AR076148A1 - Compuestos sustituidos de espiro -amida - Google Patents

Compuestos sustituidos de espiro -amida

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Publication number
AR076148A1
AR076148A1 ARP100100948A ARP100100948A AR076148A1 AR 076148 A1 AR076148 A1 AR 076148A1 AR P100100948 A ARP100100948 A AR P100100948A AR P100100948 A ARP100100948 A AR P100100948A AR 076148 A1 AR076148 A1 AR 076148A1
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Argentina
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aryl
heteroaryl
cycloalkyl
alkyl
group
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ARP100100948A
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English (en)
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Gruenenthal Chemie
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Publication of AR076148A1 publication Critical patent/AR076148A1/es

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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4355—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
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    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/47—Quinolines; Isoquinolines
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    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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Abstract

Procesos para la preparacion de estos, medicamentos que contienen estos compuestos y el uso de los compuestos sustituidos de espiro-amida para la preparacion de medicamentos, moduladores de B1R. Reivindicacion 1: Un compuesto espiro-amida sustituido de formula general (1) caracterizado por que a representa 0 o 1; t representa 1, 2 o 3; b representa 0, 1 o 2; c, d, e y f representan, independientemente uno de otro, 0, 1 o 2; D representa uno de los siguientes radicales D1 o D2; q representa 0 o 1; s representa 0 o 1; r representa 1, 2 o 3; B representa C(=O), S(=O)2 o el grupo -C(=O)-N(R9), en donde el átomo de nitrogeno de este ultimo esta enlazado al radical R1; Q1 y Q2, independientemente uno del otro, representan C, CH o N; R1 representa C1-6-alquilo, arilo, heteroarilo, -CH(arilo)2, C3-8-cicloalquilo o un arilo, heteroarilo o C3-8-cicloalquilo enlazado mediante un grupo C1-6-alquileno, un grupo C2-6-alquenileno o un grupo C2-6-alquinileno, o un arilo o grupo heteroarilo enlazado mediante un grupo C3-6 cicloalquileno; R2 representa H, C1-6-alquilo, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-6-alquileno; R3 y R4 junto con el grupo -Q1-Q2- que esta junto a ellos forman un anillo, el que es insustituido o sustituido en uno o más de sus miembros del anillo de carbono por uno o más sustituyentes, independientes uno del otro, elegidos del grupo que consiste en F, CI, Br, I, CF3, C1-6-alquilo, O-C1-6-alquilo, OH, OCF3, SH, SCF3, arilo y heteroarilo y/o puede fusionarse con al menos un arilo o heteroarilo, caracterizado por que el anillo es saturado, insaturado una o varias veces o aromático, es de 4-, 5-, 6- o 7- miembros, y puede, opcionalmente, contener uno o más heteroátomos o grupo de heteroátomos independiente uno del otro, elegidos del grupo que consiste en N, NR50, O, S, S(=O) y S(=O)2; caracterizado por que el radical R50 denota H, C1-6-alquilo, -C(=O)-R51, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-3-alquileno, y R51 denota C1-6-alquilo, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-3-alquileno; R5 representa 0, 1, 2, 3 o 4 sustituyentes que, de manera independiente uno del otro, son elegidos del grupo que consiste en F, CI, CF3, OCF3, OH, C1-6-alquilo y O-C1-6-alquilo y/o dos sustituyentes adyacentes R5 forma un arilo fusionado, heteroarilo o C4-8-cicloalquilo y/o dos sustituyentes R5 enlazados a un átomo de carbono forman un anillo carbocíclico saturado de 3, 4 o 5 miembros, el que esta insustituido o sustituido en uno o más de sus miembros de anillo de carbono por uno o más sustituyentes elegidos de manera independiente del grupo que consiste de F, CF3 y C1-6-alquilo; R6 representa 0, 1, 2, 3 o 4 sustituyentes que son elegidos de manera independiente del grupo que consiste de F, CI, Br, CF3, OCF3, OH, C1-6-alquilo, C3-8-cicloalquilo, O-C1-6-alquilo, NO2, NH2, N(H)(C1-6-alquilo) y N(C1-6-alquilo)2 y/o dos sustituyentes adyacentes R6 forman un arilo, heteroarilo o C4-8-cicloalquilo fusionado; R7 y R8 independientemente uno del otro representan 0, 1, 2, 3 o 4 sustituyentes que en cada caso son elegidos, independientemente uno del otro, del grupo que consiste en F, CI, OH, =O, C1-6-alquilo, O-C1-6-alquilo, C3-8-cicloalquilo, arilo, heteroarilo y C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-6-alquileno y/o dos sustituyentes adyacentes R7 o R8 forman un arilo o heteroarilo fusionado; R9 representa H, C1-6-alquilo, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-3-alquileno; X representa CR10aR10b, NR11 o O; Y representa CR12aR12b, NR13 o O; con la condicion de que X no denota NR11 si Y denota NR13 y con la condicion de que X e Y no denotan simultáneamente O; caracterizado por que R10a, R10b, R12a y R12b denotan, independientemente, H, F, CI, OH, C1-6-alquilo, O-C1-6-alquilo, C3-8-cicloalquilo, arilo o heteroarilo, o representan un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-6-alquileno, y/o en cada caso R10a y R10b juntos pueden representar =O y/o en cada caso R12a y R12b juntos pueden representar =O; R11 y R13, independientemente uno del otro, representan H, C1-6-alquilo, C3-8-cicloalquilo, arilo o heteroarilo, o denotan un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-6-alquileno; Z representa CR14aR14b, NR15 o O; R14a representa H, NR16R17, C1-6-alquileno-NR16R17, O-C1-6-alquileno-NR16R17, C(=O)NR16R17, C(=O)-C1-6-alquileno-NR16R17, OR18, C1-6-alquileno-OR18, C1-6-alquileno-O-C1-6-alquileno-OR18, C1-6-alquilo, C3-8-cicloalquilo, heterociclil, arilo o heteroarilo, o denotes un C3-8-cicloalquilo, heterociclil, arilo o heteroarilo enlazado mediante un grupo C1-6-alquileno, R14b representa H, NR16R17, C1-6-alquileno-NR16R17, O-C1-6-alquileno-NR16R17, C(=O)-NR16R17, C(=O)-C1-6-alquileno-NR16R17, OR18, C1-6-alquileno-OR18, C1-6-alquileno-O-C1-6-alquileno-OR18, C1-6-alquilo, C3-8-cicloalquilo, heterociclil, arilo o heteroarilo, o denota un C3-8-cicloalquilo, heterociclil, arilo o heteroarilo enlazado mediante un grupo C1-6-alquileno, R15 representa H, -C(=O)-R19, -S(=O)2-R19, -C(=O)-N(R20)-R19, CHR25R26, C1-10-alquilo, C3-8-cicloalquilo, heterociclil, arilo o heteroarilo o denota un CHR25R26, C3-8-cicloalquilo, heterociclil, arilo o heteroarilo enlazado mediante un grupo C1-6-alquileno; R16 y R17 independientemente uno del otro representan H, C1-6-alquilo o C3-8-cicloalquilo, o R16 y R17 juntos con el átomo de nitrogeno uniéndolos forman un anillo heterocíclico, que esta insustituido o sustituido en uno o más de sus miembros de anillo de carbono por uno o más sustituyentes, elegidos, independiente uno del otro, del grupo que consiste en F, CI, Br, I, CF3, C1-6-alquilo, O-C1-6-alquilo, OH, OCF3, SH, SCF3, NRARB, arilo y heteroarilo y/o puede estar fusionado con al menos un arilo o heteroarilo, caracterizado por que el anillo heterocíclico esta saturado o insaturado una o varias veces, es de 4-, 5-, 6-, o 7- miembros, y puede, opcionalmente, contener uno o más heteroátomos o grupos de heteroátomos elegidos, independientemente uno del otro, del grupo que consiste en N, NR50a, O, S, S(=O) y S(=O)2; caracterizado por que R50a denotes H, C1-6-alquilo, C(=O)R51a, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-3-alquileno, y R51a denota C1-6-alquilo, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-3-alquileno; R18 representa H, C1-6-alquilo, C3-8-cicloalquilo, heterociclil, arilo, heteroarilo o C2-6-alquileno-NR16R17 o denota un heterociclil, C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-6-alquileno; R19 representa C1-6-alquilo, arilo, heteroarilo, -CH(arilo)2, C3-8-cicloalquilo, heterociclil o un arilo, heteroarilo, C3-8-cicloalquilo o heterociclil enlazado mediante un grupo C1-6-alquileno, grupo C2-6-alquenileno o grupo C2-6-alquinileno; R20 representa H, C1-6-alquilo, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-3-alquileno; O Z en el caso donde X representa O y f representa 0, denota -(C(R21)-C(R22))-, caracterizado por que R21 y R22, juntos con los átomos de carbono uniéndolos, forman un arilo o heteroarilo fusionado; o Z en el caso donde X representa O y f representa 0, denota =(N(CR23))-, caracterizado por que el átomo N esta enlazado mediante un enlace unico al átomo O, y R23 representa H, C1-6-alquilo, C3-8-cicloalquilo, arilo o heteroarilo o denota un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-6-alquileno; R25 y R26 independientemente uno del otro representan H, C1-4-alquilo, C3-8-cicloalquilo, arilo o heteroarilo, o R25 y R26 junto con los agrupaciones CH que los unen, forman un anillo, que esta insustituido o sustituido en uno o más de sus miembros de anillo de carbono por uno o más sustituyentes, elegidos, independiente uno del otro, del grupo que consiste en F, CI, Br, I, CF3, C1-6-alquilo, O-C1-6-alquilo, OH, OCF3, SH, SCF3, NRARB, arilo y heteroarilo, caracterizado por que el anillo esta saturado o insaturado una o varias veces, es de 4-, 5-, 6-, o 7- miembros, y puede, opcionalmente, contener uno o más heteroátomos o grupos de heteroátomos elegidos, independientemente uno del otro, del grupo que consiste en N, NR50b, O, S, S(=O) y S(=O)2 caracterizado por que R50b denota H, C1-6-alquilo, -C(=O)-R51b, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-3-alquileno, y R51b denota C1-6-alquilo, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-3-alquileno; RA y RB representan, independientemente uno del otro, H, C1-6-alquilo o C3-8-cicloalquilo, o RA y R8 junto con el átomo de nitrogeno uniéndolos forman un anillo heterocíclico que esta insustituido o sustituido en uno o mas de sus miembros de anillo de carbono por uno o más sustituyentes, elegidos, independiente uno del otro, del grupo que consiste en F, CI, Br, I, CF3, C1-6-alquilo, O-C1-6-alquilo, OH, OCF3, SH, SCF3, arilo y heteroarilo, caracterizado por que el anillo heterocíclico esta saturado o insaturado una o varias veces, no es aromático, es de 4-, 5-, 6-, o 7- miembros, y puede, opcionalmente, contener uno o más heteroátomos o grupos de heteroátomos elegidos, independientemente uno del otro, del grupo que consiste en N, NRC, O, S, S(=O) y S(=O)2; caracterizado por que Rc denota H, C1-6-alquilo, -C(=O)-Rd, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante un grupo C1-3-alquileno, y Rd denota C1-6-alquilo, C3-8-cicloalquilo, arilo, heteroarilo o un C3-8-cicloalquilo, arilo o heteroarilo enlazado mediante
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Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2623491A3 (en) * 2009-04-02 2014-07-30 Merck Patent GmbH Piperidine and piperazine derivatives as autotaxin inhibitors
MX2012010772A (es) * 2010-03-19 2012-11-06 Pfizer Derivados de 2,3-dihidro-1h-inden-1-il-2,7-diazaspiro[3,5]nonano y su uso como antagonistas o agonistas inversos del receptor de grelina.
US8809552B2 (en) * 2011-11-01 2014-08-19 Hoffmann-La Roche Inc. Azetidine compounds, compositions and methods of use
TWI633087B (zh) 2012-06-13 2018-08-21 赫孚孟拉羅股份公司 新穎二氮雜螺環烷及氮雜螺環烷
SI2900669T1 (sl) 2012-09-25 2019-12-31 F. Hoffmann-La Roche Ag Derivati heksahidropirolo(3,4-C)pirola in sorodne spojine kot zaviralci avtotaksina (ATX) in kot zaviralci tvorbe lizofosfatidne kisline (LPA) za zdravljenje npr. bolezni ledvic
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
CA2923075C (en) 2013-09-12 2022-07-26 Alios Biopharma, Inc. Aza-pyridone compounds and uses thereof
SI3074400T1 (en) 2013-11-26 2018-03-30 F. Hoffmann-La Roche Ag Octahydro-cyclobut (1,2-c, 3,4-cy) dipyrrole derivatives as autoantaxine inhibitors
AU2015238541B2 (en) 2014-03-26 2019-09-19 F. Hoffmann-La Roche Ag Condensed [1,4]diazepine compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors
AU2015238537B2 (en) 2014-03-26 2019-08-01 F. Hoffmann-La Roche Ag Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors
US10214520B2 (en) * 2014-07-15 2019-02-26 Gruenenthal Gmbh Substituted azaspiro(4.5)decane derivatives
US10208045B2 (en) 2015-03-11 2019-02-19 Alios Biopharma, Inc. Aza-pyridone compounds and uses thereof
CN106008503B (zh) * 2015-03-31 2020-09-01 齐鲁制药有限公司 螺环芳基砜作为蛋白激酶抑制剂
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
PE20180479A1 (es) 2015-09-04 2018-03-07 Hoffmann La Roche Nuevos derivados de fenoximetilo
JP6845230B2 (ja) 2015-09-24 2021-03-17 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ デュアルａｔｘ／ｃａ阻害剤としての新規な二環式化合物
MA42919A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
PE20180552A1 (es) 2015-09-24 2018-04-02 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca
RU2018114289A (ru) 2015-09-24 2019-10-24 Ф. Хоффманн-Ля Рош Аг Бициклические соединения в качестве ингибиторов аутотаксина (atx)
TW201726678A (zh) 2015-10-30 2017-08-01 赫孚孟拉羅股份公司 嘧啶酮衍生物及其於治療、改善或預防病毒性疾病之用途
CN108779116A (zh) * 2015-12-22 2018-11-09 生命医药公司 多发性内分泌瘤蛋白-mll相互作用的抑制剂
AU2017206908B2 (en) 2016-01-13 2020-07-09 Grünenthal GmbH 3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives
EA034898B1 (ru) 2016-01-13 2020-04-03 Грюненталь Гмбх Производные 8-амино-2-оксо-1,3-диазаспиро[4,5]декана
TWI640514B (zh) 2016-01-13 2018-11-11 歌林達有限公司 ３－（羧甲基）－８－胺基－２－側氧基－１，３－二氮－螺－［４．５］－癸烷衍生物
ES2947636T3 (es) 2016-03-16 2023-08-14 Kura Oncology Inc Derivados de tieno[2,3-d]pirimidina sustituida como inhibidores de menina-MLL y métodos de uso
EP3491353A4 (en) 2016-07-28 2020-02-19 Mayo Foundation for Medical Education and Research SMALL MOLECULE ACTIVATORS OF PARKIN ENZYMATIC FUNCTION
EP3366683A1 (en) 2017-02-28 2018-08-29 Acousia Therapeutics GmbH Cyclic amides, acteamides and ureas useful as potassium channel openers
WO2018167001A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag Heterocyclic compounds useful as dual atx/ca inhibitors
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
US11649251B2 (en) 2017-09-20 2023-05-16 Kura Oncology, Inc. Substituted inhibitors of menin-MLL and methods of use
WO2019200114A1 (en) * 2018-04-12 2019-10-17 Arbutus Biopharma Corporation Methods for preparing substituted dihydroindene-4-carboxamide compounds
CN111434664A (zh) * 2019-01-13 2020-07-21 西南大学 亚胺螺环哌啶类化合物的合成及应用
CN117177744A (zh) 2021-01-29 2023-12-05 塞迪拉治疗股份有限公司 Cdk2抑制剂及其使用方法
CN117561058A (zh) 2021-06-26 2024-02-13 塞迪拉治疗股份有限公司 Cdk2抑制剂及其使用方法
CN113976072B (zh) * 2021-11-10 2024-02-23 武汉青风凯默生物医药科技有限公司 一种4-甲酰基-n-cbz哌啶的制备装置及方法

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2341678C (en) * 1998-09-01 2009-10-13 Bristol-Myers Squibb Company Potassium channel inhibitors and method
WO2001039723A2 (en) * 1999-12-06 2001-06-07 Euro-Celtique, S.A. Triazospiro compounds having nociceptin receptor affinity
EP1725236A4 (en) 2004-03-11 2009-05-13 Glaxo Group Ltd NEW M3 MUSCARIN ACETYLCHOLINE RECEPTOR ANTAGONISTS
JP5136929B2 (ja) 2004-03-24 2013-02-06 アボット・ラボラトリーズ 三環式ピラゾール系キナーゼ阻害薬
AU2005314601A1 (en) * 2004-10-15 2006-06-15 Bayer Pharmaceuticals Corporation Indane amides with antiproliferative activity
EP1824842A4 (en) * 2004-11-18 2009-08-26 Incyte Corp INHIBITORS OF 11-HYDROXYL STEROID DEHYDROGENASE TYPE 1 AND METHOD OF USE
US20070032475A1 (en) * 2005-04-15 2007-02-08 Ye Xiaocong M Novel compounds useful for bradykinin B1 receptor antagonism
DE102005030051A1 (de) * 2005-06-27 2006-12-28 Grünenthal GmbH Substituierte 1-Oxa-3,8-diazaspiro[4,5]-decan-2-on-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln
WO2007011811A1 (en) * 2005-07-19 2007-01-25 Merck & Co., Inc. Spirochromanone derivatives as acetyl coenzyme a carboxylase (acc) inhibitors
WO2007101007A2 (en) 2006-02-23 2007-09-07 Neurogen Corporation Aryl sulfonyl heterocycles
WO2007140383A2 (en) * 2006-05-30 2007-12-06 Neurogen Corporation Spirocyclic sulfonamides and related compounds
KR20090079914A (ko) 2006-09-29 2009-07-22 그뤼넨탈 게엠베하 치환된 설폰아미드 유도체
CA2666406A1 (en) 2006-10-16 2008-04-24 Gruenenthal Gmbh Substituted sulfonamide derivatives for use as bradykinin 1 receptor modulators

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