AR060605A1 - Derivados de diazepano como antagonistas del receptor ccr2 - Google Patents
Derivados de diazepano como antagonistas del receptor ccr2Info
- 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
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- heterocyclyl
- heteroaryl
- phenyl
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 2
- 102100031151 C-C chemokine receptor type 2 Human genes 0.000 title 1
- 101710149815 C-C chemokine receptor type 2 Proteins 0.000 title 1
- QPMLSUSACCOBDK-UHFFFAOYSA-N diazepane Chemical class C1CCNNCC1 QPMLSUSACCOBDK-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 18
- 125000000217 alkyl group Chemical group 0.000 abstract 16
- 125000000623 heterocyclic group Chemical group 0.000 abstract 16
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 13
- 125000001072 heteroaryl group Chemical group 0.000 abstract 10
- 125000004432 carbon atom Chemical group C* 0.000 abstract 8
- 125000001424 substituent group Chemical group 0.000 abstract 7
- 229910003827 NRaRb Inorganic materials 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 abstract 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 2
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000002619 bicyclic group Chemical group 0.000 abstract 2
- 150000001602 bicycloalkyls Chemical group 0.000 abstract 2
- MPVDXIMFBOLMNW-UHFFFAOYSA-N chembl1615565 Chemical compound OC1=CC=C2C=C(S(O)(=O)=O)C=C(S(O)(=O)=O)C2=C1N=NC1=CC=CC=C1 MPVDXIMFBOLMNW-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 1
- 125000006528 (C2-C6) alkyl group Chemical group 0.000 abstract 1
- 102000004497 CCR2 Receptors Human genes 0.000 abstract 1
- 108010017312 CCR2 Receptors Proteins 0.000 abstract 1
- 102000004499 CCR3 Receptors Human genes 0.000 abstract 1
- 108010017316 CCR3 Receptors Proteins 0.000 abstract 1
- 102000004274 CCR5 Receptors Human genes 0.000 abstract 1
- 108010017088 CCR5 Receptors Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000005530 alkylenedioxy group Chemical group 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
Classifications
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- C07D405/00—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
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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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- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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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
- 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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- 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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- C07D471/10—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.
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WO2009133778A1 (ja) * | 2008-04-30 | 2009-11-05 | 住友化学株式会社 | 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 |
BRPI0915761A2 (pt) | 2008-07-16 | 2015-11-03 | Hoffmann La Roche | composto de heterociclila para tratamento de doença cardiovascular |
BRPI0916574A2 (pt) * | 2008-07-28 | 2015-11-10 | Hoffmann La Roche | derivados de diazepano e piperazina moduladores de receptores de quiomiocinas |
CA2744987C (en) | 2008-12-02 | 2018-01-16 | Chiralgen, Ltd. | Method for the synthesis of phosphorus atom modified nucleic acids |
BR112012000828A8 (pt) | 2009-07-06 | 2017-10-10 | Ontorii Inc | Novas pró-drogas de ácido nucleico e métodos de uso das mesmas |
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 |
WO2012039448A1 (ja) | 2010-09-24 | 2012-03-29 | 株式会社キラルジェン | 不斉補助基 |
PL2621903T3 (pl) * | 2010-09-29 | 2017-08-31 | Intervet International B.V. | Związki n-heteroarylu |
UA109290C2 (uk) * | 2010-10-07 | 2015-08-10 | Спільні кристали і солі інгібіторів ccr3 | |
KR20130121891A (ko) * | 2010-12-01 | 2013-11-06 | 얀센 파마슈티카 엔.브이. | Ccr2의 4-치환된-사이클로헥실아미노-4-피페리디닐-아세트아미드길항제 |
US9605019B2 (en) | 2011-07-19 | 2017-03-28 | Wave Life Sciences Ltd. | Methods for the 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 |
AU2013288048A1 (en) | 2012-07-13 | 2015-01-22 | Wave Life Sciences Ltd. | Asymmetric auxiliary group |
KR101835401B1 (ko) | 2012-07-13 | 2018-03-08 | 신 니뽄 바이오메디칼 라보라토리즈, 엘티디. | 키랄 핵산 어쥬번트 |
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US10322173B2 (en) | 2014-01-15 | 2019-06-18 | Shin Nippon Biomedical Laboratories, Ltd. | Chiral nucleic acid adjuvant having anti-allergic activity, and anti-allergic agent |
WO2015108048A1 (ja) | 2014-01-15 | 2015-07-23 | 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 |
EP3095461A4 (en) | 2014-01-15 | 2017-08-23 | Shin Nippon Biomedical Laboratories, Ltd. | Chiral nucleic acid adjuvant having immunity induction activity, and immunity induction activator |
PT3094728T (pt) | 2014-01-16 | 2022-05-19 | Wave Life Sciences Ltd | Desenho quiral |
EP3177616B1 (en) * | 2014-08-04 | 2021-02-24 | 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 |
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CA2649636A1 (en) | 2007-11-01 |
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AU2007242883A1 (en) | 2007-11-01 |
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EP2010506B1 (en) | 2010-08-04 |
JP2009534346A (ja) | 2009-09-24 |
US7632829B2 (en) | 2009-12-15 |
DE602007008222D1 (de) | 2010-09-16 |
CN101472904A (zh) | 2009-07-01 |
RU2008145220A (ru) | 2010-05-27 |
KR20090008359A (ko) | 2009-01-21 |
AU2007242883B2 (en) | 2012-09-27 |
TW200808744A (en) | 2008-02-16 |
CL2007001090A1 (es) | 2008-01-11 |
ATE476424T1 (de) | 2010-08-15 |
EP2010506A1 (en) | 2009-01-07 |
WO2007122103A1 (en) | 2007-11-01 |
US20070249589A1 (en) | 2007-10-25 |
JP5016666B2 (ja) | 2012-09-05 |
BRPI0710512A2 (pt) | 2012-06-05 |
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