JP2004511518A5 - - Google Patents
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- JP2004511518A5 JP2004511518A5 JP2002535660A JP2002535660A JP2004511518A5 JP 2004511518 A5 JP2004511518 A5 JP 2004511518A5 JP 2002535660 A JP2002535660 A JP 2002535660A JP 2002535660 A JP2002535660 A JP 2002535660A JP 2004511518 A5 JP2004511518 A5 JP 2004511518A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- alkoxy
- substituted
- halogen atom
- 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.)
- Withdrawn
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- 125000005843 halogen group Chemical group 0.000 claims 18
- 125000003545 alkoxy group Chemical group 0.000 claims 14
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 125000003277 amino group Chemical group 0.000 claims 12
- 239000003795 chemical substances by application Substances 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 125000002950 monocyclic group Chemical group 0.000 claims 7
- 102000015696 Interleukins Human genes 0.000 claims 6
- 108010063738 Interleukins Proteins 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000004430 oxygen atom Chemical group O* 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 5
- 125000004760 (C1-C4) alkylsulfonylamino group Chemical group 0.000 claims 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 5
- 101150109738 Ptger4 gene Proteins 0.000 claims 5
- 125000004414 alkyl thio group Chemical group 0.000 claims 5
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 5
- 125000002619 bicyclic group Chemical group 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000004434 sulfur atom Chemical group 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 102000054727 Serum Amyloid A Human genes 0.000 claims 4
- 108700028909 Serum Amyloid A Proteins 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- -1 oxopiperidyl group Chemical group 0.000 claims 4
- 206010023230 Joint stiffness Diseases 0.000 claims 3
- 206010003246 arthritis Diseases 0.000 claims 3
- 208000018937 joint inflammation Diseases 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 2
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 2
- 238000001727 in vivo Methods 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000005476 oxopyrrolidinyl group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000005936 piperidyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims 1
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 claims 1
- 206010023232 Joint swelling Diseases 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 101710195838 Prostaglandin E2 receptor EP4 subtype Proteins 0.000 claims 1
- 102100024450 Prostaglandin E2 receptor EP4 subtype Human genes 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 238000010171 animal model Methods 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 206010020718 hyperplasia Diseases 0.000 claims 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 1
- 210000001503 joint Anatomy 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 230000008961 swelling Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24182500P | 2000-10-19 | 2000-10-19 | |
| PCT/IB2001/001942 WO2002032422A2 (en) | 2000-10-19 | 2001-10-15 | Ep4 receptor inhibitors to treat rheumatoid arthritis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004511518A JP2004511518A (ja) | 2004-04-15 |
| JP2004511518A5 true JP2004511518A5 (enExample) | 2005-04-07 |
Family
ID=22912331
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002535660A Withdrawn JP2004511518A (ja) | 2000-10-19 | 2001-10-15 | リウマチ様関節炎の治療のためのｅｐ４受容体インヒビター |
| JP2002536282A Expired - Lifetime JP4060182B2 (ja) | 2000-10-19 | 2001-10-15 | 抗炎症剤及び鎮痛剤としてのアリール又はヘテロアリール縮合イミダゾール化合物 |
| JP2007154590A Expired - Lifetime JP4703607B2 (ja) | 2000-10-19 | 2007-06-11 | 抗炎症剤及び鎮痛剤としてのアリール又はヘテロアリール縮合イミダゾール化合物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002536282A Expired - Lifetime JP4060182B2 (ja) | 2000-10-19 | 2001-10-15 | 抗炎症剤及び鎮痛剤としてのアリール又はヘテロアリール縮合イミダゾール化合物 |
| JP2007154590A Expired - Lifetime JP4703607B2 (ja) | 2000-10-19 | 2007-06-11 | 抗炎症剤及び鎮痛剤としてのアリール又はヘテロアリール縮合イミダゾール化合物 |
Country Status (49)
Families Citing this family (77)
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| US7544511B2 (en) * | 1996-09-25 | 2009-06-09 | Neuralstem Biopharmaceuticals Ltd. | Stable neural stem cell line methods |
| EP1382603B1 (en) * | 2001-04-26 | 2008-07-23 | Eisai R&D Management Co., Ltd. | Nitrogenous fused-ring compound having pyrazolyl group as substituent and medicinal composition thereof |
| CA2482382A1 (en) * | 2002-04-12 | 2003-10-23 | Pfizer Inc. | Pyrazole compounds as anti-inflammatory and analgesic agents |
| MXPA04009243A (es) | 2002-04-12 | 2005-06-08 | Pfizer | Uso de ligandos para el receptor ep4 en el tratamiento de enfermedades vinculadas a il-6. |
| WO2003086390A1 (en) * | 2002-04-12 | 2003-10-23 | Pfizer Japan Inc. | Imidazole compounds as anti-inflammatory and analgesic agents |
| AU2003293409A1 (en) | 2002-12-09 | 2004-06-30 | Karl K. Johe | Method for discovering neurogenic agents |
| US8293488B2 (en) | 2002-12-09 | 2012-10-23 | Neuralstem, Inc. | Method for screening neurogenic agents |
| KR20050084445A (ko) * | 2002-12-20 | 2005-08-26 | 다이노젠 파마세우티컬스, 인코포레이티드 | α₂δ 서브유닛 칼슘 채널 모듈레이터를 이용한 무통증방광 질환의 치료방법 |
| CN100335460C (zh) * | 2003-02-14 | 2007-09-05 | 和光纯药工业株式会社 | 使用离子交换树脂固定化铂催化剂的羟胺化合物制造方法 |
| JP4185097B2 (ja) * | 2003-03-13 | 2008-11-19 | 出光興産株式会社 | 新規含窒素複素環誘導体及びそれを用いた有機エレクトロルミネッセンス素子 |
| US20070105931A1 (en) * | 2003-08-04 | 2007-05-10 | Mayo Foundation For Medical Education And Research | Methods and compositions for inhibiting the proliferation of prostate cancer cells |
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| US7534796B2 (en) | 2005-02-18 | 2009-05-19 | Wyeth | Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7538113B2 (en) | 2005-02-18 | 2009-05-26 | Wyeth | 4-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7582634B2 (en) | 2005-02-18 | 2009-09-01 | Wyeth | 7-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor |
| IN2014DN09939A (enExample) | 2005-03-11 | 2015-08-14 | Raqualia Pharma Inc | |
| US7531542B2 (en) | 2005-05-18 | 2009-05-12 | Wyeth | Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor |
| US7582636B2 (en) | 2005-05-26 | 2009-09-01 | Wyeth | Piperazinylimidazopyridine and piperazinyltriazolopyridine antagonists of Gonadotropin Releasing Hormone receptor |
| AU2006327243A1 (en) * | 2005-12-21 | 2007-06-28 | Decode Genetics Ehf | N-linked aryl heteroaryl inhibitors of LTA4H for treating inflammation |
| EP2019675A4 (en) * | 2006-05-02 | 2011-03-02 | Merck Frosst Canada Ltd | METHOD FOR THE TREATMENT OR PREVENTION OF NEOPLASIA |
| CL2007002994A1 (es) * | 2006-10-19 | 2008-02-08 | Wyeth Corp | Compuestos derivados heterociclicos que contienen sulfamoilo, inhibidores de hsp90; composicion farmaceutica; y uso para el tratamiento del cancer, tal como cancer de mama, de colon y prostata, entre otros. |
| WO2008116304A1 (en) * | 2007-03-26 | 2008-10-02 | Merck Frosst Canada Ltd. | Naphthalene and quinoline sulfonylurea derivatives as ep4 receptor antagonists |
| DE102007037579B4 (de) | 2007-08-09 | 2012-05-16 | Emc Microcollections Gmbh | Neue Benzimidazol-2-yl-alkylamine und ihre Anwendung als mikrobizide Wirkstoffe |
| WO2009029622A2 (en) * | 2007-08-27 | 2009-03-05 | Siga Technologies, Inc. | Antiviral drugs for treatment of arenavirus infection |
| JP2011509990A (ja) | 2008-01-22 | 2011-03-31 | オキサジェン リミテッド | Ｃｒｔｈ２アンタゴニスト活性を有する化合物 |
| MX2011003166A (es) * | 2008-09-25 | 2011-04-27 | Merck Frosst Canada Ltd | Derivados de sulfonilurea beta-carbolina como antagonistas del receptor ep4. |
| JPWO2010087425A1 (ja) | 2009-01-30 | 2012-08-02 | 国立大学法人京都大学 | 前立腺癌の進行抑制剤および進行抑制方法 |
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| KR101041561B1 (ko) * | 2009-12-21 | 2011-06-15 | 짚라인코리아 (주) | 비행용 착용복 |
| CN102770159A (zh) * | 2010-02-22 | 2012-11-07 | 拉夸里亚创药株式会社 | Ep-4受体拮抗剂在治疗il-23介导疾病中的用途 |
| RU2013108868A (ru) | 2010-07-28 | 2014-09-10 | Ньюралстем, Инк. | Способы лечения и/или реверсии нейродегенеративных заболеваний и/или расстройств |
| SMT201700008T1 (it) | 2010-09-21 | 2017-03-08 | Eisai R&D Man Co Ltd | Composizione farmaceutica |
| JPWO2012102254A1 (ja) * | 2011-01-25 | 2014-06-30 | キッセイ薬品工業株式会社 | インドール誘導体、またはその薬理学的に許容される塩 |
| TW201326154A (zh) * | 2011-11-28 | 2013-07-01 | 拜耳知識產權公司 | 作為ｅｐ２受體拮抗劑之新穎２ｈ－吲唑 |
| UA115576C2 (uk) | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
| US10391086B2 (en) | 2013-03-19 | 2019-08-27 | Askat Inc. | Use of EP4 receptor antagonists in the treatment of cartilage disease |
| BR112015023663A2 (pt) * | 2013-03-19 | 2020-10-20 | Askat Inc. | uso de um composto com atividade antagonística de ep4 ou um sal farmaceuticamente aceitável deste, uso de um composto da fórmula (i), (ii), (iii), (iv), (va) ou (vb) ou um sal farmaceuticamente aceitável deste, composição farmacêutica para o tratamento de doença de cartilagem, método para o tratamento de doenças de cartilagem em um indivíduo animal, incluindo um indivíduo mamífero e composto da fórmula (i), (ii),(iii), (iv), (va) ou (vb) ou um sal farmaceuticamente aceitável deste |
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| JP6484555B2 (ja) * | 2013-08-29 | 2019-03-13 | 京都薬品工業株式会社 | 新規芳香族化合物およびその用途 |
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| US12109218B2 (en) | 2014-12-09 | 2024-10-08 | Aratana Therapeutics, Inc. | Compositions of grapiprant and methods for using the same |
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| ES2816057T3 (es) * | 2014-03-06 | 2021-03-31 | Aratana Therapeutics Inc | Procedimiento de preparación de la forma A de grapiprant |
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| WO2018162562A1 (en) | 2017-03-10 | 2018-09-13 | Bayer Pharma Aktiengesellschaft | Use of an ep4 antagonist for the treatment of inflammatory pain |
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| AU2018268311B2 (en) | 2017-05-18 | 2022-02-10 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives as PGE2 receptor modulators |
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| US11325899B2 (en) | 2017-05-18 | 2022-05-10 | Idorsia Pharmaceuticals Ltd | Benzofurane and benzothiophene derivatives as PGE2 receptor modulators |
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| RU2659169C1 (ru) * | 2017-10-31 | 2018-06-28 | Федеральное бюджетное учреждение науки "Уфимский научно-исследовательский институт медицины труда и экологии человека" | Способ прогнозирования риска развития иммуноопосредованных заболеваний у работающих в условиях обсеменённости воздуха рабочей зоны условно-патогенными микроорганизмами |
| US10973834B2 (en) | 2018-04-16 | 2021-04-13 | Arrys Therapeutics, Inc. | EP4 inhibitors and use thereof |
| WO2019245590A1 (en) | 2018-06-18 | 2019-12-26 | Avista Pharma Solutions, Inc. | Chemical compounds |
| WO2020014445A1 (en) * | 2018-07-11 | 2020-01-16 | Arrys Therapeutics, Inc. | Ep4 inhibitors and synthesis thereof |
| WO2020014465A1 (en) | 2018-07-11 | 2020-01-16 | Arrys Therapeutics, Inc. | Polymorphic compounds and uses thereof |
| CN120365272A (zh) | 2018-10-05 | 2025-07-25 | 安娜普尔纳生物股份有限公司 | 用于治疗与apj受体活性有关的疾病的化合物和组合物 |
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| WO2020160074A1 (en) | 2019-01-30 | 2020-08-06 | Avista Pharma Solutions, Inc. | Synthetic process and novel intermediates |
| WO2021027722A1 (zh) * | 2019-08-09 | 2021-02-18 | 成都先导药物开发股份有限公司 | 一种免疫调节剂 |
| US11254675B2 (en) | 2019-08-12 | 2022-02-22 | Cadila Healthcare Limited | Process for preparation of grapiprant |
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| WO2022102731A1 (ja) | 2020-11-13 | 2022-05-19 | 小野薬品工業株式会社 | Ｅｐ４拮抗薬と免疫チェックポイント阻害物質との併用によるがん治療 |
| CN116478155B (zh) * | 2022-01-17 | 2025-06-13 | 洛阳惠中兽药有限公司 | 一种格拉匹伦及其中间体的制备方法 |
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-
2001
- 2001-10-08 HN HN2001000224A patent/HN2001000224A/es unknown
- 2001-10-15 SK SK460-2003A patent/SK4602003A3/sk not_active Application Discontinuation
- 2001-10-15 DE DE60118020T patent/DE60118020T2/de not_active Expired - Lifetime
- 2001-10-15 ES ES01978702T patent/ES2258554T3/es not_active Expired - Lifetime
- 2001-10-15 CA CA002426487A patent/CA2426487A1/en not_active Abandoned
- 2001-10-15 OA OA1200300117A patent/OA12526A/en unknown
- 2001-10-15 EP EP06110920.3A patent/EP1666480B1/en not_active Expired - Lifetime
- 2001-10-15 IL IL15543901A patent/IL155439A0/xx unknown
- 2001-10-15 CN CNA018192858A patent/CN1476448A/zh active Pending
- 2001-10-15 AU AU2002210796A patent/AU2002210796B8/en not_active Ceased
- 2001-10-15 EA EA200300387A patent/EA200300387A1/ru unknown
- 2001-10-15 CZ CZ20031010A patent/CZ20031010A3/cs unknown
- 2001-10-15 CA CA002426457A patent/CA2426457C/en not_active Expired - Lifetime
- 2001-10-15 AU AU2001294122A patent/AU2001294122A1/en not_active Abandoned
- 2001-10-15 AP APAP/P/2001/002299A patent/AP2001002299A0/en unknown
- 2001-10-15 PL PL01362171A patent/PL362171A1/xx not_active Application Discontinuation
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