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2. 发明专利

ES2453950T3 4-(4-Piridinil)-benzamidas y su uso como moduladores de la actividad de ROCK 未知
公开(公告)号：ES2453950T3
公开(公告)日：2014-04-09
申请号：ES08787483
申请日：2008-08-26
申请人： ABBOTT GMBH & CO KG , ABBOTT LAB , ABBVIE DEUTSCHLAND , ABBVIE INC
发明人： MACK HELMUT , TEUSCH NICOLE , MÜLLER BERNHARD K , HORNBERGER WILFRIED , JARVIS MICHAEL F , SAUER DARYL , SWANN STEVE JR , HOBSON ADRIAN DONALD , KEDDY RYAN , BONAFOUX DOMINIQUE , VASUDEVAN ANIL
IPC分类号： C07D213/56 , A61K31/44 , A61K31/4427 , A61P9/00 , A61P25/00 , A61P29/00 , A61P35/00 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Un compuesto de la fórmula I:**Fórmula** donde: R1 y R2 son, independientemente uno del otro, hidrógeno, halógeno, hidroxi, ciano, alquilo C1-C8, haloalquilo C1- C8, alcoxi C1-C8 o haloalcoxi C1-C8; R3, R4, R9 y R6 son, independientemente uno del otro, hidrógeno, hidroxi, halógeno, ciano, alquilo C1-C8, haloalquilo C1-C8, alcoxi C1-C8, haloalcoxi C1-C8, amino, alquilamino C1-C8 o di-(alquil C1-C8)-amino; R7 es hidrógeno, alquilo C1-C8, haloalquilo C1-C8, arilo C6-C14 o arilo C6-C14-alquilo C1-C4; R8 es un grupo de la fórmula -X-W, donde X es un enlace sencillo, alquileno C1-C4 lineal o ramificado o alquileno C1-C4-O-, donde el grupo alquileno en los tres últimos radicales mencionados puede ser lineal o ramificado y puede estar parcial o totalmente halogenado y/o puede estar sustituido por un grupo hidroxilo y/o puede ser interrumpido por un átomo de oxígeno; y W es un radical cíclico seleccionado de fenilo, naftilo, antracenilo, fenantrenilo, indenilo, indanilo, dihidronaftilo, tetralinilo, indolilo, 2,3-dihidroindolilo, indoxililo, oxindolilo, indazolilo, 2,3-dihidroindazolilo, benzimidazolilo, 2,3-dihidrobenzimidazolilo, cumaronilo (benzo[b]furanilo), 2,3-dihidrobenzofuranilo, benzo- 1,3-dioxilo, benzo-1,4-dioxanilo, benzoxazolilo, 2,3-dihidrobenzoxazolilo, benzo[b]tienilo, 2,3- dihidrobenzotienilo, benzotiazolilo, 2,3-dihidrobenzotiazolilo, quinolinilo, isoquinolinilo, quinoxalinilo, quinazolinilo, cinnolinilo, cromenilo, cromenonilo, isocromenilo, cromanilo, cromanonilo, isocromanilo, acenaftenilo, dihidroacenaftenilo, fluorenilo, carbazolilo, dibenzofuranilo, dibenzotienilo, acridinilo, carbazinilo (acridanilo), fenazinilo, 9,10-dihidrofenazinilo, dibenzomorfolinilo (fenoxazinilo), dibenzotiomorfolinilo (fenotiazinilo), donde los últimos 42 radicales mencionados están unidos a través de la porción fenilo del sistema condensado al grupo X, un anillo heterocíclico de 5 o 6 miembros saturado, parcialmente insaturado o aromático que contiene como miembros de anillo 1, 2, 3 o 4 heteroátomos seleccionados entre O, S y N y opcionalmente 1 o 2 grupo carbonilos como miembros de anillo y un anillo heterocíclico de 5 o 6 miembros saturado, parcialmente insaturado o aromático que contiene como miembros de anillo 1 o 2 heteroátomos seleccionados entre O, S y N y opcionalmente 1 o 2 grupo carbonilos como miembros de anillo que está condensado con un anillo de fenilo y que está unido a través de una porción heterociclilo del sistema condensado al grupo X, donde los radicales anteriores pueden llevar 1, 2, 3, 4 o 5 sustituyentes R10.

3. 发明专利

CA2670368C NEUTRALIZING MONOCLONAL ANTIBODIES AGAINST THE NOGO-66 RECEPTOR (NGR) AND USES THEREOF 未知
公开(公告)号：CA2670368C
公开(公告)日：2018-05-29
申请号：CA2670368
申请日：2007-11-21
申请人： ABBOTT LAB , ABBOTT GMBH & CO KG
发明人： MEZLER MARIO , MOELLER ACHIM , MUELLER REINHOLD , MUELLER BERNHARD K , GHAYUR TARIQ , BARLOW EVE H , SCHMIDT MARTIN , MEYER AXEL , TEUSCH NICOLE
IPC分类号： C07K16/28 , A61K39/395 , A61P25/00 , C07K14/705 , C12N5/16 , C12N15/13 , C12P21/08
摘要： The subject invention relates to isolated proteins, particularly monoclonal antibodies, which bind to the Nogo-66 receptor. Specifically, these antibodies have the ability to inhibit the binding of the natural ligand of the Nogo-66 receptor and neutralize the Nogo-66 receptor. These antibodies or portions thereof of the invention are useful for detecting NgR and for inhibiting NgR activity, for example in a human suffering from a disorder in which NgR or Nogo-66 activity is detrimental.

5. 发明专利

CA2689117A1 5-HETEROARYL SUBSTITUTED INDAZOLES AS KINASE INHIBITORS 未知
公开(公告)号：CA2689117A1
公开(公告)日：2008-12-18
申请号：CA2689117
申请日：2008-06-04
申请人： ABBOTT GMBH & CO KG , ABBOTT LAB
发明人： WAKEFIELD BRIAN D , AKRITOPOULOU-ZANZE IRINI , MACK HELMUT , FRANK KRISTINE , LI BIQIN , VASUDEVAN ANIL , HOBSON ADRIAN , LONG ANDREW J , DJURIC STEVAN W , KOVAR PETER J , JOHNSON ERIC T , TURNER SEAN C , GEORGE DAWN , GASIECKI ALAN F , WANG LU , ST JOHN MOORE NIGEL , MICHMERHUIZEN MELISSA J , GRACIAS VIJAYA J , SARRIS KATHY , KALVIN DOUGLAS M , SHUAI QI , PATEL JYOTI R , BAKKER MARGARETHA , TEUSCH NICOLE
IPC分类号： C07D403/04 , C07D413/04 , C07D417/04
摘要： The present invention relates to compounds of formula (I) or pharmaceutic al acceptable salts, wherein A, R1, R2, R3 and m, are defined in the descrip tion. The present invention relates also to methods of making said compounds , and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janu s Kinases (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

6. 发明专利

SG182187A1 5-HETEROARYL SUBSTITUTED INDAZOLES AS KINASE INHIBITORS 未知
公开(公告)号：SG182187A1
公开(公告)日：2012-07-30
申请号：SG2012043113
申请日：2008-06-04
申请人： ABBOTT GMBH & CO KG , ABBOTT LAB
发明人： AKRITOPOULOU-ZANZE IRINI , WAKEFIELD BRIAN D , MACK HELMUT , TURNER SEAN C , GASIECKI ALAN F , GRACIAS VIJAYA J , SARRIS KATHY , KALVIN DOUGLAS M , MICHMERHUIZEN MELISSA J , SHUAI QI , PATEL JYOTI R , BAKKER MARGARETHA , TEUSCH NICOLE , KOVAR PETER J , DJURIC STEVAN W , LONG ANDREW J , VASUDEVAN ANIL , HOBSON ADRIAN , ST JOHN MOORE NIGEL , WANG LU , GEORGE DAWN , LI BIQIN , FRANK KRISTINE , JOHNSON ERIC T
摘要： 5-HETEROARYL SUBSTITUTED INDAZOLES AS KINASE INHIBITORSAbstractThe present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein A, R1,R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Ala, PAK4, PLK, CK2, KDR, MK2, JNK I, aurora, pim I and nek 2.No suitable figure

7. 发明专利

CA2697382A1 4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS 未知
公开(公告)号：CA2697382A1
公开(公告)日：2009-03-05
申请号：CA2697382
申请日：2008-08-26
申请人： ABBOTT GMBH & CO KG , ABBOTT LAB
发明人： MACK HELMUT , TEUSCH NICOLE , MUELLER BERNHARD K , HORNBERGER WILFRIED , JARVIS MICHAEL F , SAUER DARYL , SWANN STEVE JR , BONAFOUX DOMINIQUE , KEDDY RYAN , HOBSON ADRIAN DONALD , VASUDEVAN ANIL
IPC分类号： C07D213/56 , A61K31/44 , A61K31/4427 , A61P9/00 , A61P25/00 , A61P29/00 , A61P35/00 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R1 and R2 are, independently of each other, hydrogen, hydroxy, cyano, C1-C8-alkyl, C1- C8-haloalkyl, C1-C8-alkoxy or C1-C8-haloalkoxy; R3, R4, R5 and R6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, amino, C1-C8-alkylamino or di-(C1-C8-alkyl)-amino; R7 is hydrogen, C1-C8-alkyl, C1-C8-haloalkyl, aryl or aryl-C1-C8-alkyl; R8 is a group of the formula -X-W, where X is a single bond, C1-C4-alkylene or C1-C4-alkylene-O-, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected from O, S and N and optionally 1 or 2 carbonyl groups; R9 is a group of the formula -Y-Z, where Z is hydrogen, halogen, OR11, NR12R13, S(O)m-R14, phenyl which may carry 1, 2, 3 or 4 substituents R15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C1C4-alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.

8. 发明申请

WO2006077101A3 AGER-PEPTIDES AND USE THEREOF 审中-公开
标题翻译： AGER肽及其用途
公开(公告)号：WO2006077101A3
公开(公告)日：2006-09-28
申请号：PCT/EP2006000420
申请日：2006-01-18
申请人： ABBOTT GMBH & CO KG , HAHN ALFRED , LOEBBERT RALPH , TEUSCH NICOLE , MOELLER ACHIM
发明人： HAHN ALFRED , LOEBBERT RALPH , TEUSCH NICOLE , MOELLER ACHIM
IPC分类号： A61K39/00 , C07K14/47 , C07K14/705 , C07K16/00
CPC分类号： C07K14/4748 , C07K14/705
摘要： The invention relates to the identification, functionality and use of domains of the N-terminus of the receptor for Advanced Glycation End Products (AGER). Said domains are highly conserved in all AGER protein sequences, with the designated receptor multimerisation epitop (RME). They represent mediators for the AGER automatic association and heteromerisation with other proteins. The invention also relates to the identification, functionality and use of peptides which are derived from the C-domains of AGER (AGER-CDP). The inventive AGER-RMEs and AGER-CDPs are suitable as targets for identifying AGER-ligands, which modulate natural ligand exchange effects as immunogens for the active or passive immunisation of individuals, as diagnostic means which are used to identify immunogenic reactions, and as peptide ligands which are used to modulate protein-protein-exchange effects involving AGER.
摘要翻译：本发明涉及鉴定，功能和使用域从受体晚期糖化终产物（AGER）的N末端。这些结构域，称为受体多聚表位（RME）是高度保守的所有AGER蛋白质序列。设置的介质是用于与其它蛋白质的自缔合和AGER heteromerization。本发明还涉及到识别，功能和使用从AGER（AGER-CDP）的C结构域衍生的肽。时效器-RME和本发明的AGER-个CDP适合作为用于识别AGER配体调节的天然配体相互作用的目标; 作为个人的主动或被动免疫的免疫原，作为用于免疫原性反应的识别诊断剂，以及用于涉及AGER蛋白质 - 蛋白质相互作用的调节的肽配体。

9. 发明专利

DE102005017799A1 Use of heparin- or heparin derivative to treat illness associated with neurite plasticity or -growth defects, modulates interaction between Nogo receptor and ligands 未知
公开(公告)号：DE102005017799A1
公开(公告)日：2006-10-19
申请号：DE102005017799
申请日：2005-04-18
申请人： ABBOTT GMBH & CO KG
发明人： MEZLER MARIO , HAHN ALFRED , TEUSCH NICOLE , MUELLER REINHOLD , MUELLER BERNHARD K , MOELLER ACHIM
IPC分类号： A61K38/00 , A61P25/00
摘要： The active, selected from heparins or heparin derivatives, modulates interaction between the Nogo receptor and its ligands AP-Nogo66. Blocking is effected using an IC50 value of 100 mu M. The active material induces a cell concentration with an IC50 value of about 100 mu M in an actin cytoskeletal conversion (ACR) test. The active modulates the growth of neurites with an IC50 value of at most about 1000 mu M, in neuronal cell culture. The molecular weight of the active is about 500 - 10000 Daltons. The active is Clivarin, Arixtra or Heparinoides, which includes di-, tetra- and hexa- saccharide fragments. The medicament contains one or more heparins or heparin derivatives, if appropriate in the form of physiologically-compatible salts or solvates, and if appropriate, one or more compatible carriers or excipients. The active exists in doseable form, i.e. for infusion or deposition. ACTIVITY : Neuroprotective; Neuroleptic; Anticonvulsant; Vulnerary; Cerebroprotective; Antiparkinsonian;Nootropic; Virucide; Antibacterial; Cytostatic. MECHANISM OF ACTION : Nogo modulator; Heparin agonist.

10. 发明专利

DE102005002353A1 Use of receptor multimerization epitope (RME) of advanced glycation end product receptor (AGER) as immunogen, useful for preparing antibodies for diagnosis and treatment of e.g. spinal injuries or diabetic complications 未知
公开(公告)号：DE102005002353A1
公开(公告)日：2006-07-27
申请号：DE102005002353
申请日：2005-01-18
申请人： ABBOTT GMBH & CO KG
发明人： HAHN ALFRED , LOEBBERT RALF , TEUSCH NICOLE , MOELLER ACHIM
IPC分类号： C07K7/64 , A61K38/04 , A61K39/395 , A61K48/00 , C07K14/705 , C07K16/28 , C07K19/00 , C12N5/12 , C12N15/63 , C12P21/08 , G01N33/68
摘要： Use of the receptor multimerization epitope (RME) of the advanced glycation end product receptor (AGER) as an immunogen for preparing polyclonal antiserum or monoclonal antibodies against AGER-RME or AGER-CDP (= immunoglobulin-like C-domain derived peptide of AGER). RME comprises (i) a peptide fragment from the N-terminal AGER-ectodomain, capable of automultimerization; (ii) AGER-CDP or (iii) functional, immunological equivalents of AGER-RME or AGER-CDP. Independent claims are included for the following: (1) use of AGER-RME or AGER-CDP for diagnosis of diseases, or disease stages, in which autoantibodies against AGER-RME or AGER-CDP appear; (2) polyclonal anti-(AGER-RME or AGER-CDP) antibodies obtained by immunizing a mammal with AGER-RME or AGER-CDP; (3) monoclonal anti-(AGER-RME or AGER-CDP) antibodies and their antigen-binding fragments, optionally humanized; (4) monoclonal bispecific antibodies comprising (i) antigen-binding domain of the antibodies of (3) and (ii) a second antigen-binding domain specific for either a cell-surface receptor that interacts with AGER-RME or AGER-CDP, or a ligand, co-receptor or counter receptor of such receptors, also their antigen-binding fragments, optionally humanized; (5) hybrid protein that contains AGER-RME and AGER-CDP; (6) derivatives of AGER-RME or AGER-CDP in pegylated form or coupled to a marker; (7) pharmaceutical composition that contains (i) AGER-RME or AGER-CDP, (ii) nucleic acid that encodes (i), or (iii) the mono- or poly-clonal antibodies, bispecific antibodies or their fragments of items (3) and (4); (8) immunogen comprising AGER-RME or AGER-CDP in a carrier, optionally including an adjuvant; (9) method for detecting effectors of AGER; (10) expression vector containing at least one nucleic acid encoding AGER-RME or AGER-CDP, operably linked to a regulatory sequence; (11) recombinant microorganisms that contain the vector of (10); (12) hybridoma cells that produce the monoclonal antibodies of (3) and (4); (13) method for preparing AGER-RME or AGER-CDP and the hybrid proteins of (5); (14) method for preparing the monoclonal antibodies of (3); (15) functional equivalents of AGRE having a degree of homology with sequence (6; 31 amino acids) of less than 100%; and (16) combination of at least two monoclonal antibodies with different antigenic specificities, where one binds to an epitope (partially) formed by the immunoglobulin-like V domain of AGER and another binds to an antigen present in a different region of AGER. ACTIVITY : Vasotropic; Neuroprotective; Antiinflammatory; Immunosuppressive; Cytostatic; Neuroleptic; Analgesic; Antiarteriosclerotic. No details of tests for these activities are given. MECHANISM OF ACTION : Modulating interaction of AGER with its binding partners (e.g. amyloid); Vaccine.

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