AR108838A1 - Ácidos de carbamoiloximetil triazol ciclohexilo como antagonistas de lpa - Google Patents

Ácidos de carbamoiloximetil triazol ciclohexilo como antagonistas de lpa

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Publication number
AR108838A1
AR108838A1 ARP170101698A ARP170101698A AR108838A1 AR 108838 A1 AR108838 A1 AR 108838A1 AR P170101698 A ARP170101698 A AR P170101698A AR P170101698 A ARP170101698 A AR P170101698A AR 108838 A1 AR108838 A1 AR 108838A1
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AR
Argentina
Prior art keywords
substituted
independently selected
alkyl
cycloalkyl
cr7r7
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ARP170101698A
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English (en)
Inventor
Sutjano Jusuf
Tianan Fang
James R Corte
Lawrence J Kennedy
Steven J Walker
Ramesh Babu Reddigunta
Kumaravel Selvakumar
Suresh Dhanusu
Hao Zhang
Shiwei Tao
Yan Shi
Jun Shi
Jun Li
Iii Robert F Kaltenbach
Peter Tai Wah Cheng
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Bristol Myers Squibb Co
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Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR108838A1 publication Critical patent/AR108838A1/es

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
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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
    • A61K31/4439—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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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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Abstract

Estos compuestos son inhibidores selectivos del receptor de LPA. Reivindicación 1: Un compuesto caracterizado por la fórmula (1), o estereoisómeros, tautómeros, sales aceptables desde el punto de vista farmacéutico, solvatos o profármacos de aquel, en donde R² se selecciona independientemente de H y C₁₋₄ alquilo sustituido con 1 - 5 R⁹; R¹³ se selecciona independientemente de H, D y C₁₋₄ alquilo sustituido con 1 - 3 R⁹; R³ y R⁴ se seleccionan independientemente de H, C₁₋₇ alquilo sustituido con 1 - 3 R⁹, -(CR⁷R⁷)ʳ-C₃₋₈ cicloalquilo sustituido con 1 - 3 R⁸, -(CR⁷R⁷)ʳ-arilo sustituido con 1 - 3 R⁸, C₂₋₇ alquenilo sustituido con 1 - 3 R⁹, anillo heterocíclico -(CR⁷R⁷)ʳ de 5 - 6 miembros sustituido con 1 - 3 R⁹, anillo de heteroarilo -(CR⁷R⁷)ʳ de 5 - 6 miembros sustituido con 1 - 3 R⁸, o R³ y R⁴ se combinan con el N al cual están unidos para formar un anillo heterocíclico de 4 - 9 miembros sustituido con 1 - 3 R⁸; X¹, X², X³ y X⁴ se seleccionan independientemente de CR⁵ y N; siempre que no más de dos de X¹, X², X³ o X⁴ sean N; R⁵ se selecciona independientemente de H, F, Cl, OR⁷, CN, N(R⁷)₂, C₁₋₄, alquilo sustituido con 1 - 5 R⁹, C₁₋₄ alcoxi sustituido con 1 - 5 R⁹ y C₁₋₄ heteroalquilo sustituido con 1 - 5 R⁹; R⁶ es C₃₋₈ cicloalquilo que se sustituye con R¹⁰ y (-CH₂)₀₋₁R¹¹; R⁷ se selecciona independientemente de H, C₁₋₄ alquilo y C₃₋₆ cicloalquilo; o R⁷ y R⁷, junto con el átomo de carbono al que están unidos, forman un anillo C₃₋₆ cicloalquilo; R⁸ se selecciona independientemente de H, D, C₁₋₆ alquilo sustituido con 1 - 5 R⁹, C₂₋₆ alquenilo, C₂₋₆ alquinilo, fenilo, -(CH₂)ʳ-C₃₋₆ cicloalquilo, F, Cl, Br, CN, COOH y C₁₋₄ alcoxi; R⁹ se selecciona independientemente de H, D, F, Cl, NH₂, OH, OC₁₋₅ alquilo, C₁₋₅ alquilo, C₁₋₅ heteroalquilo C₃₋₆ cicloalquilo y fenilo, en donde cuando R⁹ es Cl, NH₂ u OH, no se sustituye en C₁ del alquilo al que está unido; R¹⁰ se selecciona independientemente de H, D, C₁₋₄ alquilo, F, Cl, Br, OR⁷, NHC(=O)OR⁷ y NHC(=O)OR⁷; R¹¹ se selecciona independientemente de H, CN, -C(=O)R¹², tetrazolilo, un resto de fórmula (2) y un resto de fórmula (3); R¹² se selecciona independientemente de OH, OC₁₋₄ alquilo, NH₂, NHCH₂CH₂SO₃H y NHSO₂C₁₋₄ alquilo; r se selecciona independientemente de 0, 1, 2, 3 y 4; y n se selecciona de 1, 2, 3 ó 4.
ARP170101698A 2016-06-21 2017-06-19 Ácidos de carbamoiloximetil triazol ciclohexilo como antagonistas de lpa AR108838A1 (es)

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EP (2) EP3472148B1 (es)
JP (2) JP7073281B2 (es)
KR (2) KR102377340B1 (es)
CN (2) CN114601830A (es)
AR (1) AR108838A1 (es)
AU (2) AU2017281439B2 (es)
BR (1) BR112018076558A2 (es)
CA (1) CA3029202C (es)
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AR108838A1 (es) 2016-06-21 2018-10-03 Bristol Myers Squibb Co Ácidos de carbamoiloximetil triazol ciclohexilo como antagonistas de lpa
TW201927778A (zh) 2017-12-19 2019-07-16 美商必治妥美雅史谷比公司 作為lpa拮抗劑之環己基酸三唑唑類
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CN112041302A (zh) 2017-12-19 2020-12-04 百时美施贵宝公司 作为lpa拮抗剂的吡唑o-连接的氨基甲酰基环己基酸
KR20200100753A (ko) 2017-12-19 2020-08-26 브리스톨-마이어스 스큅 컴퍼니 Lpa 길항제로서의 시클로헥실 산 피라졸 아졸
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KR20220024548A (ko) 2019-06-18 2022-03-03 브리스톨-마이어스 스큅 컴퍼니 Lpa 길항제로서의 트리아졸 카르복실산
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WO2021020429A1 (ja) 2019-07-30 2021-02-04 大正製薬株式会社 Ｌｐａ１受容体を拮抗するウレア化合物
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CN114746425A (zh) 2019-12-12 2022-07-12 奇斯药制品公司 作为lpa受体2抑制剂的噻吩并嘧啶衍生物
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