公开(公告)号：EP2222690A2

公开(公告)日：2010-09-01

申请号：EP08801032.7

申请日：2008-08-20

申请人： Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky ,  Univerzita palackeho V Olomouci

发明人： OKLESTKOVA, Jana ,  HOFFMANNOVÁ, Lucie ,  STEIGEROVÁ,, Jana ,  KOHOUT, Ladislav ,  KOLAR, Zdenek ,  STRNAD, Miroslav

IPC分类号： C07J73/00 ,  A61K31/575 ,  A61K31/58 ,  C07D313/10 ,  C07J9/00 ,  C07J17/00 ,  A61P35/04

CPC分类号： C07J17/005 ,  C07D313/06 ,  C07D313/10 ,  C07J9/00 ,  C07J73/00

摘要： The present invention relates to natural brassinosteroids of general formula (I), wherein R is CH2 or O-CH2 group, R2 is hydrogen or hydroxyl, R3 is hydroxyl, R24 is alkyl or alkenyl, which are selected from the group consisting of methyl, ethyl, propyl, isopropyl, methylen, ethylen and propylen, and R25 is alkyl selected from the group consisting of methyl and ethyl, and a pharmaceutically acceptable salt thereof, for use for treating hyperproliferation, treating proliferative diseases and reducing adverse effects of steroid dysfunction in mammals. The present invention also provides methods capable to arrest of the cell cycle by natural brassinosteroids resulting in apoptotic changes in cancer cells. More specifically, the present invention relates to use for treatment of the adverse effects of hyperproliferation on mammalian cells in vitro and in vivo, especially treatment of hyperproliferative diseases in mammals by administering compositions containing natural brassinosteroids. This invention also describes new use for treating consisting in a new therapeutic way for modifying cell viability of human breast and prostate cancer cells.

公开(公告)号：EP1401278A1

公开(公告)日：2004-03-31

申请号：EP02740217.1

申请日：2002-07-02

申请人： Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky

发明人： KOHOUT, Ladislav ,  KASAL, Alexander ,  CHODOUNSKA, HANA ,  SLAVIKOVA, Barbora ,  HNILICKOVA, Jaroslava

IPC分类号： A01N45/00

CPC分类号： A01N45/00 ,  A01N25/30 ,  A01N25/02 ,  A01N2300/00

摘要： The use of 2α,3α,17SS-trihydroxy-5α-androstan-6-one as active ingredient for plant development regulation in the form of application solution is made by dissolving active ingredients in appropriate solvent to appropriate concentration, which is then diluted with water and the application solution obtained is applied to plants.

公开(公告)号：EP2283025A1

公开(公告)日：2011-02-16

申请号：EP09721251.8

申请日：2009-03-19

申请人： Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky

发明人： SLAVIKOVA, Barbosa ,  KASAL Alexander ,  KOHOUT, Ladislav ,  BUDESINSKY, Milos ,  SWACZYNOVA, Jana

IPC分类号： C07J1/00 ,  A01N45/00

CPC分类号： C07J1/007 ,  A01N45/00 ,  Y02P20/55

摘要： 5-Fluoro-3α,17β-dihydroxy-5α-androstan-6-one IV and the method of its production are described. The synthesis consists of partial hydrolyses of 5-fluoro-6-oxo-5α-androstan-3β,17β-diyl diacetate with mild alkaline agent to 5-fluoro-3β-hydroxy-6-oxo-5α-androstan-17β-yl acetate that on solvolytic change of hydroxyl configuration in position 3 affords 5-fluoro-3α-hydroxy-6-oxo-5α-androstan-17β-yl acetate, which on deprotection afforded desired 5-fluoro-3α,17β-dihydroxy-5α-androstan-6-one IV. The invention relates also to the use of 5-fluoro-3α,17β-dihydroxy-5α-androstaii-6-one IV for influencing of plant growth, especially for increasing of plant yield and also for removal of plant stresses.

摘要翻译： 描述了5-氟-3α，17β-二羟基-5α-雄甾烷-6-酮IV及其制备方法。 该合成由5-氟-6-氧代-5α-雄甾烷-3β，17β-二乙酸二乙酯与弱碱性试剂部分水解成5-氟-3β-羟基-6-氧代-5α-雄甾烷-17β-基乙酸酯 在3位羟基构型的溶剂分解变化上得到乙酸5-氟-3α-羟基-6-氧代-5α-雄甾烷-17β-基，其在脱保护下得到所需的5-氟-3α，17β-二羟基-5α-雄甾烷 -6-one IV。 本发明还涉及5-氟-3α，17β-二羟基-5α-雄甾烷-6-酮IV用于影响植物生长，尤其用于提高植物产量并且还用于去除植物胁迫的用途。

公开(公告)号：EP2313424A2

公开(公告)日：2011-04-27

申请号：EP09775815.5

申请日：2009-07-09

申请人： Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky ,  Fyziolqgicky Ustavakademie Ved Ceske Republiky V.v

发明人： STASTNA, Eva ,  CHODOUNSKA, Hana ,  POUZAR, Vladimir ,  KAPRAS, Vojtech ,  CAIS, Ondrej ,  VYKLICKY, Ladislav ,  KOHOUT, Ladislav

IPC分类号： C07J7/00 ,  C07J31/00 ,  A61K31/58 ,  A61K31/57

CPC分类号： C07J41/0077 ,  C07J7/002 ,  C07J31/006

摘要： This invention relates to pregnane anionic compounds of general formula I in which R
1 is ester group, which is able to form ion such as sulfate, pyridinium sulfate, hemisuccinate etc., R
2 is hydrogen atom in alpha or beta configuration, and R
3 is ester group, as is acetoxy group, nicotinoyloxy group etc., and their pharmaceutically acceptable salts. Compounds of general formula I are preferably produced from the diol of formula II or diol of formula VIII, which are converted according to described sequence of reactions, to compounds of general formula I, in which R
1 is ester group, which is able to form ion such as sulfate, pyridinium sulfate, hemisuccinate etc., R
2 is hydrogen atom in alpha or beta configuration, and R
3 is ester group. The compounds of general formula I are useful as active ingredients for production of pharmaceuticals for the treatment of neurological and psychiatric diseases and conditions associated with excessive activation of NMDA receptors such as neuroprotective agents against excitotoxic damage of the central nervous system (CNS), conditions associated with excessive activation of NMDA-subtype glutamate receptors or, where this type of receptor is involved in the creation or during the certain mental and neurological diseases, in particular concerning the traumatic and hypoxic damage Io nervous tissue in the central nervous system diseases, such as Alzheimer's, Huntington's and Parkinson's disease, also in cognitive disorders in aging; the other indications could be tardive dyskinesia, amyotrophic lateral sclerosis, olivopontocerebellar degeneration, neurological problems1 associated with AIDS infection, allergic encephalomyelitis, and for medication of epilepsy, anxiety, depression, schizophrenia, chronic pain and drug addiction.

公开(公告)号：EP2142646B1

公开(公告)日：2014-11-19

申请号：EP08734303.4

申请日：2008-04-14

申请人： Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky

发明人： MACEK, Tomás ,  UHLÍK, Ondrej ,  KAMLAR, Marek ,  HARMATHA, Juraj ,  KOHOUT, Ladislav

IPC分类号： C12N9/88 ,  C07J73/00

CPC分类号： C07J73/003 ,  A01H3/04 ,  A01N59/16 ,  A01N61/00 ,  C12N9/88 ,  Y02P60/247 ,  A01N45/00 ,  A01N45/02 ,  A01N2300/00

公开(公告)号：EP2142646A2

公开(公告)日：2010-01-13

申请号：EP08734303.4

申请日：2008-04-14

申请人： Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky

发明人： MACEK, Thomás ,  UHLÍK, Ondrej ,  KAMLAR, Marek ,  HARMATHA, Juraj ,  KOHOUT, Ladislav

IPC分类号： C12N9/88 ,  C07J73/00

CPC分类号： C07J73/003 ,  A01H3/04 ,  A01N59/16 ,  A01N61/00 ,  C12N9/88 ,  Y02P60/247 ,  A01N45/00 ,  A01N45/02 ,  A01N2300/00

摘要： This invention deals with a method of increasing the yield of photosynthetic assimilation of carbon dioxide in plants by means of application of agents that increase the carboxylase activity of the enzyme ribulose 1,5-bisphosphate carboxylase/oxygenase (RuBisCO, EC 4.1.1.39). It leads as to increase of green mass of agricultural products as decrease of carbon dioxide in atmosphere.

公开(公告)号：EP2435463A2

公开(公告)日：2012-04-04

申请号：EP10744655.1

申请日：2010-05-28

申请人： Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky ,  Fyziologický Ústav Akademie VÊD Ceské Republiky V.V.I. ,  Psychiatrické Centrum Praha

发明人： CHODOUNSKÁ, Hana ,  STASTNÁ, Eva ,  KAPRAS, Vojtech ,  KOHOUT, Ladislav ,  BOROVSKÁ, Jirna ,  VYKLICKY, Ladislav ,  VALEs, Karel ,  CAIS, Ondrej ,  RAMBOUSEK, Lukás ,  STUCHLÍK, Ales ,  BUBENÍKOVÁ VALESOVÁ, Vera

IPC分类号： C07J7/00 ,  C07J41/00 ,  A61K31/57 ,  A61P25/02 ,  A61P25/08 ,  A61P25/24 ,  A61P25/18 ,  A61P25/04 ,  A61P25/30 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07J41/005 ,  C07J7/002 ,  Y02P20/55

摘要： The presented invention applies to the compounds with general formula I, where R 1 stands for a group of the general formula R 3 OOC-R 2- C (R 4 )-R 5 -, where R 2 stands for alkyl or alkenyl group with 1 to 18 carbon in a straight or a branching carbon chain, which may be substituted by one or more halogen atoms; R 3 represents either a hydrogen atom or a protecting group of carboxyl groups, preferably benzyl group; R 4 represents oxygen atom, nitrogen atom or a sulfur atom bound by a double bond or R 4 represents two hydrogen atoms; R 5 represents any at least bivalent atom, preferably an oxygen atom, nitrogen, or carbon atom, except when R 2 represents the group -(CH 2 ) n - where n = 0-3 and simultaneously R 3 represents a hydrogen atom and R 4 and R 5 represent an oxygen atom. The present invention also relates to the production process of the compounds with general formula I, where R 1 stands for as mentioned previously, the compounds with general formula I for use in treatment of various diseases of central nervous system, in treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, PTSD and other diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy and gliomas. This invention further applies to the compounds with general formula I for use in the production of veterinary and human pharmaceutical preparations for use in treatment of above mentioned diseases as well as in production of substances used in experimental research, analytic chemistry, dietary supplements or cosmetic preparations.

公开(公告)号：EP2283025B1

公开(公告)日：2011-12-07

申请号：EP09721251.8

申请日：2009-03-19

申请人： Ustav Organicke Chemie a Biochemie Akademie Ved Ceske Republiky, V.V.I.

发明人： SLAVIKOVA, Barbora ,  KASAL, Alexander ,  KOHOUT, Ladislav ,  BUDESINSKY, Milos ,  SWACZYNOVA, Jana

IPC分类号： C07J1/00 ,  A01N45/00

CPC分类号： C07J1/007 ,  A01N45/00 ,  Y02P20/55

摘要： 5-Fluoro-3α,17β-dihydroxy-5α-androstan-6-one IV and the method of its production are described. The synthesis consists of partial hydrolyses of 5-fluoro-6-oxo-5α-androstan-3β,17β-diyl diacetate with mild alkaline agent to 5-fluoro-3β-hydroxy-6-oxo-5α-androstan-17β-yl acetate that on solvolytic change of hydroxyl configuration in position 3 affords 5-fluoro-3α-hydroxy-6-oxo-5α-androstan-17β-yl acetate, which on deprotection afforded desired 5-fluoro-3α,17β-dihydroxy-5α-androstan-6-one IV. The invention relates also to the use of 5-fluoro-3α,17β-dihydroxy-5α-androstaii-6-one IV for influencing of plant growth, especially for increasing of plant yield and also for removal of plant stresses.

公开(公告)号：EP1401278B1

公开(公告)日：2005-09-28

申请号：EP02740217.1

申请日：2002-07-02

申请人： Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky

发明人： KOHOUT, Ladislav ,  KASAL, Alexander ,  CHODOUNSKA, HANA ,  SLAVIKOVA, Barbora ,  HNILICKOVA, Jaroslava

IPC分类号： A01N45/00

CPC分类号： A01N45/00 ,  A01N25/30 ,  A01N25/02 ,  A01N2300/00

摘要： The use of 2α,3α,17SS-trihydroxy-5α-androstan-6-one as active ingredient for plant development regulation in the form of application solution is made by dissolving active ingredients in appropriate solvent to appropriate concentration, which is then diluted with water and the application solution obtained is applied to plants.