AR089702A1 - Derivados de heteroarilamida que tienen propiedades antiandrogenicas - Google Patents
Derivados de heteroarilamida que tienen propiedades antiandrogenicasInfo
- Publication number
- AR089702A1 AR089702A1 ARP130100090A ARP130100090A AR089702A1 AR 089702 A1 AR089702 A1 AR 089702A1 AR P130100090 A ARP130100090 A AR P130100090A AR P130100090 A ARP130100090 A AR P130100090A AR 089702 A1 AR089702 A1 AR 089702A1
- Authority
- AR
- Argentina
- Prior art keywords
- ring
- group
- optionally substituted
- alkyl
- carbon atoms
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- 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
- A61P5/28—Antiandrogens
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
- C07D213/30—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/54—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
- C07D213/57—Nitriles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
- C07D213/61—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
Abstract
Los derivados de heteroarilamidas de la fórmula (1) tienen propiedades antiandrogénicas. También se refiere a los compuestos de la fórmula (1) para utilizar como un medicamento y a composiciones farmacéuticas que los comprenden y a su preparación. Reivindicación 1: Un derivado de heteroarilamida que tiene la fórmula (1) y N-óxidos, estereoisómeros y sales farmacéuticamente aceptables del mismo; donde R y R cada una se selecciona de modo independiente del grupo que consta de H y alquilo; z es un número entero de 0 a 3; X se selecciona del grupo que consta de O, S, S(O), SO₂, NR¹², donde R¹² se selecciona del grupo que consta de H, alquilo y COR, donde R es hidrógeno o alquilo; CH₂ y CO; o cuando z es 0, luego X puede ser N y forma junto con R¹¹ un anillo heterocíclico seleccionado del grupo que consta de morfolina, 1,2,4-triazol, imidazol y imidazol N-sustituido; y R¹¹, cuando no forma un anillo con X tal como se definió anteriormente, se selecciona del grupo que consta de alquilo, alquenilo, (per)haloalquilo, haloalquenilo, alquilo-CN y un arilo, heteroarilo, alifático o heteroalifático, un anillo de 3 - 7 miembros opcionalmente sustituido con 1 - 5 sustituyentes seleccionado del grupo que consta de alquilo, alcoxi, hidroxilo, halógeno, (per)haloalquilo, CN, NO₂, COR, COOR, CONHR, NR₂, NHCOCF₃, NHCOR, NHCONHR, NHCOOR, OCONHR, NHSO₂R, NHCSCH₃, SR, SOR y SO₂R, donde R es tal como se definió anteriormente; RB es un anillo heteroaromático que tiene un anillo de 6 miembros y está opcionalmente sustituido en uno o más átomos de carbono del anillo, cuyos miembros del anillo 1 ó 2 son átomos de N y los otros miembros del anillo son átomos de carbono, o RB es un grupo fenilo opcionalmente sustituido, el o los sustituyentes en RB se seleccionan del grupo que consta de alquilo, alcoxi, hidroxi, halógeno, (per)haloalquilo, CN, NO₂, COR, COOR, NR₂, NHCOCF₃, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, donde R es tal como se definió anteriormente; NHCSCH₃, SR, SOR y SO₂R, donde R es tal como se definió anteriormente, o, cuando RB es un grupo fenilo opcionalmente sustituido, luego dos sustituyentes pueden formar también con los átomos de carbono, a los cuales están unidos, un anillo alifático, heteroalifático o heteroaromático sustituido o no sustituido; y RA es un sistema de anillo mono o bicíclico heteroaromático que tiene 6 a 10 miembros del anillo y está opcionalmente sustituido en uno o más átomos de carbono del anillo, cuyos miembros del anillo 1 a 4 son átomos de N y los otros miembros del anillo son átomos de carbono, por lo cual cuando RB es un grupo fenilo opcionalmente sustituido, luego el anillo unido al grupo NH contiene al menos un átomo de N como un miembro del anillo, o cuando RB es un anillo heteroaromático opcionalmente sustituido, luego RA puede también ser un grupo fenilo opcionalmente sustituido, el o los sustituyentes en RA se seleccionan del grupo que consta de alquilo, alcoxi, halógeno, (per)haloalquilo, hidroxi, (CH₂)ₙCHO, donde n es un número entero 0 - 6; CN, NO₂, COR, COOR y CONHR, donde R es tal como se definió anteriormente, o cuando RA es un grupo fenilo opcionalmente sustituido, luego dos sustituyentes pueden formar también con los átomos de carbono, a los cuales están unidos, un anillo alifático, heteroalifático o heteroaromático sustituido o no sustituido.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FI20125039 | 2012-01-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR089702A1 true AR089702A1 (es) | 2014-09-10 |
Family
ID=47683784
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130100090A AR089702A1 (es) | 2012-01-13 | 2013-01-11 | Derivados de heteroarilamida que tienen propiedades antiandrogenicas |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US9650382B2 (es) |
| EP (1) | EP2802563B1 (es) |
| JP (1) | JP6234376B2 (es) |
| KR (1) | KR102058886B1 (es) |
| CN (1) | CN104066717B (es) |
| AR (1) | AR089702A1 (es) |
| AU (1) | AU2013208847B2 (es) |
| BR (1) | BR112014016896B1 (es) |
| CA (1) | CA2861713C (es) |
| DK (1) | DK2802563T3 (es) |
| EA (1) | EA029007B1 (es) |
| ES (1) | ES2640119T3 (es) |
| HK (1) | HK1201838A1 (es) |
| MX (1) | MX356499B (es) |
| NZ (1) | NZ626715A (es) |
| PL (1) | PL2802563T3 (es) |
| SG (1) | SG11201404053RA (es) |
| TW (1) | TWI635080B (es) |
| WO (1) | WO2013104830A1 (es) |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE28864T1 (de) | 1982-07-23 | 1987-08-15 | Ici Plc | Amide-derivate. |
| JP4255381B2 (ja) | 2001-12-13 | 2009-04-15 | 住友化学株式会社 | ビカルタミドの結晶およびその製造方法 |
| US7741371B2 (en) | 2002-06-17 | 2010-06-22 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| AU2003286757B2 (en) | 2002-11-01 | 2009-06-04 | Merck Sharp & Dohme Corp. | Carbonylamino-benzimidazole derivatives as androgen receptor modulators |
| AU2007275737A1 (en) | 2006-07-19 | 2008-01-24 | Osurf | Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof |
| US8461343B2 (en) | 2007-03-27 | 2013-06-11 | Sloan-Kettering Institute For Cancer Research | Synthesis of thiohydantoins |
| DE102007058747A1 (de) | 2007-12-05 | 2009-06-10 | Bayer Schering Pharma Aktiengesellschaft | Nichtsteroidale Progesteronrezeptor-Modulatoren |
| ITBO20090078A1 (it) | 2009-02-13 | 2010-08-14 | Consiglio Nazionale Ricerche | Composti per il trattamento del tumore alla prostata e procedimenti per la loro sintesi |
| EP2424853B1 (en) | 2009-04-10 | 2018-09-19 | Istituto Scientifico Romagnolo Per Lo Studio E La Cura Dei Tumori (I.R.S.T.) S.R.L. | Non-steroidal compounds for androgen receptor modulation, processes for the preparation and uses thereof |
| SI3124481T1 (en) | 2010-02-16 | 2018-06-29 | Aragon Pharmaceuticals, Inc. | Androgen receptor modulators and their use |
| FR2982261B1 (fr) | 2011-11-04 | 2014-06-13 | Galderma Res & Dev | Nouveaux amides, et leur utilisation pharmaceutique ou cosmetique |
-
2013
- 2013-01-11 AR ARP130100090A patent/AR089702A1/es active IP Right Grant
- 2013-01-11 AU AU2013208847A patent/AU2013208847B2/en active Active
- 2013-01-11 DK DK13703633.1T patent/DK2802563T3/en active
- 2013-01-11 TW TW102101023A patent/TWI635080B/zh active
- 2013-01-11 SG SG11201404053RA patent/SG11201404053RA/en unknown
- 2013-01-11 CA CA2861713A patent/CA2861713C/en active Active
- 2013-01-11 ES ES13703633.1T patent/ES2640119T3/es active Active
- 2013-01-11 NZ NZ626715A patent/NZ626715A/en unknown
- 2013-01-11 BR BR112014016896-2A patent/BR112014016896B1/pt active IP Right Grant
- 2013-01-11 WO PCT/FI2013/050027 patent/WO2013104830A1/en active Application Filing
- 2013-01-11 EP EP13703633.1A patent/EP2802563B1/en active Active
- 2013-01-11 KR KR1020147022538A patent/KR102058886B1/ko active IP Right Grant
- 2013-01-11 JP JP2014551659A patent/JP6234376B2/ja active Active
- 2013-01-11 PL PL13703633T patent/PL2802563T3/pl unknown
- 2013-01-11 CN CN201380005365.7A patent/CN104066717B/zh active Active
- 2013-01-11 US US14/371,927 patent/US9650382B2/en active Active
- 2013-01-11 MX MX2014008524A patent/MX356499B/es active IP Right Grant
- 2013-01-11 EA EA201491364A patent/EA029007B1/ru not_active IP Right Cessation
-
2015
- 2015-03-10 HK HK15102462.8A patent/HK1201838A1/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP6234376B2 (ja) | 2017-11-22 |
| EA201491364A1 (ru) | 2014-11-28 |
| AU2013208847A1 (en) | 2014-08-14 |
| ES2640119T3 (es) | 2017-10-31 |
| MX356499B (es) | 2018-05-30 |
| KR20140117531A (ko) | 2014-10-07 |
| KR102058886B1 (ko) | 2019-12-24 |
| WO2013104830A1 (en) | 2013-07-18 |
| HK1201838A1 (en) | 2015-09-11 |
| CA2861713A1 (en) | 2013-07-18 |
| TW201332974A (zh) | 2013-08-16 |
| PL2802563T3 (pl) | 2017-11-30 |
| US9650382B2 (en) | 2017-05-16 |
| EA029007B1 (ru) | 2018-01-31 |
| BR112014016896A8 (pt) | 2017-07-04 |
| NZ626715A (en) | 2016-07-29 |
| TWI635080B (zh) | 2018-09-11 |
| CN104066717B (zh) | 2019-07-30 |
| SG11201404053RA (en) | 2014-10-30 |
| BR112014016896B1 (pt) | 2021-08-17 |
| CN104066717A (zh) | 2014-09-24 |
| EP2802563B1 (en) | 2017-06-07 |
| CA2861713C (en) | 2021-08-31 |
| BR112014016896A2 (pt) | 2017-06-13 |
| US20150005308A1 (en) | 2015-01-01 |
| DK2802563T3 (en) | 2017-09-18 |
| JP2015504892A (ja) | 2015-02-16 |
| AU2013208847B2 (en) | 2017-08-31 |
| EP2802563A1 (en) | 2014-11-19 |
| MX2014008524A (es) | 2014-08-21 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |