AR045791A1 - TRIAZOL DERIVATIVES REPLACED AS AN OXITOCINE ANTAGONISTS - Google Patents

TRIAZOL DERIVATIVES REPLACED AS AN OXITOCINE ANTAGONISTS

Info

Publication number
AR045791A1
AR045791A1 ARP040103392A ARP040103392A AR045791A1 AR 045791 A1 AR045791 A1 AR 045791A1 AR P040103392 A ARP040103392 A AR P040103392A AR P040103392 A ARP040103392 A AR P040103392A AR 045791 A1 AR045791 A1 AR 045791A1
Authority
AR
Argentina
Prior art keywords
alkyl
nr7r8
alkoxy
nr7c
triazole
Prior art date
Application number
ARP040103392A
Other languages
Spanish (es)
Original Assignee
Pfizer
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
Priority claimed from GB0322159A external-priority patent/GB0322159D0/en
Priority claimed from GB0403150A external-priority patent/GB0403150D0/en
Priority claimed from GB0415110A external-priority patent/GB0415110D0/en
Application filed by Pfizer filed Critical Pfizer
Publication of AR045791A1 publication Critical patent/AR045791A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/06—Antiabortive agents; Labour repressants
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un compuesto de fórmula (1) en la que V, W, X e Y, que pueden ser iguales o diferentes, representan C-R6 o N; Z es C-H o N; R1 se selecciona entre: (i) un anillo fenilo sustituido con 2 o más sustituyentes, que pueden ser iguales o diferentes, cada uno seleccionado independientemente entre halo, alquilo C1-6, alcoxi C1-6, ciano, C(O)NR7R8, NR7R8, NR7C(O)R10 y N[C(O)R10]2; y (ii) un anillo heterocíclico aromático de 5 a 7 miembros que contiene 1-3 heteroátomos seleccionados entre N, O y S y los N-óxidos del mismo; estando dicho anillo opcionalmente sustituido con 2 o más sustituyentes, que pueden ser iguales o diferentes, seleccionados entre halo, alquilo C1-6. alcoxi C1-6, ciano, C(O)NR7R8, NR7R8, NR7C(O)R10 y N[C(O)R10]2; R2 se selecciona entre: (i) H, OH, OR9, NR7R8, NR7C(O)R10 y N[C(O)R10]2; (ii) un heterociclo de 5-7 miembros unido a N, que contiene 1-3 heteroátomos seleccionados entre N, O y S; estando dicho anillo opcionalmente sustituido con 1 o más grupos seleccionados entre alquilo C1-6, alcoxi C1-6 y C(O)NR7R8; y (iii) alquilo C1-6 opcionalmente sustituido con un heterociclo de 5-7 miembros unido a N, que contiene 1-3 heteroátomos seleccionados entre N, O y S; R3 se selecciona entre H y alquilo c1- 6; R4 se selecciona entre H, alquilo C1-6 y OR9; R5 se selecciona entre halo, alquilo C1-6, alcoxi C1-6, NR7R8, NR7C(O)R10 y N[C(O)R10]2; R6 se selecciona entre H, halo, alquilo C1-6, alcoxi C1-6, ciano, NR7R8, NR7C(O)R10, N[C(O)R10]2 y C(O)NR7R8; R7 y R8, que pueden ser iguales o diferentes, se seleccionan entre H y alquilo C1-6; R9 es alquilo C1-6, que está opcionalmente sustituido con 1 o más grupos, cada uno seleccionado independientemente entre alcoxi C1-6 y un heterociclo de 5-7 miembros unido a N, que contiene 1-3 heteroátomos seleccionados entre N, O y S; y R10 se selecciona entre alquilo C1-6 y alcoxi C1-6; un tautómero de los mismos o una sal farmacéuticamente aceptable, solvato o polimorfo de dicho compuesto o tautómero; con la condición de que el compuesto de fórmula (1)no sea: 3-etil-5-(4-imidazol-1-ilfenil)-4-(4-metoxifenil)-4H-[1,2,4]triazol, 3-(3´,5´-diclorobifenil-4-il)-4-(2-metoxifenil)-5-metil-4H-[1,2,4]triazol, 3-(3´,5´-bis-trifluorometilbifenil- 4-il)-4-(2-fluorofenil)-5-metil-4H-[1,2,4]triazol o 3-(3´,5´-bis-trifluorometilbifenil-4-il)-5-metil-4-(3-trifluorometilbifenil)-4H-[1,2,4]triazol.A compound of formula (1) in which V, W, X and Y, which may be the same or different, represent C-R6 or N; Z is C-H or N; R1 is selected from: (i) a phenyl ring substituted with 2 or more substituents, which may be the same or different, each independently selected from halo, C1-6 alkyl, C1-6 alkoxy, cyano, C (O) NR7R8, NR7R8, NR7C (O) R10 and N [C (O) R10] 2; and (ii) a 5- to 7-membered aromatic heterocyclic ring containing 1-3 heteroatoms selected from N, O and S and the N-oxides thereof; said ring being optionally substituted with 2 or more substituents, which may be the same or different, selected from halo, C1-6 alkyl. C1-6 alkoxy, cyano, C (O) NR7R8, NR7R8, NR7C (O) R10 and N [C (O) R10] 2; R2 is selected from: (i) H, OH, OR9, NR7R8, NR7C (O) R10 and N [C (O) R10] 2; (ii) a 5-7 membered heterocycle attached to N, containing 1-3 heteroatoms selected from N, O and S; said ring being optionally substituted with 1 or more groups selected from C1-6 alkyl, C1-6 alkoxy and C (O) NR7R8; and (iii) C1-6 alkyl optionally substituted with a 5-7 membered heterocycle attached to N, containing 1-3 heteroatoms selected from N, O and S; R3 is selected from H and C1-6 alkyl; R4 is selected from H, C1-6 alkyl and OR9; R5 is selected from halo, C1-6 alkyl, C1-6 alkoxy, NR7R8, NR7C (O) R10 and N [C (O) R10] 2; R6 is selected from H, halo, C1-6 alkyl, C1-6 alkoxy, cyano, NR7R8, NR7C (O) R10, N [C (O) R10] 2 and C (O) NR7R8; R7 and R8, which may be the same or different, are selected from H and C1-6 alkyl; R9 is C1-6 alkyl, which is optionally substituted with 1 or more groups, each independently selected from C1-6 alkoxy and a 5-7 membered heterocycle attached to N, containing 1-3 heteroatoms selected from N, O and S; and R10 is selected from C1-6 alkyl and C1-6 alkoxy; a tautomer thereof or a pharmaceutically acceptable salt, solvate or polymorph of said compound or tautomer; with the proviso that the compound of formula (1) is not: 3-ethyl-5- (4-imidazol-1-ylphenyl) -4- (4-methoxyphenyl) -4H- [1,2,4] triazole, 3- (3´, 5´-dichlorobiphenyl-4-yl) -4- (2-methoxyphenyl) -5-methyl-4H- [1,2,4] triazole, 3- (3´, 5´-bis- trifluoromethylbiphenyl- 4-yl) -4- (2-fluorophenyl) -5-methyl-4H- [1,2,4] triazole or 3- (3 ', 5'-bis-trifluoromethylbiphenyl-4-yl) -5- methyl-4- (3-trifluoromethylbiphenyl) -4H- [1,2,4] triazole.

ARP040103392A 2003-09-22 2004-09-21 TRIAZOL DERIVATIVES REPLACED AS AN OXITOCINE ANTAGONISTS AR045791A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0322159A GB0322159D0 (en) 2003-09-22 2003-09-22 New substituted triazoles for use as novel pharmaceuticals
GB0403150A GB0403150D0 (en) 2004-02-12 2004-02-12 Novel pharmaceuticals
GB0415110A GB0415110D0 (en) 2004-07-05 2004-07-05 Substituted triazole derivatives as oxytocin antagonists

Publications (1)

Publication Number Publication Date
AR045791A1 true AR045791A1 (en) 2005-11-16

Family

ID=34381637

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040103392A AR045791A1 (en) 2003-09-22 2004-09-21 TRIAZOL DERIVATIVES REPLACED AS AN OXITOCINE ANTAGONISTS

Country Status (12)

Country Link
EP (1) EP1673355A1 (en)
JP (1) JP2007505888A (en)
AR (1) AR045791A1 (en)
BR (1) BRPI0414663A (en)
CA (1) CA2539297C (en)
MX (1) MXPA06003158A (en)
NL (1) NL1027084C2 (en)
PA (1) PA8613001A1 (en)
PE (1) PE20050950A1 (en)
TW (1) TW200526606A (en)
UY (1) UY28524A1 (en)
WO (1) WO2005028452A1 (en)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7745630B2 (en) 2003-12-22 2010-06-29 Justin Stephen Bryans Triazolyl piperidine arginine vasopressin receptor modulators
ME01498B (en) * 2004-11-18 2014-04-20 Synta Pharmaceuticals Corp Triazole compounds that modulate hsp90 activity
AP2007004047A0 (en) * 2005-01-20 2007-06-30 Pfizer Ltd Substituted triazole derivatives as oxtocin antagonists
DE602006003416D1 (en) * 2005-03-21 2008-12-11 Pfizer Ltd SUBSTITUTED TRIAZONE DERIVATIVES AS OXYTOCINANTAGONISTS
JP2008533193A (en) * 2005-03-21 2008-08-21 ファイザー・リミテッド Substituted triazole derivatives as oxytocin antagonists
BRPI0622262A2 (en) 2005-07-09 2011-08-09 Astrazeneca Ab compound, pharmaceutical composition, use of a compound or a pharmaceutically acceptable salt thereof, and process for the preparation of a compound
JP2009504628A (en) * 2005-08-10 2009-02-05 ファイザー・リミテッド Substituted triazole derivatives as oxytocin antagonists
FR2903985B1 (en) 2006-07-24 2008-09-05 Sanofi Aventis Sa N- (AMINO-HETEROARYL) -1H-INDOLE-2-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE
FR2904316B1 (en) 2006-07-31 2008-09-05 Sanofi Aventis Sa N- (AMINO-HETEROARYL) -1H-INDOLE-2-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE.
DE102006059710A1 (en) * 2006-12-18 2008-06-19 Freie Universität Berlin Substituted 4-hydroxypyridines
FR2910473B1 (en) 2006-12-26 2009-02-13 Sanofi Aventis Sa N- (AMINO-HETEROARYL) -1H-PYRROLOPYRIDINE-2-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE.
AP3272A (en) 2008-09-22 2015-05-31 Cayman Chem Co Multiheteroaryl compounds as inhibitors of H-PGDS and their use for treating prosaglandin D2 mediated diseases
PL3037101T3 (en) 2014-12-22 2019-06-28 Ferring B.V. Oxytocin receptor antagonist therapy in the luteal phase for implantation and pregnancy in women undergoing assisted reproductive technologies
JP2020502211A (en) * 2016-12-21 2020-01-23 江蘇恒瑞医薬股▲ふん▼有限公司 Azacyclobutyltriazole derivatives having fused ring groups, their preparation and their use in medicine
CA3047641A1 (en) 2016-12-28 2018-07-05 Jiangsu Hengrui Medicine Co., Ltd. Azabicyclo-substituted triazole derivative, preparation method thereof, and application of same in medicine
TW202016091A (en) * 2018-06-20 2020-05-01 大陸商江蘇恆瑞醫藥股份有限公司 A pharmaceutically acceptable salt and crystal form of otr inhibitor and preparation method thereof
CN113004250B (en) * 2019-12-19 2022-07-26 上海森辉医药有限公司 Process for preparing substituted triazole derivatives

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000063363A (en) * 1998-08-12 2000-02-29 Yamanouchi Pharmaceut Co Ltd New triazole derivative
WO2001058880A1 (en) * 2000-02-08 2001-08-16 Yamanouchi Pharmaceutical Co., Ltd. Novel triazole derivatives
RU2002133666A (en) * 2000-05-19 2007-05-10 Мерк Патент ГмбХ (DE) TRIAZOLE DERIVATIVES
ATE297913T1 (en) * 2001-07-05 2005-07-15 Pfizer Prod Inc SULFONYL-HETEROARYL-TRIAZOLES AS ANTI-INFLAMMATORY AND ANALGESIC AGENTS
ES2249636T3 (en) * 2001-12-20 2006-04-01 Applied Research Systems Ars Holding N.V. TRIAZOLS AS ANTAGONISTS OF OXITOCINE.

Also Published As

Publication number Publication date
JP2007505888A (en) 2007-03-15
WO2005028452A1 (en) 2005-03-31
EP1673355A1 (en) 2006-06-28
CA2539297A1 (en) 2005-03-31
MXPA06003158A (en) 2006-06-05
WO2005028452A9 (en) 2005-07-21
BRPI0414663A (en) 2006-11-21
CA2539297C (en) 2010-07-20
TW200526606A (en) 2005-08-16
NL1027084A1 (en) 2005-03-24
PE20050950A1 (en) 2005-11-11
PA8613001A1 (en) 2005-08-04
UY28524A1 (en) 2005-04-29
NL1027084C2 (en) 2006-01-24

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