CR20210387A - Inhibidores de kif18a - Google Patents

Inhibidores de kif18a

Info

Publication number
CR20210387A
CR20210387A CR20210387A CR20210387A CR20210387A CR 20210387 A CR20210387 A CR 20210387A CR 20210387 A CR20210387 A CR 20210387A CR 20210387 A CR20210387 A CR 20210387A CR 20210387 A CR20210387 A CR 20210387A
Authority
CR
Costa Rica
Prior art keywords
kif18a
compounds
cancer
inhibitors
kif18a inhibitors
Prior art date
Application number
CR20210387A
Other languages
English (en)
Inventor
Ana Elena Minatti
Jian Jeffrey Chen
Kexue Li
Vu Ma
Jonathan Dante Low
Nuria A Tamayo
James Alexander Brown
Liping H Pettus
Mary Catherine Walton
Lei Jia
Matthew Paul Bourbeau
Abhisek Banerjee
Michael J Frohn
Qingyian Liu
Original Assignee
Amgen 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 Amgen Inc filed Critical Amgen Inc
Publication of CR20210387A publication Critical patent/CR20210387A/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D419/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compuestos de fórmula (I): (I), como se definen en el presente documento, e intermedios sintéticos de los mismos, que pueden modular la proteína KIF18A alterando de esta forma el proceso del ciclo celular y la proliferación celular para tratar el cáncer y enfermedades relacionadas con cáncer. La invención también incluye composiciones farmacéuticas, que incluyen los compuestos, y métodos para tratar patologías relacionadas con la actividad de KIF18A.
CR20210387A 2018-12-20 2019-12-20 Inhibidores de kif18a CR20210387A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862783061P 2018-12-20 2018-12-20
PCT/US2019/068169 WO2020132648A1 (en) 2018-12-20 2019-12-20 Kif18a inhibitors

Publications (1)

Publication Number Publication Date
CR20210387A true CR20210387A (es) 2021-08-19

Family

ID=69187977

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20210387A CR20210387A (es) 2018-12-20 2019-12-20 Inhibidores de kif18a

Country Status (21)

Country Link
US (2) US11236069B2 (es)
EP (1) EP3897852A1 (es)
JP (1) JP7407196B2 (es)
KR (1) KR20210106474A (es)
CN (1) CN113226473A (es)
AR (1) AR117490A1 (es)
AU (1) AU2019403486A1 (es)
BR (1) BR112021011989A2 (es)
CA (1) CA3123871A1 (es)
CL (1) CL2021001634A1 (es)
CO (1) CO2021008224A2 (es)
CR (1) CR20210387A (es)
EA (1) EA202191730A1 (es)
IL (1) IL283639B2 (es)
JO (1) JOP20210154B1 (es)
MA (1) MA54543A (es)
MX (1) MX2021007156A (es)
PE (1) PE20211475A1 (es)
SG (1) SG11202106520VA (es)
UY (1) UY38526A (es)
WO (1) WO2020132648A1 (es)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11236069B2 (en) * 2018-12-20 2022-02-01 Amgen Inc. KIF18A inhibitors
US20220056015A1 (en) * 2018-12-20 2022-02-24 Amgen Inc. Kif18a inhibitors
JP2023521802A (ja) * 2020-04-14 2023-05-25 アムジエン・インコーポレーテツド 新生物疾患の処置のためのkif18a阻害剤
AU2021370660A1 (en) 2020-10-27 2023-06-08 Amgen Inc. Heterocyclic spiro compounds and methods of use
WO2022232332A1 (en) 2021-04-29 2022-11-03 Amgen Inc. 2-aminobenzothiazole compounds and methods of use thereof
CN117980298A (zh) 2021-06-25 2024-05-03 杭州英创医药科技有限公司 作为kif18a抑制剂的化合物
TW202321213A (zh) 2021-07-21 2023-06-01 美商安進公司 Kif18a抑制劑化合物之鹽和固態形式
CA3230123A1 (en) * 2021-08-26 2023-03-02 Derek A. Cogan Spiro indoline inhibitors of kif18a
WO2023088441A1 (zh) 2021-11-19 2023-05-25 微境生物医药科技(上海)有限公司 Kif18a抑制剂
AR128353A1 (es) * 2022-01-26 2024-04-24 Amgen Inc Síntesis de un inhibidor de kif18a
WO2023159086A1 (en) 2022-02-16 2023-08-24 Amgen Inc. Quinazoline compounds and use thereof as inhibtors of mutant kras proteins
WO2023159087A1 (en) 2022-02-16 2023-08-24 Amgen Inc. Quinazoline compounds and use thereof as inhibtors of mutant kras proteins
WO2023174175A1 (zh) * 2022-03-17 2023-09-21 微境生物医药科技(上海)有限公司 Kif18a抑制剂
CN116903605A (zh) * 2022-04-15 2023-10-20 武汉人福创新药物研发中心有限公司 一种kif18a抑制剂及其用途
CN116554151A (zh) * 2022-05-13 2023-08-08 上海湃隆生物科技有限公司 驱动蛋白kif18a抑制剂及其应用
WO2023217233A1 (zh) * 2022-05-13 2023-11-16 上海湃隆生物科技有限公司 驱动蛋白kif18a抑制剂及其应用
WO2024002328A1 (zh) * 2022-06-30 2024-01-04 勤浩医药(苏州)有限公司 一种含氮化合物及其应用
WO2024032661A1 (zh) * 2022-08-11 2024-02-15 山东轩竹医药科技有限公司 Kif18a抑制剂及其用途
WO2024035950A1 (en) * 2022-08-12 2024-02-15 Accent Therapeutics, Inc. Inhibitors of kif18a and uses thereof
WO2024039829A1 (en) * 2022-08-18 2024-02-22 Accent Therapeutics, Inc. Inhibitors of kif18a and uses thereof
WO2024051755A1 (zh) * 2022-09-08 2024-03-14 长春金赛药业有限责任公司 Kif18a抑制剂化合物、药物组合物及其制备方法和应用
WO2024051812A1 (zh) * 2022-09-09 2024-03-14 先声再明医药有限公司 酰胺类化合物、其组合物及用途
WO2024067675A1 (zh) * 2022-09-30 2024-04-04 长春金赛药业有限责任公司 稠环类kif18a抑制剂化合物、药物组合物及其制备方法和应用
WO2024067465A1 (zh) * 2022-09-30 2024-04-04 山东轩竹医药科技有限公司 Kif18a抑制剂
CN117917405A (zh) * 2022-10-21 2024-04-23 杭州邦顺制药有限公司 Kif18a蛋白抑制剂
WO2024109923A1 (en) * 2022-11-24 2024-05-30 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
CN115594664B (zh) * 2022-11-25 2023-02-24 英矽智能科技(上海)有限公司 一类螺环衍生物作为kif18a抑制剂
WO2024114730A1 (zh) * 2022-11-30 2024-06-06 微境生物医药科技(上海)有限公司 一种用于癌症治疗的药物组合物
WO2024114787A1 (zh) * 2022-12-02 2024-06-06 深圳众格生物科技有限公司 酰胺或脲类化合物
WO2024125488A1 (zh) * 2022-12-14 2024-06-20 浙江海正药业股份有限公司 芳香酰胺类衍生物、其制备方法和其在医药上的应用
WO2024125626A1 (en) * 2022-12-16 2024-06-20 Nuphase Therapeutics (Hangzhou) Limited., Co. Nitrogenous compound, pharmaceutical composition and use thereof
CN115947717B (zh) * 2023-03-09 2023-05-30 英矽智能科技(上海)有限公司 一类kif18a抑制剂
CN116535400A (zh) * 2023-04-26 2023-08-04 上海湃隆生物科技有限公司 氮杂螺环化合物及其应用

Family Cites Families (158)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
GB2116183B (en) 1982-03-03 1985-06-05 Genentech Inc Human antithrombin iii dna sequences therefore expression vehicles and cloning vectors containing such sequences and cell cultures transformed thereby a process for expressing human antithrombin iii and pharmaceutical compositions comprising it
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
JP2762522B2 (ja) 1989-03-06 1998-06-04 藤沢薬品工業株式会社 血管新生阻害剤
US5112946A (en) 1989-07-06 1992-05-12 Repligen Corporation Modified pf4 compositions and methods of use
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5892112A (en) 1990-11-21 1999-04-06 Glycomed Incorporated Process for preparing synthetic matrix metalloprotease inhibitors
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
SG64322A1 (en) 1991-05-10 1999-04-27 Rhone Poulenc Rorer Int Bis mono and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
PT669929E (pt) 1992-11-13 2007-04-30 Immunex Corp Ligando de elk, uma citoquina
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
AU693475B2 (en) 1993-10-01 1998-07-02 Novartis Ag Pyrimidineamine derivatives and processes for the preparation thereof
US5656643A (en) 1993-11-08 1997-08-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
EP0729471A1 (en) 1993-11-19 1996-09-04 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
ATE191218T1 (de) 1993-12-17 2000-04-15 Novartis Ag Rapamycin-derivate als immunosuppressoren
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
WO1995024190A2 (en) 1994-03-07 1995-09-14 Sugen, Inc. Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
EP0756627A1 (en) 1994-04-15 1997-02-05 Amgen Inc. Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases
DK0682027T3 (da) 1994-05-03 1998-05-04 Ciba Geigy Ag Pyrrolopyrimidinderivater med antiproliferativ virkning
US6303769B1 (en) 1994-07-08 2001-10-16 Immunex Corporation Lerk-5 dna
US5919905A (en) 1994-10-05 1999-07-06 Immunex Corporation Cytokine designated LERK-6
US6057124A (en) 1995-01-27 2000-05-02 Amgen Inc. Nucleic acids encoding ligands for HEK4 receptors
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
CA2216796C (en) 1995-03-30 2003-09-02 Pfizer Inc. Quinazoline derivatives
DE69609602T2 (de) 1995-04-03 2001-04-12 Novartis Ag Pyrazolderivate und verfahren zu deren herstellung
JP3053222B2 (ja) 1995-04-20 2000-06-19 ファイザー・インコーポレーテッド Mmpおよびtnf抑制剤としてのアリールスルホニルヒドロキサム酸誘導体
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
CA2219659C (en) 1995-06-09 2008-03-18 Novartis Ag Rapamycin derivatives
SK398A3 (en) 1995-07-06 1998-07-08 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
DE19534177A1 (de) 1995-09-15 1997-03-20 Merck Patent Gmbh Cyclische Adhäsionsinhibitoren
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
ATE217873T1 (de) 1996-01-23 2002-06-15 Novartis Erfind Verwalt Gmbh Pyrrolopyrimidinen und verfahren zu deren herstellung
JP3406763B2 (ja) 1996-01-30 2003-05-12 東レ・ダウコーニング・シリコーン株式会社 シリコーンゴム組成物
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
DE19608588A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19629652A1 (de) 1996-03-06 1998-01-29 Thomae Gmbh Dr K 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
AU716383B2 (en) 1996-03-15 2000-02-24 Novartis Ag Novel N-7-heterocyclyl pyrrolo(2,3-d)pyrimidines and the use thereof
RO121900B1 (ro) 1996-04-12 2008-07-30 Warner-Lambert Company Compuşi inhibitori, ireversibili, ai tirozin kinazelor, compoziţie farmaceutică care îi conţine şi utilizarea acestora
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
CA2258548C (en) 1996-06-24 2005-07-26 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
US6258823B1 (en) 1996-07-12 2001-07-10 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
EA199900021A1 (ru) 1996-07-13 1999-08-26 Глаксо, Груп Лимитед Бициклические гетероароматические соединения в качестве ингибиторов протеинтирозинкиназы
AR007857A1 (es) 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
TR199900066T2 (xx) 1996-07-18 1999-04-21 Pfizer Inc. Matriks metalloproteazlar�n fosfinat bazl� inhibit�rleri
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
DE69738749D1 (de) 1996-08-16 2008-07-17 Schering Corp Zelloberflächen-antigen aus säugetieren und verwandte reagenzien
WO1998007726A1 (en) 1996-08-23 1998-02-26 Novartis Ag Substituted pyrrolopyrimidines and processes for their preparation
SK21499A3 (en) 1996-08-23 2000-05-16 Pfizer Arylsulfonylamino hydroxamic acid derivatives
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
WO1998014449A1 (en) 1996-10-02 1998-04-09 Novartis Ag Fused pyrazole derivatives and processes for their preparation
US6251911B1 (en) 1996-10-02 2001-06-26 Novartis Ag Pyrimidine derivatives and processes for the preparation thereof
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
US6077864A (en) 1997-01-06 2000-06-20 Pfizer Inc. Cyclic sulfone derivatives
DE69817801T2 (de) 1997-02-03 2004-03-11 Pfizer Products Inc., Groton Arylsulfonylhydroxamsäurederivate
ATE391719T1 (de) 1997-02-05 2008-04-15 Warner Lambert Co Pyrido (2,3-d) pyrimidine und 4-amino-primidine als inhibitoren der zellulären proliferation
BR9807824A (pt) 1997-02-07 2000-03-08 Pfizer Derivados de n-hidróxi-beta-sulfonil-propionamida e seu uso como inibidores de metaloproteinases de matriz
EP0960098A1 (en) 1997-02-11 1999-12-01 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
US6329375B1 (en) 1997-08-05 2001-12-11 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
TR200000368T2 (tr) 1997-08-08 2000-07-21 Pfizer Products Inc. Ariloksiariarilsülfonilamino hidroksamik asit türevleri.
JP2001520039A (ja) 1997-10-21 2001-10-30 ヒューマン ジノーム サイエンシーズ, インコーポレイテッド ヒト腫瘍壊死因子レセプター様タンパク質、tr11,tr11sv1およびtr11sv2
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
JP2002502607A (ja) 1998-02-09 2002-01-29 ジェネンテク・インコーポレイテッド 新規な腫瘍壊死因子レセプター相同体及びそれをコードする核酸
WO1999045009A1 (en) 1998-03-04 1999-09-10 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
CO5031249A1 (es) 1998-05-29 2001-04-27 Sugen Inc Pirrol substituido-2-indolinonas inhibidoras de proteinci-nasas
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
CA2336848A1 (en) 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
EP1109555A4 (en) 1998-08-31 2001-11-21 Merck & Co Inc NEW ANGIOGENIC INHIBITORS
DE69915004T2 (de) 1998-11-05 2004-09-09 Pfizer Products Inc., Groton 5-Oxo-pyrrolidine-2-Carbonsäure-Hydroxamidderivate
ATE556713T1 (de) 1999-01-13 2012-05-15 Bayer Healthcare Llc Omega-carboxyarylsubstituierte-diphenyl- harnstoffe als p38-kinasehemmer
ATE329596T1 (de) 1999-03-30 2006-07-15 Novartis Pharma Gmbh Phthalazinderivate zur behandlung von entzündlicher erkrankungen
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
AU783960B2 (en) 1999-06-07 2006-01-05 Immunex Corporation Tek antagonists
IL147442A0 (en) 1999-07-12 2002-08-14 Genentech Inc Promotion or inhibition of angiogenesis and cardiovscularization by tumor necrosis factor ligand/receptor homologs
AU783158B2 (en) 1999-08-24 2005-09-29 Ariad Pharmaceuticals, Inc. 28-epirapalogs
MXPA02004366A (es) 1999-11-05 2002-11-07 Astrazeneca Ab Derivados de quinazolina como inhibidores vegf.
ATE514676T1 (de) 1999-11-24 2011-07-15 Sugen Inc Ionisierbare indolinon derivate und deren verwendung als ptk liganden
US6515004B1 (en) 1999-12-15 2003-02-04 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
AU4721901A (en) 2000-02-25 2001-09-03 Immunex Corp Integrin antagonists
US6651123B1 (en) 2000-03-30 2003-11-18 International Business Machines Corporation File system locking
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
HU230574B1 (hu) 2000-12-21 2023-11-28 Novartis Ag Pirimidinamin-származékok és ezeket tartalmazó gyógyászati készítmények, mint angiogenézis modulátorok
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
EP1631588A2 (en) 2003-05-23 2006-03-08 Wyeth Gitr ligand and gitr ligand-related molecules and antibodies and uses thereof
DE602004017736D1 (de) 2003-07-08 2008-12-24 Novartis Ag Verwendung von rapamycin und dessen derivaten zur behandlung von knochenverlust
EP1648900A4 (en) 2003-07-11 2010-02-10 Ariad Pharma Inc PHOSPHORUS MACROCYCLES
WO2005007190A1 (en) 2003-07-11 2005-01-27 Schering Corporation Agonists or antagonists of the clucocorticoid-induced tumour necrosis factor receptor (gitr) or its ligand for the treatment of immune disorders, infections and cancer
AR045134A1 (es) 2003-07-29 2005-10-19 Smithkline Beecham Plc Compuesto de 1h - imidazo [4,5-c] piridin-ilo, composicion farmaceutica que lo comprende, proceso para prepararla, su uso para preparar dicha composicion farmaceutica, combinacion farmaceutica, uso de la combinacion farmaceutica para la preparacion de un medicamento, procedimientos para preparar dic
WO2005055808A2 (en) 2003-12-02 2005-06-23 Genzyme Corporation Compositions and methods to diagnose and treat lung cancer
BRPI0417498A (pt) 2003-12-09 2007-05-29 Us Gov Health & Human Serv método para suprimir uma resposta imune em um indivìduo; método de inibição da proliferação de um célula; método de tratamento de um distúrbio proliferativo em um indivìduo; método para selecionar um agente imunossupressor ou anti-proliferativo; composição farmacêutica e estente vascular
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
WO2006083289A2 (en) 2004-06-04 2006-08-10 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
JP4836280B2 (ja) * 2004-06-18 2011-12-14 ノバルティス バクシンズ アンド ダイアグノスティックス,インコーポレーテッド 癌を治療するためのキネシンスピンドルタンパク質(ksp)阻害剤としてのn−(1−(1−ベンジル−4−フェニル−1h−イミダゾール−2−イル)−2,2−ジメチルプロピル)ベンズアミド誘導体および関連化合物
GEP20104906B (en) 2004-08-26 2010-02-25 Pfizer Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
US7666901B2 (en) 2004-10-13 2010-02-23 Wyeth Analogs of 17-hydroxywortmannin as PI3K inhibitors
DK2343320T3 (da) 2005-03-25 2018-01-29 Gitr Inc Anti-gitr-antistoffer og anvendelser deraf
EP3530736A3 (en) 2005-05-09 2019-11-06 ONO Pharmaceutical Co., Ltd. Human monoclonal antibodies to programmed death 1 (pd-1) and methods for treating cancer using anti-pd-1 antibodies alone or in combination with other immunotherapeutics
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CA2622870A1 (en) 2005-09-20 2007-03-29 Pfizer Products Inc. Dosage forms and methods of treatment using a tyrosine kinase inhibitor
WO2007056078A2 (en) * 2005-11-02 2007-05-18 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
US20110212086A1 (en) 2006-01-19 2011-09-01 Genzyme Corporation GITR Antibodies For The Treatment of Cancer
MY180595A (en) 2006-12-07 2020-12-03 Genentech Inc Phosphoinositide 3-kinase inhibitor compounds and methods of use
EP2175884B8 (en) 2007-07-12 2017-02-22 GITR, Inc. Combination therapies employing gitr binding molecules
US8247397B2 (en) 2007-09-12 2012-08-21 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
US8354528B2 (en) 2007-10-25 2013-01-15 Genentech, Inc. Process for making thienopyrimidine compounds
CN102203258A (zh) 2008-07-02 2011-09-28 新兴产品开发西雅图有限公司 TGF-β拮抗剂多靶点结合蛋白
CN102149820B (zh) 2008-09-12 2014-07-23 国立大学法人三重大学 能够表达外源gitr配体的细胞
AR077033A1 (es) * 2009-06-11 2011-07-27 Hoffmann La Roche Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicas
LT3023438T (lt) 2009-09-03 2020-05-11 Merck Sharp & Dohme Corp. Anti-gitr antikūnai
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
PT2519543T (pt) 2009-12-29 2016-10-07 Emergent Product Dev Seattle Proteínas de ligação de heterodímero e suas utilizações
WO2011085261A1 (en) * 2010-01-08 2011-07-14 Selexagen Therapeutics, Inc. Hedgehog inhibitors
WO2013039954A1 (en) 2011-09-14 2013-03-21 Sanofi Anti-gitr antibodies
LT3031799T (lt) * 2013-08-09 2018-06-25 Takeda Pharmaceutical Company Limited Aromatinis junginys
ES2953821T3 (es) * 2018-12-20 2023-11-16 Amgen Inc Inhibidores de KIF18A
US20220056015A1 (en) * 2018-12-20 2022-02-24 Amgen Inc. Kif18a inhibitors
US11236069B2 (en) * 2018-12-20 2022-02-01 Amgen Inc. KIF18A inhibitors
WO2020132653A1 (en) * 2018-12-20 2020-06-25 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors

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