WO2011053597A1 - Inhibiteurs d'autotaxine dérivés d'acide pipémidique - Google Patents

Inhibiteurs d'autotaxine dérivés d'acide pipémidique Download PDF

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Publication number
WO2011053597A1
WO2011053597A1 PCT/US2010/054143 US2010054143W WO2011053597A1 WO 2011053597 A1 WO2011053597 A1 WO 2011053597A1 US 2010054143 W US2010054143 W US 2010054143W WO 2011053597 A1 WO2011053597 A1 WO 2011053597A1
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WO
WIPO (PCT)
Prior art keywords
atx
compounds
mmol
autotaxin
compound
Prior art date
Application number
PCT/US2010/054143
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English (en)
Inventor
Abby Louise Parrill-Baker
Daniel Lee Baker
Adrienne Hoeglund
Original Assignee
The University Of Memphis Research Foundation
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.)
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Publication date
Application filed by The University Of Memphis Research Foundation filed Critical The University Of Memphis Research Foundation
Publication of WO2011053597A1 publication Critical patent/WO2011053597A1/fr

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Classifications

    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention porte sur de nouvelles classes optimisées de composés dérivés d'acide pipémidique qui présentent une inhibition efficace d'enzymes d'autotaxine. De telles classes de composés présentent une réactivité avec l'autotaxine pour réduire finalement la taille des sites réactifs sur celle-ci afin d'empêcher la conversion de lysophosphatide choline en acide lysophosphatidique. De plus, ces composés peuvent être incorporés dans des formules posologiques pour une administration aux humains. Ainsi, ces composés procurent une manière excellente de réduction potentielle de génération de certains cancers attribuables à la présence d'autotaxine se produisant naturellement à l'intérieur du corps humain. L'invention porte également sur des procédés de désactivation d'autotaxine à certains degrés avec celle-ci de telle sorte que les composés sont compris à l'intérieur de l'invention.
PCT/US2010/054143 2009-10-26 2010-10-26 Inhibiteurs d'autotaxine dérivés d'acide pipémidique WO2011053597A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25498109P 2009-10-26 2009-10-26
US61/254,981 2009-10-26

Publications (1)

Publication Number Publication Date
WO2011053597A1 true WO2011053597A1 (fr) 2011-05-05

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ID=43922495

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2010/054143 WO2011053597A1 (fr) 2009-10-26 2010-10-26 Inhibiteurs d'autotaxine dérivés d'acide pipémidique

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WO (1) WO2011053597A1 (fr)

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013142628A2 (fr) * 2012-03-20 2013-09-26 Fred Hutchinson Cancer Research Center Composés et compositions antibiotiques, et procédés d'identification associés
WO2014133112A1 (fr) * 2013-03-01 2014-09-04 国立大学法人東京大学 Dérivé imidazopyrimidinone substitué en position 8 présentant une activité inhibitrice de l'autotaxine
US9051320B1 (en) 2014-08-18 2015-06-09 Pharmakea, Inc. Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor
US9334261B2 (en) 2013-11-22 2016-05-10 Pharmakea, Inc. Autotaxin inhibitor compounds
US9714240B2 (en) 2013-09-17 2017-07-25 Pharmakea, Inc. Vinyl autotaxin inhibitor compounds
US9850203B2 (en) 2013-09-26 2017-12-26 Pharmakea, Inc. Autotaxin inhibitor compounds
US9926318B2 (en) 2013-11-22 2018-03-27 Pharmakea, Inc. Tetracyclic autotaxin inhibitors
US9951026B2 (en) 2013-09-17 2018-04-24 Pharmakea, Inc. Heterocyclic vinyl autotaxin inhibitor compounds
US10138230B2 (en) 2015-02-04 2018-11-27 Cancer Research Technology Limited Autotaxin inhibitors
US10632104B2 (en) 2015-05-27 2020-04-28 Sabre Therapeutics Llc Autotaxin inhibitors and uses thereof
US10654846B2 (en) 2015-02-06 2020-05-19 Cancer Research Technology Limited Autotaxin inhibitory compounds

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4125615A (en) * 1976-07-22 1978-11-14 Dainippon Pharmaceutical Co., Ltd. 2-[4-(P-Aminobenzyl)-1-piperazinyl]-8-ethyl-5,8-dihydro-5-oxopyrido[2,3-d]py
US20080004285A1 (en) * 2004-12-30 2008-01-03 De Jonghe Steven C A Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
US20090306412A1 (en) * 2006-03-31 2009-12-10 Antibe Therapeutics Inc. 4-hydroxythiobenzamide derivatives of drugs

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4125615A (en) * 1976-07-22 1978-11-14 Dainippon Pharmaceutical Co., Ltd. 2-[4-(P-Aminobenzyl)-1-piperazinyl]-8-ethyl-5,8-dihydro-5-oxopyrido[2,3-d]py
US20080004285A1 (en) * 2004-12-30 2008-01-03 De Jonghe Steven C A Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
US20090306412A1 (en) * 2006-03-31 2009-12-10 Antibe Therapeutics Inc. 4-hydroxythiobenzamide derivatives of drugs

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
HOEGLUND ET AL.: "Optimization of a Pipemidic Acid Autotaxin Inhibitor.", J. MED. CHEM., vol. 53, no. 3, 2010, pages 1056 - 1066 *
PARRILL ET AL.: "Virtual screening approaches for the identification of non-lipid autotaxin inhibitors.", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 16, no. ISS 4, 15 February 2008 (2008-02-15), pages 1784 - 1795 *

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013142628A3 (fr) * 2012-03-20 2013-12-05 Fred Hutchinson Cancer Research Center Composés et compositions antibiotiques, et procédés d'identification associés
WO2013142628A2 (fr) * 2012-03-20 2013-09-26 Fred Hutchinson Cancer Research Center Composés et compositions antibiotiques, et procédés d'identification associés
WO2014133112A1 (fr) * 2013-03-01 2014-09-04 国立大学法人東京大学 Dérivé imidazopyrimidinone substitué en position 8 présentant une activité inhibitrice de l'autotaxine
US9714240B2 (en) 2013-09-17 2017-07-25 Pharmakea, Inc. Vinyl autotaxin inhibitor compounds
US9951026B2 (en) 2013-09-17 2018-04-24 Pharmakea, Inc. Heterocyclic vinyl autotaxin inhibitor compounds
US9850203B2 (en) 2013-09-26 2017-12-26 Pharmakea, Inc. Autotaxin inhibitor compounds
US9926318B2 (en) 2013-11-22 2018-03-27 Pharmakea, Inc. Tetracyclic autotaxin inhibitors
US9468628B2 (en) 2013-11-22 2016-10-18 Pharmakea, Inc Autotaxin inhibitor compounds
US9334261B2 (en) 2013-11-22 2016-05-10 Pharmakea, Inc. Autotaxin inhibitor compounds
US9999615B2 (en) 2013-11-22 2018-06-19 Pharmakea, Inc. Autotaxin inhibitor compounds
US10688081B2 (en) 2013-11-22 2020-06-23 Sabre Therapeutics Llc Autotaxin inhibitor compounds
US11344533B2 (en) 2013-11-22 2022-05-31 Sabre Therapeutics Llc Autotaxin inhibitor compounds
US11779568B2 (en) 2013-11-22 2023-10-10 Sabre Therapeutics Llc Autotaxin inhibitor compounds
US9051320B1 (en) 2014-08-18 2015-06-09 Pharmakea, Inc. Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor
US10138230B2 (en) 2015-02-04 2018-11-27 Cancer Research Technology Limited Autotaxin inhibitors
US10428061B2 (en) 2015-02-04 2019-10-01 Cancer Research Technology Limited Autotaxin inhibitors
US10654846B2 (en) 2015-02-06 2020-05-19 Cancer Research Technology Limited Autotaxin inhibitory compounds
US11453666B2 (en) 2015-02-06 2022-09-27 Cancer Research Technology Limited Autotaxin inhibitory compounds
US10632104B2 (en) 2015-05-27 2020-04-28 Sabre Therapeutics Llc Autotaxin inhibitors and uses thereof

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