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1. 发明申请

WO2009095399A2 NOVEL COMPOUNDS, USE AND PREPARATION THEREOF 审中-公开
标题翻译：新化合物，其使用和制备
公开(公告)号：WO2009095399A2
公开(公告)日：2009-08-06
申请号：PCT/EP2009/050931
申请日：2009-01-28
申请人： BIOVITRUM AB (publ) , JENMALM JENSEN, Annika , LEHMANN, Fredrik , NILSSON, Björn, M. , NORDLING, Erik , PARROW, Vendela
发明人： JENMALM JENSEN, Annika , LEHMANN, Fredrik , NILSSON, Björn, M. , NORDLING, Erik , PARROW, Vendela
IPC分类号： C07D241/20 , C07D401/04 , C07D401/14 , C07D403/12 , C07D417/14 , A61K31/497 , A61K31/4965 , A61K31/5415 , A61P35/00 , A61P17/00 , C07D407/14 , C07D409/14
CPC分类号： A61K31/497 , A61K31/4965 , C07D241/20 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I) wherein R 1 , R 2 and R 3 are as defined herein, which can act as inhibitors of protein kinases, specially the Fms-like tyrosine kinase 3 (FLT3). The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of hematological malignancies, such as AML, MLL, T-ALL, B-ALL and CMML, myeloproliferative disorders, other proliferative disorders like cancer, autoimmune disorders and skin disorders like psoriasis and atopic dermatitis.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1，R 2和R 3如本文所定义，其可以作为蛋白激酶的抑制剂，特别是Fms样酪氨酸激酶3（FLT3）。本发明还涉及该化合物在治疗中的用途，包含该化合物的药物组合物和该化合物在制备用于预防和治疗血液恶性肿瘤的药物中的用途，所述药物包括AML，MLL，T-ALL，B -ALL和CMML，骨髓增生性疾病，其他增殖性疾病如癌症，自身免疫性疾病和皮肤病，如牛皮癣和特应性皮炎。

2. 发明申请

WO2011113798A2 NEW ENZYME INHIBITOR COMPOUNDS 审中-公开
标题翻译：新型酶抑制剂化合物
公开(公告)号：WO2011113798A2
公开(公告)日：2011-09-22
申请号：PCT/EP2011053818
申请日：2011-03-14
申请人： PROXIMAGEN LTD , EVANS DAVID , CARLEY ALLISON , STEWART ALISON , HIGGINBOTTOM MICHAEL , SAVORY EDWARD , SIMPSON IAIN , NILSSON MARIANNE , HARALDSSON MARTIN , NORDLING ERIK , KOOLMEISTER TOBIAS
发明人： EVANS DAVID , CARLEY ALLISON , STEWART ALISON , HIGGINBOTTOM MICHAEL , SAVORY EDWARD , SIMPSON IAIN , NILSSON MARIANNE , HARALDSSON MARTIN , NORDLING ERIK , KOOLMEISTER TOBIAS
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04 , C07D491/08 , C07D498/08 , C07D519/00
摘要： Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase wherein R1, A, X and R2 are as defined in the claims.
摘要翻译：式（I）化合物是氨基脲敏感性胺氧化酶的抑制剂，其中R1，A，X和R2如权利要求中所定义。

3. 发明申请

WO2013037411A1 NEW ENZYME INHIBITOR COMPOUNDS 审中-公开
标题翻译：新型酶抑制剂化合物
公开(公告)号：WO2013037411A1
公开(公告)日：2013-03-21
申请号：PCT/EP2011/065967
申请日：2011-09-14
申请人： PROXIMAGEN LIMITED , EVANS, David , CARLEY, Allison , STEWART, Alison , HIGGINBOTTOM, Michael , SAVORY, Edward , SIMPSON, Iain , NILSSON, Marianne , HARALDSSON, Martin , NORDLING, Erik , KOOLMEISTER, Tobias
发明人： EVANS, David , CARLEY, Allison , STEWART, Alison , HIGGINBOTTOM, Michael , SAVORY, Edward , SIMPSON, Iain , NILSSON, Marianne , HARALDSSON, Martin , NORDLING, Erik , KOOLMEISTER, Tobias
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3- aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4- (dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3- yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H- pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1- [1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4- methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4- chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2- aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4 yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin- 4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin- 3-yl}methanol; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3- yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3- carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4- c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4- c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4- ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4- (fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4- chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.
摘要翻译： 2- {4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}乙-1-胺; 4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酸3-氨基丙酯; 1- {4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基} -4-（二甲基氨基）丁-1-酮; 5-氨基-1- {4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}戊-1-酮; N-（2-氨基乙基）-4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酰胺; N-（3-氨基丙基）-4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酰胺; 4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基] -N- [3-（二甲基氨基）丙基]哌啶-1-甲酰胺; 1 - （{4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基）哌嗪; 4 - （{4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基）吗啉; 1 - （{4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基）-1,4-二氮杂环庚烷; 1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸乙酯; 1- [1-（4-甲基苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸乙酯; 1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸; N-（2-氨基乙基）-1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酰胺; 4 - （{1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-基}羰基）吗啉; 1 - （{1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-基}羰基）哌嗪; {4- [1-（4-甲基苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基}甲醇; {4- [1-（4-甲基苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-2-基}甲醇; [（3R）-4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基]甲醇; 4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-羧酸甲酯; N-（2-氨基乙基）-4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-甲酰胺; 2- {4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基}乙-1-醇; 1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-甲酸甲酯; N-（2-氨基乙基）-1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-甲酰胺; 1 - （{1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-基}羰基）哌嗪; 4- [1-（4-甲基苯基）-1H-吡咯并[2,3-c]吡啶-3-基]吗啉; 1-（4-氯苯基）-3-（哌啶-4-基）-1H-吡咯并[2,3-c]吡啶-4-醇; N-丁基-1-（4-氯苯基）-N-甲基-1H-吡唑并[3,4-c]吡啶-3-胺; 1- [4-（氟甲基）苯基] -3-（氧代-4-基）-1H-吡唑并[3,4-c]吡啶; 和3 - （{4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-1-基}甲基）吡啶可用于抑制SSAO活性。

4. 发明申请

WO2011113798A3 INHIBITORS OF SEMICARABAZIDE - SENSITIVE AMINE OXIDASE 审中-公开
公开(公告)号：WO2011113798A3
公开(公告)日：2011-09-22
申请号：PCT/EP2011/053818
申请日：2011-03-14
申请人： Proximagen Limited , EVANS, David , CARLEY, Allison , STEWART, Alison , HIGGINBOTTOM, Michael , SAVORY, Edward , SIMPSON, Iain , NILSSON, Marianne , HARALDSSON, Martin , NORDLING, Erik , KOOLMEISTER, Tobias
发明人： EVANS, David , CARLEY, Allison , STEWART, Alison , HIGGINBOTTOM, Michael , SAVORY, Edward , SIMPSON, Iain , NILSSON, Marianne , HARALDSSON, Martin , NORDLING, Erik , KOOLMEISTER, Tobias
IPC分类号： C07D471/04 , C07D487/04 , C07D498/08 , A61K31/437 , A61P35/00 , A61P37/06 , A61P11/08 , A61P25/28 , A61P9/10
摘要： Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase wherein R 1 , A, X and R 2 are as defined in the claims.

5. 发明申请

WO2009095399A3 PYRAZINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHBITORS 审中-公开
标题翻译：吡嗪衍生物及其作为蛋白激酶抑制剂的用途
公开(公告)号：WO2009095399A3
公开(公告)日：2009-10-01
申请号：PCT/EP2009050931
申请日：2009-01-28
申请人： AKINION PHARMACEUTICALS AB , JENMALM JENSEN ANNIKA , LEHMANN FREDRIK , NILSSON BJOERN M , NORDLING ERIK , PARROW VENDELA
发明人： JENMALM JENSEN ANNIKA , LEHMANN FREDRIK , NILSSON BJOERN M , NORDLING ERIK , PARROW VENDELA
IPC分类号： C07D241/20 , A61K31/4965 , A61K31/497 , A61K31/5415 , A61P17/00 , A61P35/00 , C07D401/04 , C07D401/14 , C07D403/12 , C07D407/14 , C07D409/14 , C07D417/14
CPC分类号： A61K31/497 , A61K31/4965 , C07D241/20 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I) wherein R1, R2 and R3 are as defined herein, which can act as inhibitors of protein kinases, specially the Fms-like tyrosine kinase 3 (FLT3). The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of hematological malignancies, such as AML, MLL, T-ALL, B-ALL and CMML, myeloproliferative disorders, other proliferative disorders like cancer, autoimmune disorders and skin disorders like psoriasis and atopic dermatitis.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1，R 2和R 3如本文所定义，其可以作为蛋白激酶的抑制剂，特别是Fms样酪氨酸激酶3（FLT3）。本发明还涉及该化合物在治疗中的用途，包含该化合物的药物组合物和该化合物在制备用于预防和治疗血液恶性肿瘤的药物中的用途，所述药物包括AML，MLL，T-ALL，B -ALL和CMML，骨髓增生性疾病，其他增殖性疾病如癌症，自身免疫性疾病和皮肤病，如牛皮癣和特应性皮炎。

6. 发明申请

WO2006067224A3 SPIRO-BENZODIOXOLE AND SPIRO-BENZODIOXANE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：螺旋胆固醇和螺旋胆固醇化合物作为OREXIN受体拮抗剂
公开(公告)号：WO2006067224A3
公开(公告)日：2006-11-02
申请号：PCT/EP2005057132
申请日：2005-12-22
申请人： BIOVITRUM AB , BARKER EMMA , JENMALM JENSEN ANNIKA , NORDLING ERIK , PROUD ANDREW , SLATER MARTIN , WEBER MIKAEL
发明人： BARKER EMMA , JENMALM JENSEN ANNIKA , NORDLING ERIK , PROUD ANDREW , SLATER MARTIN , WEBER MIKAEL
IPC分类号： C07D491/10 , A61K31/357 , A61K31/36 , A61K31/438 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , C07D493/10
CPC分类号： C07D491/10 , C07D493/10
摘要： The present invention relates to compounds of Formula (I): wherein R 1 , A, Y, n and m are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of orexin-1 receptor- related disorders and orexin-2 receptor-related disorders. Examples of such disorders are obesity and related disorders such as diabetes type II, dyslipidemia and the metabolic syndrome, cardiovascular diseases such as atherosclerotic vascular disease, angina pectoris, myocardial infarction and stroke, drug addiction, and sleeping disorders.
摘要翻译：本发明涉及式（I）化合物：其中R 1，A，Y，n和m如本文所述，制备化合物的方法，包含该化合物的药物组合物，以及使用预防或治疗食欲肽-1受体相关疾病和食欲肽-2受体相关疾病的化合物和组合物。这种障碍的实例是肥胖症和相关疾病，例如II型糖尿病，血脂异常和代谢综合征，心血管疾病如动脉粥样硬化血管疾病，心绞痛，心肌梗死和中风，药物成瘾和睡眠障碍。

7. 发明申请

WO2006067224A2 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2006067224A2
公开(公告)日：2006-06-29
申请号：PCT/EP2005/057132
申请日：2005-12-22
申请人： BIOVITRUM AB , BARKER, Emma , JENMALM JENSEN, Annika , NORDLING, Erik , PROUD, Andrew , SLATER, Martin , WEBER, Mikael
发明人： BARKER, Emma , JENMALM JENSEN, Annika , NORDLING, Erik , PROUD, Andrew , SLATER, Martin , WEBER, Mikael
CPC分类号： C07D491/10 , C07D493/10
摘要： The present invention relates to compounds of Formula (I): wherein R 1 , A, Y, n and m are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of orexin-1 receptor- related disorders and orexin-2 receptor-related disorders. Examples of such disorders are obesity and related disorders such as diabetes type II, dyslipidemia and the metabolic syndrome, cardiovascular diseases such as atherosclerotic vascular disease, angina pectoris, myocardial infarction and stroke, drug addiction, and sleeping disorders.
摘要翻译：本发明涉及式（I）化合物：其中R 1，A，Y，n和m如本文所述，制备化合物的方法，包含该化合物的药物组合物，以及使用预防或治疗食欲肽-1受体相关疾病和食欲素-2受体相关疾病的化合物和组合物。这种障碍的实例是肥胖症和相关疾病，例如II型糖尿病，血脂异常和代谢综合征，心血管疾病如动脉粥样硬化性血管疾病，心绞痛，心肌梗死和中风，药物成瘾和睡眠障碍。

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