PE20110537A1 - ESPIRO-5,6-DIHIDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENOS COMO ANTAGONISTAS DE LA V1a - Google Patents

ESPIRO-5,6-DIHIDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENOS COMO ANTAGONISTAS DE LA V1a

Info

Publication number
PE20110537A1
PE20110537A1 PE2011000965A PE2011000965A PE20110537A1 PE 20110537 A1 PE20110537 A1 PE 20110537A1 PE 2011000965 A PE2011000965 A PE 2011000965A PE 2011000965 A PE2011000965 A PE 2011000965A PE 20110537 A1 PE20110537 A1 PE 20110537A1
Authority
PE
Peru
Prior art keywords
spyro
cyclohexan
benzodiazepine
triazolo
benzofuran
Prior art date
Application number
PE2011000965A
Other languages
English (en)
Inventor
Caterina Bissantz
Erwin Goetschi
Roland Jakob-Roetne
Raffaello Masciadri
Emmanuel Pinard
Hasane Ratni
Mark Rogers-Evans
Patrick Schnider
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20110537A1 publication Critical patent/PE20110537A1/es

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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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P25/18—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
    • A61P25/22—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

REFERIDA A UN COMPUESTO DERIVADO DE ESPIRODIHIDROTETRAAZABENZOAZULENO DE FORMULA (I), DONDE X-Y ES C(O)O, CH2OCH2, CH2CH2O, ENTRE OTROS; Z ES CH O N; R1 ES HALOGENO, CIANO, ALCOXI C1-C4 O ALQUILO C1-C4; R2 ES H, ALQUILO C1-C12, -S(O)2-ALQUILO C1-C12, ENTRE OTROS; R3 ES Cl O F; n ES 1 O 2; m ES UN NUMERO ENTERO DE 0 A 4. SON COMPUESTOS PREFERIDOS: 8-CLORO-1-[(1r,4'r)-3H-ESPIRO[2-BENZOFURANO-1,1'-CICLOHEXAN]-4'-IL]-4H-[1,2,4]TRIAZOLO[4,3-a][1,4]BENZODIAZEPINA-5(6H)-CARBOXILATO DE TERT-BUTILO, CLORHIDRATO DE 8-CLORO-1-[(1r,4'r)-3H-ESPIRO[2-BENZOFURANO-1,1'-CICLOHEXAN]-4'-IL]-5,6-DIHIDRO-4H-[1,2,4]TRIAZOLO[4,3-a][1,4]BENZODIAZEPINA, 8-CLORO-5-METIL-1-[(1r,4'r)-3H-ESPIRO[2-BENZOFURANO-1,1'-CICLOHEXAN]-4'-IL]-5,6-DIHIDRO-4H-[1,2,4]TRIAZOLO[4,3-a][1,4]BENZODIAZEPINA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION Y UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE LA V1a Y SON UTILES EN EL TRATAMIENTO DE LA DISMENORREA, HIPERTENSION, FALLOCARDIACO CRONICO, SINDROME NEFROTICO, ANSIEDAD, ENTRE OTROS
PE2011000965A 2008-11-13 2009-11-04 ESPIRO-5,6-DIHIDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENOS COMO ANTAGONISTAS DE LA V1a PE20110537A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08169028 2008-11-13

Publications (1)

Publication Number Publication Date
PE20110537A1 true PE20110537A1 (es) 2011-08-04

Family

ID=41353837

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011000965A PE20110537A1 (es) 2008-11-13 2009-11-04 ESPIRO-5,6-DIHIDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENOS COMO ANTAGONISTAS DE LA V1a

Country Status (24)

Country Link
US (1) US8664216B2 (es)
EP (1) EP2356123B1 (es)
JP (1) JP5567027B2 (es)
KR (1) KR101348499B1 (es)
CN (1) CN102216305B (es)
AR (1) AR074317A1 (es)
AU (1) AU2009315754B2 (es)
BR (1) BRPI0921110A2 (es)
CA (1) CA2741018A1 (es)
CL (1) CL2011001078A1 (es)
CY (1) CY1113523T1 (es)
DK (1) DK2356123T3 (es)
ES (1) ES2391932T3 (es)
HR (1) HRP20121060T1 (es)
IL (1) IL211939A (es)
MX (1) MX2011004575A (es)
PE (1) PE20110537A1 (es)
PL (1) PL2356123T3 (es)
PT (1) PT2356123E (es)
RU (1) RU2514429C2 (es)
SI (1) SI2356123T1 (es)
TW (1) TWI401257B (es)
WO (1) WO2010054961A1 (es)
ZA (1) ZA201102522B (es)

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CN102118969B (zh) 2008-06-12 2017-03-08 詹森药业有限公司 组胺h4受体的二氨基吡啶、二氨基嘧啶和二氨基哒嗪调节剂
ES2431279T3 (es) 2008-11-28 2013-11-25 F. Hoffmann-La Roche Ag Arilciclohexiléteres de dihidro-tetraazabenzoazulenos para uso como antagonistas del receptor V1A de la vasopresina
EA029167B1 (ru) * 2013-12-19 2018-02-28 Ф. Хоффманн-Ля Рош Аг Спиро-оксазолоны
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
MX2016009974A (es) 2014-01-31 2016-10-31 Dana Farber Cancer Inst Inc Derivados de diaminopirimidina bencensulfona y sus usos.
MX2017006294A (es) * 2014-11-14 2017-08-21 Hoffmann La Roche Espiro-tiazolonas.
US11306105B2 (en) * 2015-09-11 2022-04-19 Dana-Farber Cancer Institute, Inc. Cyano thienotriazolodiazepines and uses thereof
US10913752B2 (en) 2015-11-25 2021-02-09 Dana-Farber Cancer Institute, Inc. Bivalent bromodomain inhibitors and uses thereof
WO2017191117A1 (en) 2016-05-03 2017-11-09 Bayer Pharma Aktiengesellschaft V1a receptor antagonists for use in the treatment of renal diseases
EP3634963B8 (en) 2017-06-05 2023-03-29 Blackthorn Therapeutics, Inc. 1-(2-azaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives as v1a receptor antagonists for treating neuropsychological disorders
WO2020123872A1 (en) * 2018-12-12 2020-06-18 Blackthorn Therapeutics, Inc. 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives and related compounds as vasopressin antagonists for the treatment of neuro-psychological disorders
CN111533745A (zh) * 2020-05-20 2020-08-14 成都药明康德新药开发有限公司 叔丁基-3-(氨基甲基)二氢-5h-三唑并二氮杂卓-8(9h)-甲酸基酯制法

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Also Published As

Publication number Publication date
US8664216B2 (en) 2014-03-04
IL211939A (en) 2013-06-27
EP2356123B1 (en) 2012-10-03
RU2514429C2 (ru) 2014-04-27
SI2356123T1 (sl) 2013-01-31
JP5567027B2 (ja) 2014-08-06
EP2356123A1 (en) 2011-08-17
AU2009315754A8 (en) 2011-05-12
RU2011121049A (ru) 2012-12-20
CY1113523T1 (el) 2016-06-22
DK2356123T3 (da) 2012-10-15
AU2009315754B2 (en) 2013-08-15
CL2011001078A1 (es) 2011-11-11
MX2011004575A (es) 2011-06-01
HRP20121060T1 (hr) 2013-01-31
KR20110074580A (ko) 2011-06-30
AU2009315754A1 (en) 2010-05-20
KR101348499B1 (ko) 2014-01-06
PT2356123E (pt) 2012-10-31
ZA201102522B (en) 2012-10-31
ES2391932T3 (es) 2012-12-03
BRPI0921110A2 (pt) 2016-02-16
WO2010054961A1 (en) 2010-05-20
US20100120751A1 (en) 2010-05-13
PL2356123T3 (pl) 2013-03-29
CA2741018A1 (en) 2010-05-20
JP2012508711A (ja) 2012-04-12
IL211939A0 (en) 2011-06-30
TW201022271A (en) 2010-06-16
CN102216305B (zh) 2013-12-18
CN102216305A (zh) 2011-10-12
TWI401257B (zh) 2013-07-11
AR074317A1 (es) 2011-01-05

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