AR079495A1 - Derivados de fenilimidazol heteroaromaticos como inhibidores de enzima pde10a - Google Patents

Derivados de fenilimidazol heteroaromaticos como inhibidores de enzima pde10a

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Publication number
AR079495A1
AR079495A1 ARP100104668A ARP100104668A AR079495A1 AR 079495 A1 AR079495 A1 AR 079495A1 AR P100104668 A ARP100104668 A AR P100104668A AR P100104668 A ARP100104668 A AR P100104668A AR 079495 A1 AR079495 A1 AR 079495A1
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Argentina
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compound
alkyl
formula
provides
subject
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ARP100104668A
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Lundbeck & Co As H
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Publication of AR079495A1 publication Critical patent/AR079495A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Valve Device For Special Equipments (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente se dirige a compuestos, que son inhibidores de la enzima PDE10A. Proporciona una composicion farmacéutica que comprende una cantidad terapéuticamente efectiva de un compuesto y un portador farmacéuticamente aceptable. La presente también proporciona procesos para la preparacion de los compuestos de la formula 1. La presente además proporciona un método de tratar un sujeto que padece de un trastorno neurodegenerativo que comprende la administracion al sujeto de una cantidad terapéuticamente efectiva de un compuesto de la formula 1. La presente también proporciona un método para tratar a un sujeto que padece de adiccion a las drogas que comprende la administracion a un sujeto de una cantidad terapéuticamente efectiva de un compuesto de la formula 1. La presente además proporciona un método para tratar a un sujeto que padece de un trastorno psiquiátrico que comprende la administracion al sujeto de una cantidad terapéuticamente efectiva de un compuesto de la formula 1. Reivindicacion 1: Un compuesto que tiene la estructura 1 en donde HET1 es un grupo heteroaromáticos de 2 que contiene de 2 a 4 átomos de nitrogeno: en donde Y puede ser N o CH, Z puede ser N o C, y en donde HET1 puede sustituirse opcionalmente con hasta tres sustituyentes R2-R4 individualmente seleccionados de hidrogeno, alquilo C1-6 halogeno; ciano, haloalquilo C1-6; arilo, alcoxi e hidroxialquilo C1-6, y en donde * denota el punto de union, HET2 es un grupo heteroaromático de la formula 3 o 4: en donde Y puede ser N, S, O o CH, X puede ser N o CH, y en donde HET2 puede sustituirse opcionalmente con hasta tres sustituyentes R5, R6 y R7 individualmente seleccionados de hidrogeno, alquilo C1-6 halogeno; ciano, haloalquilo C1-6; arilo, alcoxi e hidroxialquilo C1-6, y en donde * denota el punto de union, -L- es un enlazante seleccionado de -S-CH2-, -CH2-S-, -CH2-CH2-, -CH=CH-, y C=C R1 se selecciona de H, alquilo C1-6 alquil C1-6 cicloalquilo C3-8; hidroxialquilo C1-6, CH2CN, CH2C(O)NH2, arilalquilo C1-6, y alquil C1-6- heterocicloalquilo, y tautomeros y sales de adicion de ácidos farmacéuticamente aceptables de los mismos, y formas polimorficas de los mismos, siempre que el compuesto no sea 2-(5-fenil-1H-imidazol-2-ilmetilsulfanil)-1H-benzoimidazol o 2-(5-fenil-1H-imidazol-2-il-sulfanil-metil)-1H-benzoimidazol.
ARP100104668A 2009-12-17 2010-12-16 Derivados de fenilimidazol heteroaromaticos como inhibidores de enzima pde10a AR079495A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DKPA200901339 2009-12-17

Publications (1)

Publication Number Publication Date
AR079495A1 true AR079495A1 (es) 2012-02-01

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ID=44246808

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104668A AR079495A1 (es) 2009-12-17 2010-12-16 Derivados de fenilimidazol heteroaromaticos como inhibidores de enzima pde10a

Country Status (36)

Country Link
US (2) US9096589B2 (es)
EP (1) EP2513107B1 (es)
JP (1) JP5901535B2 (es)
KR (1) KR101803984B1 (es)
CN (1) CN102741250B (es)
AR (1) AR079495A1 (es)
AU (1) AU2010333435B2 (es)
BR (1) BR112012017205A2 (es)
CA (1) CA2783726A1 (es)
CO (1) CO6612245A2 (es)
CR (1) CR20120319A (es)
CY (1) CY1115843T1 (es)
DK (1) DK2513107T3 (es)
DO (1) DOP2012000165A (es)
EA (1) EA023663B1 (es)
ES (1) ES2514647T3 (es)
GE (1) GEP20156241B (es)
GT (1) GT201200171A (es)
HK (1) HK1177208A1 (es)
HR (1) HRP20140898T1 (es)
IL (1) IL220327A (es)
MA (1) MA33922B1 (es)
MX (1) MX2012006969A (es)
MY (1) MY158197A (es)
NZ (1) NZ600260A (es)
PL (1) PL2513107T3 (es)
PT (1) PT2513107E (es)
RS (1) RS53579B1 (es)
SG (1) SG181674A1 (es)
SI (1) SI2513107T1 (es)
SM (1) SMT201400158B (es)
TN (1) TN2012000271A1 (es)
TW (1) TWI485151B (es)
UA (1) UA108487C2 (es)
WO (1) WO2011072694A1 (es)
ZA (1) ZA201204419B (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI485151B (zh) 2009-12-17 2015-05-21 Lundbeck & Co As H 作為pde10a酵素抑制劑之雜芳香族苯基咪唑衍生物
TWI487705B (zh) 2009-12-17 2015-06-11 Lundbeck & Co As H 作為pde10a酵素抑制劑之雜芳香族芳基***衍生物
TWI481607B (zh) * 2009-12-17 2015-04-21 Lundbeck & Co As H 作為pde10a酵素抑制劑的2-芳基咪唑衍生物
WO2011150156A2 (en) * 2010-05-26 2011-12-01 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
JO3089B1 (ar) * 2010-11-19 2017-03-15 H Lundbeck As مشتقات ايميدازول كمثبطات لانزيمات pde10a
US8552045B2 (en) 2010-11-19 2013-10-08 H. Lundbeck A/S Tricyclic imidazole compounds as PDE10 inhibitors
CA2824047C (en) 2011-01-11 2019-06-18 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
CN103476757A (zh) 2011-02-18 2013-12-25 阿勒根公司 作为磷酸二酯酶10(pde10a)的抑制剂的取代的6,7-二烷氧基-3-异喹啉醇衍生物
US9938269B2 (en) * 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
UA108711C2 (uk) * 2011-09-19 2015-05-25 Ф. Хоффманн-Ля Рош Аг Сполуки триазолопіридину як інгібітори фосфодіестерази pde10a
WO2013050527A1 (en) 2011-10-05 2013-04-11 H. Lundbeck A/S Quinazoline derivatives as pde10a enzyme inhibitors
TWI570124B (zh) 2011-12-21 2017-02-11 H 朗德貝克公司 作為pde10a酵素抑制劑的喹啉衍生物
BR112014031798A2 (pt) * 2012-06-19 2017-06-27 Sunovion Pharmaceuticals Inc compostos de heteroaril e métodos de uso destes
WO2014071044A1 (en) 2012-11-01 2014-05-08 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a)
US9790203B2 (en) * 2012-11-26 2017-10-17 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
US9200016B2 (en) 2013-12-05 2015-12-01 Allergan, Inc. Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)

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WO2008006372A1 (en) * 2006-07-10 2008-01-17 H. Lundbeck A/S (3-aryl-piperazin-1-yl), (2-aryl-morpholin-4-yl) and (2-aryl- thiomorpholin-4-yl) derivatives of 6,7-dialkoxyquinazoline, 6,7- dialkoxyphtalazine and 6,7-dialkoxyisoquinoline
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TWI501965B (zh) * 2008-06-20 2015-10-01 Lundbeck & Co As H 作為pde10a酵素抑制劑之新穎苯基咪唑衍生物
US8133897B2 (en) 2008-06-20 2012-03-13 H. Lundbeck A/S Phenylimidazole derivatives as PDE10A enzyme inhibitors
UA102693C2 (ru) 2008-06-20 2013-08-12 Х. Луннбек А/С Производные фенилимидазола как ингибиторы фермента pde10a
TWI481607B (zh) * 2009-12-17 2015-04-21 Lundbeck & Co As H 作為pde10a酵素抑制劑的2-芳基咪唑衍生物
TWI485151B (zh) 2009-12-17 2015-05-21 Lundbeck & Co As H 作為pde10a酵素抑制劑之雜芳香族苯基咪唑衍生物
TWI487705B (zh) 2009-12-17 2015-06-11 Lundbeck & Co As H 作為pde10a酵素抑制劑之雜芳香族芳基***衍生物
TW201200516A (en) 2009-12-17 2012-01-01 Lundbeck & Co As H Phenylimidazole derivatives comprising an ethynylene linker as PDE10A enzyme inhibitors

Also Published As

Publication number Publication date
EA201290516A1 (ru) 2013-01-30
TWI485151B (zh) 2015-05-21
AU2010333435A1 (en) 2012-06-21
MX2012006969A (es) 2012-07-17
AU2010333435B2 (en) 2016-09-08
KR20120112460A (ko) 2012-10-11
PL2513107T3 (pl) 2014-12-31
US20120309714A1 (en) 2012-12-06
JP2013514284A (ja) 2013-04-25
HK1177208A1 (en) 2013-08-16
TW201200515A (en) 2012-01-01
IL220327A (en) 2014-12-31
GEP20156241B (en) 2015-02-10
SI2513107T1 (sl) 2014-11-28
MY158197A (en) 2016-09-15
RS53579B1 (en) 2015-02-27
CN102741250A (zh) 2012-10-17
CY1115843T1 (el) 2017-01-25
WO2011072694A1 (en) 2011-06-23
SMT201400158B (it) 2015-01-15
TN2012000271A1 (en) 2013-12-12
ES2514647T3 (es) 2014-10-28
KR101803984B1 (ko) 2017-12-01
ZA201204419B (en) 2013-08-28
CR20120319A (es) 2012-08-16
IL220327A0 (en) 2012-08-30
US20150290191A1 (en) 2015-10-15
EP2513107A1 (en) 2012-10-24
DK2513107T3 (da) 2014-10-13
GT201200171A (es) 2015-01-16
US9096589B2 (en) 2015-08-04
CA2783726A1 (en) 2011-06-23
HRP20140898T1 (hr) 2014-11-07
JP5901535B2 (ja) 2016-04-13
EA023663B1 (ru) 2016-06-30
DOP2012000165A (es) 2012-12-15
NZ600260A (en) 2014-08-29
US9669029B2 (en) 2017-06-06
MA33922B1 (fr) 2013-01-02
PT2513107E (pt) 2014-10-22
CO6612245A2 (es) 2013-02-01
SG181674A1 (en) 2012-07-30
UA108487C2 (en) 2015-05-12
CN102741250B (zh) 2015-10-14
EP2513107B1 (en) 2014-07-30
BR112012017205A2 (pt) 2018-08-14

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