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1. 发明专利

BR112019016497A2 2-heteroaril-3-oxo-2,3-di-hidropiridazina-4-carboxamidas para o tratamento de câncer. 未知
公开(公告)号：BR112019016497A2
公开(公告)日：2022-05-10
申请号：BR112019016497
申请日：2018-02-02
申请人： BAYER AG , BAYER PHARMA AG
发明人： BADER BENJAMIN , KOBER CHRISTINA , STÖCKIGT DETLEF , IRLBACHER HORST , RÖSE LARS , GUTCHER LLONA , ZORN LUDWIG , PLATTEN MICHAEL , SCHMEES NORBERT , CARRETERO RAFAEL , RÖHN ULRIKE
IPC分类号： C07D237/04 , A61K31/501 , A61P35/00 , C07D237/24 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14
摘要： 2-heteroaril-3-oxo-2,3-di-hidropiridazina-4-carboxamidas para o tratamento de câncer. a presente invenção abrange os compostos 2-heteroaril-3-oxo-2,3-di-hidropiridazina-4-carboxamida da fórmula geral (i): (i) em que x, r1, r2, r3, r4 e r5 são como definidos neste documento, aos métodos de preparação dos compostos citados, aos compostos intermediários aplicáveis para a preparação dos compostos citados, às composições farmacêuticas e às combinações que consistem nos compostos citados para a fabricação de composições farmacêuticas para tratamento ou profilaxia de doenças, em particular de câncer ou condições com respostas imunes desreguladas ou outras desordens associadas à sinalização de ahr aberrante, como um agente isolado ou em combinação com outros agentes ativos.

2. 发明专利

CO2022001257A2 1,2,4]triazolo[1,5-c]quinazolin-5-aminas 未知
公开(公告)号：CO2022001257A2
公开(公告)日：2022-03-08
申请号：CO2022001257
申请日：2022-02-08
申请人： BAYER PHARMA AG , BAYER AG
发明人： BADER BENJAMIN , ZORN LUDWIG , BOTHE ULRICH , GÜNTHER JUDITH , PLATTEN MICHAEL , RÖSE LARS , KOBER CHRISTINA , LEFRANC JULIEN , SCHMEES NORBERT , MEIER ROBIN MICHAEL , HERBERT SIMON ANTHONY , GUTCHER ILONA , STÖCKIGT DETLEF , GORJÁNÁCZ MÁTYÁS , BUCHMANN BERND , BÖHME STEPHAN , BAUMANN DANIEL
IPC分类号： A61P35/00 , C07D487/04 , C07D519/00
摘要： La presente invención comprende compuestos de [1,2,4]triazolo[1,5-c]quinazolin-5-amina de la fórmula general (I): (I) 5 en donde R1, R2, R3, R4, R5, R6, R7 y R8 son como se definen en la presente, métodos para la preparación de dichos compuestos, compuestos intermedios útiles para la preparación de dichos compuestos, composiciones farmacéuticas y combinaciones que comprenden dichos compuestos y el uso de dichos compuestos para la elaboración de composiciones farmacéuticas para el 10 tratamiento o la profilaxis de enfermedades, en especial de cáncer o afecciones con respuestas inmunes desreguladas u otros trastornos asociados con la señalización anormal de AHR, como un único agente o en combinación con otros ingredientes activos.

6. 发明专利

PE20220967A1 [1,2,4] TRIAZOLO [1,5-C] QUINAZOLIN-5-AMINAS 未知
公开(公告)号：PE20220967A1
公开(公告)日：2022-06-10
申请号：PE2022000229
申请日：2020-08-10
申请人： BAYER AG , BAYER PHARMA AG
发明人： LEFRANC JULIEN , SCHMEES NORBERT , ZORN LUDWIG , MEIER ROBIN MICHAEL , HERBERT SIMON ANTHONY , GUNTHER JUDITH , GUTCHER ILONA , ROSE LARS , BADER BENJAMIN , STOCKIGT DETLEF , GORJANACZ MATYAS , KOBER CHRISTINA , BUCHMANN BERND , BOHME STEPHAN , BOTHE ULRICH , PLATTEN MICHAEL , BAUMANN DANIEL
IPC分类号： A61P35/00 , C07D487/04 , C07D519/00
摘要： La presente invencion esta referida a compuestos derivados de [1,2,4]triazolo[1,5-c]quinazolin-5-amina de la formula general (I); en donde R1 es fenilo o heteroarilo, opcionalmente sustituidos; R2 es hidrogeno, alquilo-C1-C4, haloalquilo-C1-C4 o cicloalquilo-C3-C6; R3 es hidrogeno, alquilo-C1-C6, fenilo o fenil-alquilo-C1-C3 donde el grupo alquilo-C1-C6 esta opcionalmente sustituido; R4 es hidroxi, alcoxi-C1-C4 o -NR11R12, o R2 y R4 juntos representan -C2-C5-alcanodiilo-X1- , -C1-C2-alcanodiilo-X2- para formar un anillo de 5- a 9- miembros; R5 a R8 son, independientemente, hidrogeno, halogeno, ciano, hidroxi, alquilo-C1-C4, alcoxi-C1-C4, haloalquilo-C1-C4, entre otros. Un compuesto seleccionado es (3S)-3-[(2-fenil[1,2,4]triazolo[1,5-c]quinazolin-5-il)amino]azepan-2-ona. Dichos compuestos son inhibidores de AHR (receptor de hidrocarburos de arilo). Tambien divulga metodos de preparacion, compuestos intermedios, composiciones farmaceuticas y combinaciones que comprenden dichos compuestos; siendo utiles para el tratamiento o la profilaxis de enfermedades, en especial de cancer o afecciones con respuestas inmunes desreguladas u otros trastornos asociados con la senalizacion anormal de AHR.

7. 发明专利

MA47447B1 2-hétéroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides pour le traitement du cancer 未知
公开(公告)号：MA47447B1
公开(公告)日：2021-02-26
申请号：MA47447
申请日：2018-02-02
申请人： BAYER PHARMA AG , BAYER AG , DEUTSCHES KREBSFORSCH
发明人： SCHMEES NORBERT , RÖSE LARS , ZORN LUDWIG , RÖHN ULRIKE , STÖCKIGT DETLEF , BADER BENJAMIN , IRLBACHER HORST , KOBER CHRISTINA , CARRETERO RAFAEL , PLATTEN MICHAEL , GUTCHER ILONA
IPC分类号： A61K31/501 , A61P35/00 , C07D237/04 , C07D237/24 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14
摘要： La présente invention concerne des composés 2-hétéroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide de formule générale (i), dans laquelle x, r1, r2, r3, r4 et r5 sont tels que définis dans la description. L'invention concerne également des procédés de préparation desdits composés, des composés intermédiaires utiles pour préparer lesdits composés, des compositions et des combinaisons pharmaceutiques comprenant lesdits composés, et l'utilisation desdits composés pour fabriquer des compositions pharmaceutiques pour le traitement ou la prophylaxie de maladies, en particulier le cancer ou les maladies avec dérèglement des réponses immunitaires ou d'autres troubles associés aux signaux ahr aberrants, en monothérapie ou en association avec d'autres principes actifs.

8. 发明专利

PH12019501846A1 2-HETEROARYL-3-OXO-2,3-DIHYDROPYRIDAZINE-4-CARBOXAMIDES FOR THE TREATMENT OF CANCER 未知
公开(公告)号：PH12019501846A1
公开(公告)日：2020-03-09
申请号：PH12019501846
申请日：2019-08-08
申请人： BAYER PHARMA AG , BAYER AG
发明人： GUTCHER ILONA , RHN ULRIKE , SCHMEES NORBERT , ZORN LUDWIG , RSE LARS , BADER BENJAMIN , KOBER CHRISTINA , CARRETERO RAFAEL , STCKIGT DETLEF , IRLBACHER HORST , PLATTEN MICHAEL
IPC分类号： A61P35/00 , A61K31/501 , C07D237/04 , C07D237/24 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14
摘要： The present invention covers 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compounds of general formula (I), in which X, 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 diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.

9. 发明专利

SG11201907232XA 2-HETEROARYL-3-OXO-2,3-DIHYDROPYRIDAZINE-4-CARBOXAMIDES FOR THE TREATMENT OF CANCER 未知
公开(公告)号：SG11201907232XA
公开(公告)日：2019-09-27
申请号：SG11201907232X
申请日：2018-02-02
申请人： BAYER AG , BAYER PHARMA AG
发明人： GUTCHER ILONA , RÖHN ULRIKE , SCHMEES NORBERT , ZORN LUDWIG , RÖSE LARS , BADER BENJAMIN , KOBER CHRISTINA , CARRETERO RAFAEL , STÖCKIGT DETLEF , IRLBACHER HORST , PLATTEN MICHAEL
IPC分类号： C07D401/14 , A61K31/501 , A61P35/00 , C07D237/04 , C07D237/24 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14
摘要： Filing Language: (26) Publication Language: (30) Priority Data: 17155406.6 17202882.1 02 February 2018 (02.02.2018) English English 09 February 2017 (09.02.2017) EP 21 November 2017 (21.11.2017) EP R 5 W N 0 I .0\" 0 © R . 0 0 2 H N 'IR O O 1-1 O 71- 1-1 3 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 16 August 2018 (16.08.2018) WIPO I PCT omit VIII °nolo olomiloollm Hollow° oimIE (10) International Publication Number WO 2018/146010 Al (51) International Patent Classification: C07D 401/14 (2006.01) C07D 409/04 (2006.01) C07D 405/14 (2006.01) C07D 413/04 (2006.01) C07D 401/04 (2006.01) CO7D 417/04 (2006.01) C07D 403/04 (2006.01) CO7D 417/14 (2006.01) C07D 237/04 (2006.01) A61K 31/501 (2006.01) C07D 237/24 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/EP2018/052627 (22) International Filing Date: (71) Applicants: BAYER AKTIENGESELLSCHAFT [DE/DE]; Kaiser-Wilhelm-Allee 1, 51373 Lev- erkusen (DE). BAYER PHARMA AKTIENGESEL- LSCHAFT [DE/DE]; Miillerstr. 178, 13353 Berlin (DE). DEUTSCHES KREBSFORSCHUNGSZEN- TRUM [DE/DE]; Im Neuenheimer Feld 280, 69120 Hei- delberg (DE). (72) Inventors: GUTCHER, Ilona; Paul-Robeson-Str. 28, 10439 Berlin (DE). ROHN, Ulrike; Boyenstr. 42, 10115 Berlin (DE). SCHMEES, Norbert; Bondickstr. 61, 13469 Berlin (DE). ZORN, Ludwig; Osianderweg 45A, 13509 Berlin (DE). ROSE, Lars; Fuchsring 82, 13465 Berlin (DE). BADER, Benjamin; Hillmannstr. 14, 13467 Berlin (DE). KOBER, Christina; Heidelberger Str. 18, 76646 Bruchsal (DE). CARRETERO, Rafael; Milhlingstr. 6, 69121 Heidelberg (DE). STOCKIGT, Detlef; Clara- Zetkin-Str. 27, 14471 Potsdam (DE). IRLBACHER, Horst; Winsstr. 47, 10405 Berlin (DE). PLATTEN, Michael; Cambridgestr. 7, 69115 Heidelberg (DE). (74) Agent: BIP PATENTS; Alfred-Nobel-Str. 10, 40789 Mon- heim am Rhein (DE). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) Published: with international search report (Art. 21(3)) with sequence listing part of description (Rule 5.2(a)) 1-1 (54) Title: 2-HETEROARYL-3-OXO-2,3-DIHYDROPYRIDAZINE-4-CARBOXAMIDES FOR THE TREATMENT OF CANCER (57) : The present invention covers 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carbox- amide compounds of general formula (I), in which X, R1, R 2 , R 3 , R4 and - lc 5 are as defined here- in, methods of preparing said compounds, intermediate compounds useful for preparing said com- pounds, pharmaceutical compositions and combinations comprising said compounds and the use of (I) said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other dis- orders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.

10. 发明专利

BR112022001628A2 [1,2,4]triazolo[1,5-c]quinazolin-5-aminas 未知
公开(公告)号：BR112022001628A2
公开(公告)日：2022-06-21
申请号：BR112022001628
申请日：2020-08-10
申请人： BAYER AG , BAYER PHARMA AG
发明人： BADER BENJARNIN , BUCHMANN BERND , KOBER CHRISTINA , BAUMANN DANIEL , STÖCKIGT DETLEF , GUTCHER ILONA , GÜNTHER JUDITH , LEFRANC JULIEN , RÖSE LARS , ZORN LUDWIG , GORJANACZ MATYÁS , PLATTEN MICHAEL , SCHMEES NORBERT , ROBIN MICHAEL MEIER , SIMON ANTHONY HERBERT , BÖHME STEPHAN , BOTHE ULRICH
IPC分类号： C07D487/04 , A61P35/00 , C07D519/00
摘要： [1,2,4]triazolo[1,5-c]quinazolin-5-aminas. a presente invenção refere-se a compostos de [1,2,4]triazolo[1,5-c]quinazolin-5-amina de fórmula geral (i): em que r1, r2, r3, r4, r5, r6, r7 e r8 são como definidos neste documento, métodos de preparação dos referidos compostos, compostos intermediários úteis para preparar os referidos compostos, composições farmacêuticas e combinações compreendendo os referidos compostos e o uso dos referidos compostos para a fabricação de composições farmacêuticas para o tratamento ou profilaxia de doenças, em particular de câncer ou condições com respostas imunes desreguladas ou outros distúrbios associados à sinalização aberrante de ahr, como agente único ou em combinação com outros ingredientes ativos.

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