ES2600161T3 - Compuestos para uso en el tratamiento de enfermedades mediadas por linfocitos T - Google Patents

Compuestos para uso en el tratamiento de enfermedades mediadas por linfocitos T Download PDF

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Publication number
ES2600161T3
ES2600161T3 ES12845460.0T ES12845460T ES2600161T3 ES 2600161 T3 ES2600161 T3 ES 2600161T3 ES 12845460 T ES12845460 T ES 12845460T ES 2600161 T3 ES2600161 T3 ES 2600161T3
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Prior art keywords
methyl
oxo
pyridinyl
indole
carboxamide
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ES12845460.0T
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English (en)
Spanish (es)
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Anna K. BASSIL
Soren BEINKE
Rabinder Kumar Prinjha
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GlaxoSmithKline Intellectual Property No 2 Ltd
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GlaxoSmithKline Intellectual Property No 2 Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
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    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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    • A—HUMAN NECESSITIES
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    • 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
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/1003—Transferases (2.) transferring one-carbon groups (2.1)
    • C12N9/1007—Methyltransferases (general) (2.1.1.)
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
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    • A61K31/33—Heterocyclic compounds
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Microbiology (AREA)
  • Biochemistry (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Otolaryngology (AREA)
ES12845460.0T 2011-11-04 2012-11-02 Compuestos para uso en el tratamiento de enfermedades mediadas por linfocitos T Active ES2600161T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161555650P 2011-11-04 2011-11-04
US201161555650P 2011-11-04
PCT/US2012/063235 WO2013067296A1 (en) 2011-11-04 2012-11-02 Method of treatment

Publications (1)

Publication Number Publication Date
ES2600161T3 true ES2600161T3 (es) 2017-02-07

Family

ID=48192800

Family Applications (1)

Application Number Title Priority Date Filing Date
ES12845460.0T Active ES2600161T3 (es) 2011-11-04 2012-11-02 Compuestos para uso en el tratamiento de enfermedades mediadas por linfocitos T

Country Status (11)

Country Link
US (2) US9242962B2 (enExample)
EP (1) EP2773754B1 (enExample)
JP (1) JP6005753B2 (enExample)
KR (1) KR20140095073A (enExample)
CN (1) CN104039956A (enExample)
AU (1) AU2012332297B2 (enExample)
BR (1) BR112014010803A2 (enExample)
CA (1) CA2854447A1 (enExample)
ES (1) ES2600161T3 (enExample)
RU (1) RU2621148C2 (enExample)
WO (1) WO2013067296A1 (enExample)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013075084A1 (en) 2011-11-18 2013-05-23 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
CA2862289C (en) 2012-02-10 2019-11-26 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
AU2013361079B2 (en) * 2012-12-21 2018-07-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
WO2014151142A1 (en) 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9045477B2 (en) 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2015023915A1 (en) 2013-08-15 2015-02-19 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
US9822103B2 (en) 2013-11-22 2017-11-21 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
WO2015120372A2 (en) * 2014-02-10 2015-08-13 University Of Rochester Compositions and methods to inhibit ezh2 for the treatment of cardiovascular diseases
CN106255693A (zh) * 2014-03-07 2016-12-21 葛兰素史密斯克莱知识产权（第2 号）有限公司 Zeste增强子同源物2的抑制剂
SMT202000123T1 (it) 2014-03-17 2020-05-08 Daiichi Sankyo Co Ltd Derivati 1,3-benzodiossolici come inibitori di ezh1 e/o di ezh2
CN107148419A (zh) * 2014-10-28 2017-09-08 葛兰素史密斯克莱知识产权（第2 号）有限公司 Zeste增强子同源物2抑制剂
JP2017533922A (ja) * 2014-11-06 2017-11-16 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド 移植片対宿主病（ｇｖｈｄ）のためのクロマチン構造を調節する組成物の使用
WO2016073956A1 (en) * 2014-11-06 2016-05-12 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ｅｚｈ２抑制劑
JP2018522045A (ja) * 2015-08-03 2018-08-09 コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． Ｅｚｈ２阻害剤および制御性ｔ細胞機能の調節
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ｅｚｈ２抑制劑
US10577350B2 (en) 2015-08-28 2020-03-03 Constellation Pharmaceuticals, Inc. Crystalline forms of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
CN105541801B (zh) * 2016-01-18 2018-07-17 常州大学 Ezh2甲基转移酶抑制剂gsk126的合成方法
EP3445365A4 (en) 2016-04-22 2019-10-16 Dana-Farber Cancer Institute, Inc. EZH2 INHIBITORS AND USES THEREOF
US10676479B2 (en) * 2016-06-20 2020-06-09 Novartis Ag Imidazolepyridine compounds and uses thereof
AU2017323112B2 (en) * 2016-09-07 2020-11-26 Haihe Biopharma Co., Ltd. Pyrido five-element aromatic ring compound, preparation method therefor and use thereof
EP3529242A1 (en) 2016-10-19 2019-08-28 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
WO2018137639A1 (zh) * 2017-01-25 2018-08-02 恩瑞生物医药科技（上海）有限公司 一种组蛋白甲基转移酶ezh2抑制剂、其制备方法及其医药用途
JP2021531340A (ja) 2018-07-09 2021-11-18 フォンダシヨン、アジール、デ、アブグルスFondation Asile Des Aveugles 眼障害を治療するためのｐｒｃ２サブユニットの阻害
TWI837231B (zh) 2018-11-29 2024-04-01 日商第一三共股份有限公司 含有ｅｚｈ１／２雙重抑制劑之醫藥組合及其用途
US20220016111A1 (en) * 2018-12-21 2022-01-20 The Walter And Eliza Hall Institute Of Medical Research Methods of Treating Inflammation
CN109761960B (zh) * 2019-02-25 2021-08-31 江苏豪森药业集团有限公司 抗耐药抗肿瘤egfr抑制剂的制备方法
CN111961034A (zh) * 2019-05-20 2020-11-20 浙江同源康医药股份有限公司 用作ret激酶抑制剂的化合物及其应用
US11535621B2 (en) * 2019-07-31 2022-12-27 Ribon Therapeutics, Inc. Heterobicyclic amides as inhibitors of CD38
CN114555112A (zh) 2019-08-22 2022-05-27 朱诺治疗学股份有限公司 T细胞疗法和zeste增强子同源物2(ezh2)抑制剂的组合疗法及相关方法
MX2022007936A (es) 2019-12-25 2022-10-27 Nippon Shinyaku Co Ltd Agente profilactico y/o terapeutico para la prostatitis cronica/sindrome de dolor pelvico cronico.
TW202241418A (zh) 2021-01-29 2022-11-01 美商律幫治療股份有限公司 作為cd38之抑制劑的喹啉及氮雜喹啉

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2584713B1 (fr) 1985-07-11 1988-09-09 Roussel Uclaf Nouveaux derives de l'indole carboxamide, leurs sels, procede et intermediaires de preparation, application a titre de medicaments et compositions les renfermant
DE10022925A1 (de) 2000-05-11 2001-11-15 Basf Ag Substituierte Indole als PARP-Inhibitoren
EP1633740B1 (en) 2003-06-19 2011-11-09 GlaxoSmithKline LLC 5-(acylamino)indazole derivatives as kinase inhibitors
US20050059682A1 (en) 2003-09-12 2005-03-17 Supergen, Inc., A Delaware Corporation Compositions and methods for treatment of cancer
AU2005229522A1 (en) * 2004-03-11 2005-10-13 Actelion Pharmaceuticals Ltd. Indol-1-yl-acetic acid derivatives
WO2007053114A1 (en) * 2005-10-31 2007-05-10 S*Bio Pte Ltd Method of predicting a response to hdac inhibitors
WO2008109534A1 (en) * 2007-03-02 2008-09-12 Mdrna, Inc. Nucleic acid compounds for inhibiting ezh2 gene expression and uses thereof
WO2009006577A2 (en) * 2007-07-03 2009-01-08 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
WO2009048958A2 (en) 2007-10-08 2009-04-16 The Board Of Regents Of The University Of Texas System Methods and compositions involving chitosan nanoparticles
AR070398A1 (es) 2008-02-22 2010-03-31 Gruenenthal Chemie Derivados sustituidos de indol
CN104557914A (zh) 2008-09-26 2015-04-29 新加坡科技研究局 3-脱氮瓶菌素衍生物
US9107942B2 (en) * 2008-10-31 2015-08-18 University Of Rochester Methods of diagnosing and treating fibrosis
US8642602B2 (en) * 2009-02-04 2014-02-04 University Of Georgia Research Foundation, Inc. Method of inhibiting fibrogenesis and treating fibrotic disease
ES2528269T3 (es) 2010-05-07 2015-02-06 Glaxosmithkline Llc Azaindazoles
WO2011140325A1 (en) 2010-05-07 2011-11-10 Glaxosmithkline Llc Indazoles
US8536179B2 (en) * 2010-05-07 2013-09-17 Glaxosmithkline Llc Indoles
EP3323820B1 (en) * 2011-02-28 2023-05-10 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds

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