CA2758474A1 - Novel p2x7r antagonists and their use - Google Patents

Novel p2x7r antagonists and their use Download PDF

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Publication number
CA2758474A1
CA2758474A1 CA2758474A CA2758474A CA2758474A1 CA 2758474 A1 CA2758474 A1 CA 2758474A1 CA 2758474 A CA2758474 A CA 2758474A CA 2758474 A CA2758474 A CA 2758474A CA 2758474 A1 CA2758474 A1 CA 2758474A1
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Canada
Prior art keywords
indol
bromo
chloro
hydroxypropyl
cycloheptylacetamide
Prior art date
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Abandoned
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CA2758474A
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English (en)
French (fr)
Inventor
Michael Boes
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Affectis Pharmaceuticals AG
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Affectis Pharmaceuticals AG
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Filing date
Publication date
Application filed by Affectis Pharmaceuticals AG filed Critical Affectis Pharmaceuticals AG
Publication of CA2758474A1 publication Critical patent/CA2758474A1/en
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/40—Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • 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
    • A61K31/4353—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
    • 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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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A—HUMAN NECESSITIES
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
CA2758474A 2009-04-14 2010-03-11 Novel p2x7r antagonists and their use Abandoned CA2758474A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09005324.0 2009-04-14
EP09005324 2009-04-14
PCT/EP2010/053097 WO2010118921A1 (en) 2009-04-14 2010-03-11 Novel p2x7r antagonists and their use

Publications (1)

Publication Number Publication Date
CA2758474A1 true CA2758474A1 (en) 2010-10-21

Family

ID=42167925

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2758474A Abandoned CA2758474A1 (en) 2009-04-14 2010-03-11 Novel p2x7r antagonists and their use

Country Status (23)

Country Link
US (2) US7919503B2 (enExample)
EP (1) EP2243772B1 (enExample)
JP (1) JP2012523440A (enExample)
KR (1) KR20120006547A (enExample)
CN (1) CN102395562A (enExample)
AT (1) ATE541832T1 (enExample)
AU (1) AU2010237302A1 (enExample)
BR (1) BRPI1014902A2 (enExample)
CA (1) CA2758474A1 (enExample)
CY (1) CY1112758T1 (enExample)
DK (1) DK2243772T3 (enExample)
EA (1) EA201101479A1 (enExample)
ES (1) ES2380908T3 (enExample)
HR (1) HRP20120271T1 (enExample)
IL (1) IL215444A0 (enExample)
MX (1) MX2011010810A (enExample)
PL (1) PL2243772T3 (enExample)
PT (1) PT2243772E (enExample)
SG (1) SG175232A1 (enExample)
SI (1) SI2243772T1 (enExample)
SM (1) SMT201200017B (enExample)
WO (1) WO2010118921A1 (enExample)
ZA (1) ZA201108305B (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8815892B2 (en) 2008-03-25 2014-08-26 Affectis Pharmaceuticals Ag P2X7R antagonists and their use
NZ587799A (en) * 2008-03-25 2012-06-29 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
MX2012013075A (es) * 2010-05-14 2012-12-17 Affectis Pharmaceuticals Ag Metodos novedosos para preparacion de antagonistas p2x7r.
WO2012110190A1 (en) 2011-02-17 2012-08-23 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
EP2701719A4 (en) * 2011-04-28 2015-04-22 Claire Mitchell METHOD FOR TREATING MACULAR OBGENATION BY MODULATION OF P2Y12 OR P2X7 RECEPTORS
WO2012163792A1 (en) 2011-05-27 2012-12-06 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
WO2012163456A1 (en) 2011-05-27 2012-12-06 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
RU2014106611A (ru) * 2011-07-22 2015-08-27 Актелион Фармасьютиклз Лтд Производные гетероциклических амидов в качестве антагонистов р2х7 рецептора
WO2013082565A1 (en) * 2011-12-02 2013-06-06 Michael Kaleko Therapies for disorders of the cornea and conjunctiva
NZ628910A (en) * 2012-01-20 2016-02-26 Actelion Pharmaceuticals Ltd Heterocyclic amide derivatives as p2x7 receptor antagonists
PL2931717T3 (pl) 2012-12-12 2017-05-31 Actelion Pharmaceuticals Ltd. Pochodne indolokarboksyamidu jako antagoniści receptora p2x7
AR094053A1 (es) 2012-12-18 2015-07-08 Actelion Pharmaceuticals Ltd Derivados de indol carboxamida como antagonistas del receptor p2x₇
EP2956457B1 (en) 2013-01-22 2016-11-23 Actelion Pharmaceuticals Ltd Heterocyclic amide derivatives as p2x7 receptor antagonists
ES2616114T3 (es) 2013-01-22 2017-06-09 Actelion Pharmaceuticals Ltd. Derivados de amida heterocíclica como antagonistas del receptor P2X7
WO2014182601A1 (en) 2013-05-08 2014-11-13 Children's Medical Center Corporation A method of preventing and treating type 1 diabetes, allograft rejection and lung fibrosis (by targeting the atp/p2x7r axis)
TW202043198A (zh) * 2019-01-17 2020-12-01 美商Ｉｆｍ Ｄｕｅ有限公司 用於治療與sting活性相關之病況的化合物及組合物

Family Cites Families (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3705175A (en) * 1969-04-01 1972-12-05 Egyt Gyogyszervegyeszeti Gyar Indazole-3-carboxylic amides
ZA981532B (en) 1997-02-26 1999-08-24 Glaxo Group Ltd Reverse hydroxamate derivatives as matrix metalloprotease inhibitors, metalloprotease inhibitors, and TNF alpha inhibitors.
ZA988967B (en) 1997-10-03 2000-04-03 Du Pont Pharm Co Lactam metalloprotease inhibitors.
SE9704544D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
SE9704546D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
SE9704545D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
EP1087937A1 (en) 1998-06-17 2001-04-04 Du Pont Pharmaceuticals Company Cyclic hydroxamic acids as metalloproteinase inhibitors
US6239151B1 (en) 1998-06-26 2001-05-29 Hoffmann-La Roche Inc. Compounds as inhibitor of tumor necrosis factor alpha release
UA59453C2 (uk) 1998-08-12 2003-09-15 Пфайзер Продактс Інк. Похідні гідроксипіпеколат гідроксамової кислоти як інгібітори матричних металопротеїназ
US20040122011A1 (en) 1998-12-23 2004-06-24 Pharmacia Corporation Method of using a COX-2 inhibitor and a TACE inhibitors as a combination therapy
US6225311B1 (en) 1999-01-27 2001-05-01 American Cyanamid Company Acetylenic α-amino acid-based sulfonamide hydroxamic acid tace inhibitors
WO2000061569A1 (en) 1999-04-09 2000-10-19 Astrazeneca Ab Adamantane derivatives
SE9901875D0 (sv) 1999-05-25 1999-05-25 Astra Pharma Prod Novel compounds
SE9904505D0 (sv) 1999-12-09 1999-12-09 Astra Pharma Prod Novel compounds
TWI258462B (en) 1999-12-17 2006-07-21 Astrazeneca Ab Adamantane derivative compounds, process for preparing the same and pharmaceutical composition comprising the same
SE9904652D0 (sv) 1999-12-17 1999-12-17 Astra Pharma Prod Novel Compounds
SE9904738D0 (sv) 1999-12-22 1999-12-22 Astra Pharma Prod Novel compounds
GB0013737D0 (en) 2000-06-07 2000-07-26 Astrazeneca Ab Novel compounds
US20040029928A1 (en) 2000-08-31 2004-02-12 Terukage Hirata Novel propenohydroxamic acid derivatives
CA2447475A1 (en) 2001-05-25 2002-12-05 Chu-Biao Xue Hydantion derivatives as inhibitors of matrix metalloproteinases
WO2003016248A2 (en) 2001-08-17 2003-02-27 Bristol-Myers Squibb Company Patent Department Bicyclic hydroxamates as inhibitors of matrix metalloproteinases and/or tnf-$g(a) converting enzyme (tace)
US6740649B2 (en) 2001-09-17 2004-05-25 Bristol-Myers Squibb Company Cyclic hydroxamic acids as inhibitors of matrix metalloproteinases and/or TNF- α converting enzyme (TACE)
WO2003031431A1 (en) 2001-10-09 2003-04-17 Bristol-Myers Squibb Company Cyclic sulfone derivatives as inhibitors of matrix metalloproteinases and/or tnf-$g(a) converting enzyme (tace)
US6884806B2 (en) 2001-10-17 2005-04-26 Bristol-Myers Squibb Company Bicyclic lactam derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
WO2003040103A1 (en) 2001-11-02 2003-05-15 Bristol-Myers Squibb Company β-SULFONE DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEINASES AND/OR TNF-α CONVERTING ENZYME (TACE)
WO2003042190A1 (en) 2001-11-12 2003-05-22 Pfizer Products Inc. N-alkyl-adamantyl derivatives as p2x7-receptor antagonists
PA8557501A1 (es) 2001-11-12 2003-06-30 Pfizer Prod Inc Benzamida, heteroarilamida y amidas inversas
SE0103836D0 (sv) 2001-11-16 2001-11-16 Astrazeneca Ab Novel compounds
AU2002359524A1 (en) 2001-11-30 2003-06-17 The Government Of The United States Of America, Represented By The Secretary, Department Of Health A P2x7 receptor antagonists
AU2002357312A1 (en) 2001-12-20 2003-07-09 Bristol-Myers Squibb Company Barbituric acid derivatives as inhibitors of tnf-alpha converting enzyme (tace) and/or matrix metalloproteinases
WO2003059353A1 (en) 2001-12-21 2003-07-24 King Pharmaceuticals Research And Development, Inc. Tyrosyl derivatives and their use as p2x7 receptor modulators
WO2003079986A2 (en) 2002-03-18 2003-10-02 Bristol-Myers Squibb Company Uracil derivatives as inhibitors of tnf-alpha converting enzyme (tace) and matrix metalloproteinases
SE0200920D0 (sv) 2002-03-25 2002-03-25 Astrazeneca Ab Novel compounds
GB0216379D0 (en) 2002-07-13 2002-08-21 Astrazeneca Ab Compounds
WO2004012663A2 (en) 2002-08-01 2004-02-12 Bristol-Myers Squibb Company Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme
US7041693B2 (en) 2002-10-04 2006-05-09 Bristol-Myers Squibb Company Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
EP1558581A4 (en) 2002-10-07 2007-07-25 Bristol Myers Squibb Co DERIVATIVES OF TRIAZOLONE AND TRIAZOLETHIONE
WO2004043349A2 (en) 2002-11-06 2004-05-27 Bristol-Myers Squibb Company Isoxazoline derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme
PA8591801A1 (es) 2002-12-31 2004-07-26 Pfizer Prod Inc Inhibidores benzamidicos del receptor p2x7.
EP1581507A1 (en) 2002-12-31 2005-10-05 Pfizer Products Inc. Benzamide inhibitors of the p2x7 receptor
ITMI20030287A1 (it) * 2003-02-18 2004-08-19 Acraf Indazolammidi dotate di attivita' analgesica metodo, per
SE0300480D0 (sv) 2003-02-21 2003-02-21 Astrazeneca Ab Novel compounds
ATE355273T1 (de) 2003-05-12 2006-03-15 Pfizer Prod Inc Benzamidinhibitoren des p2x7-rezeptors
GB0312609D0 (en) 2003-06-02 2003-07-09 Astrazeneca Ab Novel compounds
US7132432B2 (en) 2003-06-05 2006-11-07 Bristol-Myers Squibb Company Hydantoin derivatives as inhibitors of tumor necrosis factor-alpha converting enzyme (TACE)
CA2528626A1 (en) * 2003-07-09 2005-01-20 Biolipox Ab Indoles useful in the treatment of inflammation
SE0302035D0 (sv) * 2003-07-09 2003-07-09 Biolipox Ab New compound
GB0324498D0 (en) 2003-07-21 2003-11-26 Aventis Pharma Inc Heterocyclic compounds as P2X7 ion channel blockers
SE0302139D0 (sv) 2003-07-28 2003-07-28 Astrazeneca Ab Novel compounds
SE0302192D0 (sv) 2003-08-08 2003-08-08 Astrazeneca Ab Novel compounds
WO2005019182A1 (en) 2003-08-20 2005-03-03 Bayer Healthcare Ag Pyrazolylmethylbenzamide derivatives as p2xt-receptor antagonists
US7749980B2 (en) 2003-10-21 2010-07-06 Inspire Pharmaceuticals, Inc. Non-nucleotide compositions and method for treating pain
MXPA06012595A (es) 2004-04-29 2007-05-09 Abbott Lab Analogos de amino-tetrazoles y metodos de uso.
BRPI0512651A (pt) 2004-06-29 2008-03-25 Pfizer Prod Inc método para a preparação de derivados de 5-4-(2-hidroxietil)-3,5-dioxo-4,5 dihidro-3h-1,2,4-trizin-2-ila com atividade inibidora de p2x7 por reaçaõ do derivado não substituìdo na posição 4 da trizina com um oxirano na presença de um ácido de lewis
RU2006146675A (ru) 2004-06-29 2008-07-10 Пфайзер Продактс Инк. (Us) Способ получения производных 5-[4-(2-гидроксипропил)-3,5-диоксо-4,5-дигидро-3н-[1,2,4] триазин-2-ил] бензамида снятием защиты с промежуточных продуктов, содержащих защищенный гидроксил
US7241776B2 (en) 2004-08-02 2007-07-10 Abbott Laboratories Cyanoamidine P2X7 antagonists for the treatment of pain
SA05260265A (ar) 2004-08-30 2005-12-03 استرازينيكا ايه بي مركبات جديدة
SE0402925D0 (sv) 2004-11-30 2004-11-30 Astrazeneca Ab Novel Compounds
AU2005317868B2 (en) 2004-12-24 2009-06-04 Astrazeneca Ab Amide derivatives
WO2006080884A1 (en) 2005-01-27 2006-08-03 Astrazeneca Ab Novel biaromatic compounds, inhibitors of the p2x7-receptor
US20060211739A1 (en) 2005-02-08 2006-09-21 Arturo Perez-Medrano Use of selective P2X7 receptor antagonists
US7297700B2 (en) 2005-03-24 2007-11-20 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
WO2006110516A1 (en) 2005-04-11 2006-10-19 Abbott Laboratories Acylhydrazide p2x7 antagonists and uses thereof
WO2006136004A1 (en) 2005-05-05 2006-12-28 Medicure International Inc. Inhibition of atp-mediated, p2x7 dependent pathways by pyridoxal-5-phosphaste and vitamin b6 related compounds
WO2007016597A2 (en) 2005-07-29 2007-02-08 The Regents Of The University Of California Targeting tnf-alpha converting enzyme (tace)-dependent growth factor shedding in cancer therapy
US20090124555A1 (en) 2005-08-29 2009-05-14 Irma Bernatchez-Lemaire Use of histogranin and histogranin-like compounds as inhibitors of p2x7 receptor function and as anti-arthritic agents
US20100022531A1 (en) 2005-09-01 2010-01-28 Renovis, Inc. Novel compounds as p2x7 modulators and uses thereof
WO2007056046A1 (en) 2005-11-07 2007-05-18 Abbott Laboratories P2x7 receptor antagonists and methods of use
EP1963275A2 (en) 2005-11-09 2008-09-03 Abbott Laboratories P2x7 receptor antagonists and uses thereof
WO2007109182A2 (en) 2006-03-16 2007-09-27 Renovis, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
US20100184802A1 (en) 2006-03-16 2010-07-22 Kelly Michael G Bicycloheteroaryl Compounds as P2X7 Modulators and Uses Thereof
WO2007109154A2 (en) 2006-03-16 2007-09-27 Renovis, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
TWI464148B (zh) 2006-03-16 2014-12-11 Evotec Us Inc 作為ｐ２ｘ7調節劑之雙環雜芳基化合物與其用途
EP2001474B1 (en) 2006-03-16 2016-03-09 Second Genome, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
WO2007109160A2 (en) 2006-03-16 2007-09-27 Renovis, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
EP2040700B1 (en) 2006-06-06 2010-11-24 Glaxo Group Limited N- (phenylmethyl) -2- (1h-pyraz0l-4-yl) acetamide derivatives as p2x7 antagonists for the treatment of pain, inflammation and neurodegeneration
GB0611154D0 (en) 2006-06-06 2006-07-19 Glaxo Group Ltd Novel receptor antagonists and their methods of use
WO2008005368A2 (en) 2006-06-30 2008-01-10 Abbott Laboratories Piperazines as p2x7 antagonists
SI2049478T1 (sl) 2006-07-06 2012-08-31 Glaxo Group Ltd Substituirani N-fenilmetil-5-okso-prolin-2-amidi kot antagonisti receptorja P2X7 in postopki za njihovo uporabo
BRPI0812594A2 (pt) * 2007-08-10 2015-06-23 Lundbeck & Co As H Composto ou sal ou hidrato do mesmo, composição farmacêutica, métodos para modulação da atividade de um receptor p2x7, para tratamento de uma condição responsiva á modulação do receptor p2x7 em um paciente, para inibição de morte de células gangliônicas retinais em um paciente, para determinação da presença ou ausência de receptor p2x7 em uma amostra, preparação farmacêutica acondicionada, e, uso de um composto ou sal ou hidrato do mesmo.
NZ587799A (en) * 2008-03-25 2012-06-29 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use

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US20100267762A1 (en) 2010-10-21
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US20110212992A1 (en) 2011-09-01
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US7919503B2 (en) 2011-04-05
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HRP20120271T1 (hr) 2012-04-30
PT2243772E (pt) 2012-03-28
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