[go: up one dir, main page]

AR079492A1 - Moduladores de crth2 - Google Patents

Moduladores de crth2

Info

Publication number
AR079492A1
AR079492A1 ARP100104664A ARP100104664A AR079492A1 AR 079492 A1 AR079492 A1 AR 079492A1 AR P100104664 A ARP100104664 A AR P100104664A AR P100104664 A ARP100104664 A AR P100104664A AR 079492 A1 AR079492 A1 AR 079492A1
Authority
AR
Argentina
Prior art keywords
ring
halogen
independently selected
instances
independently
Prior art date
Application number
ARP100104664A
Other languages
English (en)
Inventor
James Jia
Takashi Nakai
Charles Kim
Joel Moore
Ara Mermerian
Bo Peng
Colleen Hudson
Jason Rodhe
Regina Graul
Wilmin Bartolini
Kevin Sprott
Original Assignee
Ironwood Pharmaceuticals Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43735997&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR079492(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ironwood Pharmaceuticals Inc filed Critical Ironwood Pharmaceuticals Inc
Publication of AR079492A1 publication Critical patent/AR079492A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • 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
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P27/14—Decongestants or antiallergics
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/325—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)

Abstract

Se divulgan los moduladores de CRTH2, particularmente los antagonistas de CRTH2, que son utiles para tratar varios trastornos, incluyendo el asma y los trastornos respiratorios. Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable del mismo; con la condicion de que el compuesto de formula (1) no es un compuesto seleccionado de ácido 5-[[6-metoxi-3-(4-metoxibenzoíl)-2-metil-1H-pirrol[2,3-b]piridin-1-il]metil]-a,a-dimetil-2H-tetrazol-2-acético [ns de registro CAS 1097838-63-5], ácido 5-[[5-(benzoílamino)-2-tiazolil]tio]-2H-tetrazol-2-acético [ns de registro CAS 1099441-56-1], ácido 2-butil-1-[[4-[(2-carboxibenzoíl)amino]fenil]metil]-5-cloro-1H-imidazol-4-acético [ns de registro CAS 114798-40-2], y ácido 2-butil-1-[[4-[(2-carboxibenzoíl)amino]fenil]metil]-5-cloro-1H-imidazol-4-acético [ns de registro CAS 114773-45-4], o una sal farmacéuticamente aceptable de los mismos; en donde: el anillo A es un anillo monocíclico o bicíclico seleccionado de arilo de 6 a 10 miembros, heteroarilo de 5 a 10 miembros, cicloalifático C3-10 y heterociclo de 4 a 10 miembros; en donde dicho heteroarilo o heterociclo contiene entre 0 y 3 heteroátomos del anillo independientemente seleccionados de N, O y S; el anillo B es un anillo monocíclico seleccionado de fenilo y heteroarilo de 5 a 6 miembros en donde dicho heteroarilo contiene hasta tres heteroátomos del anillo independientemente seleccionados de N, O y S; el anillo D es un heteroarilo de 5 miembros; en donde x1 se selecciona de N y C; x2 se selecciona de N y C-R2; x3 se selecciona de N y C; x4 se selecciona de N y C-R4; y x5 se selecciona de N y C-R5; siempre que al menos uno de x1 o x3 sea N, pero ambos al mismo no sean simultáneamente N; R2 se selecciona de -H, halogeno, -NO2, -CN, radical C1-6 alifático, alcoxi C1-6 y un anillo ciclopropilo, en donde R2 está independientemente sustituido con entre 0 y 3 instancias de RA; en donde cada RA está independientemente seleccionado de halogeno, -OH, alcoxi C1-2 y haloalcoxi C1-2; R4 se selecciona a partir de halogeno, -NO2, -CN, -R6, -OR6, -C(O)R6, -C(O)OR6, -N(R6)2, -S(O)pR6, -S(O)2N(R6)2, -NR6S(O)2R6, -C(O)N(R6)2 y -NR6C(O)R6; R5 se selecciona a partir de halogeno, -NO2, -CN, -R6, -OR6, -C(O)R6, -C(O)OR6, -N(R6)2, -S(O)pR6, -S(O)2N(R6)2, -NR6S(O)2R6, -C(O)N(R6)2 y -NR6C(O)R6; p es un entero seleccionado de 0, 1 y 2; cada R6 se selecciona independientemente de -H, un radical C1-6 alifático y un anillo monocíclico o bicíclico; en donde el anillo se selecciona de arilo de 6 a 10 miembros, heteroarilo de 5 a 10 miembros, cicloalifático C3-10 y heterociclo de 4 a 10 miembros; donde cuando R6 es un radical C1-6 alifático, está independientemente sustituido con entre 0 y 6 instancias de R7, cuando R6 es un anillo no aromático o un heteroarilo, está independientemente sustituido con entre 0 y 6 instancias de R8, y cuando R6 es un arilo, está independientemente sustituido con entre 0 y 6 instancias de R8'; cada R7 se selecciona independientemente a partir de halogeno, -CN, oxo, -OR9, -R10, -C(O)R9, -C(O)OR9, -S(O)mR9, -N(R9)2, -S(O)2N(R9)2, -NR9S(O)2R9, -C(O)N(R9)2 y -NR9C(O)R9; cada R8 se selecciona independientemente a partir de halogeno, -CN, -NO2, oxo, radical alifático C1-6, -R10, -C(O)R9, -C(O)OR9, -OR9, -S(O)mR9, -N(R9)2, -S(O)2N(R9)2, -NR9S(O)2R9, -C(O)N(R9)2 y -NR9C(O)R9; cada R8' se selecciona independientemente de halogeno, -CN, -NO2, radical alifático C1-6, -R10, -C(O)R9, -C(O)OR9, -OR9, -S(O)mR9, -N(R9)2, -S(O)2N(R9)2, -NR9S(O)2R9, -C(O)N(R9)2 y -NR9C(O)R9; cada R9 se selecciona independientemente de hidrogeno, radical alifático C1-6 y un anillo monocíclico o bicíclico; en donde el anillo se selecciona de arilo de 6 a 10 miembros, heteroarilo de, 5 a 10 miembros, cicloalifático C3-10 y heterociclo de 4 a 10 miembros; en donde cuando R9 es un radical alifático C1-6, está independientemente sustituido con entre 0 y 6 instancias de R11 y cuando R9 es un anillo, está independientemente sustituido con entre 0 y 3 instancias de R12; cada R10 es un anillo monocíclico o bicíclico independientemente seleccionado de arilo de 6 a 10 miembros, heteroarilo de 5 a 10 miembros, cicloalifático C3-10 y heterociclo de 4 a 10 miembros; y cada R10 está independientemente sustituido con entre 0 y 3 instancias de R12; cada R11 está independientemente seleccionado de halogeno, -CN, -OH, alcoxi C1-4 y haloalcoxi C1-4; cada R12 está independientemente seleccionado de halogeno, -CN, -OH, alcoxi C1-4, haloalcoxi C1-4, alcoxi C1-4, y haloalcoxi C1-4; R13 se selecciona de -H, radical alifático C1-6 y un anillo monocíclico o bicíclico donde el anillo se selecciona de arilo de 6 a 10 miembros, heteroarilo de 5 a 10 miembros, cicloalifático C3-10 y heterociclo de 4 a 10 miembros; donde cuando R13 es un radical alifático C1-6, está independientemente sustituido con entre 0 y 6 instancias de R14, cuando R13 es un anillo no aromático o un heteroarilo, está independientemente sustituido con entre 0 y 6 instancias de R15, y cuando R13 es un arilo, está independientemente sustituido con entre 0 y 6 instancias de R15'; cada R14 se selecciona independientemente a partir de halogeno, -CN, oxo, -OR9, -R10, -C(O)R9, -C(O)OR9, -S(O)mR9, -N(R9)2, -S(O)2N(R9)2, -NR9S(O)2R9, -C(O)N(R9)2 y -NR9C(O)R9; cada R15 se selecciona independientemente a partir de halogeno, -CN, -NO2, oxo, radical alifático C1-6, -R10, -C(O)R9, -C(O)OR9, -OR9, -S(O)mR9, -N(R9)2, -S(O)2N(R9)2, -NR9S(O)2R9, -C(O)N(R9)2 y -NR9C(O)R9; y R15' se selecciona independientemente de halogeno, -CN, -NO2, radical alifático C1-6, -R10, -C(O)R9, -C(O)OR9, -OR9, -S(O)mR9, -N(R9)2, -S(O)2N(R9)2, -NR9S(O)2R9, -C(O)N(R9)2 y -NR9C(O)R9; R16 y R17 están independientemente seleccionados de -H, deuterio, alquilo C1-6, haloalquilo C1-6, y halogeno, o alternativamente, R16 y R17 están independientemente seleccionados de alquilo C1-4 y haloalquilo C1-6, y R16 y R17 tomados en conjunto con el átomo al que están unidos forman un anillo ciclopropilo y halociclopropilo; L es un enlace seleccionado de metileno, -C(O)-, -O-, S(O)m y -NR1-; en donde cuando L es un metileno, está independientemente sustituido con entre 0 y 2 instancias de R18; m es 0, 1 o 2; R1 está seleccionado de -H, radical alifático C1-6, cicloalifático C3-6, -CO(alifático C1-6), -CO(cicloalifático C3-6), -CO-(fenilo), bencilo y -CO-(bencilo); en donde cuando R1 está seleccionado de radical alifático C1-6, -CO-(fenilo), bencilo y -CO-(bencilo), está independientemente sustituido de entre 0 y 3 instancias de RB; en donde cada RB está independientemente seleccionado de halogeno, alquilo C1-2 alcoxi C1-2; cada R18 está independientemente seleccionado de halogeno, -CN, radical alifático C1-6, radical haloalifático C1-6, y cicloalifático C3-6; o alternativamente, cada R18 está independientemente seleccionado de radical alifático C1-6 y radical haloalifático C1-6, y dos grupos R18 tomados en conjunto con el átomo al que están unidos forman un anillo ciclopropilo y halociclopropilo; o es un entero seleccionado de 0, 1 y 2; cada JB está independientemente seleccionado de halogeno, -NO2, -CN, -R19, -C(O)H, -C(O)OH, -C(O)NH2, -OH, -SH, -NH2,-C(O)R19, -C(O)OR19, -C(O)N(R20)R19, -N(R20)C(O)R19, -OR19, -SR19 y-NR19R20; o alternativamente, dos grupos JB unidos a dos anillos vecinos de los átomos del anillo B, junto con dichos átomos del anillo, forman un heterociclo de 5 a 6 miembros o un heteroarilo de 5 a 6 miembros, cada uno de los anillos esta independientemente sustituido con entre 0 y 2 instancias de RE, en donde cada RE está independientemente seleccionado de halogeno, alquilo C1-2, alcoxi C1-2, -CN y -OH; cada R20 está independientemente seleccionado de -H y un radical alifático C1-6; cada R19 está independientemente seleccionado de radical alifático C1-6, cicloalifático C3-6, fenilo, bencilo, heterociclo de 4 a 6 miembros y heteroarilo de 5 a 6 miembros; en donde cuando R19 es un radical alifático C1-6, está independientemente sustituido con entre 0 y 3 instancias de RC, donde cada RC está independientemente seleccionado de halogeno, -CN, -OH, -NH2, cicloalquilo C3-4, halocicloalquilo C3-4, -O(alquilo C1-4), -O(cicloalquilo C3-4), -O(halocicloalquilo C3-4), -O(haloalquilo C1-4), -NH(alquilo C1-4), -N(alquilo C1-4)2, y -NRV; en donde -NRV es un heterociclo de 4 a 6 miembros que contiene un átomo del anillo N ligado a JB, y en donde dicho heterociclo contiene de 0 a 2 heteroátomos adicionales del anillo seleccionados a partir de O y N; cuando R19 es un heterociclo o un heteroarilo, contiene de 1 a 3 heteroátomos del anillo seleccionados independientemente a partir de N, O y S; cuando R19 es fenilo, está independientemente sustituido con entre 0 y 3 instancias de RD, donde cada RD está independientemente seleccionado de halogeno, radical alifático C1-4, -CN, -OH, -NH2, -O(alquilo C1-4), -NH(alquilo C1-4) y -N(alquilo C1-4)2; en donde cuando R19 es un anillo no aromático o un heteroarilo, está independientemente sustituido con entre 0 y 3 instancias de RD', donde cada RD' está independientemente seleccionado de halogeno, oxo, radical alifático C1-4, -CN, -OH, -NH2, -O(alquilo C1-4), -NH(alquilo C1-4) y -N(alquilo C1-4)2; en donde L' es un enlace seleccionado de -Y-SO2-, -NR21SO2-, -SO2NR21-, -Y-C(O)-, -NR21C(O)- y -C(O)NR21-; en donde Y está seleccionado de un enlace simple, un enlace recto de alquileno C1-2 y un enlace ramificado de alquileno C2, en donde el enlace alquileno C1-2 está independientemente sustituido con entre 0 y 3 átomos de halogeno; R21 está seleccionado de hidrogeno, alquilo C1-6, haloalquilo C1-6, y anillo cicloalquilo C3-6; n es un entero seleccionado de 0, 1, 2 y 3; cada JA está independientemente seleccionado de halogeno, -NO2, -CN, -R22, -C(O)H, -C(O)OH, -C(O)NH2, -OH, -SH, y -NH2, -C(O)R22, -C(O)OR22, -C(O)N(R23)R22, -N(R23)C(O)R22, -OR22, -SR22 y -NR22R23; cada R23 está independientemente seleccionado de -H y un radical alifático C1-6; cada R22 está independientemente seleccionado de radical alifático C1-4, anillo c
ARP100104664A 2009-12-23 2010-12-16 Moduladores de crth2 AR079492A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US28984109P 2009-12-23 2009-12-23

Publications (1)

Publication Number Publication Date
AR079492A1 true AR079492A1 (es) 2012-02-01

Family

ID=43735997

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104664A AR079492A1 (es) 2009-12-23 2010-12-16 Moduladores de crth2

Country Status (21)

Country Link
US (1) US8674115B2 (es)
EP (1) EP2516416A1 (es)
JP (1) JP5731538B2 (es)
KR (1) KR20120098908A (es)
CN (1) CN102822163B (es)
AR (1) AR079492A1 (es)
AU (1) AU2010333829A1 (es)
BR (1) BR112012017756A2 (es)
CA (1) CA2785191A1 (es)
CL (1) CL2012001712A1 (es)
CO (1) CO6640201A2 (es)
CR (1) CR20120343A (es)
EA (1) EA201200855A1 (es)
EC (1) ECSP12011996A (es)
MX (1) MX2012007239A (es)
PH (1) PH12012501280A1 (es)
SG (1) SG181900A1 (es)
TW (1) TW201130810A (es)
UY (1) UY33110A (es)
WO (1) WO2011079007A1 (es)
ZA (1) ZA201204527B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012078210A1 (en) * 2010-12-08 2012-06-14 Ironwood Pharmaceuticals, Inc. Crth2 modulators and preparation thereof
JP5999387B2 (ja) * 2011-03-25 2016-09-28 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 Ｃｒｔｈ２拮抗薬としてのピラゾール化合物
US20150080381A1 (en) * 2012-04-12 2015-03-19 Ironwood Pharmaceuticals, Inc. Methods of treating alopecia and acne
WO2017104728A1 (ja) * 2015-12-16 2017-06-22 国立大学法人東京大学 食物アレルギー治療薬
TWI742074B (zh) * 2016-04-22 2021-10-11 瑞典商阿斯特捷利康公司 Mcl-1抑制劑及其使用方法
JP2023521468A (ja) * 2020-04-16 2023-05-24 エフ． ホフマン－ラ ロシュ アーゲー ビフェニル誘導体

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US3995631A (en) 1971-01-13 1976-12-07 Alza Corporation Osmotic dispenser with means for dispensing active agent responsive to osmotic gradient
US4203440A (en) 1978-10-23 1980-05-20 Alza Corporation Device having variable volume chamber for dispensing useful agent
US4627850A (en) 1983-11-02 1986-12-09 Alza Corporation Osmotic capsule
EP0192963B1 (de) 1985-02-27 1988-07-20 Werkzeugmaschinenfabrik Oerlikon-Bührle AG Schwingungsmesseinrichtung für ein Spiralkegelradgetriebe auf einer Zahnradprüfmaschine
IL92966A (en) 1989-01-12 1995-07-31 Pfizer Dispensing devices powered by hydrogel
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5324280A (en) 1990-04-02 1994-06-28 Alza Corporation Osmotic dosage system for delivering a formulation comprising liquid carrier and drug
US5565473A (en) 1990-10-12 1996-10-15 Merck Frosst Canada, Inc. Unsaturated hydroxyalkylquinoline acids as leukotriene antagonists
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
CN1071924A (zh) * 1991-10-29 1993-05-12 纳幕尔杜邦公司 除草的三唑羧酸酰胺
US5994341A (en) 1993-07-19 1999-11-30 Angiogenesis Technologies, Inc. Anti-angiogenic Compositions and methods for the treatment of arthritis
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
BR9608498B1 (pt) 1995-06-21 2008-11-18 derivados de amino bicÍclico e antagonista pgd2 contendo os mesmos.
US5859042A (en) * 1995-09-27 1999-01-12 Ono Pharmaceutical Co., Ltd. Five membered heterocyclic compounds
JP4120993B2 (ja) 1996-12-12 2008-07-16 塩野義製薬株式会社 ヘテロ環縮合ベンゼンカルボン酸アミド誘導体およびそれを含有するｐｇｄ２拮抗剤
CZ297324B6 (cs) 1996-12-13 2006-11-15 Shionogi & Co., Ltd. Benzothiofenkarboxamidové deriváty a antagonisty PGD2, které je obsahují
CA2354472C (en) 1998-12-17 2009-02-24 Alza Corporation Conversion of liquid filled gelatin capsules into controlled release systems by multiple coatings
US7217714B1 (en) 1998-12-23 2007-05-15 Agouron Pharmaceuticals, Inc. CCR5 modulators
US6342249B1 (en) 1998-12-23 2002-01-29 Alza Corporation Controlled release liquid active agent formulation dosage forms
US20010051624A1 (en) 2000-04-12 2001-12-13 Jones Thomas R. Method and compositions for the treatment of allergic conditions using PGD2 receptor antagonists
AU2001250206A1 (en) 2000-04-12 2001-10-30 Merck Frosst Canada Ltd Method and compositions for the treatment of allergic conditions using pgd2 receptor antagonists
US6878522B2 (en) 2000-07-07 2005-04-12 Baiyong Li Methods for the identification of compounds useful for the treatment of disease states mediated by prostaglandin D2
MXPA03008109A (es) 2001-03-07 2003-12-12 Pfizer Prod Inc Moduladores de la actividad de receptores de quimiocinas.
EP1424335A4 (en) 2001-09-07 2005-11-16 Ono Pharmaceutical Co INDOLE DERIVATIVES
US7153852B2 (en) 2001-09-07 2006-12-26 Ono Pharmaceutical Co., Ltd. Indole compounds, process for producing the same and drugs containing the same as the active ingredient
PL370548A1 (en) 2001-10-22 2005-05-30 Pfizer Products Inc. Piperazine derivatives with ccr1 receptor antagonist activity
SE0200356D0 (sv) 2002-02-05 2002-02-05 Astrazeneca Ab Novel use
SE0200411D0 (sv) 2002-02-05 2002-02-05 Astrazeneca Ab Novel use
ES2263960T3 (es) 2002-04-08 2006-12-16 Pfizer Inc. Derivados de tropano como moduladores de ccr5.
WO2003097042A1 (en) 2002-05-16 2003-11-27 Shionogi & Co., Ltd. Pgd2 receptor antagonist
WO2003097598A1 (en) 2002-05-16 2003-11-27 Shionogi & Co., Ltd. Compound exhibiting pgd 2 receptor antagonism
TW200307542A (en) 2002-05-30 2003-12-16 Astrazeneca Ab Novel compounds
SE0201635D0 (sv) 2002-05-30 2002-05-30 Astrazeneca Ab Novel compounds
SE0202241D0 (sv) 2002-07-17 2002-07-17 Astrazeneca Ab Novel Compounds
GB0217431D0 (en) 2002-07-27 2002-09-04 Astrazeneca Ab Novel compounds
AP2005003226A0 (en) 2002-08-12 2005-03-31 Pfizer Prod Inc Crystal forms of quinoxaline-2-carboxylic acid[4-carbamoyl-(3-fluorobenzyl)-2,7-dihydroxy-7-methyl-octyl]-amide.
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
EP1539713B1 (en) 2002-08-24 2007-12-19 Astrazeneca AB Pyrimidine derivatives as modulators of chemokine receptor activity
GB0221828D0 (en) 2002-09-20 2002-10-30 Astrazeneca Ab Novel compound
GB0221829D0 (en) 2002-09-20 2002-10-30 Astrazeneca Ab Novel compound
EP1556047A4 (en) 2002-10-04 2009-09-30 Millennium Pharm Inc ANTAGONISTS AGAINST THE PGD2 RECEPTOR FOR THE TREATMENT OF INFLAMMATORY DISEASES
US20040097554A1 (en) 2002-10-30 2004-05-20 Pfizer Inc Heteroaryl-hexanoic acid amide derivatives as immonomodulatory agents
US20040116441A1 (en) 2002-10-30 2004-06-17 Pfizer Inc Methods of using sulfonic acid derivatives
US20040092529A1 (en) 2002-10-30 2004-05-13 Pfizer Inc Methods of using piperazine derivatives
AR042628A1 (es) 2002-12-20 2005-06-29 Astrazeneca Ab Derivados de piperidina como moduladores del receptor ccr5
SE0203828D0 (sv) 2002-12-20 2002-12-20 Astrazeneca Ab Chemical compounds
SE0203820D0 (sv) 2002-12-20 2002-12-20 Astrazeneca Ab chemical compounds
ES2401079T3 (es) * 2002-12-20 2013-04-16 Amgen Inc. Moduladores del asma y de la inflamación alérgica
MXPA06001506A (es) 2003-08-04 2006-05-15 Pfizer Prod Inc Formas de dosificacion de inhibidores de la proteina de transferencia de colesteril ester e inhibidores de la hmg-coa reductasa.
JP2008500991A (ja) * 2004-05-29 2008-01-17 ７ティーエム ファーマ エイ／エス 医学的使用のためのｃｒｔｈ２レセプターリガンド
EP1758571A1 (en) 2004-05-29 2007-03-07 7TM Pharma A/S Crth2 receptor ligands for therapeutic use
EP1758874A1 (en) 2004-05-29 2007-03-07 7TM Pharma A/S Substituted thiazoleacetic acids as crth2 ligands
CN1980908A (zh) 2004-05-29 2007-06-13 7Tm制药联合股份有限公司 取代的噻唑乙酸作为crth2配体
GB0427381D0 (en) 2004-12-14 2005-01-19 Novartis Ag Organic compounds
DK2046740T3 (da) 2006-07-22 2012-08-20 Oxagen Ltd Forbindelser med CRTH2-antagonistisk virkning
JP2011509991A (ja) * 2008-01-22 2011-03-31 オキサジェン リミテッド Ｃｒｔｈ２アンタゴニスト活性を有する化合物
EP2268281A4 (en) * 2008-02-15 2012-05-02 Abbott Lab THIENOPYRROLES AND PYRROLOTHIAZOLES AS NEW THERAPEUTIC AGENTS

Also Published As

Publication number Publication date
CN102822163A (zh) 2012-12-12
CR20120343A (es) 2013-01-25
CN102822163B (zh) 2016-01-20
JP5731538B2 (ja) 2015-06-10
ECSP12011996A (es) 2012-10-30
ZA201204527B (en) 2013-09-25
US20110150834A1 (en) 2011-06-23
CO6640201A2 (es) 2013-03-22
BR112012017756A2 (pt) 2016-04-19
EP2516416A1 (en) 2012-10-31
UY33110A (es) 2011-07-29
JP2013515726A (ja) 2013-05-09
WO2011079007A1 (en) 2011-06-30
EA201200855A1 (ru) 2013-04-30
MX2012007239A (es) 2012-10-15
US8674115B2 (en) 2014-03-18
CL2012001712A1 (es) 2012-12-07
AU2010333829A1 (en) 2012-07-12
CA2785191A1 (en) 2011-06-30
PH12012501280A1 (en) 2013-02-04
KR20120098908A (ko) 2012-09-05
SG181900A1 (en) 2012-08-30
TW201130810A (en) 2011-09-16

Similar Documents

Publication Publication Date Title
AR079492A1 (es) Moduladores de crth2
MX2009003410A (es) Fosfoindoles enantiomericamente puros como inhibidores de vih.
AR075204A1 (es) Inhibidores de dpp-4 y composiciones farmaceuticas que los comprenden, utiles para tratar enfermedades metabolicas en pacientes pediatricos, particularmente diabetes mellitus tipo 2
CL2007001427A1 (es) Sal de maleato de 5-amino-3-(2',3'-di-o-acetil-beta-d-ribofuranosil)-3h-tiazolo[4,5-d]pirimidin-2-ona; procedimiento de preparacion; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de una infeccion po
PE20090622A1 (es) Nuevos derivados de bencimidazol sustituido
AR064010A1 (es) Inhibidores de la actividad de la akt
CL2013003360A1 (es) “compuestos derivados de 4-aril-n-[3-(sulfonimidoil)fenil]-1,3,5-triazin-2-amina sustituidos, inhibidores cdk; compuestos intermediarios, composición y combinación farmacéutica que los comprende; y su uso en el tratamiento de enfermedades hiperproliferativas, infecciosas inducidas por virus y/o cardiovasculares”. pct
SMT201400017B (it) Agenti assorbenti per luce uv/visible per materiali per lenti oftalmiche
ATE550329T1 (de) Heterobicyclische sulfonamidderivate zur behandlung von diabetes
BRPI0822625A2 (pt) "dispositivo espaçador modular para o tratamento de infecções por próteses"
UY32884A (es) 1-sustituido-4-(5-(fenil o heteroaril)metoxi)-pirimidin-2-il)piperazinas y piperidinas
RU2014120792A (ru) Способ лечения стромальных опухолей желудочно-кишечного тракта
AR062510A1 (es) Derivados de piridona con actividad antagonista de mch y medicamentos que comprenden estos compuestos
EA201491607A1 (ru) Модуляторы толлподобных рецепторов
AR066424A1 (es) Inhibidores de proteina activada de la 5- lipoxigenasa ( flap)
EP2403447A4 (en) MICRO-CAPACITED BIOACTIVE AGENTS FOR ORAL RELEASE AND METHOD FOR THEIR USE
EP2427193A4 (en) USE OF PDE7 INHIBITORS FOR THE TREATMENT OF MOTION FLUCTUATIONS
MA29097B1 (fr) Composes pour le traitement des infections virales par flaviviridae
ECSP066950A (es) Combinaciones de glicopirrolato y agonistas del adrenoceptor-beta2
ME02576B (me) Derivati tetrahidropirolotiazina kao inhibitori bace
EP2376091A4 (en) NEW TARGETS FOR THE TREATMENT OF HYPERCHOLESTERINMIA
DK2918288T3 (da) Anvendelse af TGF-beta-antagonister til behandling af spædbørn med risiko for udvikling af bronkopulmonal dysplasi
NO20085271L (no) Muscarin reseptoragonister som er effektive i behandling av smerte, Alzheimers sykdom og schizofreni
UA109290C2 (uk) Спільні кристали і солі інгібіторів ccr3
EA201590022A1 (ru) Новые производные 1,3-дигидро-2h-бензимидазол-2-она, замещенные гетероциклами, в качестве противовирусных средств против респираторного синцитиального вируса

Legal Events

Date Code Title Description
FA Abandonment or withdrawal