JP2005525332A5 - - Google Patents
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- Publication number
- JP2005525332A5 JP2005525332A5 JP2003566005A JP2003566005A JP2005525332A5 JP 2005525332 A5 JP2005525332 A5 JP 2005525332A5 JP 2003566005 A JP2003566005 A JP 2003566005A JP 2003566005 A JP2003566005 A JP 2003566005A JP 2005525332 A5 JP2005525332 A5 JP 2005525332A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- nitrogen
- independently
- hydroxy
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 206010057668 Cognitive disease Diseases 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 3
- -1 phenyloxy, benzyloxy Chemical group 0.000 claims 3
- 206010001897 Alzheimer's disease Diseases 0.000 claims 2
- 206010002855 Anxiety Diseases 0.000 claims 2
- 206010057666 Anxiety disease Diseases 0.000 claims 2
- 206010003736 Attention deficit/hyperactivity disease Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 230000032683 aging Effects 0.000 claims 2
- 230000036506 anxiety Effects 0.000 claims 2
- 125000005418 aryl aryl group Chemical group 0.000 claims 2
- 201000006287 attention deficit hyperactivity disease Diseases 0.000 claims 2
- 125000001589 carboacyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000005842 heteroatoms Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229920000728 polyester Polymers 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 239000011593 sulfur Substances 0.000 claims 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims 1
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- ODSVXRSHXWHNNL-UHFFFAOYSA-N 7-(benzenesulfonyl)-5-bromo-4-piperidin-1-ylpyrrolo[2,3-d]pyrimidine Chemical compound C=12C(Br)=CN(S(=O)(=O)C=3C=CC=CC=3)C2=NC=NC=1N1CCCCC1 ODSVXRSHXWHNNL-UHFFFAOYSA-N 0.000 claims 1
- 206010012378 Depression Diseases 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- RZVAJINKPMORJF-UHFFFAOYSA-N p-acetaminophenol Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
Claims (3)
- 式(I):
R1aおよびR1bは独立してハロゲン、C1−6アルキル、C1−6アルコキシ、C1−6アルカノイル、CN、CF3、OCF3、フェニルオキシ、ベンジルオキシまたはC3−6シクロアルキルオキシであり;
R2はハロゲン、C1−6アルキル、C3−6シクロアルキル、C1−6アルコキシ、C1−6アルコキシ、C1−6アルキルチオ、C1−6アルキルスルフィニル、C1−6アルキルスルホニル、C1−6アルカノイル、CN、CF3、OCH2CF3、OCF3、ヒドロキシ、ヒドロキシC1−6アルキル、ヒドロキシC1−6アルコキシ、C1−6アルコキシカルボニル、C1−6アルコキシC1−6アルコキシ、ニトロ、アミノ、N(C1−6アルキル)2、NHC1−6アルキル、C1−6アルキルアミノまたはジC1−6アルキルアミノ、C(O)OR4(ここにR4は水素またはC1−6アルキル)、CONR5R6またはNR5COR6(ここにR5およびR6は独立して水素、C1−6アルキルであるか、あるいはR5およびR6は一緒になって、窒素、イオウまたは酸素から選択されるさらなる1個の異種原子を含んでいてもよい5ないし7員のアザサイクリック環を形成する)、あるいはアリールまたはヘテロアリール(それらはいずれも上で定義されたR1aおよびR1b基により置換されていてもよい)であり;
R3は、窒素、イオウまたは酸素から選択される1ないし3個の異種原子を含む5ないし7員の複素環または二環式の複素環であり、該環は、1個またはそれ以上のC1−6アルキル基によりC−および/またはN−置換されていてもよく;
mおよびnは独立して0ないし4の整数であり;
pは0ないし5の整数であり;
X、YおよびZは独立して窒素または炭素であり、ただしX、YおよびZのうち1個または2個は窒素である]
で示される化合物またはその医薬上許容される塩もしくは溶媒和物を含む医薬組成物であって、鬱病、不安症、アルツハイマー病、老化に関連した認識低下、ADHD、肥満、軽度の認識障害および分裂病の治療または予防に使用される医薬組成物。 - R1a、R1b、R2、R3、m、n、p、P、X、YおよびZが請求項1における定義と同じである式(I)の化合物であって、
5−ブロモ−7−(フェニルスルホニル)−4−(l−ピペリジニル)−7H−ピロロ[2,3−d]ピリミジン;または
5−ヨード−7−(フェニルスルホニル)−4−(l−ピペリジニル)−7H−ピロロ[2,3−d]ピリミジン
ではない、式(IA)の化合物またはその医薬上許容される塩。 - 鬱病、不安症、アルツハイマー病、老化に関連した認識低下、ADHD、肥満、軽度の認識障害および分裂病の治療に使用される請求項2記載の化合物を含む医薬組成物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0202679.7A GB0202679D0 (en) | 2002-02-05 | 2002-02-05 | Novel compounds |
PCT/EP2003/001117 WO2003066632A1 (en) | 2002-02-05 | 2003-02-04 | Sulphonyl compounds with 5 -ht6 receptor affinity |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2005525332A JP2005525332A (ja) | 2005-08-25 |
JP2005525332A5 true JP2005525332A5 (ja) | 2006-01-05 |
Family
ID=9930462
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2003566005A Pending JP2005525332A (ja) | 2002-02-05 | 2003-02-04 | 5−ht6受容体アフィニティーを有するスルホニル化合物 |
Country Status (6)
Country | Link |
---|---|
US (1) | US20050090496A1 (ja) |
EP (1) | EP1472253A1 (ja) |
JP (1) | JP2005525332A (ja) |
AU (1) | AU2003244480A1 (ja) |
GB (1) | GB0202679D0 (ja) |
WO (1) | WO2003066632A1 (ja) |
Families Citing this family (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT1497266E (pt) * | 2002-03-27 | 2008-09-10 | Glaxo Group Ltd | Derivados de quinolina e sua utilização como ligandos 5-ht6 |
MXPA06000795A (es) | 2003-07-22 | 2006-08-23 | Arena Pharm Inc | Derivados de diaril y arilheteroaril urea como moduladores del receptor 5-ht2a de serotonina utiles para la profilaxis y tratamiento de desordenes relacionados con el mismo. |
SE0302760D0 (sv) * | 2003-10-20 | 2003-10-20 | Biovitrum Ab | New compounds |
TW200522944A (en) * | 2003-12-23 | 2005-07-16 | Lilly Co Eli | CB1 modulator compounds |
CA2554696C (en) | 2004-02-13 | 2009-06-30 | Warner-Lambert Company Llc | Androgen receptor modulators |
US7507860B2 (en) | 2004-04-13 | 2009-03-24 | Pfizer Inc. | Androgen modulators |
CA2562672C (en) | 2004-04-22 | 2009-09-29 | Warner-Lambert Company Llc | 4-cyano-phenoxy derivatives as androgen modulators |
TW200724139A (en) | 2005-05-05 | 2007-07-01 | Warner Lambert Co | Androgen modulators |
MX2007014619A (es) | 2005-05-20 | 2009-02-13 | Vertex Pharma | Pirrolopiridinas de utilidad como inhibidores de proteina quinasa. |
WO2007098418A1 (en) * | 2006-02-17 | 2007-08-30 | Memory Pharmaceuticals Corporation | Compounds having 5-ht6 receptor affinity |
AU2008216032A1 (en) * | 2007-02-16 | 2008-08-21 | Memory Pharmaceuticals Corporation | 6 ' substituted indole and indazole derivatives having 5-HT6 receptor affinity |
ES2389958T3 (es) * | 2007-03-21 | 2012-11-05 | Glaxo Group Limited | Uso de derivados de quinolina en el tratamiento del dolor |
MX2009012471A (es) * | 2007-05-24 | 2010-02-24 | Memory Pharm Corp | Compuestos 4´sustituidos que tienen afinidad al receptor 5-hidroxitriptamina 6. |
AU2008286760A1 (en) * | 2007-08-15 | 2009-02-19 | Memory Pharmaceuticals Corporation | 3' substituted compounds having 5-HT6 receptor affinity |
EP2508177A1 (en) | 2007-12-12 | 2012-10-10 | Glaxo Group Limited | Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline |
WO2009123714A2 (en) | 2008-04-02 | 2009-10-08 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
US20100016297A1 (en) * | 2008-06-24 | 2010-01-21 | Memory Pharmaceuticals Corporation | Alkyl-substituted 3' compounds having 5-ht6 receptor affinity |
US20100022581A1 (en) * | 2008-07-02 | 2010-01-28 | Memory Pharmaceuticals Corporation | Pyrrolidine-substituted azaindole compounds having 5-ht6 receptor affinity |
US20100029629A1 (en) * | 2008-07-25 | 2010-02-04 | Memory Pharmaceuticals Corporation | Acyclic compounds having 5-ht6 receptor affinity |
US20100056531A1 (en) * | 2008-08-22 | 2010-03-04 | Memory Pharmaceuticals Corporation | Alkyl-substituted 3' compounds having 5-ht6 receptor affinity |
WO2010062321A1 (en) | 2008-10-28 | 2010-06-03 | Arena Pharmaceuticals, Inc. | Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and crystalline forms related thereto |
WO2015090233A1 (en) | 2013-12-20 | 2015-06-25 | Sunshine Lake Pharma Co., Ltd. | Aromatic heterocyclic compounds and their application in pharmaceuticals |
CN105541693B (zh) | 2014-07-08 | 2018-10-16 | 广东东阳光药业有限公司 | 芳杂环类衍生物及其在药物上的应用 |
EP4119141A1 (en) | 2015-06-12 | 2023-01-18 | Axovant Sciences GmbH | Nelotanserin for the prophylaxis and treatment of rem sleep behavior disorder |
CA2992518A1 (en) | 2015-07-15 | 2017-01-19 | Axovant Sciences Gmbh | Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of hallucinations associated with a neurodegenerative disease |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2051837A (en) * | 1934-07-05 | 1936-08-25 | Siemens App Und Maschinen Gmbh | Automatic control arrangement for aircraft |
US2051832A (en) * | 1934-12-13 | 1936-08-25 | Thomas H Edelblute | Puller hoist |
US6194410B1 (en) * | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
PA8474101A1 (es) * | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
ID26698A (id) * | 1998-06-19 | 2001-02-01 | Pfizer Prod Inc | SENYAWA-SENYAWA PIROLO [2,3-d] PIRIMIDINA |
US6090761A (en) * | 1998-12-22 | 2000-07-18 | Exxon Research And Engineering Company | Non-sludging, high temperature resistant food compatible lubricant for food processing machinery |
DE60011269T2 (de) * | 1999-08-12 | 2005-06-23 | Nps Allelix Corp., Mississauga | Azaidole mit serotonin rezeptor affinität |
SE0002754D0 (sv) * | 2000-07-21 | 2000-07-21 | Pharmacia & Upjohn Ab | New pharmaceutical combination formulation and method of treatment with the combination |
GB0115109D0 (en) * | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
GB0115393D0 (en) * | 2001-06-23 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
-
2002
- 2002-02-05 GB GBGB0202679.7A patent/GB0202679D0/en not_active Ceased
-
2003
- 2003-02-04 AU AU2003244480A patent/AU2003244480A1/en not_active Abandoned
- 2003-02-04 EP EP03737311A patent/EP1472253A1/en not_active Withdrawn
- 2003-02-04 JP JP2003566005A patent/JP2005525332A/ja active Pending
- 2003-02-04 WO PCT/EP2003/001117 patent/WO2003066632A1/en active Application Filing
- 2003-02-04 US US10/503,682 patent/US20050090496A1/en not_active Abandoned
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