AR069045A1 - Derivados de amina que tienen una actividad antagonista del receptor npy y5, y sus usos - Google Patents
Derivados de amina que tienen una actividad antagonista del receptor npy y5, y sus usosInfo
- Publication number
- AR069045A1 AR069045A1 ARP080104670A ARP080104670A AR069045A1 AR 069045 A1 AR069045 A1 AR 069045A1 AR P080104670 A ARP080104670 A AR P080104670A AR P080104670 A ARP080104670 A AR P080104670A AR 069045 A1 AR069045 A1 AR 069045A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- formula
- compound
- solvate
- salt
- Prior art date
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- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C311/05—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
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- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/07—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
- C07C311/43—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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- C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
- C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
- C07C317/36—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atoms of the amino groups bound to hydrogen atoms or to carbon atoms
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- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D209/04—Indoles; Hydrogenated indoles
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
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- C07D277/62—Benzothiazoles
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Abstract
Reivindicación 1: Un compuesto de la fórmula (1): R¹-Y-N(R²)-X-N(R⁷)-Z (1) una sal farmacéuticamente aceptable o solvato del mismo caracterizado porque: R¹ es alquilo inferior opcionalmente sustituido; Y es -S(O)ₙ-, donde n es 1 ó 2, o -CO-; R² es hidrógeno o alquilo inferior opcionalmente sustituido; R¹ y R² tomados conjuntamente pueden formar alquileno inferior; R⁷ es hidrógeno o alquilo inferior opcionalmente sustituido; X es alquileno inferior opcionalmente sustituido, alquenileno inferior opcionalmente sustituido, -CO-alquileno inferior opcionalmente sustituido, -CO-alquenileno opcionalmente sustituido, o un grupo de la fórmula (2) en donde: R³, R⁴, R⁵ y R⁶, son, cada uno de ellos e independientemente entre si, hidrógeno o alquilo inferior opcionalmente sustituido; el anillo A es cicloalquileno opcionalmente sustituido, cicloalquenileno opcionalmente sustituido, bicicloalquileno opcionalmente sustituido, arileno opcionalmente sustituido o heterociclildiilo opcionalmente sustituido; p y q son cada uno de ellos e independientemente entre sí, un número entero entre 0 y 2, ni p ni q son 0, y con la condición de que el anillo A no sea un grupo de la fórmula (3) en donde R¹⁴ es fenilo opcionalmente sustituido; -NR²-X- puede ser un grupo de la fórmula (4) en donde el anillo que contiene al N es piperidindiilo, piperazindiilo, piridindiilo, pirazindiilo, pirrolidindiilo o pirrolidiilo; U es alquileno inferior o alquenileno inferior; y Z es alquilo inferior opcionalmente sustituido, alquenilo opcionalmente sustituido, amino opcionalmente sustituido, alcoxi inferior opcionalmente sustituido, carbociclilo opcionalmente sustituido o heterociclilo opcionalmente sustituido; con la condición de que Z no sea heterociclilo fusionado consistente en tres anillos, tiazolilo opcionalmente sustituido o quinazolinilo opcionalmente sustituido, y con la condición de que quede excluido un compuesto en la que X es un grupo de la fórmula (2), el anillo A sea cicloalquileno opcionalmente sustituido, q es 1, q es 0 y Z es pirimidinilo. Reivindicación 19: Una composición farmacéutica caracterizada porque comprende el compuesto, sal farmacéuticamente aceptable o solvato del mismo, de acuerdo con una cualquiera de las reivindicaciones 1 a 18 como un ingrediente activo. Reivindicación 20: Un antagonista del receptor NPY Y5 caracterizado porque comprende el compuesto, sal farmacéuticamente aceptable o solvato del mismo, de acuerdo con una cualquiera de las reivindicaciones 1 a 18, como un ingrediente activo. Reivindicación 21: Un compuesto de la fórmula (5) una sal o solvato del mismo, caracterizado porque R¹ es etilo o ter-butilo. Reivindicación 22: Un compuesto de la fórmula (6) una sal o solvato del mismo, caracterizado porque R¹ es etilo, isopropilo o ter-butilo. Reivindicación 23: Un compuesto de la fórmula (7) una sal o solvato del mismo, caracterizado porque: Z es un carbociclilo opcionalmente sustituido o heterociclilo opcionalmente sustituido. Reivindicación 24: Un compuesto de la fórmula (8) una sal o solvato del mismo, caracterizado porque R¹⁵ es NH₂ u OH; y Z es piridilo opcionalmente sustituido, piridazinilo opcionalmente sustituido, pirazinilo opcionalmente sustituido, pirimidinilo opcionalmente sustituido, quinolilo opcionalmente sustituido, isoquinolilo opcionalmente sustituido, benzotiazolilo opcionalmente sustituido, benzoxazolilo opcionalmente sustituido, benzopiridilo opcionalmente sustituido, benzopiridadiilo opcionalmente sustituido, benzimidazolilo opcionalmente sustituido, benzoxazolilo opcionalmente sustituido, tiazolopiridilo opcionalmente sustituido, benzisoxazolinonilo opcionalmente sustituido, benzoxazolinonilo opcionalmente sustituido, benzoxadinonilo opcionalmente sustituido o benzoxiazepinonilo opcionalmente sustituido.
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US (1) | US8299265B2 (es) |
EP (1) | EP2221051B1 (es) |
JP (1) | JP4375683B2 (es) |
KR (1) | KR20100075949A (es) |
CN (1) | CN101835471B (es) |
AR (1) | AR069045A1 (es) |
AU (1) | AU2008314974B2 (es) |
BR (1) | BRPI0818216A2 (es) |
CA (1) | CA2703797A1 (es) |
CL (1) | CL2008003159A1 (es) |
ES (1) | ES2445445T3 (es) |
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NZ (1) | NZ584816A (es) |
RU (1) | RU2460523C2 (es) |
SA (1) | SA08290668B1 (es) |
TW (1) | TWI367752B (es) |
WO (1) | WO2009054434A1 (es) |
ZA (1) | ZA201001954B (es) |
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EP2404902A1 (en) | 2009-03-05 | 2012-01-11 | Shionogi&Co., Ltd. | Piperidine and pyrrolidine derivatives having npy y5 receptor antagonism |
US8653125B2 (en) | 2009-03-05 | 2014-02-18 | Shionogi Co., Ltd. | Cyclohexane derivative having NPY Y5 receptor antagonism |
US8227618B2 (en) | 2009-04-23 | 2012-07-24 | Shionogi & Co., Ltd. | Amine-derivatives having NPY Y5 receptor antagonistic activity and the uses thereof |
CA2781659A1 (en) | 2009-11-25 | 2011-06-03 | Shionogi & Co., Ltd. | Method for producing cyclohexane derivative |
WO2011096462A1 (ja) * | 2010-02-04 | 2011-08-11 | 塩野義製薬株式会社 | Npy y5受容体拮抗作用を有するヘテロ環化合物 |
WO2011132075A2 (en) | 2010-04-23 | 2011-10-27 | Shionogi & Company, Ltd. | A hydrate of a cyclohexanamine derivative |
WO2011152442A1 (ja) * | 2010-06-03 | 2011-12-08 | 塩野義製薬株式会社 | 2-クロロ-6-フルオロベンゾオキサゾールの製造方法 |
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US8916594B2 (en) * | 2011-04-27 | 2014-12-23 | Shionogi & Co., Ltd. | 5-membered ring heteroaromatic derivatives having NPY Y5 receptor antagonistic activity |
WO2012147765A1 (ja) * | 2011-04-27 | 2012-11-01 | 塩野義製薬株式会社 | Npy y5受容体拮抗作用を有するベンズイミダゾール誘導体 |
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EP2719390A4 (en) * | 2011-06-07 | 2014-12-03 | Japan Science & Tech Agency | CARBON MONOXIDE (CO) - BASED INHIBITION OF FATTY ACID AND CHOLESTEROL RECEPTION |
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CN103304555B (zh) * | 2012-03-08 | 2016-03-30 | 中国医学科学院医药生物技术研究所 | 一组苯-噁唑基衍生物及其制备方法和作为impdh抑制剂的相关应用 |
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CN102775373B (zh) * | 2012-08-10 | 2014-08-20 | 青岛农业大学 | 一种n-取代氨基香豆素类化合物及其制备与应用 |
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US8299265B2 (en) | 2012-10-30 |
TWI367752B (en) | 2012-07-11 |
JPWO2009054434A1 (ja) | 2011-03-03 |
KR20100075949A (ko) | 2010-07-05 |
MX2010003950A (es) | 2010-04-30 |
ZA201001954B (en) | 2011-05-25 |
EP2221051A4 (en) | 2011-04-27 |
CN101835471A (zh) | 2010-09-15 |
CN101835471B (zh) | 2012-10-10 |
ES2445445T3 (es) | 2014-03-03 |
US20100273842A1 (en) | 2010-10-28 |
JP4375683B2 (ja) | 2009-12-02 |
EP2221051A1 (en) | 2010-08-25 |
RU2460523C2 (ru) | 2012-09-10 |
SA08290668B1 (ar) | 2012-02-12 |
CL2008003159A1 (es) | 2009-11-13 |
CA2703797A1 (en) | 2009-04-30 |
TW200924740A (en) | 2009-06-16 |
BRPI0818216A2 (pt) | 2015-09-29 |
AU2008314974A1 (en) | 2009-04-30 |
EP2221051B1 (en) | 2013-12-11 |
WO2009054434A1 (ja) | 2009-04-30 |
RU2010120808A (ru) | 2011-11-27 |
AU2008314974B2 (en) | 2013-08-22 |
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