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1. 发明授权

US08912189B2 Pyridopyrazine derivatives and their use 有权
标题翻译：吡啶并吡嗪衍生物及其用途
公开(公告)号：US08912189B2
公开(公告)日：2014-12-16
申请号：US13439107
申请日：2012-04-04
申请人： Matthias Gerlach , Irene Seipelt , Lars Blumenstein , Gilbert Mueller , Eckhard Guenther , Tilmann Schuster , Michael Teifel
发明人： Matthias Gerlach , Irene Seipelt , Lars Blumenstein , Gilbert Mueller , Eckhard Guenther , Tilmann Schuster , Michael Teifel
IPC分类号： A61K31/4985 , C07D471/04 , A61K31/501 , A61K31/5377
CPC分类号： A61K31/4985 , A61K31/501 , A61K31/5377 , C07D471/04
摘要： The present invention provides new pyridopyrazine compounds of Formula (I) which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.
摘要翻译：本发明提供了新的式（I）吡啶并吡嗪化合物，其适用于治疗或预防由哺乳动物，特别是人类中的信号转导途径和/或酶介导和/或调节的生理和/或病理生理状态。

2. 发明授权

US08658615B2 Prohibitin as target for cancer therapy 失效
标题翻译： Prohibitin作为癌症治疗的靶标
公开(公告)号：US08658615B2
公开(公告)日：2014-02-25
申请号：US13275666
申请日：2011-10-18
申请人： Krishnaraj Rajalingam , Thomas Rudel
发明人： Krishnaraj Rajalingam , Thomas Rudel
IPC分类号： C12N15/113 , C07H21/04
CPC分类号： C12N15/1135 , C12N2310/14 , G01N33/5011 , G01N2333/4704 , G01N2333/9121 , G01N2500/10
摘要： The present invention relates to pharmaceutical compositions comprising inhibitors of Prohibitin (PHB) for the prevention or/and treatment of hyperproliferative disorders.
摘要翻译：本发明涉及包含用于预防或/或治疗过度增殖性疾病的抑制剂（PHB）抑制剂的药物组合物。

3. 发明申请

US20120171159A1 NON-PATHOGENIC AND/OR ATTENUATED BACTERIA CAPABLE OF INDUCING APOPTOSIS IN MACROPHAGES, PROCESS OF MANUFACTURING AND USES THEREOF 失效
标题翻译：非致病性和/或破坏性细菌可诱发巨噬细胞病变，制造过程及其用途
公开(公告)号：US20120171159A1
公开(公告)日：2012-07-05
申请号：US13364437
申请日：2012-02-02
申请人： Joachim Fensterle , Katharina Galmbacher , Ulf Rapp , Werner Goebel , Christian Hotz
发明人： Joachim Fensterle , Katharina Galmbacher , Ulf Rapp , Werner Goebel , Christian Hotz
IPC分类号： A61K35/74 , A61P35/02 , A61P31/00 , A61P3/10 , A61P31/04 , A61P31/16 , A61P29/00 , A61P37/00 , A61P35/00 , A61P31/12
CPC分类号： C12N1/20 , A61K35/74 , C12R1/42 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/483
摘要： The invention relates to an non-pathogenic and/or attenuated bacterium which is capable of inducing apoptosis in macrophages.
摘要翻译：本发明涉及能诱导巨噬细胞凋亡的非致病和/或减毒细菌。

4. 发明授权

US08202883B2 Substituted pyrido[2,3-b]pyrazine compounds as modulators of tyrosine kinases 失效
标题翻译：取代的吡啶并[2,3-b]吡嗪化合物作为酪氨酸激酶的调节剂
公开(公告)号：US08202883B2
公开(公告)日：2012-06-19
申请号：US12117942
申请日：2008-05-09
申请人： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
发明人： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
IPC分类号： A61K31/44
CPC分类号： C07D471/04
摘要： The invention relates to pyrido[2,3-b]pyrazine compounds of formulae (Ia) and (Ib) which have activity to the modulation of misdirected cellular signal transduction processes such as tyrosine kinases, serine/threonine kinases and/or lipid kinases, their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations:
摘要翻译：本发明涉及式（Ia）和（Ib）的吡啶并[2,3-b]吡嗪化合物，其具有调节错误定向的细胞信号转导过程如酪氨酸激酶，丝氨酸/苏氨酸激酶和/或脂质激酶的活性，它们作为药物的制备和用途，特别是用于治疗基于病理性细胞增殖的恶性疾病和其它病症：

5. 发明授权

US08148546B2 Tetrahydrocarbazole derivatives as ligands of G-protein coupled receptors 有权
标题翻译：四氢咔唑衍生物作为G蛋白偶联受体的配体
公开(公告)号：US08148546B2
公开(公告)日：2012-04-03
申请号：US12109479
申请日：2008-04-25
申请人： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
发明人： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
IPC分类号： C07D209/82 , A61K31/403
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827
摘要： The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
摘要翻译：本发明提供了根据式（I）的新型四氢咔唑化合物作为G蛋白偶联受体（GPCR）的配体，其可用于治疗和/或预防由GPCR介导的哺乳动物的生理和/或病理状况或生理和/ /或可以通过调节这些受体来治疗的病理状况。

6. 发明授权

US08008324B2 Indole derivatives and their use as medicament 失效
公开(公告)号：US08008324B2
公开(公告)日：2011-08-30
申请号：US12074845
申请日：2008-03-06
申请人： Peter Emig , Gerald Bacher , Dietmar Reichert , Silke Basner , Beate Aue , Bernd Nickel , Eckhard Gunther
发明人： Peter Emig , Gerald Bacher , Dietmar Reichert , Silke Basner , Beate Aue , Bernd Nickel , Eckhard Gunther
IPC分类号： A61K31/67 , A61K31/445 , C07D215/38 , C07D215/36 , C07D401/06
CPC分类号： C07D401/12 , C07D209/18
摘要： The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.

7. 发明申请

US20100317580A1 CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF 有权
公开(公告)号：US20100317580A1
公开(公告)日：2010-12-16
申请号：US12728050
申请日：2010-03-19
申请人： Eckhard GUENTHER , Olaf Schaefer , Michael Teifel , Klaus Paulini
发明人： Eckhard GUENTHER , Olaf Schaefer , Michael Teifel , Klaus Paulini
IPC分类号： A61K38/09 , A61K31/424 , A61K38/31 , A61P35/00 , A61P35/02
CPC分类号： C12P17/188 , C07D498/18 , C07D498/22 , C07K7/23 , C07K14/6555
摘要： The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.

8. 发明授权

US07696149B2 Pharmaceutical administration form for peptides, process for its preparation, and use 失效
标题翻译：肽的药物管理形式，其制备方法和用途
公开(公告)号：US07696149B2
公开(公告)日：2010-04-13
申请号：US11028875
申请日：2005-01-04
申请人： Horst Bauer , Michael Damm , Werner Sarlikiotis
发明人： Horst Bauer , Michael Damm , Werner Sarlikiotis
IPC分类号： A61K38/00 , A61K51/00 , B01A19/00
CPC分类号： A61K47/40 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K47/12 , A61K47/26 , Y10S514/80
摘要： A method for preventing aggregation of an LHRH antagonist in a pharmaceutical composition. The method comprises combining the LHRH antagonist in the form of an acetate, gluconate, glucuronate, lactate, citrate, ascorbate, benzoate or phosphate salt and at least one of the acids for forming the salts in free acid form.
摘要翻译：一种用于预防药物组合物中LHRH拮抗剂聚集的方法。该方法包括将乙酸盐，葡萄糖酸盐，葡萄糖醛酸盐，乳酸盐，柠檬酸盐，抗坏血酸盐，苯甲酸盐或磷酸盐形式的LHRH拮抗剂与形成游离酸形式的盐的至少一种酸组合。

9. 发明申请

US20090220459A1 NON-PATHOGENIC AND/OR ATTENUATED BACTERIA CAPABLE OF INDUCING APOPTOSIS IN MACROPHAGES, PROCESS OF MANUFACTURING AND USES THEREOF 审中-公开
标题翻译：非致病性和/或破坏性细菌可诱发巨噬细胞病变，制造过程及其用途
公开(公告)号：US20090220459A1
公开(公告)日：2009-09-03
申请号：US12361843
申请日：2009-01-29
申请人： Joachim FENSTERLE , Katharina Galmbacher , Ulf Rapp , Werner Goebel , Christian Hotz
发明人： Joachim FENSTERLE , Katharina Galmbacher , Ulf Rapp , Werner Goebel , Christian Hotz
IPC分类号： A61K45/00 , C12N15/74 , C12N1/20 , A61P35/00
CPC分类号： C12N1/20 , A61K35/74 , C12R1/42 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/483
摘要： The invention relates to an non-pathogenic and/or attenuated bacterium which is capable of inducing apoptosis in macrophages.
摘要翻译：本发明涉及能诱导巨噬细胞凋亡的非致病和/或减毒细菌。

10. 发明授权

US07393834B2 LHRH-antagonists in the treatment of fertility disorders 有权
标题翻译： LHRH拮抗剂治疗生育障碍
公开(公告)号：US07393834B2
公开(公告)日：2008-07-01
申请号：US10661780
申请日：2003-09-15
申请人： Philippe Bouchard , Rene Frydman , Paul Devroey , Klaus Diedrich , Jurgen Engel
发明人： Philippe Bouchard , Rene Frydman , Paul Devroey , Klaus Diedrich , Jurgen Engel
IPC分类号： A61K38/09 , A61K31/551 , A61K31/4743
CPC分类号： A61K38/09 , C12M21/06
摘要： A method of treating infertility disorders by 1) administering an LH-RH antagonist, preferably Cetrorelix, in amounts to selectively suppress endogenous LH but not FSH secretion and 2) inducing follicle growth by administration of exogenous gonadotropin. The selective suppression OF LH allows FSH secretion to be at natural levelS thereby not affecting individual estrogen development. The LH-RH antagonist can be given as a single or dual subcutaneous dose in the range of 1 mg to 10 mg, preferably 2 mg-6 mg. In multiple dosing-posology, LH-RH antagonist can be administered subcutaneously in an amount in the range of 0.1 to 0.5 mg of LH-RH antagonist/day. LH-RH antagonist is applied starting cycle day 1 to 10, preferably on day 4 to 8, and ovulation can be induced between day 9 and 20 of the menstruation cycle by administering rec. LH, native LH-RH, LH-RH agonist or by HCG. In addition rec. LH, native LH-RH or LH-RH agonist can be given to avoid hyperstimulation syndrome and native LH-RH or a LH-RH agonist can be administered to avoid luteal phase stimulation by neutralizing the negative effects of HCG.
摘要翻译：一种通过以下方式治疗不育症：1）以选择性抑制内源性LH而不是FSH分泌的量施用LH-RH拮抗剂，优选Cetrorelix; 2）通过施用外源性促性腺激素诱导卵泡生长。选择性抑制LH允许FSH分泌处于自然水平，从而不影响个体雌激素的发育。 LH-RH拮抗剂可以以1mg至10mg，优选2mg-6mg范围内的单次或双次皮下给药。在多剂量剂量学中，LH-RH拮抗剂可以以0.1-0.5mg LH-RH拮抗剂/天的量皮下施用。 LH-RH拮抗剂在第1至10天开始循环，优选在第4至8天施用，并且可以在月经周期的第9至20天之间通过施用rec来诱导排卵。 LH，天然LH-RH，LH-RH激动剂或HCG。另外rec。可以给予LH，天然LH-RH或LH-RH激动剂以避免过度刺激综合征，并且可以施用天然LH-RH或LH-RH激动剂，以通过中和HCG的负面作用来避免黄体期刺激。

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