PE20021083A1 - MODULATORS OF THE ESTROGEN RECEPTORS - Google Patents
MODULATORS OF THE ESTROGEN RECEPTORSInfo
- Publication number
- PE20021083A1 PE20021083A1 PE2002000308A PE2002000308A PE20021083A1 PE 20021083 A1 PE20021083 A1 PE 20021083A1 PE 2002000308 A PE2002000308 A PE 2002000308A PE 2002000308 A PE2002000308 A PE 2002000308A PE 20021083 A1 PE20021083 A1 PE 20021083A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- cycloalkyl
- alkenyl
- modulators
- acetophenone
- Prior art date
Links
- 102000015694 estrogen receptors Human genes 0.000 title abstract 2
- 108010038795 estrogen receptors Proteins 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- SLRMQYXOBQWXCR-UHFFFAOYSA-N 2154-56-5 Chemical class [CH2]C1=CC=CC=C1 SLRMQYXOBQWXCR-UHFFFAOYSA-N 0.000 abstract 1
- 229940073735 4-hydroxy acetophenone Drugs 0.000 abstract 1
- 201000009273 Endometriosis Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 210000000845 cartilage Anatomy 0.000 abstract 1
- 230000007850 degeneration Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003457 sulfones Chemical class 0.000 abstract 1
- 150000003462 sulfoxides Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
- C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
- C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D411/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- 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
- A61P5/30—Oestrogens
-
- 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
-
- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D327/00—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
- C07D327/02—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms one oxygen atom and one sulfur atom
- C07D327/06—Six-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D339/00—Heterocyclic compounds containing rings having two sulfur atoms as the only ring hetero atoms
- C07D339/08—Six-membered rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Child & Adolescent Psychology (AREA)
- Psychiatry (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DE FORMULA I DONDE R1 ES H, ALQUILO C1-C5, CICLOALQUILO C3-C8, ALQUENILO C2-C5, ALQUINILO C2-C5, OR6, ENTRE OTROS; R2 ES H, ALQUILO C1-C5, CICLOALQUILO C3-C8, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; R3 ES H, ALQUILO C1-C5, CICLOALQUILO C3-C8, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; R4 ES H, ALQUILO C1-C5, CICLOALQUILO C3-C8, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; R5 ES ALQUILO C1-C5, CICLOALQUILO C3-C8, ALQUENILO C2-C5, ENTRE OTROS; X E Y SON O, S, SULFOXIDO, SULFONA; R6 ES H, ALQUILO C1-C5, BENCILO, METOXIMETILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS 2-TIOFENO-4-METOXI-ACETOFENONA, 2-TIOFENO-4-HIDROXI-ACETOFENONA, 2-TIOFENO-4-METOXI-ACETOFENONA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS MENCIONADOS SON MODULADORES DE LOS RECEPTORES ESTROGENOS Y SON UTILES PARA EL TRATAMIENTO DE OSTEOPOROSIS, DEGENERACION DE CARTILAGO, ENDOMETRIOSISREFERS TO COMPOUNDS OF FORMULA I WHERE R1 IS H, C1-C5 ALKYL, C3-C8 CYCLOALKYL, C2-C5 ALKENYL, C2-C5 ALKYNYL, OR6, AMONG OTHERS; R2 IS H, C1-C5 ALKYL, C3-C8 CYCLOALKYL, C2-C5 ALKENYL, C2-C5 ALKYL, AMONG OTHERS; R3 IS H, C1-C5 ALKYL, C3-C8 CYCLOALKYL, C2-C5 ALKENYL, C2-C5 ALKYL, AMONG OTHERS; R4 IS H, C1-C5 ALKYL, C3-C8 CYCLOALKYL, C2-C5 ALKENYL, C2-C5 ALKYL, AMONG OTHERS; R5 IS C1-C5 ALKYL, C3-C8 CYCLOALKYL, C2-C5 ALKYL, AMONG OTHERS; X AND Y ARE O, S, SULFOXIDE, SULFONE; R6 IS H, C1-C5 ALKYL, BENZYL, METOXIMETHYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE 2-THIOPHENE-4-METOXY-ACETOPHENONE, 2-THIOPHENE-4-HYDROXY-ACETOPHENONE, 2-THIOPHENE-4-METOXY-ACETOPHENONE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A PROCEDURE FOR THE PREPARATION. THE MENTIONED COMPOUNDS ARE MODULATORS OF THE ESTROGEN RECEPTORS AND ARE USEFUL FOR THE TREATMENT OF OSTEOPOROSIS, CARTILAGE DEGENERATION, ENDOMETRIOSIS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24158200P | 2000-10-19 | 2000-10-19 | |
| PCT/US2001/042735 WO2002032377A2 (en) | 2000-10-19 | 2001-10-15 | Estrogen receptor modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20021083A1 true PE20021083A1 (en) | 2002-12-16 |
Family
ID=22911282
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2002000308A PE20021083A1 (en) | 2000-10-19 | 2002-04-15 | MODULATORS OF THE ESTROGEN RECEPTORS |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP1333827A2 (en) |
| JP (1) | JP2004511502A (en) |
| KR (1) | KR20030042020A (en) |
| CN (1) | CN1469743A (en) |
| AU (2) | AU3238102A (en) |
| BG (1) | BG107676A (en) |
| BR (1) | BR0114689A (en) |
| CA (1) | CA2424729A1 (en) |
| EA (1) | EA200300474A1 (en) |
| EC (1) | ECSP034558A (en) |
| EE (1) | EE200300153A (en) |
| HU (1) | HUP0303563A2 (en) |
| IL (1) | IL154984A0 (en) |
| IS (1) | IS6761A (en) |
| MX (1) | MXPA03003485A (en) |
| NO (1) | NO20031737L (en) |
| PE (1) | PE20021083A1 (en) |
| PL (1) | PL361053A1 (en) |
| SK (1) | SK4772003A3 (en) |
| WO (1) | WO2002032377A2 (en) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030225132A1 (en) * | 2002-04-11 | 2003-12-04 | Dininno Frank P. | Estrogen receptor modulators |
| DK1501819T3 (en) * | 2002-04-24 | 2011-01-10 | Merck Sharp & Dohme | estrogen |
| PT1880744E (en) | 2002-05-10 | 2015-02-13 | Hoffmann La Roche | Bisphosphonic acids for the treatment and prevention of osteoporosis |
| AU2003292625B2 (en) * | 2002-12-26 | 2008-07-24 | Eisai R & D Management Co., Ltd. | Selective estrogen receptor modulators |
| CA2617213C (en) | 2005-07-29 | 2014-01-28 | Resverlogix Corp. | Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices |
| JPWO2007049798A1 (en) | 2005-10-27 | 2009-04-30 | 萬有製薬株式会社 | New benzooxathiin derivatives |
| PT2118074E (en) | 2007-02-01 | 2014-03-20 | Resverlogix Corp | Compounds for the prevention and treatment of cardiovascular diseases |
| ES2542835T3 (en) | 2009-01-08 | 2015-08-12 | Resverlogix Corporation | Compounds for the prevention and treatment of cardiovascular diseases |
| US9238640B2 (en) | 2009-03-18 | 2016-01-19 | Resverlogix Corp. | Anti-inflammatory agents |
| EP2421533B1 (en) | 2009-04-22 | 2018-10-17 | Resverlogix Corp. | Novel anti-inflammatory agents |
| EP2580210B1 (en) | 2010-06-10 | 2017-03-01 | Seragon Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
| US8853423B2 (en) | 2010-06-17 | 2014-10-07 | Seragon Pharmaceuticals, Inc. | Indane estrogen receptor modulators and uses thereof |
| PT2773354T (en) | 2011-11-01 | 2019-07-17 | Resverlogix Corp | Oral immediate release formulations for substituted quinazolinones |
| SG11201403002RA (en) | 2011-12-14 | 2014-07-30 | Seragon Pharmaceuticals Inc | Fluorinated estrogen receptor modulators and uses thereof |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| EP2935253B1 (en) | 2012-12-21 | 2018-08-01 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| EP3268007B1 (en) | 2015-03-13 | 2022-11-09 | Resverlogix Corp. | Compositions and therapeutic methods for the treatment of complement-associated diseases |
-
2001
- 2001-10-15 BR BR0114689-0A patent/BR0114689A/en not_active Application Discontinuation
- 2001-10-15 MX MXPA03003485A patent/MXPA03003485A/en unknown
- 2001-10-15 CN CNA018176720A patent/CN1469743A/en active Pending
- 2001-10-15 AU AU3238102A patent/AU3238102A/en active Pending
- 2001-10-15 EP EP01987654A patent/EP1333827A2/en not_active Withdrawn
- 2001-10-15 WO PCT/US2001/042735 patent/WO2002032377A2/en not_active Application Discontinuation
- 2001-10-15 HU HU0303563A patent/HUP0303563A2/en unknown
- 2001-10-15 AU AU2002232381A patent/AU2002232381B2/en not_active Ceased
- 2001-10-15 EE EEP200300153A patent/EE200300153A/en unknown
- 2001-10-15 PL PL01361053A patent/PL361053A1/en not_active Application Discontinuation
- 2001-10-15 IL IL15498401A patent/IL154984A0/en unknown
- 2001-10-15 KR KR10-2003-7005518A patent/KR20030042020A/en not_active Application Discontinuation
- 2001-10-15 SK SK477-2003A patent/SK4772003A3/en unknown
- 2001-10-15 CA CA002424729A patent/CA2424729A1/en not_active Abandoned
- 2001-10-15 EA EA200300474A patent/EA200300474A1/en unknown
- 2001-10-15 JP JP2002535616A patent/JP2004511502A/en not_active Withdrawn
-
2002
- 2002-04-15 PE PE2002000308A patent/PE20021083A1/en not_active Application Discontinuation
-
2003
- 2003-03-26 BG BG107676A patent/BG107676A/en unknown
- 2003-03-27 IS IS6761A patent/IS6761A/en unknown
- 2003-04-15 NO NO20031737A patent/NO20031737L/en unknown
- 2003-04-17 EC EC2003004558A patent/ECSP034558A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO20031737L (en) | 2003-06-19 |
| AU2002232381B2 (en) | 2004-11-18 |
| EP1333827A2 (en) | 2003-08-13 |
| HUP0303563A2 (en) | 2004-03-01 |
| NO20031737D0 (en) | 2003-04-15 |
| CN1469743A (en) | 2004-01-21 |
| JP2004511502A (en) | 2004-04-15 |
| AU3238102A (en) | 2002-04-29 |
| WO2002032377A2 (en) | 2002-04-25 |
| EA200300474A1 (en) | 2003-10-30 |
| MXPA03003485A (en) | 2003-07-14 |
| IL154984A0 (en) | 2003-10-31 |
| PL361053A1 (en) | 2004-09-20 |
| KR20030042020A (en) | 2003-05-27 |
| SK4772003A3 (en) | 2003-08-05 |
| BG107676A (en) | 2003-11-28 |
| IS6761A (en) | 2003-03-27 |
| EE200300153A (en) | 2003-06-16 |
| ECSP034558A (en) | 2003-06-25 |
| BR0114689A (en) | 2003-07-01 |
| WO2002032377A3 (en) | 2002-08-22 |
| CA2424729A1 (en) | 2002-04-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |