MX2017013563A - LIGANDOS DEGRADADORES SELECTIVOS DEL RECEPTOR ANDROGíNICO (SARD) Y SUS MíTODOS DE USO. - Google Patents
LIGANDOS DEGRADADORES SELECTIVOS DEL RECEPTOR ANDROGíNICO (SARD) Y SUS MíTODOS DE USO.Info
- Publication number
- MX2017013563A MX2017013563A MX2017013563A MX2017013563A MX2017013563A MX 2017013563 A MX2017013563 A MX 2017013563A MX 2017013563 A MX2017013563 A MX 2017013563A MX 2017013563 A MX2017013563 A MX 2017013563A MX 2017013563 A MX2017013563 A MX 2017013563A
- Authority
- MX
- Mexico
- Prior art keywords
- androgen receptor
- prostate cancer
- sard
- methods
- selective androgen
- Prior art date
Links
- 229940122793 Selective androgen receptor degrader Drugs 0.000 title abstract 3
- 239000003446 ligand Substances 0.000 title 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 3
- 206010060862 Prostate cancer Diseases 0.000 abstract 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 3
- UJOBWOGCFQCDNV-UHFFFAOYSA-N 9H-carbazole Chemical compound C1=CC=C2C3=CC=CC=C3NC2=C1 UJOBWOGCFQCDNV-UHFFFAOYSA-N 0.000 abstract 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 abstract 2
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 abstract 2
- 230000001717 pathogenic effect Effects 0.000 abstract 2
- 108010040003 polyglutamine Proteins 0.000 abstract 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 abstract 1
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 abstract 1
- 201000004384 Alopecia Diseases 0.000 abstract 1
- 206010068597 Bulbospinal muscular atrophy congenital Diseases 0.000 abstract 1
- 208000027747 Kennedy disease Diseases 0.000 abstract 1
- 206010046798 Uterine leiomyoma Diseases 0.000 abstract 1
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 abstract 1
- 239000003098 androgen Substances 0.000 abstract 1
- 201000002996 androgenic alopecia Diseases 0.000 abstract 1
- 230000001548 androgenic effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002500 effect on skin Effects 0.000 abstract 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 abstract 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 abstract 1
- 201000010260 leiomyoma Diseases 0.000 abstract 1
- 230000035772 mutation Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229920000155 polyglutamine Polymers 0.000 abstract 1
- 102000054765 polymorphisms of proteins Human genes 0.000 abstract 1
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
-
- 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
- A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
-
- 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
- A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/02—Carbamic acids; Salts of carbamic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/18—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
- C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Quinoline Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invención proporciona compuestos degradadores selectivos del receptor androgónico (SARD) novedosos de indol, indazol, bicimidazol, indolina, quinolona, isoquinolina y carbazol, composiciones farmacóuticas y sus usos para el tratamiento de cáncer de próstata, cáncer de próstata avanzado, cáncer de próstata resistente a la castración, alopecia androgónica y otras enfermedades dórmicas hiperandrogóicas. Enfermedad de Kennedy esclerosis lateral amiotrofia. (ALS) y fibromas uterinos, y métodos para reducir los niveles de receptor andrógenico de longitud completa AR-FL) que incluyen mutaciones patógenas y/o mutaciones de resistencia,variantes de empalme de AR (AR-SV) Y polimorfismos de poliglutamina patógena (polyQ) de AR en un sujeto.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562150763P | 2015-04-21 | 2015-04-21 | |
| US201562220057P | 2015-09-17 | 2015-09-17 | |
| US201562219859P | 2015-09-17 | 2015-09-17 | |
| US201562220187P | 2015-09-17 | 2015-09-17 | |
| US201562241532P | 2015-10-14 | 2015-10-14 | |
| PCT/US2016/028674 WO2016172358A1 (en) | 2015-04-21 | 2016-04-21 | Selective androgen receptor degrader (sard) ligands and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2017013563A true MX2017013563A (es) | 2018-07-06 |
Family
ID=57144548
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017013563A MX2017013563A (es) | 2015-04-21 | 2016-04-21 | LIGANDOS DEGRADADORES SELECTIVOS DEL RECEPTOR ANDROGíNICO (SARD) Y SUS MíTODOS DE USO. |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9814698B2 (es) |
| EP (1) | EP3286164B1 (es) |
| JP (1) | JP6786520B2 (es) |
| KR (1) | KR20170140291A (es) |
| CN (1) | CN107709290B (es) |
| AU (1) | AU2016252753A1 (es) |
| BR (1) | BR112017022860A2 (es) |
| CA (1) | CA2983403A1 (es) |
| MX (1) | MX2017013563A (es) |
| RU (2) | RU2019115778A (es) |
| WO (1) | WO2016172358A1 (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190077607A (ko) * | 2014-10-16 | 2019-07-03 | 지티엑스, 인코포레이티드 | Sarm을 이용하는 비뇨기 장애의 치료 방법 |
| US10865184B2 (en) | 2015-04-21 | 2020-12-15 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10441570B2 (en) | 2015-04-21 | 2019-10-15 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) Ligands and methods of use thereof |
| US10035763B2 (en) * | 2015-04-21 | 2018-07-31 | Gtx, Inc. | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US9834507B2 (en) | 2015-04-21 | 2017-12-05 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10654809B2 (en) | 2016-06-10 | 2020-05-19 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10017471B2 (en) * | 2015-04-21 | 2018-07-10 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10093613B2 (en) | 2015-04-21 | 2018-10-09 | Gtx, Inc. | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10806720B2 (en) | 2015-04-21 | 2020-10-20 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| TWI710554B (zh) | 2015-09-11 | 2020-11-21 | 日商大日本住友製藥股份有限公司 | 新穎苯并咪唑化合物及其醫藥用途 |
| CA3017388C (en) | 2016-04-01 | 2024-03-12 | Zeno Royalties & Milestones, LLC | Estrogen receptor modulators |
| CA3024615A1 (en) * | 2016-06-10 | 2017-12-14 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (sard) ligands and methods of use thereof |
| US11230523B2 (en) | 2016-06-10 | 2022-01-25 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| WO2019023651A2 (en) | 2017-07-28 | 2019-01-31 | Massachusetts Institute Of Technology | MODULATORS OF THE SMALL MOLECULE ANDROGEN RECEPTOR |
| WO2019222556A1 (en) * | 2018-05-16 | 2019-11-21 | Gtx, Inc. | Selective androgen receptor degrader (sard) ligands and methods of use thereof |
| US12202815B2 (en) | 2018-09-05 | 2025-01-21 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| CN109081808B (zh) * | 2018-09-11 | 2020-08-04 | 济南大学 | 一类含有四氢异喹啉结构的酰基苯胺类化合物、用途及其制备方法 |
| CN110963957B (zh) * | 2018-09-28 | 2021-10-22 | 深圳恩多凯医药科技有限公司 | N-芳香酰胺类化合物及其制备方法和用途 |
| CN109761778A (zh) * | 2018-12-10 | 2019-05-17 | 石家庄市度智医药科技有限公司 | 一种合成光学活性α-羟基丙酰胺衍生物的方法 |
| CN110156584B (zh) * | 2019-04-28 | 2023-04-07 | 长春金赛药业有限责任公司 | 一种(2r)-3-溴-2-羟基-2-甲基丙酸的合成方法 |
| EP3993787A4 (en) | 2019-08-06 | 2023-07-12 | Recurium IP Holdings, LLC | Estrogen receptor modulators for treating mutants |
| CA3155290A1 (en) * | 2019-09-23 | 2021-04-01 | Accutar Biotechnology Inc. | Novel substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof |
| PH12022550877A1 (en) | 2019-10-16 | 2023-03-27 | Chemocentryx Inc | Heteroaryl-biphenyl amines for the treatment of pd-l1 diseases |
| TWI755992B (zh) | 2019-12-23 | 2022-02-21 | 大陸商上海濟煜醫藥科技有限公司 | 一種蛋白降解劑化合物的製備方法和應用 |
| CN115427028A (zh) * | 2020-02-25 | 2022-12-02 | 田纳西大学研究基金会 | 选择性雄激素受体共价拮抗剂(sarca)及其使用方法 |
| CN115484947A (zh) * | 2020-02-25 | 2022-12-16 | 田纳西大学研究基金会 | 选择性雄激素受体降解剂(sard)配体及其使用方法 |
| WO2025147657A1 (en) * | 2024-01-05 | 2025-07-10 | Board Of Trustees Of Michigan State University | Methods for treating alopecia |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE28864T1 (de) | 1982-07-23 | 1987-08-15 | Ici Plc | Amide-derivate. |
| JPS60100516A (ja) | 1983-11-04 | 1985-06-04 | Takeda Chem Ind Ltd | 徐放型マイクロカプセルの製造法 |
| MY107937A (en) | 1990-02-13 | 1996-06-29 | Takeda Chemical Industries Ltd | Prolonged release microcapsules. |
| JP3277342B2 (ja) | 1992-09-02 | 2002-04-22 | 武田薬品工業株式会社 | 徐放性マイクロカプセルの製造法 |
| CA2192782C (en) | 1995-12-15 | 2008-10-14 | Nobuyuki Takechi | Production of microspheres |
| GB0003790D0 (en) | 2000-02-18 | 2000-04-05 | Astrazeneca Uk Ltd | Medical device |
| US7645898B2 (en) | 2000-08-24 | 2010-01-12 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and method of use thereof |
| US20070173546A1 (en) | 2000-08-24 | 2007-07-26 | Dalton James T | Selective androgen receptor modulators and method of use thereof |
| DE60124322T2 (de) | 2000-08-24 | 2007-05-31 | University Of Tennessee Research Foundation, Knoxville | Selektive modulatoren des androgenrezeptors und methoden zu deren verwendung |
| JP2004515494A (ja) * | 2000-12-07 | 2004-05-27 | アストラゼネカ・アクチエボラーグ | 治療剤 |
| US7741371B2 (en) | 2002-06-17 | 2010-06-22 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| CN100537520C (zh) * | 2002-06-17 | 2009-09-09 | 田纳西大学研究基金会 | N-桥连选择性雄激素受体调节剂及其使用方法 |
| JP2006506369A (ja) * | 2002-10-15 | 2006-02-23 | ユニバーシティ・オブ・テネシー・リサーチ・ファウンデーション | メチレン架橋選択的アンドロゲン受容体調節剤及びその使用方法 |
| EP1636167A2 (en) | 2003-06-10 | 2006-03-22 | SmithKline Beecham Corporation | 1-aminonaphthalenes as modulators of androgen, glucocorticoid, mineralocorticoid and progesterone receptors |
| FI20030958A0 (fi) | 2003-06-27 | 2003-06-27 | Orion Corp | Uusia yhdisteitä |
| CN1597662A (zh) | 2003-09-16 | 2005-03-23 | 中国科学院上海药物研究所 | 一类芳香酰胺化合物、制备方法及用途 |
| CA2559863A1 (en) * | 2004-03-24 | 2005-10-13 | 3M Innovative Properties Company | Amide substituted imidazopyridines, imidazoquinolines, and imidazonaphthyridines |
| US20060173037A1 (en) * | 2005-01-10 | 2006-08-03 | Nathalie Schlienger | Aminophenyl derivatives as selective androgen receptor modulators |
| EP1836202B1 (en) * | 2005-01-10 | 2016-12-21 | Acadia Pharmaceuticals Inc. | Aminophenyl derivatives as selective androgen receptor modulators |
| AR057656A1 (es) | 2005-07-01 | 2007-12-12 | Ligand Pharm Inc | Compuestos moduladores de receptores de androgeno y metodods relacionados |
| JP2009506077A (ja) * | 2005-08-26 | 2009-02-12 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 非ステロイド性抗アンドロゲン剤 |
| WO2007134449A1 (en) | 2006-05-19 | 2007-11-29 | Waratah Pharmaceuticals Inc. | Screening methods for amyloid beta modulators |
| MX2009000715A (es) | 2006-07-19 | 2009-07-22 | Osurf Ohio State University Re | Moduladores de receptor de androgeno selectivos, analogos y derivados de los mismos. |
| WO2008076918A2 (en) * | 2006-12-15 | 2008-06-26 | University Of Maryland, Baltimore | Anti-cancer agents and androgen inhibition activity compound |
| WO2008124000A2 (en) | 2007-04-02 | 2008-10-16 | Ligand Pharmaceuticals Incorporated | Thiazole derivatives as androgen receptor modulator compounds |
| US9284345B2 (en) | 2007-04-12 | 2016-03-15 | Endorecherche, Inc. | 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators |
| US7696227B2 (en) * | 2007-04-13 | 2010-04-13 | Regents Of The University Of California | Small-molecule inhibitors of the androgen receptor |
| WO2008136838A1 (en) * | 2007-05-04 | 2008-11-13 | Trustees Of Dartmouth College | Novel amide derivatives of cddo and methods of use thereof |
| WO2009010480A1 (en) | 2007-07-13 | 2009-01-22 | Euroscreen S.A. | 1-{2-[(diphenyl)amino]-ethyl}-piperidine-4-carboxylic acid benzylamide derivatives and related compounds as ccr5 agonists for the treatment of immune and inflammatory diseases |
| WO2009069736A1 (ja) | 2007-11-28 | 2009-06-04 | Kyowa Hakko Kirin Co., Ltd. | 含窒素化合物 |
| US20090142323A1 (en) | 2007-11-29 | 2009-06-04 | Quarles L Darryl | Methods for treating a disorder by regulating gprc6a |
| ES2413504T3 (es) * | 2007-12-21 | 2013-07-16 | Ligand Pharmaceuticals Inc. | Moduladores selectivos del receptor de andrógeno (SARM) y usos de los mismos |
| US9962368B2 (en) * | 2009-01-09 | 2018-05-08 | Board Of Regents Of The University Of Texas System | Pro-neurogenic compounds |
| US8450374B2 (en) * | 2009-06-29 | 2013-05-28 | University Of Delaware | Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal |
| LT3124481T (lt) * | 2010-02-16 | 2018-06-11 | Aragon Pharmaceuticals, Inc. | Androgeno receptorių moduliatoriai ir jų panaudojimas |
| FI20105806A0 (fi) | 2010-07-15 | 2010-07-15 | Medeia Therapeutics Ltd | Uudet aryyliamidijohdannaiset, joilla on antiandrogeenisia ominaisuuksia |
| WO2012143599A1 (en) | 2011-04-21 | 2012-10-26 | Orion Corporation | Androgen receptor modulating carboxamides |
| FR2982261B1 (fr) * | 2011-11-04 | 2014-06-13 | Galderma Res & Dev | Nouveaux amides, et leur utilisation pharmaceutique ou cosmetique |
| CN108143728A (zh) * | 2012-07-13 | 2018-06-12 | Gtx公司 | 选择性雄激素受体调节剂在治疗乳癌中的用途 |
| JOP20200097A1 (ar) * | 2013-01-15 | 2017-06-16 | Aragon Pharmaceuticals Inc | معدل مستقبل أندروجين واستخداماته |
| WO2015017412A1 (en) * | 2013-07-29 | 2015-02-05 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | 11-oxo-10,11-dihydrodibenzo[b,f][1,4]thiazepine s-oxide derivatives and their use as dopamine d2 receptor antagonists |
| EP3046561B1 (en) * | 2013-09-20 | 2023-02-22 | University of Pittsburgh - Of the Commonwealth System of Higher Education | Compounds for treating prostate cancer |
| MX2017013565A (es) * | 2015-04-21 | 2018-02-19 | Gtx Inc | Ligandos degradadores selectivos del receptor androgénico (sard) y sus métodos uso. |
-
2016
- 2016-04-21 AU AU2016252753A patent/AU2016252753A1/en not_active Abandoned
- 2016-04-21 JP JP2017555305A patent/JP6786520B2/ja active Active
- 2016-04-21 RU RU2019115778A patent/RU2019115778A/ru unknown
- 2016-04-21 US US15/135,334 patent/US9814698B2/en not_active Expired - Fee Related
- 2016-04-21 KR KR1020177033493A patent/KR20170140291A/ko not_active Withdrawn
- 2016-04-21 CN CN201680035642.2A patent/CN107709290B/zh active Active
- 2016-04-21 EP EP16783866.3A patent/EP3286164B1/en active Active
- 2016-04-21 MX MX2017013563A patent/MX2017013563A/es unknown
- 2016-04-21 CA CA2983403A patent/CA2983403A1/en active Pending
- 2016-04-21 WO PCT/US2016/028674 patent/WO2016172358A1/en not_active Ceased
- 2016-04-21 RU RU2017140154A patent/RU2689988C2/ru active
- 2016-04-21 BR BR112017022860A patent/BR112017022860A2/pt not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| RU2689988C2 (ru) | 2019-05-30 |
| RU2019115778A (ru) | 2019-06-24 |
| EP3286164A4 (en) | 2018-12-05 |
| KR20170140291A (ko) | 2017-12-20 |
| BR112017022860A2 (pt) | 2018-07-17 |
| US20170095446A1 (en) | 2017-04-06 |
| CN107709290B (zh) | 2023-02-28 |
| JP2018513182A (ja) | 2018-05-24 |
| EP3286164A1 (en) | 2018-02-28 |
| US9814698B2 (en) | 2017-11-14 |
| JP6786520B2 (ja) | 2020-11-18 |
| CN107709290A (zh) | 2018-02-16 |
| RU2017140154A (ru) | 2019-05-21 |
| WO2016172358A1 (en) | 2016-10-27 |
| RU2017140154A3 (es) | 2019-05-21 |
| AU2016252753A1 (en) | 2017-11-09 |
| EP3286164B1 (en) | 2024-05-29 |
| CA2983403A1 (en) | 2016-10-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MX2017013563A (es) | LIGANDOS DEGRADADORES SELECTIVOS DEL RECEPTOR ANDROGíNICO (SARD) Y SUS MíTODOS DE USO. | |
| MX2017013565A (es) | Ligandos degradadores selectivos del receptor androgénico (sard) y sus métodos uso. | |
| MX2021003784A (es) | Ligandos degradadores selectivos del receptor de androgenos (sard) y metodos de uso de los mismos. | |
| PH12018502500A1 (en) | Methods and compositions for determining resistance to androgen receptor therapy | |
| MX346147B (es) | Compuestos de 3-aril-5-substituido-isoquinolin-1-ona y su uso terapeutico. | |
| MX390878B (es) | Usos medicos de antagonista de ligando 1 de muerte programada (pd-l1). | |
| MX2013001272A (es) | Nuevo tratamiento del carcinoma de prostata. | |
| HRP20150437T1 (xx) | Diarilhidantoinski spojevi kao antagonisti androgenog receptora za lijeäśenje raka | |
| SG10201909796PA (en) | Chemosensory receptor ligand-based therapies | |
| AU2013235499A8 (en) | Estrogen receptor modulators and uses thereof | |
| PH12013500481A1 (en) | Estrogen receptor modulators and uses thereof | |
| PH12013501341A1 (en) | Morphinan compounds | |
| MX2021013965A (es) | Composiciones anticancerigenas. | |
| MX383893B (es) | Uso de agonistas del receptor tipo toll- 8 (tlr8) para tratar el cáncer. | |
| EA201390977A1 (ru) | Комбинация агониста опиоидных рецепторов и антагониста опиоидных рецепторов для лечения болезни паркинсона | |
| WO2011017534A3 (en) | Treatment of prostate cancer | |
| MX2011010782A (es) | Compuestos agonistas del receptor 5-ht4 para el tratamiento de trastornos cognitivos. | |
| MY189663A (en) | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer | |
| MX2014000964A (es) | Derivados aza heterociclicos sustituidos. | |
| MX2022010438A (es) | Ligandos degradores selectivos del receptor de andrógenos (sard) y métodos de uso de los mismos. | |
| MX2015013912A (es) | Metodos y composiciones que utilizan 4-amino-2-(2,6-dioxo-piperidi n-3-il)-isoindolin-1,3-diona para tratamiento y manejo de canceres en el sistema nervioso central. | |
| IN2015DN04172A (es) | ||
| MY189372A (en) | Indole derivatives | |
| EP2464355A4 (en) | SUBSTITUTED TRIAZOLPHTHALAZINE DERIVATIVES | |
| Barbado et al. | Cannabinoids As Antimyeloma Agents: a New Approach for the Treatment of Multiple Myeloma |