公开(公告)号：US20130066055A1

公开(公告)日：2013-03-14

申请号：US13451950

申请日：2012-04-20

申请人： Hans-Georg Lerchen ,  Lars Linden ,  Sherif El Sheikh ,  Jörg Willuda ,  Charlotte Christine Kopitz ,  Joachim Schuhmacher ,  Simone Greven ,  Christoph Mahlert ,  Beatrix Stelte-Ludwig ,  Sven Golfier ,  Rudolf Beier ,  Iring Heisler ,  Axel Harrenga ,  Karl-Heinz Thierauch ,  Sandra Bruder ,  Heike Petrul ,  Hannah Jörissen ,  Sandra Borkowski

发明人： Hans-Georg Lerchen ,  Lars Linden ,  Sherif El Sheikh ,  Jörg Willuda ,  Charlotte Christine Kopitz ,  Joachim Schuhmacher ,  Simone Greven ,  Christoph Mahlert ,  Beatrix Stelte-Ludwig ,  Sven Golfier ,  Rudolf Beier ,  Iring Heisler ,  Axel Harrenga ,  Karl-Heinz Thierauch ,  Sandra Bruder ,  Heike Petrul ,  Hannah Jörissen ,  Sandra Borkowski

IPC分类号： C07K17/02

CPC分类号： A61K31/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/5355 ,  A61K31/536 ,  A61K31/537 ,  A61K31/5377 ,  A61K39/3955 ,  A61K45/06 ,  A61K47/542 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6859 ,  A61K47/6869 ,  A61K47/6889 ,  C07K5/0205 ,  C07K5/0207 ,  C07K5/06 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/0606 ,  C07K7/02 ,  C07K7/06 ,  C07K16/18 ,  C07K16/28 ,  C07K16/2812 ,  C07K16/2863 ,  C07K16/30 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/565 ,  C07K2317/76

摘要： The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.

摘要翻译： 本申请涉及针对目标C4.4a的N，N-二烷基硫酸钠的新粘合剂 - 药物共轭物（ADC），这些ADC的活性代谢物，制备这些ADC的方法，使用这些ADC 治疗和/或预防疾病，以及使用这些ADC用于制备用于治疗和/或预防疾病的药物，更特别是过度增殖和/或血管生成疾病，例如癌症疾病。 这样的治疗可以作为单一疗法来实施，或者与其它药物组合或进一步的治疗措施。

公开(公告)号：US09649374B2

公开(公告)日：2017-05-16

申请号：US13514992

申请日：2010-11-18

申请人： Christiane Otto ,  Siegmund Wolf ,  Christoph Freiberg ,  Axel Harrenga ,  Simone Greven ,  Mark Trautwein ,  Sandra Bruder ,  Andrea Eicker ,  Andreas Wilmen

发明人： Christiane Otto ,  Siegmund Wolf ,  Christoph Freiberg ,  Axel Harrenga ,  Simone Greven ,  Mark Trautwein ,  Sandra Bruder ,  Andrea Eicker ,  Andreas Wilmen

IPC分类号： A61K39/395 ,  A61K39/00 ,  C07K16/00 ,  C07K16/28 ,  A61K45/06

CPC分类号： A61K39/3955 ,  A61K45/06 ,  A61K2039/505 ,  C07K16/28 ,  C07K16/2866 ,  C07K16/2869 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/76

摘要： The present invention is directed to the neutralizing prolactin receptor antibody 006-H08, as well as maturated forms thereof, and antigen-binding fragments, pharmaceutical compositions containing them and their use in the treatment or prevention of benign disorders and indications mediated by the prolactin receptor such as endometriosis, adenomyosis, non-hormonal female contraception, benign breast disease and mastalgia, lactation inhibition, benign prostate hyperplasia, fibroids, hyper- and normoprolactinemic hair loss, and cotreatment in combined hormone therapy to inhibit mammary epithelial cell proliferation. The antibodies of the invention block prolactin receptor-mediated signaling.

公开(公告)号：US20140141003A1

公开(公告)日：2014-05-22

申请号：US14123517

申请日：2012-05-31

申请人： Christoph Freiberg ,  Christiane Otto ,  Lars Linden ,  Axel Harrenga ,  Mark Trautwein ,  Simone Greven ,  Andreas Wilmen

发明人： Christoph Freiberg ,  Christiane Otto ,  Lars Linden ,  Axel Harrenga ,  Mark Trautwein ,  Simone Greven ,  Andreas Wilmen

IPC分类号： C07K16/28 ,  A61K45/06 ,  A61K39/395

CPC分类号： C07K16/2869 ,  A61K39/3955 ,  A61K45/06 ,  A61K2039/505 ,  C07K16/3015 ,  C07K2317/21 ,  C07K2317/33 ,  C07K2317/34 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/92

摘要： The neutralizing prolactin receptor antibody Mat3, and antigen binding fragments, pharmaceutical compositions containing them and their use in the treatment or prevention of benign disorders and indications mediated by the prolactin receptor such as endometriosis, adenomyosis, non-hormonal female contraception, benign breast disease and mastalgia, lactation inhibition, benign prostate hyperplasia, fibroids, hyper- and normoprolactinemic hair loss, and cotreatment in combined hormone therapy to inhibit mammary epithelial cell proliferation and for the treatment and prevention of antiestrogen-resistant breast cancer. The antibody blocks prolactin receptor-mediated signalling.

摘要翻译： 中和催乳素受体抗体Mat3和抗原结合片段，含有它们的药物组合物及其用于治疗或预防由催乳素受体介导的良性疾病和适应症的用途，例如子宫内膜异位症，子宫腺肌症，非激素雌性避孕，良性乳腺疾病和 乳腺，泌乳抑制，良性前列腺增生，肌瘤，高血压和正常泌乳素脱发，以及联合激素治疗中的联合抑制乳腺上皮细胞增殖和治疗和预防抗雌激素抵抗性乳腺癌。 该抗体阻断催乳素受体介导的信号传导。

公开(公告)号：US20120315276A1

公开(公告)日：2012-12-13

申请号：US13514994

申请日：2010-11-18

申请人： Christiane Otto ,  Siegmund Wolf ,  Christoph Freiberg ,  Axel Harrenga ,  Simone Greven ,  Mark Trautwein ,  Sandra Bruder

发明人： Christiane Otto ,  Siegmund Wolf ,  Christoph Freiberg ,  Axel Harrenga ,  Simone Greven ,  Mark Trautwein ,  Sandra Bruder

IPC分类号： A61K39/395 ,  C12N15/13 ,  C12N15/63 ,  A61P17/14 ,  C12N1/19 ,  C12N1/21 ,  C12P21/02 ,  C07K16/28 ,  C12N5/10

CPC分类号： A61K39/3955 ,  A61K45/06 ,  A61K2039/505 ,  C07K16/28 ,  C07K16/2866 ,  C07K16/2869 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/76

摘要： The present invention is directed to the neutralizing prolactin receptor antibody 002-H08, and antigen binding fragments, pharmaceutical compositions containing them and their use in the treatment or prevention of benign disorders and indications mediated by the prolactin receptor such as endometriosis, adenomyosis, non-hormonal female contraception, benign breast disease and mastalgia, lactation inhibition, benign prostate hyperplasia, fibroids, hyper- and normoprolactinemic hair loss, and cotreatment in combined hormone therapy to inhibit mammary epithelial cell proliferation. The antibodies of the invention block prolactin receptor-mediated signaling.

摘要翻译： 本发明涉及中和催乳素受体抗体002-H08和抗原结合片段，含有它们的药物组合物及其用于治疗或预防由催乳素受体介导的良性疾病和适应症的用途，例如子宫内膜异位症，子宫腺肌症， 激素女性避孕，良性乳腺疾病和乳腺疾病，哺乳期抑制，良性前列腺增生，纤维瘤，高血压和正常泌乳素脱发，联合激素治疗联合抑制乳腺上皮细胞增殖。 本发明的抗体阻断催乳素受体介导的信号传导。

公开(公告)号：US20130129739A1

公开(公告)日：2013-05-23

申请号：US13514996

申请日：2010-11-18

申请人： Christiane Ottto ,  Siegmund Wolf ,  Christoph Freiberg ,  Axel Harrenga ,  Simone Greven ,  Mark Trautwein ,  Sandra Bruder ,  Andrea Eicker ,  Andreas Wilmen

发明人： Christiane Ottto ,  Siegmund Wolf ,  Christoph Freiberg ,  Axel Harrenga ,  Simone Greven ,  Mark Trautwein ,  Sandra Bruder ,  Andrea Eicker ,  Andreas Wilmen

IPC分类号： C07K16/28

CPC分类号： A61K39/3955 ,  A61K45/06 ,  A61K2039/505 ,  C07K16/28 ,  C07K16/2866 ,  C07K16/2869 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/76

摘要： The present invention is directed to the neutralizing prolactin receptor antibody 005-C04, as well as maturated forms thereof, and antigen binding fragments, pharmaceutical compositions containing them and their use in the treatment or prevention of benign disorders and indications mediated by the prolactin receptor such as endometriosis, adenomyosis, non-hormonal female contraception, benign breast disease and mastalgia, lactation inhibition, benign prostate hyperplasia, fibroids, hyper- and normoprolactinemic hair loss, and cotreatment in combined hormone therapy to inhibit mammary epithelial cell proliferation. The antibodies of the invention block prolactin receptor-mediated signaling.

摘要翻译： 本发明涉及中和催乳素受体抗体005-C04及其成熟形式，以及抗原结合片段，含有它们的药物组合物及其用于治疗或预防由催乳素受体介导的良性疾病和适应症的用途，例如 作为子宫内膜异位症，子宫腺肌症，非荷尔蒙女性避孕，良性乳腺疾病和乳腺疾病，哺乳期抑制，良性前列腺增生，肌瘤，高血压和正常泌乳素脱发，联合激素治疗联合抑制乳腺上皮细胞增殖。 本发明的抗体阻断催乳素受体介导的信号传导。

公开(公告)号：US20120321619A1

公开(公告)日：2012-12-20

申请号：US13514789

申请日：2010-12-08

申请人： Lars Linden ,  Yong-Jiang Cao ,  Gabriele Leder ,  Beatrix Stelte-ludwig ,  Axel Harrenga ,  Ricarda Finnern ,  Frank Dittmer ,  Anke Mayer-Bartschmid ,  Juergen Franz ,  Simone Greven ,  Jörg Willuda ,  Jan Tebbe

发明人： Lars Linden ,  Yong-Jiang Cao ,  Gabriele Leder ,  Beatrix Stelte-ludwig ,  Axel Harrenga ,  Ricarda Finnern ,  Frank Dittmer ,  Anke Mayer-Bartschmid ,  Juergen Franz ,  Simone Greven ,  Jörg Willuda ,  Jan Tebbe

IPC分类号： C07K16/30 ,  C12N15/85 ,  A61P35/04 ,  C12P21/08 ,  A61K39/395 ,  C12N1/21 ,  C12N15/13 ,  C12N5/10

CPC分类号： C07K16/30 ,  A61K39/39558 ,  A61K2039/505 ,  C07K16/28 ,  C07K2317/21 ,  C07K2317/33 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/732 ,  C07K2317/77 ,  C07K2317/92

摘要： The present invention provides recombinant antigen-binding regions and antibodies and functional fragments containing such antigen-binding regions that are specific for the membrane-anchored, 29 kDa C4.4a polypeptide, which is over expressed in several tumors, e.g. lung, colorectal, pancreas, prostate, renal and breast cancer. These antibodies, accordingly, can be used to treat these and other disorders and conditions. Antibodies of the invention also can be used in the diagnostics field, as well as for further investigating the role of C4.4a in the progression of disorders associated with cancer. The invention also provides nucleic acid sequences encoding the foregoing antibodies, vectors containing the same, pharmaceutical compositions and kits with instructions for use.

摘要翻译： 本发明提供重组抗原结合区和抗体以及含有对多个肿瘤中过表达的膜锚定的29kDa C4,4a多肽具有特异性的此类抗原结合区的功能片段。 肺，结肠直肠，胰腺，前列腺，肾和乳腺癌。 因此，这些抗体可用于治疗这些和其他病症和病症。 本发明的抗体也可用于诊断领域，以及用于进一步研究C4.4a在与癌症相关疾病进展中的作用。 本发明还提供了编码前述抗体的核酸序列，含有该抗体的载体，药物组合物和具有使用说明书的试剂盒。