PE20110205A1 - Derivados de n-bencensulfonamida-3,4-diamino-3-ciclobuteno-1,2-diona sustituidos como antagonistas del receptor de quimiocina cxcr2 - Google Patents

Derivados de n-bencensulfonamida-3,4-diamino-3-ciclobuteno-1,2-diona sustituidos como antagonistas del receptor de quimiocina cxcr2

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Publication number
PE20110205A1
PE20110205A1 PE2011000121A PE2011000121A PE20110205A1 PE 20110205 A1 PE20110205 A1 PE 20110205A1 PE 2011000121 A PE2011000121 A PE 2011000121A PE 2011000121 A PE2011000121 A PE 2011000121A PE 20110205 A1 PE20110205 A1 PE 20110205A1
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PE
Peru
Prior art keywords
amino
alkyl
sulfonamide
methyl
cxcr2
Prior art date
Application number
PE2011000121A
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English (en)
Inventor
Urs Baettig
Anne-Marie D'souza
Peter Hunt
Neil John Press
Simon James Watson
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Novartis Ag
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Publication date
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Publication of PE20110205A1 publication Critical patent/PE20110205A1/es

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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/52—Sulfur atoms
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/48—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups having nitrogen atoms of sulfonamide groups further bound to another hetero atom
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
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    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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
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    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen 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
    • C07D307/10—Heterocyclic compounds containing five-membered rings having one oxygen 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 with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
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    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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  • Chemical & Material Sciences (AREA)
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Furan Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE BENCEN-SULFONAMIDA DE FORMULA (I) DONDE R1 ES H, CARBOCICLICO(C3-C10), ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO CON HALOGENO, CN U OH, ENTRE OTROS; R2 ES CARBOCICLICO(C3-C10), ALQUILO(C1-C6), ALCOXILO(C1-C6) OPCIONALMENTE SUSTITUIDOS, ENTRE OTROS; R3 ES H, HALOGENO O CN; R4 ES H, ALQUILO(C1-C8), CICLOALQUILO(C3-C8), ENTRE OTROS; R5 ES ALQUILO(C1-C8), CICLOALQUILO(C3-C8), CICLOALQUENILO(C5-C8), ENTRE OTROS; X ES CR14 O N, EN DONDE R14 ES H O ALQUILO(C1-C6). SON COMPUESTOS PREFERIDOS: 6-CLORO-3-[3,4-DIOXO-2-((R)-1-FENIL-PROPIL-AMINO)-CICLOBUT-1-ENIL-AMINO]-2-HIDROXI-N-METOXI-N-METIL-BENCEN-SULFONAMIDA, 6-CLORO-2-HIDROXI-N-METOXI-N-METIL-3-{2-[(R)-1-(5-METIL-FURAN-2-IL)-PROPIL-AMINO]-3,4-DIOXO-CICLOBUT-1-ENIL-AMINO}-BENCEN-SULFONAMIDA, 6-CLORO-3-{3,4-DIOXO-2-[(S)-(TETRAHIDRO-TIOFEN-3-IL)-AMINO]-CICLOBUT-1-ENIL-AMINO}-2-HIDROXI-N-METOXI-N-METIL-BENCEN-SULFONAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE QUIMIOCINA CXCR2 SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD OBSTRUCTIVA CRONICA PULMONAR, ENFISEMA, CANCER DE OVARIO, FIBROSIS PULMONAR
PE2011000121A 2008-08-04 2009-08-03 Derivados de n-bencensulfonamida-3,4-diamino-3-ciclobuteno-1,2-diona sustituidos como antagonistas del receptor de quimiocina cxcr2 PE20110205A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08161765 2008-08-04
US16162709P 2009-03-19 2009-03-19

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PE20110205A1 true PE20110205A1 (es) 2011-04-07

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PE2011000121A PE20110205A1 (es) 2008-08-04 2009-08-03 Derivados de n-bencensulfonamida-3,4-diamino-3-ciclobuteno-1,2-diona sustituidos como antagonistas del receptor de quimiocina cxcr2

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US (5) US7989497B2 (es)
EP (1) EP2310359B1 (es)
JP (1) JP5303645B2 (es)
KR (1) KR101310503B1 (es)
CN (1) CN102171183B (es)
AR (1) AR075071A1 (es)
AU (1) AU2009279123B2 (es)
BR (1) BRPI0916995B8 (es)
CA (1) CA2732932C (es)
CO (1) CO6341623A2 (es)
CU (2) CU24038B1 (es)
DK (1) DK2310359T3 (es)
EA (1) EA020374B1 (es)
EC (1) ECSP11010804A (es)
ES (1) ES2458596T3 (es)
HK (1) HK1155151A1 (es)
HN (1) HN2011000341A (es)
HR (1) HRP20140350T1 (es)
IL (1) IL210836A (es)
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MA (1) MA32536B1 (es)
MX (1) MX2011001378A (es)
MY (1) MY155626A (es)
NZ (1) NZ590708A (es)
PE (1) PE20110205A1 (es)
PL (1) PL2310359T3 (es)
PT (1) PT2310359E (es)
RS (1) RS53264B (es)
SI (1) SI2310359T1 (es)
SV (1) SV2011003831A (es)
TW (1) TWI430791B (es)
UA (1) UA103198C2 (es)
UY (1) UY32025A (es)
WO (1) WO2010015613A1 (es)
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Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA103198C2 (en) 2008-08-04 2013-09-25 Новартис Аг Squaramide derivatives as cxcr2 antagonists
US8648118B2 (en) 2010-12-17 2014-02-11 Boehringer Ingelheim International Gmbh Bicyclic ring system substituted amide functionalised phenols as medicaments
US8648070B2 (en) * 2010-12-17 2014-02-11 Boehringer Ingelheim International Gmbh Bicyclic ring system substituted sulfonamide functionalised phenols as medicaments
BR112014004963A2 (pt) * 2011-09-02 2017-03-21 Novartis Ag sal de colina do composto anti-inflamatório ciclobutanodiona substituído
AU2016201916A1 (en) * 2011-09-02 2016-04-21 Novartis Ag Choline salt of an anti-inflammatory substituted cyclobutenedione compound
FR2981934B1 (fr) * 2011-10-28 2013-12-20 Galderma Res & Dev Nouveaux composes di-substitues de la diamino-3,4-cyclobutene-3-dione-1,2 utiles dans le traitement de pathologies mediees par des chimiokines.
FR2981935B1 (fr) * 2011-10-28 2015-08-07 Galderma Res & Dev Nouveaux composes di-substitues de la diamino-3,4-cyclobutene-3-dione-1,2 utiles dans le traitement de pathologies mediees par des chimiokines.
EP2764866A1 (en) 2013-02-07 2014-08-13 IP Gesellschaft für Management mbH Inhibitors of nedd8-activating enzyme
EP3011012B1 (en) 2013-06-18 2018-09-12 New York University Cellular factors involved in the cytotoxicity of staphylococcus aureus leukocidins: novel therapeutic targets
FR3030515B1 (fr) * 2014-12-23 2017-01-20 Galderma Res & Dev Nouveaux composes antagonistes des recepteurs cxcr1 et cxcr2 aux chimiokines, et leur utilisation dans le traitement de pathologies mediees par des chimiokines
TWI734715B (zh) 2015-11-19 2021-08-01 美商卡默森屈有限公司 趨化因子受體調節劑
TWI724056B (zh) 2015-11-19 2021-04-11 美商卡默森屈有限公司 Ｃｘｃｒ２抑制劑
US10660909B2 (en) 2016-11-17 2020-05-26 Syntrix Biosystems Inc. Method for treating cancer using chemokine antagonists
KR20200037857A (ko) * 2017-08-14 2020-04-09 알러간, 인코포레이티드 3,4-이치환된 3-시클로부텐-1,2-디온 및 그의 용도
BR112020008888A2 (pt) 2017-11-16 2020-10-20 Novartis Ag terapias de combinação
MA50424A (fr) 2018-01-08 2020-08-26 Chemocentryx Inc Méthodes de traitement du psoriasis pustuleux généralisé avec un antagoniste de ccr6 ou cxcr2
WO2019165315A1 (en) 2018-02-23 2019-08-29 Syntrix Biosystems Inc. Method for treating cancer using chemokine antagonists alone or in combination
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
AU2019344107B2 (en) 2018-09-21 2022-09-15 Pfizer Inc. N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamides useful as CCR6 inhibitors
WO2020128972A1 (en) 2018-12-20 2020-06-25 Novartis Ag Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
US20220144807A1 (en) 2019-02-15 2022-05-12 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
CN113329792A (zh) 2019-02-15 2021-08-31 诺华股份有限公司 取代的3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途
CN112759549B (zh) * 2019-11-05 2023-07-28 中国医学科学院药物研究所 3-取代氨基-4-((取代吡啶基)氨基)环丁-3-烯-1,2-二酮类化合物
CN112851635B (zh) * 2019-11-28 2022-09-16 中国医学科学院药物研究所 环状砜类化合物及其制备方法、用途和药物组合物
US20230056470A1 (en) 2019-12-20 2023-02-23 Novartis Ag Uses of anti-tgf-beta antibodies and checkpoint inhibitors for the treatment of proliferative diseases
WO2021260528A1 (en) 2020-06-23 2021-12-30 Novartis Ag Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
EP4188549A1 (en) 2020-08-03 2023-06-07 Novartis AG Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
TW202304979A (zh) 2021-04-07 2023-02-01 瑞士商諾華公司 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途
AR125874A1 (es) 2021-05-18 2023-08-23 Novartis Ag Terapias de combinación

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5354763A (en) * 1993-11-17 1994-10-11 American Home Products Corporation Substituted N-heteroaryl and N-aryl-1,2-diaminocyclobutene-3,4-diones
US6166050A (en) 1998-12-14 2000-12-26 American Home Products Corporation 3,4-diamino-3-cyclobutene-1,2-dione derivatives which inhibit leukocyte adhesion mediated by VLA-4
DE69928286T2 (de) * 1999-01-13 2006-07-13 Warner-Lambert Co. Llc Benzenesulfonamid-derivative und ihre verwendung als mek-inhibitoren
EP1351933B1 (en) * 2001-01-16 2006-11-22 SmithKline Beecham Corporation Il-8 receptor antagonists
WO2002079122A2 (en) 2001-03-30 2002-10-10 Smithkline Beecham Corporation Methods of synthesizing phenol-containing compounds
US20040106794A1 (en) 2001-04-16 2004-06-03 Schering Corporation 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
US7132445B2 (en) 2001-04-16 2006-11-07 Schering Corporation 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
SI1381590T1 (sl) 2001-04-16 2007-10-31 Schering Corp 3,4-disubstituirani ciklobuten-1,2-dioni kot ligandi CXC-kemokinskega receptorja
US20040053953A1 (en) 2002-03-18 2004-03-18 Schering Corporation Treatment of chemokine mediated diseases
AR047739A1 (es) 2004-01-30 2006-02-15 Schering Corp Polimorfos cristalinos de un ligando receptor de cxc-quimiocina
DE102005001053A1 (de) 2005-01-07 2006-07-20 Merck Patent Gmbh Quadratsäurederivate
JP2008530284A (ja) 2005-02-10 2008-08-07 ワッカー ケミー アクチエンゲゼルシャフト 保護されたイソシアネート基を有する粒子を含有する塗料
CN101203509B (zh) 2005-02-16 2013-05-08 默沙东公司 具有cxcr3拮抗剂活性的胺-连接的吡啶基和苯基取代的哌嗪-哌啶
DE102005035742A1 (de) 2005-07-29 2007-02-01 Merck Patent Gmbh Quadratsäurederivate II
WO2008005570A1 (en) 2006-07-07 2008-01-10 Schering Corporation 3,4-di-substituted cyclobutene-1,2-diones as cxc-chemokine receptor ligands
CA2695613A1 (en) * 2006-12-19 2008-06-26 Pharmos Corporation Sulfonamide derivatives with therapeutic indications
US8450348B2 (en) 2007-02-21 2013-05-28 Forma Tm, Llc Derivatives of squaric acid with anti-proliferative activity
ES2386489T3 (es) * 2007-06-06 2012-08-21 Novartis Ag Compuestos ciclobutanediona sustituidos anti-inflamatorios
CA2692269A1 (en) 2007-07-03 2009-01-08 Schering Corporation Process and intermediates for the synthesis of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds
US20100249439A1 (en) 2007-07-05 2010-09-30 Vincenzo Liotta Process for controlled crystal size in 1,2-substituted 3,4-dioxo-1-cyclobutene compounds
WO2009012375A2 (en) 2007-07-19 2009-01-22 Wyeth Squarate kinase inhibitors
EP2252327A2 (en) 2007-12-04 2010-11-24 Schering Corporation Methods of treating copd
TWI439462B (zh) 2007-12-10 2014-06-01 Novartis Ag 作為ｅｎａｃ阻抑劑之螺環胍化合物
UA103198C2 (en) * 2008-08-04 2013-09-25 Новартис Аг Squaramide derivatives as cxcr2 antagonists
WO2010063802A1 (en) 2008-12-05 2010-06-10 Novartis Ag 3, 4-di-substituted cyclobutene- 1, 2 -diones as cxcr2 receptor antagonists
WO2010091543A1 (en) 2009-02-10 2010-08-19 Merck Sharp & Dohme Corp. Novel hydrazino-cyclobut-3-ene-1, 2-dione derivatives as cxcr2 antagonists
BR112014004963A2 (pt) 2011-09-02 2017-03-21 Novartis Ag sal de colina do composto anti-inflamatório ciclobutanodiona substituído

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