NO328563B1 - Substituerte benzopyraner som selektive ostrogenreseptor - agonister - Google Patents
Substituerte benzopyraner som selektive ostrogenreseptor - agonister Download PDFInfo
- Publication number
- NO328563B1 NO328563B1 NO20042583A NO20042583A NO328563B1 NO 328563 B1 NO328563 B1 NO 328563B1 NO 20042583 A NO20042583 A NO 20042583A NO 20042583 A NO20042583 A NO 20042583A NO 328563 B1 NO328563 B1 NO 328563B1
- Authority
- NO
- Norway
- Prior art keywords
- mmol
- preparation
- benzopyran
- add
- dihydro
- Prior art date
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- 150000001562 benzopyrans Chemical class 0.000 title abstract 2
- 229940127406 Estrogen Receptor Agonists Drugs 0.000 title 1
- 238000002360 preparation method Methods 0.000 claims abstract description 251
- 150000001875 compounds Chemical class 0.000 claims abstract description 111
- 150000003839 salts Chemical class 0.000 claims abstract description 35
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 26
- 201000010099 disease Diseases 0.000 claims abstract description 23
- 108010041356 Estrogen Receptor beta Proteins 0.000 claims abstract description 21
- 102000000509 Estrogen Receptor beta Human genes 0.000 claims abstract description 17
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims abstract description 12
- 206010060862 Prostate cancer Diseases 0.000 claims abstract description 11
- 230000001404 mediated effect Effects 0.000 claims abstract description 7
- VZWXIQHBIQLMPN-UHFFFAOYSA-N chromane Chemical compound C1=CC=C2CCCOC2=C1 VZWXIQHBIQLMPN-UHFFFAOYSA-N 0.000 claims description 102
- 229910052739 hydrogen Inorganic materials 0.000 claims description 23
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 19
- 239000001257 hydrogen Substances 0.000 claims description 19
- -1 -OH Chemical group 0.000 claims description 15
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims description 12
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims description 12
- 238000011282 treatment Methods 0.000 claims description 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 7
- KYNSBQPICQTCGU-UHFFFAOYSA-N Benzopyrane Chemical compound C1=CC=C2C=CCOC2=C1 KYNSBQPICQTCGU-UHFFFAOYSA-N 0.000 claims description 7
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Classifications
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
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- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/78—Ring systems having three or more relevant rings
- C07D311/80—Dibenzopyrans; Hydrogenated dibenzopyrans
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P13/00—Drugs for disorders of the urinary system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/94—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Reproductive Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrane Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33276601P | 2001-11-19 | 2001-11-19 | |
| US36362202P | 2002-03-11 | 2002-03-11 | |
| PCT/US2002/033622 WO2003044006A1 (en) | 2001-11-19 | 2002-11-07 | Substituted benzopyrans as selective estrogen receptor-beta agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO20042583L NO20042583L (no) | 2004-06-18 |
| NO328563B1 true NO328563B1 (no) | 2010-03-22 |
Family
ID=26988373
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20042583A NO328563B1 (no) | 2001-11-19 | 2004-06-18 | Substituerte benzopyraner som selektive ostrogenreseptor - agonister |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US7217734B2 (de) |
| EP (1) | EP1448544B1 (de) |
| JP (1) | JP4381810B2 (de) |
| KR (1) | KR100950616B1 (de) |
| CN (1) | CN1312147C (de) |
| AT (1) | ATE362471T1 (de) |
| AU (1) | AU2002359283B2 (de) |
| CA (1) | CA2467013C (de) |
| CY (1) | CY1106726T1 (de) |
| DE (1) | DE60220179T2 (de) |
| DK (1) | DK1448544T3 (de) |
| EA (1) | EA007382B1 (de) |
| EC (1) | ECSP045113A (de) |
| ES (1) | ES2286322T3 (de) |
| HK (1) | HK1068349A1 (de) |
| HR (1) | HRP20040439A2 (de) |
| HU (1) | HU229351B1 (de) |
| IL (3) | IL161325A0 (de) |
| MX (1) | MXPA04004703A (de) |
| NO (1) | NO328563B1 (de) |
| NZ (1) | NZ531850A (de) |
| PL (1) | PL205733B1 (de) |
| PT (1) | PT1448544E (de) |
| WO (1) | WO2003044006A1 (de) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA05011243A (es) * | 2003-04-21 | 2005-12-15 | Lilly Co Eli | Benzopiranos substituidos como agonistas selectivos del receptor beta de estrogeno. |
| ATE457308T1 (de) * | 2003-04-21 | 2010-02-15 | Lilly Co Eli | Substituierte benzopyrane als selektive antagonisten am östrogenrezeptor-beta |
| BRPI0514974A (pt) | 2004-09-07 | 2008-07-01 | Wyeth Corp | composto, composição, métodos de tratar ou inibir uma doença ou condição, estados de doença induzidos por radical livre em um mamìfero, dano à junta secundário aos procedimentos artroscópicos ou cirúrgicos em um mamìfero, infertilidade em um mamìfero, de diminuir os nìveis de colesterol, triglicerìdeos, lp(a), ou ldl, de fornecer realce na cognição ou neuroproteção, de contracepção em um mamìfero, e para preparar um composto, e, produto |
| JP2008516949A (ja) * | 2004-10-18 | 2008-05-22 | イーライ リリー アンド カンパニー | 選択的エストロゲン受容体βアゴニストとしての置換ベンゾピラン |
| US20060166933A1 (en) * | 2004-11-18 | 2006-07-27 | Jain Nareshkumar F | Novel 2H-chromene derivatives as selective estrogen receptor modulators |
| WO2006088716A1 (en) * | 2005-02-15 | 2006-08-24 | Eli Lilly And Company | Substituted tetralins as selective estrogen receptor-beta agonists |
| US9623021B2 (en) | 2007-01-22 | 2017-04-18 | Gtx, Inc. | Nuclear receptor binding agents |
| US9604931B2 (en) | 2007-01-22 | 2017-03-28 | Gtx, Inc. | Nuclear receptor binding agents |
| US8063102B2 (en) | 2009-03-13 | 2011-11-22 | N.V. Organon | Tetrahydronaphthalen-2-ol derivatives |
| TW201043595A (en) | 2009-03-13 | 2010-12-16 | Organon Nv | Tetrahydronaphthalen-2-ol derivatives |
| WO2015082643A1 (en) | 2013-12-05 | 2015-06-11 | Karo Bio Ab | Estrogen receptor beta agonists for use in treating mesothelioma |
| CA2998875C (en) | 2015-09-17 | 2023-08-29 | Ohio State Innovation Foundation | Carborane compounds and methods of use thereof |
| WO2021183760A1 (en) * | 2020-03-11 | 2021-09-16 | Ohio State Innovation Foundation | Methods of modulating t-cell activation using estrogen receptor beta (erβ) agonists |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3901926A (en) | 1973-04-02 | 1975-08-26 | Abbott Lab | Alkylphenyl benzopyrans |
| KR100263137B1 (ko) | 1995-09-08 | 2000-08-01 | 오테스코그 페르 | 오판 수용체 |
| WO1999002512A1 (en) * | 1997-07-09 | 1999-01-21 | Novo Nordisk A/S | Dl-2,3-diaryl-2h-1-benzopyrans |
| CA2367895A1 (en) | 1999-03-17 | 2000-09-21 | Signal Pharmaceuticals, Inc. | Compounds and methods for modulation of estrogen receptors |
| US6593322B1 (en) | 1999-03-17 | 2003-07-15 | Signal Pharmaceuticals, Inc. | Compounds and methods for modulation of estrogen receptors |
| CZ20013714A3 (cs) | 1999-04-16 | 2002-08-14 | Astrazeneca Ab | Léčivo pro léčení nemocí spojených s receptorem - beta estrogenu |
| CA2396059A1 (en) | 1999-12-30 | 2001-07-12 | Signal Pharmaceuticals, Inc. | Compounds and methods for modulation of estrogen receptors |
| ATE529419T1 (de) * | 2000-03-01 | 2011-11-15 | Organon Nv | Chromanderivate als estrogene verbindungen |
| JP2003528858A (ja) | 2000-03-27 | 2003-09-30 | アクゾ・ノベル・エヌ・ベー | エストロゲン関連治療用のノンステロイド系四環式化合物 |
| GB2361642A (en) | 2000-10-24 | 2001-10-31 | Karobio Ab | Estrogen receptor beta (ERbeta) agonists for use in cancer treatment |
| UA83620C2 (ru) | 2001-12-05 | 2008-08-11 | Уайт | Замещенные бензоксазолы и их аналоги как эстрогенные агенты |
| TWI306450B (en) | 2001-12-13 | 2009-02-21 | Wyeth Corp | Substituted phenyl naphthalenes as estrogenic agents |
| US6630508B1 (en) | 2002-02-11 | 2003-10-07 | Eli Lilly And Company | Substituted benzopyrans as selective estrogen receptor β agonists |
-
2002
- 2002-11-07 NZ NZ531850A patent/NZ531850A/en not_active IP Right Cessation
- 2002-11-07 EA EA200400695A patent/EA007382B1/ru not_active IP Right Cessation
- 2002-11-07 DK DK02793806T patent/DK1448544T3/da active
- 2002-11-07 CN CNB028229916A patent/CN1312147C/zh not_active Expired - Fee Related
- 2002-11-07 JP JP2003545643A patent/JP4381810B2/ja not_active Expired - Fee Related
- 2002-11-07 IL IL16132502A patent/IL161325A0/xx unknown
- 2002-11-07 ES ES02793806T patent/ES2286322T3/es not_active Expired - Lifetime
- 2002-11-07 US US10/493,092 patent/US7217734B2/en not_active Expired - Fee Related
- 2002-11-07 HU HU0402628A patent/HU229351B1/hu not_active IP Right Cessation
- 2002-11-07 PL PL374510A patent/PL205733B1/pl unknown
- 2002-11-07 CA CA2467013A patent/CA2467013C/en not_active Expired - Fee Related
- 2002-11-07 KR KR1020047007563A patent/KR100950616B1/ko not_active IP Right Cessation
- 2002-11-07 AU AU2002359283A patent/AU2002359283B2/en not_active Ceased
- 2002-11-07 PT PT02793806T patent/PT1448544E/pt unknown
- 2002-11-07 MX MXPA04004703A patent/MXPA04004703A/es active IP Right Grant
- 2002-11-07 DE DE60220179T patent/DE60220179T2/de not_active Expired - Lifetime
- 2002-11-07 WO PCT/US2002/033622 patent/WO2003044006A1/en active IP Right Grant
- 2002-11-07 EP EP02793806A patent/EP1448544B1/de not_active Expired - Lifetime
- 2002-11-07 AT AT02793806T patent/ATE362471T1/de active
-
2004
- 2004-04-08 IL IL161325A patent/IL161325A/en not_active IP Right Cessation
- 2004-05-18 HR HR20040439A patent/HRP20040439A2/hr not_active Application Discontinuation
- 2004-05-19 EC EC2004005113A patent/ECSP045113A/es unknown
- 2004-06-18 NO NO20042583A patent/NO328563B1/no not_active IP Right Cessation
-
2005
- 2005-01-24 HK HK05100628A patent/HK1068349A1/xx not_active IP Right Cessation
-
2007
- 2007-07-13 CY CY20071100932T patent/CY1106726T1/el unknown
- 2007-09-10 IL IL185867A patent/IL185867A/en not_active IP Right Cessation
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