AR078731A1 - Octahidropirrolo (3,4-c) pirroles disustituidos como moduladores del receptor de orexina - Google Patents

Octahidropirrolo (3,4-c) pirroles disustituidos como moduladores del receptor de orexina

Info

Publication number
AR078731A1
AR078731A1 ARP100103874A ARP100103874A AR078731A1 AR 078731 A1 AR078731 A1 AR 078731A1 AR P100103874 A ARP100103874 A AR P100103874A AR P100103874 A ARP100103874 A AR P100103874A AR 078731 A1 AR078731 A1 AR 078731A1
Authority
AR
Argentina
Prior art keywords
group
substituted
alkyl
halo
methyl
Prior art date
Application number
ARP100103874A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR078731A1 publication Critical patent/AR078731A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—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
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Emergency Medicine (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Tales compuestos pueden ser utiles en composiciones farmacéuticas y en los métodos para el tratamiento de estados de enfermedad, trastornos o afecciones mediadas por la actividad de la orexina, tal como el insomnio. Reivindicacion 1: Una entidad química que es un compuesto de la Formula (1): en donde: R1 es un miembro seleccionado del grupo que consiste de: A) fenilo insustituido o sustituido con uno o dos miembros Ra y sustituido en la posicion orto con Rb; Ra se selecciona independientemente del grupo que consiste de: -H, halo, alquilo de -C1-4, alcoxi de -C1-4, y -NO2, en donde dos miembros adyacentes Ra pueden venir juntos para formar un anillo aromático de seis miembros; Rb es un miembro seleccionado del grupo que consiste de: a) halo, alcoxi de -C1-4, alquilo de -C1-4, -CF3, -OCF3, o -CN; b) un anillo de heteroarilo de 5 miembros que contiene un oxígeno o un miembro de azufre; c) un anillo de heteroarilo de 5 a 6 miembros que contiene uno, dos o tres miembros de nitrogeno, opcionalmente contiene un miembro de oxígeno, sustituido o no sustituido con halo o alquilo de -C1-4 y d) fenilo insustituido o sustituido con halo, -CH3, o -CF3; B) piridina insustituida o sustituida con uno o dos miembros Rc y sustituida con Rd, en donde Rd se coloca adyacente al punto de union por R1; Rc es alquilo de C1-4; Rd es un miembro seleccionado del grupo que consiste de: a) anillo de heteroarilo de 5-6 miembros seleccionado del grupo que consiste de: 1H-1,2,3-triazol-1-ilo, 2H-1,2,3-triazol-2-ilo, 1H-pirazol-5-ilo, 3-metil-1,2,4-oxadiazol-5-ilo, piridinilo, 3-metil-piridin-2-ilo; 1-(tetrahidro-2H-piran-2-il)-1H-pirazol-5-il), fenilo, y pirimidin-2-ilo; y b) -CF3, -Br y alcoxi de -C1-4; C) anillo de heteroarilo de 5 miembros seleccionado del grupo que consiste de: 2-metil-1,3-tiazol-ilo, 1H-pirazol-5-ilo, oxazol, isoxazolilo, tiofen-2-ilo, y furan-2-ilo, cada uno sustituido con fenilo insustituido o sustituido con -F; y D) anillo de arilo o heteroarilo de 5-13 miembros seleccionado del grupo que consiste de: 3-metilfuran-2-ilo, 9H-fluoreno, quinolina, cinnolina; 3-(1H-pirrol-1-iI)tiofen-2-ilo, 8-[1,2,3]-triazol-2-iI-naftalen-1-ilo, 2,3-dihidro-1,4-benzodioxin-5-ilo, 1H-indol-7-ilo, 4-fluoronaftalen-1-ilo, y naftalen-1-ilo, R2 es un miembro seleccionado del grupo que consiste de: A) un anillo de heteroarjio de 6 miembros que contiene dos miembros de nitrogeno sustituidos con uno o más miembros independientemente seleccionados del grupo que consiste de halo, alquilo de -C1-4, -CD3, -D, alcoxi de -C1-4, ciclopropilo, morfolin-2-ilo, alquilo de -CO2C1-4, -CO2H, -CH2OH, -C(O)N(alquilo de C1-4)2, -CF3, -CN, -OH, -NO2, -N(alquilo de C1-4)2, fenilo, furan-2-ilo, tiofen-2-ilo, 1H-pirazol-4-iIo, y pirrolidin-1-ilo; B) piridina sustituida con uno o dos miembros independientemente seleccionados del grupo que consiste de: halo, alquilo de -C1-4, alcoxi de -C1-4 y -CF3; C) anillo de heteroaribo de 9 miembros seleccionado del grupo que consiste de benzooxazol-2-ilo, 6-fluoro-1,3-benzotiazol, 1,3-benzotiazol, 6-metoxi-1,3-benzotiazol, 6-metil-1,3-benzotiazol, 6-cloro-benzotiazol-2-ilo, y 4-metil-6,7-dihidro-5H-ciclopenta[d]pirimidina; D) anillo de heteroarilo de 10 miembros seleccionados del grupo que consiste de quinoxalin-2-ilo, 3-metilquinoxalin-2-ilo, 6,7-difluoroquinoxalin-2-ilo, 3-(trifluorometil)quinoxabina, quinolina, 4-metilquinolina, y 6-fluoroquinazolin-2-ilo; y E) 4-metil-1,3,5-triazin-2-ilo o 2-metilpirimidin-4(3H)-ona; y sales farmacéuticamente aceptables de los compuestos de la Formula 1.
ARP100103874A 2009-10-23 2010-10-22 Octahidropirrolo (3,4-c) pirroles disustituidos como moduladores del receptor de orexina AR078731A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US25450909P 2009-10-23 2009-10-23

Publications (1)

Publication Number Publication Date
AR078731A1 true AR078731A1 (es) 2011-11-30

Family

ID=43385633

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP100103874A AR078731A1 (es) 2009-10-23 2010-10-22 Octahidropirrolo (3,4-c) pirroles disustituidos como moduladores del receptor de orexina
ARP190100557A AR114667A2 (es) 2009-10-23 2019-03-07 Octahidropirrolo[3,4-c]pirroles disustituidos como moduladores del receptor de orexina

Family Applications After (1)

Application Number Title Priority Date Filing Date
ARP190100557A AR114667A2 (es) 2009-10-23 2019-03-07 Octahidropirrolo[3,4-c]pirroles disustituidos como moduladores del receptor de orexina

Country Status (38)

Country Link
US (8) USRE48841E1 (es)
EP (3) EP3581575A1 (es)
JP (1) JP5759470B2 (es)
KR (3) KR20120105449A (es)
CN (1) CN102781942B (es)
AR (2) AR078731A1 (es)
AU (2) AU2010310595B2 (es)
BR (1) BR112012010820B1 (es)
CA (1) CA2778484C (es)
CL (1) CL2010001162A1 (es)
CO (1) CO6541572A2 (es)
CR (1) CR20120273A (es)
CY (2) CY1117743T1 (es)
DK (2) DK2491038T3 (es)
EA (1) EA022766B1 (es)
EC (1) ECSP12011908A (es)
ES (2) ES2585806T3 (es)
HK (2) HK1175463A1 (es)
HR (2) HRP20160781T1 (es)
HU (2) HUE043962T2 (es)
IL (1) IL219234A (es)
JO (2) JO3267B1 (es)
LT (1) LT3093291T (es)
ME (2) ME03452B (es)
MX (1) MX2012004753A (es)
NI (1) NI201200062A (es)
NZ (1) NZ599629A (es)
PE (1) PE20110404A1 (es)
PL (2) PL2491038T3 (es)
PT (2) PT2491038T (es)
RS (2) RS59004B1 (es)
SI (2) SI3093291T1 (es)
SM (1) SMT201600216B (es)
TR (1) TR201910327T4 (es)
TW (1) TWI481613B (es)
UA (1) UA107812C2 (es)
UY (1) UY32966A (es)
WO (1) WO2011050198A1 (es)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2491038T3 (pl) * 2009-10-23 2016-10-31 Dwupodstawione oktahydropirolo[3,4-c]pirole jako modulatory receptora oreksyny
WO2012145581A1 (en) 2011-04-20 2012-10-26 Janssen Pharmaceutica Nv Disubstituted octahy-dropyrrolo [3,4-c] pyrroles as orexin receptor modulators
US8501768B2 (en) * 2011-05-17 2013-08-06 Hoffmann-La Roche Inc. Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds
TWI555747B (zh) 2011-11-08 2016-11-01 艾克泰聯製藥有限公司 ２－（１，２，３－***－２－基）苯甲醯胺及３－（１，２，３－***－２－基）吡啶醯胺衍生物
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
EP2811997B1 (en) 2012-02-07 2018-04-11 Eolas Therapeutics Inc. Substituted prolines/piperidines as orexin receptor antagonists
SG10201702540UA (en) 2012-06-04 2017-05-30 Actelion Pharmaceuticals Ltd Benzimidazole-proline derivatives
DK2884978T3 (da) * 2012-08-16 2019-09-30 Scripps Research Inst Nye Kappa-opioidligander
JP6244365B2 (ja) 2012-10-10 2017-12-06 アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ ［オルトビ−（ヘテロ−）アリール］−［２−（メタビ−（ヘテロ−）アリール）−ピロリジン−１−イル］−メタノン誘導体であるオレキシン受容体アンタゴニスト
CN103012293A (zh) * 2012-12-13 2013-04-03 同济大学 一种抗失眠药物mk-4305中间体的合成方法
US9403813B2 (en) 2013-03-12 2016-08-02 Actelion Pharmaceuticals Ltd. Azetidine amide derivatives as orexin receptor antagonists
TW201444849A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途
TW201444821A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代之哌啶化合物及其作為食慾素受體調節劑之用途
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途
MX2015017961A (es) * 2013-07-03 2016-10-14 Abide Therapeutics Inc Compuestos orgánicos pirrolo-pirrol carbamato y relacionados, composiciones farmacéuticas y usos médicos de los mismos.
ES2696708T3 (es) 2013-12-04 2019-01-17 Idorsia Pharmaceuticals Ltd Uso de derivados de bencimidazol-prolina
WO2016020403A1 (en) * 2014-08-04 2016-02-11 Sandoz Ag Preparation of a benzoic acid derivative and its use for the preparation of suvorexant
ES2901418T3 (es) 2014-08-13 2022-03-22 Eolas Therapeutics Inc Difluoropirrolidinas como moduladores del receptor de orexina
CN107108566B (zh) 2014-09-11 2020-11-24 詹森药业有限公司 取代的2-氮杂双环化合物以及它们作为食欲素受体调节剂的用途
CN106349228B (zh) 2015-07-17 2019-07-09 广东东阳光药业有限公司 取代的喹唑啉酮类化合物及其制备方法和用途
CN106749269B (zh) * 2015-11-23 2019-01-04 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
WO2017088731A1 (zh) * 2015-11-24 2017-06-01 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
TN2018000280A1 (en) 2016-02-12 2020-01-16 Astrazeneca Ab Halo-substituted piperidines as orexin receptor modulators.
CR20180433A (es) * 2016-03-10 2018-11-07 Janssen Pharmaceutica Nv Métodos para tratar la depresión con antagonistas del receptor de orexina-2
CN109496213B (zh) 2016-05-12 2022-03-04 H.隆德贝克有限公司 螺环化合物及其制备和使用方法
CN105949203B (zh) * 2016-05-24 2018-07-13 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其使用方法和用途
CN107759620B (zh) * 2016-08-16 2021-11-12 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其使用方法和用途
JOP20190107A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
CN108299437B (zh) * 2017-01-13 2022-07-08 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
GB201702174D0 (en) * 2017-02-09 2017-03-29 Benevolentai Bio Ltd Orexin receptor antagonists
TWI756418B (zh) 2017-05-03 2022-03-01 瑞士商愛杜西亞製藥有限公司 2-([1,2,3]***-2-基)-苯甲酸衍生物之製備
GB201707499D0 (en) * 2017-05-10 2017-06-21 Benevolentai Bio Ltd Orexin receptor antagonists
GB201707504D0 (en) * 2017-05-10 2017-06-21 Benevolentai Bio Ltd Orexin receptor antagonists
KR20200046061A (ko) 2017-08-29 2020-05-06 룬드벡 라 졸라 리서치 센터 인코포레이티드 스피로사이클 화합물 및 이를 제조하고 사용하는 방법
PE20200665A1 (es) 2017-08-29 2020-06-11 Lundbeck La Jolla Research Center Inc Compuestos espirociclicos y sus metodos de preparacion y uso
US11324724B2 (en) 2017-09-28 2022-05-10 Boehringer Ingelheim International Gmbh N-(2,2-difluoroethyl)-N-[(pyrimidinylamino)propanyl]arylcarboxamides
CN109988169B (zh) * 2017-12-29 2022-02-01 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
CN109988170B (zh) * 2017-12-29 2022-04-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
CN109988171A (zh) * 2017-12-29 2019-07-09 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
GB201809295D0 (en) 2018-06-06 2018-07-25 Institute Of Cancer Res Royal Cancer Hospital Lox inhibitors
WO2020023723A1 (en) * 2018-07-27 2020-01-30 Icahn School Of Medicine At Mount Sinai Method of treating aggression with orexin receptor antagonists
EA202191356A1 (ru) * 2018-11-14 2021-08-11 Янссен Фармацевтика Нв Усовершенствованные способы синтеза для получения конденсированных гетероциклических соединений в качестве модуляторов рецептора орексина
GB201818750D0 (en) 2018-11-16 2019-01-02 Institute Of Cancer Res Royal Cancer Hospital Lox inhibitors
CN112142713A (zh) * 2019-06-27 2020-12-29 山东润博生物科技有限公司 一种咪草烟的合成方法
EP4010325A1 (en) * 2019-08-07 2022-06-15 Janssen Pharmaceutica NV Improved synthetic methods of making (2h-1,2,3-triazol-2-yl)phenyl compounds as orexin receptor modulators
CN112876478B (zh) * 2019-11-29 2022-07-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物的晶型
CN112876479B (zh) * 2019-11-29 2022-07-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物的晶型
CN112876477B (zh) * 2019-11-29 2022-07-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物的晶型
CN112876481B (zh) * 2019-11-29 2022-07-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物的晶型
CN112876480B (zh) * 2019-11-29 2022-07-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物的晶型
WO2022122009A1 (zh) * 2020-12-11 2022-06-16 苏州晶云药物科技股份有限公司 吡咯类衍生化合物的晶型及其制备方法
WO2022194122A1 (zh) * 2021-03-16 2022-09-22 上海翰森生物医药科技有限公司 含氮杂环的多环化合物及其制备方法和应用
CN114063673B (zh) * 2021-11-09 2023-03-03 万华化学集团股份有限公司 一种反应釜温度控制方法、***及存储介质
WO2023163964A1 (en) 2022-02-24 2023-08-31 Teva Czech Industries S.R.O. Solid state forms of seltorexant
WO2023180556A1 (en) 2022-03-24 2023-09-28 Janssen Pharmaceutica Nv Methods for treating agitation in subjects with mild cognitive impairment or major neurocognition disorder
TW202409039A (zh) * 2022-07-15 2024-03-01 美商百健Ｍａ公司 依莫帕米結合蛋白抑制劑及其用途
WO2024056016A1 (zh) * 2022-09-14 2024-03-21 江苏豪森药业集团有限公司 含氮杂环的多环化合物的自由碱晶型及其制备方法
WO2024109672A1 (zh) * 2022-11-23 2024-05-30 江苏恩华药业股份有限公司 一种二取代八氢吡咯并[3,4-c]吡咯甲基酮衍生物及其应用

Family Cites Families (151)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL7503310A (nl) 1975-03-20 1976-09-22 Philips Nv Verbindingen met antidepressieve werking.
GB1526331A (en) 1976-01-14 1978-09-27 Kefalas As Phthalanes
KR19990022524A (ko) 1995-06-06 1999-03-25 웨인스톡 스티븐 에프. 퀴놀리지논형화합물
GB9519563D0 (en) 1995-09-26 1995-11-29 Merck Sharp & Dohme Therapeutic agents
AU3555200A (en) 1999-03-17 2000-10-04 F. Hoffmann-La Roche Ag Oxazolone derivatives and their use as alpha-1 adrenoreceptor modulators
US6375897B1 (en) 2000-02-14 2002-04-23 Ansys Technologies, Inc. Urine collection cup
MY145722A (en) 2000-04-27 2012-03-30 Abbott Lab Diazabicyclic central nervous system active agents
US6809105B2 (en) 2000-04-27 2004-10-26 Abbott Laboratories Diazabicyclic central nervous system active agents
AU779266B2 (en) 2000-05-11 2005-01-13 Banyu Pharmaceutical Co., Ltd. N-acyltetrahydroisoquinoline derivatives
SE0100326D0 (sv) 2001-02-02 2001-02-02 Astrazeneca Ab New compounds
WO2002070527A1 (en) 2001-03-02 2002-09-12 Akzo Nobel N.V. Mass-selective purification of organometallics
WO2002070523A1 (en) 2001-03-07 2002-09-12 Pfizer Products Inc. Modulators of chemokine receptor activity
HUP0400326A2 (hu) 2001-06-28 2004-09-28 Smithkline Beecham P.L.C. Orexin receptor antagonistákként alkalmazható ciklikus N-(aril-karbonil)-amin-származékok és ezeket tartalmazó gyógyszerkészítmények
US6455722B1 (en) 2001-06-29 2002-09-24 Pabu Services, Inc. Process for the production of pentaerythritol phosphate alcohol
GB2383315B (en) 2001-12-18 2005-04-06 Christopher Donald Clarke Vehicle imaging system
GB0130341D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
DE10226943A1 (de) 2002-06-17 2004-01-08 Bayer Ag Phenylaminopyrimidine und ihre Verwendung
JP4498922B2 (ja) 2002-07-09 2010-07-07 アクテリオン ファーマシューティカルズ リミテッド ７，８，９，１０−テトラヒドロ−６Ｈ−アゼピノ、６，７，８，９−テトラヒドロ−ピリドおよび２，３−ジヒドロ−２Ｈ−ピロロ［２，１−ｂ］−キナゾリノン誘導体
CA2498091C (en) 2002-10-11 2011-03-22 Actelion Pharmaceuticals Ltd. Sulfonylamino-acetic acid derivatives
GB0225944D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
DE602004021786D1 (de) 2003-03-26 2009-08-13 Actelion Pharmaceuticals Ltd Tetrahydroisochinolylacetamidderivate zur verwendung als orexinrezeptorantagonisten
DE602004011204T2 (de) 2003-04-28 2008-12-24 Actelion Pharmaceuticals Ltd. Quinoxalin-3-on-verdindungen als orexin-rezeptor antagonisten.
US20040242641A1 (en) 2003-05-27 2004-12-02 Buckley Michael J. (1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane is an effective analgesic agent
WO2005005439A1 (en) 2003-07-09 2005-01-20 Suven Life Sciences Limited Benzothiazino indoles
TW200507850A (en) 2003-07-25 2005-03-01 Kyowa Hakko Kogyo Kk Pharmaceutical composition
WO2005023231A1 (en) 2003-09-10 2005-03-17 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Polypyrimidine tract binding protein promotes insulin secretory granule biogenesis
US20050065178A1 (en) 2003-09-19 2005-03-24 Anwer Basha Substituted diazabicycloakane derivatives
US7399765B2 (en) 2003-09-19 2008-07-15 Abbott Laboratories Substituted diazabicycloalkane derivatives
PL1691811T3 (pl) 2003-12-11 2014-12-31 Sunovion Pharmaceuticals Inc Skojarzenie leku uspokajającego i modulatora neuroprzekaźnikowego oraz sposoby poprawy jakości snu i leczenia depresji
HUP0400405A3 (en) 2004-02-10 2009-03-30 Sanofi Synthelabo Pyrimidine derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates
CN1926109B (zh) 2004-03-01 2011-04-13 埃科特莱茵药品有限公司 经取代的1,2,3,4-四氢异喹啉衍生物
US7435831B2 (en) 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
CN1950082B (zh) 2004-03-03 2013-02-06 凯莫森特里克斯股份有限公司 双环和桥连的含氮杂环化物
JP5236944B2 (ja) 2004-07-22 2013-07-17 カムブァ、アイピー、ヴェンチュァズ、エル、ピー 微生物感染を治療するためのリファマイシン誘導体
WO2006012396A1 (en) 2004-07-22 2006-02-02 Glaxo Group Limited Antibacterial agents
FR2874011B1 (fr) 2004-08-03 2007-06-15 Sanofi Synthelabo Derives de sulfonamides, leur preparation et leur application en therapeutique
WO2006052542A2 (en) 2004-11-04 2006-05-18 Neurogen Corporation Arylalkyl ureas as cb1 antagonists
WO2006056848A1 (en) 2004-11-24 2006-06-01 Pfizer Limited Octahydropyrrolo[3,4-c]pyrrole derivatives
DE102004061344A1 (de) 2004-12-20 2006-07-06 Siemens Ag Verfahren zur sicheren Auslegung eines Systems, zugehörige Systemkomponente und Software
RU2007146444A (ru) 2005-05-13 2009-06-20 Лексикон Фармасьютикалз, Инк. (Us) Полициклические соединения и способы их применения
WO2006124897A2 (en) 2005-05-13 2006-11-23 Lexicon Genetics Incorporated Methods and compositions for improving cognition
GB0510204D0 (en) 2005-05-19 2005-06-22 Chroma Therapeutics Ltd Enzyme inhibitors
US20080175795A1 (en) 2005-06-30 2008-07-24 Bexel Pharmaceuticals, Inc. Novel derivatives of amino acids for treatment of obesity and related disorders
GB0514018D0 (en) 2005-07-07 2005-08-17 Ionix Pharmaceuticals Ltd Chemical compounds
CA2620124A1 (en) * 2005-08-26 2007-03-01 Merck And Co., Inc. Diazaspirodecane orexin receptor antagonists
FR2896798A1 (fr) 2006-01-27 2007-08-03 Sanofi Aventis Sa Derives de sulfonamides, leur preparation et leur application en therapeutique
FR2896799B1 (fr) 2006-02-02 2008-03-28 Sanofi Aventis Sa Derives de sulfonamides, leur preparation et leur application en therapeutique
US7553836B2 (en) 2006-02-06 2009-06-30 Bristol-Myers Squibb Company Melanin concentrating hormone receptor-1 antagonists
WO2007126935A2 (en) 2006-03-29 2007-11-08 Merck & Co., Inc. Diazepan orexin receptor antagonists
WO2007126934A2 (en) 2006-03-29 2007-11-08 Merck & Co., Inc. Amidoethylthioether orexin receptor antagonists
JP2009535324A (ja) 2006-04-26 2009-10-01 アクテリオン ファーマシューティカルズ リミテッド 新規なピラゾロ−テトラヒドロピリジン誘導体
WO2007146761A2 (en) 2006-06-12 2007-12-21 Neurogen Corporation Diaryl pyrimidinones and related compounds
PL2049529T3 (pl) * 2006-07-14 2011-01-31 Merck Sharp & Dohme Podstawione związki diazepanowe - antagoniści receptora oreksyny
WO2008008517A2 (en) 2006-07-14 2008-01-17 Merck & Co., Inc. Bridged diazepan orexin receptor antagonists
WO2008008551A2 (en) 2006-07-14 2008-01-17 Merck & Co., Inc. 2-substituted proline bis-amide orexin receptor antagonists
EP2069332B1 (en) 2006-08-15 2011-03-02 Actelion Pharmaceuticals Ltd. Azetidine compounds as orexin receptor antagonists
WO2008026149A1 (en) 2006-08-28 2008-03-06 Actelion Pharmaceuticals Ltd 1,4,5,6, 7,8-hexahydro-i^1s-triaza-azulene derivatives as orexin receptor antagonists
JP2010503714A (ja) 2006-09-18 2010-02-04 エフ．ホフマン−ラ ロシュ アーゲー オクタヒドロピロロ［３，４−ｃ］ピロール誘導体、抗ウイルス剤としてのそれらの使用
TW200823227A (en) 2006-09-29 2008-06-01 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives
WO2008052139A2 (en) 2006-10-25 2008-05-02 Somaxon Pharmaceuticals, Inc. Ultra low dose doxepin and methods of using the same to treat sleep disorders
AU2007325403A1 (en) 2006-11-07 2008-06-05 Lexicon Pharmaceuticals, Inc. Methods of treating cognitive impairment and dementia
PE20081229A1 (es) 2006-12-01 2008-08-28 Merck & Co Inc Antagonistas de receptor de orexina de diazepam sustituido
US20110077200A1 (en) 2006-12-06 2011-03-31 Somaxon Pharmaceuticals, Inc. Combination therapy using low-dose doxepin for the improvement of sleep
RU2009127842A (ru) 2006-12-22 2011-01-27 Актелион Фармасьютиклз Лтд (Ch) ПРОИЗВОДНЫЕ 5,6,7,8-ТЕТРАГИДРОИМИДАЗО[1.5-а]ПИРАЗИНА
CL2008000836A1 (es) 2007-03-26 2008-11-07 Actelion Pharmaceuticals Ltd Compuestos derivados de tiazolidina, antagonistas del receptor de orexina; composicion farmaceutica que los comprende; y su uso en el tratamiento de neurosis emocional, depresion grave, trastornos psicoticos, alzheimer, parkinson, dolor, entre otras.
EP2142554B1 (en) 2007-04-25 2015-01-14 Bristol-Myers Squibb Company Non-basic melanin concentrating hormone receptor-1 antagonists
JP2010527924A (ja) 2007-05-18 2010-08-19 メルク・シャープ・エンド・ドーム・コーポレイション オキソ架橋ジアゼパンオレキシン受容体アンタゴニスト
FR2918061B1 (fr) * 2007-06-28 2010-10-22 Sanofi Aventis Derives de 6-cycloamino-3-(pyridin-4-yl)imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique.
US20090022670A1 (en) 2007-07-03 2009-01-22 Giuseppe Alvaro Novel compounds
WO2009004584A1 (en) 2007-07-03 2009-01-08 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.3.0]octane compounds
GB0712888D0 (en) 2007-07-03 2007-08-15 Glaxo Group Ltd Novel compounds
US20090011994A1 (en) 2007-07-06 2009-01-08 Bristol-Myers Squibb Company Non-basic melanin concentrating hormone receptor-1 antagonists and methods
WO2009011775A1 (en) 2007-07-13 2009-01-22 Merck & Co., Inc. Amidoethyl alkylamino orexin receptor antagonists
FR2918986B1 (fr) 2007-07-19 2009-09-04 Sanofi Aventis Sa Derives de 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]- pyridazine, leur preparation et leur application en therapeutique
CN101874028B (zh) 2007-07-27 2012-11-14 埃科特莱茵药品有限公司 2-氮杂-二环[3.3.0]辛烷衍生物
EP2185503A1 (en) 2007-08-02 2010-05-19 F. Hoffmann-Roche AG Monoamide derivatives as orexin receptor antagonists
EP2188282B1 (en) 2007-08-15 2013-01-23 Actelion Pharmaceuticals Ltd. 1,2-diamido-ethylene derivatives as orexin antagonists
CA2699328A1 (en) 2007-09-24 2009-04-02 Actelion Pharmaceuticals Ltd Pyrrolidines and piperidines as orexin receptor antagonists
WO2009058238A1 (en) 2007-10-29 2009-05-07 Merck & Co., Inc. Substituted diazepan orexin receptor antagonists
DE102007052177A1 (de) 2007-10-30 2009-05-07 Novega Produktionssysteme Gmbh Ortungsbake
EP2058001A1 (en) 2007-11-08 2009-05-13 Crossbeta Biosciences B.V. Enhancement of immunogenicity of antigens
CA2705411A1 (en) 2007-12-21 2009-07-02 F. Hoffmann-La Roche Ag Heteroaryl derivatives as orexin receptor antagonists
US8003649B2 (en) 2007-12-21 2011-08-23 Astrazeneca Ab Bicyclic derivatives for use in the treatment of androgen receptor associated conditions-155
GB0806536D0 (en) 2008-04-10 2008-05-14 Glaxo Group Ltd Novel compounds
KR20110022631A (ko) 2008-05-27 2011-03-07 인트라-셀룰라 써래피스, 인코퍼레이티드. 수면 장애 및 다른 장애를 치료하기 위한 방법 및 조성물
MX2011000462A (es) 2008-07-29 2011-04-05 Hoffmann La Roche Pirrolidin-3-ilmetil-amina como antagonista de orexina.
AR072899A1 (es) 2008-08-07 2010-09-29 Merck Sharp & Dohme Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad.
US20100267730A1 (en) 2008-10-09 2010-10-21 Giuseppe Alvaro Novel compounds
US8129384B2 (en) 2008-10-09 2012-03-06 Glaxo Group Limited Imidazo[1,2-a]pyrazines as orexin receptor antagonists
US8093255B2 (en) 2008-10-09 2012-01-10 Glaxo Group Limited Imidazo[1,2-A]pyrimidines as orexin receptor antagonists
EP2348856B1 (en) 2008-10-21 2013-08-14 Merck Sharp & Dohme Corp. 2,4-disubstituted pyrrolidine orexin receptor antagonists
US8710076B2 (en) 2008-10-21 2014-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
WO2010048017A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. Disubstituted azepan orexin receptor antagonists
CA2740190A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,3-disubstituted piperidine orexin receptor antagonists
US8466281B2 (en) 2008-10-21 2013-06-18 Merck Sharp & Dohme Corp. 2,5-disubstituted morpholine orexin receptor antagonists
EP2350066B1 (en) 2008-10-21 2013-08-28 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
JP2012507540A (ja) 2008-10-30 2012-03-29 メルク・シャープ・エンド・ドーム・コーポレイション ピリダジンカルボキサミド・オレキシン受容体アンタゴニスト
CA2741648A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. 2,5-disubstituted phenyl carboxamide orexin receptor antagonists
PE20110852A1 (es) 2008-10-30 2011-11-25 Merck Sharp & Dohme Antagonistas del receptor de orexina de isonicotinamida
EP2358712A1 (en) 2008-11-26 2011-08-24 Glaxo Group Limited Piperidine derivatives useful as orexin receptor antagonists
EP2358711A1 (en) 2008-11-26 2011-08-24 Glaxo Group Limited Piperidine derivatives useful as orexin receptor antagonists
EP2358713A1 (en) 2008-11-26 2011-08-24 Glaxo Group Limited Imidazopyridazine derivatives acting as orexin antagonists
UY32276A (es) 2008-12-02 2010-05-31 Glaxo Group Ltd Derivados de n-{[1s,4s,6s)-3-(2-piridinilcarbonil)-3-azabiciclo[4.1.0]hept-4-il}metil}-2heteroarilamina y uso de los mismos
EA201170742A1 (ru) 2008-12-02 2012-01-30 Глэксо Груп Лимитед Производные n-{[(1r,4s,6r)-3-(2-пиридинилкарбонил)-3-азабицикло[4.1.0]гепт-4-ил]метил}-2-гетероариламинов и их применения
GB0823467D0 (en) 2008-12-23 2009-01-28 Glaxo Group Ltd Novel Compounds
US20100214135A1 (en) 2009-02-26 2010-08-26 Microsoft Corporation Dynamic rear-projected user interface
AU2010240871A1 (en) 2009-04-24 2011-10-27 Glaxo Group Limited 3 -azabicyclo [4.1.0] heptanes used as orexin antagonists
JP2013502447A (ja) 2009-08-24 2013-01-24 グラクソ グループ リミテッド 睡眠障害の治療のためのオレキシン受容体アンタゴニストとしての５−メチル−ピペリジン誘導体
WO2011023585A1 (en) 2009-08-24 2011-03-03 Glaxo Group Limited Piperidine derivatives used as orexin antagonists
PL2491038T3 (pl) 2009-10-23 2016-10-31 Dwupodstawione oktahydropirolo[3,4-c]pirole jako modulatory receptora oreksyny
EP2491034B1 (en) 2009-10-23 2013-12-18 Janssen Pharmaceutica, N.V. Fused heterocyclic compounds as orexin receptor modulators
EP2491031B1 (en) 2009-10-23 2013-08-07 Janssen Pharmaceutica N.V. Fused heterocyclic compounds as orexin receptor modulators
US8877773B2 (en) 2009-10-24 2014-11-04 Indiana University Research And Technology Corporation Methods for treating chronic obstructive pulmonary disease
TWI410630B (zh) 2009-11-10 2013-10-01 Ct Lab Inc 一種用以治療與食慾素受體１、食慾素受體２、體抑素受體２或多巴胺ｄ２ｌ受體相關之疾病的方法和組合物
AU2010336386B2 (en) 2009-12-23 2016-01-21 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors
EP2653469A4 (en) 2010-12-17 2014-05-07 Taisho Pharmaceutical Co Ltd pyrazole
WO2012089607A1 (en) 2010-12-28 2012-07-05 Glaxo Group Limited Novel compounds with a 3a-azabicyclo [4.1.0] heptane core acting on orexin receptors
WO2012089606A1 (en) 2010-12-28 2012-07-05 Glaxo Group Limited Azabicyclo [4.1.0] hept - 4 - yl derivatives as human orexin receptor antagonists
WO2012145581A1 (en) 2011-04-20 2012-10-26 Janssen Pharmaceutica Nv Disubstituted octahy-dropyrrolo [3,4-c] pyrroles as orexin receptor modulators
WO2012153729A1 (ja) 2011-05-10 2012-11-15 大正製薬株式会社 ヘテロ芳香環誘導体
TW201315730A (zh) 2011-07-05 2013-04-16 大正製藥股份有限公司 甲基哌啶衍生物
EP2768305A4 (en) 2011-10-21 2015-04-29 Merck Sharp & Dohme 2,5-DISUBSTITUTED THIOMORPHOLIN OREXINE RECEPTOR ANTAGONISTS
EP2811997B1 (en) 2012-02-07 2018-04-11 Eolas Therapeutics Inc. Substituted prolines/piperidines as orexin receptor antagonists
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
ES2656972T3 (es) 2012-02-23 2018-03-01 Vanderbilt University Análogos de 5-aminotieno [2,3-c] piridazin-6-carboxamida como moduladores alostéricos positivos del receptor de acetilcolina muscarínico M4
JP2014015452A (ja) 2012-06-15 2014-01-30 Taisho Pharmaceutical Co Ltd ピラゾール誘導体を含有する医薬
IN2014DN10490A (es) 2012-06-15 2015-08-21 Taisho Pharmaceutical Co Ltd
MX2014015298A (es) 2012-06-15 2015-03-05 Taisho Pharmaceutical Co Ltd Derivado de anillo heteroaromatico de alquilo de cadena ramificada.
JP2014111586A (ja) 2012-11-09 2014-06-19 Taisho Pharmaceutical Co Ltd ヘテロ芳香環誘導体を含有する医薬
EP2925321A4 (en) 2012-11-27 2016-04-27 Merck Sharp & Dohme 2-pyridylamino-4-nitrile-piperidinyl orexin receptor antagonists
JP2016028017A (ja) 2012-12-13 2016-02-25 大正製薬株式会社 フッ素置換ピペリジン化合物
JP2014141480A (ja) 2012-12-28 2014-08-07 Taisho Pharmaceutical Co Ltd メチルピペリジン誘導体を含有する医薬
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途
WO2015018027A1 (en) 2013-08-08 2015-02-12 Merck Sharp & Dohme Corp. Thiazole orexin receptor antagonists
CA3205777A1 (en) 2013-12-03 2015-06-11 Intra-Cellular Therapies, Inc. Heterocycle fused gamma-carboline compounds for use in treatment of schizophrenia
US9586934B2 (en) 2013-12-09 2017-03-07 Merck Sharp & Dohme Corp. 2-pyridyloxy-4-methyl orexin receptor antagonists
JP5930010B2 (ja) 2013-12-13 2016-06-08 大正製薬株式会社 ヘテロ芳香環メチル環状アミン誘導体を含有する医薬
JP2015131802A (ja) 2013-12-13 2015-07-23 大正製薬株式会社 分岐鎖アルキルヘテロ芳香環誘導体を含有する医薬
US9617246B2 (en) 2013-12-18 2017-04-11 Merck Sharp & Dohme Corp. Thioether-piperidinyl orexin receptor antagonists
TW201613891A (en) 2014-02-12 2016-04-16 Eolas Therapeutics Inc Substituted prolines / piperidines as orexin receptor antagonists
TW201613864A (en) 2014-02-20 2016-04-16 Takeda Pharmaceutical Novel compounds
JP2017100950A (ja) 2014-04-04 2017-06-08 大正製薬株式会社 オキソ複素環誘導体
JP2017100951A (ja) 2014-04-04 2017-06-08 大正製薬株式会社 オキサゾリジノン及びオキサジナノン誘導体
WO2015180060A1 (zh) 2014-05-28 2015-12-03 杭州普晒医药科技有限公司 一种二氮杂环庚烷化合物的盐及其晶型与无定型物
ES2901418T3 (es) 2014-08-13 2022-03-22 Eolas Therapeutics Inc Difluoropirrolidinas como moduladores del receptor de orexina
US20160051533A1 (en) 2014-08-20 2016-02-25 Ladd Research LLC Diagnosis and pharmacological treatment of seasonal affective disorder and symptoms of seasonality
GB201415569D0 (en) 2014-09-03 2014-10-15 C4X Discovery Ltd Therapeutic Compounds
CN106349228B (zh) 2015-07-17 2019-07-09 广东东阳光药业有限公司 取代的喹唑啉酮类化合物及其制备方法和用途
GB201601703D0 (en) 2016-01-29 2016-03-16 C4X Discovery Ltd Therapeutic compounds
CR20180433A (es) * 2016-03-10 2018-11-07 Janssen Pharmaceutica Nv Métodos para tratar la depresión con antagonistas del receptor de orexina-2
GB201820458D0 (en) 2018-12-14 2019-01-30 Heptares Therapeutics Ltd Ox1 antagonists

Also Published As

Publication number Publication date
AR114667A2 (es) 2020-09-30
JP2013508403A (ja) 2013-03-07
RS54945B1 (sr) 2016-11-30
SMT201600216B (it) 2016-08-31
KR20170135989A (ko) 2017-12-08
HRP20191220T1 (hr) 2019-10-18
CA2778484C (en) 2018-07-31
JOP20180019A1 (ar) 2019-01-30
KR20170136645A (ko) 2017-12-11
EA022766B1 (ru) 2016-02-29
CN102781942A (zh) 2012-11-14
PT3093291T (pt) 2019-07-25
NZ599629A (en) 2013-12-20
DK2491038T3 (da) 2016-07-18
US20120208812A1 (en) 2012-08-16
US8653263B2 (en) 2014-02-18
IL219234A (en) 2015-02-26
IL219234A0 (en) 2012-06-28
US9079911B2 (en) 2015-07-14
CY1121848T1 (el) 2020-07-31
SI2491038T1 (sl) 2016-08-31
ES2585806T3 (es) 2016-10-10
PL2491038T3 (pl) 2016-10-31
JP5759470B2 (ja) 2015-08-05
US20140179697A1 (en) 2014-06-26
WO2011050198A1 (en) 2011-04-28
US11059828B2 (en) 2021-07-13
PL3093291T3 (pl) 2019-11-29
US20240109901A1 (en) 2024-04-04
CO6541572A2 (es) 2012-10-16
HUE028650T2 (en) 2016-12-28
RS59004B1 (sr) 2019-08-30
JO3267B1 (ar) 2018-09-16
AU2015242975A1 (en) 2015-11-05
JOP20180019B1 (ar) 2023-09-17
AU2010310595A1 (en) 2012-05-17
EA201270591A1 (ru) 2012-11-30
PE20110404A1 (es) 2011-07-08
UY32966A (es) 2011-04-29
US20150335651A1 (en) 2015-11-26
BR112012010820A2 (pt) 2016-04-05
ME02437B (me) 2016-09-20
BR112012010820B1 (pt) 2021-09-14
NI201200062A (es) 2013-04-19
PT2491038T (pt) 2016-07-14
USRE48841E1 (en) 2021-12-07
AU2015242975B2 (en) 2017-06-01
AU2010310595B2 (en) 2015-07-16
EP3093291B1 (en) 2019-05-08
KR101859409B1 (ko) 2018-05-18
HRP20160781T1 (hr) 2016-09-23
TW201217377A (en) 2012-05-01
CA2778484A1 (en) 2011-04-28
US11667644B2 (en) 2023-06-06
CR20120273A (es) 2012-10-25
HK1175463A1 (zh) 2013-07-05
US20170129901A1 (en) 2017-05-11
KR20120105449A (ko) 2012-09-25
EP2491038B1 (en) 2016-04-06
US20210347781A1 (en) 2021-11-11
EP2491038A1 (en) 2012-08-29
SI3093291T1 (sl) 2019-08-30
ES2735411T3 (es) 2019-12-18
MX2012004753A (es) 2012-09-07
UA107812C2 (en) 2015-02-25
TR201910327T4 (tr) 2019-07-22
HK1231463A1 (zh) 2017-12-22
TWI481613B (zh) 2015-04-21
CN102781942B (zh) 2015-09-23
EP3093291A1 (en) 2016-11-16
CL2010001162A1 (es) 2011-04-08
HUE043962T2 (hu) 2019-09-30
ME03452B (me) 2020-01-20
EP3581575A1 (en) 2019-12-18
US20200048263A1 (en) 2020-02-13
DK3093291T3 (da) 2019-07-29
KR101859400B1 (ko) 2018-05-18
CY1117743T1 (el) 2017-05-17
LT3093291T (lt) 2019-07-10
ECSP12011908A (es) 2012-07-31

Similar Documents

Publication Publication Date Title
AR078731A1 (es) Octahidropirrolo (3,4-c) pirroles disustituidos como moduladores del receptor de orexina
AR078733A1 (es) Compuestos heterociclicos fusionados como moduladores del receptor de orexina
AR078732A1 (es) Compuestos heterociclicos fusionados como moduladores del receptor de la orexina
PE20120774A1 (es) COMPUESTOS DERIVADOS DE PIRAZOLO[3,4-d]PIRIMIDINDIONA COMO MODULADORES DE TRPA1
PE20161400A1 (es) Derivados de isoindolin-1-ona con actividad positiva del modulador alosterico del receptor colinergico muscarinico m1 para el tratamiento de la enfermedad de alzheimer
CN104507481B (zh) 用于治疗、改善或预防病毒疾病的7‑氧代‑4,7‑二氢‑吡唑并[1,5‑a]嘧啶衍生物
PE20160521A1 (es) Inhibidores de autotaxina que comprenden un nucleo ciclico de anillo heteroaromatico-bencil-amida
TWI659025B (zh) 吲哚啉－２－酮或吡咯并－吡啶－２－酮之衍生物
RU2015102057A (ru) НОВЫЕ КОНДЕНСИРОВАННЫЕ ПИРИДИНОВЫЕ ПРОИЗВОДНЫЕ, ПРИМЕНИМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ТИРОЗИНКИНАЗЫ с-MET
PE20230376A1 (es) Compuestos moduladores de la diacilglicerol quinasa
RU2018123779A (ru) Новые соединения
PE20080944A1 (es) Derivados de pirimidina como inhibidores del receptor de cinasa activina(alk-5)
ES2865182T3 (es) Inhibidor de URAT1
TW200536851A (en) Compounds and methods of use
AR062125A1 (es) Compuestos que modulan el receptor cb2 y su utilizacion como medicamentos
PE20180227A1 (es) Benzamidas sustituidas con 1,3-tiazol-2-ilo
PE20081752A1 (es) Sal de napadisilato de 5-(2-{[6-(2,2-difluoro-2-feniletoxi)hexil]amino}-1-hidroxietil)-8-hidroxiquinolin-2-(1h)-ona como agonista del receptor adrenergico b2
RU2012105284A (ru) Спиро-аминосоединения, пригодные для лечения нарушений сна и лекарственного привыкания
PE20121510A1 (es) Isoquinolinonas y quinazolinonas sustituidas
ECSP088867A (es) Derivados de pirimidina como inhibidores de fi3q
PE20090717A1 (es) Derivados de quinolina como inhibidores de la pi3 quinasa
PE20190653A1 (es) Nuevos derivados de pirrol, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen
NZ716420A (en) Fused heterocyclic compounds as sodium channel modulators
AR058984A1 (es) Derivados de ciclohexil piperazinil metanona
PE20130576A1 (es) Compuestos heterociclicos de nitrogeno utiles como inhibidores de pde10

Legal Events

Date Code Title Description
FG Grant, registration