGENTS AND PROCESS OF MAKING THEREOF

Provided herein are compositions and processes of making of anticancer compounds useful for cancer treatments. These cyclohexenone compounds show an unexpected result against certain cancer cells compared to their known analogs. 3. The compound of claim 1 , wherein R is a hydrogen claim 1 , C(═O)CH claim 1 , C(═O)CH claim 1 , or C(═O)CH.4. The compound of claim 1 , wherein each of R claim 1 , Rand Rindependently is hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , pentyl claim 1 , hexyl claim 1 , or heptyl.5. The compound of claim 1 , wherein each of Rand Rindependently is (CHCH═C(CH)(CH))—R.6. The compound of claim 5 , wherein Ris H claim 5 , NH claim 5 , NHCH claim 5 , N(CH) claim 5 , OCH claim 5 , OCH claim 5 , C(═O)CH claim 5 , C(═O)CH claim 5 , C(═O)OCH claim 5 , C(═O)OCH claim 5 , C(═O)NHCH claim 5 , C(═O)NHCH claim 5 , C(═O)NH claim 5 , OC(═O)CH claim 5 , OC(═O)CH claim 5 , OC(═O)OCH claim 5 , OC(═O)OCH claim 5 , OC(═O)NHCH claim 5 , OC(═O)NHCH claim 5 , or OC(═O)NH.7. The compound of claim 5 , wherein Ris CHC(CH)OH claim 5 , CHC(CH)OCH claim 5 , CHCOOH claim 5 , CHCOOH claim 5 , CHOH claim 5 , CHOH claim 5 , CHPh claim 5 , CHPh claim 5 , CHCH═C(CH)(CHO) claim 5 , CHCH═C(CH)(C(═O)CH) claim 5 , 5 or 6-membered lactone claim 5 , aryl claim 5 , or glucosyl claim 5 , wherein 5 or 6-membered lactone claim 5 , aryl claim 5 , and glucosyl are optionally substituted with one or more substituents selected from NRR claim 5 , OR claim 5 , OC(═O)R claim 5 , C(═O)OR claim 5 , C(═O)R claim 5 , C(═O)NRR claim 5 , C-Calkyl claim 5 , C-Calkenyl claim 5 , C-Calkynyl claim 5 , C-Ccycloalkyl claim 5 , and C-Chaloalkyl.8. The compound of claim 7 , wherein Ris C—C alkyl optionally substituted with one or more substituents selected from NRR claim 7 , OR claim 7 , OC(═O)R claim 7 , C(═O)OR claim 7 , C(═O)R claim 7 , C(═O)NRR claim 7 , C-Calkyl claim 7 , C-Calkenyl claim 7 , C-Calkynyl claim 7 , C-Ccycloalkyl claim 7 , and C-Chaloalkyl.9. The ...

Novel synthesis routes for prostaglandins and prostaglandin intermediates using metathesis

Methods of synthesizing prostaglandins, prostaglandin analogs and their synthetic intermediates are described. The methods can comprise metal-catalyzed metathesis reactions. Also provided are synthetic intermediates that can be used in the synthesis of the prostaglandins and prostaglandin analogs.

Processes for the preparation of hydroxylated cyclohexyl compounds

The present application relates to processes for the preparation of polyhydroxylated cyclohexyl compounds such as the compounds of Formula I:

TETRAHYDRO-ISOHUMULONE DERIVATIVES, METHODS OF MAKING AND USING

The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARγ, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPARγ modulation such as diabetes. 1. A method of inhibiting inflammation or treating a condition associated with inflammation in a subject in need thereof comprising administering a therapeutically effective amount of a tetrahydro-iso-alpha acid (THIAA) derivative selected from the group consisting of(4R,5R)-3,4-dihydroxy-4-(1-hydroxy-4-methylpentyl)-2-(N-methoxy-3-methylbutanimidoyl)-5-(3-methylbutyl)cyclopent-2-en-1-one (KDT0005), (4R,5R)-4-hydroxy-2-{1-[(2-hydroxyethyl)amino]-3-methylbutylidene}-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopentane-1,3-dione (KDT0017), (4R,5R)-4-hydroxy-5-[3-methylbutyl)-2-methyl-1-(methylamino)butylidene]-4-(4-methylpentanoyl)cyclopentane-1,3-dione (KDT0020), (4R,5R)-2-[1-(benzylamino)-3-methylbutylidene]-4-hydroxy-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopentane-1,3-dione (KDT0024), (1S,5R)-2-hydroxy-3-(3-methylbutanoyl)-5-(3-methylbutyl)-1-(4-methylpentanoyl)-4-oxocyclopent-2-en-1-yl 2,2-dimethylpropanoate (KDT0033), (1S,5R)-2-hydroxy-3-(3-methylbutanoyl)-5-(3-methylbutyl)-1-(4-methylpentanoyl)-4-oxocyclopent-2-en-1-yl 3,3-dimethylbutanoate (KDT0034), but-3-yn-1-yl (1S,5R)-2-hydroxy-3-(3-methylbutanoyl)-5-(3-methylbutyl)-1-(4-methylpentanoyl)-4-oxocyclopent-2-en-1-yl carbonate (KDT0035), (1S,5R)-2-hydroxy-5-(3-methylbutyl)-1-(4-methylpentanoyl)-3-(2-methylpropanoyl)-4-oxocyclopent-2-en-1-yl decanoate (KDT0036), (1S,5R)-2-hydroxy-5-(3-methylbutyl)-1-(4-methylpentanoyl)-3-(2-methylpropanoyl)-4-oxocyclopent-2-en-1-yl 2-methylpropyl carbonate (KDT0037), 5-[(1S,5R)-1,2-dihydroxy-3-(3-methylbutanoyl)-5-(3-methylbutyl)-4-oxocyclopent-2-en-1-yl]-2- ...

SYNTHESIS OF DELTA 12-PGJ3 AND RELATED COMPOUNDS

In one aspect, the present invention provides novel derivatives of Δ-PGJand modular synthetic pathways to obtaining Δ-PGJand derivatives thereof. In some aspects, the present derivatives of Δ-PGJare useful as chemotherapeutic agents. The present disclosure also describes compositions of these derivatives as well as methods of use of the derivatives thereof. 46.-. (canceled)7. The compound of claim 1 , wherein Yis O.8. The compound of claim 1 , wherein Yis N—OH or N—OMe.9. The compound of claim 8 , wherein Yis N—OMe.1095.-. (canceled)97. The compound of claim 96 , wherein Ais alkenediyl.98. (canceled)99. The compound of claim 96 , wherein z is 1 claim 96 , 2 claim 96 , 3 claim 96 , or 4.100101.-. (canceled)102. The compound of claim 96 , wherein Xis O.103. The compound of claim 96 , wherein Xis alkenyl.104. (canceled)107. A pharmaceutical composition comprising a compound of and an excipient.108. (canceled)109. The pharmaceutical composition of claim 107 , wherein the composition is formulated for oral claim 107 , topical claim 107 , intraarterial claim 107 , intraperitoneal claim 107 , or intravenous administration.110114-. (canceled)115. A method of treating a disease or disorder in a patient in need thereof comprising administering to the patient a pharmaceutically effective amount of a compound or composition of or a pharmaceutically acceptable salt or optical isomer thereof.116. The method of claim 115 , wherein the disease is cancer.117118.-. (canceled)119. The method of claim 116 , wherein the cancer is leukemia.120130.-. (canceled)132293.-. (canceled)295434.-. (canceled) This application claims the benefit of U.S. Provisional Application 61/882,093, filed on Sep. 25, 2013, U.S. Provisional Application 61/897,681, filed on Oct. 30, 2013, U.S. Provisional Application 61/920,302, filed on Dec. 23, 2013, U.S. Provisional Application 61/954,295, filed on Mar. 17, 2014, and U.S. Provisional Application 61/979,276, filed on Apr. 14, 2014, the entire contents of each ...

POLYPRENYLATED PHLOROGLUCINOL COMPOUNDS AS POTENT P-GLYCOPROTEIN INDUCERS

The present invention relates to the polyprenylated phloroglucinol compounds of formulae I and II. The present invention also provides synthesis and p-glycoprotein induction activity of the alkyl- and acyl-polyprenylated phloroglucinol compounds. Further, use of the compounds as p-glycoprotein inducers and methods of treatment of Alzheimer's disease using compounds of the invention are also provided. 2. The compound as claimed in claim 1 , wherein the substitution on the alkyl or the acyl group is at one or more positions and selected from the group comprising of chloro claim 1 , fluoro claim 1 , iodo claim 1 , and nitro.3. The compound as claimed in wherein the benzyl group is selected from the group comprising of 2-iodo benzyl claim 1 , 2-chloro claim 1 , 6-fluoro benzyl claim 1 , 2 claim 1 ,6-dichloro benzyl claim 1 , 4-chloro benzyl claim 1 , 2-nitro benzyl claim 1 , and 3-nitro benzyl.5. A process for the preparation of the compounds of formula I and II as claimed in claim 1 , comprising the steps of—(i) reacting garcinol or isogarcinol with alkyl or acyl halide in presence of a base in a solvent at a temperature ranging between 0 to 35° C. for a period of time between 0 to 60 minutes to obtain a crude mixture; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(ii) optionally purifying the crude mixture column chromatography using an eluent to obtain the compounds of .'}6. The process as claimed in wherein the alkyl halide is selected from group comprising of methyl halide claim 5 , ethyl halide claim 5 , propyl halide claim 5 , isopropyl halide claim 5 , n-butyl halide claim 5 , isobutyl halide claim 5 , isovaleryl halide claim 5 , propargyl halide claim 5 , allyl halide claim 5 , prenyl halide claim 5 , geranyl halide claim 5 , and halides of other long aliphatic chains with chain length from C-C claim 5 , and acyl halide is selected from the group comprising of acetyl halide claim 5 , benzyl halide claim 5 , benzoyl halide and butanoyl halide.7. The ...

新的萜类和大环类化合物

本发明涉及的新的萜类和大环类化合物是TGR5的激活剂，且能用于预防和/或治疗2型糖尿病、肥胖、神经病和/或肾病。

Method of preparing humilones

Process for the preparation of pyrazole carboxylic acid amides

The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide.

Process for the preparation of pyrazole carboxylic acid amides

The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide.

Process for the preparation of pyrazole carboxylic acid amides

本发明涉及一种制备3-二氟甲基-1-甲基-1H-吡唑-4-羧酸(9-二氯亚甲基-1，2，3，4-四氢-1，4-桥亚甲基-萘基-5-基)-酰胺的工艺。

Process for the preparation of pyrazole carboxylic acid amides

本发明涉及一种制备3-二氟甲基-1-甲基-1H-吡唑-4-羧酸(9-二氯亚甲基-1，2，3，4-四氢-1，4-桥亚甲基-萘基-5-基)-酰胺的工艺。

Process for the preparation of pyrazole carboxylic acid amides

The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide.

Therapeutical novel (3,2,0)bicycloheptanone oxime ether

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Bicyclooctane compounds, their production, compositions containing them and their pharmaceutical use

Dearylated isopentenyl acyl phloroglucinol derivative and pharmaceutical composition and application thereof

本发明提供了去芳化异戊烯基酰基间苯三酚类衍生物及其制备方法，具有治疗癫痫、高血压、帕金森病，疼痛、肿瘤、睡眠障碍等疾病的药物组合物及其应用，属于药物技术领域。本发明提供的化合物hypatone B，hyphenrone J和hyphenrone K具有显著抑制Ca v 3.1低电压门控钙离子通道的活性，其中化合物hyphenrone K是目前活性最强的天然抑制剂，IC 50 比阳性对照咪拉地尔低一个数量级，具有潜在的药用价值。

Method of producing (4,2,0)-bicycloctane derivatives of their pharmaceutically acceptable non-toxic salts

Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3): <IMAGE> (1) <IMAGE> (2) <IMAGE> (3) wherein: n is 2 or 3; R1 is CH2OH, CHO, CO2R or CO2H; R2 is hydrogen or methyl; and R3 is linear or branched alkyl having 5-10 carbon atoms, <IMAGE> +TR or (CH2)mphenyl optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen, in which a is 0, 1 or 2; b is 3-7; m is 1 or 2; and R is <IMAGE> +TR <IMAGE> in which each R4 is independently hydrogen or lower alkyl having 1-6 carbon atoms, and the pharmaceutically acceptable, non-toxic salts and esters thereof.

Derivatives of glyoxyl-cyclohexenedione, method of their synthesis, herbicide composition, method of weed inhibition

FIELD: organic chemistry. SUBSTANCE: invention proposes compounds of the formula (I): $$$ which were used as herbicides exhibiting effect with respect to dicotyledonous weed, methods of their synthesis and using. EFFECT: improved method of synthesis, enhanced effectiveness of herbicides. 6 cl, 4 tbl ЭУ5 ООС ПЫ Го (19) РИ (11) 2 100 346 (13) Сл ОМК © 07С 49/603, 49/172, 49/175, А 01 М 35/06 РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4830743/04, 19.07.1990 (71) Заявитель: Шелл Интернэшнл Рисерч Маатсхаппий Б.В. (30) Приоритет: 21.07.1989 ОЕ Р 39242412 (МЫ) (46) Дата публикации: 27.12.1997 (72) Изобретатель: Ханс Иоахим Биссингер[ОЕ], | Людвиг Шредер[ОЕ], Хельмут 49/784, 1987. 2. ЗИ, патент, 1209016, кл. А Фрусторфер[ОЕ] Манфред Гарех ОЕ] 01 М 31/06, 1982. () (73) Патентообладатель: Шелл Интернэшнл Рисерч Маатсхаппий Б.В. (Ме) < (54) ПРОИЗВОДНЫЕ ГЛИОКСИЛ-ЦИКЛОГЕКСЕНДИОНА, СПОСОБ ИХ ПОЛУЧЕНИЯ, ГЕРБИЦИДНАЯ < КОМПОЗИЦИЯ, СПОСОБ ПОДАВЛЕНИЯ НЕЖЕЛАТЕЛЬНОГО РОСТА РАСТЕНИЙ < (57) Реферат: которые находят использование в © Предложены соединения формулы 1: качестве гербицидов, эффективных против двудольных сорняков, способы их получения © и использования. 5 з.п. ф-лы, 4 табл. == Сс' — О Эт 0О0б0гс ПЧ Го (19) КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ 12) АВЗТКАСТ ОЕ 1МУЕМТОМ ВИ “” 2400 346 ' (51) 1пЕ. С1.6 13) Сл С 07С 49/603, 49/172, 49/175, А 01 М 35/06 (21), (22) АррИсаНоп: 4830743/04, 19.07.1990 (30) Рпогйу: 21.07.1989 ОЕ Р 3924241.2 (46) Рае ог рибИсаНоп: 27.12.1997 (72) |пуетог: (71) АррИсапе: эре! |егпейзпп! Кизегсй МааКварри В.М. (МЕ) КПап$ 1оакКМт Вззтаег[ОЕ], Циама эпгедегоЕ], Кпе’тще ВаЧгизпа ОЕ], ЕПК Кадда [ОЕ], Мо Чдапа ЕгиЗогег[ОЕ], Маптеа Сагекп ОЕ] (73) Ргорпеюг: эпе! \егпейзйп! К зегсй МааКПарри В.М. (МЕ) (54) РДЕКМАТМЕЗ$З ОЕ СЕУОХУЕ-СУСЕОНЕХЕМЕОЮМЕ, МЕТНОО ОЕ ТНЕКВ ЗУМТНЕ$!$, НЕКВСТОЕ СОМРОЗГОМ, МЕТНОО ОЕ \МЕЕО 1МНВГОМ (57) АБЗгасЕ: НЕГО: огдапс спептгу. ЗОВЗТАМСЕ: пуепНоп ...

Method of producing (4,2,0)bicyclooctane derivatives of their pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable non-toxic esters

Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3): <IMAGE> (1) <IMAGE> (2) <IMAGE> (3) wherein: n is 2 or 3; R1 is CH2OH, CHO, CO2R or CO2H; R2 is hydrogen or methyl; and R3 is linear or branched alkyl having 5-10 carbon atoms, <IMAGE> +TR or (CH2)mphenyl optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen, in which a is 0, 1 or 2; b is 3-7; m is 1 or 2; and R is <IMAGE> +TR <IMAGE> in which each R4 is independently hydrogen or lower alkyl having 1-6 carbon atoms, and the pharmaceutically acceptable, non-toxic salts and esters thereof.

Patent FR2485520B1

Patent FR2291192B1

PRODUCTS EXTRACTED FROM A COMMIPHORA PLANT, IN PARTICULAR FROM THE COMMIPHORA MUKUL PLANT, AND EXTRACTS CONTAINING THEM AND THEIR APPLICATIONS, IN PARTICULAR IN COSMETICS

ANTITUMOR-4-HYDROXY-2-CYCLOPENTENONES.

PROSTACYCLINE DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR THERAPEUTIC APPLICATIONS

L'INVENTION A POUR OBJET: (CF DESSIN DANS BOPI) DANS LAQUELLE R REPRESENTE UN ATOME D'HYDROGENE OU UN GROUPE ALKYLE AYANT DE 1 A 15 ATOMES DE CARBONE; R REPRESENTE UN GROUPE ALKYLE OU ALCENYLE; ET N REPRESENTE UN ENTIER DE 1 A 8, ET LEURS SELS PHARMACEUTIQUEMENT ACCEPTABLES. CES COMPOSES ONT UNE ACTIVITE INHIBITRICE DE L'AGREGATION PLAQUETTAIRE. THE SUBJECT OF THE INVENTION: (CF DRAWING IN BOPI) IN WHICH R REPRESENTS A HYDROGEN ATOM OR AN ALKYL GROUP HAVING FROM 1 TO 15 CARBON ATOMS; R REPRESENTS AN ALKYL OR ALCENYL GROUP; AND N REPRESENTS A WHOLE OF 1 TO 8, AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS. THESE COMPOUNDS HAVE AN ACTIVITY INHIBITORING PLATELET AGGREGATION.

PRODUCTS EXTRACTED FROM A PLANT OF THE GENUS COMMIPHORA, PARTICULARLY FROM THE PLANT COMMIPHORA MUKUL, AND EXTRACTS CONTAINING THEM AND THEIR APPLICATIONS IN PARTICULAR IN COSMETICS

Products of formula (I) extracted from a plant of the genus Commiphora, particularly the Commiphora mukul plant, wherein R is (a) a CH2OH grouping, (b) a COOH grouping, and salts or esters thereof are described. These products and the extracts containing them are effective cosmetic agents against wrinkles.

Patent FR2330676B1

Method of producing derivatives of cis-dicyclo/3,3,0/ octane

CYCLOALIFATIC PHARMASOEYTIC COMPOUNDS

Tetrahydro-isohumulone derivatives, methods of making and using

The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARy, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPARy modulation such as diabetes.

New cis-bicyclo (3.3.0) octane derivatives, pharmaceutical compositions containing them and processes for the preparation of these compounds and pharmaceutical compositions.

Antiandrogenic cyclo- and bicycloalkenes

Forbindelser med formlene (1), (n) Og (111), O u <CH-(CH ) -CH(OR)R 2 n l = CK-(CH ) -CH(OR)R 2 n l (i) (ii) CH-(CH ) -CH(OR)R 2 n l (iii) hvor R er H, alkyl med l til 6 karbonatomer. eller CO- R2 hcor R2 er alkyl med l til 6 karbonatomer; ^ er E, CH3 eller (CH3)B-CH3: n er et heltall med verdiene 2 til 10, m er et heltall med verdiene l til 6. har antlandrogen aktivitet på sekundære androgene reseptor- seter. Forbindelsene er nyttige for behandling av pattedyr, Inkludert mennesker, som Ilder av åene, hannkjønnsskallethet. adhesjoner og kelolder. For- bindelsene er også effektive for behandling av andre sykdommer eller tilstander som er relatert til androgene reseptorer. slik som uønsket dannelse av brystkapsler hos kvinner etter brystpkningskirurgi, osteoarthrltis og symptomer på Alzheimer's sykdom. Forbindelsene har også hemmende effekt på metabollsmen av visse mikroorganismer og fungus av typen, hvis metabolisme normalt er kjent å bli kontrollert av antlandrogene forbindelser.

Processes for the preparation of hydroxylated cyclohexyl compounds

The present application relates to processes for the preparation of polyhydroxylated cyclohexyl compounds such as the compounds of Formula I: (see formula I)

Fused ring phenylpyrazole compounds

D.N. 4671A FUSED RING PHENYLPYRAZOLE COMPOUNDS ABSTRACT Compounds of the formula where R is hydrogen, methyl, ethyl, propyl, 2-propenyl or 2-propynyl and R' is hydrogen or fluoro possess glucocorticoid activity. The compounds where R is H are prepared by reacting a compound of the formula

Oxygenated alkyl substituted bicyclo alkanes

A compound of the formula ##STR1## wherein Q is CO, CH(OR), CR(OH), or CR (OC)-lower alkyl); R is H, or C 1-2 -alkyl; X is hydroxyalkyl, methoxy-C 2-11 -alkyl, ethoxy-C 2-11 -alkyl or oxo-C 2-11 -alkyl, formyl-C 2-11 -alkyl, carboxy-C 2-11 -alkyl or (C 1-2 -alkyl) oxycarbonyl-C 2-11 -alkyl; c is 1 or 2; p or w are 0, 1 or 2 and the sum of p and w is 1 to 4; and a pharmaceutically acceptable salt thereof.

Hydroxylated or glycosylate unsatd. derivs. of spiro vetivone - as aromatising agents for tobacco

New concentrated substances (A) comprises a mono- or disubstd., hydroxy or glycosyloxy deriv. (I) of spirovetivvone. Also claimed are smoking materials based on tobacco (substitutes) and contg. 0.01-2 wt. % of (A) as aromatising agent. Pref. cpds. (I) are formulae (Ia) and (Ib) (where one of R1 and R2 is H and the other is OH or glycosyloxy derived from a mono- or disaccharide; the dotted lines represent the possible posns for an optional double bond; R3 is OH or glycosyloxy as for R1- 2). The glycosyloxy gp. is pref. derived from beta-d-glu 2). The glycosyloxy gp. is pref. derived from beta-d-glucose.

Hyperforin derivatives, the use thereof and formulations containing them

The use of the reduction products of hyperforin and adhyperforin, pharmaceutically acceptable salts or esters thereof, in the pharmaceutical and/or nutritional field, in particular in the treatment of depression and Alzheimer's disease.

PESTICIDES.

Hitherto unknown structural analogues of vitamin D

ANALOGY PROCEDURE FOR THE PREPARATION OF NEW THERAPEUTIC ACTIVITIES (3,2,0) -BICYCLOHEPTANOXIMETERS AND THEIR NON-TOXIC SALTS.

Phenylpyrazole compounds useful as anti-inflammatory agents and preparation thereof

Compounds of the formula where R is hydrogen, methyl, ethyl, propyl, 2-propenyl or 2-propynyl; an R' is hydrogen or fluoro possess glucocorticoid activity. The compounds where R is H are prepared by reacting a compound of the formula with (1H, 3H)-pyrimidine-2,4,5,6-tetrone, The compounds where R is other than hydrogen are prepared by reacting a compound where R is hydrogen with the appropriate alkylating agent.

Compound and pharmaceutical composition

There are provided novel compounds that have been extracted and isolated from a plant belonging to the family Compositae. Compounds represented by general formula (I): wherein R 1 represents hydroxyl and R 2 represents methoxy.

Process for production of new /3.2.0/-bicyclohepthanonoxim ethers and medical compositions containing these active substances

Anti-androgenic cyclo and bicyclo alkenes

Compounds having the formula (i), (ii) and (iii), ##STR1## where R is H, alkyl of 1 to 6 carbons, or CO--R 2 where R 2 is alkyl of 1 to 6 carbons; R 1 is H, CH 3 , or (CH 2 ) m --CH 3 ; n is an integer having the values of 2 to 10, m is an integer having the values of 1 to 6, have anti-androgen activity on secondary androgen receptor sites. The compounds are useful for treating mammals, including humans afflicted with acne, male pattern baldness, adhesions and keloids. The compounds are also effective for treating other diseases or conditions which are related to androgen receptors, such as undesirable formation of breast capsules in females after breast augmentation surgery, osteoarthritis and symptoms of Alzheimer's disease. The compounds also have inhibitory effect on the metabolism of certain microorganisms and fungi of the kind, the metabolism of which is normally known to be controllable by anti-androgen compounds.

Novel structural analogues of vitamin d

The present invention relates to analogues of vitamin D, which lack the combined presence of the trans-fused six-membered C-ring and of five-membered D-ring, but still possess a central part consisting of a subsituted chain of five atoms, atoms which correspond to positions 8, 14, 13 17 and 20 of vitamin D, and at the ends of which are connected, at position 20 a structural moiety representing part of the side chain of vitamin D or of an analogue of vitamin D, and at position 8 the .DELTA.(5,7)-diene moiety connected to the A-ring of the active 1-alpha-hydroxy metabolite or of an established vitamin D analogue, to their preparation process, to preparation intermediates, to pharmaceutical preparations comprising these compounds and to their use in medicine.

Process for preparing /4,2,0/bicyclooctane derivatives and pharmaceutical compositions containing such active substances

Patent JPS4881850A

Process for obtaining new derivatives of cis-bicyclo-/3,3.0/-octane

Cholecalciferol derivative

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Composition containing oxocarbon and use thereof

Process for preparing bicyclooctane derivatives with valuable therapeutic properties

Method for preparing stable extract of Hypericum perforatum el

히퍼리컴 퍼포라툼 엘의 안정 추출물, 그리고 그의 제조방법 및 그의 약학조성물 Stable extract of Hypericum perforatum el, preparation method thereof and pharmaceutical composition thereof 본 발명은 히퍼포린을 함유하는 히퍼리컴 퍼포라툼 엘(세인트 존 맥아즙)의 개선된 추출물에 있어서, 상기 히퍼포린은 안정화제에 의해 분해 또는 열화에 대해 안정성을 가지고 있는 것을 특징으로 하는 히퍼리컴 퍼포라툼 엘의 안정 추출물에 관한 것이다. The present invention provides an improved extract of Hypericum perforatum el (St. John's wort) containing hyperporin, wherein the hyperporin is stable to degradation or degradation by a stabilizer. A stable extract of Hypericum perforatum el.

Novel (3.2.0.) bicycloheptanone oxime ethers with valuable therapeutic properties

Compounds useful in treating cardiovascular disorders are the carboxylic acids depicted in formulas (1) and (2)as well as their pharmaceutically acceptable, non-toxic salts and esters, wherein:n is an integer from one to four;R₁ is hydroxy;R₂ is hydrogen; orR₁ and R_z together are an oxo group;R₃iswhereinA is -CH₂-CH₂-; trans-CH=_CH-; -C≡C-; andR₄ is linear or branched alkyl of one to twelve carbons, cycloalkyl of three to eight carbons; phenyl optionally substituted with one or two identical substituents selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, trifluoromethyl, and halo; or optionally substituted phenylalkyl.

Prostaglandin derivatives of the .delta.2-pgf.sub.2 and .delta.2-pge.sub.2 series and process for their manufacture

Abstract of the disclosure: Compounds of the formula X which are structurally related to natural prostaglandins and process for their manufacture. The compounds have valuable pharmacological properties and, therefore, they can be used as medicaments.

Ketone compounds and compositions for cholesterol management and related uses

BICYCLE LOCK DERIVATIVES FOR USE AS AN AGAINST THROMBOSIS

New terpenes and macrocycles.

Nuevos terpenos y macrociclos son activadores de TGR5 y se pueden usar para la prevención y/o el tratamiento de diabetes de tipo 2, obesidad, neuropatía y/o nefropatía.

Curcusone diterpenoids and uses thereof

The present disclosure provides the first asymmetric total synthesis and target identification of the curcusone natural products. The novel convergent synthesis is built upon a cheap and abundant chiral pool molecule (8) and features a thermal [3,3]-sigmatropic rearrangement and an FeCl3-promoted global hydrolysis/adol condensation cascade to rapidly construct the critical cycloheptadienone core. By performing chemoproteomics with the alkyne probe 37, we identified the previously "undruggable" oncogenic protein BRAT1 as a key cellular target of 1d. Furthermore, 1d inhibits BRAT1 in cancer cells, thereby reducing cancer cell migration, increasing susceptibility to DNA damage, and inducing chemosensitization to the approved drug etoposide. Compound 1d is the first known small-molecule inhibitor for BRAT1, a master regulator of the DDR and DNA repair. Composition matters and methods of uses are within the scope of this disclosure.

NEW STRUCTURAL VITAMIN D DERIVATIVES

Prostaglandin derivatives

What is disclosed are compounds of the formula <IMAGE> I which are structurally related to natural prostaglandins and a process for their manufacture. The compounds have valuable pharamacological properties and, therefore, they can be used as medicaments.

Sclareol derivatives and their use as smoke-flavour enhancing agents

Pentacyclic phenylpyrazole compounds as anti-inflammatory agents

Compounds of the formula ##STR1## where R is hydrogen, methyl, ethyl, propyl, 2-propenyl or 2-propynyl; and R' is hydrogen or fluoro possess anti-inflammatory activity. The compounds where R is H are prepared by reacting a compound of the formula ##STR2## with (1H,3H)-pyrimidine-2,4,5,6-tetrone. The compounds where R is other than hydrogen are prepared by reacting a compound where R is hydrogen with the appropriate alkylating agent.

Novel structural analogues of vitamin D

Bicyclooctane compounds, their production, compositions containing them and their pharmaceutical use

A bicyclooctane derivative has the formula: wherein R, is hydrogen or C 1-4 alkyl, X is ethylene or vinylene, and Y, and Y2 are independently hydrogen or a hydroxyl-protecting group. These compounds, or pharmaceutical pharmaceutically acceptable salts of such compounds in which R, is hydrogen, are chemically stable, have platelet antiaggregation activity without undesirable pharmacological activity and exhibit the duration of high biological activity. They can be prepared from the corresponding 7-keto derivative or 2-aldehyde compound with a Wittig reagent and made up into pharmaceutical compositions.

Vitamin D3 fluorinated homolog

Process for the preparation of therapeutically useful 23,24-didehydro-25-hydroxycalciferol derivatives

GLIOXYL-SYCLOHEXENE-DIONS OF DIKOTILEDONE TO BE USED AS HERBICIDE, EFFECTIVE TO HERBS.

Didehydro- VITAMIN D3 DERIVATIVES.

Ketone compounds and compositions for cholesterol management and related uses

The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention a re also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents .

Ketone compounds and use thereof in preparation of pharmaceutical compositions

A PROCEDURE FOR PREPARING NEW DERIVATIVES OF (4.2.0) BICYCLOOCTANE.

Compounds useful in treating cardiovascular disorders' such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3):wherein:n is 2 or 3;R₁ is CH₂0H, CHO, CO₂R or CO₂H;R₂ is hydrogen or methyl; andR₃ is linear or branched alkyl having 5-10 carbon atoms,optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen,in whicha is 0, 1 or 2;b is 3-7;m is 0, 1 or 2; andorin which R₄ is independently hydrogenor lower alkyl having 1-6 carbon atoms;and the pharmaceutically acceptable, non-toxic salts and esters thereof.

Processes for the preparation of hydroxylated cyclohexyl compounds

The present application relates to processes for the preparation of polyhydroxylated cyclohexyl compounds of Formula I:

Synthesis of 3-keto-cyclopentene-5-oxy derivatives

Didehydrovitamin D ▲ Lower 3 ▼ Derivative

Synthesis and biological activities of new tricyclic-bis-enones (TBEs)

This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-γ, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.

Electron withdrawing group substituted and macrocyclic pgj3 analogs and methods of treatment thereof

In some aspects, the present disclosure provides compounds of the formula: wherein the variables are as defined herein. In some embodiments, the present disclosure provides macrocylic compounds and oligomers thereof of formula I. As described herein, these compounds may be used to treat cancer or other hyperproliferative diseases.

PROCESS FOR THE PREPARATION OF NEW CYCLIC 1,3-DICARBONYL COMPOUNDS

Novel 8-(lower alkyl)bicyclo(4.2.0)octane derivatives with valuable therapeutic properties

Antibacterial compounds

There is an ongoing need for new antibiotics which may be effective against bacteria that are otherwise difficult to control. The present invention therefore relates to new antibacterial triketone compounds of Formula (1), or salts, metal complexes or tautomeric forms of these compounds. The compounds have potential as novel antibiotics. Thus, the invention also relates to methods of treatment or prevention of bacterial infections using the compounds, and to compositions containing them.

METHODS FOR SYNTHESIS OF INGENOL AND ITS INTERMEDIATE COMPOUNDS

A PROCEDURE FOR PREPARING NEW DERIVATIVES OF (4.2.0) BICYCLOOCTANE

Herbicide

Products extracted from a plant of the genus commiphora, particularly the commiphora mukul plant, extracts containing same and applications thereof, for example in cosmetics

Cyclopentanone derivs. - useful in perfume and toilet prepn.s

New structural analogues of vitamin D

Anti-androgenic cyclo and bicyclo alkenes

Compounds having formulae (i), (ii) and (iii), where R is H, alkyl of 1 to 6 carbons, or CO-R2 where R2 is alkyl of 1 to 6 carbons; R1 is H, CH3, or (CH2)m-CH3; n is an integer having the values of 2 to 10, m is an integer having the values of 1 to 6, have anti-androgen activity on secondary androgen receptor sites. The compounds are useful for treating mammals including humans afflicted with acne, male pattern baldness, adhesions and keloids. The compounds are so effective for treating other diseases or conditions which are related to androgen receptors, such as undesirable formation of breast capsules in females after breast augmentation surgery, osteoarthritis and symptom of Alzheimer's disease. The compounds also have inhibitory effect on the metabolism of certain microorganisms and fungi of the kind, the metabolism of which is normally known to be controllable by antiandrogen compounds.

The terpane type compound structure of Euphorbia lathyris two resets method for transformation and its application of derivative

本发明属生物药物领域，涉及新型续随子二萜烷型化合物的制备及在抗肿瘤药物中的应用。所述化合物的结构特征是续随子二萜烷中骈合的三元环发生开环并重排，得到羟基和丙烯基取代的开环化合物。此类化合物是由5/11/3环系的续随子二萜烷型化合物经过拉曼被孢霉Mortierella ramanniana生物转化得到；该类续随子二萜烷型化合物经重排羟化后水溶性增强，提高成药性。进一步，可用于制备抗肿瘤活性的药物或药物组合物。

Terpenoid and preparation method and application thereof

本发明提供了式I所示的萜类化合物或其药学上可接受的盐、酯或水合物。本发明还提供了萜类化合物的制备方法和用途。本发明从益母草中分离得到的降碳二萜类新化合物，为首次从自然界获得的降碳半日花烷型二萜，在体外能明显缩短凝血酶原时间（PT）、活化部分凝血酶原时间（APTT）和凝血酶时间（TT），而且还能明显增加血液中血纤蛋白原（FIB）的量，对凝血功能具有一定的增强作用，为新颖的天然凝血药物的开发提供了新的选择。