JP2007533707A5 - - Google Patents
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- Publication number
- JP2007533707A5 JP2007533707A5 JP2007508908A JP2007508908A JP2007533707A5 JP 2007533707 A5 JP2007533707 A5 JP 2007533707A5 JP 2007508908 A JP2007508908 A JP 2007508908A JP 2007508908 A JP2007508908 A JP 2007508908A JP 2007533707 A5 JP2007533707 A5 JP 2007533707A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cyano
- optionally substituted
- nitro
- compound according
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 36
- 150000001875 compounds Chemical class 0.000 claims 25
- 125000004093 cyano group Chemical group *C#N 0.000 claims 23
- -1 cyano, formyl Chemical group 0.000 claims 14
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 11
- 125000001153 fluoro group Chemical group F* 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000001309 chloro group Chemical group Cl* 0.000 claims 8
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 4
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 claims 3
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 239000003098 androgen Substances 0.000 claims 2
- 102000001307 androgen receptors Human genes 0.000 claims 2
- 108010080146 androgen receptors Proteins 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 2
- 125000004284 isoxazol-3-yl group Chemical group [H]C1=C([H])C(*)=NO1 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000003145 oxazol-4-yl group Chemical group O1C=NC(=C1)* 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 claims 2
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- KGNITIORKHRLEL-UHFFFAOYSA-N 1-(furan-2-ylmethyl)-n-methyl-3-(2-nitrophenyl)sulfanylindol-6-amine Chemical compound C=1N(CC=2OC=CC=2)C2=CC(NC)=CC=C2C=1SC1=CC=CC=C1[N+]([O-])=O KGNITIORKHRLEL-UHFFFAOYSA-N 0.000 claims 1
- RRRBPKKMUGCKTD-UHFFFAOYSA-N 1-[(3,5-difluorophenyl)methyl]-n-methyl-3-(2-nitrophenyl)sulfanylindol-6-amine Chemical compound C=1N(CC=2C=C(F)C=C(F)C=2)C2=CC(NC)=CC=C2C=1SC1=CC=CC=C1[N+]([O-])=O RRRBPKKMUGCKTD-UHFFFAOYSA-N 0.000 claims 1
- QBGKDQIZNDJGFH-UHFFFAOYSA-N 1-[[1-[(3,5-difluorophenyl)methyl]-3-(2-nitrophenyl)sulfanylindol-6-yl]amino]propan-2-one Chemical compound C=1N(CC=2C=C(F)C=C(F)C=2)C2=CC(NCC(=O)C)=CC=C2C=1SC1=CC=CC=C1[N+]([O-])=O QBGKDQIZNDJGFH-UHFFFAOYSA-N 0.000 claims 1
- BSXCJNDVWKVFSF-UHFFFAOYSA-N 2-[1-[(3,5-difluorophenyl)methyl]-6-(methylamino)indol-3-yl]sulfanylbenzonitrile Chemical compound C=1N(CC=2C=C(F)C=C(F)C=2)C2=CC(NC)=CC=C2C=1SC1=CC=CC=C1C#N BSXCJNDVWKVFSF-UHFFFAOYSA-N 0.000 claims 1
- VGYVEJBRPJPPGJ-UHFFFAOYSA-N 2-[[1-[(3,5-difluorophenyl)methyl]-3-(2-nitrophenyl)sulfanylindol-6-yl]amino]acetonitrile Chemical compound [O-][N+](=O)C1=CC=CC=C1SC(C1=CC=C(NCC#N)C=C11)=CN1CC1=CC(F)=CC(F)=C1 VGYVEJBRPJPPGJ-UHFFFAOYSA-N 0.000 claims 1
- MQWIOFLGUYHMNX-UHFFFAOYSA-N 2-[[1-[(3,5-difluorophenyl)methyl]-3-(2-nitrophenyl)sulfanylindol-6-yl]amino]ethanol Chemical compound C=1N(CC=2C=C(F)C=C(F)C=2)C2=CC(NCCO)=CC=C2C=1SC1=CC=CC=C1[N+]([O-])=O MQWIOFLGUYHMNX-UHFFFAOYSA-N 0.000 claims 1
- 125000006288 3,5-difluorobenzyl group Chemical group [H]C1=C(F)C([H])=C(C([H])=C1F)C([H])([H])* 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 239000002583 male contraceptive agent Substances 0.000 claims 1
- ZNYRFQLLMACTIT-UHFFFAOYSA-N n-methyl-3-(2-nitrophenyl)sulfanyl-1-(pyridin-2-ylmethyl)indol-6-amine Chemical compound C=1N(CC=2N=CC=CC=2)C2=CC(NC)=CC=C2C=1SC1=CC=CC=C1[N+]([O-])=O ZNYRFQLLMACTIT-UHFFFAOYSA-N 0.000 claims 1
- 125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US56504304P | 2004-04-23 | 2004-04-23 | |
| EP04101700 | 2004-04-23 | ||
| EP04101700.5 | 2004-04-23 | ||
| US60/565,043 | 2004-04-23 | ||
| PCT/EP2005/051766 WO2005102998A1 (en) | 2004-04-23 | 2005-04-21 | Novel androgens |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007533707A JP2007533707A (ja) | 2007-11-22 |
| JP2007533707A5 true JP2007533707A5 (https=) | 2008-06-19 |
| JP4997101B2 JP4997101B2 (ja) | 2012-08-08 |
Family
ID=34929000
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007508908A Expired - Fee Related JP4997101B2 (ja) | 2004-04-23 | 2005-04-21 | 新規アンドロゲン |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US7812036B2 (https=) |
| EP (1) | EP1742912B1 (https=) |
| JP (1) | JP4997101B2 (https=) |
| CN (1) | CN1956954B (https=) |
| AR (1) | AR049885A1 (https=) |
| AT (1) | ATE478844T1 (https=) |
| AU (1) | AU2005235751B2 (https=) |
| BR (1) | BRPI0510078A (https=) |
| CA (1) | CA2562571C (https=) |
| DE (1) | DE602005023145D1 (https=) |
| ES (1) | ES2349754T3 (https=) |
| IL (1) | IL178562A (https=) |
| MX (1) | MXPA06012201A (https=) |
| MY (1) | MY144304A (https=) |
| PE (1) | PE20060196A1 (https=) |
| TW (1) | TW200602317A (https=) |
| WO (1) | WO2005102998A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA05004929A (es) | 2002-11-07 | 2005-08-18 | Akzo Nobel Nv | Indoles utiles en el tratamiento de enfermedades relacionadas a receptor de androgeno. |
| US8268872B2 (en) | 2008-02-22 | 2012-09-18 | Radius Health, Inc. | Selective androgen receptor modulators |
| CA2716320C (en) | 2008-02-22 | 2014-01-28 | Radius Health, Inc. | Selective androgen receptor modulators |
| AU2011212813B2 (en) | 2010-02-04 | 2014-10-23 | Radius Health, Inc. | Selective androgen receptor modulators |
| HUE030072T2 (en) | 2010-05-12 | 2017-04-28 | Radius Health Inc | Therapeutic prescriptions |
| US8642632B2 (en) | 2010-07-02 | 2014-02-04 | Radius Health, Inc. | Selective androgen receptor modulators |
| US9133182B2 (en) | 2010-09-28 | 2015-09-15 | Radius Health, Inc. | Selective androgen receptor modulators |
| US9421264B2 (en) | 2014-03-28 | 2016-08-23 | Duke University | Method of treating cancer using selective estrogen receptor modulators |
| ES3055185T3 (en) | 2014-03-28 | 2026-02-10 | Univ Duke | Treatment of an estrogen receptor positive breast cancer using a selective estrogen receptor modulator |
| MX389702B (es) | 2016-06-22 | 2025-03-20 | Ellipses Pharma Ltd | Compuestos para usarse en el tratamiento de cancer de mama que expresa el receptor de androgenos (ar+). |
| JP7481115B2 (ja) | 2017-01-05 | 2024-05-10 | ラジウス ファーマシューティカルズ，インコーポレイテッド | Ｒａｄ１９０１－２ｈｃｌの多形性形態 |
| MX2020013713A (es) | 2018-07-04 | 2021-03-02 | Radius Pharmaceuticals Inc | Formas polimorficas de rad1901-2hcl. |
| EP3924328A1 (en) | 2019-02-12 | 2021-12-22 | Radius Pharmaceuticals, Inc. | Processes and compounds |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ179580A (en) | 1974-12-30 | 1978-04-03 | Mcneilab Inc | 2-or 3-(w-tertiaryaminoalkyl)-thioindoles and the corresponding sulfinyl and sulfonyl analogs |
| US4059583A (en) * | 1975-11-13 | 1977-11-22 | Mcneil Laboratories, Incorporated | Substituted indoles |
| JPS63313770A (ja) | 1987-06-16 | 1988-12-21 | Sumitomo Chem Co Ltd | イサチン誘導体、その製造法およびそれを有効成分とする除草剤 |
| EP0303306B1 (en) | 1987-08-08 | 1993-03-10 | Akzo N.V. | Contraceptive implant |
| DE3924052A1 (de) | 1989-07-21 | 1991-01-24 | Bayer Ag | N- (indol-6-yl)-heterocyclen |
| FR2662713B1 (fr) | 1990-05-29 | 1994-04-08 | Oreal | Procede de teinture de fibres keratiniques avec un aminoindole associe a un derive quinonique. |
| US5938792A (en) * | 1991-04-18 | 1999-08-17 | L'oreal | Process for dyeing keratinous fibers with aminoindoles and oxidation dye precursors at basic Ph's and dyeing agents |
| FR2675380A1 (fr) | 1991-04-18 | 1992-10-23 | Oreal | Procede de teinture des fibres keratiniques avec des aminoindoles, a ph basique, compositions mises en óoeuvre et nouveaux composes. |
| GB9204365D0 (en) | 1992-02-28 | 1992-04-08 | Pfizer Ltd | Indoles |
| US5482960A (en) | 1994-11-14 | 1996-01-09 | Warner-Lambert Company | Nonpeptide endothelin antagonists |
| JP3107290B2 (ja) * | 1996-05-20 | 2000-11-06 | 株式会社日立製作所 | 燃料装荷方法 |
| HUP9904215A3 (en) | 1996-11-25 | 2002-01-28 | Procter & Gamble | 2-imidazolinylaminoindole compounds useful as alpha-2 adrenoceptor agonists |
| IL123813A0 (en) | 1997-04-11 | 1998-10-30 | Akzo Nobel Nv | Drug delivery system for two or more active substances |
| US5969155A (en) * | 1997-04-11 | 1999-10-19 | The United States Of America As Represented By The Secretary Of The Army | Conversion of trinitrotoluene into high value compounds |
| EA200000868A1 (ru) | 1998-02-25 | 2001-04-23 | Дженетикс Инститьют, Инк. | Ингибиторы фосфолипаз |
| HUP0100156A3 (en) | 1998-02-25 | 2002-12-28 | Genetics Inst Inc Cambridge | Indole derivatives as inhibitors of phospholipase a2 and use of them for producing pharmaceutical compositions |
| GB9819033D0 (en) | 1998-09-01 | 1998-10-28 | Cerebrus Ltd | Chemical compounds VI |
| US6645974B2 (en) * | 2001-07-31 | 2003-11-11 | Merck & Co., Inc. | Androgen receptor modulators and methods for use thereof |
| TWI317634B (en) * | 2001-12-13 | 2009-12-01 | Nat Health Research Institutes | Aroyl indoles compounds |
| AU2002367424A1 (en) | 2001-12-28 | 2003-07-24 | Takeda Chemical Industries, Ltd. | Androgen receptor antagonists |
| JP4316232B2 (ja) * | 2001-12-28 | 2009-08-19 | 武田薬品工業株式会社 | アンドロゲン受容体拮抗剤 |
| RU2337909C2 (ru) * | 2002-02-01 | 2008-11-10 | Ф.Хоффманн-Ля Рош Аг | Замещенные индолы и фармацевтическая композиция, обладающая агонистической активностью в отношении альфа-1a/l адренорецептора |
| UA79504C2 (en) * | 2002-11-07 | 2007-06-25 | Organon Nv | Indols for treating diseases associated with androgen receptors |
| MXPA05004929A (es) * | 2002-11-07 | 2005-08-18 | Akzo Nobel Nv | Indoles utiles en el tratamiento de enfermedades relacionadas a receptor de androgeno. |
| RU2313524C2 (ru) * | 2003-05-09 | 2007-12-27 | Ф.Хоффманн-Ля Рош Аг | МИТИЛИНДОЛЫ И МЕТИЛПИРРОЛОПИРИДИНЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ АКТИВНОСТЬЮ α-1-АДРЕНЕРГИЧЕСКИХ АГОНИСТОВ |
-
2005
- 2005-04-13 TW TW094111712A patent/TW200602317A/zh unknown
- 2005-04-21 MX MXPA06012201A patent/MXPA06012201A/es active IP Right Grant
- 2005-04-21 AU AU2005235751A patent/AU2005235751B2/en not_active Ceased
- 2005-04-21 BR BRPI0510078-0A patent/BRPI0510078A/pt not_active IP Right Cessation
- 2005-04-21 WO PCT/EP2005/051766 patent/WO2005102998A1/en not_active Ceased
- 2005-04-21 DE DE602005023145T patent/DE602005023145D1/de not_active Expired - Lifetime
- 2005-04-21 ES ES05737941T patent/ES2349754T3/es not_active Expired - Lifetime
- 2005-04-21 CA CA2562571A patent/CA2562571C/en not_active Expired - Fee Related
- 2005-04-21 JP JP2007508908A patent/JP4997101B2/ja not_active Expired - Fee Related
- 2005-04-21 EP EP05737941A patent/EP1742912B1/en not_active Expired - Lifetime
- 2005-04-21 AT AT05737941T patent/ATE478844T1/de not_active IP Right Cessation
- 2005-04-21 PE PE2005000446A patent/PE20060196A1/es not_active Application Discontinuation
- 2005-04-21 CN CN2005800164068A patent/CN1956954B/zh not_active Expired - Fee Related
- 2005-04-21 US US11/587,192 patent/US7812036B2/en not_active Expired - Fee Related
- 2005-04-22 AR ARP050101602A patent/AR049885A1/es unknown
- 2005-04-22 MY MYPI20051785A patent/MY144304A/en unknown
-
2006
- 2006-10-15 IL IL178562A patent/IL178562A/en not_active IP Right Cessation
-
2010
- 2010-09-22 US US12/887,607 patent/US20110009428A1/en not_active Abandoned
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