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1. 发明授权

US09505829B2 Anti-NGF antibodies and their use 有权
标题翻译：抗NGF抗体及其用途
公开(公告)号：US09505829B2
公开(公告)日：2016-11-29
申请号：US13817721
申请日：2011-08-19
申请人： Susan E. Lacy , Jeffrey A. Barbon , Meha Chhaya , Emma Fung , Charles W. Hutchins , Diane M. Lang , Eve H. Barlow , Mary Leddy , Ravi Chari
发明人： Susan E. Lacy , Jeffrey A. Barbon , Meha Chhaya , Emma Fung , Charles W. Hutchins , Diane M. Lang , Eve H. Barlow , Mary Leddy , Ravi Chari
IPC分类号： C07K16/22 , A61K39/395
CPC分类号： C07K16/22 , A61K39/3955 , A61K2039/505 , C07K2317/24 , C07K2317/31 , C07K2317/50 , C07K2317/51 , C07K2317/515 , C07K2317/54 , C07K2317/55 , C07K2317/565 , C07K2317/569 , C07K2317/60 , C07K2317/622 , C07K2317/624 , C07K2317/626 , C07K2317/64 , C07K2317/73 , C07K2317/76 , C07K2317/92 , C07K2317/94 , G01N33/566
摘要： The present disclosure encompasses NGF binding proteins, specifically to antibodies that are chimeric, CDR grafted and canonized antibodies, and methods of making and uses thereof. The antibodies, or antibody portions, of the disclosure are useful for detecting NGF and for inhibiting NGF activity, e.g., in a mammal subject suffering from a disorder in which NGF activity is detrimental.
摘要翻译：本公开内容涵盖NGF结合蛋白，特别是嵌合抗体，CDR移植和标准化抗体的抗体，及其制备和使用方法。本公开的抗体或抗体部分可用于检测NGF和抑制NGF活性，例如在患有NGF活性有害的病症的哺乳动物受试者中。

2. 发明授权

US09018206B2 Carboxamide compounds and their use as calpain inhibitors 有权
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：US09018206B2
公开(公告)日：2015-04-28
申请号：US13610975
申请日：2012-09-12
申请人： Helmut Mack , Andreas Kling , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
发明人： Helmut Mack , Andreas Kling , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
IPC分类号： C07D211/76 , C07D233/34 , C07D239/10 , C07D207/22 , C07D211/78 , C07D233/32 , C07D275/03 , C07D401/06 , C07D405/12 , C07D409/12 , C07D417/12 , C07D207/26
CPC分类号： C07D207/22 , C07D207/26 , C07D207/28 , C07D211/76 , C07D211/78 , C07D213/81 , C07D233/32 , C07D233/34 , C07D239/10 , C07D275/03 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式I的化合物，其中R 1，R 2，R 3a，R 3b，R 4，Q，Y，A和X具有权利要求和说明书中所述的含义及其互变异构体及其药学上合适的盐。特别地，化合物具有通式Ia和Ib，其中R1，r，R2b，R3a，R3b，R4，Y和X具有权利要求中提及的含义，包括其互变异构体及其药学上合适的盐。在这些化合物中，优选其中Y为CH2-CH2，CH2-CH2-CH2，N（Ry＃）-CH2，N（Ry＃）-CH2-CH2或CH = CH-CH≡，各自任选具有1 或2个H原子被相同或不同的基团Ry取代，其中Ry和Ry＃具有权利要求中提及的含义。

3. 发明申请

US20140343286A1 ANTI-VIRAL COMPOUNDS 审中-公开
公开(公告)号：US20140343286A1
公开(公告)日：2014-11-20
申请号：US14365519
申请日：2011-12-15
申请人： Allan C. Krueger , Warren M. Kati , Clarence J. Maring , Rolf Wagner , Charles W. Hutchins
发明人： Allan C. Krueger , Warren M. Kati , Clarence J. Maring , Rolf Wagner , Charles W. Hutchins
IPC分类号： C07D403/14 , C07D401/14
CPC分类号： C07D403/14 , A61K31/4427 , C07D401/14
摘要： The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.

4. 发明授权

US08877794B2 Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy 有权
标题翻译：苯烷基胺衍生物，含有它们的药物组合物及其在治疗中的用途
公开(公告)号：US08877794B2
公开(公告)日：2014-11-04
申请号：US13206937
申请日：2011-08-10
申请人： Frauke Pohlki , Udo Lange , Wilhelm Amberg , Michael Ochse , Berthold Behl , Charles W. Hutchins , Wilfried Hornberger , Mario Mezler , Sean Turner
发明人： Frauke Pohlki , Udo Lange , Wilhelm Amberg , Michael Ochse , Berthold Behl , Charles W. Hutchins , Wilfried Hornberger , Mario Mezler , Sean Turner
IPC分类号： A61K31/135 , C07C211/27 , C07C311/10 , C07D403/12 , C07D231/18 , C07D207/267 , C07D401/12 , C07C311/05 , C07D205/04 , C07D233/42 , C07C311/04 , C07D295/135 , C07D207/08
CPC分类号： C07C311/06 , C07C311/04 , C07C311/05 , C07C311/10 , C07C2601/02 , C07C2601/04 , C07D205/04 , C07D207/08 , C07D207/267 , C07D231/18 , C07D233/42 , C07D233/84 , C07D295/135 , C07D401/12 , C07D403/12
摘要： The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
摘要翻译：本发明涉及式（I）的苯烷基胺衍生物或其生理上耐受的盐。本发明涉及包含这种苯烷基胺衍生物的药物组合物，以及这种苯烷基胺衍生物用于治疗目的的用途。酚烷基胺衍生物是GlyT1抑制剂。

5. 发明授权

US08624002B2 Prostaglandin E2 binding proteins and uses thereof 有权
标题翻译：前列腺素E2结合蛋白及其用途
公开(公告)号：US08624002B2
公开(公告)日：2014-01-07
申请号：US12499646
申请日：2009-07-08
申请人： Jjijie Gu , Charles W. Hutchins , Rong-rong Zhu , Jianwei Shen , Maria C. Harris , Eileen Belanger , Anwar Murtaza , Edit Tarcsa , William B. Stine , Chung-ming Hsieh
发明人： Jjijie Gu , Charles W. Hutchins , Rong-rong Zhu , Jianwei Shen , Maria C. Harris , Eileen Belanger , Anwar Murtaza , Edit Tarcsa , William B. Stine , Chung-ming Hsieh
IPC分类号： C07K16/18
CPC分类号： C07K16/18 , A61K31/405 , A61K31/573 , A61K39/39533 , A61K2039/505 , C07K16/26 , C07K2317/21 , C07K2317/24 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/622 , C07K2317/76 , Y02A50/386 , Y02A50/401 , Y02A50/41 , Y02A50/412 , Y02A50/478 , Y02A50/481
摘要： The present invention encompasses prostaglandin E2 (PGE2) binding proteins. The invention relates to antibodies that are wild-type, chimeric, CDR grafted and humanized. Preferred antibodies have high affinity for prostaglandin E2 and neutralize prostaglandin E2 activity in vitro and in vivo. An antibody of the invention can be a full-length antibody, or an antigen-binding portion thereof. Methods of making and methods of using the antibodies of the invention are also provided. The antibodies, or antigen-binding portions, of the invention are useful for detecting prostaglandin E2 and for inhibiting prostaglandin E2 activity, e.g., in a human subject suffering from a disorder in which prostaglandin E2 activity is detrimental.
摘要翻译：本发明包括前列腺素E2（PGE2）结合蛋白。本发明涉及野生型，嵌合型，CDR移植和人源化的抗体。优选的抗体对前列腺素E2具有高亲和力，并在体外和体内中和前列腺素E2活性。本发明的抗体可以是全长抗体或其抗原结合部分。还提供了制备方法和使用本发明抗体的方法。本发明的抗体或抗原结合部分可用于检测前列腺素E2和用于抑制前列腺素E2活性，例如在患有前列腺素E2活性有害的病症的人类受试者中。

6. 发明授权

US08563617B2 Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy 有权
公开(公告)号：US08563617B2
公开(公告)日：2013-10-22
申请号：US12706326
申请日：2010-02-16
申请人： Wilhelm Amberg , Michael Ochse , Udo Lange , Andreas Kling , Berthold Behl , Wilfried Homberger , Mario Mezler , Charles W. Hutchins
发明人： Wilhelm Amberg , Michael Ochse , Udo Lange , Andreas Kling , Berthold Behl , Wilfried Homberger , Mario Mezler , Charles W. Hutchins
IPC分类号： A61K31/16 , C07C215/70
CPC分类号： C07C311/05 , C07C215/64 , C07C217/74 , C07C233/18 , C07C233/19 , C07C233/69 , C07C255/58 , C07C271/24 , C07C307/06 , C07C309/65 , C07C311/07 , C07C311/09 , C07C311/10 , C07C311/13 , C07C311/14 , C07C311/17 , C07C311/18 , C07C311/20 , C07C311/24 , C07C317/18 , C07C317/28 , C07C2601/02 , C07C2601/04 , C07C2602/10 , C07D205/04 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/27 , C07D207/36 , C07D207/48 , C07D213/71 , C07D231/18 , C07D233/84 , C07D249/12 , C07D261/08 , C07D265/30 , C07D275/02 , C07D295/096 , C07D295/135 , C07D305/08 , C07D333/34 , C07D401/12 , C07D403/12 , C07D409/12 , C07F7/081
摘要： The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.

7. 发明授权

US08541424B2 Anti-viral compounds 有权
标题翻译：抗病毒化合物
公开(公告)号：US08541424B2
公开(公告)日：2013-09-24
申请号：US12644427
申请日：2009-12-22
申请人： David A. DeGoey , Pamela L. Donner , Warren M. Kati , Charles W. Hutchins , Mark A. Matulenko , Tammie K. Jinkerson , Ryan G. Keddy
发明人： David A. DeGoey , Pamela L. Donner , Warren M. Kati , Charles W. Hutchins , Mark A. Matulenko , Tammie K. Jinkerson , Ryan G. Keddy
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00
CPC分类号： C07D471/04
摘要： Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
摘要翻译：描述了有效抑制丙型肝炎病毒（“HCV”）复制的化合物。本发明还涉及制备这种化合物的方法，包含这些化合物的组合物，以及使用这些化合物治疗HCV感染的方法。

8. 发明授权

US08486931B2 Substituted oxindole compounds 有权
标题翻译：取代的羟吲哚化合物
公开(公告)号：US08486931B2
公开(公告)日：2013-07-16
申请号：US12529542
申请日：2008-02-29
申请人： Herve Genesle , Thorsten Oost , Charles W. Hutchins , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch , Astrid Netz , Alfred Hahn
发明人： Herve Genesle , Thorsten Oost , Charles W. Hutchins , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch , Astrid Netz , Wolfgang Wernet
IPC分类号： A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/551
CPC分类号： C07D401/14 , C07D401/04 , C07D401/12 , C07D471/08
摘要： The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
摘要翻译：本发明涉及通式（I）的化合物，其中A，B，R1，R2和Het具有权利要求1中给出的含义; Y是下式的二价基团，其中D是C 1 -C 3 - 亚烷基，其中D可以具有取代基R 5; R 3是氢，C 1 -C 8烷基或与R 4一起是可以具有基团R 5a的C 1 -C 3亚烷基，或与R 5一起为C 1 -C 3 - 亚烷基，并且R 4是氢，C 1 -C 8 - 烷基或与 R 3是可以具有基团R 5a的C 1 -C 3亚烷基，或与R 5一起为C 1 -C 3 - 亚烷基，其中R 5与存在的R a a为键或C 1 -C 3 - 亚烷基; 并且其中满足以下条件之一：R 3与R 4一起可以具有基团R 5a的C 1 -C 3 - 亚烷基; 或R 3与R 5一起为C 1 -C 3 - 亚烷基; 或R 4与R 5一起为C 1 -C 3 - 亚烷基，其中基团B为苯基或萘基时，基团A不同于苯基; 以及包含这些化合物的药物及其用于预防和/或治疗加压素依赖性和/或催产素依赖性疾病的用途。

9. 发明申请

US20130150367A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：US20130150367A1
公开(公告)日：2013-06-13
申请号：US13610975
申请日：2012-09-12
申请人： Helmut Mack , Andreas Kling , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
发明人： Helmut Mack , Andreas Kling , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
IPC分类号： C07D207/22 , C07D275/03 , C07D409/12 , C07D401/06 , C07D417/12 , C07D405/12 , C07D211/78 , C07D233/32
CPC分类号： C07D207/22 , C07D207/26 , C07D207/28 , C07D211/76 , C07D211/78 , C07D213/81 , C07D233/32 , C07D233/34 , C07D239/10 , C07D275/03 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式I的化合物，其中R 1，R 2，R 3a，R 3b，R 4，Q，Y，A和X具有权利要求和说明书中所述的含义及其互变异构体及其药学上合适的盐。特别地，化合物具有通式Ia和Ib，其中R1，r，R2b，R3a，R3b，R4，Y和X具有权利要求中提及的含义，包括其互变异构体及其药学上合适的盐。在这些化合物中，优选其中Y为CH2-CH2，CH2-CH2-CH2，N（Ry＃）-CH2，N（Ry＃）-CH2-CH2或CH = CH-CH =，各自任选具有1 或2个H原子被相同或不同的基团Ry取代，其中Ry和Ry＃具有权利要求中提及的含义。

10. 发明申请

US20120295881A1 TETRALINE AND INDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY 有权
标题翻译：四环素和吲哚衍生物，含有它们的药物组合物及其在治疗中的使用
公开(公告)号：US20120295881A1
公开(公告)日：2012-11-22
申请号：US13546434
申请日：2012-07-11
申请人： Udo Lange , Wilhelm Amberg , Michael Ochse , Berthold Behl , Frauke Pohlki , Charles W. Hutchins
发明人： Udo Lange , Wilhelm Amberg , Michael Ochse , Berthold Behl , Frauke Pohlki , Charles W. Hutchins
IPC分类号： A61K31/18 , C07D233/84 , A61K31/4164 , A61P25/18 , A61K31/397 , C07D403/12 , A61K31/4178 , A61P25/00 , C07C311/14 , C07D205/04
CPC分类号： C07D233/84 , C07C311/05 , C07C311/10 , C07C311/14 , C07C2601/02 , C07C2601/04 , C07C2602/08 , C07C2602/10 , C07D205/04 , C07D403/12
摘要： The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.
摘要翻译：本发明涉及式（I）的四氢化萘和二氢化茚衍生物或其生理上耐受的盐。本发明涉及包含这种四氢化萘和二氢化茚衍生物的药物组合物，以及这些四氢化萘和二氢化茚衍生物用于治疗目的的用途。四氢化萘和茚满衍生物是GlyT1抑制剂。

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