AR051713A1 - Derivado de pirrol sustituido - Google Patents
Derivado de pirrol sustituidoInfo
- Publication number
- AR051713A1 AR051713A1 ARP050105189A ARP050105189A AR051713A1 AR 051713 A1 AR051713 A1 AR 051713A1 AR P050105189 A ARP050105189 A AR P050105189A AR P050105189 A ARP050105189 A AR P050105189A AR 051713 A1 AR051713 A1 AR 051713A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- optionally substituted
- atom
- substituted
- optionally
- Prior art date
Links
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 150000003233 pyrroles Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000003396 thiol group Chemical group [H]S* 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- -1 1,3-dioxolan-2-yl Chemical group 0.000 abstract 1
- 229940123407 Androgen receptor antagonist Drugs 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 239000003936 androgen receptor antagonist Substances 0.000 abstract 1
- 102000001307 androgen receptors Human genes 0.000 abstract 1
- 108010080146 androgen receptors Proteins 0.000 abstract 1
- 230000008485 antagonism Effects 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
- C07D207/327—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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
La presente proporciona un nuevo derivado de pirrol que tiene un excelente antagonismo de los receptores de androgenos, el cual está representado por la formula (1) en donde R1 representa un átomo de H, un grupo ciano o un grupo representado por la formula COORA (en donde RA representa un grupo alquilo C1-6 opcionalmente sustituido, R2 y R4 son iguales o diferentes, y cada uno representa un átomo de H, un grupo alquilo C1-6, un grupo cicloalquilo C3-6, un grupo trifluorometilo, un grupo aminoalquilo C1-6, un grupo aminoalquilo C1-6 mono- o disustituido, un grupo alquilo C1-6 opcionalmente halogenado sustituido con un grupo hidroxilo opcionalmente sustituido, un grupo alquenilo C2-6 ustituido con un grupo hidroxilo opcionalmente sustituido, un grupo alquilo C1-6 sustituido con un grupo tiol opcionalmente sustituido y opcionalmente oxidado, un grupo tiol opcionalmente sustituido y opcionalmente oxidado, un grupo ciano, un grupo acilo, un grupo oxazolilo opcionalmente sustituido o un grupo 1,3-dioxolan-2-ilo; R3 representa un grupo representado por la formula (2) (en donde X representa un átomo de halogeno, Y representa un átomo de C o un átomo de N, Alk representa un grupo alquileno C1-4 opcionalmente sustituido, y RB representa un átomo de H o un grupo acilo), y R5 representa un grupo fenilo que tiene un grupo ciano en la posicion 4 o en la posicion 3, y también puede estar sustituido, o una de sus sales. LA presente también proporciona un antagonista del receptor de androgenos que contiene el derivado pirrol, o una de sus sales.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2004361641 | 2004-12-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR051713A1 true AR051713A1 (es) | 2007-01-31 |
Family
ID=35883518
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050105189A AR051713A1 (es) | 2004-12-14 | 2005-12-12 | Derivado de pirrol sustituido |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20080176906A1 (es) |
| EP (1) | EP1824841A1 (es) |
| JP (1) | JP2008523052A (es) |
| AR (1) | AR051713A1 (es) |
| PE (1) | PE20060734A1 (es) |
| TW (1) | TW200628446A (es) |
| WO (1) | WO2006064944A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2172559A1 (en) | 2007-06-13 | 2010-04-07 | Takeda Pharmaceutical Company Limited | Screening method |
| GB0711776D0 (en) * | 2007-06-18 | 2007-07-25 | Syngenta Participations Ag | Substituted aromatic heterocyclic compounds as fungicides |
| EA201070323A1 (ru) * | 2007-08-30 | 2010-10-29 | Такеда Фармасьютикал Компани Лимитед | Замещенное производное пиразола |
| CN104188971B (zh) | 2007-12-21 | 2017-05-03 | 配体药物公司 | 选择性雄激素受体调节剂(sarm)及其应用 |
| US20090270361A1 (en) * | 2008-03-26 | 2009-10-29 | Takeda Pharmaceutical Company Limited | Substituted pyrazole derivatives and use thereof |
| EP3241826B1 (en) | 2009-02-25 | 2019-10-30 | Takeda Pharmaceutical Company Limited | Process for producing pyrrole compound |
| EA201390598A1 (ru) | 2010-10-22 | 2013-08-30 | Астеллас Фарма Инк. | Антагонист мутантного андрогенного рецептора |
| CA2970565A1 (en) * | 2014-12-15 | 2016-06-23 | Bayer Pharma Aktiengesellschaft | Antibody-drug conjugates (adcs) of ksp inhibitors with aglycosylated anti-tweakr antibodies |
| CN105218437A (zh) * | 2015-10-31 | 2016-01-06 | 高大元 | 一种3-氯-5-溴-2-吡啶甲酸的合成方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6017924A (en) * | 1996-06-27 | 2000-01-25 | Ligand Pharmaceuticals Incorporated | Androgen receptor modulator compounds and methods |
| GB0016453D0 (en) * | 2000-07-04 | 2000-08-23 | Hoffmann La Roche | Pyrrole derivatives |
| US6861432B2 (en) * | 2001-11-23 | 2005-03-01 | Schering Aktiengesellschaft | Piperazine derivatives that destabilize androgen receptors |
| WO2003057669A1 (fr) * | 2001-12-28 | 2003-07-17 | Takeda Chemical Industries, Ltd. | Antagonistes du recepteur androgene |
| SI1557411T1 (es) * | 2002-07-12 | 2013-01-31 | Astellas Pharma Inc | |
| JP2006515605A (ja) * | 2003-01-17 | 2006-06-01 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | アンドロゲンレセプターアンタゴニスト |
-
2005
- 2005-12-08 TW TW094143316A patent/TW200628446A/zh unknown
- 2005-12-12 PE PE2005001433A patent/PE20060734A1/es not_active Application Discontinuation
- 2005-12-12 AR ARP050105189A patent/AR051713A1/es not_active Application Discontinuation
- 2005-12-13 US US11/793,113 patent/US20080176906A1/en not_active Abandoned
- 2005-12-13 WO PCT/JP2005/023215 patent/WO2006064944A1/en active Application Filing
- 2005-12-13 JP JP2007545156A patent/JP2008523052A/ja not_active Withdrawn
- 2005-12-13 EP EP05816739A patent/EP1824841A1/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| JP2008523052A (ja) | 2008-07-03 |
| WO2006064944A1 (en) | 2006-06-22 |
| TW200628446A (en) | 2006-08-16 |
| US20080176906A1 (en) | 2008-07-24 |
| EP1824841A1 (en) | 2007-08-29 |
| PE20060734A1 (es) | 2006-09-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |