SG11201608843TA - 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS - Google Patents

1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS

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Publication number
SG11201608843TA
SG11201608843TA SG11201608843TA SG11201608843TA SG11201608843TA SG 11201608843T A SG11201608843T A SG 11201608843TA SG 11201608843T A SG11201608843T A SG 11201608843TA SG 11201608843T A SG11201608843T A SG 11201608843TA SG 11201608843T A SG11201608843T A SG 11201608843TA
Authority
SG
Singapore
Prior art keywords
pyridin
ones
pyrazolo
pyrrolo
inhibitors
Prior art date
Application number
SG11201608843TA
Inventor
Andrew P Combs
Thomas P Maduskuie Jr
Nikoo Falahatpisheh
Original Assignee
Incyte Corp
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
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of SG11201608843TA publication Critical patent/SG11201608843TA/en

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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
    • 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
    • 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
    • A61K31/495—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
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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
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    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
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SG11201608843TA 2014-04-23 2015-04-22 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS SG11201608843TA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461983289P 2014-04-23 2014-04-23
PCT/US2015/027047 WO2015164480A1 (en) 2014-04-23 2015-04-22 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS

Publications (1)

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SG11201608843TA true SG11201608843TA (en) 2016-11-29

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SG10201809353TA SG10201809353TA (en) 2014-04-23 2015-04-22 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
SG11201608843TA SG11201608843TA (en) 2014-04-23 2015-04-22 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS

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US (7) US9540368B2 (en)
EP (3) EP4218766A1 (en)
JP (2) JP6572237B2 (en)
KR (2) KR102430144B1 (en)
CN (1) CN106414442B (en)
AR (1) AR100160A1 (en)
AU (3) AU2015249810B2 (en)
BR (1) BR112016024626B1 (en)
CA (1) CA2946731C (en)
CL (1) CL2016002681A1 (en)
CR (2) CR20200231A (en)
CY (2) CY1122948T1 (en)
DK (2) DK3674302T3 (en)
EA (2) EA039678B1 (en)
EC (1) ECSP16088983A (en)
ES (2) ES2942723T3 (en)
FI (1) FI3674302T3 (en)
HR (2) HRP20230340T1 (en)
HU (2) HUE061770T2 (en)
IL (3) IL248415B (en)
LT (2) LT3674302T (en)
MA (1) MA39985B1 (en)
ME (1) ME03763B (en)
MX (2) MX2016013851A (en)
MY (1) MY180775A (en)
NZ (3) NZ725930A (en)
PE (1) PE20170144A1 (en)
PH (1) PH12016502115A1 (en)
PL (2) PL3674302T3 (en)
PT (2) PT3674302T (en)
RS (2) RS64231B1 (en)
SG (2) SG10201809353TA (en)
SI (2) SI3674302T1 (en)
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Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20151990A1 (en) 2013-03-15 2016-01-13 Incyte Corp TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS
JP2016523964A (en) 2013-07-08 2016-08-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Tricyclic heterocycles as BET protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EP4218766A1 (en) 2014-04-23 2023-08-02 Incyte Holdings Corporation 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
TWI712603B (en) 2014-09-15 2020-12-11 美商英塞特公司 Tricyclic heterocycles as bet protein inhibitors
CN107108613B (en) 2014-11-10 2020-02-25 基因泰克公司 Bromodomain inhibitors and uses thereof
MA40943A (en) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc SUBSTITUTED PYRROLOPYRIDINES USED AS BROMODOMA INHIBITORS
MA40940A (en) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc SUBSTITUTED PYRROLOPYRIDINES USED AS BROMODOMA INHIBITORS
EP3250571B1 (en) 2015-01-29 2022-11-30 Genentech, Inc. Therapeutic compounds and uses thereof
AR104259A1 (en) * 2015-04-15 2017-07-05 Celgene Quanticel Res Inc BROMODOMINUM INHIBITORS
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
KR20180039117A (en) * 2015-08-11 2018-04-17 네오메드 인스티튜트 Aryl-substituted dihydroquinolinone, its preparation and its use as a pharmaceutical
BR112018002547A2 (en) 2015-08-12 2018-09-18 Neomed Inst substituted benzimidazoles, their preparation and their use as pharmaceuticals
WO2017066876A1 (en) 2015-10-21 2017-04-27 Neomed Institute Substituted imidazopyridines, their preparation and their use as pharmaceuticals
TW201722966A (en) 2015-10-29 2017-07-01 英塞特公司 Amorphous solid form of a BET protein inhibitor
US10519151B2 (en) 2016-01-28 2019-12-31 Neomed Institute Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals
EP3442972B1 (en) 2016-04-15 2020-03-04 AbbVie Inc. Bromodomain inhibitors
KR102460046B1 (en) * 2016-06-20 2022-10-31 인사이트 코포레이션 Crystalline solid form of BET inhibitor
EP3539960A4 (en) 2016-11-10 2020-03-18 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Nitrogenous macrocyclic compound, preparation method therefor, pharmaceutical composition and application thereof
TW201825490A (en) * 2017-01-11 2018-07-16 大陸商江蘇豪森藥業集團有限公司 Pyrrolo[2,3-c]pyridine derivatives, preparation methods and pharmaceutical uses thereof
SG11202000418XA (en) 2017-07-18 2020-02-27 Nuvation Bio Inc Heterocyclic compounds as adenosine antagonists
BR112020000962A2 (en) 2017-07-18 2020-07-14 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
JP7254075B2 (en) 2017-11-06 2023-04-07 サントル ナショナル ドゥ ラ ルシェルシュ シアンティフィック Xanthine derivatives and their use as inhibitors of the bromodomain of BET proteins
US11466034B2 (en) 2017-12-20 2022-10-11 Betta Pharmaceuticals Co., Ltd. Compound functioning as bromodomain protein inhibitor, and composition
CN111683932A (en) * 2018-02-06 2020-09-18 上海海和药物研究开发有限公司 Compound with BET inhibition activity, preparation method and application thereof
CN110776508B (en) * 2018-07-27 2021-07-16 海创药业股份有限公司 BRD4 inhibitor and preparation method and application thereof
CN109580433B (en) * 2018-10-26 2021-05-28 中国辐射防护研究院 Source term estimation method for diffusion of conventional explosive radioactive aerosol
EP3873474A4 (en) 2018-10-30 2022-07-13 Nuvation Bio Inc. Heterocyclic compounds as bet inhibitors
CN109432093A (en) * 2018-12-23 2019-03-08 黄泳华 The synergy system for the acetylcholinesterase inhibitor being made of Pyrazolopyridine ketone compounds
EP3911324A4 (en) 2019-01-18 2022-08-17 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
JP2022517419A (en) 2019-01-18 2022-03-08 ニューベイション・バイオ・インコーポレイテッド Heterocyclic compounds as adenosine antagonists
JP2022529575A (en) * 2019-03-17 2022-06-23 シャンハイ リンジーン バイオファーマ カンパニー リミテッド Pyrrole amide pyridone compound, manufacturing method and use
CN110003204B (en) * 2019-04-30 2020-08-11 上海勋和医药科技有限公司 BET protein inhibitor, preparation method and application thereof
WO2020253711A1 (en) * 2019-06-17 2020-12-24 中国科学院上海药物研究所 Pyrrolopyridone compound, preparation method therefor, and composition and use thereof
US20220388985A1 (en) * 2019-06-19 2022-12-08 Ribon Therapeutics, Inc. Targeted protein degradation of parp14 for use in therapy
MX2022000050A (en) 2019-07-02 2022-05-24 Nuvation Bio Inc Heterocyclic compounds as bet inhibitors.
CN112625036A (en) * 2019-10-08 2021-04-09 上海海和药物研究开发股份有限公司 Compound with BRD4 inhibitory activity, preparation method and application thereof
EP4081521A1 (en) 2019-12-27 2022-11-02 Lupin Limited Substituted tricyclic compounds
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
MX2022015220A (en) * 2020-06-03 2023-03-08 Incyte Corp Combination of ruxolitinib with incb057643 for treatment of myeloproliferative neoplasms.
EP4183785A1 (en) 2020-12-01 2023-05-24 Chengdu Easton Biopharmaceuticals Co., Ltd. Novel n-heterocyclic bet bromodomain inhibitor, and preparation method therefor and medical use thereof
WO2022132049A1 (en) * 2020-12-17 2022-06-23 National University Of Singapore Treating cancers using bet inhibitors
CR20230402A (en) 2021-01-19 2023-11-21 Lupin Ltd Pharmaceutical combinations of sos1 inhibitors for treating and/or preventing cancer

Family Cites Families (167)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2404E (en) 1899-12-05 1904-03-26 Louis Olivier Victor Parmentie Letter copy machine
JPS59170313A (en) 1983-03-14 1984-09-26 Kurimoto Iron Works Ltd Screen gate
JPS6053449A (en) 1983-09-01 1985-03-27 M K Seikou Kk Car washer
JPS6085739U (en) 1983-11-18 1985-06-13 クラリオン株式会社 Pinch roller device in tape recorder
JPS6243003U (en) 1985-09-05 1987-03-14
JPH0314566A (en) 1989-06-09 1991-01-23 Sankyo Co Ltd Benzimidazole derivative
US5244912A (en) 1991-03-28 1993-09-14 Eli Lilly And Company 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz(cd)indoles and pharmaceutical use thereof
FR2710915B1 (en) 1993-10-04 1995-11-24 Synthelabo Piperidine derivatives, their preparation and their therapeutic use.
GB9410469D0 (en) 1994-05-25 1994-07-13 Erba Farmitalia Imidazolylalkyl derivatives of imidazo (5,1-c) (1,4) benzoxazin-1-one and process for their preparation
FR2731708B1 (en) 1995-03-13 1997-04-30 Synthelabo PIPERIDINE DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR THERAPEUTIC APPLICATION
FR2747678B1 (en) 1996-04-22 1998-05-22 Synthelabo COMPOUNDS DERIVED FROM IMIDAZOBENZOXAZINE, PROCESSES FOR THEIR PREPARATION AND THERAPEUTIC USES
US6287693B1 (en) 1998-02-25 2001-09-11 John Claude Savoir Stable shaped particles of crystalline organic compounds
NZ531172A (en) 2000-04-21 2005-07-29 Upjohn Co Heterocyclic amine-type compounds for treating fibromyalgia and chronic fatigue syndrome
US20040089753A1 (en) 2000-06-28 2004-05-13 Holland Simon Joseph Wet milling process
ATE284886T1 (en) 2000-08-08 2005-01-15 Sanofi Aventis BENZIMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE
FR2816619B1 (en) 2000-11-15 2003-01-31 Sanofi Synthelabo BENZIMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
US6919334B2 (en) 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
EP1562956A4 (en) 2002-11-22 2007-10-10 Japan Tobacco Inc Fused bicyclic nitrogen-containing heterocycles
EP1462103A1 (en) 2003-03-25 2004-09-29 Faust Pharmaceuticals NO donors, combination products and uses as modulators of neurotransmitter release
EP1719761A4 (en) 2004-02-23 2007-10-10 Dainippon Sumitomo Pharma Co Novel heterocyclic compound
EP1732541A4 (en) 2004-04-07 2008-03-05 Takeda Pharmaceutical Cyclic compounds
US7713954B2 (en) 2004-09-30 2010-05-11 Roche Palo Alto Llc Compositions and methods for treating cognitive disorders
DE102005011058A1 (en) 2005-03-10 2006-09-14 Merck Patent Gmbh Substituted tetrahydro-pyrrolo-quinoline derivatives
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
EP1912989A2 (en) 2005-08-05 2008-04-23 AstraZeneca AB Tricyclic benzimidazoles and their use as metabotropic glutamate receptor modulators
US8975259B2 (en) 2007-04-27 2015-03-10 University Of Rochester Compositions and methods for inhibiting G protein signaling
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
WO2009020559A2 (en) 2007-08-03 2009-02-12 The J. David Gladstone Institutes Agents that inhibit p-tefb interactions and methods of use thereof
KR101600634B1 (en) 2007-12-28 2016-03-07 미쓰비시 타나베 파마 코퍼레이션 Antitumor agent
DE102008052618A1 (en) 2008-10-21 2010-04-22 Henkel Ag & Co. Kgaa Tricyclic aldehydes and C, H-acidic compounds
US8669249B2 (en) 2009-03-27 2014-03-11 Takeda Pharmaceutical Company Limited Poly (ADP-ribose) polymerase (PARP) inhibitors
TW201103941A (en) 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
TW201105681A (en) 2009-06-10 2011-02-16 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
WO2011024987A1 (en) 2009-08-31 2011-03-03 塩野義製薬株式会社 Aromatic fused heterocyclic derivative and pharmaceutical composition containing same
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
PL2722334T3 (en) 2009-11-05 2016-06-30 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
EP2955524A3 (en) 2009-11-05 2016-03-23 GlaxoSmithKline LLC Novel process
DK2496582T3 (en) 2009-11-05 2016-03-21 Glaxosmithkline Llc Benzodiazepine-BROMDOMAeNEINHIBITOR.
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
CA2812043A1 (en) 2010-04-23 2011-10-27 Kineta, Inc. Pyrimidinedione anti-viral compounds
WO2011143657A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Male contraceptive compositions and methods of use
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
JP5935030B2 (en) 2010-05-14 2016-06-15 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 Compositions and methods for treating leukemia
PL2902030T3 (en) 2010-05-14 2017-07-31 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
WO2011161031A1 (en) 2010-06-22 2011-12-29 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (en) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc BROMODOMINIUM INHIBITORS AND USES OF THE SAME
JP5766820B2 (en) 2011-02-09 2015-08-19 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Heterocyclic compounds as PI3 kinase inhibitors
WO2012116170A1 (en) 2011-02-23 2012-08-30 Ming-Ming Zhou Inhibitors of bromodomains as modulators of gene expression
CN103562210B (en) 2011-03-21 2016-05-25 弗·哈夫曼-拉罗切有限公司 PI3K 110 δ are had to optionally benzo oxygen azepine * compound and using method
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2721031B1 (en) 2011-06-17 2016-01-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
CA2840380A1 (en) 2011-06-24 2012-12-27 Dana-Farber Cancer Institute, Inc. Selective inhibitors of histone deacetylase isoform 6 and methods thereof
JP2013010719A (en) 2011-06-30 2013-01-17 Dainippon Sumitomo Pharma Co Ltd Benzimidazolone and oxindole derivative, and pharmaceutical application of them
EP2736528A4 (en) 2011-07-29 2015-03-18 Philadelphia Children Hospital Compositions and methods for the treatment of hiv
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013029548A1 (en) 2011-08-31 2013-03-07 Otsuka Pharmaceutical Co., Ltd. Quinolone compound
DE102011082013A1 (en) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-thieno [3,2-f] [1,2,4] triazolo [4,3-a] [1,4] diazepines
EP2757887B1 (en) 2011-09-22 2017-04-26 VIIV Healthcare UK Limited Pyrrolopyridinone compounds and methods for treating hiv
CN103857391B (en) 2011-09-30 2016-06-08 沈阳蓝桑医药生物技术研发有限公司 Pharmaceutical composition containing Rayleigh lattice lactone and application thereof
WO2013060636A1 (en) 2011-10-25 2013-05-02 Sanofi 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
ES2745471T3 (en) 2011-11-01 2020-03-02 Resverlogix Corp Oral immediate-release formulations for substituted quinazolinones
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20150133434A1 (en) 2012-03-28 2015-05-14 The J. David Gladstone Institutes Compositions and Methods for Reactivating Latent Immunodeficiency Virus
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281396A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
WO2013155695A1 (en) 2012-04-20 2013-10-24 Abbott Laboratories Isoindolone derivatives
TWI602820B (en) 2012-06-06 2017-10-21 星宿藥物公司 Bromodomain inhibitors and uses thereof
US9624244B2 (en) 2012-06-06 2017-04-18 Constellation Pharmaceuticals, Inc. Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof
BR112014031068A2 (en) 2012-06-12 2017-06-27 Abbvie Inc pyridinone and pyridazinone derivatives
MX2014015986A (en) 2012-06-25 2016-02-11 Oncoethix Gmbh Method of treating lymphoma using thienotriazolodiazepine compounds.
WO2014015175A1 (en) 2012-07-18 2014-01-23 Massachusetts Institute Of Technology Compositions and methods for modulating brd4 bioactivity
US9890147B2 (en) 2012-08-16 2018-02-13 Bayer Pharma Aktiengesellshaft 2,3-benzodiazepines
US20150238507A1 (en) 2012-08-16 2015-08-27 Glaxosmithkline Llc Benzodiazepines for treating small cell lung cancer
RU2015115634A (en) 2012-09-28 2016-11-20 Онкоэтикс Гмбх PHARMACEUTICAL COMPOSITION containing thienotriazolodiazepine compounds
CN104781259B (en) 2012-09-28 2018-06-01 拜耳制药股份公司 Inhibit the 5- aryl triazoles and azepine * of BET albumen
WO2014074775A1 (en) 2012-11-09 2014-05-15 Jacobus Pharmaceutical Company, Inc. Heteroaryl derivatives and uses thereof
US9422290B2 (en) 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
ES2625945T3 (en) 2012-11-14 2017-07-21 Glaxosmithkline Llc Thieno [3,2-c] pyridin-4 (5H) -ones as bet inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
CA2895404A1 (en) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydropyridopyrazinones
WO2014095775A1 (en) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydroquinoxalinones
JP2016507496A (en) 2012-12-21 2016-03-10 ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． Novel heterocyclic compounds as bromodomain inhibitors
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
US10053454B2 (en) 2013-02-27 2018-08-21 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2970285B1 (en) 2013-03-11 2019-04-17 AbbVie Inc. Fused tetracyclic bromodomain inhibitors
WO2014164596A1 (en) 2013-03-11 2014-10-09 The Regents Of The University Of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
US9050346B2 (en) 2013-03-11 2015-06-09 Abbvie Inc. Bromodomain inhibitors
CA2905071A1 (en) 2013-03-12 2014-10-09 Abbvie Inc. Dihydro-pyrrolopyridinone bromodomain inhibitors
KR102224992B1 (en) 2013-03-12 2021-03-10 애브비 인코포레이티드 Tetracyclic bromodomain inhibitors
US9493411B2 (en) 2013-03-12 2016-11-15 Abbvie Inc. Pyrrole-3-carboxamide bromodomain inhibitors
EA028174B1 (en) 2013-03-14 2017-10-31 Глаксосмитклайн Интеллекчуал Проперти (№2) Лимитед 2,3-disubstituted 1-acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
EA201591746A1 (en) 2013-03-14 2016-08-31 КОНВЕРДЖЕН ЭлЭлСи METHODS AND COMPOSITIONS FOR INHIBITING BRODOMODEN-CONTAINING PROTEINS
CN105189515B (en) 2013-03-14 2018-07-03 葛兰素史克知识产权第二有限公司 Furopyridine class as bromine structural domain inhibitor
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
PE20151990A1 (en) 2013-03-15 2016-01-13 Incyte Corp TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS
HUE039380T2 (en) 2013-03-15 2018-12-28 Plexxikon Inc Heterocyclic compounds and uses thereof
JP2016519660A (en) 2013-03-15 2016-07-07 エピジェネティクス・インコーポレイテッド Oxazolo [5,4-c] quinolin-2-one compounds as bromodomain inhibitors
WO2014154762A1 (en) 2013-03-27 2014-10-02 Boehringer Ingelheim International Gmbh Dihydroquinazolinone analogues as brd4 inhibitors
JP6370368B2 (en) 2013-03-27 2018-08-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Indolinone analogs as BRD4 inhibitors
TWI530499B (en) 2013-03-28 2016-04-21 吉李德科學股份有限公司 Benzimidazolone derivatives as bromodomain inhibitors
US10435364B2 (en) 2013-04-17 2019-10-08 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
WO2014173241A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
TWI527811B (en) 2013-05-09 2016-04-01 吉李德科學股份有限公司 Benzimidazole derivatives as bromodomain inhibitors
EP3412675A1 (en) 2013-05-27 2018-12-12 Novartis AG Imidazopyrrolidinone derivatives and their use in the treatment of disease
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
EA028175B1 (en) 2013-05-28 2017-10-31 Новартис Аг Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease
WO2014191911A1 (en) 2013-05-28 2014-12-04 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease
JP2016521722A (en) 2013-06-17 2016-07-25 バイエル ファーマ アクチエンゲゼルシャフト Substituted phenyl-2,3-benzodiazepine
ITMI20130991A1 (en) 2013-06-17 2014-12-18 Industrie De Nora Spa CURRENT MEASUREMENT SYSTEM PRESENT IN ELECTRODES IN INTERCONNECTED ELECTROLYTIC CELLS.
CA2915622C (en) 2013-06-21 2020-08-18 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
EP3010503B1 (en) 2013-06-21 2020-03-11 Zenith Epigenetics Ltd. Novel bicyclic bromodomain inhibitors
AR096758A1 (en) 2013-06-28 2016-02-03 Abbvie Inc BROMODOMINIUM CRYSTAL INHIBITORS
CA2916542A1 (en) 2013-06-28 2014-12-31 Abbvie Inc. Bromodomain inhibitors
JP2016523964A (en) 2013-07-08 2016-08-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Tricyclic heterocycles as BET protein inhibitors
JP6441334B2 (en) 2013-07-16 2018-12-19 ビーエーエスエフ ソシエタス・ヨーロピアＢａｓｆ Ｓｅ Herbicidal azine
BR112016001457A2 (en) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc TRANSCRIPTION FACTOR INHIBITORS AND THEIR USES
KR101672096B1 (en) 2013-09-30 2016-11-02 주식회사 엘지화학 Heterocyclic compound and organic light emitting device comprising the same
MX371386B (en) 2013-10-18 2020-01-27 Celgene Quanticel Res Inc Bromodomain inhibitors.
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015081246A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
WO2015089075A1 (en) 2013-12-09 2015-06-18 Abbvie Inc. Dihydropyridinone and dihydropyridazinone derivatives useful as bromodomain inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
US9822107B2 (en) 2013-12-20 2017-11-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
EP3092227B1 (en) 2014-01-09 2018-07-11 Orion Corporation Bicyclic heterocyclic derivatives as bromodomain inhibitors
JP2017511801A (en) 2014-02-28 2017-04-27 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン 9H-pyrimido [4,5-b] indoles and related analogs as BET bromodomain inhibitors
CA2944277C (en) 2014-04-23 2022-12-13 Basf Se Diaminotriazine compounds as herbicides
PT3134386T (en) 2014-04-23 2020-08-25 Takeda Pharmaceuticals Co Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease
EP4218766A1 (en) 2014-04-23 2023-08-02 Incyte Holdings Corporation 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
KR20170002550A (en) 2014-05-02 2017-01-06 온코에틱스 게엠베하 Method of treating resistant non-hodgkin lymphoma, medulloblastoma, and/or alk+ non-small cell lung cancer using thienotriazolodiazepine compounds
CA2947601A1 (en) 2014-05-02 2015-11-05 Oncoethix Gmbh Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds
WO2015169953A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating glioma using thienotriazolodiazepine compounds
JP2017519727A (en) 2014-05-08 2017-07-20 オンコエシックス ゲーエムベーハー Method for treating three types of negative breast cancer using thienotriazolodiazepine compounds
EP3148543B1 (en) 2014-05-30 2020-04-08 Icahn School of Medicine at Mount Sinai Small molecule transcription modulators of bromodomains
RS58730B1 (en) 2014-06-20 2019-06-28 Constellation Pharmaceuticals Inc Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
TWI712603B (en) 2014-09-15 2020-12-11 美商英塞特公司 Tricyclic heterocycles as bet protein inhibitors
EP3209656B1 (en) 2014-10-24 2020-04-01 Bristol-Myers Squibb Company Indole carboxamides compounds useful as kinase inhibitors
MA40943A (en) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc SUBSTITUTED PYRROLOPYRIDINES USED AS BROMODOMA INHIBITORS
WO2016123709A1 (en) 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins
WO2016186453A1 (en) 2015-05-20 2016-11-24 Kainos Medicine, Inc. Quinoline derivatives as bromodomain inhibitors
CN111138458A (en) 2015-05-29 2020-05-12 盐野义制药株式会社 Nitrogen-containing tricyclic derivatives having HIV replication inhibiting effect
CN105039258B (en) 2015-07-03 2018-04-17 北京大学 Method and composition by non-neuronal cell reprogramming for neuron cell
TW201722966A (en) 2015-10-29 2017-07-01 英塞特公司 Amorphous solid form of a BET protein inhibitor
CN105254635A (en) 2015-10-30 2016-01-20 中国药科大学 Imidazo pyrazine compound, medicine composition of imidazo pyrazine compound and purpose of imidazo pyrazine compound
US20170127985A1 (en) 2015-11-11 2017-05-11 Medtronic Minimed, Inc. Sensor set
WO2017103670A1 (en) 2015-12-14 2017-06-22 Zenith Epigenetics Lid. 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors
US10519151B2 (en) 2016-01-28 2019-12-31 Neomed Institute Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals
EP3412669A4 (en) 2016-02-05 2019-09-04 Chia Tai Tianqing Pharmaceutical Group Co.,Ltd Tricyclic compound for bromodomain-containing protein inhibitor and preparation, pharmaceutical composition, and application thereof
KR102460046B1 (en) 2016-06-20 2022-10-31 인사이트 코포레이션 Crystalline solid form of BET inhibitor
CN108069958A (en) 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 A kind of nitrogen-containing hetero cyclics, its preparation method, pharmaceutical composition and application

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