SG11201901197PA - Amino-pyrrolopyrimidinone compounds and methods of use thereof - Google Patents

Amino-pyrrolopyrimidinone compounds and methods of use thereof

Info

Publication number
SG11201901197PA
SG11201901197PA SG11201901197PA SG11201901197PA SG11201901197PA SG 11201901197P A SG11201901197P A SG 11201901197PA SG 11201901197P A SG11201901197P A SG 11201901197PA SG 11201901197P A SG11201901197P A SG 11201901197PA SG 11201901197P A SG11201901197P A SG 11201901197PA
Authority
SG
Singapore
Prior art keywords
chuo
tokyo
limited
international
daiichi sankyo
Prior art date
Application number
SG11201901197PA
Inventor
Craig Bates
Sudharshan Eathiraj
Hiroaki Inagaki
Jean-Marc Lapierre
Takayuki Momose
Kiyoshi Nakayama
Takashi Odagiri
Masahiro Ota
Yusuke Ota
Yoshihiro Shibata
Manish Tandon
Tomoyuki Tsunemi
Original Assignee
Arqule Inc
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 Arqule Inc filed Critical Arqule Inc
Publication of SG11201901197PA publication Critical patent/SG11201901197PA/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10Transferases (2.)
    • C12N9/12Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/02Halogenated hydrocarbons
    • A61K31/025Halogenated hydrocarbons carbocyclic
    • A61K31/03Halogenated hydrocarbons carbocyclic aromatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 01 March 2018 (01.03.2018) W I PO I PCT omit VIII °nolo III uall 11°1°11mm oimIE (10) International Publication Number WO 2018/039310 Al (51) International Patent Classification: C07D 487/04 (2006.01) A61K 31/519 (2006.01) CO7D 405/12 (2006.01) (21) International Application Number: PCT/US2017/048152 (22) International Filing Date: 23 August 2017 (23.08.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/378,868 24 August 2016 (24.08.2016) US 62/378,871 24 August 2016 (24.08.2016) US 62/378,872 24 August 2016 (24.08.2016) US (71) Applicant: ARQULE, INC. [US/US]; One Wall Street, Burlington, Massachusetts 01803 (US). (72) Inventors: BATES, Craig; 53 Tenney Road, Pelham, New Hampshire 03076 (US). EATHIRAJ, Sudharshan; 24 Ptarmigan Drive, Shrewsbury, Massachusetts 01545 (US). INAGAKI, Hiroaki; c/o DAIICHI SANKYO COM- PANY, LIMITED, 3-5-1, Nihonbashi Honcho, Chuo-ku, Tokyo 103-8426 (JP). LAPIERRE, Jean-Marc; 1 Alexan- dria Drive, Pelham, New Hampshire 03076 (US). MO- MOSE, Takayuki; c/o Daiichi Sankyo Company, Limit- ed, 3-5-1, Nibonbashi Honcho, Chuo-ku, Tokyo 103-8426 (JP). NAKAYAMA, Kiyoshi; c/o Daiichi Sankyo Compa- ny, Limited, 3-5-1, Nihonbashi Honcho, Chuo-Ku, Tokyo 103-8426 (JP). ODAGIRI, Takashi; c/o Daiichi Sankyo Company, Limited, 3-5-1, Nihonbashi Honcho, Chuo-Ku, Tokyo 103-8426 (JP). OTA, Masahiro; c/o Daiichi Sankyo Company, Limited, 3-5-1, Nihonbashi Honcho, Chuo-Ku, Tokyo 103-8426 (JP). OTA, Yusuke; c/o Daiichi Sankyo Company, Limited, 3-5-1, Nihonbashi Honcho, Chuo-Ku, Tokyo 103-8426 (JP). SHIBATA, Yoshihiro; c/o Dai- ichi Sankyo Company, Limited, 3-5-1, Nihonbashi Hon- cho, Chuo-Ku, Tokyo 103-8426 (JP). TANDON, Manish; 51 Lovering Avenue, Framingham, Massachusetts 01701 (US). TSUNEMI, Tomoyuki; c/o DAIICHI SANKYO COMPANY, LIMITED, 3-5-1, Nihonbashi Honcho, Chuo- ku, Tokyo 103-8426 (JP). (74) Agent: PAVAO, Matthew et al.; Cooley LLP, 1299 Penn- sylvania Avenue, Suite 700, Washington, District of Colum- bia 20004 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) Published: with international search report (Art. 21(3)) (54) Title: AMINO-PYRROLOPYRIMIDINONE COMPOUNDS AND METHODS OF USE THEREOF (57) : The application relates to a compound of Formula (I): or a pharmaceutically accept- able salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of BTK, a pharmaceutical composition comprising a compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role. (I) O O cc C
SG11201901197PA 2016-08-24 2017-08-23 Amino-pyrrolopyrimidinone compounds and methods of use thereof SG11201901197PA (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662378872P 2016-08-24 2016-08-24
US201662378868P 2016-08-24 2016-08-24
US201662378871P 2016-08-24 2016-08-24
PCT/US2017/048152 WO2018039310A1 (en) 2016-08-24 2017-08-23 Amino-pyrrolopyrimidinone compounds and methods of use thereof

Publications (1)

Publication Number Publication Date
SG11201901197PA true SG11201901197PA (en) 2019-03-28

Family

ID=61241149

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201901197PA SG11201901197PA (en) 2016-08-24 2017-08-23 Amino-pyrrolopyrimidinone compounds and methods of use thereof

Country Status (14)

Country Link
US (2) US11020398B2 (en)
EP (1) EP3504213A4 (en)
JP (1) JP2019530650A (en)
KR (1) KR20190035925A (en)
CN (1) CN109890821A (en)
AU (1) AU2017315343A1 (en)
BR (1) BR112019003504A2 (en)
CA (1) CA3034010A1 (en)
MX (1) MX2019002212A (en)
PH (1) PH12019500395A1 (en)
RU (1) RU2019108280A (en)
SG (1) SG11201901197PA (en)
TW (1) TW201811795A (en)
WO (1) WO2018039310A1 (en)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109890821A (en) 2016-08-24 2019-06-14 艾科尔公司 Amino-pyrrolopyrimidine ketone compound and its application method
EP3710431A4 (en) 2017-11-03 2021-07-07 Aclaris Therapeutics, Inc. Substituted pyrrolopyrimidine jak inhibitors and methods of making and using the same
CN109956870A (en) * 2017-12-14 2019-07-02 南京卡文迪许生物工程技术有限公司 A kind of Luo Shasi his synthetic method and its midbody compound
EP3774767A1 (en) * 2018-04-05 2021-02-17 Beth Israel Deaconess Medical Center, Inc. Aryl hydrocarbon receptor modulators and uses thereof
CA3108065A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide
CN112823005A (en) * 2018-08-10 2021-05-18 阿克拉瑞斯治疗股份有限公司 Pyrrolopyrimidine ITK inhibitors
EP4134369A1 (en) * 2018-08-13 2023-02-15 ArQule, Inc. Solid forms of tetrahydropyranyl amino-pyrrolopyrimidinone compounds
KR20220004726A (en) 2019-05-02 2022-01-11 어클라리스 쎄라퓨틱스, 인코포레이티드 Substituted pyrrolopyridines as JAK inhibitors
US20220235049A1 (en) * 2019-05-31 2022-07-28 Fochon Pharmaceuticals, Ltd. SUBSTITUTED PYRROLO [2, 3-b] PYRIDINE AND PYRAZOLO [3,4-b] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
JP7473642B2 (en) 2019-11-13 2024-04-23 ジャージアン・ロングチャーム・バイオ-テック・ファーマ・カンパニー・リミテッド Pyrrolopyrimidine Compounds as BTK Inhibitors and Their Use - Patent application
CN112812100B (en) * 2019-11-18 2022-04-05 四川海思科制药有限公司 Compound capable of degrading BTK kinase, preparation method and pharmaceutical application thereof
CN112608318B (en) * 2019-12-16 2023-09-08 成都海博为药业有限公司 Compound as protein kinase inhibitor and application thereof
CN111320634A (en) * 2020-04-14 2020-06-23 浙江工业大学 Preparation method of acetoxyl substituted pyrrolo [2,3-d ] pyrimidine derivative
EP4240337A1 (en) * 2020-11-05 2023-09-13 Merck Sharp & Dohme LLC Methods for treating hematologic malignancies with amino-pyrrolopyrimidinone compounds
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
US11530222B2 (en) * 2021-02-03 2022-12-20 Accutar Biotechnology Inc. Substituted pyrrolopyrimidine and pyrazolopyrimidine as Bruton's tyrosine kinase (BTK) degraders
CN112574200B (en) * 2021-02-26 2021-06-11 安润医药科技(苏州)有限公司 Small molecule inhibitors of BTK and/or mutant C481S of BTK
CN115028633B (en) * 2021-03-08 2023-12-22 药雅科技(上海)有限公司 Preparation and application of pyrrolopyrimidine compound
WO2022213932A1 (en) * 2021-04-06 2022-10-13 广州必贝特医药股份有限公司 Pyrrolopyrimidinone compound and application thereof
CN114761410B (en) * 2021-04-06 2023-08-25 广州必贝特医药股份有限公司 Pyrrolopyrimidinone compounds and application thereof
KR20240004588A (en) * 2021-05-12 2024-01-11 제지앙 롱샴 바이오-테크 파르마. 씨오., 엘티디. Crystalline form of pyrrolopyrimidine compounds and method for producing the same
AU2022280865A1 (en) * 2021-05-28 2023-11-09 Merck Sharp & Dohme Llc Synthesis of btk inhibitor and intermediates thereof
CN114409654A (en) * 2021-12-30 2022-04-29 安徽普利药业有限公司 Intermediate synthesis method of BTK inhibitor
WO2023192183A1 (en) * 2022-03-29 2023-10-05 Merck Sharp & Dohme Llc Pharmaceutical combinations and methods of use of amino-pyrrolopyrimidinone compound
CN115894500A (en) * 2022-11-02 2023-04-04 中国药科大学 Compound serving as BTK kinase inhibitor and preparation method and application thereof

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
RU2103272C1 (en) 1992-04-03 1998-01-27 Дзе Апджон Компани Bicyclic heterocyclic amines and their pharmaceutically acceptable salts as inhibitors of reactive oxygen
DE69738468T2 (en) 1996-08-23 2009-01-08 Novartis Ag SUBSTITUTED PYRROLOPYRIMIDINES AND METHOD FOR THE PRODUCTION THEREOF
GB0031080D0 (en) 2000-12-20 2001-01-31 Novartis Ag Organic compounds
JPWO2002051849A1 (en) 2000-12-26 2004-04-22 第一製薬株式会社 Cdk4 activity inhibitor
JP2003321472A (en) 2002-02-26 2003-11-11 Takeda Chem Ind Ltd Grk inhibitor
FR2842525B1 (en) 2002-07-16 2005-05-13 Aventis Pharma Sa 3-GUANIDINOCARBONYL-1-HETEROARYL-INDOLE DERIVATIVES, PROCESS FOR THE PREPARATION AS MEDICAMENTS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
WO2005051393A1 (en) 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
EP1696920B8 (en) 2003-12-19 2015-05-06 Plexxikon Inc. Compounds and methods for development of ret modulators
US20070066641A1 (en) 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
WO2005080377A1 (en) 2004-02-20 2005-09-01 Kirin Beer Kabushiki Kaisha COMPOUND HAVING TGF-β INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006032631A1 (en) 2004-09-22 2006-03-30 Janssen Pharmaceutica N.V. Inhibitors of the interaction between mdm2 and p53
US7906528B2 (en) 2004-10-05 2011-03-15 Novartis International Pharmaceutical Ltd. Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
AR054416A1 (en) 2004-12-22 2007-06-27 Incyte Corp PIRROLO [2,3-B] PIRIDIN-4-IL-AMINAS AND PIRROLO [2,3-B] PIRIMIDIN-4-IL-AMINAS AS INHIBITORS OF THE JANUS KINASES. PHARMACEUTICAL COMPOSITIONS.
CA2608733A1 (en) 2005-05-17 2007-02-01 Plexxikon, Inc. Pyrrol (2,3-b) pyridine derivatives protein kinase inhibitors
EP1957498B1 (en) 2005-05-20 2017-02-15 MethylGene Inc. Inhibitors of vegf receptor and hgf receptor signaling
PL2474545T3 (en) 2005-12-13 2017-04-28 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
CA2644649C (en) 2006-03-22 2014-06-17 Janssen Pharmaceutica N.V. Cyclic-alkylaminederivatives as inhibitors of the interaction between mdm2 and p53
EP2007373A4 (en) 2006-03-29 2012-12-19 Foldrx Pharmaceuticals Inc Inhibition of alpha-synuclein toxicity
US7998978B2 (en) 2006-05-01 2011-08-16 Pfizer Inc. Substituted 2-amino-fused heterocyclic compounds
EP1889847A1 (en) 2006-07-10 2008-02-20 DeveloGen Aktiengesellschaft Pyrrolopyrimidines for pharmaceutical compositions
AU2007332143B2 (en) 2006-12-11 2012-11-08 Bionomics Limited Chemical compounds and processes
WO2008075007A1 (en) 2006-12-21 2008-06-26 Cancer Research Technology Limited Morpholino-substituted bicycloheteroaryl compounds and their use as anti cancer agents
US20080161254A1 (en) 2007-01-03 2008-07-03 Virobay, Inc. Hcv inhibitors
US20100129933A1 (en) 2007-04-26 2010-05-27 Forschungszentrum Karlsruhe Gmbh Method for detecting the binding between mdm2 and the proteasome
WO2008135232A1 (en) 2007-05-02 2008-11-13 Riccardo Cortese Use and compositions of purine derivatives for the treatment of proliferative disorders
BRPI0820342A2 (en) 2007-11-07 2015-05-26 Foldrx Pharmaceuticals Inc Protein Traffic Modulation
US8138194B2 (en) 2008-04-30 2012-03-20 National Health Research Institutes Fused bicyclic pyrimidine compounds as aurora kinase inhibitors
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
PE20091846A1 (en) 2008-05-19 2009-12-16 Plexxikon Inc PIRROLO [2,3-d] -PYRIMIDINE DERIVATIVES AS KINE MODULATORS
WO2010002954A1 (en) 2008-07-02 2010-01-07 Wyeth (2-aryl-7h-pyrrolo[2,3-d]pyrimidin-4-yl)morpholine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
WO2010030757A2 (en) 2008-09-10 2010-03-18 Kalypsys Inc. Aminopyrimidine inhibitors of histamine receptors for the treatment of disease
CL2009001884A1 (en) 2008-10-02 2010-05-14 Incyte Holdings Corp Use of 3-cyclopentyl-3- [4- (7h-pyrrolo [2,3-d] pyrimidin-4-yl) -1h-pyrazol-1-yl) propanonitrile, janus kinase inhibitor, and use of a composition that understands it for the treatment of dry eye.
MX2011007326A (en) 2009-01-08 2011-10-19 Curis Inc Phosphoinositide 3-kinase inhibitors with a zinc binding moiety.
CA2776690C (en) 2009-10-06 2020-05-12 Millennium Pharmaceuticals, Inc. Heterocyclic compounds useful as pdk1 inhibitors
CN105906631A (en) 2009-11-18 2016-08-31 普莱希科公司 Compounds and methods for kinase modulation, and indications therefor
NZ601508A (en) 2009-12-30 2013-07-26 Arqule Inc Substituted naphthalenyl-pyrimidine compounds and the use thereof in the treatment of cancer
BR112012016376A2 (en) * 2009-12-30 2019-09-24 Arqule Inc substituted pyrrolo-aminopyrimide compounds
JP2013525308A (en) 2010-04-16 2013-06-20 キュリス,インコーポレイテッド Treatment of cancer with K-RAS mutation
TWI619713B (en) * 2010-04-21 2018-04-01 普雷辛肯公司 Compounds and methods for kinase modulation, and indications therefor
US8604032B2 (en) 2010-05-21 2013-12-10 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
WO2011149827A1 (en) 2010-05-24 2011-12-01 Glaxosmithkline Llc Compounds and methods
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
US8609672B2 (en) 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
WO2012048058A2 (en) 2010-10-06 2012-04-12 J-Pharma Co., Ltd. Developing potent urate transporter inhibitors: compounds designed for their uricosuric action
PT2672967T (en) 2011-02-07 2018-12-07 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
US20130096136A1 (en) 2011-09-30 2013-04-18 Methylgene Inc. Inhibitors of Protein Tyrosine Kinase Activity
WO2013082476A1 (en) 2011-11-30 2013-06-06 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
WO2013082275A1 (en) 2011-11-30 2013-06-06 Trustees Of Boston College Inhibitors of phosphodiesterases 11 (pde11) and methods of use to elevate cortisol production
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
US20130310340A1 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
WO2013182612A1 (en) 2012-06-07 2013-12-12 Bayer Pharma Aktiengesellschaft Glucose transport inhibitors
US20140018361A1 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2014015523A1 (en) 2012-07-27 2014-01-30 Hutchison Medipharma Limited Novel heteroaryl and heterocycle compounds, compositions and methods
US9688661B2 (en) 2012-08-02 2017-06-27 Nerviano Medical Sciences S.R.L. Substituted pyrroles active as kinases inhibitors
CN103664996B (en) 2012-08-31 2017-10-03 中国医学科学院医药生物技术研究所 Indole derivatives and preparation method thereof
AU2013312477B2 (en) * 2012-09-06 2018-05-31 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
TW201412740A (en) 2012-09-20 2014-04-01 Bayer Pharma AG Substituted pyrrolopyrimidinylamino-benzothiazolones
CN104812389B (en) 2012-09-24 2020-07-17 润新生物公司 Certain chemical entities, compositions, and methods
CN104781260A (en) 2012-09-26 2015-07-15 拜耳制药股份公司 Substituted indazol-pyrrolopyrimidines useful in the treatment of hyperfoliferative disorders
WO2014048869A1 (en) 2012-09-26 2014-04-03 Bayer Pharma Aktiengesellschaft Substituted indazol-pyrrolopyrimidines useful in the treatment of hyperproliferative diseases
US9388189B2 (en) 2012-10-16 2016-07-12 Almirall, S.A. Pyrrolotriazinone derivatives as PI3K inhibitors
US9718816B2 (en) 2013-03-15 2017-08-01 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as CARM1 inhibitors and uses thereof
WO2014152114A1 (en) 2013-03-15 2014-09-25 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as btk inhibitors
GB201309085D0 (en) 2013-05-20 2013-07-03 Redx Pharma Ltd Compounds
AU2014274093B2 (en) 2013-05-30 2018-11-08 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
TN2016000005A1 (en) 2013-07-08 2017-07-05 Bayer Pharma AG Substituted pyrazolo-pyridinamines
HUE054560T2 (en) 2013-12-05 2021-09-28 Pfizer Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
US9580416B2 (en) 2014-07-02 2017-02-28 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
US20170283440A1 (en) 2014-09-17 2017-10-05 Epizyme, Inc. Carm1 inhibitors and uses thereof
GB201419015D0 (en) 2014-10-24 2014-12-10 Orca Pharmaceuticals Ltd Compounds
AU2015417922B2 (en) 2015-12-23 2018-12-20 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
CN109890821A (en) 2016-08-24 2019-06-14 艾科尔公司 Amino-pyrrolopyrimidine ketone compound and its application method

Also Published As

Publication number Publication date
US20190358233A1 (en) 2019-11-28
AU2017315343A1 (en) 2019-02-28
US20180055846A1 (en) 2018-03-01
PH12019500395A1 (en) 2019-05-20
KR20190035925A (en) 2019-04-03
US11020398B2 (en) 2021-06-01
TW201811795A (en) 2018-04-01
CA3034010A1 (en) 2018-03-01
RU2019108280A (en) 2020-09-25
WO2018039310A1 (en) 2018-03-01
JP2019530650A (en) 2019-10-24
EP3504213A1 (en) 2019-07-03
EP3504213A4 (en) 2020-01-15
CN109890821A (en) 2019-06-14
BR112019003504A2 (en) 2019-05-21
MX2019002212A (en) 2019-07-08

Similar Documents

Publication Publication Date Title
SG11201901197PA (en) Amino-pyrrolopyrimidinone compounds and methods of use thereof
SG11201805154YA (en) Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
SG11201909955XA (en) Formulations of anti-lag3 antibodies and co-formulations of anti-lag3 antibodies and anti-pd-1 antibodies
SG11201804758QA (en) Aqueous pharmaceutical formulation comprising anti-pd-1 antibody avelumab
SG11201901747VA (en) Inhibitors of cellular metabolic processes
SG11201900135YA (en) N-(phenylsulfonyl)benzamides and related compounds as bcl-2 inhibitors
SG11201810600WA (en) Fxr (nr1h4) modulating compounds
SG11201804152RA (en) Heterocyclic compounds as immunomodulators
SG11201806863WA (en) Tetracyclic pyridone compounds as antivirals
SG11201408318RA (en) Compositions and methods for transmucosal absorption
SG11201810628XA (en) Nasal pharmaceutical compositions with a porous excipient
SG11201805044WA (en) Compounds useful as kinase inhibitors
SG11201408261UA (en) Syringe
SG11201408641UA (en) Phenoxyethyl piperidine compounds
SG11201805570WA (en) Systems and methods for long term transdermal administration
SG11201407580YA (en) Composition comprising two antibodies engineered to have reduced and increased effector function
SG11201807720TA (en) Methods and systems for determining antibiotic susceptibility
SG11201804721SA (en) Modulators of complement activity
SG11201810970WA (en) Anti-egfr antibody drug conjugates
SG11201903287PA (en) Anti-respiratory syncytial virus antibodies, and methods of their generation and use
SG11201407546QA (en) Novel ring-substituted n-pyridinyl amides as kinase inhibitors
SG11201901658PA (en) Beta-lactamase inhibitor compounds
SG11201810177VA (en) Pet-imaging immunomodulators
SG11201906959RA (en) Aryl hydrocarbon receptor (ahr) modulator compounds
SG11201807597UA (en) Methods of treating depression using orexin-2 receptor antagonists