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1. 发明授权

EP1165085B1 PHTHALAZINE DERIVATIVES FOR TREATING INFLAMMATORY DISEASES 有权
标题翻译：酞炎症性疾病的治疗
公开(公告)号：EP1165085B1
公开(公告)日：2006-06-14
申请号：EP00920604.6
申请日：2000-03-28
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BOLD, Guido , DAWSON KING, Janet , FREI, Jörg , HENG, Richard , MANLEY, Paul, William , WIETFELD, Bernhard , WOOD, Jeanette, Marjorie
IPC分类号： A61K31/50 , C07D401/06 , C07D401/12 , C07D401/14 , C07D471/04 , A61P29/00 , A61P19/02
CPC分类号： C07D401/06 , A61K31/501 , A61K31/502 , C07D401/14
摘要： The invention relates to the treatment of an inflammatory disease, and/or pain with an inhibitor of VEGF receptor tyrosine kinase of formula (I), wherein r is 0 to 2, n is 0 to 3, R1 and R2 a) are independently in each case 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-, -CH2-S-, -CH2-NH-, -CH2-O-CH2-, -CH2-S-CH2-, -CH2-NH-CH2-, oxa (-O-), thia (-S-), imino (-NH-), -CH2-O-CH2-, -CH2-S-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.

2. 发明公开

EP1326857A2 DIAZACYCLOALKANEDIONE DERIVATIVES WHICH ARE USEFUL AS LFA-1 ANTAGONISTS 审中-公开
标题翻译： DIAZACYCLOALKANDIONE，作为LFA-1拮抗剂能有效
公开(公告)号：EP1326857A2
公开(公告)日：2003-07-16
申请号：EP01980462.4
申请日：2001-10-01
申请人： Novartis AG , Novartis Pharma GmbH
发明人： ALBERT, Rainer , DAWSON KING, Janet , EHRHARDT, Claus , WATTANASIN, Sompong , WEITZ SCHMIDT, Gabriele , WELZENBACH, Karl
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , A61K31/4965 , A61K31/551 , C07D241/08 , C07D243/08 , C07D401/12
摘要： Compounds of formula (I) wherein R is carboxy, esterified carboxy or amidated carboxy; R1 and R3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di- lower alkylamino or mercapto)-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, cycloalkyl, aryl, biaryl, (cycloalkyl, aryl or biaryl)-lower alkyl, or (carboxy, esterified carboxy or amidated carboxy)-lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, arylaminocarbonyl, or aryl-(oxy, thio or amino); n is 1 or 2; Y is lower-alkylene or lower alkenylene; and pharmaceutically acceptable salts thereof; which are useful as LFA-1 antagonists.

3. 发明申请

WO2008071771A2 INHIBITION OF GPR4 审中-公开
标题翻译： GPR4的抑制
公开(公告)号：WO2008071771A2
公开(公告)日：2008-06-19
申请号：PCT/EP2007/063899
申请日：2007-12-13
申请人： NOVARTIS AG , SEUWEN, Klaus , BILLY, Eric , SUPLY, Thomas , WYDER, Lorenza , DAWSON KING, Janet , LUDWIG, Marie-Gabrielle , MUELLER, Matthias , NATH, Puneeta , JONES, Carol Elizabeth
发明人： SEUWEN, Klaus , BILLY, Eric , SUPLY, Thomas , WYDER, Lorenza , DAWSON KING, Janet , LUDWIG, Marie-Gabrielle , MUELLER, Matthias , NATH, Puneeta , JONES, Carol Elizabeth
IPC分类号： C12N15/11 , A61K48/00 , A01K67/027
CPC分类号： C12N15/1138 , A01K67/0275 , A01K2217/075 , A01K2227/105 , A01K2267/03 , C07K14/723 , C12N15/8509 , C12N2310/14 , G01N2333/726
摘要： The present invention relates to the use of a GPR4 inhibitor for the manufacture of a medicament for the inhibition of angiogenesis, for instance for the inhibition of tumour growth in the treatment of cancer. In a preferred embodiment, said inhibitor is a siRNA, preferably double-stranded. In addition, the present invention further encompasses non-human animals wherein the GPR4 has been inactivated, for instance a knock-out mouse lacking GPR4, and the use of said animals as an experimental model for angiogenesis and for screening for compounds modulating angiogenesis.
摘要翻译：本发明涉及GPR4抑制剂在制备用于抑制血管生成的药物中的用途，例如用于抑制癌症治疗中的肿瘤生长。在优选的实施方案中，所述抑制剂是siRNA，优选双链。此外，本发明还包括其中GPR4已被灭活的非人动物，例如缺乏GPR4的敲除小鼠，以及所述动物用作血管发生的实验模型并用于筛选调节血管生成的化合物。

4. 发明申请

WO2015198240A2 COMPOSITIONS AND METHODS FOR LONG ACTING PROTEINS 审中-公开
标题翻译：长期作用蛋白的组成和方法
公开(公告)号：WO2015198240A2
公开(公告)日：2015-12-30
申请号：PCT/IB2015/054737
申请日：2015-06-24
申请人： NOVARTIS AG , DAWSON KING, Janet , GHOSH, Joy , NUESSLEIN-HILDESHEIM, Barbara
发明人： DAWSON KING, Janet , GHOSH, Joy , NUESSLEIN-HILDESHEIM, Barbara
IPC分类号： C07K14/47
CPC分类号： C07K14/525 , C07K16/241 , C07K2317/72 , C07K2319/33
摘要： The present invention provides peptide tags that can be linked to a therapeutic molecule in order to decrease the clearance of the therapeutic molecule from the synovial joint, thereby increasing its intra-articular half-life.
摘要翻译：本发明提供了可以与治疗分子连接的肽标签，以便降低治疗分子与滑膜关节的清除率，从而增加其关节内半衰期。

5. 发明申请

WO2007096150A3 ORGANIC COMPOUNDS 审中-公开
公开(公告)号：WO2007096150A3
公开(公告)日：2007-08-30
申请号：PCT/EP2007/001507
申请日：2007-02-21
申请人： NOVARTIS AG , BOLLINGER, Pietro , PRASHAD, Mahavir , RISS, Bernhard , DAWSON KING, Janet , HIESTAND, Peter, C. , LIU, Yugang , KING, Jonathan , SCHMID, Vincent , SCHUERCH, Friedrich
发明人： BOLLINGER, Pietro , PRASHAD, Mahavir , RISS, Bernhard , DAWSON KING, Janet , HIESTAND, Peter, C. , LIU, Yugang , KING, Jonathan , SCHMID, Vincent , SCHUERCH, Friedrich
IPC分类号： C07D495/04
摘要： The present invention relates to novel aza-thia-benzoazulene derivatives of formula I as defined in the claims, their preparation, the use of these novel compounds for the preparation of pharmaceutical compositions, the use of these novel compounds and compositions for managing arthritis and arthritis-related conditions as well as in the treatment of pain in animals and humans. More particularly, the present invention relates to pharmaceutical, preferably veterinary compositions and methods for reducing inflammation and pain associated with acute inflammation of body parts, particularly joints, due to injury or due to arthritic conditions or other disease conditions.

6. 发明公开

EP2094847A2 INHIBITION OF GPR4 审中-公开
标题翻译： GPR 4抑制
公开(公告)号：EP2094847A2
公开(公告)日：2009-09-02
申请号：EP07857546.1
申请日：2007-12-13
申请人： Novartis AG
发明人： SEUWEN, Klaus , BILLY, Eric , SUPLY, Thomas , WYDER, Lorenza , DAWSON KING, Janet , LUDWIG, Marie-Gabrielle , MUELLER, Matthias , NATH, Puneeta , JONES, Carol Elizabeth
IPC分类号： C12N15/11 , A61K48/00 , A01K67/027
CPC分类号： C12N15/1138 , A01K67/0275 , A01K2217/075 , A01K2227/105 , A01K2267/03 , C07K14/723 , C12N15/8509 , C12N2310/14 , G01N2333/726
摘要： The present invention relates to the use of a GPR4 inhibitor for the manufacture of a medicament for the inhibition of angiogenesis, for instance for the inhibition of tumour growth in the treatment of cancer. In a preferred embodiment, said inhibitor is a siRNA, preferably double-stranded. In addition, the present invention further encompasses non-human animals wherein the GPR4 has been inactivated, for instance a knock-out mouse lacking GPR4, and the use of said animals as an experimental model for angiogenesis and for screening for compounds modulating angiogenesis.

7. 发明公开

EP1989209A2 ORGANIC COMPOUNDS 有权
标题翻译：氮杂 - 硫杂benzazulene衍生物及其药物用途dered
公开(公告)号：EP1989209A2
公开(公告)日：2008-11-12
申请号：EP07722883.1
申请日：2007-02-21
申请人： NOVARTIS AG
发明人： BOLLINGER, Pietro , PRASHAD, Mahavir , RISS, Bernhard , DAWSON KING, Janet , HIESTAND, Peter, C. , LIU, Yugang , KING, Jonathan , SCHMID, Vincent , SCHUERCH, Friedrich
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to novel aza-thia-benzoazulene derivatives of formula I as defined in the claims, their preparation, the use of these novel compounds for the preparation of pharmaceutical compositions, the use of these novel compounds and compositions for managing arthritis and arthritis-related conditions as well as in the treatment of pain in animals and humans. More particularly, the present invention relates to pharmaceutical, preferably veterinary compositions and methods for reducing inflammation and pain associated with acute inflammation of body parts, particularly joints, due to injury or due to arthritic conditions or other disease conditions.

8. 发明公开

EP3160991A2 COMPOSITIONS AND METHODS FOR LONG ACTING PROTEINS 审中-公开
标题翻译：用于长效蛋白质的组合物和方法
公开(公告)号：EP3160991A2
公开(公告)日：2017-05-03
申请号：EP15745554.4
申请日：2015-06-24
申请人： Novartis AG
发明人： DAWSON KING, Janet , GHOSH, Joy , NUESSLEIN-HILDESHEIM, Barbara
IPC分类号： C07K14/47
CPC分类号： C07K14/525 , C07K16/241 , C07K2317/72 , C07K2319/33
摘要： The present invention provides peptide tags that can be linked to a therapeutic molecule in order to decrease the clearance of the therapeutic molecule from the synovial joint, thereby increasing its intra-articular half-life.
摘要翻译：本发明提供了可与治疗性分子连接的肽标签，以降低治疗性分子从滑液关节的清除率，由此增加其关节内半衰期。

9. 发明公开

EP1165085A1 PHTHALAZINE DERIVATIVES FOR TREATING INFLAMMATORY DISEASES 有权
标题翻译：酞炎症性疾病的治疗
公开(公告)号：EP1165085A1
公开(公告)日：2002-01-02
申请号：EP00920604.6
申请日：2000-03-28
申请人： Novartis AG , Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
发明人： BOLD, Guido , DAWSON KING, Janet , FREI, Jörg , HENG, Richard , MANLEY, Paul, William , WIETFELD, Bernhard , WOOD, Jeanette, Marjorie
IPC分类号： A61K31/50 , C07D401/06 , C07D401/12 , C07D401/14 , C07D471/04 , A61P29/00 , A61P19/02
CPC分类号： C07D401/06 , A61K31/501 , A61K31/502 , C07D401/14
摘要： The invention relates to the treatment of an inflammatory disease, and/or pain with an inhibitor of VEGF receptor tyrosine kinase of formula (I), wherein r is 0 to 2, n is 0 to 3, R1 and R2 a) are independently in each case 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-, -CH2-S-, -CH2-NH-, -CH2-O-CH2-, -CH2-S-CH2-, -CH2-NH-CH2-, oxa (-O-), thia (-S-), imino (-NH-), -CH2-O-CH2-, -CH2-S-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.

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