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1. 发明申请

WO2008098025A1 ARYLSULFONAMIDE COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR 审中-公开
标题翻译：调节CB2受体的ARYLSULFONAMIDE化合物
公开(公告)号：WO2008098025A1
公开(公告)日：2008-08-14
申请号：PCT/US2008/053117
申请日：2008-02-06
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG , THOMSON, David , RIETHER, Doris , ZINDELL, Renee, M. , HICKEY, Eugene, Richard , ERMANN, Monika , JENKINS, James, Edward , MUSHI, Innocent , TAYLOR, Malcolm , AMOUZEGH, Patricia , WALKER, Edward
发明人： THOMSON, David , RIETHER, Doris , ZINDELL, Renee, M. , HICKEY, Eugene, Richard , ERMANN, Monika , JENKINS, James, Edward , MUSHI, Innocent , TAYLOR, Malcolm , AMOUZEGH, Patricia , WALKER, Edward
IPC分类号： A01N41/06 , A61K31/18
CPC分类号： C07D401/12 , C07D215/08 , C07D217/06 , C07D271/06 , C07D413/04 , C07D413/12 , C07D417/12
摘要： Compounds are provided which bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) and the formula (IA) wherein, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and X have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators.
摘要翻译：提供了与CB2受体的激动剂，拮抗剂或反向激动剂结合的化合物，具有通式（I）和式（IA）的化合物，其中R 1，R 2， 2，R 3，R 4，R 5，R 6，R 6， 7，R 8，8

2. 发明申请

WO2009055357A1 DIAZEPANE COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR 审中-公开
标题翻译：调节CB2受体的DIAZEPANE化合物
公开(公告)号：WO2009055357A1
公开(公告)日：2009-04-30
申请号：PCT/US2008/080591
申请日：2008-10-21
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG , CIRILLO, Pier, Francesco , HICKEY, Eugene, Richard , RIETHER, Doris , WU, Lifen , ZINDELL, Renee , AMOUZEGH, Patricia , ERMANN, Monika , WALKER, Edward
发明人： CIRILLO, Pier, Francesco , HICKEY, Eugene, Richard , RIETHER, Doris , WU, Lifen , ZINDELL, Renee , AMOUZEGH, Patricia , ERMANN, Monika , WALKER, Edward
IPC分类号： C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14 , C07D495/04 , C07D495/14 , A61P29/00 , A61K31/5513
CPC分类号： C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14 , C07D495/04 , C07D495/14
摘要： Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
摘要翻译：公开了式（I）的化合物。根据本发明的化合物与CB2受体结合并且是激动剂，拮抗剂或反向激动剂，并且可用于治疗炎症。作为激动剂的那些化合物另外可用于治疗疼痛。

3. 发明申请

WO2011092128A1 SUBSTITUTED NAPHTHYRIDINES AND THEIR USE AS SYK KINASE INHIBITORS 审中-公开
标题翻译：取代的萘啶酮及其作为SYK激酶抑制剂的用途
公开(公告)号：WO2011092128A1
公开(公告)日：2011-08-04
申请号：PCT/EP2011/050871
申请日：2011-01-21
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , HOFFMANN, Matthias , DAHMANN, Georg , FIEGEN, Dennis , HANDSCHUH, Sandra , KLICIC, Jasna , LINZ, Guenter , SCHAENZLE, Gerhard , SCHNAPP, Andreas , EAST, Stephen P. , MAZANETZ, Michael Philip , SCOTT, John , WALKER, Edward
发明人： HOFFMANN, Matthias , DAHMANN, Georg , FIEGEN, Dennis , HANDSCHUH, Sandra , KLICIC, Jasna , LINZ, Guenter , SCHAENZLE, Gerhard , SCHNAPP, Andreas , EAST, Stephen P. , MAZANETZ, Michael Philip , SCOTT, John , WALKER, Edward
IPC分类号： C07D471/04 , C07D519/00 , A61K31/4375
CPC分类号： C07D471/04 , C07D498/04 , C07D519/00
摘要： The invention relates to new substituted naphthyridines of formula (1), as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R 1 is selected from among -O-R 3 or -NR 3 R 4 , R 3 is C 1-6 -alkyl which is substituted by R 5 and R 6 R 5 is selected from hydrogen, branched or linear C 1-6 -alkyl, C 2-6 -alkenyl, -C 1-6 -alkylen-O-C 1-3 -alkyl, C 1-3 -haloalkyl, R 6 is ring X wherein n is either 0 or 1, and Formula (I) is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH 2 , CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, -C 1-3 -alkyl, -C 1-3 -haloalkyl, -O-C 1-3 -alkyl, -C 1-3 -alkanol and halogen, and wherein R 4 , R 2 , R 7 , R 8 , R 9 , R 10 , R 11 and Q may have the meanings as given in claim 1, as well as pharmaceutical compositions containing these compounds.
摘要翻译：本发明涉及新的式（1）取代的萘啶，以及其药理学上可接受的盐，非对映异构体，对映异构体，外消旋体，水合物或溶剂合物，其中R 1选自-O-R 3或-NR 3 R 4，R 3是C 1-6 被R5和R6 R5取代的 - 烷基选自氢，支链或直链C 1-6 - 烷基，C 2-6 - 烯基，-C 1-6 - 亚烷基-O-C 1-3 - 烷基，C 1-3 - 卤代烷基 R6为环X，其中n为0或1，式（I）为单键或双键，其中A，B，D和E各自独立地选自CH 2，CH，C， N，NH，O或S，并且其中环X通过位置A，B，D或E连接到分子，其中所述环X可以任选地被一个，两个或三个残基进一步取代，每个残基各自独立地选自：的氧代，羟基，-C 1-3 - 烷基，-C 1-3 - 卤代烷基，-O-C 1-3 - 烷基，-C 1-3 - 链烷醇和卤素，其中R4，R2，R7，R8，R9， R10，R11和Q可以具有给定的含义在权利要求1中，以及含有这些化合物的药物组合物。

4. 发明申请

WO2015140054A1 HETEROARYL SYK INHIBITORS 审中-公开
标题翻译： HETEROARYL SYK抑制剂
公开(公告)号：WO2015140054A1
公开(公告)日：2015-09-24
申请号：PCT/EP2015/055237
申请日：2015-03-12
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人： DAHMANN, Georg , HOFFMANN, Matthias , KLICIC, Jasna , LAMB, David James , MCCARTHY, Clive , NAPIER, Spencer , PARRISH, Karen , SCOTT, John , SWANTEK FITZGERALD, Jennifer L. , WALKER, Edward
IPC分类号： C07D403/14 , C07D471/04 , C07D487/04 , A61K31/505 , A61P11/06
CPC分类号： C07D487/04 , A61K31/416 , A61K31/4184 , A61K31/427 , A61K31/437 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： The invention relates to new substituted heteroarylsof formula (1) wherein A is selected from the group consisting of N and CH, D is selected from the group consisting of S and O, E is C, T is C, G is C, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R 1 , M and R 3 are defined according to claim 1, and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
摘要翻译：本发明涉及新的取代杂芳基式（1）其中A选自N和CH，D选自S和O，E是C，T是C，G是C，其中环1中的每个断点（虚线）双键选自单键或双键，条件是环1的所有单键和双键以这样的方式排列，使得它们都与环2一起形成芳香环体系，其中根据权利要求1定义R1，M和R3以及上述化合物，用于治疗选自哮喘，COPD，过敏性鼻炎，过敏性皮炎，狼疮性红斑狼疮，狼疮性肾炎和类风湿关节炎。

5. 发明申请

WO2015140055A1 HETEROARYL SYK INHIBITORS 审中-公开
标题翻译： HETEROARYL SYK抑制剂
公开(公告)号：WO2015140055A1
公开(公告)日：2015-09-24
申请号：PCT/EP2015/055242
申请日：2015-03-12
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人： DAHMANN, Georg , HOFFMANN, Matthias , KLICIC, Jasna , LAMB, David James , MCCARTHY, Clive , NAPIER, Spencer , PARRISH, Karen , SCOTT, John , SWANTEK FITZGERALD, Jennifer L. , WALKER, Edward
IPC分类号： C07D403/14 , C07D471/04 , C07D487/04 , A61K31/505 , A61P11/06
CPC分类号： C07D487/04 , A61K31/416 , A61K31/4184 , A61K31/427 , A61K31/437 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： The invention relates to new substituted heteroaryls of formula 1 wherein A is selected from the group consisting of N and CH D is selected from the group consisting of CH, N, NH, E is C, T is selected from the group consisting of C and N, G is selected from the group consisting of C and N, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R 1 , M and R 3 are defined according to claim 1, and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
摘要翻译：本发明涉及式1的新的取代杂芳基，其中A选自N和CH D选自CH，N，NH，E是C，选择T 从C和N组成的组中，G选自C和N，并且其中环1中的每个断点（虚线）双键选自单键或双键，条件是条件是环1的所有单键和双键以这样的方式排列，使得它们都与环2一起形成芳族环系，并且其中根据权利要求1定义R1，M和R3以及上述用于治疗选自哮喘，COPD，过敏性鼻炎，过敏性皮炎，狼疮性红斑狼疮，狼疮性肾炎和类风湿性关节炎的疾病。

6. 发明申请

WO2015140051A8 HETEROARYL SYK INHIBITORS 审中-公开
公开(公告)号：WO2015140051A8
公开(公告)日：2015-09-24
申请号：PCT/EP2015/055228
申请日：2015-03-12
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人： DAHMANN, Georg , HOFFMANN, Matthias , KLICIC, Jasna , LAMB, David James , MCCARTHY, Clive , NAPIER, Spencer , PARRISH, Karen , SCOTT, John , SWANTEK FITZGERALD, Jennifer L. , WALKER, Edward
IPC分类号： C07D413/12 , C07D417/12 , C07D498/04 , C07D513/04 , A61K31/505 , A61P11/06
摘要： The invention relates to new substituted heteroaryls of formula (1), wherein A is selected from the group consisting of N and CH, D is CH, E is selected from the group consisting of C and N, T is C, G is selected from the group consisting of C and N, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R 1 , M and R 3 are defined according to claim 1, and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes,lupus nephritisand rheumatoid arthritis.

7. 发明申请

WO2013050616A1 MODULATION OF STRUCTURED POLYPEPTIDE SPECIFICITY 审中-公开
标题翻译：结构多肽特异性的调节
公开(公告)号：WO2013050616A1
公开(公告)日：2013-04-11
申请号：PCT/EP2012/069898
申请日：2012-10-08
申请人： BICYCLE THERAPEUTICS LIMITED , TITE, John , WALKER, Edward , STACE, Catherine , TEUFEL, Daniel
发明人： TITE, John , WALKER, Edward , STACE, Catherine , TEUFEL, Daniel
IPC分类号： C40B40/02 , C07K1/107
CPC分类号： C07K7/56 , A61K38/10 , A61K38/12 , C07K1/00 , C07K1/1075 , C07K2/00 , C07K7/08
摘要： The invention describes peptide ligands specific for human plasma Kallikrein.
摘要翻译：本发明描述了对人血浆激肽释放酶特异性的肽配体。

8. 发明申请

WO2013050615A1 MODULATION OF STRUCTURED POLYPEPTIDE SPECIFICITY 审中-公开
标题翻译：结构多肽特异性的调节
公开(公告)号：WO2013050615A1
公开(公告)日：2013-04-11
申请号：PCT/EP2012/069897
申请日：2012-10-08
申请人： BICYCLE THERAPEUTICS LIMITED , TITE, John , WALKER, Edward , STACE, Catherine , HEINIS, Christian
发明人： TITE, John , WALKER, Edward , STACE, Catherine , HEINIS, Christian
IPC分类号： C40B40/02 , C07K1/107
CPC分类号： C07K7/56 , A61K38/10 , A61K38/12 , C07K1/00 , C07K1/1075 , C07K2/00 , C07K7/08
摘要： The invention describes a method for selecting a polypeptide ligand having a desired level of specificity for a target, wherein the polypeptide ligand comprises a polypeptide comprising at least three reactive groups, separated by at least two loop sequences, and a molecular scaffold which formscovalent bonds with the reactive groups of the polypeptide such that at least two polypeptide loops are formed on the molecular scaffold, comprising (i) screening at least two different sets of polypeptide ligands against the target, and selecting one or more ligands from each library which interact with the target; (ii) comparing the activity of the selected ligands with one or more paralogues or orthologues of the target; and (iii) further selecting one or more ligands according to their activity towardssaid one or more paralogues or orthologues; wherein said two or more different sets of ligands differ in the length of the polypeptide loops formed on the molecular scaffold.
摘要翻译：本发明描述了一种用于选择对靶标具有期望的特异性水平的多肽配体的方法，其中多肽配体包含多肽，该多肽配体包含至少三个由至少两个环序列分开的反应性基团的多肽，以及分子支架，其与所述多肽的反应性基团使得在分子支架上形成至少两个多肽环，其包含（i）筛选针对靶的至少两种不同组的多肽配体，以及从每个文库中选择一个或多个与目标; （ii）将所选配体的活性与目标的一个或多个旁系同源物或直向同源物进行比较; 和（iii）根据它们的活性进一步选择一种或多种配体，所述配体依赖于一个或多个旁系同源物或直向同源物; 其中所述两种或更多种不同的配体组在分子支架上形成的多肽环的长度不同。

9. 发明申请

WO2009126932A2 FORTIFIED LIQUID PROTEIN COMPOSITIONS AND METHODS OF MAKING SAME 审中-公开
标题翻译：透液液蛋白组合物及其制备方法
公开(公告)号：WO2009126932A2
公开(公告)日：2009-10-15
申请号：PCT/US2009/040273
申请日：2009-04-10
申请人： PROVIDE NUTRITION , WALKER, Edward
发明人： WALKER, Edward
IPC分类号： A23L2/66 , A23L2/52 , A23J3/22 , A23L2/60 , A23L2/56
CPC分类号： A23L2/52 , A23L2/66 , A23L33/17 , A23L33/175 , A23L33/18
摘要： A fortified liquid protein composition and method includes hydrolyzed collagen and a desired abundance of sulfur containing amino acids and optionally taurine.
摘要翻译：强化的液体蛋白质组合物和方法包括水解的胶原蛋白和所需的含量的含硫氨基酸和任选的牛磺酸。

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