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公开(公告)号：US20230212532A1
公开(公告)日：2023-07-06
申请号：US17759954
申请日：2021-02-01
发明人： Oliver KENSCH , Kai THEDE , Petra HELFRICH , Lilly SKALDEN , Ludwig ZORN , Sabine TRENNER , Jens BURMEISTER , Nils KRETSCHMANN , Florian RICHTER , Wayne COCO , Marcus LUDWIG , Dalia BULUT , Frank BERENDES , Jens PILLING , Jakob WAGNER , Ruben LINNHOFF
CPC分类号： C12N9/0071 , C12P33/06 , C12Y114/14001
摘要： The present invention relates to novel recombinant Bacillus megaterium cytochrome P450-monooxygenase (P450-BM3) variants for the C19 hydroxylation of steroids and derivatives thereof or for improved BM3 protein expression. In particular, the present invention also relates to methods and processes using P450-BM3 variants for the production of estrone and estradiol. The invention further relates to nucleotide sequences, constructs and vectors for the expression of these P450-BM3 variants
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公开(公告)号：US20170114070A1
公开(公告)日：2017-04-27
申请号：US15127782
申请日：2015-03-18
发明人： Kai THEDE , Eckhard BENDER , William SCOTT , Anja GIESE , Ludwig ZORN , Ningshu LIU , Ursula MÖNNING , Franziska SIEGEL , Stefan GOLZ , Andrea HÄGEBARTH , Philip LIENAU , Florian PUEHLER , Daniel BASTING , Dirk SCHNEIDER , Manfred MÖWES , Jens GEISLER
IPC分类号： C07D491/08 , A61K31/501 , C07D403/04 , A61K31/506 , C07D237/20 , A61K31/5377 , C07D241/20 , C07D253/07 , A61K31/53 , C07D239/42 , A61K31/497 , A61K31/541 , A61K45/06 , C07C233/54 , C07D295/15 , C07C233/25 , C07C205/45 , C07C229/64 , C07D241/24 , C07C205/59 , C07D401/04
CPC分类号： C07D491/08 , A61K9/0007 , A61K9/0019 , A61K9/0056 , A61K9/08 , A61K9/10 , A61K9/19 , A61K9/2018 , A61K9/205 , A61K9/2054 , A61K9/2063 , A61K9/4858 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K45/06 , C07C205/45 , C07C205/59 , C07C229/64 , C07C233/25 , C07C233/54 , C07D237/20 , C07D239/42 , C07D241/20 , C07D241/24 , C07D241/28 , C07D253/07 , C07D295/15 , C07D401/04 , C07D403/04 , A61K2300/00
摘要： The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20160263122A1
公开(公告)日：2016-09-15
申请号：US14778568
申请日：2014-03-17
发明人： Kai THEDE , William SCOTT , Eckhard BENDER , Stefan GOLZ , Andrea HÄGEBARTH , Philip LIENAU , Florian PUEHLER , Daniel BASTING , Dirk SCHNEIDER , Manfred MOWES , Anja RICHTER , Ludwig ZORN , Ningshu LIU , Ursula MONNING , Franziska SIEGEL
IPC分类号： A61K31/5377 , C07C205/45 , C07D213/75 , C07C233/54 , C07D295/15 , C07C233/15 , C07D213/82 , C07D333/38 , C07D285/135 , C07D295/155 , C07C205/59 , C07C317/44 , C07C229/64 , C07D213/76 , C07D213/73 , C07C255/56 , A61K31/5386 , A61K31/4439 , A61K31/496 , A61K31/433 , A61K31/4418 , A61K31/4995 , A61K31/551 , A61K31/553 , A61K45/06 , C07D277/56
CPC分类号： A61K31/5377 , A61K31/433 , A61K31/4418 , A61K31/4439 , A61K31/496 , A61K31/4995 , A61K31/5386 , A61K31/551 , A61K31/553 , A61K45/06 , C07C205/45 , C07C205/59 , C07C229/64 , C07C233/15 , C07C233/54 , C07C255/56 , C07C317/44 , C07D207/34 , C07D213/73 , C07D213/75 , C07D213/76 , C07D213/82 , C07D231/14 , C07D263/34 , C07D271/06 , C07D271/07 , C07D271/113 , C07D277/46 , C07D277/56 , C07D285/135 , C07D295/15 , C07D295/155 , C07D333/38 , C07D401/12 , C07D417/12 , C07D487/08 , C07D498/08
摘要： The present invention relates to substituted N-(phenyl-heteroaryl)-3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-phenyl-heteroaryl-carboxamides of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease such as cancer, wherein i.a.: LA represents an optionally substituted methylene or ethylene group; LB represents —N(H)—C(═0)- or —C(═0)—N(H)—; R1 represents an optionally substituted 5- to 8-membered heterocycloalkyl, 4- to 10-membered heterocycloalkenyl, aryl, heteroaryl or —N(R7)(Ci-C6-alkyl) group; R2 represents an optionally substituted 5- or 6-membered heteroaryl group; R3 represents an optionally substituted phenyl group.
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![ANALOGUES OF 3-(5-METHYL-1,3-THIAZOL-2-YL)-N-{(1R)-1-[2-(TRIFLUORO-METHYL)PYRIMIDIN-5-YL]ETHYL}BENZAMIDE](/abs-image/US/2023/01/19/US20230013419A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230013419A1
公开(公告)日：2023-01-19
申请号：US17620410
申请日：2020-06-25
发明人： Antje ROTTMANN , Oliver Martin FISCHER , Kai THEDE , Simon Anthony HERBERT , Ursula GANZER , Andrea ROTGERI , Elisabeth POOK
IPC分类号： C07D417/12 , A61P31/12
摘要： The present invention covers P2X3 inhibitor compounds of general formula (I) in which R1 and R2 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 diseases, in particular of neurogenic disorders, as a sole agent or in combination with other active ingredients.
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5.发明申请公开(公告)号：US20180044306A1
公开(公告)日：2018-02-15
申请号：US15552249
申请日：2016-02-16
发明人： Kai THEDE , Eckhard BENDER , William J. SCOTT , Anja GIESE , Ludwig ZORN , Ningshu LIU , Ursula MÖNNING , Franziska SIEGEL , Stefan GOLZ , Andrea HÄGEBARTH , Philip LIENAU , Florian PÜHLER , Daniel BASTING , Dirk SCHNEIDER , Manfred MÖWES , Jens GEISLER
IPC分类号： C07D285/135 , C07D417/04 , A61K31/5377 , A61K45/06 , A61K31/496
CPC分类号： C07D285/135 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20170107212A1
公开(公告)日：2017-04-20
申请号：US15127780
申请日：2015-03-18
发明人： Kai THEDE , Eckhard BENDER , William SCOTT , Anja GIESE , Ludwig ZORN , Ningshu LIU , Ursula MÖNNING , Franziska SIEGEL , Stefan GOLZ , Andrea HÄGEBARTH , Philip LIENAU , Florian PUEHLER , Daniel BASTING , Dirk SCHNEIDER , Manfred MÖWES , Jens GEISLER
IPC分类号： C07D417/14 , A61K31/5377 , C07D417/04 , A61K45/06 , C07D409/04 , A61K31/497 , A61K31/506 , C07D401/04 , A61K31/496
CPC分类号： C07D417/14 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/14 , C07D409/04 , C07D417/04
摘要： The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20160052898A1
公开(公告)日：2016-02-25
申请号：US14778603
申请日：2014-03-20
发明人： Kai THEDE , William Johnston SCOTT , Eckhard BENDER , Stefan GOLZ , Andrea HÄGEBARTH , Philip LIENAU , Florian PUEHLER , Daniel BASTING , Dirk SCHNEIDER , Manfred MÖWES , Anja RICHTER , Ludwig ZORN , Ningshu LIU , Ursula MÖNNING , Franziska SIEGEL
IPC分类号： C07D295/15 , C07D491/08 , C07D498/08 , C07D333/24 , C07D307/54 , C07D491/107 , C07D267/10 , C07D211/42 , C07D211/46 , C07C237/40 , C07D207/12 , C07D231/10 , C07D265/30
CPC分类号： C07D295/15 , C07C233/54 , C07C233/80 , C07C237/40 , C07C237/42 , C07C237/44 , C07C271/24 , C07C317/44 , C07C317/48 , C07C317/50 , C07C323/63 , C07C2601/02 , C07D205/04 , C07D207/12 , C07D211/42 , C07D211/44 , C07D211/46 , C07D231/10 , C07D231/12 , C07D265/30 , C07D267/10 , C07D295/145 , C07D295/26 , C07D307/54 , C07D333/24 , C07D413/12 , C07D491/08 , C07D491/10 , C07D491/107 , C07D498/08
摘要： The present invention relates to substituted N-biphenyl-3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-biphenyl-carboxamides of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disorder, as a sole agent or in combination with other active ingredients.
摘要翻译： 本发明涉及如本文所述和定义的取代的N-联苯-3-乙酰氨基 - 苯甲酰胺和通式（I）的N- [3-（乙酰氨基）苯基] - 联苯 - 甲酰胺，制备所述化合物的方法， 可用于制备所述化合物的中间体化合物，包含所述化合物的药物组合物和组合，以及所述化合物用于制备用于治疗或预防疾病特别是过度增殖性疾病的药物组合物作为唯一试剂或在 与其他活性成分组合。
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8.发明申请公开(公告)号：US20180042931A1
公开(公告)日：2018-02-15
申请号：US15552251
申请日：2016-02-16
发明人： Kai THEDE , Eckhard BENDER , William J. SCOTT , Anja GIESE , Ludwig ZORN , Ningshu LIU , Ursula MÖNNING , Franziska SIEGEL , Stefan GOLZ , Andrea HÄGEBARTH , Philip LIENAU , Florian PÜHLER , Daniel BASTING , Dirk SCHNEIDER , Manfred MÖWES
IPC分类号： A61K31/5377 , A61K45/06 , C07D239/26 , C07D213/40 , C07D231/12 , C07D239/34 , C07D239/42 , C07D213/64 , C07D213/73 , C07D213/61
CPC分类号： A61K31/5377 , A61K45/06 , C07D213/40 , C07D213/61 , C07D213/64 , C07D213/73 , C07D231/12 , C07D239/26 , C07D239/34 , C07D239/42 , C07D403/04
摘要： The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) wherein LA represents *CH2** or *Δ**; wherein indicates the point of attachment to the carbonyl group, and ** indicates the point of attachment to R1; LB represents *N(H)—C(═O)** or *C(═O)—N(H)**; wherein * indicates the point of attachment to R2, and ** indicates the point of attachment to the phenyl group; R1 represents a group selected from: (AA); wherein * indicates the point of attachment to LA, R2 represents: (BB) wherein * indicates the point of attachment to R3, and ** indicates the point of attachment to LB R3 represents a group selected from: (CC); wherein * indicates the point of attachment to R2; R4 and R5 represent a hydrogen atom; and R6 represents a halogen atom or group selected from: —CH3, —O—CH3, —O—CHF2, —O—CF3, and —O-cyclopropyl; to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular, of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.
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9.发明申请公开(公告)号：US20180028507A1
公开(公告)日：2018-02-01
申请号：US15552228
申请日：2016-02-16
发明人： Kai THEDE , Eckhard BENDER , William J. SCOTT , Anja GIESE , Ludwig ZORN , Ningshu LIU , Ursula MÖNNING , Franziska SIEGEL , Stefan GOLZ , Andrea HÄGEBARTH , Philip LIENAU , Florian PÜHLER , Daniel BASTING , Dirk SCHNEIDER , Manfred MÖWES
IPC分类号： A61K31/435 , C07D401/14 , C07D213/75 , C07D401/12 , C07C237/44 , C07D213/73
CPC分类号： A61K31/435 , C07C237/44 , C07D213/73 , C07D213/75 , C07D401/12 , C07D401/14
摘要： The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients, in which: R1 represents a group selected from: C1-C3-alkoxy-C2-C3-alkyl-, (A), (B), (C), (D), (E), (F), (G) or (H); wherein * indicates the point of attachment to the rest of the molecule; R2 represents a group selected from: (I), (J) or (K); wherein * indicates the point of attachment to the rest of the molecule.
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