AR074317A1 - Espiro-5,6 dihidro -4h-2,3,5,10b-tetraaza-benzo(e)azulenos - Google Patents
Espiro-5,6 dihidro -4h-2,3,5,10b-tetraaza-benzo(e)azulenosInfo
- Publication number
- AR074317A1 AR074317A1 ARP090104354A ARP090104354A AR074317A1 AR 074317 A1 AR074317 A1 AR 074317A1 AR P090104354 A ARP090104354 A AR P090104354A AR P090104354 A ARP090104354 A AR P090104354A AR 074317 A1 AR074317 A1 AR 074317A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- halogen
- cyano
- unsubstituted
- Prior art date
Links
Classifications
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- 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
Abstract
Los compuestos actúan como moduladores del receptor de la V1a y son útiles como agentes terapéuticos que actúan tanto a nivel central como periférico en estados patológicos tales como la dismenorrea, disfunción sexual masculina o femenina, hipertensión, fallo cardíaco crónico, secreción inapropiada de vasopresina, cirrosis hepática, síndrome nefrótico, ansiedad, trastornos depresivos, trastornos obsesivo-compulsivo, trastornos del espectro autista, esquizofrenia y comportamiento agresivo. Reivindicación 1: El compuesto de la fórmula general (1) en la que X-Y es C(RaRb)-O, en el que Ra y Rb en cada caso con independencia entre sí son H o alquilo C1-4, C(RcRd)-S(O)p, en el que Rc y Rd en cada caso con independencia entre sí son H o alquilo C1-4; C(O)O, CH2OCH2, CH2CH2O, Z es CH o N; R1 es halógeno, ciano, alcoxi C1-4 o alquilo C1-4; R2 es H, alquilo C1-12, sin sustituir o sustituido por uno o más OH, halógeno, ciano o alcoxi C1-12, -(CH2)q-Re, en el que Re es fenilo o heteroarilo de 5 o 6 eslabones, cada uno de ellos está sin sustituir o sustituido por uno o más sustituyentes elegidos con independencia entre A, -(CH2)rNRiRii, -C(O)-alquilo C1-12, en el que alquilo C1-12 está sin sustituir o sustituido por uno o más OH, halógeno, ciano o alcoxi C1-12; -C(O)(CH2)qOC(O)-alquilo C1-12, -C(O)(CH2)qNRiRii, -C(O)O-alquilo C1-12 en el que alquilo está sin sustituir o sustituido por uno o más OH, halógeno, ciano o alcoxi C1-12, -S(O)2-alquilo C1-12, o -S(O)2NRiRii; Ri y Rii en cada caso con independencia entre sí son H, alquilo C1-12, o junto con el N, al que están unidos, forman un heterocicloalquilo de 3 a 7 eslabones que contiene uno o dos heteroátomos elegidos entre N, O y S, dicho heterocicloalquilo está sin sustituir o sustituido por uno o más sustituyentes elegidos con independencia entre B, A es halógeno, ciano, OH, alquilo C1-7, halo-alquilo C1-7 o alcoxi C1-7; B es oxo, halógeno, OH, alquilo C1-7 o alcoxi C1-7, R3 es Cl o F; n es el número 1 o 2; m es el número 0, 1, 2, 3 o 4; p es el número 0, 1 o 2, q es el número 1, 2, 3 o 4, r es el número 2, 3 o 4, o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP08169028 | 2008-11-13 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR074317A1 true AR074317A1 (es) | 2011-01-05 |
Family
ID=41353837
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090104354A AR074317A1 (es) | 2008-11-13 | 2009-11-11 | Espiro-5,6 dihidro -4h-2,3,5,10b-tetraaza-benzo(e)azulenos |
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) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101600278B1 (ko) | 2008-06-12 | 2016-03-08 | 얀센 파마슈티카 엔.브이. | 히스타민 h4 수용체의 다이아미노-피리딘, 피리미딘, 및 피리다진 조절제 |
EP2370441B1 (en) | 2008-11-28 | 2013-09-11 | F. Hoffmann-La Roche AG | Arylcyclohexylethers of dihydrotetraazabenzoazulenes for use as vasopressin v1a receptor antagonists |
MX370663B (es) * | 2013-12-19 | 2019-12-19 | Hoffmann La Roche | Espiro-oxazolonas. |
CA2936865A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Diaminopyrimidine benzenesulfone derivatives and uses thereof |
US10793571B2 (en) | 2014-01-31 | 2020-10-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
CN107001382B (zh) | 2014-11-14 | 2019-10-25 | 豪夫迈·罗氏有限公司 | 螺-噻唑酮 |
CN108472300A (zh) | 2015-09-11 | 2018-08-31 | 达纳-法伯癌症研究所股份有限公司 | 氰基噻吩并三唑并二氮杂环庚三烯及其用途 |
SG10201913450PA (en) | 2015-11-25 | 2020-03-30 | Dana Farber Cancer Inst 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 |
US20230084719A1 (en) * | 2018-12-12 | 2023-03-16 | 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 |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5521173A (en) | 1995-01-17 | 1996-05-28 | American Home Products Corporation | Tricyclic benzazepine vasopressin antagonists |
WO1999006409A1 (en) | 1997-07-30 | 1999-02-11 | American Home Products Corporation | Tricyclic vasopressin agonists |
HU229074B1 (en) * | 1999-01-19 | 2013-07-29 | Ortho Mcneil Pharm Inc | Tricyclic benzodiazepines as vasopressin receptor antagonists |
US7022699B2 (en) | 2001-04-12 | 2006-04-04 | Wyeth | Cyclohexenyl phenyl diazepines vasopressin and oxytocin receptor modulators |
GB0303852D0 (en) | 2003-02-19 | 2003-03-26 | Pfizer Ltd | Triazole compounds useful in therapy |
DE10360792A1 (de) | 2003-12-23 | 2005-07-28 | Grünenthal GmbH | Spirocyclische Cyclohexan-Derivate |
GB0400700D0 (en) | 2004-01-13 | 2004-02-18 | Pfizer Ltd | Compounds useful in therapy |
AP2006003768A0 (en) * | 2004-05-25 | 2006-10-31 | Pfizer Prod Inc | TetraazabenzoÄeÜazulene derivatives and analogs tehereof |
KR100840852B1 (ko) | 2004-05-25 | 2008-06-23 | 화이자 프로덕츠 인크. | 테트라아자벤조[e]아줄렌 유도체 및 이의 유사체 |
EP1632494A1 (en) | 2004-08-24 | 2006-03-08 | Ferring B.V. | Vasopressin v1a antagonists |
MX2007002248A (es) * | 2004-08-25 | 2008-10-02 | Pfizer | Triazolobenzodiazepinas y su uso como antagonistas de vasopresina. |
US20080188478A1 (en) | 2005-04-26 | 2008-08-07 | Pfizer Inc. | Compounds Useful In Therapy |
CA2608718A1 (en) | 2005-05-18 | 2006-11-23 | Pfizer Limited | 1, 2, 4-triazole derivatives as vasopressin antagonists |
KR101129791B1 (ko) | 2007-01-12 | 2012-03-23 | 에프. 호프만-라 로슈 아게 | 스파이로피페리딘 글리신아마이드 유도체 |
SG171742A1 (en) | 2008-11-18 | 2011-07-28 | Hoffmann La Roche | Alkylcyclohexylethers of dihydrotetraazabenzoazulenes |
US8420633B2 (en) * | 2010-03-31 | 2013-04-16 | Hoffmann-La Roche Inc. | Aryl-cyclohexyl-tetraazabenzo[e]azulenes |
US8461151B2 (en) * | 2010-04-13 | 2013-06-11 | Hoffmann-La Roche Inc. | Aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes |
US8492376B2 (en) * | 2010-04-21 | 2013-07-23 | Hoffmann-La Roche Inc. | Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes |
US8481528B2 (en) * | 2010-04-26 | 2013-07-09 | Hoffmann-La Roche Inc. | Heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes |
US8513238B2 (en) | 2010-05-10 | 2013-08-20 | Hoffmann-La Roche Inc. | Heteroaryl-cyclohexyl-tetraazabenzo[E]azulenes |
-
2009
- 2009-11-04 SI SI200930413T patent/SI2356123T1/sl unknown
- 2009-11-04 RU RU2011121049/04A patent/RU2514429C2/ru not_active IP Right Cessation
- 2009-11-04 BR BRPI0921110A patent/BRPI0921110A2/pt not_active IP Right Cessation
- 2009-11-04 PT PT09745058T patent/PT2356123E/pt unknown
- 2009-11-04 PE PE2011000965A patent/PE20110537A1/es not_active Application Discontinuation
- 2009-11-04 DK DK09745058.9T patent/DK2356123T3/da active
- 2009-11-04 PL PL09745058T patent/PL2356123T3/pl unknown
- 2009-11-04 JP JP2011535965A patent/JP5567027B2/ja not_active Expired - Fee Related
- 2009-11-04 CN CN2009801452677A patent/CN102216305B/zh not_active Expired - Fee Related
- 2009-11-04 WO PCT/EP2009/064565 patent/WO2010054961A1/en active Application Filing
- 2009-11-04 CA CA2741018A patent/CA2741018A1/en not_active Abandoned
- 2009-11-04 MX MX2011004575A patent/MX2011004575A/es active IP Right Grant
- 2009-11-04 KR KR1020117010757A patent/KR101348499B1/ko not_active IP Right Cessation
- 2009-11-04 ES ES09745058T patent/ES2391932T3/es active Active
- 2009-11-04 AU AU2009315754A patent/AU2009315754B2/en not_active Ceased
- 2009-11-04 EP EP09745058A patent/EP2356123B1/en not_active Not-in-force
- 2009-11-06 US US12/613,554 patent/US8664216B2/en not_active Expired - Fee Related
- 2009-11-10 TW TW098138124A patent/TWI401257B/zh not_active IP Right Cessation
- 2009-11-11 AR ARP090104354A patent/AR074317A1/es unknown
-
2011
- 2011-03-24 IL IL211939A patent/IL211939A/en not_active IP Right Cessation
- 2011-04-05 ZA ZA2011/02522A patent/ZA201102522B/en unknown
- 2011-05-12 CL CL2011001078A patent/CL2011001078A1/es unknown
-
2012
- 2012-11-12 CY CY20121101074T patent/CY1113523T1/el unknown
- 2012-12-21 HR HRP20121060AT patent/HRP20121060T1/hr unknown
Also Published As
Publication number | Publication date |
---|---|
MX2011004575A (es) | 2011-06-01 |
JP2012508711A (ja) | 2012-04-12 |
EP2356123B1 (en) | 2012-10-03 |
CN102216305A (zh) | 2011-10-12 |
US8664216B2 (en) | 2014-03-04 |
IL211939A0 (en) | 2011-06-30 |
ES2391932T3 (es) | 2012-12-03 |
CN102216305B (zh) | 2013-12-18 |
RU2514429C2 (ru) | 2014-04-27 |
AU2009315754B2 (en) | 2013-08-15 |
PT2356123E (pt) | 2012-10-31 |
AU2009315754A1 (en) | 2010-05-20 |
IL211939A (en) | 2013-06-27 |
DK2356123T3 (da) | 2012-10-15 |
CA2741018A1 (en) | 2010-05-20 |
WO2010054961A1 (en) | 2010-05-20 |
KR101348499B1 (ko) | 2014-01-06 |
BRPI0921110A2 (pt) | 2016-02-16 |
PL2356123T3 (pl) | 2013-03-29 |
AU2009315754A8 (en) | 2011-05-12 |
TW201022271A (en) | 2010-06-16 |
EP2356123A1 (en) | 2011-08-17 |
HRP20121060T1 (hr) | 2013-01-31 |
CY1113523T1 (el) | 2016-06-22 |
RU2011121049A (ru) | 2012-12-20 |
US20100120751A1 (en) | 2010-05-13 |
SI2356123T1 (sl) | 2013-01-31 |
PE20110537A1 (es) | 2011-08-04 |
TWI401257B (zh) | 2013-07-11 |
CL2011001078A1 (es) | 2011-11-11 |
KR20110074580A (ko) | 2011-06-30 |
ZA201102522B (en) | 2012-10-31 |
JP5567027B2 (ja) | 2014-08-06 |
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