JP6435315B2 - 高活性抗新生物薬及び抗増殖剤 - Google Patents

高活性抗新生物薬及び抗増殖剤 Download PDF

Info

Publication number
JP6435315B2
JP6435315B2 JP2016503044A JP2016503044A JP6435315B2 JP 6435315 B2 JP6435315 B2 JP 6435315B2 JP 2016503044 A JP2016503044 A JP 2016503044A JP 2016503044 A JP2016503044 A JP 2016503044A JP 6435315 B2 JP6435315 B2 JP 6435315B2
Authority
JP
Japan
Prior art keywords
compound
tert
synthesis
chloro
carbamate
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.)
Active
Application number
JP2016503044A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016518337A (ja
JP2016518337A5 (enExample
Inventor
ジェイ、コープランド、ストラム
ジョン、エマーソン、ビージ
パトリック、ジョセフ、ロバーツ
フランシス、ハビエル、タバレス
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.)
G1 Therapeutics Inc
Original Assignee
G1 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 G1 Therapeutics Inc filed Critical G1 Therapeutics Inc
Publication of JP2016518337A publication Critical patent/JP2016518337A/ja
Publication of JP2016518337A5 publication Critical patent/JP2016518337A5/ja
Application granted granted Critical
Publication of JP6435315B2 publication Critical patent/JP6435315B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • A61K31/33—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
    • A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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 three hetero rings
    • C07D487/20—Spiro-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
    • A61K31/495—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
    • A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A61K47/6867—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from a cell of a blood cancer
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0468—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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 three hetero rings
    • C07D487/14—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Cell Biology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2016503044A 2013-03-15 2014-03-14 高活性抗新生物薬及び抗増殖剤 Active JP6435315B2 (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201361798772P 2013-03-15 2013-03-15
US61/798,772 2013-03-15
US201361861374P 2013-08-01 2013-08-01
US61/861,374 2013-08-01
US201361911354P 2013-12-03 2013-12-03
US61/911,354 2013-12-03
US201461949795P 2014-03-07 2014-03-07
US61/949,795 2014-03-07
PCT/US2014/029274 WO2014144740A2 (en) 2013-03-15 2014-03-14 Highly active anti-neoplastic and anti-proliferative agents

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2018202981A Division JP6703583B2 (ja) 2013-03-15 2018-10-29 高活性抗新生物薬及び抗増殖剤

Publications (3)

Publication Number Publication Date
JP2016518337A JP2016518337A (ja) 2016-06-23
JP2016518337A5 JP2016518337A5 (enExample) 2017-04-20
JP6435315B2 true JP6435315B2 (ja) 2018-12-05

Family

ID=51527866

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2016503044A Active JP6435315B2 (ja) 2013-03-15 2014-03-14 高活性抗新生物薬及び抗増殖剤
JP2018202981A Active JP6703583B2 (ja) 2013-03-15 2018-10-29 高活性抗新生物薬及び抗増殖剤
JP2020082401A Pending JP2020128408A (ja) 2013-03-15 2020-05-08 高活性抗新生物薬及び抗増殖剤

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2018202981A Active JP6703583B2 (ja) 2013-03-15 2018-10-29 高活性抗新生物薬及び抗増殖剤
JP2020082401A Pending JP2020128408A (ja) 2013-03-15 2020-05-08 高活性抗新生物薬及び抗増殖剤

Country Status (7)

Country Link
US (6) US20140271460A1 (enExample)
EP (1) EP2967050A4 (enExample)
JP (3) JP6435315B2 (enExample)
CN (2) CN105407723A (enExample)
CA (2) CA3152117A1 (enExample)
HK (1) HK1222766A1 (enExample)
WO (1) WO2014144740A2 (enExample)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9259399B2 (en) 2007-11-07 2016-02-16 Cornell University Targeting CDK4 and CDK6 in cancer therapy
US8691830B2 (en) 2010-10-25 2014-04-08 G1 Therapeutics, Inc. CDK inhibitors
EP3216792B1 (en) 2012-03-29 2020-05-27 G1 Therapeutics, Inc. Lactam kinase inhibitors
WO2014144847A2 (en) 2013-03-15 2014-09-18 G1 Therapeutics, Inc. Hspc-sparing treatments for rb-positive abnormal cellular proliferation
CN105407723A (zh) 2013-03-15 2016-03-16 G1治疗公司 高效的抗赘生剂和抗增生剂
WO2015161285A1 (en) 2014-04-17 2015-10-22 G1 Therapeutics, Inc. Tricyclic lactams for use in the protection of hematopoietic stem and progenitor cells against ionizing radiation
EP3191098A4 (en) 2014-09-12 2018-04-25 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
WO2016040848A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors
CN109789143A (zh) * 2016-07-01 2019-05-21 G1治疗公司 基于嘧啶的抗增殖剂
MX383803B (es) * 2016-07-01 2025-03-14 G1 Therapeutics Inc Sintesis de n-(heteroaril)-pirrolo[3,2-d]pirimidin-2-aminas.
WO2018005863A1 (en) 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based compounds for the treatment of cancer
WO2018005533A1 (en) 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Antiproliferative pyrimidine-based compounds
CA3045465A1 (en) 2016-12-05 2018-06-14 G1 Therapeutics, Inc. Preservation of immune response during chemotherapy regimens
MX2019008158A (es) * 2017-01-06 2019-12-09 G1 Therapeutics Inc Terapia de combinacion para el tratamiento del cancer.
US11395821B2 (en) 2017-01-30 2022-07-26 G1 Therapeutics, Inc. Treatment of EGFR-driven cancer with fewer side effects
KR102659211B1 (ko) * 2017-06-29 2024-04-18 쥐원 쎄라퓨틱스, 인크. G1t38의 형체 형태 및 그의 제조 방법
WO2019133864A1 (en) * 2017-12-29 2019-07-04 Accutar Biotechnology DUAL INHIBITORS OF PARP1 and CDK
JP2021509680A (ja) * 2018-01-08 2021-04-01 ジー１、セラピューティクス、インコーポレイテッドＧ１ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． Ｇ１ｔ３８の優れた投与レジメン
TWI875756B (zh) 2019-05-05 2025-03-11 美商基尼特奇公司 Ｃｄｋ抑制劑
JP2023508357A (ja) 2019-12-23 2023-03-02 アキュター バイオテクノロジー インコーポレイテッド エストロゲン受容体分解剤とサイクリン依存性キナーゼ阻害剤との癌治療用組み合わせ
EP4652997A2 (en) 2020-05-19 2025-11-26 Pharmacosmos Holding A/s Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders
BR112022024484A2 (pt) * 2020-06-11 2022-12-27 Lunella Biotech Inc Terapias contra o câncer com o inibidor seletivo de cdk4/6
US10988479B1 (en) 2020-06-15 2021-04-27 G1 Therapeutics, Inc. Morphic forms of trilaciclib and methods of manufacture thereof
CN117903147B (zh) * 2024-01-10 2025-07-25 沈阳药科大学 一种曲拉西利及其中间体的制备方法

Family Cites Families (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5591855A (en) 1994-10-14 1997-01-07 Cephalon, Inc. Fused pyrrolocarbazoles
US5628984A (en) 1995-07-31 1997-05-13 University Of North Carolina At Chapel Hill Method of detecting lung disease
EP0964864B1 (en) 1997-02-05 2008-04-09 Warner-Lambert Company LLC Pyrido 2,3-d pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US20040006074A1 (en) 1998-04-28 2004-01-08 The Government Of The United States Of America Cyclin dependent kinase (CDK)4 inhibitors and their use for treating cancer
EP1086105B1 (en) 1998-06-16 2006-03-01 THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES Fused azepinone cyclin dependent kinase inhibitors
ATE380548T1 (de) 1999-01-29 2007-12-15 Univ Illinois Verwendung von p53 inhibitoren zur behandlung von nebenerscheinungen bei der krebstherapie
AU6314900A (en) 1999-07-26 2001-02-13 Banyu Pharmaceutical Co., Ltd. Biarylurea derivatives
US6387900B1 (en) 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
US6291504B1 (en) 1999-10-20 2001-09-18 Dupont Pharmaceuticals Company Acylsemicarbazides and their uses
US6867198B2 (en) 1999-12-16 2005-03-15 Eli Lilly And Company Agents and methods for the treatment of proliferative diseases
US7053070B2 (en) 2000-01-25 2006-05-30 Warner-Lambert Company Pyrido[2,3-d]pyrimidine-2,7-diamine kinase inhibitors
DK1686130T3 (da) 2000-06-26 2009-04-06 Pfizer Prod Inc Pyrrolo-[2,3-d]-pyrimidinforbindelser som immunsuppressive midler
ES2220811T3 (es) 2000-09-29 2004-12-16 Eli Lilly And Company Procedimiento y compuestos para el tratamiento de enfermedades proliferativas.
AU2002228692A1 (en) 2000-12-01 2002-06-11 Bristol-Myers Squibb Pharma Company 3-(2,4-dimethylthiazol-5-yl) indeno(1,2-c)pyrazol-4-one derivatives as cdk inhibitors
DE60228692D1 (de) 2001-02-28 2008-10-16 Univ Temple Verwendung von alpha, beta ungesättigten arylsulfonen zum schutz von zellen und geweben vor toxizität ionischer strahlung
KR100863624B1 (ko) * 2001-05-11 2008-10-15 보드 오브 리전츠, 더 유니버시티 오브 텍사스 시스템 Ｃｄ26을 발현하는 세포와 연관된 질환의 치료제로사용되는 항-ｃｄ26 단클론항체
MEP46108A (en) 2002-01-22 2011-02-10 Warner Lambert Co 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d]PYRIMIDIN-7-ONES
CA2495787A1 (en) 2002-05-01 2003-11-13 Chromos Molecular Systems, Inc. Methods for delivering nucleic acid molecules into cells and assessment thereof
EP1590341B1 (en) 2003-01-17 2009-06-17 Warner-Lambert Company LLC 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
BRPI0410563B8 (pt) 2003-05-22 2021-05-25 Nerviano Medical Sciences Srl compostos de pirazol-quinazolina, seus processos de preparação e composições farmacêuticas
PT1648889E (pt) 2003-07-11 2008-12-10 Warner Lambert Co Sal isetionato de um inibidor selectivo da cdk4
CA2543308C (en) 2003-10-23 2012-03-06 F. Hoffman-La Roche Ag Triaza-spiropiperidine derivatives for use as glyt-1 inhibitors in the treatment of neurological and neuropsychiatric disorders
GB0327380D0 (en) 2003-11-25 2003-12-31 Cyclacel Ltd Method
BRPI0509580A (pt) 2004-03-30 2007-11-27 Pfizer Prod Inc combinações de inibidores de transdução de sinal
WO2005100999A2 (en) 2004-04-08 2005-10-27 Cornell Research Foundation, Inc. Functional immunohistochemical cell cycle analysis as a prognostic indicator for cancer
ITMI20040874A1 (it) 2004-04-30 2004-07-30 Ist Naz Stud Cura Dei Tumori Derivati indolici ed azaindolici con azione antitumorale
ES2411975T3 (es) 2005-01-14 2013-07-09 Janssen Pharmaceutica Nv Pirimidinas heterocíclicas anilladas de 5 miembros como inhibidores de cinasas
BRPI0606319A2 (pt) 2005-01-21 2009-06-16 Astex Therapeutics Ltd compostos farmacêuticos
EP2354139A1 (en) 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
EP1779848A1 (en) 2005-10-28 2007-05-02 Nikem Research S.R.L. V-ATPase inhibitors for the treatment of inflammatory and autoimmune diseases
US7579351B2 (en) 2005-12-09 2009-08-25 Hoffmann-La Roche Inc. Tricyclic amide derivatives
JP2009524589A (ja) 2005-12-22 2009-07-02 ワイス 置換されたイソキノリン−１，３（２ｈ，４ｈ）−ジオン、１−チオキソ−１，４−ジヒドロ−２ｈ−イソキノリン−３−オン誘導体、および１，４−ジヒドロ−３（２ｈ）−イソキノロン、ならびにキナーゼインヒビターとしてのそれらの使用
CN101415409B (zh) 2006-04-05 2012-12-05 诺瓦提斯公司 用于治疗癌症的治疗剂的组合
US20070270362A1 (en) 2006-05-18 2007-11-22 The University Of Washington Methods and compositions for prevention or treatment of inflammatory-related diseases and disorders
US8222256B2 (en) 2006-07-05 2012-07-17 Exelixis, Inc. Methods of using IGFIR and ABL kinase modulators
JP2010513317A (ja) 2006-12-14 2010-04-30 パナシー ファーマシューティカルズ インコーポレーティッド サイクリン依存性キナーゼの阻害による神経保護方法
KR20090091306A (ko) 2006-12-22 2009-08-27 노파르티스 아게 암, 염증 및 바이러스 감염 치료용 ｃｄｋ 억제제로서의 헤테로아릴-헤테로아릴 화합물
CA2690748A1 (en) 2007-06-25 2008-12-31 Neurogen Corporation Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues
US9259399B2 (en) 2007-11-07 2016-02-16 Cornell University Targeting CDK4 and CDK6 in cancer therapy
WO2009085185A1 (en) 2007-12-19 2009-07-09 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
JP5579715B2 (ja) 2008-07-29 2014-08-27 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ ｃｄｋ阻害剤および抗悪性腫瘍剤を含む治療用組合せ
US8685980B2 (en) 2008-08-22 2014-04-01 Novartis Ag Pyrrolopyrimidine compounds and their uses
CA2738925A1 (en) 2008-10-01 2010-04-08 The University Of North Carolina At Chapel Hill Hematopoietic protection against chemotherapeutic compounds using selective cyclin-dependent kinase 4/6 inhibitors
WO2010051127A2 (en) 2008-10-01 2010-05-06 The University Of North Carolina At Chapel Hill Hematopoietic protection against ionizing radiation using selective cyclin-dependent kinase 4/6 inhibitors
PA8852901A1 (es) 2008-12-22 2010-07-27 Lilly Co Eli Inhibidores de proteina cinasa
WO2010132725A2 (en) 2009-05-13 2010-11-18 The University Of North Carolina At Chapel Hill Cyclin dependent kinase inhibitors and methods of use
US9040519B2 (en) 2010-02-18 2015-05-26 Medivation Technologies, Inc. Fused tetracyclic pyrido [4,3-B] indole and pyrido [3,4-B] indole derivatives and methods of use
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
UY33226A (es) * 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6
EP2632467B1 (en) * 2010-10-25 2016-06-22 G1 Therapeutics, Inc. Cdk inhibitors
US8691830B2 (en) 2010-10-25 2014-04-08 G1 Therapeutics, Inc. CDK inhibitors
AU2011323455B2 (en) 2010-11-02 2017-07-27 Promega Corporation Coelenterazine derivatives and methods of using same
CN103501789A (zh) 2010-11-17 2014-01-08 北卡罗来纳大学查珀尔希尔分校 通过抑制增殖性激酶cdk4和cdk6保护肾组织免于局部缺血
HUE024504T2 (en) 2010-12-23 2016-01-28 Sanofi Sa Pyrimidine derivatives, a process for their preparation and their use in medicine
WO2012129344A1 (en) * 2011-03-23 2012-09-27 Amgen Inc. Fused tricyclic dual inhibitors of cdk 4/6 and flt3
BR112013033940A2 (pt) 2011-07-01 2017-02-14 Novartis Ag terapia combinada compreendendo um inibidor de cdk4/6 e um inibidor de pi3k para uso no tratamento de câncer
EP3216792B1 (en) 2012-03-29 2020-05-27 G1 Therapeutics, Inc. Lactam kinase inhibitors
CN104302620A (zh) 2012-04-26 2015-01-21 弗朗西斯·泽维尔·塔瓦雷斯 内酰胺的合成
US9241941B2 (en) 2012-09-20 2016-01-26 Memorial Sloan-Kettering Cancer Center Methods for treatment of lymphomas with mutations in cell cycle genes
CN105407723A (zh) 2013-03-15 2016-03-16 G1治疗公司 高效的抗赘生剂和抗增生剂
WO2014144847A2 (en) 2013-03-15 2014-09-18 G1 Therapeutics, Inc. Hspc-sparing treatments for rb-positive abnormal cellular proliferation
US20140274896A1 (en) 2013-03-15 2014-09-18 G1 Therapeutics, Inc. Transient Protection of Hematopoietic Stem and Progenitor Cells Against Ionizing Radiation
BR112015025711A8 (pt) 2013-04-08 2019-12-17 Janssen Pharmaceutica Nv uso de ibrutinibe e coposição farmacêutica compreendendo ibrutinibe e um agente anticâncer
US20160257688A1 (en) 2013-10-24 2016-09-08 Francis Xavier Tavares Process for Synthesis of Lactams
US10314842B2 (en) 2013-12-02 2019-06-11 Cornell University Methods for treating B cell proliferative disorders
WO2015161285A1 (en) 2014-04-17 2015-10-22 G1 Therapeutics, Inc. Tricyclic lactams for use in the protection of hematopoietic stem and progenitor cells against ionizing radiation
EP3191098A4 (en) 2014-09-12 2018-04-25 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
WO2016040848A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors
US20160220569A1 (en) 2015-02-03 2016-08-04 G1 Therapeutics, Inc. CDK4/6 Inhibitor Dosage Formulations For The Protection Of Hematopoietic Stem And Progenitor Cells During Chemotherapy

Also Published As

Publication number Publication date
US20230248733A1 (en) 2023-08-10
US10709711B2 (en) 2020-07-14
JP6703583B2 (ja) 2020-06-03
US20140271460A1 (en) 2014-09-18
JP2016518337A (ja) 2016-06-23
CN105407723A (zh) 2016-03-16
CA2906157C (en) 2022-05-17
JP2020128408A (ja) 2020-08-27
US20200345743A1 (en) 2020-11-05
CN107417691B (zh) 2020-06-26
US20180015096A1 (en) 2018-01-18
EP2967050A2 (en) 2016-01-20
CA2906157A1 (en) 2014-09-18
JP2019094324A (ja) 2019-06-20
CN107417691A (zh) 2017-12-01
US20160310499A1 (en) 2016-10-27
CA3152117A1 (en) 2014-09-18
US20190125752A1 (en) 2019-05-02
WO2014144740A2 (en) 2014-09-18
HK1222766A1 (zh) 2017-07-14
WO2014144740A3 (en) 2014-11-27
EP2967050A4 (en) 2016-09-28

Similar Documents

Publication Publication Date Title
JP6703583B2 (ja) 高活性抗新生物薬及び抗増殖剤
JP7250737B2 (ja) Ｒｂポジティブ異常細胞増殖に対するｈｓｐｃ温存治療
US20150297608A1 (en) Tricyclic Lactams for Use as Anti-Neoplastic and Anti-Proliferative Agents
JP2019070042A (ja) インドールアミン２，３−ジオキシゲナーゼの阻害剤としての活性を有するベンゾイミダゾールおよびイミダゾピリジンカルボキシミドアミド化合物

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170313

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20170313

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20171205

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20180305

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180605

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180622

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180925

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20181012

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20181112

R150 Certificate of patent or registration of utility model

Ref document number: 6435315

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313111

Free format text: JAPANESE INTERMEDIATE CODE: R313113

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250