PE20191323A1 - PIRAZOLO[3,4-b]PIRIDINAS E IMIDAZO[1,5-b]PIRIDAZINAS COMO INHIBIDORES DE PDE1 - Google Patents

PIRAZOLO[3,4-b]PIRIDINAS E IMIDAZO[1,5-b]PIRIDAZINAS COMO INHIBIDORES DE PDE1

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Publication number
PE20191323A1
PE20191323A1 PE2019001294A PE2019001294A PE20191323A1 PE 20191323 A1 PE20191323 A1 PE 20191323A1 PE 2019001294 A PE2019001294 A PE 2019001294A PE 2019001294 A PE2019001294 A PE 2019001294A PE 20191323 A1 PE20191323 A1 PE 20191323A1
Authority
PE
Peru
Prior art keywords
pyrazolo
methyl
branched
alkyl
linear
Prior art date
Application number
PE2019001294A
Other languages
English (en)
Inventor
Jan Kehler
Lars Kyhn Rasmussen
Morten Langgård
Mikkel Jessing
Paulo Jorge Vieira Vital
Karsten Juhl
Mauro Marigo
Original Assignee
H Lundbeck As
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 H Lundbeck As filed Critical H Lundbeck As
Publication of PE20191323A1 publication Critical patent/PE20191323A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • 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
    • A61P25/14—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
    • A61P25/28—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

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

Abstract

Referido a un compuesto de formula I y sales aceptables del mismo, donde: Y1 = N-R1, Y2 = C e Y3 = C, o Y1 = C-R1, Y2 = N e Y3 = C; Z1 se selecciona de NH, CH2 , O y S; Z2 se selecciona entre NH, CH2 , O y S; R1 es hidrogeno, alquilo C1-4 lineal o ramificado y cicloalquilo C3-4 monociclico saturado, opcionalmente sustituido con uno o mas halogenos; R2 es alquilo C1-6 lineal o ramificado, cicloalquilo C3-6 monociclico saturado, oxetanilo, tetrahidrofuranilo y tetrahidropiranilo, todos opcionalmente sustituidos con uno o mas halogenos; R3 es un heteroarilo de 5 o 6 miembros, que puede estar opcionalmente sustituido con uno o mas sustituyentes seleccionados de alquilo C1-4 lineal o ramificado, entre otros; y R4 es un heteroarilo de 5 o 6 miembros. Son compuestos preferidos: 6-(2-etoxi-3-piridil)-3-isopropil-1-metil-N-[(1-metilimidazol-4-il) metil]pirazolo[3,4-b]piridin-4-amina; 6-(2-etoxi-3-piridil)-3-isopropil-1-metil-N-[(2-metiloxazol-4-il)metil]pirazolo[3,4-b]piridin-4-amina; entre otros. Dichos compuestos son inhibidores de la enzima fosfodiesterasa tipo 1 (PDE1), utiles en el tratamiento de trastornos neurodegenerativos y psiquiatricos. Tambien se refiere a una composicion farmaceutica que comprende dichos compuestos.
PE2019001294A 2016-12-22 2017-12-20 PIRAZOLO[3,4-b]PIRIDINAS E IMIDAZO[1,5-b]PIRIDAZINAS COMO INHIBIDORES DE PDE1 PE20191323A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA201600784 2016-12-22
DKPA201700404 2017-07-06

Publications (1)

Publication Number Publication Date
PE20191323A1 true PE20191323A1 (es) 2019-09-24

Family

ID=60812077

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2019001294A PE20191323A1 (es) 2016-12-22 2017-12-20 PIRAZOLO[3,4-b]PIRIDINAS E IMIDAZO[1,5-b]PIRIDAZINAS COMO INHIBIDORES DE PDE1

Country Status (23)

Country Link
US (2) US10351561B2 (es)
EP (1) EP3558988B1 (es)
JP (1) JP7074758B2 (es)
KR (1) KR20190095301A (es)
CN (1) CN110099901B (es)
AU (1) AU2017384481A1 (es)
BR (1) BR112018017067A2 (es)
CA (1) CA3046588A1 (es)
CL (1) CL2019001669A1 (es)
CO (1) CO2019005538A2 (es)
CR (1) CR20190302A (es)
DO (1) DOP2019000169A (es)
EC (1) ECSP19043790A (es)
ES (1) ES2882335T3 (es)
IL (1) IL267561A (es)
JO (1) JOP20190126A1 (es)
MX (1) MX2019007509A (es)
PE (1) PE20191323A1 (es)
PH (1) PH12019501324A1 (es)
RU (1) RU2019116251A (es)
TW (1) TW201829405A (es)
WO (1) WO2018115067A1 (es)
ZA (1) ZA201904236B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
JOP20190126A1 (ar) 2016-12-22 2019-05-28 H Lundbeck As بيرازولو [3، 4-b] بيريدينات وإيميدازو [1، 5-b] بيريدازينات على هيئة مثبطات PDE1
WO2019115566A1 (en) 2017-12-14 2019-06-20 H. Lundbeck A/S Combination treatments comprising administration of 1h-pyrazolo[4,3-b]pyridines
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
TW201927784A (zh) 2017-12-20 2019-07-16 丹麥商Ｈ 朗德貝克公司 作為pde1抑制劑之大環
US11535611B2 (en) 2017-12-20 2022-12-27 H. Lundbeck A/S Pyrazolo[3,4-B]pyridines and imidazo[1,5-B]pyridazines as PDE1 inhibitors
US10766893B2 (en) 2017-12-20 2020-09-08 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors

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US10766893B2 (en) 2017-12-20 2020-09-08 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors

Also Published As

Publication number Publication date
US10351561B2 (en) 2019-07-16
CN110099901A (zh) 2019-08-06
CO2019005538A2 (es) 2019-06-11
EP3558988A1 (en) 2019-10-30
ZA201904236B (en) 2020-12-23
JP7074758B2 (ja) 2022-05-24
RU2019116251A3 (es) 2021-03-31
MX2019007509A (es) 2019-09-04
CA3046588A1 (en) 2018-06-28
CL2019001669A1 (es) 2019-09-06
IL267561A (en) 2019-08-29
BR112018017067A2 (pt) 2019-07-02
CN110099901B (zh) 2023-01-03
ES2882335T3 (es) 2021-12-01
JP2020502230A (ja) 2020-01-23
ECSP19043790A (es) 2019-06-30
EP3558988B1 (en) 2021-07-07
AU2017384481A1 (en) 2019-06-13
TW201829405A (zh) 2018-08-16
WO2018115067A1 (en) 2018-06-28
RU2019116251A (ru) 2021-01-22
CR20190302A (es) 2019-08-21
US20180179200A1 (en) 2018-06-28
KR20190095301A (ko) 2019-08-14
JOP20190126A1 (ar) 2019-05-28
DOP2019000169A (es) 2019-07-31
US20190352302A1 (en) 2019-11-21
US10689379B2 (en) 2020-06-23
PH12019501324A1 (en) 2019-09-16

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