IL165321A - אסטראטריאנים המותמרים בעמדה אלפה– 9 כאסטרוגנים הפעילים באופן בררני - Google Patents

אסטראטריאנים המותמרים בעמדה אלפה– 9 כאסטרוגנים הפעילים באופן בררני

Info

Publication number: IL165321A
Authority: IL; Israel
Prior art keywords: oestra; triene; vinyl; diol; homo
Prior art date: 2002-06-11

Application number

IL165321A

Other languages

English (en)

Original Assignee

Bayer Schering Pharma Ag

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2002-06-11

Filing date

2004-11-22

Publication date

2009-08-03

2004-11-22 Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag

2009-08-03 Publication of IL165321A publication Critical patent/IL165321A/he

Links

239000000262 estrogen Substances 0.000 title claims description 32
229940011871 estrogen Drugs 0.000 title description 30
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-1 trifluoromethylthio, methoxy, ethoxy Chemical group 0.000 claims description 84
150000001875 compounds Chemical class 0.000 claims description 48
238000011282 treatment Methods 0.000 claims description 35
125000004432 carbon atom Chemical group C* 0.000 claims description 23
210000002307 prostate Anatomy 0.000 claims description 20
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 16
238000002560 therapeutic procedure Methods 0.000 claims description 16
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 14
238000004519 manufacturing process Methods 0.000 claims description 14
238000000338 in vitro Methods 0.000 claims description 13
125000000217 alkyl group Chemical group 0.000 claims description 12
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 12
210000000988 bone and bone Anatomy 0.000 claims description 10
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 10
201000010099 disease Diseases 0.000 claims description 8
229910052731 fluorine Inorganic materials 0.000 claims description 8
230000002265 prevention Effects 0.000 claims description 8
239000004215 Carbon black (E152) Substances 0.000 claims description 7
125000003710 aryl alkyl group Chemical group 0.000 claims description 7
125000004093 cyano group Chemical group *C#N 0.000 claims description 7
229930195733 hydrocarbon Natural products 0.000 claims description 7
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125000003118 aryl group Chemical group 0.000 claims description 6
239000011737 fluorine Substances 0.000 claims description 6
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238000011321 prophylaxis Methods 0.000 claims description 6
125000001424 substituent group Chemical group 0.000 claims description 6
ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims description 5
WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 5
ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 5
208000007984 Female Infertility Diseases 0.000 claims description 5
GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 5
229910052794 bromium Inorganic materials 0.000 claims description 5
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 5
125000005111 carboxyalkoxy group Chemical group 0.000 claims description 5
239000000460 chlorine Substances 0.000 claims description 5
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206010021928 Infertility female Diseases 0.000 claims description 4
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208000001132 Osteoporosis Diseases 0.000 claims description 4
125000000753 cycloalkyl group Chemical group 0.000 claims description 4
125000001072 heteroaryl group Chemical group 0.000 claims description 4
206010020718 hyperplasia Diseases 0.000 claims description 4
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 4
125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims description 4
125000003107 substituted aryl group Chemical group 0.000 claims description 4
PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 3
125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 3
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 3
125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 3
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GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 claims description 3
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CPEONABTMRSIKA-UHFFFAOYSA-N 1,4$l^{2}-oxazinane Chemical compound C1COCC[N]1 CPEONABTMRSIKA-UHFFFAOYSA-N 0.000 claims description 2
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125000003342 alkenyl group Chemical group 0.000 claims description 2
125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
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LXLNOGZWGYFWQV-MFWBVCSQSA-N (8S,9R,13S,14S,16R)-9-ethenyl-17-fluoro-13-methyl-7,8,11,12,14,15,16,17-octahydro-6H-cyclopenta[a]phenanthrene-3,16-diol Chemical compound FC1[C@]2(C)[C@@H](C[C@H]1O)[C@@H]1CCC=3C=C(C=CC3[C@]1(CC2)C=C)O LXLNOGZWGYFWQV-MFWBVCSQSA-N 0.000 claims 1
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NJQITWAKELCMAY-DABHTEOTSA-N (8s,9r,13r,14s,16r)-9-ethenyl-13-methyl-7,8,11,12,14,15,16,17-octahydro-6h-cyclopenta[a]phenanthrene-3,16-diol Chemical compound C1CC2=CC(O)=CC=C2[C@]2(C=C)[C@@H]1[C@@H]1C[C@@H](O)C[C@@]1(C)CC2 NJQITWAKELCMAY-DABHTEOTSA-N 0.000 claims 1
VWAHIVOFRSQMGC-OBJCFNGXSA-N (8s,9s,13r,14s,16r)-13-methyl-9-propyl-7,8,11,12,14,15,16,17-octahydro-6h-cyclopenta[a]phenanthrene-3,16-diol Chemical compound C1CC2=CC(O)=CC=C2[C@]2(CCC)[C@@H]1[C@@H]1C[C@@H](O)C[C@@]1(C)CC2 VWAHIVOFRSQMGC-OBJCFNGXSA-N 0.000 claims 1
ZKGGIOCJNCBSDH-KNOXWWKRSA-N C(C)(=O)O[C@H]1C[C@H]2[C@@H]3CCC[C@@]3(C)CC[C@@]2(C=2C=CC(=CC12)O)C=C Chemical compound C(C)(=O)O[C@H]1C[C@H]2[C@@H]3CCC[C@@]3(C)CC[C@@]2(C=2C=CC(=CC12)O)C=C ZKGGIOCJNCBSDH-KNOXWWKRSA-N 0.000 claims 1
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Classifications

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- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
- C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids

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Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Immunology (AREA)
Physical Education & Sports Medicine (AREA)
Reproductive Health (AREA)
Rheumatology (AREA)
Endocrinology (AREA)
Epidemiology (AREA)
Orthopedic Medicine & Surgery (AREA)
Neurology (AREA)
Pregnancy & Childbirth (AREA)
Pain & Pain Management (AREA)
Cardiology (AREA)
Biomedical Technology (AREA)
Diabetes (AREA)
Gynecology & Obstetrics (AREA)
Neurosurgery (AREA)
Urology & Nephrology (AREA)
Transplantation (AREA)
Heart & Thoracic Surgery (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Steroid Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

IL165321A 2002-06-11 2004-11-22 אסטראטריאנים המותמרים בעמדה אלפה– 9 כאסטרוגנים הפעילים באופן בררני IL165321A (he)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
DE10226326A DE10226326A1 (de)	2002-06-11	2002-06-11	9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene
PCT/EP2003/006172 WO2003104253A2 (de)	2002-06-11	2003-06-11	9-alpha-substituierte estratriene als selektiv wirksame estrogene

Publications (1)

Publication Number	Publication Date
IL165321A true IL165321A (he)	2009-08-03

Family

ID=29723144

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL165321A IL165321A (he)	2002-06-11	2004-11-22	אסטראטריאנים המותמרים בעמדה אלפה– 9 כאסטרוגנים הפעילים באופן בררני

Country Status (28)

Country	Link
EP (1)	EP1517914B1 (he)
JP (1)	JP4615998B2 (he)
KR (1)	KR101006612B1 (he)
CN (1)	CN1293090C (he)
AR (1)	AR040188A1 (he)
AT (1)	ATE303397T1 (he)
AU (1)	AU2003242683B9 (he)
BR (1)	BR0312140A (he)
CA (1)	CA2486495C (he)
CR (1)	CR10289A (he)
CU (1)	CU23414B7 (he)
DE (2)	DE10226326A1 (he)
DK (1)	DK1517914T3 (he)
EA (1)	EA008442B1 (he)
EC (1)	ECSP055530A (he)
ES (1)	ES2248770T3 (he)
HR (1)	HRP20050009B1 (he)
IL (1)	IL165321A (he)
MX (1)	MXPA04012491A (he)
NO (1)	NO329563B1 (he)
PE (1)	PE20040613A1 (he)
PL (1)	PL209910B1 (he)
RS (1)	RS50878B (he)
TW (1)	TWI286140B (he)
UA (1)	UA78062C2 (he)
UY (1)	UY27844A1 (he)
WO (1)	WO2003104253A2 (he)
ZA (1)	ZA200500217B (he)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE10027887A1 (de)	2000-05-31	2001-12-13	Jenapharm Gmbh	Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
PT1689410E (pt) *	2003-11-26	2008-08-18	Bayer Schering Pharma Ag	Prevenção e tratamento de doenças cardíacas hipertensivas pelos estrogénios selectivos 8beta-vinil-estra-1,3,5(10)-trieno-3,17beta-diol e 17beta-fluoro-9alfa-vinil-estra-1,3,5(10)-trieno-3,16alfa-diol
US7534780B2 (en)	2004-05-21	2009-05-19	Bayer Schering Pharma Aktiengesellschaft	Estradiol prodrugs
DE102005057224A1 (de) *	2005-11-29	2007-05-31	Bayer Schering Pharma Ag	Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
US20110052699A1 (en) *	2008-02-13	2011-03-03	Adrian Funke	Drug delivery system with stabilising effect
EP2143432A1 (en)	2008-07-11	2010-01-13	Bayer Schering Pharma AG	9-alpha estratriene derivatives as ER-beta selective ligands for the prevention and treatment of intestinal cancer
JP2012509286A (ja) *	2008-11-21	2012-04-19	バイエルファーマアクチエンゲゼルシャフト	薬物送達システム
EP3185881B1 (en)	2014-08-26	2022-03-09	Betanien Hospital	Methods, agents and compositions for treatment of inflammatory conditions
WO2020051329A1 (en) *	2018-09-07	2020-03-12	Trustees Of Dartmouth College	C19 scaffolds and steroids and methods of use and manufacture thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE2336432A1 (de) *	1973-07-13	1975-01-30	Schering Ag	3.17.18-trihydroxy-1.3.5(10)-oestratriene
US6154158A (en) *	1998-06-30	2000-11-28	Qualcomm Incorporated	Digital-to-analog converter D.C. offset correction comparing converter input and output signals
DE19906159A1 (de) *	1999-02-09	2000-08-10	Schering Ag	16-Hydroxyestratriene als selektiv wirksame Estrogene
EP1226155B1 (de) *	1999-11-02	2007-05-02	Bayer Schering Pharma AG	18-nor-steroide als selektiv wirksame estrogene
SK14632002A3 (sk) *	2000-04-12	2003-03-04	Schering Aktiengesellschaft	Substituované estratriény a ich použitie ako selektívne účinných estrogénov

2002
- 2002-06-11 DE DE10226326A patent/DE10226326A1/de not_active Ceased
2003
- 2003-06-10 PE PE2003000575A patent/PE20040613A1/es not_active Application Discontinuation
- 2003-06-11 RS YUP-1070/04A patent/RS50878B/sr unknown
- 2003-06-11 CN CNB038135027A patent/CN1293090C/zh not_active Expired - Fee Related
- 2003-06-11 AU AU2003242683A patent/AU2003242683B9/en not_active Ceased
- 2003-06-11 EP EP03757065A patent/EP1517914B1/de not_active Expired - Lifetime
- 2003-06-11 PL PL373090A patent/PL209910B1/pl not_active IP Right Cessation
- 2003-06-11 AT AT03757065T patent/ATE303397T1/de active
- 2003-06-11 DE DE50301116T patent/DE50301116D1/de not_active Expired - Lifetime
- 2003-06-11 KR KR1020047020133A patent/KR101006612B1/ko not_active Expired - Fee Related
- 2003-06-11 EA EA200401544A patent/EA008442B1/ru not_active IP Right Cessation
- 2003-06-11 UY UY27844A patent/UY27844A1/es not_active Application Discontinuation
- 2003-06-11 WO PCT/EP2003/006172 patent/WO2003104253A2/de not_active Ceased
- 2003-06-11 ES ES03757065T patent/ES2248770T3/es not_active Expired - Lifetime
- 2003-06-11 DK DK03757065T patent/DK1517914T3/da active
- 2003-06-11 BR BR0312140-2A patent/BR0312140A/pt not_active IP Right Cessation
- 2003-06-11 MX MXPA04012491A patent/MXPA04012491A/es active IP Right Grant
- 2003-06-11 AR ARP030102079A patent/AR040188A1/es active IP Right Grant
- 2003-06-11 HR HRP20050009AA patent/HRP20050009B1/hr not_active IP Right Cessation
- 2003-06-11 JP JP2004511321A patent/JP4615998B2/ja not_active Expired - Fee Related
- 2003-06-11 CA CA2486495A patent/CA2486495C/en not_active Expired - Fee Related
- 2003-06-11 TW TW092115863A patent/TWI286140B/zh not_active IP Right Cessation
- 2003-11-06 UA UAA200500212A patent/UA78062C2/uk unknown
2004
- 2004-11-22 IL IL165321A patent/IL165321A/he not_active IP Right Cessation
- 2004-12-10 CU CU20040282A patent/CU23414B7/es not_active IP Right Cessation
2005
- 2005-01-10 EC EC2005005530A patent/ECSP055530A/es unknown
- 2005-01-10 NO NO20050127A patent/NO329563B1/no not_active IP Right Cessation
2006
- 2006-01-10 ZA ZA200500217A patent/ZA200500217B/en unknown
2008
- 2008-09-16 CR CR10289A patent/CR10289A/es not_active Application Discontinuation

Also Published As

Publication number	Publication date
ATE303397T1 (de)	2005-09-15
HRP20050009A2 (en)	2005-04-30
ECSP055530A (es)	2005-03-10
UA78062C2 (en)	2007-02-15
CA2486495A1 (en)	2003-12-18
HRP20050009B1 (hr)	2013-07-31
WO2003104253A2 (de)	2003-12-18
CU23414B7 (es)	2009-09-08
EA008442B1 (ru)	2007-06-29
WO2003104253A3 (de)	2004-09-16
NO20050127D0 (no)	2005-01-10
EP1517914B1 (de)	2005-08-31
DE50301116D1 (de)	2005-10-06
MXPA04012491A (es)	2005-06-08
BR0312140A (pt)	2005-04-05
JP4615998B2 (ja)	2011-01-19
RS50878B (sr)	2010-08-31
KR20050009745A (ko)	2005-01-25
CA2486495C (en)	2011-04-19
PL373090A1 (en)	2005-08-08
AU2003242683A1 (en)	2003-12-22
AR040188A1 (es)	2005-03-16
PL209910B1 (pl)	2011-11-30
JP2005533053A (ja)	2005-11-04
AU2003242683B9 (en)	2009-08-27
EA200401544A1 (ru)	2005-06-30
KR101006612B1 (ko)	2011-01-10
HK1081203A1 (en)	2006-05-12
CR10289A (es)	2008-11-26
TWI286140B (en)	2007-09-01
CN1659181A (zh)	2005-08-24
CN1293090C (zh)	2007-01-03
EP1517914A2 (de)	2005-03-30
PE20040613A1 (es)	2004-12-01
RS107004A (sr)	2006-10-27
UY27844A1 (es)	2003-12-31
NO20050127L (no)	2005-03-11
TW200407331A (en)	2004-05-16
ZA200500217B (en)	2006-03-29
DK1517914T3 (da)	2006-01-16
ES2248770T3 (es)	2006-03-16
NO329563B1 (no)	2010-11-15
DE10226326A1 (de)	2004-01-15
AU2003242683B2 (en)	2009-07-02

Legal Events

Date	Code	Title	Description
2013-06-27	KB	Patent renewed
2018-01-31	MM9K	Patent not in force due to non-payment of renewal fees

Publication	Publication Date	Title
US7414043B2 (en)	2008-08-19	9-α-substituted estratrienes as selectively active estrogens
US7378404B2 (en)	2008-05-27	8β-hydrocarbyl-substituted estratrienes for use as selective estrogens
EP1169336B1 (en)	2006-02-01	Ent-steroids as selectively active estrogens
CA2486495C (en)	2011-04-19	9-alpha-substituted estratrienes as selectively active estrogens
JP2003513102A (ja)	2003-04-08	選択的な作用を有するエストロゲンとしての１８−ノル−ステロイド
EP2176282B1 (en)	2012-08-22	8-beta-substituted 16.alpha.-fluoro-estratrienes as selectively active estrogens
JP2003534248A (ja)	2003-11-18	選択的活性エストロゲンとしての８β−ヒドロカルビル置換エストラトリエン
NZ536882A (en)	2007-07-27	9-Alpha-substituted estratrienes as selectively active estrogens
US20030171345A1 (en)	2003-09-11	8Beta-substituted 11beta-aryl-estra-1,3,5,(10)-triene derivatives
HK1142612A (en)	2010-12-10	8-beta-substituted estratrienes as selectively active estrogens