Title:
神経保護特性を有する両親媒性化合物
Document Type and Number:
Japanese Patent JP6437636
Kind Code:
B2
Abstract:
The present invention provides amphiphilic compounds with a tetradecahydrophenanthrene skeleton of formula (I), wherein R1-R5 are as defined herein, and their enantiomers, exhibiting neuroprotective effects, for use as medicaments for treating neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain , addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing said compound.
Inventors:
Gudva, Eva
Haudunska, Hana
Kaplus, Voitev
Vikritsky, Ladislav
Valles, charles
Yarn, Ulriff
Haudunska, Hana
Kaplus, Voitev
Vikritsky, Ladislav
Valles, charles
Yarn, Ulriff
Application Number:
JP2017511948A
Publication Date:
December 12, 2018
Filing Date:
August 25, 2015
Export Citation:
Assignee:
Ustaf Organikke Hemier Abiohemie Academia Ved Zeer, Wei Wei
Fizio Logikki Ustaf Ave Zeer, V.V.E.
Fizio Logikki Ustaf Ave Zeer, V.V.E.
International Classes:
C07C305/20; A23L33/10; A61K8/37; A61K8/46; A61K31/185; A61K31/215; A61K31/56; A61K31/568; A61K31/5685; A61K31/57; A61K31/575; A61K31/58; A61P9/10; A61P23/00; A61P25/00; A61P25/04; A61P25/08; A61P25/14; A61P25/18; A61P25/20; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P35/00; A61Q19/08; A61Q90/00; C07C69/40; C07C229/24; C07J1/00; C07J9/00; C07J13/00; C07J31/00; C07J41/00; C07J43/00
Foreign References:
US5888996 | ||||
WO1998005337A1 | ||||
WO2010136000A1 | ||||
WO2001016601A1 | ||||
WO2012110010A1 | ||||
WO2012019106A1 |
Other References:
BOLGER M B,IN VITRO AND IN VIVO ACTIVITY OF 16,17-DEHYDRO-EPIPREGNANOLONES: 17,20-BOND TORSIONAL 以下備考,PHARMACEUTICAL RESEARCH,米国,SPRINGER NEW YORK LLC,1996年,VOL:13, NR:10,PAGE(S):1488 - 1494,ENERGY ANALYSIS AND D-RING CONFORMATION,URL,http://dx.doi.org/10.1023/A:1016019327120
Journal of Medicinal Chemistry,1968年,Vol.11(1),p.117-125
Brain Research,1979年,Vol.160(2),p.295-305
JIRINA BOROVSKA,ACCESS OF INHIBITORY NEUROSTEROIDS TO THE NMDA RECEPTOR,BRITISH JOURNAL OF PHARMACOLOGY,英国,2012年 5月 8日,VOL:166, NR:3,PAGE(S):1069 - 1083,URL,http://dx.doi.org/10.1111/j.1476-5381.2011.01816.x
ATKINSON R M,ACTION OF SOME STEROIDS ON THE CENTRAL NERVOUS SYSTEM OF THE MOUSE. II. PHARMACOLOGY,JOURNAL OF MEDICINAL CHEMISTRY,米国,AMERICAN CHEMICAL SOCIETY,1965年 7月,VOL:8, NR:4,PAGE(S):426 - 432,URL,http://dx.doi.org/10.1021/jm00328a004
O'DELL L E,EPIPREGNANOLONE AND A NOVEL SYNTHETIC NEUROACTIVE STEROID REDUCE ALCOHOL SELF-ADMINISTRATION IN RATS,PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR,米国,ELSEVIER,2005年 6月 9日,VOL:81, NR:3,PAGE(S):543 - 550,URL,http://dx.doi.org/10.1016/j.pbb.2005.03.020
STASTNA E,SYNTHESIS OF C3, C5, AND C7 PREGNANE DERIVATIVES AND THEIR EFFECT ON NMDA RECEPTOR 以下備考,STEROIDS,米国,ELSEVIER SCIENCE PUBLISHERS,2008年11月24日,VOL:74, NR:2,PAGE(S):256 - 263,RESPONSES IN CULTURED RAT HIPPOCAMPAL NEURONS,URL,http://dx.doi.org/10.1016/j.steroids.2008.11.011
Journal of Medicinal Chemistry,1968年,Vol.11(1),p.117-125
Brain Research,1979年,Vol.160(2),p.295-305
JIRINA BOROVSKA,ACCESS OF INHIBITORY NEUROSTEROIDS TO THE NMDA RECEPTOR,BRITISH JOURNAL OF PHARMACOLOGY,英国,2012年 5月 8日,VOL:166, NR:3,PAGE(S):1069 - 1083,URL,http://dx.doi.org/10.1111/j.1476-5381.2011.01816.x
ATKINSON R M,ACTION OF SOME STEROIDS ON THE CENTRAL NERVOUS SYSTEM OF THE MOUSE. II. PHARMACOLOGY,JOURNAL OF MEDICINAL CHEMISTRY,米国,AMERICAN CHEMICAL SOCIETY,1965年 7月,VOL:8, NR:4,PAGE(S):426 - 432,URL,http://dx.doi.org/10.1021/jm00328a004
O'DELL L E,EPIPREGNANOLONE AND A NOVEL SYNTHETIC NEUROACTIVE STEROID REDUCE ALCOHOL SELF-ADMINISTRATION IN RATS,PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR,米国,ELSEVIER,2005年 6月 9日,VOL:81, NR:3,PAGE(S):543 - 550,URL,http://dx.doi.org/10.1016/j.pbb.2005.03.020
STASTNA E,SYNTHESIS OF C3, C5, AND C7 PREGNANE DERIVATIVES AND THEIR EFFECT ON NMDA RECEPTOR 以下備考,STEROIDS,米国,ELSEVIER SCIENCE PUBLISHERS,2008年11月24日,VOL:74, NR:2,PAGE(S):256 - 263,RESPONSES IN CULTURED RAT HIPPOCAMPAL NEURONS,URL,http://dx.doi.org/10.1016/j.steroids.2008.11.011
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