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公开(公告)号：US20200181171A1
公开(公告)日：2020-06-11
申请号：US16635356
申请日：2018-07-02
Applicant: MERCK PATENT GMBH
Inventor： Eva-Maria TANZER , Kai SCHIEMANN , Markus KLEIN
IPC: C07D513/04 , C07D519/00
Abstract: The invention relates to thiazolopyridine derivatives of the general formula I, and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
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公开(公告)号：US20170348380A1
公开(公告)日：2017-12-07
申请号：US15624777
申请日：2017-06-16
Applicant: Merck Patent GmbH
Inventor： Markus KLEIN , Ralf WODOPIA , Hans GUEHRING , Sven LINDEMANN
CPC classification number: A61K38/08 , A61K9/0019
Abstract: The present invention relates to pharmaceutical preparations and medicaments for intraarticular administration, comprising pepstatin, and to the preparation and use thereof, in particular in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia, particularly preferably in arthrosis.
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公开(公告)号：US20160228493A1
公开(公告)日：2016-08-11
申请号：US15041712
申请日：2016-02-11
Applicant: Merck Patent GmbH
Inventor： Markus KLEIN , Christos TSAKLAKIDIS , Hans GUEHRING , Brigitta LEUTHNER
IPC: A61K38/08 , C07K7/06 , C07K5/10 , A61K38/07 , C07K5/117 , A61K38/06 , C07K5/062 , A61K38/05 , C07K5/087 , C07K1/107 , C07K5/083
CPC classification number: A61K38/08 , A61K38/05 , A61K38/06 , A61K38/07 , A61K45/06 , C07K1/1075 , C07K5/0205 , C07K5/06043 , C07K5/0808 , C07K5/0812 , C07K5/1002 , C07K5/101 , C07K5/1024 , C07K7/06
Abstract: The present invention relates to compounds of the formula (I) and in particular medicaments comprising at least one compound of the formula (I) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological states in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.
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4.发明申请公开(公告)号：US20160175381A1
公开(公告)日：2016-06-23
申请号：US14910317
申请日：2014-07-07
Applicant: MERCK PATENT GMBH
Inventor： Markus KLEIN , Ralf WODOPIA , Hans GUEHRING , Sven LINDEMANN
CPC classification number: A61K38/08 , A61K9/0019
Abstract: The present invention relates to pharmaceutical preparations and medicaments for intraarticular administration, comprising pepstatin, and to the preparation and use thereof, in particular in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia, particularly preferably in arthrosis.
Abstract translation: 本发明涉及用于关节内给药的药物制剂和药物，包括胃酶抑素，以及其制备和用途，特别是治疗和/或预防关节炎，创伤性软骨损伤，关节炎，疼痛，异常性疼痛或痛觉过敏，特别优选 在关节病。
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公开(公告)号：US20200207720A1
公开(公告)日：2020-07-02
申请号：US16640490
申请日：2018-08-20
Applicant: Merck Patent GmbH
Inventor： Eva-Maria TANZER , Kai SCHIEMANN , Markus KLEIN
IPC: C07D235/30 , C07D401/12 , C07D413/14 , C07D403/12 , C07D413/04 , C07D405/04 , C07D403/10 , C07D405/14 , C07D471/04 , C07D491/107 , C07D491/113 , C07D498/10 , C07D471/10 , C07D417/14 , C07D403/04 , A61P35/04 , C07D491/048 , C07D491/052
Abstract: The invention relates to benzimidazole derivatives of the general formula I, and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
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Patent Agency Ranking
公开(公告)号：US20170081361A1
公开(公告)日：2017-03-23
申请号：US15364598
申请日：2016-11-30
Applicant: Merck Patent GmbH
Inventor： Christos TSAKLAKIDIS , Markus KLEIN
Abstract: The present invention relates to compounds of the formula (I) and in particular to medicaments comprising at least one compound of the formula (I) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries arthritis, pain, allodynia or hyperalgesia.
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公开(公告)号：US20160145297A1
公开(公告)日：2016-05-26
申请号：US14897718
申请日：2014-05-14
Applicant: MERCK PATENT GMBH
Inventor： Markus KLEIN
CPC classification number: C07K5/0207 , A61K9/0019 , A61K38/06 , A61K38/07 , A61K38/08 , C07K7/02
Abstract: The present invention relates to compounds of the formula I and in particular medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.
Abstract translation: 本发明涉及式I化合物，特别是包含至少一种式I化合物的药物，其用于治疗和/或预防涉及组织蛋白酶D的触发中的生理和/或病理生理状况，在 特别用于治疗和/或预防关节炎，创伤性软骨损伤，关节炎，疼痛，异常性疼痛或痛觉过敏。
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公开(公告)号：US20220306588A1
公开(公告)日：2022-09-29
申请号：US17693527
申请日：2022-03-14
Applicant: Merck Patent GmbH
Inventor： Eva-Maria TANZER , Kai SCHIEMANN , Markus KLEIN
IPC: C07D235/30 , A61P35/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D498/10
Abstract: The invention relates to benzimidazole derivatives of the general formula I, and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
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9.发明申请SUBSTITUTED CARBOXYLIC ACID DERIVATIVES AS AGGRECANASE INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS 有权取代的羧酸衍生物作为治疗OSTEOARTHRITIS的AGGRECANASE抑制剂公开(公告)号：US20150368188A1
公开(公告)日：2015-12-24
申请号：US14765913
申请日：2014-01-16
Applicant: MERCK PATENT GMBH
Inventor： Markus KLEIN , Sven LINDEMANN
IPC: C07C237/22 , C07D277/56 , A61K31/426 , C07D213/40 , A61K31/4406 , C07D231/12 , A61K31/415 , C07D211/66 , A61K31/451 , C07D295/215 , A61K31/495 , C07D277/30 , C07D241/12 , A61K31/4965 , C07D241/24 , C07D305/08 , A61K31/337 , A61K31/197
CPC classification number: C07C237/22 , A61K31/197 , A61K31/337 , A61K31/415 , A61K31/426 , A61K31/4406 , A61K31/451 , A61K31/495 , A61K31/4965 , C07C233/83 , C07D211/34 , C07D211/66 , C07D213/40 , C07D213/56 , C07D213/81 , C07D213/82 , C07D231/12 , C07D233/64 , C07D241/12 , C07D241/24 , C07D277/30 , C07D277/56 , C07D295/215 , C07D305/08
Abstract: The present invention relates to compounds of the formula I and in particular medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological states in the triggering of which ADAMTS5 is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, hepatocirrhosis, traumatic cartilage injuries, pain, allodynia or hyperalgesia.
Abstract translation: 本发明涉及式I化合物，特别是包含至少一种式I化合物的药物，其用于治疗和/或预防涉及ADAMTS5的触发中的生理和/或病理生理状态，特别是 用于治疗和/或预防骨关节炎，肝硬化，创伤性软骨损伤，疼痛，异常性疼痛或痛觉过敏。
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10.发明申请2 AMINO-3,4-DIHYDRCQUINAZOLINE DERIVATIVES AND THE USE THEREOF AS CATHEPSIN D INHIBITORS 有权2氨基-3,4-二氢喹啉酮衍生物及其作为CATHEPSIN D抑制剂的用途公开(公告)号：US20150361053A1
公开(公告)日：2015-12-17
申请号：US14768252
申请日：2014-01-20
Applicant: MERCK PATENT GMBH
Inventor： Markus KLEIN , Christos TSAKLAKIDIS
IPC: C07D239/84 , C07D403/06 , A61K31/5377 , C07D239/95 , C07C331/28 , A61K31/538 , C07C213/02 , C07C201/12 , C07C209/22 , C07C209/36 , A61K31/517 , C07D413/06
CPC classification number: C07D239/84 , A61K31/517 , A61K31/5377 , A61K31/538 , C07C201/12 , C07C209/22 , C07C209/36 , C07C213/02 , C07C331/28 , C07D239/95 , C07D403/06 , C07D413/06
Abstract: The present invention relates to compounds of the formula (I) and in particular to medicaments comprising at least one compound of the formula (I) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.
Abstract translation: 本发明涉及式（I）化合物，特别涉及包含至少一种式（I）化合物的药物，用于治疗和/或预防触发组织蛋白酶的生理和/或病理生理条件 D涉及，特别是用于治疗和/或预防骨关节炎，创伤性软骨损伤，关节炎，疼痛，异常性疼痛或痛觉过敏。
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