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2. 发明专利

JP5300729B2 Their use as replacement dihydropyrazolone acids and hif- prolyl-4-hydroxylase inhibitor 有权
公开(公告)号：JP5300729B2
公开(公告)日：2013-09-25
申请号：JP2009533700
申请日：2007-10-17
申请人：バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH
发明人：カイ・テーデ , インゴ・フランメ , フェリックス・エーメ , イェンス−ケリム・エアギューデン , フリーデリケ・シュトール , ヨアヒム・シューマッハー , ハンノ・ヴィルト , ペーター・コルクホーフ , ハルトムート・ベック , メティン・アクババ , マリオ・イェスケ
IPC分类号： C07D401/14 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K31/616 , A61K31/7048 , A61K31/714 , A61K45/00 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P17/02 , A61P25/16 , A61P25/28 , A61P27/06 , A61P29/00 , A61P35/00 , A61P43/00 , C07D413/14 , C07D417/14 , C07D471/04
CPC分类号： C07D417/14 , C07D401/14
摘要： Substituted dihydropyrazolone derivatives (I) are new. Substituted dihydropyrazolone derivatives of formula (I) are new. R 1>heteroaryl compounds of formula (a) or (b); A : C-R 4> or N, where maximum two ring members of A are simultaneously N; E : C-R 5> or N, where maximum two ring members of E are simultaneously N; R 2>nitrogen containing heteroaryl-group of formula (c)-(o); a1, a2 : point of attachment with the dihydropyrazolthione ring; G : C-R 6> or N, where maximum two ring members of G are simultaneously N; J : O, S or N-R 7>; L : C-R 8> or N, where maximum two ring members of L are simultaneously N; M : C-R 9> or N, where maximum two ring members of M are simultaneously N; R 4>, R 6>, R 8>, R 9>H, halo, cyano, NO 2, (1-6C)-alkyl (substituted with 1-3 of T), (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5- or 6-membered heteroaryl (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of T 1>), -C(=O)-R 1> 0>, -C(=O)-OR 1> 1>, -C(=O)-NR 1> 2>R 1> 3>, -O-C(=O)-R 1> 4>, -O-C(=O)-NR 1> 5>R 1> 6>, -NR 1> 7>-C(=O)-R 1> 8>, -NR 1> 9>-C(=O)-OR 2> 0>, -NR 2> 1>-C(=O)-NR 2> 2>R 2> 3>, -NR 2> 4>-SO 2-R 2> 5>, -SO 2-R 2> 6>, -SO 2-NR 2> 7>R 2> 8>, -OR 2> 9>, -SR 3> 0> or -NR 3> 1>R 3> 2>; T : halo, CN, oxo, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5- or 6-membered heteroaryl, -C(=O)-R 1>0, -C(=O)-OR 1> 1>, -C(=O)-NR 1> 2>R 1> 3>, -O-C(=O)-R 1> 4>, -O-C(=O)-NR 1> 5>R 1> 6>, -NR 1> 7>-C(=O)-R 1> 8>, -NR 1> 9>-C(=O)-OR 2> 0>, -NR 2> 1>-C(=O)-NR 2> 2>R 2> 3>, -NR 2> 4>-SO 2-R 2> 5>, -SO 2-R 2> 6>, -SO 2-NR 2> 7>R 2> 8>, -OR 2> 9>, -SR 3> 0> or -NR 3> 1>R 3> 2>, where the cycloalkyl-, heterocycloalkyl-, phenyl- and heteroaryl are substituted by 1-3 of halo, CN, (1-4C)-alkyl, trifluoromethyl, OH, (1-4C)-alkoxy, trifluoromethoxy, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl and/or (1-4C)-alkoxycarbonyl; T 1>(1-6C)-alkyl, halo, CN, oxo, -C(=O)-R 1> 0>, -C(=O)-OR 1> 1>, -C(=O)-NR 1> 2>R 1> 3>, -O-C(=O)-R 1> 4>, -O-C(=O)-NR 1> 5>R 1> 6>, -NR 1> 7>-C(=O)-R 1> 8>, -NR 1> 9>-C(=O)-OR 2> 0>, -NR 2> 1>-C(=O)-NR 2> 2>R 2> 3>, -NR 2> 4>-SO 2-R 2> 5>, -SO 2-R 2> 6>, -SO 2-NR 2> 7>R 2> 8>, -OR 2> 9>, -SR 3> 0> or -NR 3> 1>R 3> 2>, where the alkyl is substituted with 1-3 of halo, CN, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl, (1-4C)-alkoxycarbonyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5- or 6-membered heteroaryl; either R 1> 0>-R 1> 2>, R 1> 4>, R 1> 5>, R 1> 8>, R 2> 0>, R 2> 2>, R 2> 5>-R 2> 7>, R 2> 9>-R 3> 1>H, (1-6C)-alkyl (substituted with 1-3 of halo, cyano, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl, (1-4C)-alkoxycarbonyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5- or 6-membered heteroaryl), (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5- or 6-membered heteroaryl (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of halo, cyano, (1-4C)-alkyl, trifluoromethyl, OH, (1-4C)-alkoxy, trifluoromethoxy, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl or (1-4C)-alkoxycarbonyl); and R 1> 3>, R 1> 6>, R 1> 7>, R 1> 9>, R 2> 1>, R 2> 3>, R 2> 4>, R 2> 8>, R 3> 2>H or (1-6C)-alkyl, which is optionally substituted with halo, CN, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl or (1-4C)-alkoxycarbonyl; or R 1> 2>R 1> 3>, R 1> 5>R 1> 6>, R 1> 7>R 1> 8>, R 1> 9>R 2> 0>, R 2> 1>R 2> 2>, R 2> 2>R 2> 3>, R 2> 4>R 2> 5>, R 2> 7>R 2> 8>, R 3> 1>R 3> 2>5- or 6-membered heterocycloalkyl ring; R 5>H, halo, CN, nitro, (1-6C)-alkyl, trifluoromethyl, OH, (1-6C)-alkoxy, trifluoromethoxy, amino, mono-(1-6C)-alkylamino, di-(1-6C)-alkylamino, hydroxycarbonyl or (1-6C)-alkoxycarbonyl; R 7>H, (1-6C)-alkyl (substituted with 1-3 of T) , (3-7C)-cycloalkyl, 4-7 membered (hetero)cycloalkyl, phenyl, or 5- or 6-membered heteroaryl (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of T 1>); and R 3>H, (1-6C)-alkyl or (3-7C)-cycloalkyl. Independent claims are included for: (1) the preparations of (I); and (2) a medicament comprising (I) and an inert, non-toxic auxiliary material. [Image] [Image] [Image] [Image] [Image] - ACTIVITY : Cardiovascular-Gen; Cardiant; Antianemic; Nephrotropic; Antianginal; Cerebroprotective; Vasotropic; Antiarteriosclerotic; Hypotensive; Respiratory-Gen; Antiarthritic; Antirheumatic; Ophthalmological; Antiparkinsonian; Neuroprotective; Nootropic; Analgesic; Vulnerary; Anabolic; Endocrine-Gen; Antidiabetic; Antimicrobial; Antiinflammatory. - MECHANISM OF ACTION : Hypoxia-inducible transcription factor (HIF)-prolyl-4-hydroxylase inhibitor. The ability of (I) to inhibit the activity of HIF-prolyl-4-hydroxylase was tested in in-vitro using the method described in Oehme F., Jonghaus W., Narouz-Ott L., Huetter J., Flamme I., Anal. Biochem. 330 (1), 74-80 (2004). The results showed that (I) exhibited an IC 5 0 value of = 30 mu M.

3. 发明专利

JP5306999B2 5-aryl-substituted dihydro pyridopyrimidine acids and dihydropyridazine acids and their use as mineralocorticoid antagonist 有权
公开(公告)号：JP5306999B2
公开(公告)日：2013-10-02
申请号：JP2009513573
申请日：2007-05-25
申请人：バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH
发明人：サンティアゴ・フィゲロア・ペレス , ペーター・コルクホーフ , ラース・ベルファッカー , インゴ・フランメ , カール−ハインツ・シュレンマー , アレクサンダー・クール , ロルフ・グロッサー , クラウス・ミュンター , アンドレアス・クノール
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present application relates to novel aryl- or heteroaryl-substitued pyrido[2,3-d] pyrimidines of formula (I), pharmaceuitical compositions of the same, and a process for their preparation. Formula(I) is: wherein Ar is an aryl or heteroaryl substituent, and R1, R2, R3, Ar, D, and E are as defined in the specification. Compounds and compositions of the present invention can be used in the treatment and/or prophylaxis of various disorders in humans and animals, including aldosteronism, high blood pressure, chronic heart failure, the sequelae of a myocardial infarction, cirrhosis of the liver, renal failure, and stroke.

4. 发明专利

JP2013520470A Bisaryl - bonded aryl triazolone and its applications 有权
公开(公告)号：JP2013520470A
公开(公告)日：2013-06-06
申请号：JP2012554345
申请日：2011-02-25
申请人：バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH
发明人：シャンタル・フュルストナー , イェルク・ケルデニッヒ , マルティナ・デルベック , ペーター・コルクホーフ , アクセル・クレッチュマー , インゴ・プルシュケル , エリザベート・ポーク , カルステン・シュメック , フーベルト・トリューベル
IPC分类号： C07D249/12 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K45/00 , A61P1/16 , A61P9/00 , A61P9/04 , A61P35/00 , A61P43/00 , C07D401/06 , C07D403/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06
CPC分类号： A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K45/06 , C07D249/12 , C07D401/06 , C07D403/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06
摘要：本出願は、新規なビスアリール-結合5-アリール-1,2,4-トリアゾロン誘導体、それらの製造方法、それらの単独又は組合せでの疾患の処置及び/又は予防のための使用及びまたそれらの疾患の処置及び/又は予防、より具体的には心血管疾患の処置及び/又は予防のための医薬の製造のための使用に関する。

5. 发明专利

JP5367586B2 Substituted 4-aryl-1,4-dihydro-1,6-naphthyridine amides and their use 有权
公开(公告)号：JP5367586B2
公开(公告)日：2013-12-11
申请号：JP2009550238
申请日：2008-02-19
申请人：バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH
发明人：ラルス・ベルファッカー , ペーター・コルクホーフ , カール−ハインツ・シュレンマー , ロルフ・グロッサー , アダム・ニーチェ , マルティナ・クライン , クラウス・ミュンター , バルバラ・アルブレヒト−キュッパー , エルケ・ハルトマン
IPC分类号： C07D471/04 , A61K31/4375 , A61K45/00 , A61P1/16 , A61P5/42 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12
CPC分类号： C07D471/04
摘要： 1,6-Naphthyridine or 8-azaquinazoline derivatives (I) are new. 1,6-Naphthyridine or 8-azaquinazoline derivatives of formula (I) are new. D : N or CR 4>; R 4>H, F, CF 3 or 1-4C alkyl; Ar : 5-R 5>-6-R 6>-2-methyl-4-oxo-4H-1-benz opyran-8-yl; 3-R 6>-4-R 8>-1-naphthyl optionally substituted with 1-3 of R 7>; 7-R 6>-8-R 8>-5-quinolinyl optionally substituted with 1-2 of R 7>; or 2-R 9>-3-R 10>-4-R 8>-5-R 6>-phenyl; R 5>H, F, Cl, CN, NO 2, CF 3 or 1-4C alkyl; R 6>H or F; R 7>halo, 1-4C alkyl, CF 3, 1-4C alkoxy or OCF 3; R 8>CN or NO 2; R 9>H or halo; optionally fluorinated 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio of di(1-4C alkyl)amino; or phenyl optionally substituted with halo, 1-4C alkyl or CF 3; R 10>H, halo or 1-4C alkyl; R 1>optionally fluorinated 1-4C alkyl; R 2>1-6C alkyl optionally substituted with 3-7C cycloalkyl or F; or SO 2R 11>; R 11>1-6C alkyl, CF 3 or 3-7C cycloalkyl; or phenyl or heteroaryl optionally substituted with 1-2 of halo, CN, 1-4C alkyl, CF 3, 1-4C alkoxy and/or OCF 3; R 3>H, F, CF 3 or 1-4C alkyl. An independent claim is also included for a process for preparing (I). [Image] - ACTIVITY : Hypotensive; Cardiant; Hepatotropic; Nephrotropic; Cerebroprotective. - MECHANISM OF ACTION : Mineralocorticoid receptor (MR) antagonist. 4-(4-cyano-2-methoxypheny l)-5-ethoxy-2-methyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide had an IC 50 of 35 nM when tested on cells expressing a GAL4-MR chimera.

6. 发明专利

JP5307709B2 Substituted 4-aryl-1,4-dihydro-1,6-naphthyridines and their use 有权
公开(公告)号：JP5307709B2
公开(公告)日：2013-10-02
申请号：JP2009513580
申请日：2007-06-01
申请人：バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH
发明人：サンティアゴ・フィゲロア・ペレス , ペーター・コルクホーフ , ラース・ベルファッカー , インゴ・フランメ , カール−ハインツ・シュレンマー , ロルフ・グロッサー , クラウス・ミュンター , アンドレアス・クノール , アダム・ニーチェ
IPC分类号： C07D471/04 , A61K31/4375 , A61K45/00 , A61P1/16 , A61P3/12 , A61P9/10 , A61P9/12 , A61P13/12
CPC分类号： C07D471/04
摘要： The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridines, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.

7. 发明专利

JP2013537209A Substituted phenyl acetamide and phenylpropanamide and the use of them 有权
公开(公告)号：JP2013537209A
公开(公告)日：2013-09-30
申请号：JP2013528661
申请日：2011-09-14
申请人：バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH
发明人：シャンタル・ヒュルストナー , イェルク・ケルデニッヒ , マルティナ・デルベック , ペーター・コルクホーフ , アクセル・クレッチュマー , エリザベート・ポーク , カルステン・シュメック , フーベルト・トリューベル
IPC分类号： C07D249/12 , A61K31/4196 , A61K45/00 , A61P1/16 , A61P3/14 , A61P9/04 , A61P13/02 , A61P43/00 , C07D409/04
CPC分类号： A61K31/4196 , A61K45/06 , C07D249/12 , C07D409/04
摘要： The present application relates to novel substituted phenylacetamides and phenylpropanamides, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.

8. 发明专利

JP5300813B2 Replacement dihydropyrazolone compounds for the treatment of cardiovascular and blood diseases 有权
公开(公告)号：JP5300813B2
公开(公告)日：2013-09-25
申请号：JP2010229627
申请日：2010-10-12
申请人：バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH
发明人：カイ・テーデ , インゴ・フランメ , フェリックス・エーメ , イェンス−ケリム・エアギューデン , フリーデリケ・シュトール , ヨアヒム・シューマッハー , ハンノ・ヴィルト , ペーター・コルクホーフ , ハルトムート・ベック , イェルク・ケルデニッヒ , メティン・アクババ , マリオ・イェスケ
IPC分类号： C07D401/14 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K45/00 , A61P7/06 , A61P9/00 , A61P9/04 , A61P13/12 , C07D403/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/08 , C07D487/04
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K45/06 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Pyrazol-3-one compounds (I) and their salts, solvates and solvate of the salts, are new, where (I) excludes 3-methyl-1-(pyridin-2-yl)-4-(1 -pyridin-2-yl-3-methyl-1H-pyrazol-5-yl)-2H-3-pyrazolin-5(1H)-one. Pyrazol-3-one compounds of formula (I) and their salts, solvates and solvate of the salts, are new, where (I) excludes 3-methyl-1-(pyridin-2-yl)-4-(1-pyridin-2-yl-3-methyl-1H-pyrazol-5-yl) -2H-3-pyrazolin-5(1H)-one. R 1>nitrogen containing aryl group of formula (a)-(d); A : C-R 4> or N, where maximum two ring members of A are simultaneously N; E : O, S or N-R 5>; R 2>nitrogen containing heteroaryl-group of formula (e)-(q); a1, a2 : point of attachment with the dihydropyrazolone ring; G : C-R 6> or N, where maximum two ring members of G are simultaneously N; J : O, S or N-R 7>; L : C-R 8> or N, where maximum two ring members of L are simultaneously N; R 4>, R 6>, R 8>H, halo, cyano, NO 2, (1-6C)-alkyl (substituted with 1-3 of T), (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5- or 6-membered heteroaryl (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of T 1>), -C(=O)-R 9>, -C(=O)-R 1> 0>, -C(=O)-NR 1> 1>R 1> 2>, -O-C(=O)-R 1> 3>, -O-C(=O)-NR 1> 4>R 1> 5>, -NR 1> 6>-C(=O)-R 1> 7>, -NR 1> 8>-C(=O)-OR 1> 9>, -NR 2> 0>-C(=O)-NR 2> 1>R 2> 2>, -NR 2> 3>-SO 2-R 2> 4>, -SO 2-R 2> 5>, -SO 2-NR 2> 6>R 2> 7>, -OR 2> 8>, -SR 2> 9> or -NR 3> 0>R 3> 1>; T : halo, CN, oxo, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5- or 6-membered heteroaryl, -C(=O)-R 9>, -C(=O)-OR 1> 0>, -C(=O)-NR 1> 1>R 1> 2>, -O-C(=O)-R 1> 3>, -O-C(=O)-NR 1> 4>R 1> 5>, -NR 1> 6>-C(=O)-R 1> 7>, -NR 1> 8>-C(=O)-OR 1> 9>, -NR 2> 0>-C(=O)-NR 2> 1>R 2> 2>, -NR 2> 3>-SO 2-R 2> 4>, -SO 2-R 2> 5>, -SO 2-NR 2> 6>R 2> 7>, -OR 2> 8>, -SR 2> 9> or -NR 3> 0>R 3> 1>, where the cycloalkyl-, heterocycloalkyl-, phenyl- and heteroaryl are substituted by 1-3 of halo, CN, (1-4C)-alkyl, trifluoromethyl, OH, (1-4C)-alkoxy, trifluoromethoxy, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl and/or (1-4C)-alkoxycarbonyl; T 1>(1-6C)-alkyl, halo, CN, oxo, -C(=O)-R 9>, -C(=O)-OR 1> 0>, -C(=O)-NR 1> 1>R 1> 2>, -O-C(=O)-R 1> 3>, -O-C(=O)-NR 1> 4>R 1> 5> -NR 1> 6>-C(=O)-R 1> 7>, -NR 1> 8>-C(=O)-OR 1> 9>, -NR 2> 0>-C(=O)-NR 2> 1>R 2> 2>, -NR 2> 3>-SO 2-R 2> 4>, -SO 2-R 2> 5>, -SO 2-NR 2> 6>R 2> 7>, -OR 2> 8>, -SR 2> 9> or -NR 3> 0>R 3> 1>, where the alkyl is substituted with 1-3 of halo, CN, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl, (1-4C)-alkoxycarbonyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5- or 6-membered heteroaryl; either R 9>-R 1> 1>, R 1> 3>, R 1> 4>, R 1> 7>, R 1> 9>, R 2> 1>, R 2> 4>, R 2> 5>, R 2> 6>, R 2> 8>-R 3> 0>H, (1-6C)-alkyl (substituted with 1-3 of halo, cyano, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl, (1-4C)-alkoxycarbonyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5- or 6-membered heteroaryl), (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of halo, cyano, (1-4C)-alkyl, trifluoromethyl, OH, (1-4C)-alkoxy, trifluoromethoxy, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl or (1-4C)-alkoxycarbonyl); and R 1> 2>, R 1> 5>, R 1> 6>, R 1> 8>, R 2> 0>, R 2> 2>, R 2> 3>, R 2> 7>, R 3> 1>H or (1-6C)-alkyl, which is optionally substituted with halo, CN, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl or (1-4C)-alkoxycarbonyl; or R 1> 1>R 1> 2>, R 1> 4>R 1> 5>, R 1> 6>R 1> 7>, R 1> 8>R 1> 9>, R 2> 0>R 2> 1>, R 2> 1>R 2> 2>, R 2> 3>R 2> 4>, R 2> 6>R 2> 7>, R 3> 0>R 3> 1>5- or 6-membered heterocycloalkyl ring; R 5>, R 7>H, (1-6C)-alkyl (substituted by T), (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl and 5- or 6-membered heteroaryl (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of T 1>); and R 3>H, (1-6C)-alkyl or (3-7C)-cycloalkyl. Independent claims are included for: (1) preparations of (I); and (2) a medicament comprising (I) and inert, non-toxic auxiliary material. [Image] [Image] [Image] [Image] - ACTIVITY : Cardiant; Antianemic; Nephrotropic; Antianginal; Cerebroprotective; Vasotropic; Antiarteriosclerotic; Hypotensive; Dermatological; Antimicrobial; Antiinflammatory; Gastrointestinal-Gen; Antiarthritic; Antirheumatic; Ophthalmological; Antiparkinsonian; Neuroprotective; Nootropic; Analgesic; Vulnerary; Anabolic; Endocrine-Gen; Antidiabetic. - MECHANISM OF ACTION : Hypoxia-inducible transcription factor (HIF)-prolyl-4-hydroxylase inhibitor.

9. 发明专利

JP5247712B2 Replacement dihydropyrazolone compounds for the treatment of cardiovascular and blood diseases 有权
公开(公告)号：JP5247712B2
公开(公告)日：2013-07-24
申请号：JP2009533691
申请日：2007-10-12
申请人：バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH
发明人：カイ・テーデ , インゴ・フランメ , フェリックス・エーメ , イェンス−ケリム・エアギューデン , フリーデリケ・シュトール , ヨアヒム・シューマッハー , ハンノ・ヴィルト , ペーター・コルクホーフ , ハルトムート・ベック , イェルク・ケルデニッヒ , メティン・アクババ , マリオ・イェスケ
IPC分类号： C07D401/14 , A61K31/197 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/525 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/616 , A61K31/7068 , A61K33/24 , A61K36/18 , A61K45/00 , A61P7/06 , A61P9/00 , A61P9/04 , A61P13/12 , C07D403/14 , C07D417/14 , C07D451/04 , C07D471/04
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K45/06 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Pyrazol-3-one compounds (I) and their salts, solvates and solvate of the salts, are new, where (I) excludes 3-methyl-1-(pyridin-2-yl)-4-(1 -pyridin-2-yl-3-methyl-1H-pyrazol-5-yl)-2H-3-pyrazolin-5(1H)-one. Pyrazol-3-one compounds of formula (I) and their salts, solvates and solvate of the salts, are new, where (I) excludes 3-methyl-1-(pyridin-2-yl)-4-(1-pyridin-2-yl-3-methyl-1H-pyrazol-5-yl) -2H-3-pyrazolin-5(1H)-one. R 1>nitrogen containing aryl group of formula (a)-(d); A : C-R 4> or N, where maximum two ring members of A are simultaneously N; E : O, S or N-R 5>; R 2>nitrogen containing heteroaryl-group of formula (e)-(q); a1, a2 : point of attachment with the dihydropyrazolone ring; G : C-R 6> or N, where maximum two ring members of G are simultaneously N; J : O, S or N-R 7>; L : C-R 8> or N, where maximum two ring members of L are simultaneously N; R 4>, R 6>, R 8>H, halo, cyano, NO 2, (1-6C)-alkyl (substituted with 1-3 of T), (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5- or 6-membered heteroaryl (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of T 1>), -C(=O)-R 9>, -C(=O)-R 1> 0>, -C(=O)-NR 1> 1>R 1> 2>, -O-C(=O)-R 1> 3>, -O-C(=O)-NR 1> 4>R 1> 5>, -NR 1> 6>-C(=O)-R 1> 7>, -NR 1> 8>-C(=O)-OR 1> 9>, -NR 2> 0>-C(=O)-NR 2> 1>R 2> 2>, -NR 2> 3>-SO 2-R 2> 4>, -SO 2-R 2> 5>, -SO 2-NR 2> 6>R 2> 7>, -OR 2> 8>, -SR 2> 9> or -NR 3> 0>R 3> 1>; T : halo, CN, oxo, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl, 5- or 6-membered heteroaryl, -C(=O)-R 9>, -C(=O)-OR 1> 0>, -C(=O)-NR 1> 1>R 1> 2>, -O-C(=O)-R 1> 3>, -O-C(=O)-NR 1> 4>R 1> 5>, -NR 1> 6>-C(=O)-R 1> 7>, -NR 1> 8>-C(=O)-OR 1> 9>, -NR 2> 0>-C(=O)-NR 2> 1>R 2> 2>, -NR 2> 3>-SO 2-R 2> 4>, -SO 2-R 2> 5>, -SO 2-NR 2> 6>R 2> 7>, -OR 2> 8>, -SR 2> 9> or -NR 3> 0>R 3> 1>, where the cycloalkyl-, heterocycloalkyl-, phenyl- and heteroaryl are substituted by 1-3 of halo, CN, (1-4C)-alkyl, trifluoromethyl, OH, (1-4C)-alkoxy, trifluoromethoxy, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl and/or (1-4C)-alkoxycarbonyl; T 1>(1-6C)-alkyl, halo, CN, oxo, -C(=O)-R 9>, -C(=O)-OR 1> 0>, -C(=O)-NR 1> 1>R 1> 2>, -O-C(=O)-R 1> 3>, -O-C(=O)-NR 1> 4>R 1> 5> -NR 1> 6>-C(=O)-R 1> 7>, -NR 1> 8>-C(=O)-OR 1> 9>, -NR 2> 0>-C(=O)-NR 2> 1>R 2> 2>, -NR 2> 3>-SO 2-R 2> 4>, -SO 2-R 2> 5>, -SO 2-NR 2> 6>R 2> 7>, -OR 2> 8>, -SR 2> 9> or -NR 3> 0>R 3> 1>, where the alkyl is substituted with 1-3 of halo, CN, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl, (1-4C)-alkoxycarbonyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5- or 6-membered heteroaryl; either R 9>-R 1> 1>, R 1> 3>, R 1> 4>, R 1> 7>, R 1> 9>, R 2> 1>, R 2> 4>, R 2> 5>, R 2> 6>, R 2> 8>-R 3> 0>H, (1-6C)-alkyl (substituted with 1-3 of halo, cyano, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl, (1-4C)-alkoxycarbonyl, (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl or 5- or 6-membered heteroaryl), (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of halo, cyano, (1-4C)-alkyl, trifluoromethyl, OH, (1-4C)-alkoxy, trifluoromethoxy, oxo, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl or (1-4C)-alkoxycarbonyl); and R 1> 2>, R 1> 5>, R 1> 6>, R 1> 8>, R 2> 0>, R 2> 2>, R 2> 3>, R 2> 7>, R 3> 1>H or (1-6C)-alkyl, which is optionally substituted with halo, CN, OH, trifluoromethoxy, (1-4C)-alkoxy, amino, mono-(1-4C)-alkylamino, di-(1-4C)-alkylamino, hydroxycarbonyl or (1-4C)-alkoxycarbonyl; or R 1> 1>R 1> 2>, R 1> 4>R 1> 5>, R 1> 6>R 1> 7>, R 1> 8>R 1> 9>, R 2> 0>R 2> 1>, R 2> 1>R 2> 2>, R 2> 3>R 2> 4>, R 2> 6>R 2> 7>, R 3> 0>R 3> 1>5- or 6-membered heterocycloalkyl ring; R 5>, R 7>H, (1-6C)-alkyl (substituted by T), (3-7C)-cycloalkyl, 4-7-membered heterocycloalkyl, phenyl and 5- or 6-membered heteroaryl (where the (hetero)cycloalkyl, phenyl and heteroaryl are substituted with 1-3 of T 1>); and R 3>H, (1-6C)-alkyl or (3-7C)-cycloalkyl. Independent claims are included for: (1) preparations of (I); and (2) a medicament comprising (I) and inert, non-toxic auxiliary material. [Image] [Image] [Image] [Image] - ACTIVITY : Cardiant; Antianemic; Nephrotropic; Antianginal; Cerebroprotective; Vasotropic; Antiarteriosclerotic; Hypotensive; Dermatological; Antimicrobial; Antiinflammatory; Gastrointestinal-Gen; Antiarthritic; Antirheumatic; Ophthalmological; Antiparkinsonian; Neuroprotective; Nootropic; Analgesic; Vulnerary; Anabolic; Endocrine-Gen; Antidiabetic. - MECHANISM OF ACTION : Hypoxia-inducible transcription factor (HIF)-prolyl-4-hydroxylase inhibitor.

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