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1. 发明申请

US20130324517A1 CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD 有权
标题翻译： CYPIC PYRIMIDIN-4-CARBOXAMIDES作为CCR2受体拮抗剂用于治疗炎症，哮喘和COPD
公开(公告)号：US20130324517A1
公开(公告)日：2013-12-05
申请号：US13949696
申请日：2013-07-24
申请人： Heiner EBEL , Sara FRATTINI , Riccardo GIOVANNINI , Christoph HOENKE , Thomas TRIESELMANN , Patrick TIELMANN , Stefan SCHEUERER , Silke HOBBIE , Frank BUETTNER
发明人： Heiner EBEL , Sara FRATTINI , Riccardo GIOVANNINI , Christoph HOENKE , Thomas TRIESELMANN , Patrick TIELMANN , Stefan SCHEUERER , Silke HOBBIE , Frank BUETTNER
IPC分类号： A61K31/506 , C07D405/14 , C07D403/14 , C07D471/10 , C07D403/06 , A61K31/5377 , A61K31/55 , A61K31/553 , A61K31/551 , C07D401/06 , C07D417/14 , C07D471/04 , C07D498/10 , C07D451/02 , C07D413/14 , C07D491/052 , C07D401/14
CPC分类号： C07D498/10 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/10 , C07D491/052 , Y02A50/385 , Y02A50/409 , Y02A50/411
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
摘要翻译：本发明涉及CCR2（CC趋化因子受体2）的新型拮抗剂及其用于治疗疾病，特别是肺疾病如哮喘和COPD的药物的用途。

2. 发明申请

US20120053164A1 CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD 审中-公开
标题翻译： CYPIC PYRIMIDIN-4-CARBOXAMIDES作为CCR2受体拮抗剂用于治疗炎症，哮喘和COPD
公开(公告)号：US20120053164A1
公开(公告)日：2012-03-01
申请号：US13140591
申请日：2009-12-17
申请人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Thomas Trieselmann , Patrick Tielmann , Stefan Scheuerer , Silke Hobbie , Frank Buettner
发明人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Thomas Trieselmann , Patrick Tielmann , Stefan Scheuerer , Silke Hobbie , Frank Buettner
IPC分类号： A61K31/506 , C07D405/14 , C07D413/14 , A61K31/5377 , C07D403/14 , A61K31/55 , C07D401/06 , C07D471/10 , C07D417/14 , C07D471/04 , C07D498/10 , C07D451/02 , A61K31/553 , C07D403/06 , A61K31/551 , A61P29/00 , A61P11/00 , A61P11/06 , A61P25/00 , A61P37/00 , A61P9/00 , A61P13/12 , A61P3/10 , A61P9/10 , A61P25/04 , C07D401/14
CPC分类号： C07D498/10 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/10 , C07D491/052 , Y02A50/385 , Y02A50/409 , Y02A50/411
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. Formula (I), wherein A is selected from among a single bond, ═CH—, —CH2—, —O—, —S—, and —NH—; wherein n is 1, 2 or 3; wherein Z is C or N, the other variables are as defined in the claims, as well as in form of their acid addition salts with pharmacologically acceptable acids.
摘要翻译：本发明涉及CCR2（CC趋化因子受体2）的新型拮抗剂及其用于治疗疾病，特别是肺疾病如哮喘和COPD的药物的用途。式（I）其中A选自单键，-CH =，-CH 2 - ， - O - ， - S - 和-NH-; 其中n为1,2或3; 其中Z是C或N，其它变量如权利要求中所定义，以及其与药理学上可接受的酸的酸加成盐的形式。

3. 发明申请

US20060247230A1 Novel Piperidine-Substituted Indoles 有权
标题翻译：新型哌啶取代的吲哚
公开(公告)号：US20060247230A1
公开(公告)日：2006-11-02
申请号：US11380232
申请日：2006-04-26
申请人： Domnic Martyres , Pascale Pouzet , Christoph Hoenke , Peter Seither , Silke Hobbie , Thierry Bouyssou
发明人： Domnic Martyres , Pascale Pouzet , Christoph Hoenke , Peter Seither , Silke Hobbie , Thierry Bouyssou
IPC分类号： A61K31/541 , A61K31/454 , C07D417/14 , C07D413/14 , C07D403/14 , C07D405/14
CPC分类号： C07D401/04
摘要： Disclosed are novel piperidine-substituted indoles- or heteroderivatives thereof of the formula 1: wherein R1, R5, R6, R7, A, B, D-E, Y, i, j, n and m are defined as below. The compounds of formula 1 are useful as agonists or antagonists of CCR-3. The present invention is also directed to pharmaceutically acceptable salts thereof, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了式1的新的哌啶取代的吲哚或其异构衍生物：其中R 1，R 5，R 6，R SUP > 7 ，A，B，DE，Y，i，j，n和m定义如下。式1的化合物可用作CCR-3的激动剂或拮抗剂。本发明还涉及其药学上可接受的盐，更特别的是提供药物组合物，其包含药学上可接受的载体和治疗有效量的至少一种本发明的化合物或其药学上可接受的盐。

4. 发明授权

US08835440B2 Cyclic pyrimidin-4-carboxamides as CCR2 receptor antagonists for treatment of inflammation, asthma and COPD 有权
标题翻译：循环嘧啶-4-甲酰胺作为治疗炎症，哮喘和COPD的CCR2受体拮抗剂
公开(公告)号：US08835440B2
公开(公告)日：2014-09-16
申请号：US13949696
申请日：2013-07-24
申请人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Thomas Trieselmann , Patrick Tielmann , Stefan Scheuerer , Silke Hobbie , Frank Buettner
发明人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Thomas Trieselmann , Patrick Tielmann , Stefan Scheuerer , Silke Hobbie , Frank Buettner
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04 , C07D498/10 , C07D403/06 , A61K31/55 , C07D491/052 , C07D401/06 , A61K31/553 , C07D405/14 , C07D471/10 , C07D407/14 , C07D417/14 , A61K31/5377 , A61K31/551 , C07D471/04 , C07D403/14 , C07D451/02 , C07D401/14 , A61K31/506 , C07D413/14
CPC分类号： C07D498/10 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/10 , C07D491/052 , Y02A50/385 , Y02A50/409 , Y02A50/411
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
摘要翻译：本发明涉及CCR2（CC趋化因子受体2）的新型拮抗剂及其用于治疗疾病，特别是肺疾病如哮喘和COPD的药物的用途。

5. 发明申请

US20140142135A1 4-DIMETHYLAMINO-PHENYL-SUBSTITUTED NAPHTHYRIDINES, AND USE THEREOF AS MEDICAMENTS 有权
标题翻译： 4-二甲基苯胺基 - 取代的萘啶，并作为药物使用
公开(公告)号：US20140142135A1
公开(公告)日：2014-05-22
申请号：US14071016
申请日：2013-11-04
申请人： Dennis FIEGEN , Sandra HANDSCHUH , Silke HOBBIE , Matthias HOFFMANN , Takeshi KONO , Yayoi SATO , Andreas SCHNAPP , Annette SCHULER-METZ
发明人： Dennis FIEGEN , Sandra HANDSCHUH , Silke HOBBIE , Matthias HOFFMANN , Takeshi KONO , Yayoi SATO , Andreas SCHNAPP , Annette SCHULER-METZ
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , 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 R1 and R6 may have the meanings as described in claim 1, as well as medicaments which contain these compounds. Further, the invention relates to methods of treating a disease selected from asthma, COPD, allergic rhinitis, adult respiratory distress syndrome, bronchitis, allergic dermatitis, contact dermatitis, idiopathic thrombocytopenic purpura, rheumatoid arthritis and allergic rhinoconjunctivitis by administrating an appropriate amount of a compound of formula 1 to a patient in need thereof.
摘要翻译：本发明涉及式1的新的取代的萘啶，以及其药学上可接受的盐，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和R 6可以具有权利要求1所述的含义，以及含有这些化合物。此外，本发明涉及通过施用适量的化合物治疗选自哮喘，COPD，变应性鼻炎，成人呼吸窘迫综合征，支气管炎，过敏性皮炎，接触性皮炎，特发性血小板减少性紫癜，类风湿性关节炎和过敏性鼻炎的疾病的方法式1给有需要的患者。

6. 发明申请

US20110263549A1 4-DIMETHYLAMINO-PHENYL-SUBSTITUTED NAPHTHYRIDINES, AND USE THEREOF AS MEDICAMENTS 有权
标题翻译： 4-二甲基苯胺基 - 取代的萘啶，并作为药物使用
公开(公告)号：US20110263549A1
公开(公告)日：2011-10-27
申请号：US13057330
申请日：2009-07-23
申请人： Dennis Fiegen , Sandra Handschuh , Silke Hobbie , Matthias Hoffmann , Takeshi Kono , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
发明人： Dennis Fiegen , Sandra Handschuh , Silke Hobbie , Matthias Hoffmann , Takeshi Kono , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
IPC分类号： A61K31/573 , A61K31/4375 , A61P11/00 , A61P19/10 , A61P1/04 , A61P31/14 , A61P7/06 , A61P25/00 , C07D471/04 , A61P19/02
CPC分类号： C07D471/04 , C07D519/00
摘要： The invention relates to novel substituted naphthyridines of formula 1 as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates, or solvates thereof. In formula 1, R1 can represent a group A selected from among the group comprising —O—R3, —NR3 R4, —CR3R4R5, -(ethyne)-R3, —S—R3, —SO—R3, and SO2—R3, or R1 represents a group B selected from among the group comprising: —C6-10-aryl;—a five-membered to ten-membered, monocyclic or bicyclic heteroaryl containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heteroaryl is linked to the structure according to formula 1 via a C atom or an N atom;—a three-membered to ten-membered, monocyclic or bicyclic, saturated or partially saturated heterocycle containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heterocycle is linked to the structure according to formula 1 via a C atom or an N atom; and—a 5-membered to 11-membered spiro group which can optionally contain 1, 2, or 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said spiro group is linked to the structure according to formula 1 via a C atom or an N atom, wherein said group B can be optionally substituted as described in claims 1, and R3,R4,R5,R6, and m can have the meanings indicated in claim 1. The invention also relates to pharmaceutical compositions containing said compounds.
摘要翻译：本发明涉及式1的新型取代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，外消旋物，水合物或溶剂合物。在式1中，R 1可以表示选自-O-R 3，-NR 3 R 4，-CR 3 R 4 R 5， - （乙炔）-R 3，-S-R 3，-SO-R 3和SO 2 -R 3的基团A，或R 1表示选自包括以下基团的基团：-C 6-10 - 芳基; - 含有1至3个独立地选自以下的杂原子的五元至十元单环或双环杂芳基：N，O，和S，其中所述杂芳基通过C原子或N原子连接到根据式1的结构; - 含有1至3个独立选择的杂原子的三元至十元单环或双环饱和或部分饱和的杂环包括N，O和S的基团，其中所述杂环通过C原子或N原子连接到根据式1的结构; 和可以任选地含有1,2或3个独立地选自包括N，O和S的基团的杂原子的5元至11元螺环，其中所述螺环与根据式1的结构连接通过C原子或N原子，其中所述基团B可以如权利要求1所述任选被取代，并且R 3，R 4，R 5，R 6和m可以具有权利要求1中所示的含义。本发明还涉及药物组合物含有所述化合物。

7. 发明授权

US07759365B2 Piperidine-substituted indoles 有权
标题翻译：哌啶取代的吲哚
公开(公告)号：US07759365B2
公开(公告)日：2010-07-20
申请号：US11380232
申请日：2006-04-26
申请人： Domnic Martyres , Pascale Pouzet , Christoph Hoenke , Peter Seither , Silke Hobbie , Thierry Bouyssou
发明人： Domnic Martyres , Pascale Pouzet , Christoph Hoenke , Peter Seither , Silke Hobbie , Thierry Bouyssou
IPC分类号： A61K31/454 , C07D403/14
CPC分类号： C07D401/04
摘要： Disclosed are novel piperidine-substituted indoles- or heteroderivatives thereof of the formula 1: wherein R1, R5, R6, R7, A, B, D-E, Y, i, j, n and m are defined as below. The compounds of formula 1 are useful as agonists or antagonists of CCR-3. The present invention is also directed to pharmaceutically acceptable salts thereof, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了式1的新的哌啶取代的吲哚或其异构衍生物：其中R1，R5，R6，R7，A，B，D-E，Y，i，j，n和m如下定义。式1的化合物可用作CCR-3的激动剂或拮抗剂。本发明还涉及其药学上可接受的盐，更特别的是提供药物组合物，其包含药学上可接受的载体和治疗有效量的至少一种本发明的化合物或其药学上可接受的盐。

8. 发明授权

US08653262B2 CCR2 receptor antagonists and uses thereof 有权
标题翻译： CCR2受体拮抗剂及其用途
公开(公告)号：US08653262B2
公开(公告)日：2014-02-18
申请号：US12602274
申请日：2008-05-29
申请人： Heiner Ebel , Silke Hobbie
发明人： Heiner Ebel , Silke Hobbie
IPC分类号： C07D403/04 , C07D413/14 , C07D401/14 , A61P11/06
CPC分类号： C07D231/38 , C07D401/04 , C07D401/14 , C07D413/12
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
摘要翻译：本发明涉及CCR2（CC趋化因子受体2）的新型拮抗剂及其用于治疗疾病，特别是肺疾病如哮喘和COPD的药物的用途。

9. 发明申请

US20110201608A1 SUBSTITUTED NAPHTHYRIDINES AND USE THEREOF AS MEDICINES 审中-公开
标题翻译：取代的萘啶酮及其作为药物的用途
公开(公告)号：US20110201608A1
公开(公告)日：2011-08-18
申请号：US13057288
申请日：2009-07-23
申请人： Matthias Hoffmann , Thierry Bouyssou , Georg Dahamnn , Harald Engelhardt , Dennis Fiegen , Sandra Handschum , Silke Hobbie , Takeshi Kono , Ulrich Reiser , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
发明人： Matthias Hoffmann , Thierry Bouyssou , Georg Dahamnn , Harald Engelhardt , Dennis Fiegen , Sandra Handschum , Silke Hobbie , Takeshi Kono , Ulrich Reiser , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/496 , A61P11/06 , A61P19/02 , A61P1/04 , A61P17/06 , A61P35/00 , A61P17/00 , A61P11/00
CPC分类号： C07D471/04 , C07D487/04 , C07D487/10 , C07D513/04
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 R1 denotes a group A selected from among —O—R3, —NR3R4, —CR3R4R5, -(ethyne)-R3, —S—R3, —SO—R3 and SO2—R3 or R1 denotes a group B selected from among C6-10-aryl, five- to ten-membered, mono- or bicyclic heteroaryl with 1-3 heteroatoms selected independently of one another from among N, O and S; while this heteroaryl is linked to the structure according to formula 1 via either a C atom or an N atom, three- to ten-membered, mono- or bicyclic, saturated or partially saturated heterocyclic group with 1-3 heteroatoms selected independently of one another from among N, O and S, while this heterocyclic group is linked to the structure according to formula 1 via either a C atom or an N atom, and 5- to 11-membered spiro group which may optionally contain 1, 2 or 3 heteroatoms selected independently of one another from among N, O and S, while this spiro group is linked to the structure according to formula 1 via either a C atom or an N atom, while this group B may optionally be substituted as described in claim 1 and wherein R2 is and R3, R4, R5, R6, R6′, R7, R8, R9, R10, V, n and m may have the meanings given in claim 1, as well as pharmaceutical compositions containing these compounds.
摘要翻译：本发明涉及式1的新取代的萘啶，以及其药学上可接受的盐，非对映异构体，对映异构体，外消旋体，水合物或溶剂化物，其中R1表示选自-O-R3，-NR3R4，-CR3R4R5，（乙炔）-R 3，-S-R 3，-SO-R 3和SO 2 -R 3或R 1表示选自C 6-10 - 芳基，5至10元，单 - 或双环杂芳基和1-3 从N，O和S中彼此独立地选择的杂原子; 而该杂芳基通过C原子或N原子连接到根据式1的结构，具有1-3个互相独立选择的杂原子的三至十元，单环或二环，饱和或部分饱和的杂环基 N，O和S中的至少一个，而该杂环基通过C原子或N原子与根据式1的结构连接，并且可以任选地含有1,2或3个杂原子的5至11元螺环 N，O和S彼此独立地选择，而该螺环通过C原子或N原子连接到根据式1的结构，而该基团B可以任选地被如权利要求1和其中R2是和R3，R4，R5，R6，R6'，R7，R8，R9，R10，V，n和m可以具有权利要求1中给出的含义，以及含有这些化合物的药物组合物。

10. 发明申请

US20100204209A1 CCR2 Receptor Antagonists and Uses Thereof 有权
标题翻译： CCR2受体拮抗剂及其用途
公开(公告)号：US20100204209A1
公开(公告)日：2010-08-12
申请号：US12602274
申请日：2008-05-29
申请人： Heiner Ebel , Stefan Peters , Silke Hobbie
发明人： Heiner Ebel , Stefan Peters , Silke Hobbie
IPC分类号： A61K31/55 , C07D403/04 , A61K31/496 , C07D413/06 , A61K31/5377 , C07D403/00 , A61K31/501 , C07D403/14 , A61P11/06 , A61P11/00
CPC分类号： C07D231/38 , C07D401/04 , C07D401/14 , C07D413/12
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
摘要翻译：本发明涉及CCR2（CC趋化因子受体2）的新型拮抗剂及其用于治疗疾病，特别是肺疾病如哮喘和COPD的药物的用途。

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