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BR112012033241A2 - [1,8]naftiridinas substituídas por 2,4-diarila como inibidores de quinase para uso contra câncer - Google Patents

[1,8]naftiridinas substituídas por 2,4-diarila como inibidores de quinase para uso contra câncer

Info

Publication number
BR112012033241A2
BR112012033241A2 BR112012033241A BR112012033241A BR112012033241A2 BR 112012033241 A2 BR112012033241 A2 BR 112012033241A2 BR 112012033241 A BR112012033241 A BR 112012033241A BR 112012033241 A BR112012033241 A BR 112012033241A BR 112012033241 A2 BR112012033241 A2 BR 112012033241A2
Authority
BR
Brazil
Prior art keywords
kinase inhibitors
diaryl
substituted naphthyridines
compounds
treatment
Prior art date
Application number
BR112012033241A
Other languages
English (en)
Inventor
Alfred Jonczyk
Christiane Amendt
Dieter Dorsch
Frank Zenke
Guenter Hoelzemann
Original Assignee
Merck Patent Gmbh
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44487155&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112012033241(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of BR112012033241A2 publication Critical patent/BR112012033241A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • 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
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    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P35/04—Antineoplastic agents specific for metastasis
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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Abstract

[1,8]naftiridinas substituídas por 2,4-diarila como inibidores de quinase para uso contra câncer. a presente invenção refere-se a novos derivados de [1,8] naftiridina de fórmula (i) e ao uso de tais compostos em que a inibição, regulação e/ou modulação de transdução de sinal por proteínas consumidoras de atp como quinases desempenha um papel, particularmente para inibidores de quinases receptoras de tgf-beta, e ao uso de tais compostos para o tratamento de doenças induzidas por quinase, em particular para o tratamento de tumores.
BR112012033241A 2010-06-28 2011-05-31 [1,8]naftiridinas substituídas por 2,4-diarila como inibidores de quinase para uso contra câncer BR112012033241A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10006683 2010-06-28
PCT/EP2011/002692 WO2012000595A1 (en) 2010-06-28 2011-05-31 2,4- diaryl - substituted [1,8] naphthyridines as kinase inhibitors for use against cancer

Publications (1)

Publication Number Publication Date
BR112012033241A2 true BR112012033241A2 (pt) 2016-11-16

Family

ID=44487155

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012033241A BR112012033241A2 (pt) 2010-06-28 2011-05-31 [1,8]naftiridinas substituídas por 2,4-diarila como inibidores de quinase para uso contra câncer

Country Status (21)

Country Link
US (1) US8791113B2 (pt)
EP (1) EP2585461B1 (pt)
JP (1) JP5826261B2 (pt)
KR (1) KR20130038336A (pt)
CN (1) CN102958930B (pt)
AR (1) AR081994A1 (pt)
AU (1) AU2011273931B2 (pt)
BR (1) BR112012033241A2 (pt)
CA (1) CA2803665C (pt)
CL (1) CL2012003680A1 (pt)
CO (1) CO6612243A2 (pt)
EA (1) EA201300052A1 (pt)
EC (1) ECSP13012408A (pt)
ES (1) ES2792799T3 (pt)
IL (1) IL223496A (pt)
MX (1) MX2012014549A (pt)
NZ (1) NZ603456A (pt)
PE (1) PE20130376A1 (pt)
PH (1) PH12012502391A1 (pt)
SG (1) SG186855A1 (pt)
WO (1) WO2012000595A1 (pt)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8778398B2 (en) 2008-11-04 2014-07-15 Jazz Pharmaceuticals, Inc. Immediate release formulations and dosage forms of gamma-hydroxybutyrate
SG182803A1 (en) * 2010-02-05 2012-09-27 Merck Patent Gmbh Hetaryl-[1,8]naphthyridine derivatives
CA2794171C (en) 2010-03-24 2018-07-03 Jazz Pharmaceuticals, Inc. Controlled release dosage forms for high dose, water soluble and hygroscopic drug substances
DE102011009961A1 (de) * 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
AU2013323508B2 (en) * 2012-09-28 2017-11-02 Merck Sharp & Dohme Corp. Novel compounds that are ERK inhibitors
EP2900223B1 (en) * 2012-09-28 2017-10-25 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
JP6669499B2 (ja) 2013-02-15 2020-03-18 カラ ファーマシューティカルズ インコーポレイテッド 治療用化合物
CA2900680C (en) 2013-02-20 2021-08-10 Kala Pharmaceuticals, Inc. Quinoline and quinazoline compounds and uses thereof for treating and/or preventing diseases
US9688688B2 (en) 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
CN103113369A (zh) * 2013-03-21 2013-05-22 云南大学 一种具有抗肿瘤活性的苯并[b][1,8]-萘啶-2-(1H)-亚胺衍生物及合成方法
SG11201602996RA (en) 2013-10-18 2016-05-30 Celgene Quanticel Res Inc Bromodomain inhibitors
CN106061261B (zh) 2013-11-01 2018-04-24 卡拉制药公司 治疗化合物的结晶形式及其用途
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
KR102373700B1 (ko) 2014-04-02 2022-03-11 인터뮨, 인크. 항섬유성 피리디논
CN104086543A (zh) * 2014-06-19 2014-10-08 湖南华腾制药有限公司 一种制备4-氯-1,8-二氮萘的方法
US10398662B1 (en) 2015-02-18 2019-09-03 Jazz Pharma Ireland Limited GHB formulation and method for its manufacture
CN111689963A (zh) * 2015-04-02 2020-09-22 默克专利股份公司 咪唑酮基喹啉和其作为atm激酶抑制剂的用途
AR104259A1 (es) 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
WO2017184462A1 (en) 2016-04-18 2017-10-26 Celgene Quanticel Research, Inc. Therapeutic compounds
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
UY37341A (es) 2016-07-22 2017-11-30 Flamel Ireland Ltd Formulaciones de gamma-hidroxibutirato de liberación modificada con farmacocinética mejorada
US11986451B1 (en) 2016-07-22 2024-05-21 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
US11504347B1 (en) 2016-07-22 2022-11-22 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
US11602512B1 (en) 2016-07-22 2023-03-14 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
US11602513B1 (en) 2016-07-22 2023-03-14 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
US12186296B1 (en) 2016-07-22 2025-01-07 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
RU2729999C1 (ru) * 2016-07-29 2020-08-13 Шанхай Инли Фармасьютикал Ко., Лтд Азотсодержащее гетероциклическое ароматическое соединение, способ его получения, фармацевтическая композиция на его основе и его применение
WO2018048746A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
EP3509422A4 (en) 2016-09-08 2020-05-20 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
AU2017324716B2 (en) 2016-09-08 2020-08-13 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
CN108779115B (zh) 2016-10-14 2021-02-26 江苏恒瑞医药股份有限公司 五元杂芳环并桥环类衍生物、其制备方法及其在医药上的应用
JP2020500177A (ja) 2016-11-14 2020-01-09 ジエンス ヘンルイ メデイシンカンパニー リミテッドＪｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．，Ｌｔｄ． ３，４−ビピリジルピラゾール誘導体、およびその製造方法およびその医療応用
CN106810550A (zh) * 2017-01-10 2017-06-09 湖南华腾制药有限公司 一种萘啶衍生物的制备方法
US20180263936A1 (en) 2017-03-17 2018-09-20 Jazz Pharmaceuticals Ireland Limited Gamma-hydroxybutyrate compositions and their use for the treatment of disorders
CN109983015B (zh) * 2017-03-22 2021-09-03 江苏恒瑞医药股份有限公司 6-吡唑-[1,2,4]三唑并[4,3-a]吡啶-3-酰胺类衍生物、其制备方法及其在医药上的应用
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
CN111868237A (zh) 2017-10-05 2020-10-30 弗尔康医疗公司 P38抑制剂降低dux4表达的用途
US11400052B2 (en) 2018-11-19 2022-08-02 Jazz Pharmaceuticals Ireland Limited Alcohol-resistant drug formulations
EP3930702A1 (en) 2019-03-01 2022-01-05 Flamel Ireland Limited Gamma-hydroxybutyrate compositions having improved pharmacokinetics in the fed state
EP3959197A4 (en) * 2019-04-24 2022-10-12 Children's Medical Center Corporation PAPD5 INHIBITORS AND METHODS OF USE THEREOF
AU2021205893A1 (en) 2020-01-08 2022-06-23 Synthis Therapeutics, Inc. ALK5 inhibitor conjugates and uses thereof
US11618751B1 (en) 2022-03-25 2023-04-04 Ventus Therapeutics U.S., Inc. Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives
TW202139986A (zh) 2020-02-21 2021-11-01 愛爾蘭商爵士製藥愛爾蘭有限責任公司 治療原發性嗜睡症之方法
KR20220159386A (ko) * 2020-02-28 2022-12-02 레믹스 테라퓨틱스 인크. 스플라이싱을 조절하기 위한 화합물 및 방법
CN112608327B (zh) * 2021-01-28 2021-11-02 河南大学 呋喃并喹啉衍生物、其制备方法及应用
US11319319B1 (en) 2021-04-07 2022-05-03 Ventus Therapeutics U.S., Inc. Compounds for inhibiting NLRP3 and uses thereof
CN114836384A (zh) * 2022-01-26 2022-08-02 安徽理工大学环境友好材料与职业健康研究院(芜湖) 一种三氯乙烯诱导人源肝细胞恶性转化的方法及其应用
US11583510B1 (en) 2022-02-07 2023-02-21 Flamel Ireland Limited Methods of administering gamma hydroxybutyrate formulations after a high-fat meal
US11779557B1 (en) 2022-02-07 2023-10-10 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
US12331048B2 (en) 2022-10-31 2025-06-17 Ventus Therapeutics U.S., Inc. Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 inhibitors
WO2024258967A1 (en) 2023-06-13 2024-12-19 Synthis Therapeutics, Inc. Anti-cd5 antibodies and their uses

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
EP1165555B1 (en) 1999-03-11 2003-07-16 Neurogen Corporation Aryl fused 2,4-disubstituted pyridines: nk3 receptor ligands
WO2000061186A1 (en) 1999-04-08 2000-10-19 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
WO2001095196A1 (en) 2000-04-07 2001-12-13 Hong Dong Pyo Lottery type selling method and apparatus using computer network
AU2003229305A1 (en) 2002-05-17 2003-12-02 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-Beta INHIBITORS
WO2004010929A2 (en) 2002-07-25 2004-02-05 Scios, Inc. METHODS FOR IMPROVEMENT OF LUNG FUNCTION USING TGF-β INHIBITORS
EP1603908B1 (en) 2003-03-12 2008-06-11 Millennium Pharmaceuticals, Inc. Quinazoline derivatives as tgf-beta inhibitors
EP1708712A1 (en) 2003-12-24 2006-10-11 Scios, Inc. Treatment of malignant gliomas with tgf-beta inhibitors
EP1724268A4 (en) 2004-02-20 2010-04-21 Kirin Pharma Kk COMPOUNDS WITH TGF-BETA-HEMMENDER EFFECT AND PHARMACEUTICAL COMPOSITION CONTAINING THEM
US7511056B2 (en) 2004-11-10 2009-03-31 Eli Lilly And Company TGF-β inhibitors
JP4865258B2 (ja) 2005-06-21 2012-02-01 キヤノン株式会社 １，８−ナフチリジン化合物及びそれを用いた有機発光素子
US8410109B2 (en) 2005-07-29 2013-04-02 Resverlogix Corp. Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices
US20100093738A1 (en) * 2006-10-06 2010-04-15 Basf Se Fungicidal Compounds and Fungicidal Compositions
JP4751856B2 (ja) 2007-07-03 2011-08-17 本田技研工業株式会社 車体側部構造
CA2727103A1 (en) * 2008-07-03 2010-01-07 Merck Patent Gmbh Naphthyridinones as aurora kinase inhibitors
WO2010033906A2 (en) 2008-09-19 2010-03-25 President And Fellows Of Harvard College Efficient induction of pluripotent stem cells using small molecule compounds
SG182803A1 (en) * 2010-02-05 2012-09-27 Merck Patent Gmbh Hetaryl-[1,8]naphthyridine derivatives
EP2539336B1 (en) * 2010-02-22 2014-10-22 Merck Patent GmbH Hetarylaminonaphthyridines
DE102011009961A1 (de) * 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate

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