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11. 发明申请

US20180319807A2 [8-(PHENYLSULFONYL)-3,8-DIAZABICYCLO[3.2.1]OCT-3-YL](1H-1,2,3-TRIAZOL-4-YL)METHANONES 审中-公开
公开(公告)号：US20180319807A2
公开(公告)日：2018-11-08
申请号：US15596383
申请日：2017-05-16
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： Marcus KOPPITZ , Holger SIEBENEICHER , Holger STEUBER , Antonius TER LAAK , Reinhard NUBBEMEYER , Antje ROTTMANN , Horst IRLBACHER , Benjamin BADER , Michaele PETERS , Andrea WAGENFELD , Ildiko TEREBESI
IPC分类号： C07D487/08 , A61K31/4995 , A61K45/06
CPC分类号： C07D487/08 , A61K31/4995 , A61K45/06
摘要： The present invention covers [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of disorders, in particular of gynecological disorders, hyperproliferative disorders, metabolic disorders, or inflammatory disorders as a sole agent or in combination with other active ingredients.

12. 发明申请

US20170342082A1 [8-(PHENYLSULFONYL)-3,8-DIAZABICYCLO[3.2.1]OCT-3-YL](1H-1,2,3-TRIAZOL-4-YL)METHANONES 审中-公开
公开(公告)号：US20170342082A1
公开(公告)日：2017-11-30
申请号：US15596383
申请日：2017-05-16
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： Marcus KOPPITZ , Holger SIEBENEICHER , Holger STEUBER , Antonius TER LAAK , Reinhard NUBBEMEYER , Antje ROTTMANN , Horst IRLBACHER , Benjamin BADER , Michaele PETERS , Andrea WAGENFELD , Ildiko TEREBESI
IPC分类号： C07D487/08 , A61K45/06 , A61K31/4995
CPC分类号： C07D487/08 , A61K31/4995 , A61K45/06
摘要： The present invention covers [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of disorders, in particular of gynecological disorders, hyperproliferative disorders, metabolic disorders, or inflammatory disorders as a sole agent or in combination with other active ingredients.

13. 发明公开

US20230174508A1 SUBSTITUTED INDAZOLES, METHODS FOR THE PRODUCTION THEREOF, PHARMACEUTICAL PREPARATIONS THAT CONTAIN SAID NEW SUBSTITUTED INDAZOLES, AND USE OF SAID NEW SUBSTITUTED INDAZOLES TO PRODUCE DRUGS 审中-公开
公开(公告)号：US20230174508A1
公开(公告)日：2023-06-08
申请号：US17869673
申请日：2022-07-20
申请人： Bayer Pharma Aktiengesellschaft
发明人： Ulrich BOTHE , Holger SIEBENEICHER , Nicole SCHMIDT , Reinhard NUBBEMEYER , Ulf BÖMER , Judith GÜNTHER , Holger STEUBER , Martin LANGE , Christian STEGMANN , Andreas SUTTER , Alexandra RAUSCH , Christian FRIEDRICH , Peter HAUFF
IPC分类号： C07D401/12 , C07F7/18 , A61P19/02 , A61K31/4439 , C07D405/14
CPC分类号： C07D401/12 , C07F7/1804 , A61P19/02 , A61K31/4439 , C07D405/14
摘要： The present application relates to novel substituted indazoles, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis and endometriosis-associated pain and other endometriosis-associated symptoms such as dysmenorrhoea, dyspareunia, dysuria and dyschezia, of lymphoma, rheumatoid arthritis, spondyloarthritis (especially psoriatic spondyloarthritis and Bekhterev's disease), lupus erythematosus, multiple sclerosis, macular degeneration, COPD, gout, fatty liver disorders, insulin resistance, neoplastic disorders and psoriasis.

14. 发明申请

US20220204474A1 SUBSTITUTED INDAZOLES USEFUL FOR TREATMENT AND PREVENTION OF ALLERGIC AND/OR INFLAMMATORY DISEASES IN ANIMALS 有权
公开(公告)号：US20220204474A1
公开(公告)日：2022-06-30
申请号：US17570550
申请日：2022-01-07
申请人： Bayer Pharma Aktiengesellschaft
发明人： Gerald BEDDIES , Adrian FOSTER , Ulrich BOTHE , Nicole SCHMIDT , Ulf BOEMER , Reinhard NUBBEMEYER , Maria De Lourdes MOTTIER
IPC分类号： C07D401/12 , C07D405/14
摘要： The present application relates to the use of substituted indazoles for treatment and/or prophylaxis of allergic and/or inflammatory diseases in animals, especially for treatment and/or prophylaxis of atopic dermatitis, Flea Allergy Dermatitis, inflammatory bowel disease, osteoarthritis and inflammatory pain, non-infectious recurrent airway disease, insect hypersensitivity, asthma, respiratory disease, mastitis and endometritis in animals.

15. 发明申请

US20190233395A1 SUBSTITUTED INDAZOLES, METHODS FOR THE PRODUCTION THEREOF, PHARMACEUTICAL PREPARATIONS THAT CONTAIN SAID NEW SUBSTITUTED INDAZOLES, AND USE OF SAID NEW SUBSTITUTED INDAZOLES TO PRODUCE DRUGS 审中-公开
公开(公告)号：US20190233395A1
公开(公告)日：2019-08-01
申请号：US16377025
申请日：2019-04-05
申请人： Bayer Pharma Aktiengesellschaft
发明人： Ulrich BOTHE , Holger SIEBENEICHER , Nicole SCHMIDT , Reinhard NUBBEMEYER , Ulf BÖMER , Judith GÜNTHER , Holger STEUBER , Martin LANGE , Christian STEGMANN , Andreas SUTTER , Alexandra RAUSCH , Christian FRIEDRICH , Peter HAUFF
IPC分类号： C07D401/12 , C07F7/18 , A61P19/02 , A61K31/4439 , C07D405/14
摘要： The present application relates to novel substituted indazoles, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis and endometriosis-associated pain and other endometriosis-associated symptoms such as dysmenorrhoea, dyspareunia, dysuria and dyschezia, of lymphoma, rheumatoid arthritis, spondyloarthritis (especially psoriatic spondyloarthritis and Bekhterev's disease), lupus erythematosus, multiple sclerosis, macular degeneration, COPD, gout, fatty liver disorders, insulin resistance, neoplastic disorders and psoriasis.

16. 发明申请

US20180338980A1 AROMATIC SULFONAMIDE DERIVATIVES 审中-公开
公开(公告)号：US20180338980A1
公开(公告)日：2018-11-29
申请号：US15580830
申请日：2016-06-07
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： Stefan WERNER , Stefanie MESCH , Nico BRÄUER , Elisabeth POOK , Henrik DAHLLÖF , Reinhard NUBBEMEYER , Maren OSMERS , Bernd KALTHOF
IPC分类号： A61K31/5377 , C07D413/10 , A61K31/444 , A61K31/496 , C07D401/10
摘要： Substituted aromatic sulfonamides of formula (I) pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.

17. 发明申请

US20180289685A1 COMBINATIONS OF INHIBITORS OF IRAK4 WITH INHIBITORS OF BTK 审中-公开
公开(公告)号：US20180289685A1
公开(公告)日：2018-10-11
申请号：US15570212
申请日：2016-04-29
申请人： Bayer Pharma Aktiengesellschaft
发明人： Ulrich BOTHE , Antje Margret WENGNER , Holger SIEBENEICHER , Nicole SCHMIDT , Reinhard NUBBEMEYER , Ulf BÖMER , Judith GÜNTHER , Holger STEUBER , Martin LANGE , Christian STEGMANN , Andreas SUTTER , Roland NEUHAUS
IPC分类号： A61K31/4439 , A61K31/519 , A61K45/06 , A61P35/00
摘要： The present application relates to novel combinations of at least two components, component A and component B: ⋅component A is an IRAK4-inhibiting compound of the formula (I) as defined herein, or a diastereomer, an enantiomer, a metabolite, a salt, a solvate or a solvate of a salt thereof; ⋅component B is a BTK-inhibiting compound, or a pharmaceutically acceptable salt thereof; and, optionally, ⋅one or more components C which are pharmaceutical products; in which one or two of the above-defined compounds A and B are optionally present in pharmaceutical formulations ready for simultaneous, separate or sequential administration, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis, lymphoma, macular degeneration, COPD, neoplastic disorders and psoriasis.

18. 发明申请

US20160052936A1 SPIROINDOLINE DERIVATIVES FOR USE AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：用于促性腺激素释放激素受体拮抗剂的螺旋体衍生物
公开(公告)号：US20160052936A1
公开(公告)日：2016-02-25
申请号：US14783458
申请日：2014-04-08
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： Olaf PANKNIN , Sven RING , Stefan BÄURLE , Andrea WAGENFELD , Reinhard NUBBEMEYER , Katrin NOWAK-REPPEL , Gernot LANGER
IPC分类号： C07D495/10
CPC分类号： C07D495/10
摘要： Spiroindoline derivatives, processes for their preparation and pharmaceutical compositions thereof, their use for the treatment of diseases, and their use for the manufacture of medicaments for the treatment of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine leiomyoma (fibroids), polycystic ovarian disease, menorrhagia, dysmenorrhea, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception, infertility and assisted reproductive therapy such as in vitro fertilization. The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
摘要翻译：螺二氢吲哚衍生物，其制备方法及其药物组合物，其用于治疗疾病的用途及其用于制备用于治疗男性和女性中的疾病，特别是性激素相关疾病的药物，特别是那些选自子宫内膜异位症，子宫平滑肌瘤（子宫肌瘤），多囊性卵巢疾病，月经过多，痛经，多毛症，早熟性青春期，性腺类固醇依赖性肿瘤，如前列腺癌，乳腺和卵巢癌，性腺垂体腺瘤，睡眠呼吸暂停，易怒肠综合征，经前期综合征，良性前列腺肥大，避孕，不育症和辅助生殖治疗如体外受精。本申请特别涉及作为促性腺激素释放激素（GnRH）受体拮抗剂的螺二氢吲哚衍生物。

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