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1. 发明授权

US07645760B2 1-(4-Benzyl-piperazin-1-yl)-3-phenyl-propenone derivatives 失效
标题翻译： 1-（4-苄基 - 哌嗪-1-基）-3-苯基 - 丙烯酮衍生物
公开(公告)号：US07645760B2
公开(公告)日：2010-01-12
申请号：US10532331
申请日：2003-10-24
申请人： Birgit Bollbuck , Jorg Eder , Richard Heng , Laszio Revesz , Achim Schlapbach , Rudolf Walchli
发明人： Birgit Bollbuck , Jorg Eder , Richard Heng , Laszio Revesz , Achim Schlapbach , Rudolf Walchli
IPC分类号： C07D241/10 , C07D295/027 , A61K31/4965
CPC分类号： C07D295/185 , C07D207/14 , C07D207/16 , C07D207/28 , C07D211/48 , C07D211/58 , C07D215/38 , C07D233/74
摘要： A compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein the symbols have meaning as defined, which are antagonists of CCR-1 and which find use pharmaceutically for treatment of diseases and conditions in which CCR-1 is implicated, e.g. inflammatory diseases.
摘要翻译：式（I）化合物或其药学上可接受的盐或酯，其中符号具有如上所定义的含义，其是CCR-1的拮抗剂，其可用于治疗CCR-1涉及的疾病和病症的药学上可用，例如炎性疾病。

2. 发明申请

US20090169558A1 BICYCLIC AROMATIC COMPOUNDS USEFUL AS INHIBITORS OF MITOGEN-ACTIVATED PROTEIN KINASE-ACTIVATED PROTEIN KINASE-2 审中-公开
标题翻译：作为活化蛋白激活蛋白激酶蛋白激酶-2的抑制剂的双相芳族化合物有用
公开(公告)号：US20090169558A1
公开(公告)日：2009-07-02
申请号：US12089335
申请日：2006-10-04
申请人： Richard Heng , Guido Koch , Achim Schlapbach , Juraj Velcicky , Rudolf Wälchli
发明人： Richard Heng , Guido Koch , Achim Schlapbach , Juraj Velcicky , Rudolf Wälchli
IPC分类号： A61K31/519 , C07D487/04 , A61K31/52 , A61K39/395
CPC分类号： C07D487/04 , C07D513/04
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1-R6, A and Y are as defined in the specification.
摘要翻译：式（I）化合物或其药学上可接受的盐或前药酯：其中基团R 1 -R 6，A和Y如说明书中所定义。

3. 发明授权

US09233111B2 Pyrrolo pyrimidine derivatives 有权
标题翻译：吡咯并嘧啶衍生物
公开(公告)号：US09233111B2
公开(公告)日：2016-01-12
申请号：US14130536
申请日：2012-07-07
申请人： Richard Heng , Elizabeth Kate Hoegenauer , Guido Koch , Robert Alexander Pulz , Anna Vulpetti , Rudolf Waelchli
发明人： Richard Heng , Elizabeth Kate Hoegenauer , Guido Koch , Robert Alexander Pulz , Anna Vulpetti , Rudolf Waelchli
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： A61K31/519 , C07D487/04
摘要： The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
摘要翻译：本发明描述了与布鲁顿酪氨酸激酶（Btk）相互作用的新的吡咯并嘧啶衍生物及其药学上可接受的盐。因此，新的吡咯并嘧啶可能有效治疗自身免疫疾病，炎性疾病，过敏性疾病，气道疾病如哮喘和慢性阻塞性肺疾病（COPD），移植排斥反应，癌症。的造血起源或实体瘤。

4. 发明授权

US07329660B2 Phthalazine derivatives for treating inflammatory diseases 失效
标题翻译：用于治疗炎性疾病的酞嗪衍生物
公开(公告)号：US07329660B2
公开(公告)日：2008-02-12
申请号：US11441961
申请日：2006-05-26
申请人： Guido Bold , Janet D King , Joerg Frei , Richard Heng , Paul W Manley , Bernhard Wietfeld , Jeanette M Wood
发明人： Guido Bold , Janet D King , Joerg Frei , Richard Heng , Paul W Manley , Bernhard Wietfeld , Jeanette M Wood
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495
CPC分类号： C07D401/06 , A61K31/501 , A61K31/502 , C07D401/14
摘要： The invention relates to the treatment of leukemias with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.
摘要翻译：本发明涉及用式I的VEGF受体酪氨酸激酶的活性抑制剂治疗白血病，所述取代基在说明书中定义; 以及新的酞嗪衍生物; 制备方法; 其用于治疗人或动物体的过程中的应用; 其用于治疗疾病，特别是由眼睛新生血管形成引起的疾病，例如年龄相关性黄斑变性或糖尿病性视网膜病，或其它对酪氨酸激酶（例如增殖性疾病）的抑制作用的疾病; 哺乳动物治疗这种疾病的方法; 以及这种化合物用于制造特别是上述疾病的药物制剂的用途。

5. 发明申请

US20070196270A1 Compounds As Ccri Antagonists 审中-公开
标题翻译：化合物作为Ccri拮抗剂
公开(公告)号：US20070196270A1
公开(公告)日：2007-08-23
申请号：US10599819
申请日：2005-04-25
申请人： Richard Heng , Laszlo Revesz , Achim Schlapbach , Rudolf Walchli
发明人： Richard Heng , Laszlo Revesz , Achim Schlapbach , Rudolf Walchli
IPC分类号： A61K51/00 , C07D471/02 , A61K31/495 , A61K31/4745 , A61K31/407
CPC分类号： C07D451/14 , C07D451/04 , C07D487/08
摘要： A compound of formula I, or a pharmaceutically acceptable salt or ester thereof, wherein the symbols have meaning as defined, which are antagonists of CCR-1 and which find use pharmaceutically for treatment of diseases and conditions in which CCR-1 is implicated, e.g. inflammatory diseases.
摘要翻译：式I化合物或其药学上可接受的盐或酯，其中符号具有如上所定义的含义，其是CCR-1的拮抗剂，其可用于治疗CCR-1涉及的疾病和病症的药学上可用的药物。炎性疾病。

6. 发明申请

US20060173004A1 1-(4-Benzyl-piperazin-1-yl)-3-phenyl-propenone derivatives 失效
标题翻译： 1-（4-苄基 - 哌嗪-1-基）-3-苯基 - 丙烯酮衍生物
公开(公告)号：US20060173004A1
公开(公告)日：2006-08-03
申请号：US10532331
申请日：2003-10-24
申请人： Birgit Bollbuck , Jorg Eder , Richard Heng , Laszlo Revesz , Achim Schlapbach , Rudolf Walchli
发明人： Birgit Bollbuck , Jorg Eder , Richard Heng , Laszlo Revesz , Achim Schlapbach , Rudolf Walchli
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/497 , C07D413/02 , C07D403/02
CPC分类号： C07D295/185 , C07D207/14 , C07D207/16 , C07D207/28 , C07D211/48 , C07D211/58 , C07D215/38 , C07D233/74
摘要： A compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein the symbols have meaning as defined, which are antagonists of CCR-1 and which find use pharmaceutically for treatment of diseases and conditions in which CCR-1 is implicated, e.g. inflammatory diseases.
摘要翻译：式（I）化合物或其药学上可接受的盐或酯，其中符号具有如上所定义的含义，其是CCR-1的拮抗剂，其可用于治疗CCR-1涉及的疾病和病症，例如炎性疾病。

7. 发明申请

US20140243306A1 NOVEL PYRROLO PYRIMIDINE DERIVATIVES 有权
标题翻译：新型吡咯啉吡啶衍生物
公开(公告)号：US20140243306A1
公开(公告)日：2014-08-28
申请号：US14130536
申请日：2012-07-07
申请人： Richard Heng , Elizabeth Kate Hoegenauer , Guido Koch , Robert Alexander Pulz , Anna Vulpetti , Rudolf Waelchli
发明人： Richard Heng , Elizabeth Kate Hoegenauer , Guido Koch , Robert Alexander Pulz , Anna Vulpetti , Rudolf Waelchli
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： A61K31/519 , C07D487/04
摘要： The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
摘要翻译：本发明描述了与布鲁顿酪氨酸激酶（Btk）相互作用的新的吡咯并嘧啶衍生物及其药学上可接受的盐。因此，新的吡咯并嘧啶可能有效治疗自身免疫疾病，炎性疾病，过敏性疾病，气道疾病如哮喘和慢性阻塞性肺疾病（COPD），移植排斥反应，癌症。的造血起源或实体瘤。

8. 发明授权

US06686347B2 Phthalazine derivatives for treating inflammatory diseases 失效
标题翻译：用于治疗炎性疾病的酞嗪衍生物
公开(公告)号：US06686347B2
公开(公告)日：2004-02-03
申请号：US09964025
申请日：2001-09-26
申请人： Guido Bold , Janet Dawson King , Jörg Frei , Richard Heng , Paul William Manley , Bernhard Wietfeld , Jeanette Marjorie Wood
发明人： Guido Bold , Janet Dawson King , Jörg Frei , Richard Heng , Paul William Manley , Bernhard Wietfeld , Jeanette Marjorie Wood
IPC分类号： A61K3133
CPC分类号： C07D401/06 , A61K31/501 , A61K31/502 , C07D401/14
摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.
摘要翻译：本发明涉及治疗炎症性疾病，特别是炎性类风湿病或风湿性疾病，和/或具有式I的VEGF受体酪氨酸激酶的活性抑制剂的疼痛，所述取代基在本说明书中定义;以及新的酞嗪衍生物; 制备方法; 其用于治疗人或动物体的过程中的应用; 其用于治疗疾病，特别是由眼睛新生血管形成引起的疾病，例如年龄相关性黄斑变性或糖尿病性视网膜病，或其它对酪氨酸激酶（例如增殖性疾病）的抑制作用的疾病; 哺乳动物治疗这种疾病的方法; 以及这种化合物用于制造特别是上述疾病的药物制剂的用途。

9. 发明申请

US20050176711A1 Phthalazine derivatives for treating inflammatory diseases 审中-公开
公开(公告)号：US20050176711A1
公开(公告)日：2005-08-11
申请号：US11099292
申请日：2005-04-05
申请人： Guido Bold , Janet King , Joerg Frei , Richard Heng , Paul Manley , Bernhard Wietfeld , Jeanette Wood
发明人： Guido Bold , Janet King , Joerg Frei , Richard Heng , Paul Manley , Bernhard Wietfeld , Jeanette Wood
IPC分类号： A61K31/502 , A61K31/506 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/14 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/04 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P43/00 , C07D401/06 , C07D401/14 , A61K31/53 , A61K31/501 , C07D43/02
CPC分类号： C07D401/06 , A61K31/501 , A61K31/502 , C07D401/14
摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, wherein r is 0 to 2, n is 0 to 3 R1 and R2 a) are independently in each case a lower alkyl; b) together form a bridge of subformula I*, wherein the bond is achieved via the two terminal C atoms and m is 0 to 4, or c) together form a bridge of subformula I**, wherein one or two of the ring members T1, T2, T3 and T4 are nitrogen, and the others are in each case CH, and the bond is achieved via atoms T1 and T4; G is —C(═O)—, —CHF—, —CF2—, lower alkylene, C2-C6alkenylene, lower alkylene or C3-C6alkenylene substituted by acyloxy or hydroxy, —CH2—O—, —CH2S—, —CH2—NH—, —CH2—O—CH2—, —CH2—S—CH2—, —CH2—NH—CH2—, oxa (—O—), thia (—S—), imino (—NH—), —CH2—O—CH2—, —CH2S—CH2— or —CH2—NH—CH2—; A, B, D, E and T are independently N or CH subject to the proviso that at least one and not more than three of these radicals are N; Q is lower alkyl, lower alkoxy or halogen; Ra and Ra′ are each independently H or lower alkyl; X is imino, oxa, or thia; Y is hydrogen, aryl, heteroaryl, or unsubstituted or substituted cycloalkyl; and Z is mono- or disubstituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl phenylsulfonyl, phenyl-lower alkylsulfonyl, alkylphenylsulfonyl, or (alternatively or, in a broader aspect of the invention, in addition) selected from the group consisting of ureido, halo-lower alkylthio, halo-lower alkansulfonyl, pyrazolyl, lower-alkyl pyrazolyl and C2-C7alkenyl; wherein—if more than 1 radical Z (m≧2) is present—the substituents Z are selected independently from each other; and wherein the bonds characterized in subformula I* by a wavy line are either single or double bonds; or an N-oxide of said compound, wherein 1 or more N atoms carry an oxygen atom; or a pharmaceutically acceptable salt thereof; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularisation, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.

10. 发明授权

US06911440B2 Phthalazine derivatives for treating inflammatory diseases 失效
标题翻译：用于治疗炎性疾病的酞嗪衍生物
公开(公告)号：US06911440B2
公开(公告)日：2005-06-28
申请号：US10723238
申请日：2003-11-26
申请人： Guido Bold , Janet Dawson King , Jörg Frei , Richard Heng , Paul William Manley , Bernhard Wietfeld , Jeanette Marjorie Wood
发明人： Guido Bold , Janet Dawson King , Jörg Frei , Richard Heng , Paul William Manley , Bernhard Wietfeld , Jeanette Marjorie Wood
IPC分类号： A61K31/502 , A61K31/506 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/14 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/04 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P43/00 , C07D401/06 , C07D401/14 , A61K31/33 , A61K31/44 , C07D237/00 , C07D401/00 , C07D487/00
CPC分类号： C07D401/06 , A61K31/501 , A61K31/502 , C07D401/14
摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.
摘要翻译：本发明涉及治疗炎症性疾病，特别是炎性类风湿病或风湿性疾病，和/或具有式I的VEGF受体酪氨酸激酶的活性抑制剂的疼痛，该说明书中定义的取代基; 以及新的酞嗪衍生物; 其制备方法，其用于治疗人或动物体的方法中的应用; 其用于治疗疾病，特别是由眼睛新生血管形成引起的疾病，例如年龄相关性黄斑变性或糖尿病性视网膜病，或其它对酪氨酸激酶（例如增殖性疾病）的抑制作用的疾病的用途; 哺乳动物治疗这种疾病的方法; 以及这种化合物用于制造特别是上述疾病的药物制剂的用途。

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