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AR077156A1 - Inhibidores de transportador de glicina-1 - Google Patents

Inhibidores de transportador de glicina-1

Info

Publication number
AR077156A1
AR077156A1 ARP070102897A ARP070102897A AR077156A1 AR 077156 A1 AR077156 A1 AR 077156A1 AR P070102897 A ARP070102897 A AR P070102897A AR P070102897 A ARP070102897 A AR P070102897A AR 077156 A1 AR077156 A1 AR 077156A1
Authority
AR
Argentina
Prior art keywords
amino
alkyl
alkoxy
haloalkoxy
haloalkyl
Prior art date
Application number
ARP070102897A
Other languages
English (en)
Inventor
Albert Amegadzie
Wenyuan Qian
Stephen Hitchcock
Xiaoyang Xia
Scott S Harried
Original Assignee
Amgen Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38565553&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR077156(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of AR077156A1 publication Critical patent/AR077156A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K31/495—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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A—HUMAN NECESSITIES
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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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • C07D213/02—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
    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—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
    • C07D243/08—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 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D295/14—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D295/14—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20—Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms

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  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
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  • Hospice & Palliative Care (AREA)
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  • Physical Education & Sports Medicine (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1) caracterizado porque n es un numero entero de 1 a 3; R1 y R2 se seleccionan independientemente de hidrogeno, alquilo, haloalquilo, alcoxi, haloalcoxi, arilo, heteroarilo, cicloalquilo, o heterociclilo, en donde los anillos mencionados anteriormente se sustituyen opcionalmente con Ra, Rb, o Rc independientemente seleccionados de alquilo, halo, haloalquilo, alcoxi, haloalcoxi, hidroxi, ciano, amino monosustituido, o amino disustituido; o R1 y R2, cuando se unen al mismo átomo de carbono, se pueden combinar para formar cicloalquilo o heterociclilo saturado monocíclico para proporcionar un anillo espiro, en donde el cicloalquilo o el heterocíclico monocíclico saturado puede ser opcionalmente sustituido con Rd, Re, o Rf independientemente seleccionado de alquilo, alcoxi, fluoro, fluoroalquilo, fluoroalcoxi, hidroxi, amino monosustituido o amino disustituido; o R1 y R2, cuando se unen en las posiciones 2 y 5 o 3 y 6 de los átomos de carbono del anillo de piperazina, pueden combinarse para formar una cadena de alquileno C1-3 en donde uno de los átomos de carbono en la cadena de alquileno se reemplaza opcionalmente mediante un -NR-, -O-, -S(O)n- (donde R es hidrogeno o alquilo y n es 0-2) y además en donde uno o dos átomos de hidrogeno en la cadena de alquileno puede ser opcionalmente sustituido con uno o dos alquilo; R3, R4 y R5 son independientemente hidrogeno, alquilo, fluoro o fluoroalquilo; y Ar1 y Ar2 son independientemente arilo, heteroarilo, cicloalquilo, o heterociclilo donde cada uno de los anillos mencionados anteriormente se sustituye opcionalmente con Rg; Rh o Ri donde Rg es alquilo, -C=C-R6 (donde R6 es arilo o heteroarilo), halo, haloalquilo, haloalcoxi, alquiltio, ciano, alcoxi, amino, amino monosustituido, amino disustituido, sulfonilo, acilo, carboxi, alcoxicarbonilo, hidroxialquilo, alcoxialquilo, aminoalquilo, hidroxialcoxi, alcoxialcoxi, aminoalcoxi, aminosulfonilo, aminocarbonilo, o acilamino y Rh y Ri se seleccionan i independientemente de alquilo, halo, haloalquilo, haloalcoxi, alquiltio, ciano, alcoxi, amino, amino monosustituido, amino disustituido, sulfonilo, acilo, carboxi, alcoxicarbonilo, hidroxialquilo, alcoxialquilo, aminoalquilo, hidroxialcoxi, alcoxialcoxi, aminoalcoxi, aminosulfonilo, aminocarbonilo, acilamino, arilo, heteroarilo, cicloalquilo, o heterociclilo donde el anillo aromático o alicíclico en Rg, Rh y Ri es opcionalmente sustituido con Rj, Rk o Rl que se seleccionan independientemente de alquilo, halo, haloalquilo, haloalcoxi, alquiltio, ciano, alcoxi, amino, amino monosustituido, amino disustituido, sulfonilo, acilo, carboxi, alcoxicarbonilo, hidroxialquilo alcoxialquilo, aminoalquilo, hidroxialcoxi, alcoxialcoxi, aminoalcoxi, aminosulfonilo, aminocarbonilo, o aciloamino; o una sal farmacéuticamente aceptable de los mismos siempre y cuando: el compuesto de la formula (1) no sea ácido 2-(4- benzidrilpiperazin-1-il)acético, ácido 2-(4-((4-clorofenil) (fenil)metil)piperazin-1-il)acético, ácido 2-((2R,5S)-4-( R)-(4-(1H-tetrazol-5-il)fenil)(3-hidroxifenil)metil)-2,5-dimetilpiperazin-1-il)acético o 2-((2R,5S)-4-((R)-(4-cianofenil) (3-hidroxifenil)metil)-2,5-dimetilpiperazin-1-il)ácido acético.
ARP070102897A 2006-06-28 2007-06-28 Inhibidores de transportador de glicina-1 AR077156A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US81693606P 2006-06-28 2006-06-28
US85002706P 2006-10-06 2006-10-06

Publications (1)

Publication Number Publication Date
AR077156A1 true AR077156A1 (es) 2011-08-10

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ID=38565553

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070102897A AR077156A1 (es) 2006-06-28 2007-06-28 Inhibidores de transportador de glicina-1

Country Status (29)

Country Link
US (4) US7538114B2 (es)
EP (3) EP2565183A1 (es)
JP (1) JP5179486B2 (es)
KR (2) KR101288781B1 (es)
AR (1) AR077156A1 (es)
AU (1) AU2007265467C1 (es)
BR (1) BRPI0713381A2 (es)
CA (1) CA2655159C (es)
CR (1) CR10570A (es)
CY (1) CY1115119T1 (es)
DK (1) DK2041088T3 (es)
EA (1) EA014959B3 (es)
ES (1) ES2452822T3 (es)
HK (1) HK1126205A1 (es)
HR (1) HRP20140336T1 (es)
IL (1) IL195473A (es)
MX (1) MX2008015448A (es)
MY (1) MY153714A (es)
NO (1) NO20090402L (es)
NZ (1) NZ573129A (es)
PE (2) PE20120223A1 (es)
PL (1) PL2041088T3 (es)
PT (1) PT2041088E (es)
RS (1) RS53277B (es)
SG (1) SG172685A1 (es)
SI (1) SI2041088T1 (es)
TW (1) TWI429631B (es)
WO (1) WO2008002583A1 (es)
ZA (1) ZA201004216B (es)

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EP2231601B1 (en) * 2007-12-12 2014-06-18 Amgen Inc. Glycine transporter-1 inhibitors
CN103096893B (zh) 2010-06-04 2016-05-04 阿尔巴尼分子研究公司 甘氨酸转运体-1抑制剂、其制备方法及其用途
US9012489B2 (en) 2011-08-03 2015-04-21 Boehringer Ingelheim International Gmbh Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament
JOP20130213B1 (ar) 2012-07-17 2021-08-17 Takeda Pharmaceuticals Co معارضات لمستقبلht3-5
EP3134406A1 (en) 2014-04-24 2017-03-01 Dart Neuroscience (Cayman) Ltd Substituted 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole and 4,5,6,7-tetrahydro-2h-pyrazolo [4,3-c]pyridine compounds as glyt1 inhibitors
EP3201203B1 (en) 2014-09-29 2021-05-19 Takeda Pharmaceutical Company Limited Crystalline form of 1-(1-methyl-1h-pyrazol-4-yl)-n-((1r,5s,7s)-9-methyl-3-oxa-9-azabicyclo[3.3.1]nonan-7-yl)-1h-indole-3-carboxamide
EP3215500A1 (en) 2014-11-05 2017-09-13 Dart NeuroScience (Cayman) Ltd. Substituted azetidinyl compounds as glyt1 inhibitors
KR101753617B1 (ko) 2016-05-10 2017-07-11 주식회사 뉴로벤티 피페라진-1-카복사미딘 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 자폐 범주성 장애 예방 및 치료용 약학적 조성물

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