AR120339A2 - CRISTALES DE SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA - Google Patents

CRISTALES DE SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA

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Publication number
AR120339A2
AR120339A2 ARP200102993A ARP200102993A AR120339A2 AR 120339 A2 AR120339 A2 AR 120339A2 AR P200102993 A ARP200102993 A AR P200102993A AR P200102993 A ARP200102993 A AR P200102993A AR 120339 A2 AR120339 A2 AR 120339A2
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AR
Argentina
Prior art keywords
methyl
cyclopent
fluoropyridin
pyrazolo
imidazo
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Application number
ARP200102993A
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English (en)
Inventor
Peng Li
Lawrence P Wennogle
Robert Davis
Original Assignee
Intra Cellular Therapies Inc
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Publication date
Application filed by Intra Cellular Therapies Inc filed Critical Intra Cellular Therapies Inc
Publication of AR120339A2 publication Critical patent/AR120339A2/es

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    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-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
    • A61K31/505Pyrimidines; 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C55/02Dicarboxylic acids
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/15Fumaric acid
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
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  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
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  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Sales de adición y cristales de sales de un compuesto terapéutico con actividad inhibitoria de PDE I. Reivindicación 1: El compuesto (6aR,9aS)-5,6a,7,8,9,9a-hexahidro-5-metil-3-(fenilamino)-2-((4-(6-fluoropiridin-2-il)fenil)metil)-ciclopent[4,5]imidazo[1,2-a]pirazolo[4,3-e]pirimidin-4(2H)-ona en una forma de sal por adición de ácidos ácida seleccionado de sal de fumarato, clorhidrato, (1-hidrox-2)-naftoato, benzosulfonato, fosfato, mesilato, tartrato, sulfato y bromhidrato. Reivindicación 7: Los cristales de sal de acuerdo con la reivindicación 4, 5 ó 6, caracterizados porque los cristales de sal exhiben un patrón de difracción de polvos por rayos X que comprende al menos cinco valores de ángulo 2-q seleccionados de los establecidos en la siguiente tabla: @@@@@@@@@
ARP200102993A 2012-06-21 2020-10-29 CRISTALES DE SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA AR120339A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261662355P 2012-06-21 2012-06-21

Publications (1)

Publication Number Publication Date
AR120339A2 true AR120339A2 (es) 2022-02-09

Family

ID=49769726

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP130102175 AR091507A1 (es) 2012-06-21 2013-06-19 SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA
ARP200102993A AR120339A2 (es) 2012-06-21 2020-10-29 CRISTALES DE SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP130102175 AR091507A1 (es) 2012-06-21 2013-06-19 SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA

Country Status (19)

Country Link
US (1) US9469647B2 (es)
EP (2) EP3733675A1 (es)
JP (3) JP6506687B2 (es)
KR (1) KR102175024B1 (es)
CN (2) CN104602695B (es)
AR (2) AR091507A1 (es)
AU (1) AU2013278081B2 (es)
BR (2) BR112014032338B1 (es)
CA (1) CA2876001C (es)
DK (1) DK2863918T3 (es)
ES (1) ES2769523T3 (es)
HK (1) HK1210017A1 (es)
IL (2) IL236069B (es)
MX (1) MX352831B (es)
PL (1) PL2863918T3 (es)
RU (1) RU2652116C2 (es)
TW (1) TWI652271B (es)
UY (1) UY34870A (es)
WO (1) WO2013192556A2 (es)

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AR091507A1 (es) * 2012-06-21 2015-02-11 Intra Cellular Therapies Inc SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA
EP3702358A1 (en) 2013-06-21 2020-09-02 Intra-Cellular Therapies, Inc. Process for preparing salts of a known pde1 inhibitor

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JP6853794B2 (ja) 2021-03-31
EP2863918A2 (en) 2015-04-29
IL236069A0 (en) 2015-01-29
TWI652271B (zh) 2019-03-01
HK1210017A1 (en) 2016-04-15
JP2018065868A (ja) 2018-04-26
EP3733675A1 (en) 2020-11-04
MX2014015904A (es) 2015-07-17
BR122021026665B1 (pt) 2022-12-06
JP2015520243A (ja) 2015-07-16
RU2652116C2 (ru) 2018-04-25
CA2876001C (en) 2021-06-08
KR102175024B1 (ko) 2020-11-05
CN104602695A (zh) 2015-05-06
AU2013278081B2 (en) 2017-06-29
CA2876001A1 (en) 2013-12-27
PL2863918T3 (pl) 2020-05-18
AU2013278081A1 (en) 2015-01-22
EP2863918B1 (en) 2019-12-25
AR091507A1 (es) 2015-02-11
JP2020012003A (ja) 2020-01-23
EP2863918A4 (en) 2016-01-13
WO2013192556A2 (en) 2013-12-27
TW201406763A (zh) 2014-02-16
US9469647B2 (en) 2016-10-18
BR112014032338A2 (pt) 2018-05-15
RU2015101647A (ru) 2016-08-10
CN107602572A (zh) 2018-01-19
WO2013192556A3 (en) 2014-02-27
KR20150023386A (ko) 2015-03-05
UY34870A (es) 2014-01-31
IL236069B (en) 2020-04-30
US20150259353A1 (en) 2015-09-17
MX352831B (es) 2017-12-11
DK2863918T3 (da) 2020-03-23
BR112014032338B1 (pt) 2022-04-26
JP6506687B2 (ja) 2019-04-24
CN104602695B (zh) 2017-08-29
IL273276A (en) 2020-04-30
ES2769523T3 (es) 2020-06-26

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