ZA200100201B - Novel antiestrogens, a method for the production thereof, and their pharmaceutical application. - Google Patents
Novel antiestrogens, a method for the production thereof, and their pharmaceutical application. Download PDFInfo
- Publication number
- ZA200100201B ZA200100201B ZA200100201A ZA200100201A ZA200100201B ZA 200100201 B ZA200100201 B ZA 200100201B ZA 200100201 A ZA200100201 A ZA 200100201A ZA 200100201 A ZA200100201 A ZA 200100201A ZA 200100201 B ZA200100201 B ZA 200100201B
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- ZA
- South Africa
- Prior art keywords
- group
- stands
- bicyclo
- optionally substituted
- methyl
- Prior art date
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- 238000000034 method Methods 0.000 title claims description 28
- 238000004519 manufacturing process Methods 0.000 title claims description 15
- 230000001833 anti-estrogenic effect Effects 0.000 title description 18
- 229940046836 anti-estrogen Drugs 0.000 title description 12
- 239000000328 estrogen antagonist Substances 0.000 title description 12
- 150000001875 compounds Chemical class 0.000 claims description 175
- -1 heteroaryl radical Chemical class 0.000 claims description 69
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 54
- 229910052799 carbon Inorganic materials 0.000 claims description 43
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 38
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 33
- 125000000217 alkyl group Chemical group 0.000 claims description 30
- 229910052739 hydrogen Inorganic materials 0.000 claims description 27
- 125000006239 protecting group Chemical group 0.000 claims description 27
- 239000001257 hydrogen Substances 0.000 claims description 21
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 15
- 125000002947 alkylene group Chemical group 0.000 claims description 14
- 125000004432 carbon atom Chemical group C* 0.000 claims description 14
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- 239000000126 substance Substances 0.000 claims description 13
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- YCBSHDKATAPNIA-UHFFFAOYSA-N non-3-ene Chemical compound CCCCCC=CCC YCBSHDKATAPNIA-UHFFFAOYSA-N 0.000 claims description 12
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
- C07D303/02—Compounds containing oxirane rings
- C07D303/12—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
- C07D303/18—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by etherified hydroxyl radicals
- C07D303/20—Ethers with hydroxy compounds containing no oxirane rings
- C07D303/22—Ethers with hydroxy compounds containing no oxirane rings with monohydroxy compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
- C07C217/14—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/16—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C317/18—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/10—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C323/11—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/12—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C43/00—Ethers; Compounds having groups, groups or groups
- C07C43/02—Ethers
- C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
- C07C43/23—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/14—All rings being cycloaliphatic
- C07C2602/24—All rings being cycloaliphatic the ring system containing nine carbon atoms, e.g. perhydroindane
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Endocrinology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Epoxy Compounds (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19826213A DE19826213A1 (de) | 1998-06-09 | 1998-06-09 | Neue Antiestrogene, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung |
Publications (1)
Publication Number | Publication Date |
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ZA200100201B true ZA200100201B (en) | 2002-01-08 |
Family
ID=7870694
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ZA200100201A ZA200100201B (en) | 1998-06-09 | 2001-01-08 | Novel antiestrogens, a method for the production thereof, and their pharmaceutical application. |
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US (3) | US6166075A (es) |
EP (1) | EP1086077B1 (es) |
JP (1) | JP2002517482A (es) |
KR (1) | KR20010052688A (es) |
CN (1) | CN1305457A (es) |
AR (1) | AR023629A1 (es) |
AT (1) | ATE263755T1 (es) |
AU (1) | AU759942B2 (es) |
BR (1) | BR9911103A (es) |
CA (1) | CA2334780A1 (es) |
CO (1) | CO5050355A1 (es) |
DE (2) | DE19826213A1 (es) |
DK (1) | DK1086077T3 (es) |
ES (1) | ES2220072T3 (es) |
HU (1) | HUP0102211A3 (es) |
IL (1) | IL139863A0 (es) |
PE (1) | PE20000541A1 (es) |
PL (1) | PL344309A1 (es) |
PT (1) | PT1086077E (es) |
WO (1) | WO1999064393A1 (es) |
ZA (1) | ZA200100201B (es) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE19826213A1 (de) * | 1998-06-09 | 1999-12-16 | Schering Ag | Neue Antiestrogene, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung |
US6525069B1 (en) | 1998-12-18 | 2003-02-25 | Bristol-Myers Squibb Pharma Co. | N-ureidoalkyl-piperidines as modulators of chemokine receptor activity |
DE10039199A1 (de) * | 2000-08-10 | 2002-02-21 | Schering Ag | Kombinationspräparate aus einem ERß selektiven Estrogen und einem SERM oder Antiestrogen |
WO2002064142A1 (en) * | 2001-02-15 | 2002-08-22 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with antiestrogen agents |
DE10142881A1 (de) * | 2001-09-03 | 2003-04-03 | Jomed Gmbh | Implantate mit Combretastatin A-4 (CA4) |
US7183445B2 (en) | 2003-05-31 | 2007-02-27 | Janssen Pharmaceutica N.V | Cyclohexyl derivatives as selective estrogen receptor modulators |
US7750631B2 (en) * | 2007-06-22 | 2010-07-06 | Morpho Detection, Inc. | Passenger inspection system and methods for using the same |
US20090234024A1 (en) | 2008-02-04 | 2009-09-17 | Hooman Shadnia | Estrogenic compounds, process for their production and pharmaceutical uses thereof |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
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US4133814A (en) * | 1975-10-28 | 1979-01-09 | Eli Lilly And Company | 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents |
FR2685332A1 (fr) * | 1991-12-20 | 1993-06-25 | Roussel Uclaf | Nouveaux 19-nor sterouides ayant en position 11beta une chaine thiocarbonee, leur procede de preparation et les intermediaires et leur application a titre de medicaments. |
US5482949A (en) * | 1993-03-19 | 1996-01-09 | Eli Lilly And Company | Sulfonate derivatives of 3-aroylbenzo[b]thiophenes |
FR2744445B1 (fr) * | 1996-02-01 | 1998-10-02 | Roussel Uclaf | Composes biphenyles nouveaux et/ou a titre de medicament, compositions pharmaceutiques les contenant, leur procede de preparation et les intermediaires de ce procede |
DE19826213A1 (de) * | 1998-06-09 | 1999-12-16 | Schering Ag | Neue Antiestrogene, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung |
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1998
- 1998-06-09 DE DE19826213A patent/DE19826213A1/de not_active Withdrawn
-
1999
- 1999-06-07 PE PE1999000482A patent/PE20000541A1/es not_active Application Discontinuation
- 1999-06-08 CO CO99035556A patent/CO5050355A1/es unknown
- 1999-06-09 WO PCT/EP1999/004049 patent/WO1999064393A1/de not_active Application Discontinuation
- 1999-06-09 DK DK99931059T patent/DK1086077T3/da active
- 1999-06-09 HU HU0102211A patent/HUP0102211A3/hu unknown
- 1999-06-09 DE DE59909123T patent/DE59909123D1/de not_active Expired - Fee Related
- 1999-06-09 KR KR1020007013943A patent/KR20010052688A/ko not_active Application Discontinuation
- 1999-06-09 AU AU47716/99A patent/AU759942B2/en not_active Ceased
- 1999-06-09 PL PL99344309A patent/PL344309A1/xx not_active Application Discontinuation
- 1999-06-09 CN CN99807191A patent/CN1305457A/zh active Pending
- 1999-06-09 AT AT99931059T patent/ATE263755T1/de not_active IP Right Cessation
- 1999-06-09 JP JP2000553403A patent/JP2002517482A/ja active Pending
- 1999-06-09 ES ES99931059T patent/ES2220072T3/es not_active Expired - Lifetime
- 1999-06-09 PT PT99931059T patent/PT1086077E/pt unknown
- 1999-06-09 IL IL13986399A patent/IL139863A0/xx unknown
- 1999-06-09 CA CA002334780A patent/CA2334780A1/en not_active Abandoned
- 1999-06-09 BR BR9911103-9A patent/BR9911103A/pt not_active IP Right Cessation
- 1999-06-09 AR ARP990102729A patent/AR023629A1/es not_active Application Discontinuation
- 1999-06-09 US US09/328,451 patent/US6166075A/en not_active Expired - Fee Related
- 1999-06-09 EP EP99931059A patent/EP1086077B1/de not_active Expired - Lifetime
-
2000
- 2000-11-07 US US09/706,806 patent/US6559181B1/en not_active Expired - Fee Related
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2001
- 2001-01-08 ZA ZA200100201A patent/ZA200100201B/en unknown
-
2003
- 2003-02-21 US US10/369,577 patent/US7074829B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
US6166075A (en) | 2000-12-26 |
BR9911103A (pt) | 2001-03-06 |
ES2220072T3 (es) | 2004-12-01 |
CO5050355A1 (es) | 2001-06-27 |
AR023629A1 (es) | 2002-09-04 |
KR20010052688A (ko) | 2001-06-25 |
EP1086077A1 (de) | 2001-03-28 |
AU759942B2 (en) | 2003-05-01 |
PL344309A1 (en) | 2001-10-22 |
EP1086077B1 (de) | 2004-04-07 |
WO1999064393A1 (de) | 1999-12-16 |
HUP0102211A3 (en) | 2002-12-28 |
CA2334780A1 (en) | 1999-12-16 |
CN1305457A (zh) | 2001-07-25 |
HUP0102211A2 (hu) | 2002-03-28 |
ATE263755T1 (de) | 2004-04-15 |
US6559181B1 (en) | 2003-05-06 |
PT1086077E (pt) | 2004-08-31 |
IL139863A0 (en) | 2002-02-10 |
AU4771699A (en) | 1999-12-30 |
DK1086077T3 (da) | 2004-08-02 |
PE20000541A1 (es) | 2000-08-10 |
US20030162830A1 (en) | 2003-08-28 |
DE59909123D1 (de) | 2004-05-13 |
DE19826213A1 (de) | 1999-12-16 |
US7074829B2 (en) | 2006-07-11 |
JP2002517482A (ja) | 2002-06-18 |
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