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AR109931A1 - Compuesto inhibidor de la prostaglandina d sintasa hematopoyética (h-pgds), composición farmacéutica que lo comprende y uso del compuesto para fabricar un medicamento - Google Patents

Compuesto inhibidor de la prostaglandina d sintasa hematopoyética (h-pgds), composición farmacéutica que lo comprende y uso del compuesto para fabricar un medicamento

Info

Publication number
AR109931A1
AR109931A1 ARP170102843A ARP170102843A AR109931A1 AR 109931 A1 AR109931 A1 AR 109931A1 AR P170102843 A ARP170102843 A AR P170102843A AR P170102843 A ARP170102843 A AR P170102843A AR 109931 A1 AR109931 A1 AR 109931A1
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
fluoro
oxo
independently selected
Prior art date
Application number
ARP170102843A
Other languages
English (en)
Inventor
Eugene L Stuart
Smith Emilie Despagnet
Stephen Andrew Thomson
Barry George Shearer
Christie Schulte
Ashley Paul Hancock
Yu Guo
David Norman Deaton
Original Assignee
Glaxosmithkline Ip Dev Ltd
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 Glaxosmithkline Ip Dev Ltd filed Critical Glaxosmithkline Ip Dev Ltd
Publication of AR109931A1 publication Critical patent/AR109931A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
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    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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    • 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
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/40—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20—Oxygen atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C07D257/06—Five-membered rings with nitrogen atoms directly attached to the ring carbon atom
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    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
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    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
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    • 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
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    • 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
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Hydrogenated Pyridines (AREA)
  • Quinoline Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Furan Compounds (AREA)

Abstract

Un compuesto inhibidor de la prostaglandina D sintasa hematopoyética (H-PGDS) que está representado por la fórmula (1), en donde: X se selecciona de: carbono y nitrógeno; Y se selecciona de: hidrógeno y CH₃; Y¹ está ausente o CH₃; Z es NH u O; a es 0 ó 1; R se selecciona de: O, NH, CH₂ y alquilo C₁ sustituido con halógeno; R¹ se selecciona de: arilo, arilo sustituido de 1 a 4 veces con Rᵃ, heteroarilo, heteroarilo sustituido de 1 a 4 veces con Rᵃ, bicicloheteroarilo, y bicicloheteroarilo sustituido de 1 a 4 veces con Rᵃ; R² se selecciona de: O y S; R³ se selecciona de: arilo, arilo sustituido de 1 a 4 veces con Rᵇ, cicloalquilo, cicloalquilo sustituido de 1 a 4 veces con Rᵇ, heterociclo, heterociclo sustituido de 1 a 4 veces con Rᵇ, heteroarilo, heteroarilo sustituido de 1 a 4 veces con Rᵇ, bicicloheteroarilo, y bicicloheteroarilo sustituido de 1 a 4 veces con Rᵇ; cada Rᵃ se selecciona independientemente de: fluoro, cloro, bromo, yodo, -OH, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con 1 a 5 sustituyentes independientemente seleccionados de: fluoro, cloro, bromo, yodo, alquiloxi C₁₋₄, -OH, alquilo C₁₋₄, oxo, -COOH, -NO₂, -NH₂ y -CN, ciano, -O-alquilo C₁₋₆, -O-alquilo C₁₋₆ sustituido con 1 a 5 sustituyentes independientemente seleccionados de: fluoro, cloro, bromo, yodo, alquiloxi C₁₋₄, -OH, alquilo C₁₋₄, oxo, -COOH, -NO₂, -NH₂ y -CN, -C(O)O-alquilo C₁₋₆, y -C(O)O-alquilo C₁₋₆ sustituido de 1 a 5 veces con fluoro; cada Rᵇ se selecciona independientemente de: ciano, fluoro, cloro, bromo, yodo, alquilo C₁₋₆, Rᵉ, -O-alquilo C₁₋₆, -ORᵉ, oxo, hidroxilo, cicloalquilo, cicloalquilo sustituido de 1 a 4 veces con Rᶠ, amino, -NHRˣ, donde Rˣ se selecciona de arilo, heteroarilo, cicloalquilo, heterocicloalquilo, -O-alquilo C₁₋₆, -O-alquilo C₁₋₆ sustituido con de 1 a 6 sustituyentes independientemente seleccionados de: fluoro, oxo, y -OH, alquilo C₁₋₆, y alquilo C₁₋₆ sustituido con de 1 a 6 sustituyentes independientemente seleccionados de: fluoro, oxo, -OH, -OC₁₋₆alquilo, -COOH, -NH₂, -NH-cicloalquilo, y -CN, heteroarilo, heteroarilo sustituido de 1 a 4 veces con Rᶠ, heterociclo, heterociclo sustituido de 1 a 4 veces con Rᶠ, -SO₂H, y -SO₂-alquilo C₁₋₆; cada Rᶠ se selecciona independientemente de: fluoro, cloro, bromo, yodo, alquilo C₁₋₆, Rᵉ, oxo, -OH, amino, -NHRˣ¹, donde Rˣ¹ se selecciona de arilo, heteroarilo, cicloalquilo, heterocicloalquilo, alquilo C₁₋₆, y alquilo C₁₋₆ sustituido con de 1 a 6 sustituyentes independientemente seleccionados de: fluoro, oxo, -OH, -O-alquilo C₁₋₆, -COOH, -NH₂, y -CN, -NRˣ²Rˣ³, donde Rˣ² y Rˣ³ se selecciona uno independientemente de: arilo, heteroarilo, cicloalquilo, heterocicloalquilo, alquilo C₁₋₆, y alquilo C₁₋₆ sustituido con 1 a 6 sustituyentes independientemente seleccionados de: fluoro, oxo, -OH, -COOH, -NH₂, y -CN, nitro, y ciano, y cada Rᵉ se selecciona independientemente de: alquilo C₁₋₆ sustituido con 1 a 9 sustituyentes independientemente seleccionados de: fluoro, cloro, bromo, yodo, alquilo C₁₋₆, -O-alquilo C₁₋₆, -O-alquilo C₁₋₆ sustituido con 1 a 6 sustituyentes independientemente seleccionados de: fluoro, oxo, -OH, -COOH, -NH₂, -CN, y fenilo, oxo, =N, hidroxilo, amino, -NHRˣˣ, o =NRˣˣ, donde Rˣˣ se selecciona de arilo, heteroarilo, cicloalquilo, heterocicloalquilo, ciano, alquilo C₁₋₆, y alquilo C₁₋₆ sustituido con 1 a 6 sustituyentes independientemente seleccionados de: fluoro, oxo, -OH, -COOH, -O-C₁₋₅ alquilo, -O-alquilo C₁₋₅ sustituido de 1 a 6 veces con fluoro, -NRˣˣ¹Rˣˣ², donde Rˣˣ¹ y Rˣˣ² se selecciona cada uno independientemente de: arilo, heteroarilo, cicloalquilo, heterocicloalquilo, alquilo C₁₋₆, y alquilo C₁₋₆ sustituido con 1 a 6 sustituyentes independientemente seleccionados de: fluoro, oxo, -OH, -COOH, -NH₂, y -CN, arilo, arilo sustituido de 1 a 4 veces con Rˣˣ³, donde Rˣˣ³ se selecciona de: fluoro, cloro, bromo, yodo, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con 1 a 6 sustituyentes independientemente seleccionados de: fluoro, oxo, -OH, -COOH, -NH₂, y -CN, -O-alquilo C₁₋₅, y -O-alquilo C₁₋₆ sustituido con 1 a 6 independientemente sustituyentes seleccionados de: fluoro, oxo, -OH, -COOH, -NH₂, y -CN, cicloalquilo, cicloalquilo sustituido de 1 a 4 veces con Rˣˣ⁴, donde Rˣˣ⁴ se selecciona de: fluoro, cloro, bromo, yodo, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con 1 a 6 sustituyentes independientemente seleccionados de: fluoro, oxo, -OH, -COOH, -NH₂, y -CN, -O-alquilo C₁₋₅, y -O-alquilo C₁₋₆ sustituido con 1 a 6 independientemente sustituyentes seleccionados de: fluoro, oxo, -OH, -COOH, -NH₂, y -CN, nitro, y ciano; o una de sus sales farmacéuticamente aceptables. Los compuestos descritos pueden ser útiles en el tratamiento de la distrofia muscular de Duchenne. Composiciones farmacéuticas que comprenden los compuestos descritos y uso de los compuestos para fabricar un medicamento.
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Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JOP20190072A1 (ar) 2016-10-13 2019-04-07 Glaxosmithkline Ip Dev Ltd مشتقات 1، 3 سيكلوبوتان ثنائي الاستبدال أو آزيتيدين كمثبطات للإنزيم المخلق للبروستاجلاندين d المكون للدم
BR112019026452A2 (pt) * 2017-06-13 2020-07-14 Glaxosmithkline Intellectual Property Development Limited compostos químicos como inibidores de h-pgds
CR20200054A (es) * 2017-08-09 2020-03-21 Denali Therapeutics Inc Compuestos, composiciones y métodos
PT3676297T (pt) 2017-09-01 2023-08-29 Denali Therapeutics Inc Compostos, composições e métodos
TWI877136B (zh) 2019-02-13 2025-03-21 美商戴納立製藥公司 化合物、組合物及方法
US12091392B2 (en) 2019-02-13 2024-09-17 Denali Therapeutics Inc. Compounds, compositions and methods
WO2021152113A1 (en) 2020-01-31 2021-08-05 Bayer Aktiengesellschaft Substituted 2,3-benzodiazepines derivatives
TW202204334A (zh) 2020-04-08 2022-02-01 美商阿吉歐斯製藥公司 Menin抑制劑及治療癌症之使用方法
CN113582880B (zh) * 2020-04-30 2023-11-17 南京药石科技股份有限公司 一种（3-氨基二环[1.1.1]戊烷-1-基）氨基甲酸叔丁酯的制备方法
CN111574473A (zh) * 2020-06-04 2020-08-25 宁夏农林科学院农业资源与环境研究所（宁夏土壤与植物营养重点实验室） 一种氨基噻唑类化合物的合成方法
CN115916776A (zh) * 2020-06-09 2023-04-04 艾尼莫生物科技公司 胶原蛋白1翻译抑制剂及其使用方法
CN111549000B (zh) * 2020-06-18 2022-07-29 中国医学科学院整形外科医院 一种过表达Hpgds的重组脂肪干细胞、制备方法及其应用
WO2021256569A1 (ja) 2020-06-19 2021-12-23 佐藤製薬株式会社 Ｈ－ｐｇｄｓを阻害する縮環化合物
CN114085167A (zh) * 2021-12-13 2022-02-25 华中药业股份有限公司 一种杂质ts-3a的制备方法
CA3240926A1 (en) 2021-12-17 2023-06-22 Sato Pharmaceutical Co., Ltd. Azaindole derivative inhibiting h-pgds
EP4448492A1 (en) 2021-12-17 2024-10-23 Reglagene, Inc. Compositions and methods of making and using small molecules in the treatment of cancer
US20250250265A1 (en) * 2022-04-15 2025-08-07 Vanderbilt University Benzothiazole-phenylsulfonyl-piperidine analogs as activators of nacylphosphatidylethanolamine hydrolyzing phospholipase d
AU2024229823A1 (en) * 2023-02-28 2025-09-11 Reglagene, Inc. Compositions and methods for making and using small molecules for the treatment of health conditions

Family Cites Families (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4031221A (en) * 1974-06-17 1977-06-21 American Hoechst Corporation Method of treating pain and hypertension
US4956359A (en) 1985-02-28 1990-09-11 A. H. Robins Company, Inc. 3-aryloxy and 3-arylthioazetidinecarboxamides as anticonvulsants and antiepileptics
FI87559C (fi) 1985-02-28 1993-01-25 Robins Co Inc A H Foerfarande foer framstaellning av aktiva 3-fenyloxiazetidinkarboxamider
US6809088B2 (en) * 1997-03-24 2004-10-26 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them
GB9801501D0 (en) 1998-01-23 1998-03-18 Cerebrus Ltd Chemical compounds - II
GB9917385D0 (en) 1999-07-23 1999-09-22 Cerebrus Ltd Chemical compounds-I
US6576265B1 (en) 1999-12-22 2003-06-10 Acell, Inc. Tissue regenerative composition, method of making, and method of use thereof
EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
EP1745034A1 (en) * 2004-02-11 2007-01-24 Amgen Inc. Vanilloid receptor ligands and their use in treatments
WO2005094805A1 (ja) 2004-04-01 2005-10-13 Institute Of Medicinal Molecular Design. Inc. イミン誘導体及びアミド誘導体
CA2563963A1 (en) 2004-04-28 2005-11-10 Pfizer Inc. 3-heterocyclyl-4-phenyl-triazole derivatives as inhibitors of the vasopressin v1a receptor
AP2007004047A0 (en) * 2005-01-20 2007-06-30 Pfizer Ltd Substituted triazole derivatives as oxtocin antagonists
WO2007003961A2 (en) 2005-06-30 2007-01-11 Prosidion Limited Gpcr agonists
GB0514017D0 (en) * 2005-07-07 2005-08-17 Ionix Pharmaceuticals Ltd Chemical compounds
TW200720255A (en) 2005-07-13 2007-06-01 Taiho Pharmaceutical Co Ltd Benzoimidazole compound capable of inhibiting prostaglandin d synthetase
JP2007051121A (ja) 2005-07-22 2007-03-01 Taiho Yakuhin Kogyo Kk プロスタグランジンｄ合成酵素を阻害するピリミジン化合物
AR056871A1 (es) 2005-10-04 2007-10-31 Aventis Pharma Inc Compuestos de pirimidina amida como inhibidores de pgds
US20070208426A1 (en) * 2006-03-03 2007-09-06 Sdgi Holdings, Inc. Spinal implant with improved surface properties for delivery
JP2009529577A (ja) * 2006-03-10 2009-08-20 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 可溶性エポキシドヒドロラーゼインヒビター及びその使用方法
JPWO2008023720A1 (ja) 2006-08-23 2010-01-14 アステラス製薬株式会社 ウレア化合物又はその塩
WO2008075172A2 (en) 2006-12-19 2008-06-26 Pfizer Products Inc. Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases
PT2142516E (pt) 2007-03-30 2013-03-07 Sanofi Sa Compostos de hidrazida de pirimidina como inibidores de pgds
GB0706793D0 (en) 2007-04-05 2007-05-16 Evotec Ag Compounds
BRPI0909782B8 (pt) 2008-03-04 2021-05-25 Vernalis R&D Ltd composto derivado de azetidina e composição farmacêutica compreendendo dito composto
JP2011524894A (ja) 2008-06-18 2011-09-08 ファイザー・リミテッド ニコチンアミド誘導体
EP2307377A1 (en) 2008-06-18 2011-04-13 Pfizer Limited Nicotinamide derivatives
WO2010024903A1 (en) * 2008-08-29 2010-03-04 Yangbo Feng BENZO[d]OXAZOLES AND BENZO[d]THIAZOLES AS KINASE INHIBITORS
PE20110843A1 (es) 2008-09-22 2011-12-08 Cayman Chem Co Derivados de 5-(1h-imidazol-5-il)-2-fenilpirimidina, como inhibidores de prostaglandina d sintasa hematopoyetica
RU2496778C2 (ru) * 2009-03-09 2013-10-27 Тайхо Фармасьютикал Ко., Лтд. Пиперазиновое соединение, ингибирующее простагландин-d-синтазу
US20120196854A1 (en) 2009-10-06 2012-08-02 Kyowa Hakko Kirin Co., Ltd. Pharmaceutical composition comprising aromatic heterocyclic compound
SG179199A1 (en) 2009-10-08 2012-04-27 Sanofi Sa Phenyloxadiazole derivatives as pgds inhibitors
PH12012501385A1 (en) 2010-01-22 2014-10-22 Taiho Pharmaceutical Co Ltd Piperazine compound having a pgds inhibitory effect
AU2011253058A1 (en) * 2010-05-13 2012-12-06 Amgen Inc. Heteroaryloxycarbocyclyl compounds as PDE10 inhibitors
WO2011143495A1 (en) * 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
US9050334B2 (en) * 2010-07-16 2015-06-09 Innov88 Llc MIF inhibitors and their uses
RS54544B1 (sr) * 2010-09-13 2016-06-30 Novartis Ag Triazin-oksadiazoli
KR101400192B1 (ko) 2010-12-31 2014-05-27 제일모직 주식회사 포지티브형 감광성 수지 조성물, 이를 사용하여 제조된 감광성 수지막 및 상기 감광성 수지막을 포함하는 반도체 소자
EP3354640A3 (en) 2011-04-13 2018-10-31 Innovimmune Biotherapeutics, Inc. Mif inhibitors and their uses
CA2834920A1 (en) 2011-05-23 2012-11-29 Sanofi Process for the preparation of deuterated compounds containing n-alkyl groups
WO2013074387A1 (en) 2011-11-14 2013-05-23 Merck Sharp & Dohme Corp. Imidazole derivatives
EP2832731A4 (en) 2012-03-27 2015-08-19 Shionogi & Co AROMATIC HETEROCYCLIC CHAIN 5-CORE DERIVED DERIVATIVE HAVING TRPV4 INHIBITORY ACTIVITY
TWI585088B (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并［１，２－ｂ］嗒衍生物
US20150376198A1 (en) 2013-02-18 2015-12-31 The Scripps Research Institute Modulators of vasopressin receptors with therapeutic potential
WO2014179144A1 (en) 2013-04-29 2014-11-06 E. I. Du Pont De Nemours And Company Fungicidal heterocyclic compounds
EP3145925B1 (en) 2014-05-19 2020-11-04 Boehringer Ingelheim Animal Health USA Inc. Anthelmintic compounds
TWI695831B (zh) * 2014-09-13 2020-06-11 香港商南北兄弟藥業投資有限公司 Ｃｒｔｈ２拮抗劑化合物及其用途
JP6708661B2 (ja) * 2015-03-30 2020-06-10 ミッション セラピューティクス リミティド Ｕｓｐ３０阻害剤としての１−シアノ−ピロリジン化合物
US20210238162A1 (en) 2015-12-17 2021-08-05 Glaxosmithkline Intellectual Property Development Limited Chemical compounds
JOP20190072A1 (ar) 2016-10-13 2019-04-07 Glaxosmithkline Ip Dev Ltd مشتقات 1، 3 سيكلوبوتان ثنائي الاستبدال أو آزيتيدين كمثبطات للإنزيم المخلق للبروستاجلاندين d المكون للدم

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