RU2416616C2 - Пролекарства соединений 2,4-пиримидиндиамина и их применения - Google Patents

Пролекарства соединений 2,4-пиримидиндиамина и их применения Download PDF

Info

Publication number
RU2416616C2
RU2416616C2 RU2007131430/04A RU2007131430A RU2416616C2 RU 2416616 C2 RU2416616 C2 RU 2416616C2 RU 2007131430/04 A RU2007131430/04 A RU 2007131430/04A RU 2007131430 A RU2007131430 A RU 2007131430A RU 2416616 C2 RU2416616 C2 RU 2416616C2
Authority
RU
Russia
Prior art keywords
prodrugs
compound
compound according
pyrimidinediamine
phosphate
Prior art date
Application number
RU2007131430/04A
Other languages
English (en)
Russian (ru)
Other versions
RU2007131430A (ru
Inventor
Раджиндер СИНГХ (US)
Раджиндер Сингх
Сомасекхар БХАМИДИПАТИ (US)
Сомасекхар БХАМИДИПАТИ
Эстебан МАСУДА (US)
Эстебан МАСУДА
Валентино Дж. СТЕЛЛА (US)
Валентино Дж. СТЕЛЛА
Томас САН (US)
Томас Сан
Original Assignee
Райджел Фармасьютикалз, Инк.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36295425&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RU2416616(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Райджел Фармасьютикалз, Инк. filed Critical Райджел Фармасьютикалз, Инк.
Publication of RU2007131430A publication Critical patent/RU2007131430A/ru
Application granted granted Critical
Publication of RU2416616C2 publication Critical patent/RU2416616C2/ru

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • 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
    • A61P17/10—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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574—Esters of oxyacids of phosphorus
    • C07F9/65742—Esters of oxyacids of phosphorus non-condensed with carbocyclic rings or heterocyclic rings or ring systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Pregnancy & Childbirth (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
RU2007131430/04A 2005-01-19 2006-01-19 Пролекарства соединений 2,4-пиримидиндиамина и их применения RU2416616C2 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US64542405P 2005-01-19 2005-01-19
US60/645,424 2005-01-19
US65462005P 2005-02-18 2005-02-18
US60/654,620 2005-02-18

Publications (2)

Publication Number Publication Date
RU2007131430A RU2007131430A (ru) 2009-02-27
RU2416616C2 true RU2416616C2 (ru) 2011-04-20

Family

ID=36295425

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2007131430/04A RU2416616C2 (ru) 2005-01-19 2006-01-19 Пролекарства соединений 2,4-пиримидиндиамина и их применения

Country Status (29)

Country Link
US (13) US7449458B2 (https=)
EP (2) EP1856135B1 (https=)
JP (2) JP4801096B2 (https=)
KR (1) KR101278397B1 (https=)
CN (1) CN101115761B (https=)
AT (1) ATE451381T1 (https=)
AU (1) AU2006206458B2 (https=)
BE (1) BE2020C511I2 (https=)
BR (1) BRPI0606318B8 (https=)
CA (1) CA2591948C (https=)
CY (2) CY1109888T1 (https=)
DE (1) DE602006010979D1 (https=)
DK (1) DK1856135T3 (https=)
ES (1) ES2337496T3 (https=)
FI (1) FIC20200014I1 (https=)
FR (1) FR20C1019I2 (https=)
HU (1) HUS2000011I1 (https=)
IL (1) IL183890A (https=)
LT (1) LTC1856135I2 (https=)
LU (1) LUC00153I2 (https=)
MX (2) MX2007007189A (https=)
NL (1) NL301039I2 (https=)
NO (2) NO339146B1 (https=)
NZ (1) NZ555947A (https=)
PL (1) PL1856135T3 (https=)
PT (1) PT1856135E (https=)
RU (1) RU2416616C2 (https=)
SI (1) SI1856135T1 (https=)
WO (1) WO2006078846A1 (https=)

Families Citing this family (243)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
CA2526285A1 (en) * 2003-05-15 2004-12-23 Arqule, Inc. Inhibitors of p38 and methods of using the same
WO2005012294A1 (en) * 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
US7754714B2 (en) 2004-05-18 2010-07-13 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
EP2258704A1 (en) * 2004-10-19 2010-12-08 ArQule, Inc. Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 map kinase
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
SI1814878T1 (sl) 2004-11-24 2012-06-29 Rigel Pharmaceuticals Inc Spojine spiro-2,4-pirimidindiamina in njihova uporaba
AU2006206458B2 (en) 2005-01-19 2012-10-25 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
US8227455B2 (en) 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
EP1883302A4 (en) * 2005-05-03 2009-05-20 Rigel Pharmaceuticals Inc JAK KINASE HEMMER AND ITS USE
BRPI0610876B8 (pt) 2005-06-08 2021-05-25 Rigel Pharmaceuticals Inc composto, formulação farmacêutica, e métodos de inibir uma atividade de uma jak cinase, e de inibir uma cascata de transdução de sinal em que jak3 cinase desempenha um papel
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
JP2008543855A (ja) 2005-06-13 2008-12-04 ライジェル ファーマシューティカルズ， インコーポレイテッド 変形性骨疾患を処置するための方法および組成物
ATE352714T1 (de) * 2005-06-17 2007-02-15 Magneti Marelli Powertrain Spa Brennstoffeinspritzventil
US20100041678A1 (en) * 2005-10-31 2010-02-18 Rigel Pharmaceuticals, Inc. Compositions and methods for treating inflammatory disorders
US20090306028A1 (en) * 2005-10-31 2009-12-10 Payan Donald G Compositions and methods for treating inflammatory disorders
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US7659280B2 (en) 2006-02-17 2010-02-09 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
ES2622493T3 (es) * 2006-02-24 2017-07-06 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta de JAK
WO2007123892A2 (en) * 2006-04-17 2007-11-01 Arqule Inc. Raf inhibitors and their uses
JP5468899B2 (ja) 2006-07-20 2014-04-09 アフィニウム ファーマシューティカルズ， インク． Ｆａｂｉインヒビターとしてのアクリルアミド誘導体
JP5161233B2 (ja) 2006-10-19 2013-03-13 ライジェル ファーマシューティカルズ， インコーポレイテッド 自己免疫疾患の処置のためのｊａｋキナーゼの阻害剤としての２，４−ピリミジンアミン誘導体
US20090048214A1 (en) * 2006-11-15 2009-02-19 Rigel Pharmaceuticals, Inc Methods for Treating Renal Tumors Using 2, 4-Pyrimidinediamine Drug and Prodrug Compounds
ATE540041T1 (de) 2006-11-21 2012-01-15 Rigel Pharmaceuticals Inc Prodrug-salze von 2,4-pyrimidindiaminverbindungen und anwendungen davon
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7834024B2 (en) * 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
WO2009003136A1 (en) * 2007-06-26 2008-12-31 Rigel Pharmaceuticals, Inc. Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders
CN101903357A (zh) 2007-07-17 2010-12-01 里格尔药品股份有限公司 作为pkc抑制剂的环状胺取代的嘧啶二胺
US20090088371A1 (en) * 2007-08-28 2009-04-02 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
UA102825C2 (ru) * 2007-11-07 2013-08-27 Райджел Фармасьютикалз, Инк. Фармацевтическая композиция, полученная влажным гранулированием с использованием вещества, которое связывает воду
HUE030912T2 (en) 2008-02-15 2017-06-28 Rigel Pharmaceuticals Inc Pyrimidine-2-amine compounds and their use as inhibitors of yak kinases
MX2010009159A (es) * 2008-02-22 2010-09-14 Rigel Pharmaceuticals Inc Uso de 2,4-pirimidindiaminas para el tratamiento de aterosclerosis.
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
AU2009238590A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
MX353308B (es) * 2008-05-21 2018-01-08 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
AU2013205510A1 (en) * 2008-05-21 2013-05-16 Ariad Pharmaceuticals, Inc. Phosphorous derivatives as kinase inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
ES2527137T3 (es) 2008-07-28 2015-01-21 Pfizer Inc. Compuestos de fenantrenona, composiciones y procedimientos
US20110172217A1 (en) * 2008-09-05 2011-07-14 Shionogi & Co., Ltd. Ring-fused morpholine derivative having pi3k-inhibiting activity
CA2972242A1 (en) 2008-09-18 2010-04-22 Auspex Pharmaceuticals, Inc. Benzoquinoline inhibitors of vesicular monoamine transporter 2
EP2361254A1 (en) * 2008-12-05 2011-08-31 ArQule, Inc. Raf inhibitors and their uses
AR074776A1 (es) 2008-12-18 2011-02-09 Sanofi Aventis Metodo para tratar la degeneracion macular; modulando el sistema inmunitario del paciente
BRPI1006942A2 (pt) 2009-01-23 2016-04-12 Rigel Pharmaceuticals Inc composto, composição farmacêutica, kit, métodos para inibir uma atividade de uma jak quinase, para tratar uma doença, para tratar a rejeição de transplante de aloenxerto em um receptor de transplante, para tratar uma reação de hipersensibilidade, e para inibir uma cascata de transdução de sinal, e, uso do composto
US8367689B2 (en) 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK
UA108077C2 (xx) * 2009-07-02 2015-03-25 Синтез динатрієвої солі n4-(2,2-диметил-4-$(дигідрофосфонокси)метил]-3-оксо-5-піридо$1,4]оксазин-6-іл)-5-фтор-n2-(3,4,5-триметоксифеніл)-2,4-піримідиндіаміну
EP2454265A2 (en) 2009-07-17 2012-05-23 Rigel Pharmaceuticals, Inc. Deuterated 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
CN106420756A (zh) * 2009-07-28 2017-02-22 里格尔药品股份有限公司 抑制jak途径的组合物和方法
JP5681723B2 (ja) 2009-11-20 2015-03-11 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用
EP2512246B1 (en) 2009-12-17 2015-09-30 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
KR101445012B1 (ko) 2009-12-17 2014-09-26 머크 샤프 앤드 돔 코포레이션 Ｓｙｋ 억제제로서의 아미노피리미딘
EP2539347A2 (en) * 2010-02-24 2013-01-02 Auspex Pharmaceuticals, Inc. Trimethoxyphenyl inhibitors of tyrosine kinase
CA2792278C (en) 2010-04-13 2019-05-14 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses
JP6073221B2 (ja) 2010-07-28 2017-02-01 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｊａｋ経路の阻害のための組成物および方法
MX336875B (es) 2010-08-10 2016-02-04 Celgene Avilomics Res Inc Sal de besilato de un inhibidor de tirosina cinasa de bruton (btk).
WO2012061303A1 (en) 2010-11-01 2012-05-10 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
EP2635284B1 (en) 2010-11-01 2019-12-18 Celgene CAR LLC Heterocyclic compounds and uses thereof
WO2012064706A1 (en) 2010-11-10 2012-05-18 Avila Therapeutics, Inc. Mutant-selective egfr inhibitors and uses thereof
EP2489663A1 (en) 2011-02-16 2012-08-22 Almirall, S.A. Compounds as syk kinase inhibitors
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
CA2834062A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
EP2706853B1 (en) 2011-05-10 2017-06-14 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
UY34072A (es) 2011-05-17 2013-01-03 Novartis Ag Derivados sustituidos de indol
WO2012167423A1 (en) 2011-06-08 2012-12-13 Hutchison Medipharma Limited Substituted pyridopyrazines as novel syk inhibitors
HRP20190186T4 (hr) * 2011-07-28 2024-12-20 Rigel Pharmaceuticals, Inc. Nove formulacije (trimetoksifenilamino)pirimidinila
EP2763975B1 (en) 2011-10-05 2016-04-06 Merck Sharp & Dohme Corp. 3-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
US9216173B2 (en) 2011-10-05 2015-12-22 Merck Sharp & Dohme Corp. 2-Pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
WO2013052391A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
US9364476B2 (en) 2011-10-28 2016-06-14 Celgene Avilomics Research, Inc. Methods of treating a Bruton's Tyrosine Kinase disease or disorder
MX363551B (es) 2011-11-23 2019-03-27 Portola Pharmaceuticals Inc Star Compuestos derivados de pirazina como inhibidores de cinasa.
BR112014022790B1 (pt) 2012-03-15 2022-04-19 Celgene Car Llc Sais de um inibidor de quinase de receptor de fator do crescimento epidermal, composição farmacêutica e usos do mesmo
CA2866852C (en) 2012-03-15 2020-12-29 Celgene Avilomics Research, Inc. Solid forms of an epidermal growth factor receptor kinase inhibitor
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
WO2013173506A2 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
AU2013279021C1 (en) 2012-06-19 2017-03-16 Debiopharm International Sa Prodrug derivatives of (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
EP2863913B1 (en) 2012-06-20 2018-09-12 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
EP2863914B1 (en) 2012-06-20 2018-10-03 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
CN102746337B (zh) * 2012-06-21 2014-12-17 成都苑东药业有限公司 一种2，4-嘧啶二胺类化合物及其制备方法
EP2863916B1 (en) 2012-06-22 2018-07-18 Merck Sharp & Dohme Corp. Substituted pyridine spleen tyrosine kinase (syk) inhibitors
EP2863915B1 (en) 2012-06-22 2017-12-06 Merck Sharp & Dohme Corp. SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS
US9353066B2 (en) 2012-08-20 2016-05-31 Merck Sharp & Dohme Corp. Substituted phenyl-Spleen Tyrosine Kinase (Syk) inhibitors
EP4345100A3 (en) 2012-09-18 2024-04-10 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9550780B2 (en) 2012-09-18 2017-01-24 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
WO2014048065A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
WO2014074421A1 (en) * 2012-11-07 2014-05-15 Merck Sharp & Dohme Corp. Prodrug bipyridylaminopyridines as syk inhibitors
EP2931281B1 (en) 2012-12-12 2018-01-17 Merck Sharp & Dohme Corp. Amino-pyrimidine-containing spleen tyrosine kinase inhibitors
EP2934525B1 (en) 2012-12-21 2019-05-08 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
US9126950B2 (en) 2012-12-21 2015-09-08 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
MX2015009952A (es) 2013-02-08 2015-10-05 Celgene Avilomics Res Inc Inhibidores de cinasas reguladas por señales extracelulares (erk) y sus usos.
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
EP2988749B1 (en) 2013-04-26 2019-08-14 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
WO2014176210A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
WO2015084622A1 (en) 2013-12-03 2015-06-11 Auspex Pharmaceuticals, Inc. Methods of manufacturing benzoquinoline compounds
SI3083648T1 (sl) 2013-12-20 2019-02-28 Rigel Pharmaceuticals, Inc., Farmacevtski postopek in vmesne spojine
US9822107B2 (en) 2013-12-20 2017-11-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2015095444A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2015094997A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2015131080A1 (en) 2014-02-28 2015-09-03 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2015138273A1 (en) 2014-03-13 2015-09-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
US10053455B2 (en) * 2014-03-24 2018-08-21 Ab Science Diazaspiroalkaneone-substituted oxazole derivatives as spleen tyrosine kinase inhibitors
CN117088931A (zh) 2014-08-12 2023-11-21 莫纳什大学 定向淋巴的前药
EP3179858B1 (en) 2014-08-13 2019-05-15 Celgene Car Llc Forms and compositions of an erk inhibitor
CN107148425B (zh) 2014-10-29 2021-08-03 拜斯科阿迪有限公司 对mt1-mmp特异性的双环肽配体
TWI788655B (zh) 2015-02-27 2023-01-01 美商林伯士拉克許米公司 酪胺酸蛋白質激酶2(tyk2)抑制劑及其用途
AU2016229949B2 (en) 2015-03-06 2021-04-08 Auspex Pharmaceuticals Llc Methods for the treatment of abnormal involuntary movement disorders
WO2016172053A1 (en) 2015-04-24 2016-10-27 Rigel Pharmaceuticals, Inc. Methods of treating ibrutinib-resistant disease
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
TWI707852B (zh) 2015-09-02 2020-10-21 美商林伯士拉克許米公司 Tyk2 抑制劑及其用途
US11738087B2 (en) 2015-09-08 2023-08-29 Monash University Lymph directing prodrugs
US10683308B2 (en) 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
AU2016342027B2 (en) 2015-10-23 2021-05-13 Navitor Pharmaceuticals, Inc. Modulators of Sestrin-GATOR2 interaction and uses thereof
EP3389664A4 (en) 2015-12-14 2020-01-08 Raze Therapeutics Inc. MTHFD2 CAFFEIN INHIBITORS AND USES THEREOF
RS61312B1 (sr) 2016-02-26 2021-02-26 Debiopharm Int Sa Lek za lečenje infekcija dijabetskog stopala
DK3426243T3 (da) 2016-03-09 2021-07-19 Raze Therapeutics Inc 3-phosphoglyceratdehydrogenase-inhibitorer og anvendelser deraf
EP4234552A3 (en) 2016-03-09 2023-10-18 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
CA3019394A1 (en) 2016-04-08 2017-10-12 X4 Pharmaceuticals, Inc. Methods for treating cancer
ES2870920T3 (es) 2016-06-21 2021-10-28 X4 Pharmaceuticals Inc Inhibidores de CXCR4 y usos de los mismos
CN109640988A (zh) 2016-06-21 2019-04-16 X4 制药有限公司 Cxcr4抑制剂及其用途
EP3472129A4 (en) 2016-06-21 2019-12-04 X4 Pharmaceuticals, Inc. CXCR4 INHIBITORS AND USES THEREOF
US10323036B2 (en) 2016-10-14 2019-06-18 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
EP3528816A4 (en) 2016-10-21 2020-04-08 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND USES THEREOF
WO2018089499A1 (en) 2016-11-08 2018-05-17 Navitor Pharmaceuticals, Inc. PHENYL AMINO PIPERIDINE mTORC INHIBITORS AND USES THEREOF
CA3043768A1 (en) 2016-11-29 2018-06-07 PureTech Health LLC Exosomes for delivery of therapeutic agents
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
WO2018115203A1 (en) 2016-12-23 2018-06-28 Bicyclerd Limited Peptide derivatives having novel linkage structures
US10624968B2 (en) 2017-01-06 2020-04-21 Bicyclerd Limited Compounds for treating cancer
TW202515876A (zh) 2017-03-08 2025-04-16 日商武田藥品工業股份有限公司 Tyk2抑制劑及其用途
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
WO2018191146A1 (en) 2017-04-10 2018-10-18 Navitor Pharmaceuticals, Inc. Heteroaryl rheb inhibitors and uses thereof
PL3615019T3 (pl) 2017-04-26 2026-01-19 Navitor Pharmaceuticals, Inc. Modulator interakcji sestryna-gator2 do zastosowania w leczeniu depresji opornej na leczenie
US10857196B2 (en) 2017-04-27 2020-12-08 Bicycletx Limited Bicyclic peptide ligands and uses thereof
EP3645549A1 (en) 2017-06-26 2020-05-06 BicycleRD Limited Bicyclic peptide ligands with detectable moieties and uses thereof
SI3658557T1 (sl) 2017-07-28 2024-10-30 Takeda Pharmaceutical Company Limited Zaviralci TYK2 in njihova uporaba
JP7670481B2 (ja) 2017-08-04 2025-04-30 バイスクルテクス・リミテッド Ｃｄ１３７に対して特異的な二環式ペプチドリガンド
WO2019034868A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited CONJUGATES PEPTIDE BICYCLIC-LIGAND PPR-A AND USES THEREOF
WO2019034866A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited BICYCLIC PEPTIDE LIGANDS CONJUGATES AND USES THEREOF
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
CA3077739A1 (en) 2017-08-29 2019-03-07 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
US11358948B2 (en) 2017-09-22 2022-06-14 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
WO2019060742A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc AGENTS FOR DEGRADING PROTEINS AND USES THEREOF
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. MYCOPHENOLIC ACID LIPID PRODRUGS AND THEIR USES
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2019140387A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
JP7229257B2 (ja) 2018-01-29 2023-02-28 メルク パテント ゲーエムベーハー Ｇｃｎ２阻害剤およびその使用
BR112020015396A2 (pt) 2018-01-29 2020-12-08 Merck Patent Gmbh Inididores de gcn2 e usos dos mesmos
CN111902429A (zh) 2018-02-23 2020-11-06 拜斯科技术开发有限公司 多聚体双环肽配体
EP3759086A1 (en) 2018-02-27 2021-01-06 Artax Biopharma Inc. Chromene derivatives as inhibitors of tcr-nck interaction
HRP20241163T1 (hr) 2018-04-24 2024-11-22 Merck Patent Gmbh Antiproliferacijski spojevi i njihova uporaba
ES2969982T3 (es) 2018-04-24 2024-05-23 Vertex Pharma Compuestos de pteridinona y usos de los mismos
WO2019241789A1 (en) 2018-06-15 2019-12-19 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
IL279489B2 (en) 2018-06-22 2025-10-01 Bicycletx Ltd Bicyclic peptide ligands specific for nectin-4, a drug conjugate containing the peptide ligands and a pharmaceutical composition containing the drug conjugate
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
WO2020010177A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Tricyclic crbn ligands and uses thereof
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
WO2020051424A1 (en) 2018-09-07 2020-03-12 Pic Therapeutics Eif4e inhibitors and uses thereof
CN113271940A (zh) 2018-10-15 2021-08-17 林伯士拉克许米公司 Tyk2抑制剂和其用途
WO2020084305A1 (en) 2018-10-23 2020-04-30 Bicycletx Limited Bicyclic peptide ligands and uses thereof
EP3870158A4 (en) 2018-10-24 2022-08-10 Navitor Pharmaceuticals, Inc. Polymorphic compounds and uses thereof
WO2020092845A1 (en) 2018-11-01 2020-05-07 Rigel Pharmaceuticals, Inc. Method and composition embodiments for treating acute myeloid leukemia
CA3119773A1 (en) 2018-11-30 2020-06-04 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CA3120866A1 (en) 2018-11-30 2020-06-04 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
GB201820288D0 (en) 2018-12-13 2019-01-30 Bicycle Tx Ltd Bicycle peptide ligaands specific for MT1-MMP
GB201820325D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for psma
GB201820295D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for MT1-MMP
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
WO2020128527A1 (en) 2018-12-21 2020-06-25 Bicyclerd Limited Bicyclic peptide ligands specific for pd-l1
US12492224B2 (en) 2018-12-21 2025-12-09 Bicycletx Limited Bicyclic peptide ligands specific for PD-L1
CN113348021B (zh) 2019-01-23 2025-07-11 武田药品工业株式会社 Tyk2抑制剂和其用途
TN2021000159A1 (en) 2019-02-14 2023-04-04 Debiopharm Int Sa Afabicin formulation, method for making the same and uses thereof
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
SG11202110828UA (en) 2019-04-02 2021-10-28 Bicycletx Ltd Bicycle toxin conjugates and uses thereof
CN120574283A (zh) 2019-04-05 2025-09-02 凯麦拉医疗公司 Stat降解剂和其用途
CA3141826A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
WO2020251972A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
SG11202113174SA (en) 2019-06-14 2021-12-30 Debiopharm Int Sa Medicament and use thereof for treating bacterial infections involving biofilm
PH12022500002A1 (en) 2019-06-28 2023-04-03 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
TWI860386B (zh) 2019-07-30 2024-11-01 英商拜西可泰克斯有限公司 異質雙環肽複合物
EP4013420B1 (en) 2019-08-14 2023-11-01 Rigel Pharmaceuticals, Inc. Method of blocking or ameliorating cytokine release syndrome
US11845724B2 (en) 2019-09-11 2023-12-19 Vincere Biosciences, Inc. USP30 inhibitors and uses thereof
MX2022002877A (es) 2019-09-13 2022-08-08 Nimbus Saturn Inc Antagonistas de cinasa progenitora hematopoyetica 1 (hpk1) y sus usos.
US11723890B2 (en) 2019-11-01 2023-08-15 Navitor Pharmaceuticals, Inc. Methods of treatment using an mTORC1 modulator
AU2020397938A1 (en) 2019-12-05 2022-06-23 Janssen Pharmaceutica Nv Rapamycin analogs and uses thereof
WO2021119159A1 (en) 2019-12-10 2021-06-17 Kymera Therapeutics, Inc. Irak degraders and uses thereof
KR20220145325A (ko) 2019-12-17 2022-10-28 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
WO2021133917A1 (en) 2019-12-23 2021-07-01 Kymera Therapeutics, Inc. Smarca inhibitors and uses thereof
EP4081308A4 (en) 2019-12-23 2024-01-24 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
IL295362A (en) 2020-02-05 2022-10-01 Puretech Lyt Inc Lipid drug inhibitors of neurosteroids
TW202146393A (zh) 2020-03-03 2021-12-16 美商皮克醫療公司 Eif4e抑制劑及其用途
KR20230005160A (ko) 2020-03-19 2023-01-09 카이메라 쎄라퓨틱스 인코포레이티드 Mdm2 분해제 및 이의 용도
US20230250110A1 (en) 2020-06-03 2023-08-10 Kymera Therapeutics, Inc. Deuterated irak degraders and uses thereof
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
AU2021322934A1 (en) 2020-08-03 2023-03-30 Bicycletx Limited Peptide-based linkers
CA3186504A1 (en) 2020-08-17 2022-02-24 Stephen J. Blakemore Bicycle conjugates specific for nectin-4 and uses thereof
US12331046B2 (en) 2020-10-23 2025-06-17 Nimbus Clotho, Inc. CTPS1 inhibitors and uses thereof
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CA3200814A1 (en) 2020-12-02 2022-06-09 Alfredo C. Castro Tead inhibitors and uses thereof
EP4259144A4 (en) 2020-12-09 2025-08-20 Kymera Therapeutics Inc SMARCA DEGRADING AGENTS AND THEIR USES
CN116867758A (zh) 2020-12-30 2023-10-10 凯麦拉医疗公司 Irak降解剂和其用途
MX2023009060A (es) 2021-02-02 2023-09-29 Liminal Biosciences Ltd Antagonistas de gpr84 y usos de estos.
US12378229B2 (en) 2021-02-02 2025-08-05 Liminal Biosciences Limited GPR84 antagonists and uses thereof
EP4291235A4 (en) 2021-02-12 2025-01-08 Nimbus Saturn, Inc. HPK1 ANTAGONISTS AND USES THEREOF
US12171768B2 (en) 2021-02-15 2024-12-24 Kymera Therapeutics, Inc. IRAK4 degraders and uses thereof
CN116867494A (zh) 2021-02-15 2023-10-10 凯麦拉医疗公司 Irak4降解剂和其用途
US11926625B2 (en) 2021-03-05 2024-03-12 Nimbus Saturn, Inc. HPK1 antagonists and uses thereof
WO2022213062A1 (en) 2021-03-29 2022-10-06 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
US12325697B2 (en) 2021-04-09 2025-06-10 Nimbus Clio, Inc. CBL-B modulators and uses thereof
WO2022221866A1 (en) 2021-04-16 2022-10-20 Ikena Oncology, Inc. Mek inhibitors and uses thereof
KR20240020735A (ko) 2021-05-07 2024-02-15 카이메라 쎄라퓨틱스 인코포레이티드 Cdk2 분해제 및 그 용도
CN113624665A (zh) * 2021-07-30 2021-11-09 中国药科大学 一种抗肿瘤候选化合物在治疗结直肠癌药物中的应用及测定方法
CA3229560A1 (en) 2021-08-25 2023-03-02 Christopher L. Vandeusen Eif4e inhibitors and uses thereof
US12157732B2 (en) 2021-08-25 2024-12-03 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
CA3236265A1 (en) 2021-10-29 2023-05-04 William Leong Irak4 degraders and synthesis thereof
AU2022379973A1 (en) 2021-11-08 2024-06-27 Progentos Therapeutics, Inc. Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CA3243560A1 (en) 2022-01-31 2023-08-03 Kymera Therapeutics, Inc. Iraqi Degradation Agents and Their Uses
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
US11878958B2 (en) 2022-05-25 2024-01-23 Ikena Oncology, Inc. MEK inhibitors and uses thereof
US20260028330A1 (en) 2022-08-02 2026-01-29 Liminal Biosciences Limited Heteroaryl carboxamide and related gpr84 antagonists and uses thereof
IL318577A (en) 2022-08-02 2025-03-01 Liminal Biosciences Ltd ARYL-TRIAZOLYL AND RELATED GPR84 ANTAGONISTS AND THEIR USES
KR20250056924A (ko) 2022-08-02 2025-04-28 리미널 바이오사이언시스 리미티드 치환된 피리돈 gpr84 길항제 및 이의 용도
WO2024112894A1 (en) 2022-11-22 2024-05-30 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
AU2024312190A1 (en) 2023-06-23 2025-07-03 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CN119431398A (zh) * 2023-07-31 2025-02-14 中国科学院上海有机化学研究所 R406及其衍生物协同trail的抗肿瘤应用
AU2024344754A1 (en) 2023-09-21 2026-04-02 Takeda Pharmaceutical Company Limited Tyk2 inhibitors for use in the treatment of inflammatory bowel disease
CN118702735B (zh) * 2024-07-15 2025-12-30 河北常山生化药业股份有限公司 福坦替尼杂质及其制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2135481C1 (ru) * 1992-03-31 1999-08-27 Агурон Фармасьютикалз, Инк. Хиназолиновые соединения или их фармацевтически приемлемые соли и фармацевтическая композиция

Family Cites Families (150)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1029650B (de) 1954-03-15 1958-05-08 Franz Litzka Zusatzeinrichtung fuer Schneidmotoren
GR80171B (en) 1983-08-29 1985-01-02 Ciba Geigy Ag N-(2-nitrophenyl)-4-aminopyrimidine derivatives process for the preparation thereof and use
DE3618353A1 (de) 1986-05-31 1987-12-03 Hoechst Ag Schaedlingsbekaempfungsmittel auf der basis von aminopyrimidin-derivaten sowie neue aminopyrimidin-verbindungen
JPS6312485A (ja) 1986-06-25 1988-01-19 日立米沢電子株式会社 トレ−
IE63502B1 (en) 1989-04-21 1995-05-03 Zeneca Ltd Aminopyrimidine derivatives useful for treating cardiovascular disorders
JPH03127790A (ja) 1989-10-11 1991-05-30 Morishita Pharmaceut Co Ltd Ｎ―（１ｈ―テトラゾール―５―イル）―２―アニリノ―５―ピリミジンカルボキシアミド類及びその合成中間体
TW224941B (https=) 1989-11-08 1994-06-11 Yamanouchi Pharma Co Ltd
GB9012592D0 (en) 1990-06-06 1990-07-25 Smithkline Beecham Intercredit Compounds
DE4029650A1 (de) 1990-09-19 1992-03-26 Hoechst Ag 2-anilino-pyrimidine, verfahren zu ihrer herstellung, sie enthaltene mittel und ihre verwendung als fungizide
US5728536A (en) 1993-07-29 1998-03-17 St. Jude Children's Research Hospital Jak kinases and regulation of Cytokine signal transduction
BR9407799A (pt) 1993-10-12 1997-05-06 Du Pont Merck Pharma Composição de matéria método de tratamento e composição farmaceutica
IL112290A (en) 1994-01-12 1999-01-26 Novartis Ag Transformed aryl and the troiryl pyrimidines and herbicides containing them
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
TW440563B (en) 1996-05-23 2001-06-16 Hoffmann La Roche Aryl pyrimidine derivatives and a pharmaceutical composition thereof
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
US6004985A (en) 1996-10-09 1999-12-21 Berlex Laboratories, Inc. Thio acid derived monocylic N-heterocyclics as anticoagulants
GB9705361D0 (en) 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
US6093820A (en) 1997-10-02 2000-07-25 Taro Pharmaceutical Industries Ltd. Method and reagents for N-alkylating ureides
GB9723859D0 (en) 1997-11-12 1998-01-07 Zeneca Ltd Compound,composition and use
EP1054004B1 (en) 1997-12-15 2008-07-16 Astellas Pharma Inc. Novel pyrimidine-5-carboxamide derivatives
US6436989B1 (en) * 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
AU754965B2 (en) 1997-12-31 2002-11-28 University Of Kansas, The Water soluble prodrugs of tertiary amine containing drugs and methods of making thereof
EA200000840A1 (ru) 1998-02-17 2001-02-26 Туларик, Инк. Антивирусные производные пиримидина
EA002973B1 (ru) 1998-03-27 2002-12-26 Янссен Фармацевтика Н.В. Производные пиримидина в качестве ингибиторов репликации вируса иммунодефицита человека
KR100643419B1 (ko) 1998-03-27 2006-11-10 얀센 파마슈티카 엔.브이. Ｈｉｖ를 억제하는 피리미딘 유도체
ATE342892T1 (de) 1998-08-29 2006-11-15 Astrazeneca Ab Pyrimidine verbindungen
DE19851421A1 (de) 1998-11-07 2000-05-11 Boehringer Ingelheim Pharma Neue Pyrimidine, deren Herstellung und Verwendung
SK287270B6 (sk) 1998-11-10 2010-05-07 Janssen Pharmaceutica N. V. Derivát pyrimidínu
US6127376A (en) 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
DE19917785A1 (de) 1999-04-20 2000-10-26 Bayer Ag 2,4-Diamino-pyrimidin-Derivate
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
DE19945982A1 (de) 1999-09-24 2001-03-29 Knoll Ag Geschwindigkeitsbestimmte Partikel
TR200200763T2 (tr) 1999-09-24 2003-09-22 Janssen Pharmaceutica N.V. Antiviral bileşimler
PL354784A1 (en) 1999-09-30 2004-02-23 Neurogen Corporation Certain alkylene diamine-substituted heterocycles
WO2001030782A2 (en) 1999-10-29 2001-05-03 Syngenta Participations Ag Novel herbicides
EP1246823A1 (en) 1999-12-28 2002-10-09 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
US6362172B2 (en) 2000-01-20 2002-03-26 Bristol-Myers Squibb Company Water soluble prodrugs of azole compounds
AU3704101A (en) 2000-02-17 2001-08-27 Amgen Inc Kinase inhibitors
GB0004886D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US6525051B2 (en) 2000-03-27 2003-02-25 Schering Aktiengesellschaft N-heterocyclic derivatives as NOS inhibitors
KR20020093966A (ko) * 2000-04-27 2002-12-16 바실리어 파마슈티카 아게 항균제로서의 크로메닐메틸 피리미딘디아민
AU783981C (en) 2000-05-08 2007-05-03 Janssen Pharmaceutica N.V. HIV replication inhibitors
AU782948B2 (en) 2000-05-08 2005-09-15 Janssen Pharmaceutica N.V. Prodrugs of HIV replication inhibiting pyrimidines
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
WO2002022605A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6448401B1 (en) 2000-11-20 2002-09-10 Bristol-Myers Squibb Company Process for water soluble azole compounds
US6989385B2 (en) 2000-12-21 2006-01-24 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
BR0116452A (pt) 2000-12-21 2003-09-30 Glaxo Group Ltd Composto, composição farmacêutica, uso de um composto
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
ES2316546T3 (es) 2001-02-20 2009-04-16 Astrazeneca Ab 2-arilamino-pirimidinas para el tratamiento de trastornos asociados a gsk3.
BR0209774A (pt) 2001-05-29 2004-06-01 Schering Ag Pirimidinas inibidoras de cdk, sua preparação e aplicação como medicamento
CA2450769A1 (en) 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
CA2450934A1 (en) 2001-06-19 2002-12-27 Marco Dodier Pyrimidine inhibitors of phosphodiesterase (pde) 7
AU2002315388A1 (en) 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel phenylamino-pyrimidines and uses thereof
AU2002316421B2 (en) 2001-06-26 2008-05-15 Bristol-Myers Squibb Company N-heterocyclic inhibitors of TNF-ALPHA expression
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
WO2003026664A1 (en) 2001-09-26 2003-04-03 Bayer Corporation 2-phenylamino-4- (5-pyrazolylamino) -pyramidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
WO2003040141A1 (en) 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
WO2003032994A2 (de) 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg 5-substituierte 4-amino-2-phenylamino-pyrimidinderivate und ihre verwendung als beta-amyloid modulatoren
ATE407678T1 (de) 2001-10-17 2008-09-15 Boehringer Ingelheim Pharma Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
JP2003127790A (ja) 2001-10-25 2003-05-08 Nippon Soken Inc メータ装置
KR101031720B1 (ko) 2001-11-28 2011-04-29 비티지 인터내셔널 리미티드 질소함유 헤테로아릴 화합물을 함유하는 알츠하이머병의예방약 또는 치료약 또는 아밀로이드 단백질 섬유화억제제
SE0104140D0 (sv) 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
WO2003055489A1 (en) 2001-12-21 2003-07-10 Bayer Pharmaceuticals Corporation 2,4-diamino-pyrimidine derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
EP1470121B1 (en) 2002-01-23 2012-07-11 Bayer HealthCare LLC Pyrimidine derivatives as rho-kinase inhibitors
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US6998391B2 (en) 2002-02-07 2006-02-14 Supergen.Inc. Method for treating diseases associated with abnormal kinase activity
AU2003209077A1 (en) 2002-02-08 2003-09-02 Smithkline Beecham Corporation Pyrimidine compounds
AU2003220970A1 (en) 2002-03-01 2003-09-16 Smithkline Beecham Corporation Diamino-pyrimidines and their use as angiogenesis inhibitors
EP1483260A1 (de) 2002-03-11 2004-12-08 Schering Aktiengesellschaft Cdk inhibitorische 2-heteroaryl-pyrimidine, deren herstellung und verwendung als arzneimittel
US7288547B2 (en) 2002-03-11 2007-10-30 Schering Ag CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
GEP20074230B (en) 2002-03-20 2007-11-12 Bristol Myers Squibb Co Phosphate prodrugs of fluorooxindoles
AU2003301758A1 (en) 2002-05-06 2004-05-25 Bayer Pharmaceuticals Corporation Use of pyrimidine derivates for the manifacture of a medicament for the treatment of hyper-proliferative disorders
WO2003095448A1 (en) 2002-05-06 2003-11-20 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
AR039540A1 (es) 2002-05-13 2005-02-23 Tibotec Pharm Ltd Compuestos microbicidas con contenido de pirimidina o triazina
JP2005528443A (ja) 2002-05-30 2005-09-22 バーテックス　ファーマシューティカルズ　インコーポレイテッド Ｊａｋキナーゼおよびｃｄｋ２プロテインキナーゼのインヒビター
CA2489648A1 (en) 2002-06-17 2003-12-24 Smithkline Beecham Corporation Chemical process
EP1518855B1 (en) 2002-06-28 2011-10-26 Astellas Pharma Inc. Diaminopyrimidinecarboxa mide derivative
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
AU2003249539A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Cyclic compounds containing zinc binding groups as matrix metalloproteinase inhibitors
AU2003262642B2 (en) 2002-08-14 2010-06-17 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
AU2003286876A1 (en) 2002-11-01 2004-06-07 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
EP1560824A1 (en) 2002-11-05 2005-08-10 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
JP2006508997A (ja) 2002-11-28 2006-03-16 シエーリング アクチエンゲゼルシャフト Ｃｈｋ−、Ｐｄｋ−およびＡｋｔ−阻害性ピリミジン、それらの製造および薬剤としての使用
WO2004050068A1 (en) 2002-11-29 2004-06-17 Janssen Pharmaceutica N.V. Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base
JPWO2004054617A1 (ja) 2002-12-13 2006-04-20 協和醗酵工業株式会社 中枢疾患の予防および／または治療剤
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
BRPI0407329A (pt) 2003-02-07 2006-01-10 Janssen Pharmaceutica Nv Derivados de pirimidina para a prevenção de infecção de hiv
ES2325440T3 (es) 2003-02-20 2009-09-04 Smithkline Beecham Corporation Compuestos de pirimidina.
CL2004000306A1 (es) 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidina sustituidas con indano; proceso para su preparacion; composicion farmaceutica que lo comprende; combinacion farmaceutica; y su uso para el tratamiento o profilaxis de una enfermedad infecciosa.
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
MXPA05011523A (es) 2003-04-30 2006-01-23 Inst For Pharm Discovery Inc Heteroarilos sustituidos como inhibidores de proteinas de tirosina fosfatasas.
GB0311276D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
EP1651595A2 (en) 2003-05-30 2006-05-03 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
WO2005009980A1 (en) 2003-07-22 2005-02-03 Neurogen Corporation Substituted pyridin-2-ylamine analogues
US7442698B2 (en) 2003-07-24 2008-10-28 Amgen Inc. Substituted heterocyclic compounds and methods of use
WO2005012294A1 (en) 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
EP1648875A1 (en) 2003-07-30 2006-04-26 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
ATE506953T1 (de) 2003-08-07 2011-05-15 Rigel Pharmaceuticals Inc 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
PT1660458E (pt) 2003-08-15 2012-04-27 Novartis Ag 2,4-pirimidinodiaminas úteis no tratamento de doenças neoplásicas, desordens inflamatórias e do sistema imunitário
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
US20070105839A1 (en) 2003-09-18 2007-05-10 Patricia Imbach 2, 4-Di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
DE10349423A1 (de) 2003-10-16 2005-06-16 Schering Ag Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
PE20051046A1 (es) 2003-11-28 2006-01-11 Novartis Ag Derivados de diaril-urea en el tratamiento de enfermedades dependientes de la quinasa de proteina
MY141255A (en) 2003-12-11 2010-03-31 Memory Pharm Corp Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs
WO2005063722A1 (en) 2003-12-19 2005-07-14 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
US7745625B2 (en) 2004-03-15 2010-06-29 Bristol-Myers Squibb Company Prodrugs of piperazine and substituted piperidine antiviral agents
US7754714B2 (en) 2004-05-18 2010-07-13 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
US20060047135A1 (en) 2004-08-30 2006-03-02 Chadwick Scott T Process for preparing chloromethyl di-tert-butylphosphate
JP2008511659A (ja) 2004-09-01 2008-04-17 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物の合成
EP1794134A1 (de) 2004-09-29 2007-06-13 Bayer Schering Pharma Aktiengesellschaft Substituierte 2-anilinopyrimidine als zellzyklus -kinase oder rezeptortyrosin-kinase inhibitoren, deren herstellung und verwendung als arzneimittel
CA2584808A1 (en) 2004-10-29 2006-05-11 Rigel Pharmaceuticals, Inc. Substituted pyridines with activity on syk kinase
SI1814878T1 (sl) 2004-11-24 2012-06-29 Rigel Pharmaceuticals Inc Spojine spiro-2,4-pirimidindiamina in njihova uporaba
US7442716B2 (en) 2004-12-17 2008-10-28 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
ATE519759T1 (de) 2004-12-30 2011-08-15 Exelixis Inc Pyrimidinderivate als kinasemodulatoren und anwendungsverfahren
AU2006206458B2 (en) * 2005-01-19 2012-10-25 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
EP1883302A4 (en) 2005-05-03 2009-05-20 Rigel Pharmaceuticals Inc JAK KINASE HEMMER AND ITS USE
BRPI0610876B8 (pt) 2005-06-08 2021-05-25 Rigel Pharmaceuticals Inc composto, formulação farmacêutica, e métodos de inibir uma atividade de uma jak cinase, e de inibir uma cascata de transdução de sinal em que jak3 cinase desempenha um papel
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
JP2008543855A (ja) 2005-06-13 2008-12-04 ライジェル ファーマシューティカルズ， インコーポレイテッド 変形性骨疾患を処置するための方法および組成物
EP1904479A2 (fr) 2005-07-11 2008-04-02 Sanofi-Aventis Nouveaux derives de 2,4-dianilinopyrimidines, leur preparation, a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
ES2344275T3 (es) 2005-07-28 2010-08-23 Intervet International Bv Nuevos (tio) carbamatos de benzimidazol con actividad antiparasitaria y sintesis de ellos.
JP4981673B2 (ja) 2005-09-13 2012-07-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物およびその製造方法
US7508791B2 (en) 2005-10-31 2009-03-24 Kyocera Corporation Wireless communication coding and transmission systems and methods
WO2007053844A2 (en) 2005-10-31 2007-05-10 Rigel Pharmaceuticals, Inc. Compositions and methods for treating inflammatory disorders
US20070098828A1 (en) 2005-11-01 2007-05-03 Gonzalez-Villasenor Lucia I Methods and compositions for the prevention and regression of neovascularization
JP5191391B2 (ja) 2005-11-01 2013-05-08 ターゲジェン インコーポレーティッド キナーゼのビ−アリールメタ−ピリミジン阻害剤
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
WO2007085540A1 (en) 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
US7659280B2 (en) 2006-02-17 2010-02-09 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
ES2622493T3 (es) 2006-02-24 2017-07-06 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta de JAK
US7631707B2 (en) * 2006-03-29 2009-12-15 Cyrus Solutions Corporation Shape memory alloy actuated steerable drilling tool
US20090192158A1 (en) 2006-05-02 2009-07-30 Stacia Kargman Methods for Treating or Preventing Neoplasias
US7776855B2 (en) 2006-07-27 2010-08-17 Janssen Pharmaceutica N.V. Antimicrobial oxazolidinone prodrugs
JP5161233B2 (ja) 2006-10-19 2013-03-13 ライジェル ファーマシューティカルズ， インコーポレイテッド 自己免疫疾患の処置のためのｊａｋキナーゼの阻害剤としての２，４−ピリミジンアミン誘導体
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US9815606B2 (en) 2015-04-29 2017-11-14 Barton Group, Inc. Flexible stand-up pouch container for flowable products

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2135481C1 (ru) * 1992-03-31 1999-08-27 Агурон Фармасьютикалз, Инк. Хиназолиновые соединения или их фармацевтически приемлемые соли и фармацевтическая композиция

Also Published As

Publication number Publication date
AU2006206458A1 (en) 2006-07-27
MX2007007189A (es) 2010-09-28
DK1856135T3 (da) 2010-04-12
FR20C1019I1 (https=) 2020-07-17
US20060211657A1 (en) 2006-09-21
EP1856135A1 (en) 2007-11-21
NL301039I1 (nl) 2020-04-29
KR20070098926A (ko) 2007-10-05
ATE451381T1 (de) 2009-12-15
NO2020010I1 (no) 2020-05-13
WO2006078846A1 (en) 2006-07-27
PL1856135T3 (pl) 2010-05-31
CA2591948C (en) 2013-11-12
US20170291909A1 (en) 2017-10-12
US8211888B2 (en) 2012-07-03
US7538108B2 (en) 2009-05-26
US20200270271A1 (en) 2020-08-27
US8476263B2 (en) 2013-07-02
US10577381B2 (en) 2020-03-03
US7449458B2 (en) 2008-11-11
JP2011236234A (ja) 2011-11-24
KR101278397B1 (ko) 2013-06-25
US8785437B2 (en) 2014-07-22
US9532998B2 (en) 2017-01-03
IL183890A (en) 2012-04-30
HUS2000011I1 (hu) 2020-06-29
CY2020012I1 (el) 2020-11-25
RU2007131430A (ru) 2009-02-27
US20090124580A1 (en) 2009-05-14
CY2020012I2 (el) 2020-11-25
BRPI0606318B8 (pt) 2021-05-25
LTPA2020507I1 (lt) 2020-06-25
LUC00153I2 (https=) 2021-02-15
AU2006206458B2 (en) 2012-10-25
US7989448B2 (en) 2011-08-02
NO339146B1 (no) 2016-11-14
ES2337496T3 (es) 2010-04-26
US20160136191A1 (en) 2016-05-19
CA2591948A1 (en) 2006-07-27
MX346822B (es) 2017-03-28
JP2008527048A (ja) 2008-07-24
US20190292197A1 (en) 2019-09-26
IL183890A0 (en) 2007-10-31
US8211889B2 (en) 2012-07-03
DE602006010979D1 (de) 2010-01-21
FIC20200014I1 (fi) 2020-05-19
EP2161275A1 (en) 2010-03-10
EP1856135B1 (en) 2009-12-09
BE2020C511I2 (https=) 2025-09-05
BRPI0606318B1 (pt) 2021-02-02
US20110319613A1 (en) 2011-12-29
CN101115761B (zh) 2012-07-18
US20120232036A1 (en) 2012-09-13
PT1856135E (pt) 2010-02-26
HK1108896A1 (en) 2008-05-23
SI1856135T1 (sl) 2010-04-30
CN101115761A (zh) 2008-01-30
NZ555947A (en) 2010-11-26
LTC1856135I2 (lt) 2021-07-12
CY1109888T1 (el) 2014-09-10
US20120108810A1 (en) 2012-05-03
FR20C1019I2 (fr) 2021-10-15
US20140357598A1 (en) 2014-12-04
NO20074179L (no) 2007-10-18
US20060234983A1 (en) 2006-10-19
US9266912B2 (en) 2016-02-23
LUC00153I1 (https=) 2020-05-08
US20130338357A1 (en) 2013-12-19
US7563892B1 (en) 2009-07-21
BRPI0606318A2 (pt) 2009-06-16
JP4801096B2 (ja) 2011-10-26
NL301039I2 (nl) 2020-05-12

Similar Documents

Publication Publication Date Title
RU2416616C2 (ru) Пролекарства соединений 2,4-пиримидиндиамина и их применения
USRE48898E1 (en) Prodrugs of 2,4-pyrimidinediamine compounds and their uses
HK1142079A (en) Prodrugs of 2,4-pyrimidinediamine compounds and their uses
HK1108896B (en) Prodrugs of 2,4-pyrimidinediamine compounds and their uses