AU2011215638B2 - Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mGluR4 allosteric potentiators, compounds, and methods of treating neurological dysfunction - Google Patents

Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mGluR4 allosteric potentiators, compounds, and methods of treating neurological dysfunction Download PDF

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AU2011215638B2
AU2011215638B2 AU2011215638A AU2011215638A AU2011215638B2 AU 2011215638 B2 AU2011215638 B2 AU 2011215638B2 AU 2011215638 A AU2011215638 A AU 2011215638A AU 2011215638 A AU2011215638 A AU 2011215638A AU 2011215638 B2 AU2011215638 B2 AU 2011215638B2
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optionally substituted
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aryl
heteroaryl
cycloalkyl
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AU2011215638A1 (en
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Yiu-Yin Cheung
P. Jeffrey Conn
Darren W. Engers
Rocco D. Gogliotti
Corey R. Hopkins
Craig W. Lindsley
Colleen M. Niswender
James M. Salovich
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Vanderbilt University
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems
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    • 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
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    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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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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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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AU2011215638A 2010-02-11 2011-02-11 Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mGluR4 allosteric potentiators, compounds, and methods of treating neurological dysfunction Ceased AU2011215638B2 (en)

Priority Applications (1)

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AU2013202881A AU2013202881A1 (en) 2010-02-11 2013-04-08 Pyrazolopyridine, Pyrazolopyrazine, Pyrazolopyrimidine, Pyrazolothiophene and Pyrazolothiazole Compounds as mGluR4 Allosteric Potentiators, Compositions, and Methods of Treating Neurological Dysfunction

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US30348110P 2010-02-11 2010-02-11
US61/303,481 2010-02-11
US201161430521P 2011-01-06 2011-01-06
US61/430,521 2011-01-06
PCT/US2011/024618 WO2011100607A1 (en) 2010-02-11 2011-02-11 Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction

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Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2751176A1 (en) 2009-01-28 2010-08-05 Vanderbilt University Substituted 1,1,3,3-tetraoxidobenzo[d][1,3,2]dithiazoles as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US8759377B2 (en) 2009-11-23 2014-06-24 Vanderbilt University Substituted dioxopiperidines and dioxopyrrolidines as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
BR112012020273A8 (pt) * 2010-02-11 2017-12-26 Univ Vanderbilt compostos de pirazolopiridina, pirazolopirazina, pirazolopirimidina, pirazolotiofeno e pirazolotiazol como pontencializadores alostéricos de mglur4, composições e métodos de tratamento de disfunção neurológica
AU2012310168B2 (en) 2011-09-15 2015-07-16 Novartis Ag 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase
WO2013060029A1 (en) * 2011-10-28 2013-05-02 Merck Sharp & Dohme Corp Allosteric modulators of metabotropic glutamate receptors
EP2791108B1 (en) 2011-12-15 2016-07-27 Pfizer Limited Sulfonamide derivatives
WO2013192346A1 (en) 2012-06-20 2013-12-27 Vanderbilt University Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mglur5 receptors
JP6402115B2 (ja) * 2013-02-04 2018-10-10 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 神経学的疾患および状態の処置に有用なスピロ−キナゾリノン誘導体
BR112015027440B1 (pt) * 2013-05-10 2023-04-11 Jiangsu Hansoh Pharmaceutical Co., Ltd Derivado de [1,2,4]triazol[4,3-a]piridina, seus usos e seu processo de preparação, e composição farmacêutica
MX363708B (es) 2013-10-14 2019-03-29 Eisai R&D Man Co Ltd Compuestos de quinolina selectivamente sustituidos.
SG10201704327RA (en) 2013-10-14 2017-06-29 Eisai R&D Man Co Ltd Selectively substituted quinoline compounds
EP3134404A1 (en) * 2014-04-25 2017-03-01 Pfizer Inc. Heteroaromatic compounds and their use as dopamine d1 ligands
US9980945B2 (en) 2015-01-13 2018-05-29 Vanderbilt University Benzoisoxazole-substituted compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US10221172B2 (en) 2015-01-13 2019-03-05 Vanderbilt University Benzothiazole and benzisothiazole-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US10526323B2 (en) 2015-01-30 2020-01-07 Vanderbilt University Indazole and azaindazole substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US10227343B2 (en) 2015-01-30 2019-03-12 Vanderbilt University Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US10221175B2 (en) 2015-04-24 2019-03-05 Vanderbilt University Substituted pyrrolo[3,4-e]indolizines, imidazo[1,2-a]pyrrolo[3,4-e]pyridines, pyrrolo[3,4-e][1,2,4]triazolo[1,5-a]pyridines and pyrrolo[3,4-e][1,2,4]triazolo[4,3-a]pyridines as positive allosteric modulators of muscarinic acetylcholine receptor M1
WO2016176460A1 (en) 2015-04-29 2016-11-03 Janssen Pharmaceutica Nv Azabenzimidazoles and their use as ampa receptor modulators
WO2016179351A1 (en) 2015-05-05 2016-11-10 Northwestern University Treatment of levodopa-induced dyskinesias
US10710997B2 (en) 2016-09-01 2020-07-14 Vanderbilt University Isoquinoline amide and isoquinoline amide-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US10294222B2 (en) 2016-09-01 2019-05-21 Vanderbilt University Benzomorpholine and benzomorpholine-substituted compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
WO2018080918A1 (en) * 2016-10-26 2018-05-03 Janssen Pharmaceutica Nv 3-aryl-2h-pyrazolo[4,3-b]pyridine compounds and their use as ampa receptor modulators
US11008335B2 (en) * 2016-11-07 2021-05-18 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor M4
US10968227B2 (en) 2016-11-08 2021-04-06 Vanderbilt University Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
WO2018089544A1 (en) 2016-11-08 2018-05-17 Vanderbilt University Isoquinoline amine compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US11319304B2 (en) 2017-06-28 2022-05-03 Vanderbilt University Pyridine quinoline compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
EA202090467A1 (ru) 2017-08-16 2020-06-18 Вандербилт Юниверсити ИНДАЗОЛОВЫЕ СОЕДИНЕНИЯ КАК АЛЛОСТЕРИЧЕСКИЕ ПОТЕНЦИАТОРЫ mGLuR4, КОМПОЗИЦИИ И СПОСОБЫ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ ДИСФУНКЦИЙ
US20220089609A1 (en) 2018-07-26 2022-03-24 Domain Therapeutics Substituted quinazolinone derivatives and their use as positive allosteric modulators of mglur4
CN111620874B (zh) * 2019-02-28 2022-11-15 汇瀚医疗科技有限公司 取代5,6-双杂环氨基化合物作为wnt信号通路抑制剂及其治疗应用
CN115605483A (zh) * 2020-07-06 2023-01-13 莫尔根生物有限公司（Kr） 三环双内酯化合物、其生产方法及用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1810463A1 (de) * 1967-11-24 1970-10-29 Eastman Kodak Co 1H-Pyrazolo-[3,2-c]-s-triazole
WO2005019171A1 (en) * 2003-08-18 2005-03-03 Astrazeneca Ab Substituted indole derivatives for pharmaceutical composition for treating respiratory diseases
WO2005054232A1 (en) * 2003-11-26 2005-06-16 Astrazeneca Ab 1-acetic acid-indole, -indazole and-benzimidazole derivatives usful for the treatment of respiratory disorders
WO2008089307A2 (en) * 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer
US20080200458A1 (en) * 2007-01-18 2008-08-21 Joseph Barbosa Methods and compositions for the treatment of body composition disorders
WO2009018415A1 (en) * 2007-07-31 2009-02-05 Vertex Pharmaceuticals Incorporated Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6638926B2 (en) * 2000-09-15 2003-10-28 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7368285B2 (en) 2001-03-07 2008-05-06 Senomyx, Inc. Heteromeric umami T1R1/T1R3 taste receptors and isolated cells that express same
US7160913B2 (en) * 2002-09-13 2007-01-09 Thomas Jefferson University Methods and kit for treating Parkinson's disease
WO2005007096A2 (en) * 2003-07-11 2005-01-27 Merck & Co., Inc. Treatment of movement disorders with a metabotropic glutamate 4 receptor positive allosteric modulator
DK2395004T3 (en) 2005-06-22 2016-03-21 Plexxikon Inc Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
BR112012020273A8 (pt) * 2010-02-11 2017-12-26 Univ Vanderbilt compostos de pirazolopiridina, pirazolopirazina, pirazolopirimidina, pirazolotiofeno e pirazolotiazol como pontencializadores alostéricos de mglur4, composições e métodos de tratamento de disfunção neurológica

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1810463A1 (de) * 1967-11-24 1970-10-29 Eastman Kodak Co 1H-Pyrazolo-[3,2-c]-s-triazole
WO2005019171A1 (en) * 2003-08-18 2005-03-03 Astrazeneca Ab Substituted indole derivatives for pharmaceutical composition for treating respiratory diseases
WO2005054232A1 (en) * 2003-11-26 2005-06-16 Astrazeneca Ab 1-acetic acid-indole, -indazole and-benzimidazole derivatives usful for the treatment of respiratory disorders
WO2008089307A2 (en) * 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer
US20080200458A1 (en) * 2007-01-18 2008-08-21 Joseph Barbosa Methods and compositions for the treatment of body composition disorders
WO2009018415A1 (en) * 2007-07-31 2009-02-05 Vertex Pharmaceuticals Incorporated Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof

Non-Patent Citations (13)

* Cited by examiner, † Cited by third party
Title
Bernotas, R. et al., Bioorganic & Medicinal Chemistry Letters, 2009, Vol. 19, pages 6935-6938 *
Bruni, P. et al., Journal of Heterocyclic Chemistry, 1979, Vol. 16, pages 779-782 *
Burke, M. et al., Tetrahedron Letters, 2008, Vol. 49, pages 4579-4581 *
CAS Registry Number 717851-76-8; STN Entry Date 28 July 2004 *
Debenham, S. et al., Bioorganic & Medicinal Chemistry Letters, 2008, Vol. 18, pages 4798-4801 *
Eberson, L., Journal of Organic Chemistry, 1984, Vol. 49, No. 12, pages 2135-2139 *
Farfan, N. et al., Journal of Heterocyclic Chemistry, 1990, Vol. 27, pages 1745-1749 *
Ghattas, A.-B., Synthetic Communications, 2001, Vol. 31, No. 16, pages 2447-2456 *
Guo, Y.-J. et al., Advanced Synthesis & Catalysis, 2009, Vol. 351, pages 2615-2618 *
Jones, L. et al., Journal of Medicinal Chemistry, 2009, Vol. 52, pages 1219-1223 *
Lesuisse, D. et al., Bioorganic & Medicinal Chemistry Letters, 2010, Vol. 20, pages 2344-2349 *
Shen, H. et al., Bioorganic & Medicinal Chemistry Letters, 2009, Vol. 19, pages 5716-5721 *
Yadav, J. et al., Synthesis, 2009, No. 9, pages 1520-1524 *

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