BRPI0114704B8 - composto de imidazol fundido a arila ou heteroarila, suas composições farmacêuticas, bem como seu uso - Google Patents

composto de imidazol fundido a arila ou heteroarila, suas composições farmacêuticas, bem como seu uso

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Publication number
BRPI0114704B8
BRPI0114704B8 BRPI0114704A BR0114704A BRPI0114704B8 BR PI0114704 B8 BRPI0114704 B8 BR PI0114704B8 BR PI0114704 A BRPI0114704 A BR PI0114704A BR 0114704 A BR0114704 A BR 0114704A BR PI0114704 B8 BRPI0114704 B8 BR PI0114704B8
Authority
BR
Brazil
Prior art keywords
alkyl
optionally containing
heteroatoms selected
aryl
well
Prior art date
Application number
BRPI0114704A
Other languages
English (en)
Other versions
BRPI0114704B1 (pt
BR0114704A (pt
Inventor
Kawai Akiyoshi
Taniguchi Kana
Shinjyo Katsuhiro
Nakao Kazunari
Matsumizu Miyako
Uneo Naomi
Nukui Seiji
Kato Tomoki
Miyake Yoriko
Hashizume Yoshinobu
Okumura Yoshiyuki
Original Assignee
Askat Inc
Pfizer
Raqualia Pharma Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Askat Inc, Pfizer, Raqualia Pharma Inc filed Critical Askat Inc
Publication of BR0114704A publication Critical patent/BR0114704A/pt
Publication of BRPI0114704B1 publication Critical patent/BRPI0114704B1/pt
Publication of BRPI0114704B8 publication Critical patent/BRPI0114704B8/pt

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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
    • C07D213/60—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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Abstract

"compostos de imidazol fundidos a arila ou heteroarila como agentes antiinflamatórios e analgésicos". esta invenção proporciona um composto com a fórmula (i): ou os seus sais farmaceuticamente aceitáveis, em que y^ 1^, y^ 2^, y^ 3^ e y^ 4^ sejam selecionados independentemente de entre n, ch, etc.; r^ 1^ seja alquila c~ 1-8~, etc.; q^ 1^ seja um anel monocíclico ou bicíclico aromático com 512 membros, contendo opcionalmente até 4 heteroátomos selecionados de entre o, n e s, etc.; a seja um anel monocíclico aromático com 5-6 membros, contendo opcionalmente até 3 heteroátomos selecionados de entre o,n e s, etc.; b seja um alquileno c~ 1-6~ opcionalmente substituído com um grupo oxo, etc.; w seja nh, o, etc.;r^ 2^ seja h, alquila c~ 1-4~, etc.; z seja um anel monocíclico ou bicíclico aromático com 5-12 membros, contendo opcionalmente até 3 heteroátomos selecionados de entre o, n e s, etc.; l seja halo, alquila c~ 1-4~, etc.; m seja 0, 1 ou 2; r^ 3^ e r^ 4^ sejam selecionados independentemente de entre h e alquila c^ 1-4^; r^ 5^ seja h, alquila c~ 1-4~, etc.; q^ 2^ seja um anel monocíclico ou bicíclico aromático com 5-12 membros, contendo opcionalmente até 3 heteroátomos selecionados de entre o, n e s, etc. estes compostos são úteis para o tratamento médico de condições mediados por prostaglandina, tais como algias, febre ou inflamação, etc. esta invenção também refere-se a uma composição farmacêutica incluindo o composto acima.
BRPI0114704A 2000-10-19 2001-10-15 composto de imidazol fundido a arila ou heteroarila, suas composições farmacêuticas, bem como seu uso BRPI0114704B8 (pt)

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PCT/IB2001/001940 WO2002032900A2 (en) 2000-10-19 2001-10-15 Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents

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Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2003087061A1 (en) * 2002-04-12 2003-10-23 Pfizer Japan Inc. Pyrazole compounds as anti-inflammatory and analgesic agents
BR0309305A (pt) 2002-04-12 2005-02-15 Pfizer Compostos de imidazol como agentes antiinflamatórios e analgésicos
AU2003214525B2 (en) 2002-04-12 2008-09-25 Pfizer Inc. Use of EP4 receptor ligands in the treatment of IL-6 involved diseases
EP1576134B1 (en) 2002-12-09 2013-03-06 Judith Kelleher-Andersson Method for discovering neurogenic agents
US8293488B2 (en) 2002-12-09 2012-10-23 Neuralstem, Inc. Method for screening neurogenic agents
WO2004058168A2 (en) * 2002-12-20 2004-07-15 Dynogen Pharmaceuticals, Inc. METHODS OF TREATING NON-PAINFUL BLADDER DISORDERS USING α2δ SUBUNIT CALCIUM CHANNEL MODULATORS
US7618914B2 (en) * 2003-02-14 2009-11-17 Wako Pure Chemical Industries, Ltd. Method for producing hydroxylamine compound using platinum catalyst fixed on ion-exchange resin
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
WO2005013902A2 (en) * 2003-08-04 2005-02-17 Mayo Foundation For Medical Education And Research Methods and compositions for inhibiting the proliferation of prostate cancer cells
FR2860514A1 (fr) 2003-10-03 2005-04-08 Sanofi Synthelabo Derives d'arylalkylcarbamates, leur preparation et leur application en therapeutique
JP4495168B2 (ja) * 2003-12-23 2010-06-30 エフ．ホフマン−ラ ロシュ アーゲー 抗ｃｃｐおよびインターロイキン６の測定による慢性関節リウマチの評価方法
US20090036495A1 (en) * 2004-04-20 2009-02-05 Pfizer, Inc. Combinations Comprising Alpha-2-Delta Ligands and Ep4 Receptor Antagonists
US7271271B2 (en) * 2004-06-28 2007-09-18 Amgen Sf, Llc Imidazolo-related compounds, compositions and methods for their use
KR101429284B1 (ko) 2004-11-17 2014-08-11 뉴럴스템, 인크. 신경퇴행성 증상의 치료를 위한 인간 신경 세포의 이식
US7442716B2 (en) * 2004-12-17 2008-10-28 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
CA2591724C (en) * 2004-12-17 2014-08-05 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1h-phenantrho[9,10-d]imidazoles as mpges-1 inhibitors
US7960407B2 (en) * 2005-03-11 2011-06-14 Requalia Pharma Inc. Crystal forms of an imidazole derivative
WO2007073405A1 (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 METHODS FOR TREATING OR PREVENTING 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.
CA2681146A1 (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
CA2698075C (en) 2007-08-27 2016-04-12 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
WO2010034110A1 (en) * 2008-09-25 2010-04-01 Merck Frosst Canada Ltd. Beta-carboline sulphonylurea derivatives as ep4 receptor antagonists
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
CA2754702C (en) 2009-04-22 2016-06-07 Yukinori Take Selective ep4 antagonistic substance for treatment of cancer
KR101041561B1 (ko) * 2009-12-21 2011-06-15 짚라인코리아 (주) 비행용 착용복
CA2789665C (en) * 2010-02-22 2020-06-16 Raqualia Pharma Inc. Use of ep4 receptor antagonists in the treatment of il-23 mediated diseases
MY168084A (en) 2010-07-28 2018-10-11 Neuralstem Inc Methods for treating and/or reversing neurodegenerative diseases and/or disorders
RU2606510C2 (ru) 2010-09-21 2017-01-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Фармацевтическая композиция
WO2012102254A1 (ja) * 2011-01-25 2012-08-02 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
CN107496421A (zh) * 2013-03-19 2017-12-22 株式会社ＡｓｋＡｔ Ep4受体拮抗剂在软骨疾病的治疗中的用途
WO2014153280A1 (en) * 2013-03-22 2014-09-25 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
ES2704232T3 (es) * 2013-08-29 2019-03-15 Kyoto Pharma Ind Compuesto aromático y uso del mismo en el tratamiento de trastornos asociados con el metabolismo óseo
TW201607943A (zh) 2013-12-19 2016-03-01 拜耳製藥公司 作為ｅｐ４配體之新穎苯并咪唑衍生物
CA2941008C (en) * 2014-03-06 2022-07-26 Aratana Therapeutics, Inc. Compositions of grapiprant and methods for using the same
CN107501263A (zh) 2014-03-06 2017-12-22 阿莱塔纳治疗学股份有限公司 Grapiprant的结晶形式
MX2017005186A (es) 2014-10-20 2017-07-26 Neuralstem Inc Celulas madre neurales estables que comprenden un polinucleótido exógeno que codifica un factor de crecimiento y métodos de uso de las mismas.
PL3319959T3 (pl) 2015-07-06 2022-02-14 Alkermes, Inc. Hetero-haloinhibitory deacetylazy histonowej
US10421756B2 (en) 2015-07-06 2019-09-24 Rodin Therapeutics, Inc. Heterobicyclic N-aminophenyl-amides as inhibitors of histone deacetylase
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
CN105486851A (zh) * 2015-11-20 2016-04-13 中国药科大学 一种基于荧光共振能量转移技术的前列腺素受体4筛选模型
US10342785B2 (en) 2016-11-04 2019-07-09 Askat Inc. Use of EP4 receptor antagonists for the treatment of NASH-associated liver cancer
JP6756925B2 (ja) 2017-01-11 2020-09-16 ロダン・セラピューティクス，インコーポレーテッド ヒストンデアセチラーゼの二環式阻害剤
WO2018162562A1 (en) 2017-03-10 2018-09-13 Bayer Pharma Aktiengesellschaft Use of an ep4 antagonist for the treatment of inflammatory pain
ES2929309T3 (es) 2017-05-18 2022-11-28 Idorsia Pharmaceuticals Ltd Derivados de benzofurano y benzotiofeno como moduladores del receptor PGE2
PL3625222T3 (pl) 2017-05-18 2021-12-27 Idorsia Pharmaceuticals Ltd Pochodne fenylu jako modulatory receptora pge2
CN110612299A (zh) 2017-05-18 2019-12-24 爱杜西亚药品有限公司 作为pge2受体调节剂的嘧啶衍生物
AR111874A1 (es) 2017-05-18 2019-08-28 Idorsia Pharmaceuticals Ltd Derivados de pirimidina
ES2894124T3 (es) 2017-05-18 2022-02-11 Idorsia Pharmaceuticals Ltd Derivados de indol N-sustituidos
JP7152471B2 (ja) 2017-08-07 2022-10-12 ロダン・セラピューティクス，インコーポレーテッド ヒストン脱アセチル化酵素の二環阻害剤
WO2019038156A1 (en) 2017-08-22 2019-02-28 Bayer Pharma Aktiengesellschaft USE OF AN EP4 ANTAGONIST FOR THE TREATMENT OF ARTHRITIS
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
AU2019255196A1 (en) 2018-04-16 2020-11-12 Arrys Therapeutics, Inc. EP4 inhibitors and use thereof
US10239885B1 (en) 2018-06-18 2019-03-26 Avista Pharma Solutions, Inc. Compound 1-[2-[4-(2-ethyl-6,8-dimethylimidazo[1,2-α]pyrazin-3-yl)phenyl]ethyl]-3-(p-tolylsulfonyl)urea as a prostaglandin EP4 receptor antagonist
WO2020014465A1 (en) * 2018-07-11 2020-01-16 Arrys Therapeutics, Inc. Polymorphic compounds and uses thereof
EP3820469A4 (en) * 2018-07-11 2022-04-13 Arrys Therapeutics, Inc. EP4 INHIBITORS AND USE THEREOF
EP4364798A2 (en) 2018-10-05 2024-05-08 Annapurna Bio Inc. Compounds and compositions for treating conditions associated with apj receptor activity
EP3917932A4 (en) 2019-01-30 2022-09-28 Avista Pharma Solutions, Inc. CHEMICAL COMPOUNDS
EP3917935A4 (en) 2019-01-30 2022-11-16 Avista Pharma Solutions, Inc. SYNTHESIS PROCESS AND NEW 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
WO2021226162A1 (en) 2020-05-05 2021-11-11 Arrys Therapeutics, Inc. Ep4 antagonists and their use in the treatment of proliferative diseases
EP4245301A1 (en) 2020-11-13 2023-09-20 ONO Pharmaceutical Co., Ltd. Cancer treatment by combined use of ep4 antagonist and immune checkpoint inhibitor

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8804439D0 (en) * 1988-02-25 1988-03-23 Pfizer Ltd Dihydropyridines
IL94805A (en) * 1989-06-28 1994-04-12 Ciba Geigy Ag Certain translocated carboxylic acids (a) Arylsulfonamide - and pyridyl - or imidazolil (), process for their preparation and pharmaceutical preparations containing them
GB9009469D0 (en) * 1990-04-27 1990-06-20 British Bio Technology Compounds
GB9010404D0 (en) * 1990-05-09 1990-06-27 Pfizer Ltd Therapeutic agents
GB2330307A (en) * 1998-02-07 1999-04-21 Glaxo Group Ltd EP4 Receptor antagonists as bone resorption inhibitors
EP1071648A2 (en) * 1998-03-13 2001-01-31 Merck Frosst Canada & Co. Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment
EP1148877A4 (en) 1998-10-15 2003-01-22 Merck & Co Inc METHOD FOR INHIBITING BONE RESORPTION
EP1121133A1 (en) * 1998-10-15 2001-08-08 Merck & Co., Inc. Methods for stimulating bone formation
JP2000191615A (ja) * 1998-10-20 2000-07-11 Takeda Chem Ind Ltd 芳香族アミン誘導体、その製造法および剤
DK1183245T3 (da) 1999-04-22 2007-09-24 Lundbeck & Co As H Selektive NPY(Y5)-antagonister
HUP0201291A3 (en) 1999-04-28 2002-11-28 Sanofi Aventis Deutschland Di-aryl acid derivatives as ppar receptor ligands and pharmaceutical compositions containing them
GB0031302D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Napthalene derivatives
GB0031315D0 (en) 2000-12-21 2001-02-07 Glaxo Group Ltd Indole derivatives
GB0031295D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Naphthalene derivatives

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