AU2019255196A1 - EP4 inhibitors and use thereof - Google Patents

EP4 inhibitors and use thereof Download PDF

Info

Publication number
AU2019255196A1
AU2019255196A1 AU2019255196A AU2019255196A AU2019255196A1 AU 2019255196 A1 AU2019255196 A1 AU 2019255196A1 AU 2019255196 A AU2019255196 A AU 2019255196A AU 2019255196 A AU2019255196 A AU 2019255196A AU 2019255196 A1 AU2019255196 A1 AU 2019255196A1
Authority
AU
Australia
Prior art keywords
groups
alkyl
carbon atoms
group
alkoxy
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
AU2019255196A
Other languages
English (en)
Inventor
Jeffrey Ecsedy
Mark Manfredi
Atsushi Nagahisa
Takako Okumura
Yukinori Take
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Askat Inc
Arrys Therapeutics Inc
Original Assignee
Askat Inc
Arrys Therapeutics 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 Askat Inc, Arrys Therapeutics Inc filed Critical Askat Inc
Publication of AU2019255196A1 publication Critical patent/AU2019255196A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
    • 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/26—Lymph; Lymph nodes; Thymus; Spleen; Splenocytes; Thymocytes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19—Cytokines; Lymphokines; Interferons
    • A61K38/20—Interleukins [IL]
    • A61K38/208—IL-12
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39541—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against normal tissues, cells
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/545—Medicinal preparations containing antigens or antibodies characterised by the dose, timing or administration schedule
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biomedical Technology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Zoology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cell Biology (AREA)
  • Developmental Biology & Embryology (AREA)
  • Virology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biotechnology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
AU2019255196A 2018-04-16 2019-04-16 EP4 inhibitors and use thereof Abandoned AU2019255196A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862658494P 2018-04-16 2018-04-16
US62/658,494 2018-04-16
US201862737219P 2018-09-27 2018-09-27
US62/737,219 2018-09-27
PCT/US2019/027603 WO2019204257A1 (en) 2018-04-16 2019-04-16 Ep4 inhibitors and use thereof

Publications (1)

Publication Number Publication Date
AU2019255196A1 true AU2019255196A1 (en) 2020-11-12

Family

ID=66589884

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2019255196A Abandoned AU2019255196A1 (en) 2018-04-16 2019-04-16 EP4 inhibitors and use thereof

Country Status (7)

Country Link
US (3) US10973834B2 (https=)
EP (1) EP3781162A1 (https=)
JP (2) JP2021522211A (https=)
CN (1) CN112292128A (https=)
AU (1) AU2019255196A1 (https=)
CA (1) CA3096546A1 (https=)
WO (1) WO2019204257A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10973834B2 (en) 2018-04-16 2021-04-13 Arrys Therapeutics, Inc. EP4 inhibitors and use thereof
US20210315909A1 (en) 2018-07-11 2021-10-14 Arrys Therapeutics, Inc. Polymorphic compounds and uses thereof
JP7640458B2 (ja) 2018-10-05 2025-03-05 アンナプルナ バイオ インコーポレイテッド Ａｐｊ受容体活性に関連する状態を処置するための化合物および組成物
EP3722319A1 (en) * 2019-04-09 2020-10-14 Rottapharm Biotech S.r.l. Pharmaceutical combination of an ep4 antagonist and immune checkpoint inhibitors for the treatment of tumours
CN110386941A (zh) * 2019-08-15 2019-10-29 上海邦耀生物科技有限公司 Ep4受体拮抗剂和pd-1抑制剂联合用于癌症的治疗
CN115697317A (zh) * 2020-04-08 2023-02-03 株式会社AskAt Ep4受体拮抗剂用于治疗肝癌、黑色素瘤、淋巴瘤和白血病的应用
WO2021226162A1 (en) * 2020-05-05 2021-11-11 Arrys Therapeutics, Inc. Ep4 antagonists and their use in the treatment of proliferative diseases
US11857551B1 (en) 2020-07-10 2024-01-02 Ting Therapeutics Llc Methods for the prevention and treatment of hearing loss
EP4215214A4 (en) * 2020-09-16 2024-07-03 Osaka University THERAPEUTIC AGENT AGAINST CANCER, IMMUNOSTIMULANT AND SCREENING METHOD FOR ANTI-CANCER SUBSTANCE
CN114907267A (zh) * 2021-02-08 2022-08-16 中国科学院上海药物研究所 用于抗肿瘤的药物组合

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HN2001000224A (es) 2000-10-19 2002-06-13 Pfizer Compuestos de imidazol condensado con arilo o heteroarilo como agentes anti - inflamatorios y analgesicos.
CN1867551B (zh) 2003-09-03 2013-09-11 拉夸里亚创药株式会社 作为前列腺素e2拮抗剂的苯基或吡啶基酰胺化合物
TWI309240B (en) 2004-09-17 2009-05-01 Hoffmann La Roche Anti-ox40l antibodies
CN101137656B (zh) 2005-03-11 2010-12-22 拉夸里亚创药株式会社 咪唑衍生物的晶型
AU2006230099B2 (en) 2005-03-25 2012-04-19 Gitr, Inc. GITR binding molecules and uses therefor
PL1879573T3 (pl) 2005-05-10 2013-05-31 Incyte Holdings Corp Modulatory 2,3-dioksygenazy indoloaminy i sposoby ich zastosowania
CN104356236B (zh) 2005-07-01 2020-07-03 E.R.施贵宝&圣斯有限责任公司 抗程序性死亡配体1(pd-l1)的人单克隆抗体
CA2634198C (en) 2005-12-20 2014-06-03 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
ES2444574T3 (es) 2006-09-19 2014-02-25 Incyte Corporation N-hidroxiamidinoheterociclos como moduladores de la indolamina 2,3-dioxigenasa
CL2007002650A1 (es) 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
EP1987839A1 (en) 2007-04-30 2008-11-05 I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease
ES2776406T3 (es) 2007-07-12 2020-07-30 Gitr Inc Terapias de combinación que emplean moléculas de enlazamiento a GITR
EP2044949A1 (en) 2007-10-05 2009-04-08 Immutep Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response
JP5583592B2 (ja) 2007-11-30 2014-09-03 ニューリンク ジェネティクス コーポレイション Ｉｄｏ阻害剤
US20110176972A1 (en) 2008-05-29 2011-07-21 Saint-Gobain Centre De Recherches et D'Etudes Eur Cellular structure containing aluminium titanate
AR072999A1 (es) 2008-08-11 2010-10-06 Medarex Inc Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos
AU2009333580B2 (en) 2008-12-09 2016-07-07 Genentech, Inc. Anti-PD-L1 antibodies and their use to enhance T-cell function
EP3431085B1 (en) 2009-04-22 2023-10-11 AskAt Inc. Selective ep4 receptor antagonistic substance for treatment of cancer
JP5594754B2 (ja) 2009-07-13 2014-09-24 国立大学法人 東京大学 運行実績を活用したオンデマンドバスの運行スケジューリングシステム及びその方法
EP2473531A4 (en) 2009-09-03 2013-05-01 Merck Sharp & Dohme Anti-gitr antibodies
US8722720B2 (en) 2009-10-28 2014-05-13 Newlink Genetics Corporation Imidazole derivatives as IDO inhibitors
PH12012500881A1 (en) 2009-12-10 2017-07-26 Hoffmann La Roche Antibodies binding preferentially human csf1r extracellular domain 4 and their use
ES2600355T3 (es) 2010-02-22 2017-02-08 Raqualia Pharma Inc. Uso de un antagonista del receptor EP4 en el tratamiento de dermatitis de contacto alérgica y psoriasis
JP5998060B2 (ja) 2010-03-04 2016-09-28 マクロジェニクス，インコーポレーテッド Ｂ７−ｈ３と反応性のある抗体、その免疫学的に活性なフラグメントおよびその使用
CN102918061B (zh) 2010-03-05 2016-06-08 霍夫曼-拉罗奇有限公司 针对人csf-1r的抗体及其用途
MX378336B (es) 2010-05-04 2025-03-10 Five Prime Therapeutics Inc Anticuerpos que se unen a factor estimulante de colonias 1 (csf1r).
PT2614082T (pt) 2010-09-09 2018-12-03 Pfizer Moléculas de ligação a 4-1bb
PH12013501201A1 (en) 2010-12-09 2013-07-29 Univ Pennsylvania Use of chimeric antigen receptor-modified t cells to treat cancer
NO2694640T3 (https=) 2011-04-15 2018-03-17
KR101970025B1 (ko) 2011-04-20 2019-04-17 메디뮨 엘엘씨 Ｂ7-ｈ1 및 ｐｄ-1과 결합하는 항체 및 다른 분자들
HRP20201595T1 (hr) 2011-11-28 2020-12-11 Merck Patent Gmbh Anti-pd-l1 protutijela i njihova uporaba
US20150004175A1 (en) * 2011-12-13 2015-01-01 Yale University Compositions and Methods for Reducing CTL Exhaustion
BR112014012624A2 (pt) 2011-12-15 2018-10-09 F Hoffmann-La Roche Ag anticorpos, composição farmacêutica, ácido nucleico, vetores de expressão, célula hospedeira, método para a produção de um anticorpo recombinante e uso do anticorpo
RU2014136332A (ru) 2012-02-06 2016-03-27 Дженентек, Инк. Композиции и способы применения ингибиторов csf1r
AR090263A1 (es) 2012-03-08 2014-10-29 Hoffmann La Roche Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma
EP2847220A1 (en) 2012-05-11 2015-03-18 Five Prime Therapeutics, Inc. Methods of treating conditions with antibodies that bind colony stimulating factor 1 receptor (csf1r)
AR091649A1 (es) 2012-07-02 2015-02-18 Bristol Myers Squibb Co Optimizacion de anticuerpos que se fijan al gen de activacion de linfocitos 3 (lag-3) y sus usos
CN107759690A (zh) 2012-08-31 2018-03-06 戊瑞治疗有限公司 用结合群落刺激因子1受体(csf1r)的抗体治疗病状的方法
CN107496421A (zh) 2013-03-19 2017-12-22 株式会社ＡｓｋＡｔ Ep4受体拮抗剂在软骨疾病的治疗中的用途
US10391086B2 (en) 2013-03-19 2019-08-27 Askat Inc. Use of EP4 receptor antagonists in the treatment of cartilage disease
NZ733234A (en) 2014-03-06 2018-08-31 Aratana Therapeutics Inc Crystalline forms of grapiprant
KR102535283B1 (ko) * 2014-05-23 2023-05-22 에자이 알앤드디 매니지먼트 가부시키가이샤 암의 치료를 위한 조합 요법
UY36390A (es) * 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen
HUE057799T2 (hu) * 2016-07-07 2022-06-28 Ono Pharmaceutical Co EP4 antagonistát és immunellenõrzõpont gátlót tartalmazó kombináció
US10342785B2 (en) * 2016-11-04 2019-07-09 Askat Inc. Use of EP4 receptor antagonists for the treatment of NASH-associated liver cancer
US20190365680A1 (en) 2016-11-04 2019-12-05 Askat Inc. Use of ep4 receptor antagonists for the treatment of nash-associated liver cancer
US10973834B2 (en) * 2018-04-16 2021-04-13 Arrys Therapeutics, Inc. EP4 inhibitors and use thereof
US20210315909A1 (en) 2018-07-11 2021-10-14 Arrys Therapeutics, Inc. Polymorphic compounds and uses thereof
EP3820469A4 (en) 2018-07-11 2022-04-13 Arrys Therapeutics, Inc. EP4 INHIBITORS AND SYNTHESIS THEREOF
CN113260363A (zh) 2018-09-27 2021-08-13 阿瑞斯医疗有限公司 格拉普兰特(grapiprant)单位剂型
CN115697317A (zh) * 2020-04-08 2023-02-03 株式会社AskAt Ep4受体拮抗剂用于治疗肝癌、黑色素瘤、淋巴瘤和白血病的应用

Also Published As

Publication number Publication date
US10973834B2 (en) 2021-04-13
CN112292128A (zh) 2021-01-29
EP3781162A1 (en) 2021-02-24
WO2019204257A1 (en) 2019-10-24
US20190314390A1 (en) 2019-10-17
JP2023165946A (ja) 2023-11-17
CA3096546A1 (en) 2019-10-24
US20240066040A1 (en) 2024-02-29
US20210290641A1 (en) 2021-09-23
JP2021522211A (ja) 2021-08-30

Similar Documents

Publication Publication Date Title
US20240066040A1 (en) Ep4 inhibitors and use thereof
US12577208B2 (en) TEAD inhibitors and uses thereof
US20240254120A1 (en) Ep4 inhibitors and synthesis thereof
US12295962B2 (en) Polymorphic compounds and uses thereof
AU2022258968A1 (en) Mek inhibitors and uses thereof
CA3196535A1 (en) Combination of an ahr inhibitor with a pdx inhibitor or doxorubicine
US12459895B2 (en) MEK inhibitors and uses thereof
CN108778332B (zh) Pd-1抗体与ido抑制剂联合在制备抗肿瘤的药物中的用途
CA3113468A1 (en) Grapiprant unit dosage forms
CA3239728A1 (en) Methods of treating cancer
WO2025096647A1 (en) Methods of treating tumors
TW202432586A (zh) 用於治療癌症之組合療法
CN118574613A (zh) 治疗癌症的方法

Legal Events

Date Code Title Description
MK4 Application lapsed section 142(2)(d) - no continuation fee paid for the application