ES2649995T3 - Benzamidas - Google Patents

Benzamidas Download PDF

Info

Publication number
ES2649995T3
ES2649995T3 ES12738368.5T ES12738368T ES2649995T3 ES 2649995 T3 ES2649995 T3 ES 2649995T3 ES 12738368 T ES12738368 T ES 12738368T ES 2649995 T3 ES2649995 T3 ES 2649995T3
Authority
ES
Spain
Prior art keywords
atoms
cyc
het3
hal
het1
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES12738368.5T
Other languages
English (en)
Inventor
Henry Yu
Jiezhen LI
Thomas E. Richardson
Pandi BHARATHI
Brian H. Heasley
Andreas Goutopoulos
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Application granted granted Critical
Publication of ES2649995T3 publication Critical patent/ES2649995T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/505—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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Reproductive Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Furan Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Saccharide Compounds (AREA)

Abstract

Un compuesto de la fórmula (I-A)I**Fórmula** en donde R1 significa -(CY2)n-E-(CY2)n-Het3, -(CY2)n-Cyc-Het3, -(CY2)n-NHCO-Het3, -(CY2)n-C(Y)(OH)-(CY2)n-Het3, -(CY2)n-Het1, -(CY2)n-NHCO-Het1, -(CY2)n-Ar, -(CY2)n-C(Y)(OH)-(CY2)n-Ar, -(CY2)n-Cyc, -(CY2)n-CONH-Cyc, A, -(CYR8)n-OY, -(CY2)n-COOY, -(CYR8)n-CO-(CY2)n-N(R8)2, -(CY2)n-[C(Y)OH]]m-(CYR8)n-NY2, [-(CY2)n-O]m- (CYR8)n-NYCOY, -(CY2)n-NYCOOY, -(CY2)n-NYCON(R8)2, -(CY2)n-NHCO-CH>=CH2 o -(CY2)n-NHCO-NH- (CY2)n>=CH2; R3 significa Het1, Het3, Ar, H, A o Cyc; R5 significa E-Ar, H, A, COOA o Het1; R8, Y significan, de manera independiente entre sí, H o A; X significa CO o -(CY2)m; E significa -(CY2)m-, CO, -COO- o SO2; A significa alquilo no ramificado o ramificado que tiene 1-10 átomos de C, en donde 1-7 átomos de H se pueden reemplazar de manera independiente entre sí por Hal y/o OH; Cyc significa cicloalquilo que tiene 3-7 átomos de C, en donde 1-4 átomos de H se pueden reemplazar de manera independiente entre sí por Hal y/o OH; Ar significa un carbociclo mono o bicíclico insaturado o aromático que tiene 5-10 átomos de C, que se pueden sustituir con al menos un sustituyente seleccionado del grupo de A, Hal, OY, COOY, CONH2, NHCOY, -(CH2)n- NY2, SO2NH2, NO2, CN y Het2; Het1 significa un heterociclo mono o bicíclico insaturado o aromático que tiene 1-9 átomos de C y 1-3 átomos de N, O y/o S, que se pueden mono o disustituir con al menos un sustituyente seleccionado del grupo de Hal, A, Cyc, OY, CONH2, NHCOY, -(CH2)n-NY2, SO2NY2, NHSO2Y, CN y Ar; Het2 significa imidazolilo, pirazilo, tiazilo o tetrazilo, que pueden estar monosustituidos con metilo; Het3 significa un heterociclo monocíclico saturado que tiene 3-6 átomos de C y 1-3 átomos de N, O y/o S, que se pueden mono, di o trisustituir con al menos un sustituyente seleccionado del grupo de >=O, A, Hal, -(CY2)n-Cyc, - (CY2)n-OY, COY, COOY, CONY2, NHCOY, NY2, CN, SO2Y y -(CY2)n-Ar; Hal significa F, CI, Br o I; y m, n significan, de manera independiente entre sí, 0, 1, 2 ó 3; y/o una sal fisiológicamente aceptable de los mismos, siempre que se excluya el compuesto 3-(3-cloro-benzoilamino)-N-[2-(2,4-dicloro-fenil)-etil]-4-(4-etil-piperazin-1-il)- benzamida.

Description

imagen1
imagen2
imagen3
imagen4
imagen5
imagen6
imagen7
imagen8
imagen9
imagen10
imagen11
imagen12
imagen13
imagen14
imagen15
imagen16
imagen17
imagen18
imagen19
imagen20
imagen21
imagen22
imagen23
imagen24
imagen25
imagen26
imagen27
imagen28
imagen29
imagen30
imagen31
imagen32
imagen33
imagen34
imagen35
imagen36
imagen37
imagen38
imagen39
imagen40
imagen41
imagen42
imagen43
imagen44
imagen45
imagen46
imagen47
imagen48
imagen49
imagen50
imagen51
imagen52
imagen53
imagen54
imagen55
imagen56
imagen57
imagen58
imagen59
imagen60
imagen61
imagen62
imagen63
imagen64
imagen65
imagen66
imagen67
imagen68
imagen69
imagen70
imagen71
imagen72
imagen73
imagen74
imagen75
imagen76
imagen77
imagen78
imagen79
imagen80
imagen81
imagen82
imagen83
imagen84
imagen85
imagen86
imagen87
imagen88
imagen89
imagen90
imagen91
imagen92
imagen93
imagen94
imagen95
imagen96
imagen97
imagen98
imagen99
imagen100
imagen101
imagen102
imagen103
imagen104
imagen105
imagen106
imagen107
imagen108
imagen109
imagen110
imagen111
imagen112
imagen113
imagen114
imagen115
imagen116
imagen117
imagen118
imagen119
imagen120
imagen121
imagen122
imagen123
imagen124
imagen125
imagen126
imagen127
imagen128
imagen129
imagen130
imagen131
imagen132
imagen133
imagen134
imagen135
imagen136
imagen137
imagen138
imagen139
imagen140
imagen141
imagen142
imagen143
imagen144
imagen145
imagen146
imagen147
imagen148
imagen149
imagen150
imagen151
imagen152
imagen153
imagen154
imagen155
imagen156
imagen157
imagen158
imagen159
imagen160
imagen161
imagen162
imagen163
imagen164
imagen165
imagen166
imagen167
imagen168
imagen169
imagen170
imagen171
imagen172
imagen173
imagen174
imagen175
imagen176
imagen177
imagen178
imagen179
imagen180
imagen181
imagen182
imagen183
imagen184

Claims (1)

  1. imagen1
    imagen2
    imagen3
    imagen4
    imagen5
    imagen6
    191
    imagen7
    imagen8
ES12738368.5T 2011-07-18 2012-07-17 Benzamidas Active ES2649995T3 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161508861P 2011-07-18 2011-07-18
US201161508861P 2011-07-18
US201161526342P 2011-08-23 2011-08-23
US201161526342P 2011-08-23
PCT/US2012/047038 WO2013012848A1 (en) 2011-07-18 2012-07-17 Benzamides

Publications (1)

Publication Number Publication Date
ES2649995T3 true ES2649995T3 (es) 2018-01-16

Family

ID=46551951

Family Applications (2)

Application Number Title Priority Date Filing Date
ES17187673T Active ES2899000T3 (es) 2011-07-18 2012-07-17 Benzamidas
ES12738368.5T Active ES2649995T3 (es) 2011-07-18 2012-07-17 Benzamidas

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES17187673T Active ES2899000T3 (es) 2011-07-18 2012-07-17 Benzamidas

Country Status (10)

Country Link
US (3) US9181226B2 (es)
EP (2) EP2734517B1 (es)
JP (2) JP6162694B2 (es)
CN (1) CN103702993B (es)
AU (2) AU2012284184B2 (es)
CA (1) CA2834199C (es)
ES (2) ES2899000T3 (es)
HK (1) HK1195557A1 (es)
IL (1) IL230463A (es)
WO (1) WO2013012848A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013012848A1 (en) * 2011-07-18 2013-01-24 Merck Patent Gmbh Benzamides
JP6219844B2 (ja) 2012-01-10 2017-10-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ 卵胞刺激ホルモンの調節因子としてのベンズアミド誘導体
US9809571B2 (en) 2013-01-07 2017-11-07 University Of Southern California Deoxyuridine triphosphatase inhibitors
CA2902755C (en) 2013-03-11 2021-02-16 Merck Patent Gmbh 6-[4-(1h-imidazol-2-yl)piperidin-1-yl]pyrimidin-4-amine derivatives as modulators of kinase activity
CN104717415B (zh) * 2013-12-12 2019-03-01 华为技术有限公司 一种摄像装置
WO2015196335A1 (en) 2014-06-23 2015-12-30 Tocopherx, Inc. Pyrazole compounds as modulators of fshr and uses thereof
KR102579848B1 (ko) * 2014-12-05 2023-09-18 풀모사이드 리미티드 항진균 화합물
US10570100B2 (en) 2015-07-08 2020-02-25 University Of Southern California Deoxyuridine triphosphatase inhibitors containing amino sulfonyl linkage
CN107922330A (zh) 2015-07-08 2018-04-17 Cv6治疗(Ni)有限公司 含乙内酰脲的脱氧尿苷三磷酸酶抑制剂
WO2017006283A1 (en) 2015-07-08 2017-01-12 Cv6 Therapeutics (Ni) Limited Deoxyuridine triphosphatase inhibitors containing cyclopropano linkage
WO2017006270A1 (en) 2015-07-08 2017-01-12 University Of Southern California Deoxyuridine triphosphatase inhibitors
EP3365324A1 (en) 2015-10-22 2018-08-29 The Procter and Gamble Company Synthesis of cyclohexane carboxamide derivatives useful as sensates in consumer products
US10829457B2 (en) 2016-11-23 2020-11-10 Cv6 Therapeutics (Ni) Limited Nitrogen ring linked deoxyuridine triphosphatase inhibitors
US11168059B2 (en) 2016-11-23 2021-11-09 Cv6 Therapeutics (Ni) Limited Amino sulfonyl compounds
WO2018098204A1 (en) 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited 6-membered uracil isosteres
WO2018128720A1 (en) 2017-01-05 2018-07-12 Cv6 Therapeutics (Ni) Limited Uracil containing compounds

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07258224A (ja) * 1994-03-24 1995-10-09 Dai Ichi Seiyaku Co Ltd 二環性化合物
JPH0959236A (ja) * 1995-08-23 1997-03-04 Dai Ichi Seiyaku Co Ltd ベンズアミド化合物
CA2245586A1 (en) * 1996-02-06 1997-08-14 Japan Tobacco Inc. Novel compounds and pharmaceutical use thereof
FR2765221B1 (fr) * 1997-06-25 1999-07-30 Synthelabo Derives de 4-[(1h-imidazol-4-yl)piperidin-1-yl]anilide, leur preparation et leur application en therapeutique
AR013693A1 (es) * 1997-10-23 2001-01-10 Uriach & Cia Sa J Nuevas piperidinas y piperazinas como inhibidores de la agregacion plaquetaria
DE69931975T2 (de) 1998-08-07 2006-10-05 Applied Research Systems Ars Holding N.V. FSH Mimetika zur Behandlung von Infertilität
US7101878B1 (en) * 1998-08-20 2006-09-05 Agouron Pharmaceuticals, Inc. Non-peptide GNRH agents, methods and intermediates for their preparation
US7008945B1 (en) 1999-03-17 2006-03-07 Astrazeneca Ab Amide derivatives
SE9904652D0 (sv) * 1999-12-17 1999-12-17 Astra Pharma Prod Novel Compounds
EP1307193A1 (en) 2000-07-27 2003-05-07 Affymax Research Institute Agonists of follicle stimulating hormone activity
US20040010033A1 (en) * 2001-02-20 2004-01-15 Pfizer Inc. Non-peptide GnRH agents, methods and intermediates for their preparation
SE0101387D0 (sv) * 2001-04-20 2001-04-20 Astrazeneca Ab Novel compounds
AU2003202115A1 (en) * 2002-02-12 2003-09-04 Pfizer Inc. Non-peptide compounds affecting the action of gonadotropin-releasing hormone (gnrh)
MXPA04012566A (es) * 2002-06-13 2005-04-19 Pfizer Agentes no peptidicos reguladores de la gnrh, composiciones farmaceuticas y procedimientos para su uso.
AU2003299124A1 (en) * 2002-09-20 2004-04-23 Laboratoires Serono Sa Piperazine derivatives and methods of use
SE0203070D0 (en) 2002-10-16 2002-10-16 Astrazeneca Ab Novel compounds
FR2851563B1 (fr) * 2003-02-26 2005-04-22 Sod Conseils Rech Applic Nouveaux derives de benzimidazole et d'imidazo-pyridine et leur utilisation en tant que medicament
US7700583B2 (en) * 2003-04-11 2010-04-20 High Point Pharmaceuticals, Llc 11β-hydroxysteroid dehydrogenase type 1 active compounds
FR2862971B1 (fr) 2003-11-28 2006-03-24 Sod Conseils Rech Applic Nouveaux derives de benzimidazole et d'imidazo-pyridine et leur utilisation en tant que medicament
WO2005108370A1 (ja) 2004-04-16 2005-11-17 Ajinomoto Co., Inc. ベンゼン化合物
US7718703B2 (en) 2005-01-25 2010-05-18 Mitsubishi Tanabe Pharma Corporation Norvaline derivative and method for preparation thereof
JP5301986B2 (ja) * 2005-06-22 2013-09-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 医薬組成物用のチエノピリミジン類
WO2007002742A1 (en) * 2005-06-28 2007-01-04 Pharmacopeia, Inc. Substituted [1,4]-diazepanes as cxcr3 antagonists and their use in the treatment of inflammatory disorders
WO2007008541A2 (en) * 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
BRPI0616574A2 (pt) * 2005-09-27 2009-11-24 Shionogi & Co derivado de sulfonamida tendo atividade antagonìstica de receptor de pgd2
KR20090047391A (ko) * 2006-04-07 2009-05-12 데벨로겐 악틴게젤샤프트 약제학적 조성물을 위한 Ｍｎｋ1/Ｍｎｋ2 억제 활성을 갖는티에노피리미딘
US20110071130A1 (en) * 2006-05-08 2011-03-24 Pharmacopeia, Inc. 2-aminobenzimidazoles for treating neurodegenerative diseases
US20140249135A1 (en) * 2007-03-01 2014-09-04 Novartis Ag Pim kinase inhibitors and methods of their use
MX2009009304A (es) 2007-03-01 2009-11-18 Novartis Ag Inhibidores de cinasa pim y metodos para su uso.
GB0705656D0 (en) * 2007-03-23 2007-05-02 Addex Pharmaceuticals Sa Novel compounds E1
WO2008123469A1 (ja) * 2007-03-30 2008-10-16 Japan Tobacco Inc. ６員環アミド化合物およびその用途
WO2008124614A1 (en) * 2007-04-06 2008-10-16 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
EP2219649A2 (en) * 2007-11-22 2010-08-25 Boehringer Ingelheim International Gmbh Use of mnk inhibitors for the treatment of alzheimer's disease
AU2008345225A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
PE20091576A1 (es) * 2008-02-19 2009-11-05 Sanofi Aventis DERIVADOS DE 3-(AMIDO O SULFAMIDO)-4-(4-AZINIL SUSTITUIDO)BENZAMIDA COMO INHIBIDORES DEL RECEPTOR DE QUIMIOQUINAS CxCR3
UY32138A (es) * 2008-09-25 2010-04-30 Boehringer Ingelheim Int Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables
US20100137386A1 (en) * 2008-12-01 2010-06-03 Tesshi Yamada Tnik inhibitor and the use
US8969342B2 (en) * 2009-03-20 2015-03-03 Brandeis University Compounds and methods for treating mammalian gastrointestinal microbial infections
TWI461426B (zh) 2009-05-27 2014-11-21 Merck Sharp & Dohme （二氫）咪唑並異〔５，１－ａ〕喹啉類
WO2013006308A2 (en) * 2011-07-01 2013-01-10 Merck Patent Gmbh Dihydropyrazoles
WO2013012848A1 (en) * 2011-07-18 2013-01-24 Merck Patent Gmbh Benzamides
JP6219844B2 (ja) * 2012-01-10 2017-10-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ 卵胞刺激ホルモンの調節因子としてのベンズアミド誘導体

Also Published As

Publication number Publication date
IL230463A (en) 2016-12-29
US9181226B2 (en) 2015-11-10
CA2834199A1 (en) 2013-01-24
AU2017200985A1 (en) 2017-03-02
CA2834199C (en) 2020-01-07
CN103702993A (zh) 2014-04-02
US9498475B2 (en) 2016-11-22
EP2734517B1 (en) 2017-08-30
CN103702993B (zh) 2015-11-25
WO2013012848A1 (en) 2013-01-24
EP3263568A1 (en) 2018-01-03
JP6162694B2 (ja) 2017-07-12
US20170022191A1 (en) 2017-01-26
JP6254730B2 (ja) 2017-12-27
AU2012284184A1 (en) 2013-11-07
IL230463A0 (en) 2014-03-31
EP2734517A1 (en) 2014-05-28
JP2014520886A (ja) 2014-08-25
AU2012284184B2 (en) 2017-03-09
HK1195557A1 (zh) 2014-11-14
ES2899000T3 (es) 2022-03-09
US20130023522A1 (en) 2013-01-24
US20160022670A1 (en) 2016-01-28
US9938262B2 (en) 2018-04-10
JP2017141244A (ja) 2017-08-17
EP3263568B1 (en) 2021-08-25

Similar Documents

Publication Publication Date Title
ES2649995T3 (es) Benzamidas
JP2017536335A5 (es)
AR081058A1 (es) Derivados de arilmetoxi isoindolina, composiciones que los comprenden y su uso en el tratamiento del cancer.
AR110922A1 (es) Compuestos inhibidores del vih
AR090240A1 (es) Derivados de triazolopirazina
AR097866A1 (es) Derivados de 4-azaindol
BR112015009850A2 (pt) compostos de piridila substituídos por heteroarila úteis como moduladores de quinase
AR089818A1 (es) Inhibidor de la quinasa que regula la señal de la apoptosis
AR096621A1 (es) Inhibidores de isómeros de la fosfatidilinositol 3-quinasa (pi3k)
AR094277A1 (es) Derivados de fumarato sustituidos con deuterio
AR094313A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR099376A1 (es) Compuestos de diaminopirimidilo sustituidos, sus composiciones y métodos de tratamiento con aquellos
ES2587953T3 (es) Amidas cíclicas como inhibidores de MetAP-2
AR076435A1 (es) Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos
AR091858A1 (es) INHIBIDORES DE CISTATIONIN-g-LIASA (CSE)
JP2018502048A5 (es)
AR088423A1 (es) Ligadores p1 ciclicos como inhibidores del factor xia
AR093805A1 (es) Derivados de piridina agonistas del receptor 2 de cannabinoides
AR103170A1 (es) Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de desordenes inflamatorios y osteoartritis
AR092684A1 (es) Compuestos de sulfonamida sustituidos
AR061134A1 (es) Derivados de tioxantina
GT201300096A (es) Composiciones farmaceuticas que contienen un inhibidor de dgat1
ES2587304T3 (es) Derivados de diaminopirimidina y procedimientos para la preparación de los mismos
AR108906A1 (es) Heterociclos de biarilmetilo
AR089944A1 (es) Derivados de tetrahidro-quinazolinona