MD20140054A2 - Compuşi noi de benzopiran, compoziţii şi utilizări ale acestora - Google Patents
Compuşi noi de benzopiran, compoziţii şi utilizări ale acestora Download PDFInfo
- Publication number
- MD20140054A2 MD20140054A2 MDA20140054A MD20140054A MD20140054A2 MD 20140054 A2 MD20140054 A2 MD 20140054A2 MD A20140054 A MDA20140054 A MD A20140054A MD 20140054 A MD20140054 A MD 20140054A MD 20140054 A2 MD20140054 A2 MD 20140054A2
- Authority
- MD
- Moldova
- Prior art keywords
- compositions
- estrogen
- benzopyran compounds
- compounds
- chromen
- Prior art date
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- 150000001562 benzopyrans Chemical class 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title 1
- KDVXAPCZVZMPMU-XBBWARJSSA-N (2s)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-[(3r)-3-methylpyrrolidin-1-yl]ethoxy]phenyl]-2h-chromen-7-ol Chemical compound C1[C@H](C)CCN1CCOC1=CC=C([C@H]2C(=C(C)C3=CC=C(O)C=C3O2)C=2C=CC(O)=CC=2)C=C1 KDVXAPCZVZMPMU-XBBWARJSSA-N 0.000 abstract 3
- 230000001833 anti-estrogenic effect Effects 0.000 abstract 3
- KDVXAPCZVZMPMU-COBFLCELSA-N 3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-[(3r)-3-methylpyrrolidin-1-yl]ethoxy]phenyl]-2h-chromen-7-ol Chemical compound C1[C@H](C)CCN1CCOC1=CC=C(C2C(=C(C)C3=CC=C(O)C=C3O2)C=2C=CC(O)=CC=2)C=C1 KDVXAPCZVZMPMU-COBFLCELSA-N 0.000 abstract 2
- 229940046836 anti-estrogen Drugs 0.000 abstract 2
- 239000000328 estrogen antagonist Substances 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 102000015694 estrogen receptors Human genes 0.000 abstract 1
- 108010038795 estrogen receptors Proteins 0.000 abstract 1
- 230000001076 estrogenic effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- 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
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Reproductive Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Sunt propuşi compuşi de benzopiran cu activitate antiestrogenică puternică şi în mod esenţial fără activitate estrogenică, care reprezintă 3-(4-hidroxifenil)-4-metil-2-(4-{2-[(3R)-3-metilpirolidin-1-il]etoxi}fenil)-2H-cromen-7-ol (OP-1038):şi enantiomerul (2S)-3-(4-hidroxifenil)-4-metil-2-(4-{2-[(3R)-3-metilpirolidin-1-il]etoxi}fenil)-2H-cromen-7-ol (OP-1074):.OP-1074 reprezintă un antiestrogen pur în urma testării în calitate de agonist şi un antiestrogen complet, la testare în calitate de antagonist. Aceşti compuşi sunt utili pentru tratamentul sau prevenirea diferitor stări care se modulează prin receptorul pentru estrogeni la mamifere, inclusiv la om.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161576890P | 2011-12-16 | 2011-12-16 | |
| PCT/US2012/070168 WO2013090921A1 (en) | 2011-12-16 | 2012-12-17 | Novel benzopyran compounds, compositions and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MD20140054A2 true MD20140054A2 (ro) | 2014-10-31 |
Family
ID=48613277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDA20140054A MD20140054A2 (ro) | 2011-12-16 | 2012-12-17 | Compuşi noi de benzopiran, compoziţii şi utilizări ale acestora |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US9018244B2 (ro) |
| EP (1) | EP2791128A4 (ro) |
| JP (1) | JP2015505856A (ro) |
| KR (1) | KR20140103335A (ro) |
| CN (1) | CN104169266A (ro) |
| AP (1) | AP2014007657A0 (ro) |
| AU (1) | AU2012353660A1 (ro) |
| BR (1) | BR112014014767A2 (ro) |
| CA (1) | CA2857061A1 (ro) |
| CL (1) | CL2014001533A1 (ro) |
| CR (1) | CR20140259A (ro) |
| CU (1) | CU20140066A7 (ro) |
| DO (1) | DOP2014000135A (ro) |
| EA (1) | EA201490897A1 (ro) |
| EC (1) | ECSP14009619A (ro) |
| HK (1) | HK1199246A1 (ro) |
| IL (1) | IL233118A0 (ro) |
| MA (1) | MA35722B1 (ro) |
| MD (1) | MD20140054A2 (ro) |
| MX (1) | MX2014007198A (ro) |
| NI (1) | NI201400057A (ro) |
| PE (1) | PE20150099A1 (ro) |
| PH (1) | PH12014501237A1 (ro) |
| SG (1) | SG11201402564QA (ro) |
| TN (1) | TN2014000243A1 (ro) |
| WO (1) | WO2013090921A1 (ro) |
| ZA (1) | ZA201404733B (ro) |
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| HUE033581T2 (hu) | 2010-06-10 | 2017-12-28 | Seragon Pharmaceuticals Inc | Ösztrogén receptor modulátorok és alkalmazásaik |
| SG11201403002RA (en) | 2011-12-14 | 2014-07-30 | Seragon Pharmaceuticals Inc | Fluorinated estrogen receptor modulators and uses thereof |
| WO2014203132A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Substituted benzopyran compounds, compositions and uses thereof |
| WO2014203129A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Combinations of benzopyran compounds, compositions and uses thereof |
| CN104725333A (zh) * | 2013-12-20 | 2015-06-24 | 北京蓝贝望生物医药科技股份有限公司 | 一种新的氮杂环庚烷衍生物的制备方法 |
| AU2015228859A1 (en) * | 2014-03-13 | 2016-07-07 | F. Hoffmann-La Roche Ag | Therapeutic combinations with estrogen receptor modulators |
| US9855270B2 (en) * | 2014-03-13 | 2018-01-02 | Genentech, Inc. | Methods and compositions for modulating estrogen receptor mutants |
| AU2016301196B2 (en) | 2015-08-06 | 2022-09-08 | Dana-Farber Cancer Institute, Inc. | Tunable endogenous protein degradation |
| DK3355884T3 (da) | 2015-10-01 | 2021-08-02 | Olema Pharmaceuticals Inc | Tetrahydro-1h-pyrido[3,4-b]indol-antiøstrogenlægemidler |
| HRP20220640T1 (hr) | 2015-10-27 | 2022-07-08 | Sun Pharma Advanced Research Company Limited | Novi heterociklični antiestrogeni |
| ES2935125T3 (es) | 2015-12-09 | 2023-03-01 | Univ Illinois | Reguladores a la baja selectivos de los receptores de estrógenos con base en benzotiofeno |
| CN109562107A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
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| RS65966B1 (sr) | 2018-02-16 | 2024-10-31 | Constellation Pharmaceuticals Inc | Inhibitori p300/cbp hat |
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| RS60617B1 (sr) | 2012-06-07 | 2020-09-30 | Aragon Pharmaceuticals Inc | Kristalni oblici modulatora receptora androgena |
| ES2764381T3 (es) | 2012-07-27 | 2020-06-03 | Aragon Pharmaceuticals Inc | Métodos y composiciones para determinar la resistencia a la terapia de receptor de andrógenos |
| CN115737643A (zh) | 2012-09-26 | 2023-03-07 | 阿拉贡药品公司 | 用于治疗非转移性去势抵抗性前列腺癌的抗雄激素 |
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-
2012
- 2012-12-17 EP EP20120858374 patent/EP2791128A4/en not_active Withdrawn
- 2012-12-17 AP AP2014007657A patent/AP2014007657A0/xx unknown
- 2012-12-17 WO PCT/US2012/070168 patent/WO2013090921A1/en not_active Ceased
- 2012-12-17 CA CA2857061A patent/CA2857061A1/en not_active Abandoned
- 2012-12-17 US US13/717,326 patent/US9018244B2/en not_active Expired - Fee Related
- 2012-12-17 JP JP2014547552A patent/JP2015505856A/ja active Pending
- 2012-12-17 SG SG11201402564QA patent/SG11201402564QA/en unknown
- 2012-12-17 CN CN201280062009.4A patent/CN104169266A/zh active Pending
- 2012-12-17 HK HK14112731.3A patent/HK1199246A1/xx unknown
- 2012-12-17 PE PE2014000963A patent/PE20150099A1/es not_active Application Discontinuation
- 2012-12-17 AU AU2012353660A patent/AU2012353660A1/en not_active Abandoned
- 2012-12-17 MX MX2014007198A patent/MX2014007198A/es unknown
- 2012-12-17 KR KR1020147019676A patent/KR20140103335A/ko not_active Ceased
- 2012-12-17 MD MDA20140054A patent/MD20140054A2/ro not_active Application Discontinuation
- 2012-12-17 BR BR112014014767A patent/BR112014014767A2/pt not_active IP Right Cessation
- 2012-12-17 EA EA201490897A patent/EA201490897A1/ru unknown
-
2014
- 2014-05-28 CR CR20140259A patent/CR20140259A/es unknown
- 2014-06-02 PH PH12014501237A patent/PH12014501237A1/en unknown
- 2014-06-02 MA MA37096A patent/MA35722B1/fr unknown
- 2014-06-03 TN TNP2014000243A patent/TN2014000243A1/fr unknown
- 2014-06-11 CL CL2014001533A patent/CL2014001533A1/es unknown
- 2014-06-11 CU CU2014000066A patent/CU20140066A7/es unknown
- 2014-06-12 IL IL233118A patent/IL233118A0/en unknown
- 2014-06-13 NI NI201400057A patent/NI201400057A/es unknown
- 2014-06-16 DO DO2014000135A patent/DOP2014000135A/es unknown
- 2014-06-26 ZA ZA2014/04733A patent/ZA201404733B/en unknown
- 2014-07-16 EC ECIEPI20149619A patent/ECSP14009619A/es unknown
-
2015
- 2015-03-17 US US14/660,248 patent/US20150197506A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EA201490897A1 (ru) | 2015-03-31 |
| NI201400057A (es) | 2014-10-01 |
| US20130178445A1 (en) | 2013-07-11 |
| WO2013090921A1 (en) | 2013-06-20 |
| MX2014007198A (es) | 2014-10-13 |
| US9018244B2 (en) | 2015-04-28 |
| IL233118A0 (en) | 2014-08-03 |
| HK1199246A1 (en) | 2015-06-26 |
| AU2012353660A1 (en) | 2014-06-12 |
| AP2014007657A0 (en) | 2014-05-31 |
| CU20140066A7 (es) | 2014-10-02 |
| PH12014501237A1 (en) | 2014-09-08 |
| PE20150099A1 (es) | 2015-01-30 |
| CN104169266A (zh) | 2014-11-26 |
| CL2014001533A1 (es) | 2014-10-17 |
| BR112014014767A2 (pt) | 2017-06-13 |
| CR20140259A (es) | 2014-08-21 |
| TN2014000243A1 (fr) | 2015-09-30 |
| EP2791128A1 (en) | 2014-10-22 |
| ECSP14009619A (es) | 2015-09-30 |
| MA35722B1 (fr) | 2014-12-01 |
| KR20140103335A (ko) | 2014-08-26 |
| SG11201402564QA (en) | 2014-09-26 |
| US20150197506A1 (en) | 2015-07-16 |
| CA2857061A1 (en) | 2013-06-20 |
| EP2791128A4 (en) | 2015-04-22 |
| ZA201404733B (en) | 2016-04-28 |
| DOP2014000135A (es) | 2014-08-31 |
| JP2015505856A (ja) | 2015-02-26 |
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