AR060605A1 - Derivados de diazepano como antagonistas del receptor ccr2 - Google Patents

Derivados de diazepano como antagonistas del receptor ccr2

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Publication number
AR060605A1
AR060605A1 ARP070101679A ARP070101679A AR060605A1 AR 060605 A1 AR060605 A1 AR 060605A1 AR P070101679 A ARP070101679 A AR P070101679A AR P070101679 A ARP070101679 A AR P070101679A AR 060605 A1 AR060605 A1 AR 060605A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
heterocyclyl
heteroaryl
phenyl
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ARP070101679A
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English (en)
Inventor
Patrizi Mattei
Olivier Roche
Johannes Aebi
Luke Green
Fabienne Ricklin
Peter Zahm
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Hoffmann La Roche
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Publication of AR060605A1 publication Critical patent/AR060605A1/es

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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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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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Abstract

Así como las sales farmacéuticamente aceptables de los mismos. Estos compuestos son antagonistas del receptor CCR-2, del receptor CCR-5 y/o del receptor CCR-3 y pueden utilizarse como medicamentos. Reivindicacion 1: Compuestos de la formula (1) en la que A es arilo o heteroarilo, dicho arilo y dicho heteroarilo están opcionalmente sustituidos de 1 a 3 veces por sustituyentes elegidos con independencia entre el grupo formado por halogeno, benciloxi, heteroaril-alcoxi C1-6, alquilo C1-6, alcoxi C1-6 y halo-alcoxi C1-6, o dicho arilo y dicho heteroarilo están opcionalmente sustituidos por alquilenodioxi C1-6; X es -N(R1)(R2) o -N+(R1)(R2)(R7); i) R1 y R2 son con independencia entre sí H, alquilo C1-6, alquenilo C3-6, alquinilo C3-6, hidroxialquilo C2-6, alcoxi C1-6-alquilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, bicicloalquilo C7-10, fenil-alquilo C1-3, heteroaril-alquilo C1-3, heterociclilo o heterociclil-alquilo C1-6, en el que el cicloalquilo de dicho cicloalquilo C3-7 y dicho cicloalquil C3-7-alquilo C1-6, el fenilo de dicho fenil-alquilo C1-3, el heteroarilo de dicho heteroaril-alquilo C1-3 y el heterociclilo de dicho heterociclilo y dicho heterociclil-alquilo C1-6 están opcionalmente sustituidos de una a tres veces por sustituyentes elegidos con independencia entre el grupo formado por Rd; o R1 y R2, junto con el átomo de nitrogeno al que están unidos, forman un heterociclilo opcionalmente sustituido de una a tres veces por sustituyentes elegidos entre el grupo formado por Rd, y uno de los átomos de carbono del anillo de dicho heterociclilo formado por R1 y R2 está opcionalmente sustituido por un grupo carbonilo; y/o uno de los átomos de carbono del anillo del heterociclilo formado por R1 y R2 puede ser un átomo de carbono de otro anillo, que sea cicloalquilo C3-7, o heterociclilo, uno o dos átomos de carbono de dicho otro anillo están opcionalmente reemplazados por un grupo carbonilo, y dicho otro anillo está opcionalmente sustituido por alquilo C1-6; R3 y R4 son con independencia entre si hidrogeno, hidroxi, alquilo C1-6, alcoxi C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, alcoxi C1-6-carbonilo, carboxilo, hidroxialquilo C1-6, alcoxi C1- 6-alquilo C1-6, halogeno o halo-alquilo C1-6; o R3 y R4, junto con el átomo de carbono al que están unidos, forman un cicloalquilo C3-7 o heterociclilo opcionalmente sustituido de una a tres veces por sustituyentes elegidos entre el grupo formado por alquilo C1-4 alquilo, haloalquilo C1-4 y halogeno; o bien ii) R1 es H, alquilo C1-6, alquenilo C3-6, alquinilo C3-6, hidroxi-alquilo C1-6, alcoxi C1-6-alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, bicicloalquilo C7-10, fenil- alquilo C1-3, heteroaril-alquilo C1-3; heterociclilo o heterociclil-alquilo C1-6, en el que el cicloalquilo de dicho cicloalquilo C3-7 y dicho cicloalquil C3-7-alquilo C1-6, el fenilo de dicho fenil-alquilo C1-3, el heteroarilo de dicho heteroaril- alquilo C1-3 y el heterociclilo de dicho heterociclilo y dicho heterociclil-alquilo C1-6 están opcionalmente sustituidos de 1 a 3 veces por sustituyentes elegidos con independencia entre el grupo formado por Rd; R3 es H, alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, halogeno o halo-alquilo C1-6; R2 y R4, junto con el átomo de N al que está unido R2, el átomo de C al que está unido R4 y el alquileno C1-2 entre dicho átomo de N y dicho átomo de C, si lo hubiera, forman un heterociclilo opcionalmente sustituido de 1 a 3 veces por sustituyentes elegidos entre el grupo formado por alquilo C1-6 y F; R5 y R6 con independencia entre sí son H, F, alquilo C1-6 o cicloalquilo C3-7; R7 es alquilo C1-6; R8, R9, R10, R11, R12 y R13 son con independencia entre sí H, alquilo C1-6 o cicloalquilo C3-7; Rd es hidroxi, ciano, NRaRb, halogeno, alquilo C1-6, halo-alquilo C1-6, hidroxi-alquilo C1-6, alcoxi C1-6, alcoxi C1-6- alquilo C1-6, cicloalquilo C3-7, alcoxi C1-6-carbonilo, acilo, -C(O)NRaRb, -NRa-C(O)-Rb, -NRa-C(O)-ORb, -NRa-C(O)-NRb, -NRa-SO2-Rb, -NRa-SO2-NRbRc, -OC(O)NRaRb, -OC(O)ORa, alquilsulfonilo C1-6, alquilsulfinilo C1-6, alquiltio C1-6, fenilo, fenil-alquilo C1-3, heteroarilo, heteroaril-alquilo C1-3 y heterociclilo, y el fenilo de dicho fenilo y dicho fenil-alquilo C1-3, el heteroarilo de dicho heteroarilo y dicho heteroaril-alquilo C1-3 y el heterociclilo están opcionalmente sustituidos de una a tres veces por sustituyentes elegidos con independencia entre el grupo formado por hidroxi, ciano, NRaRb, halogeno, alquilo C1-6, halo-alquilo C1-6, hidroxi-alquilo C1-6, alcoxi C1-6-carbonilo, acilo, -C(O)NRaRb, --NRa-C(O)-Rb, -NRa-C(O)-ORb, -NRa-C(O)-NRb, -NRa-SO2-Rb, -NRa-SO2-NRbRc, - OC(O)NRaRb, -OC(O)ORa, alquilsulfonilo C1-6, alquilsulfinilo C1-6, alquiltio C1-6, y uno o dos átomos de carbono del anillo del heterociclilo están opcionalmente sustituidos por un grupo carbonilo; Ra, Rb y Rc son con independencia hidrogeno o alquilo C1-6; n es un numero entero de 0 a 3; m es un numero entero de 0 a 3; m+n es un numero entero de 1 a 5; o profármacos o sales farmacéuticamente aceptables de los mismos; en los que, a menos que se indique lo contrario, el término ôariloö significa fenilo o naftilo; el término ôheterocicliloö significa restos no aromáticos, mono- o bicíclicos, de cuatro a nueve átomos en el anillo, de los cuales de 1 a 3 son heteroátomos, elegidos con independencia entre N, O y S(O)n (en el que n es un numero entero de 0 a 2), los demás átomos del anillo son C; el término ôheteroariloö significa un resto monocíclico o bicíclico de 5 a 10 átomos en el anillo, que tiene de 1 a 3 heteroátomos en el anillo, elegidos con independencia entre N, O y S, los demás átomos del anillo son C; el término ôaciloö significa R-C(O)-, en el que R es alquilo C1-6, halo-alquilo C1-6, cicloalquilo C3-7 o cicloalquil C3-7-alquilo C1-6.
ARP070101679A 2006-04-20 2007-04-19 Derivados de diazepano como antagonistas del receptor ccr2 AR060605A1 (es)

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EP (1) EP2010506B1 (es)
JP (1) JP5016666B2 (es)
KR (1) KR101176697B1 (es)
CN (1) CN101472904B (es)
AR (1) AR060605A1 (es)
AT (1) ATE476424T1 (es)
AU (1) AU2007242883B2 (es)
BR (1) BRPI0710512A2 (es)
CA (1) CA2649636A1 (es)
CL (1) CL2007001090A1 (es)
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JP2009286778A (ja) * 2008-04-30 2009-12-10 Sumitomo Chemical Co Ltd ｔｅｒｔ−ブチル３−アミノピペリジン−１−カルボキシレートの製造方法およびその中間体
MX2011000404A (es) 2008-07-16 2011-03-04 Hoffmann La Roche Nuevos compuestos heterociclilo para el tratamiento de enfermedades cardiovasculares.
CN102112451B (zh) * 2008-07-28 2014-01-22 弗·哈夫曼-拉罗切有限公司 用作趋化因子受体调节剂的二氮杂环庚烷和哌嗪衍生物
SG171914A1 (en) 2008-12-02 2011-07-28 Chiralgen Ltd Method for the synthesis of phosphorus atom modified nucleic acids
AU2010270714B2 (en) 2009-07-06 2015-08-13 Wave Life Sciences Ltd. Novel nucleic acid prodrugs and methods use thereof
US8471004B2 (en) * 2009-10-07 2013-06-25 Hoffman-La Roche Inc. Bicyclic compounds
WO2011149841A1 (en) 2010-05-25 2011-12-01 Janssen Pharmaceutica Nv SUBSTITUTED THIAZOLIDINEDIONE INDAZOLES, INDOLES AND BENZOTRIAZOLES AS ESTROGEN-RELATED RECEPTOR-α MODULATORS
US10428019B2 (en) 2010-09-24 2019-10-01 Wave Life Sciences Ltd. Chiral auxiliaries
WO2012041873A1 (en) * 2010-09-29 2012-04-05 Intervet International B.V. N-heteroaryl compounds
UA109290C2 (uk) * 2010-10-07 2015-08-10 Спільні кристали і солі інгібіторів ccr3
ES2525837T3 (es) * 2010-12-01 2014-12-30 Janssen Pharmaceutica, N.V. Antagonistas de ccr2 de ciclohexilamino-4-piperidinil-acetamida sustituida en posición 4
DK2734208T3 (en) 2011-07-19 2017-06-19 Wave Life Sciences Ltd PROCEDURES FOR SYNTHESIS OF FUNCTIONALIZED NUCLEIC ACIDS
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
US9598458B2 (en) 2012-07-13 2017-03-21 Wave Life Sciences Japan, Inc. Asymmetric auxiliary group
SG11201500232UA (en) 2012-07-13 2015-04-29 Wave Life Sciences Pte Ltd Chiral control
JP6246121B2 (ja) 2012-07-13 2017-12-13 株式会社新日本科学 キラル核酸アジュバント
JPWO2015108047A1 (ja) 2014-01-15 2017-03-23 株式会社新日本科学 免疫誘導活性を有するキラル核酸アジュバンド及び免疫誘導活性剤
EP3095460A4 (en) 2014-01-15 2017-08-23 Shin Nippon Biomedical Laboratories, Ltd. Chiral nucleic acid adjuvant having anti-allergic activity, and anti-allergic agent
JPWO2015108048A1 (ja) 2014-01-15 2017-03-23 株式会社新日本科学 抗腫瘍作用を有するキラル核酸アジュバンド及び抗腫瘍剤
US10160969B2 (en) 2014-01-16 2018-12-25 Wave Life Sciences Ltd. Chiral design
WO2016020405A1 (en) * 2014-08-04 2016-02-11 Sandoz Ag Novel routes of synthesis for the preparation of suvorexant
CN110963959B (zh) * 2018-09-30 2023-01-24 南京药石科技股份有限公司 一种合成n-保护及非保护的3-羟基-4,4-二甲基哌啶的制备方法
CN111423454B (zh) * 2020-04-24 2021-06-22 苏州大学 哌嗪类化合物及其在制备趋化因子受体ccr2拮抗剂中的应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003081937A (ja) 2001-09-07 2003-03-19 Bayer Ag ベンゼンスルホンアミド誘導体
WO2003095029A1 (en) 2002-05-10 2003-11-20 F. Hoffmann-La Roche Ag Bisphosphonic acid for the treatment and prevention of osteoporosis
EP1608374B9 (en) * 2003-03-24 2009-04-08 Axikin Pharmaceuticals, Inc. 2-phenoxy- and 2-phenylsulfomamide derivatives with ccr3 antagonistic activity for the treatment of asthma and other inflammatory or immunological disorders
NZ543287A (en) 2003-04-15 2008-08-29 Merck & Co Inc Benzoxazinyl-amidocyclopentyl-heterocyclic modulators of chemokine receptors
CA2521625A1 (en) * 2003-04-17 2004-11-04 Merck & Co., Inc. Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity
EP1847537A1 (en) 2006-04-21 2007-10-24 F. Hoffmann-La Roche Ag Dicarboxamide derivatives

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ATE476424T1 (de) 2010-08-15
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CL2007001090A1 (es) 2008-01-11
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US20070249589A1 (en) 2007-10-25
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