JP4801096B2 - ２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用 - Google Patents

２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用 Download PDF

Info

Publication number
JP4801096B2
JP4801096B2 JP2007552272A JP2007552272A JP4801096B2 JP 4801096 B2 JP4801096 B2 JP 4801096B2 JP 2007552272 A JP2007552272 A JP 2007552272A JP 2007552272 A JP2007552272 A JP 2007552272A JP 4801096 B2 JP4801096 B2 JP 4801096B2
Authority
JP
Japan
Prior art keywords
compound
prodrugs
prodrug
phosphate
pharmaceutically acceptable
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2007552272A
Other languages
English (en)
Japanese (ja)
Other versions
JP2008527048A (ja
Inventor
ラジンダー シン，
ソマセカール バーミディパティ，
エステバン マスダ，
ヴァレンティーノ ジェー． ステラ，
トーマス サン，
Original Assignee
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
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=JP4801096(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 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 filed Critical 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
Publication of JP2008527048A publication Critical patent/JP2008527048A/ja
Application granted granted Critical
Publication of JP4801096B2 publication Critical patent/JP4801096B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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
    • 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
    • C07F9/6564—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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
JP2007552272A 2005-01-19 2006-01-19 ２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用 Active JP4801096B2 (ja)

Applications Claiming Priority (5)

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
PCT/US2006/001945 WO2006078846A1 (en) 2005-01-19 2006-01-19 Prodrugs of 2,4-pyrimidinediamine compounds and their uses

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2011152261A Division JP2011236234A (ja) 2005-01-19 2011-07-08 ２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用

Publications (2)

Publication Number Publication Date
JP2008527048A JP2008527048A (ja) 2008-07-24
JP4801096B2 true JP4801096B2 (ja) 2011-10-26

Family

ID=36295425

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2007552272A Active JP4801096B2 (ja) 2005-01-19 2006-01-19 ２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用
JP2011152261A Pending JP2011236234A (ja) 2005-01-19 2011-07-08 ２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2011152261A Pending JP2011236234A (ja) 2005-01-19 2011-07-08 ２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用

Country Status (27)

Country Link
US (13) US7449458B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (2) EP1856135B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (2) JP4801096B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
KR (1) KR101278397B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (1) CN101115761B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AT (1) ATE451381T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (1) AU2006206458B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (1) BRPI0606318B8 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2591948C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CY (2) CY1109888T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DE (1) DE602006010979D1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DK (1) DK1856135T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ES (1) ES2337496T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
FI (1) FIC20200014I1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HU (1) HUS2000011I1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (1) IL183890A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
LT (1) LTC1856135I2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
LU (1) LUC00153I2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (2) MX2007007189A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NL (1) NL301039I2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NO (2) NO339146B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NZ (1) NZ555947A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PL (1) PL1856135T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PT (1) PT1856135E (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
RU (1) RU2416616C2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SI (1) SI1856135T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2006078846A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010510322A (ja) * 2006-11-21 2010-04-02 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プロドラッグ塩およびそれらの使用

Families Citing this family (229)

* 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
NZ537752A (en) * 2002-07-29 2006-12-22 Rigel Pharmaceuticals Inc Use of 2,4-pyrimidinediamine compounds in the preparation of medicaments for treating autoimmune diseases
JP4939220B2 (ja) * 2003-05-15 2012-05-23 アークル インコーポレイテッド ｐ３８の阻害物質としてのイミダゾチアゾール類およびイミダゾオキサゾール誘導体
ES2421139T3 (es) * 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
WO2005118544A2 (en) 2004-05-18 2005-12-15 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
JP2008517064A (ja) * 2004-10-19 2008-05-22 アークル インコーポレイテッド Ｐ３８ｍａｐキナーゼのイミダゾオキサゾールおよびイミダゾチアゾール阻害剤の合成
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
JP5095409B2 (ja) 2004-11-24 2012-12-12 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 スピロ２，４−ピリミジンジアミン化合物およびその使用
MX2007007189A (es) 2005-01-19 2010-09-28 Rigel Pharmaceuticals Inc Prodrogas de compuestos de 2,4-pirimidindiamina y sus usos.
US8227455B2 (en) 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
CA2604551A1 (en) * 2005-05-03 2007-03-08 Rigel Pharmaceuticals, Inc. Jak kinase inhibitors and their uses
MX286273B (es) * 2005-06-08 2011-05-04 Rigel Pharmaceuticals Inc Composiciones y metodos para inhibicion de la via jak.
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
ES2279500T3 (es) * 2005-06-17 2007-08-16 Magneti Marelli Powertrain S.P.A. Inyector de carburante.
US20090306028A1 (en) * 2005-10-31 2009-12-10 Payan Donald G Compositions and methods for treating inflammatory disorders
US20100041678A1 (en) * 2005-10-31 2010-02-18 Rigel Pharmaceuticals, Inc. 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
SI1984357T1 (sl) * 2006-02-17 2014-02-28 Rigel Pharmaceuticals, Inc. Spojine 2,4-pirimidindiamina za zdravljenje ali preventivo avtoimunih bolezni
WO2007098507A2 (en) * 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
EP2013218A2 (en) * 2006-04-17 2009-01-14 Arqule, Inc. Raf inhibitors and their uses
WO2008009122A1 (en) 2006-07-20 2008-01-24 Affinium Pharmaceuticals, Inc. Acrylamide derivatives as fab i inhibitors
CA2673125C (en) 2006-10-19 2015-04-21 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2008061201A1 (en) * 2006-11-15 2008-05-22 Rigel Pharmaceuticals, Inc. Methods for treating renal tumors using 2,4-pyrimidinediamine drug and prodrug compounds
US7947698B2 (en) 2007-03-23 2011-05-24 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
US20090012045A1 (en) * 2007-06-26 2009-01-08 Rigel Pharmaceuticals, Inc. Methods of 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
WO2009029682A1 (en) * 2007-08-28 2009-03-05 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
HRP20181174T1 (hr) * 2007-11-07 2018-09-21 Rigel Pharmaceuticals, Inc. Mokro granuliranje korištenjem sekvestranta za vodu
DK2265607T3 (en) 2008-02-15 2017-03-13 Rigel Pharmaceuticals Inc PYRIMIDIN-2-AMINE COMPOUNDS AND THEIR USE AS INHIBITORS OF JAK KINASES
ES2610880T3 (es) * 2008-02-22 2017-05-03 Rigel Pharmaceuticals, Inc. Uso de 2,4-pirimidinadiaminas para el tratamiento de la aterosclerosis
MX2010011463A (es) 2008-04-16 2011-06-03 Portola Pharm Inc 2,6-diamino-pirimidin-5-il-carboxamidas como inhibidores de syk o jak quinasas.
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
CA2723185A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
NO2300013T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) * 2008-05-21 2018-02-03
AU2013205506B2 (en) * 2008-05-21 2016-04-21 Takeda Pharmaceutical Company Limited Phosphorous derivatives as kinase inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
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
EP2361248B1 (en) 2008-06-27 2018-09-19 Celgene CAR LLC Heteroaryl compounds and uses thereof
EA018024B1 (ru) 2008-07-28 2013-04-30 Пфайзер Инк. Фенантреноновые соединения, композиции и способы
JPWO2010027002A1 (ja) * 2008-09-05 2012-02-02 塩野義製薬株式会社 Ｐｉ３ｋ阻害活性を有する縮環モルホリン誘導体
DK2326643T3 (da) 2008-09-18 2013-08-05 Auspex Pharmaceuticals Inc Benzoquinolin-inhibitorer fra vesikulær monoamin-transporter 2
BRPI0921862A2 (pt) * 2008-12-05 2015-12-29 Arqule Inc inibidores de raf e seus usos
AR074776A1 (es) 2008-12-18 2011-02-09 Sanofi Aventis Metodo para tratar la degeneracion macular; modulando el sistema inmunitario del paciente
PL2389372T3 (pl) 2009-01-23 2016-02-29 Rigel Pharmaceuticals Inc Kompozycje i sposoby hamowania szlaku JAK
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
WO2011009075A2 (en) 2009-07-17 2011-01-20 Rigel Pharmaceuticals, Inc. Deuterated 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
AU2010281404A1 (en) * 2009-07-28 2012-02-09 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
ES2524127T3 (es) * 2009-11-20 2014-12-04 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidinodiamina y sus profármacos y sus usos
US8735417B2 (en) 2009-12-17 2014-05-27 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
EP2558474B1 (en) * 2010-04-13 2015-11-25 Rigel Pharmaceuticals, Inc. 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
AU2011282742B2 (en) 2010-07-28 2015-08-27 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
CN103096716B (zh) 2010-08-10 2016-03-02 西建阿维拉米斯研究公司 Btk抑制剂的苯磺酸盐
CN103269704B (zh) 2010-11-01 2018-07-06 西建卡尔有限责任公司 杂环化合物和其用途
JP5956999B2 (ja) 2010-11-01 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド ヘテロアリール化合物およびその使用
US8796255B2 (en) 2010-11-10 2014-08-05 Celgene Avilomics Research, 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
WO2012154520A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
JP2014513686A (ja) 2011-05-10 2014-06-05 メルク・シャープ・アンド・ドーム・コーポレーション Ｓｙｋ阻害薬としてのアミノピリミジン
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
MX339685B (es) 2011-07-28 2016-06-06 Rigel Pharmaceuticals Inc Formulaciones de (trimetoxifenilamino) pirimidinilo nuevas.
WO2013052391A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. PHENYL 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
US8987456B2 (en) 2011-10-05 2015-03-24 Merck Sharp & Dohme Corp. 3-pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
AR088570A1 (es) 2011-10-28 2014-06-18 Celgene Avilomics Res Inc Metodos para tratar una enfermedad o trastorno relacionado con la tirosina quinasa de bruton
SG11201402570QA (en) 2011-11-23 2014-06-27 Portola Pharm Inc Pyrazine kinase inhibitors
WO2013138502A1 (en) 2012-03-15 2013-09-19 Celgene Avilomics Research, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
JP6317319B2 (ja) 2012-03-15 2018-04-25 セルジーン シーエーアール エルエルシー 上皮成長因子受容体キナーゼ阻害剤の固体形態
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
SG11201408100YA (en) 2012-06-19 2015-01-29 Debiopharm Int 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
WO2013192128A1 (en) 2012-06-20 2013-12-27 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
US9416111B2 (en) 2012-06-22 2016-08-16 Merck Sharp & Dohme Corp. Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors
EP2884982B1 (en) 2012-08-20 2017-09-20 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
US9550780B2 (en) 2012-09-18 2017-01-24 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
BR112015005894B1 (pt) 2012-09-18 2022-03-29 Auspex Pharmaceuticals, Inc Composto, composição farmacêutica, método para tratar um distúrbio mediado por vmat2 e formulação farmacêutica de liberação prolongada
US9586931B2 (en) 2012-09-28 2017-03-07 Merck Sharp & Dohme Corp. Triazolyl derivatives as Syk inhibitors
US20150299125A1 (en) * 2012-11-07 2015-10-22 Merck Sharp & Dohme Corp. Prodrug bipyridylaminopyridines as syk inhibitors
WO2014093191A1 (en) 2012-12-12 2014-06-19 Merck Sharp & Dohme Corp. AMINO-PYRIMIDINE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
US9598405B2 (en) 2012-12-21 2017-03-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
WO2014100748A1 (en) 2012-12-21 2014-06-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
TW201446745A (zh) 2013-02-08 2014-12-16 Celgene Avilomics Res Inc Ｅｒｋ抑制劑及其用途
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
US9745295B2 (en) 2013-04-26 2017-08-29 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2014176216A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines 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
MX369956B (es) 2013-12-03 2019-11-27 Auspex Pharmaceuticals Inc Metodos para preparar compuestos de benzoquinolina.
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
PL3083648T3 (pl) * 2013-12-20 2019-05-31 Rigel Pharmaceuticals Inc Sposób farmaceutyczny i półprodukty
US9783531B2 (en) 2013-12-20 2017-10-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2015095445A1 (en) 2013-12-20 2015-06-25 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
EP3110820B1 (en) 2014-02-28 2022-04-06 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
CN117164657A (zh) 2014-08-12 2023-12-05 莫纳什大学 定向淋巴的前药
US10005760B2 (en) 2014-08-13 2018-06-26 Celgene Car Llc Forms and compositions of an ERK inhibitor
PT3215518T (pt) 2014-10-29 2021-05-25 Bicyclerd Ltd Ligantes de péptido bicíclicos específicos para mt1-mmp
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
KR102335744B1 (ko) 2015-03-06 2021-12-07 오스펙스 파마슈티칼스, 인코포레이티드 비정상적 불수의 운동 장애의 치료 방법
US20180296579A1 (en) 2015-04-24 2018-10-18 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
WO2017040757A1 (en) 2015-09-02 2017-03-09 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
CA2997106C (en) 2015-09-08 2024-06-04 Monash University Lymph directing prodrugs
US10683308B2 (en) 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
MX389001B (es) 2015-10-23 2025-03-20 Navitor Pharm Inc Moduladores de interacción de sestrina-gator2 y sus usos.
WO2017106352A1 (en) 2015-12-14 2017-06-22 Raze Therapeutics, Inc. Caffeine inhibitors of mthfd2 and uses thereof
CN108778286A (zh) 2016-02-26 2018-11-09 德彪药业国际股份公司 用于治疗糖尿病足感染的药物
EP3426244B1 (en) 2016-03-09 2023-06-07 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
HRP20211220T1 (hr) 2016-03-09 2021-10-29 Raze Therapeutics Inc. Inhibitori 3-fosfoglicerat dehidrogenaze i njihova upotreba
EP3440112A4 (en) 2016-04-08 2019-10-09 X4 Pharmaceuticals, Inc. METHOD FOR THE TREATMENT OF CANCER
CA3027500A1 (en) 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
US10988465B2 (en) 2016-06-21 2021-04-27 X4 Pharmaceuticals, Inc. CXCR4 inhibitors and uses thereof
EP3808748A1 (en) 2016-06-21 2021-04-21 X4 Pharmaceuticals, Inc. Substituted piperidines as cxcr4-inhibitors
WO2018071794A1 (en) 2016-10-14 2018-04-19 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
US10647713B2 (en) 2016-10-21 2020-05-12 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
US10414727B2 (en) 2016-11-08 2019-09-17 Navitor Pharmaceuticals, Inc. Phenyl amino piperidine mTORC inhibitors and uses thereof
CN110177544A (zh) 2016-11-29 2019-08-27 普尔泰克健康有限公司 用于递送治疗剂的外泌体
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
CN110603261A (zh) 2016-12-23 2019-12-20 拜斯科阿迪有限公司 具有新型键结构的肽衍生物
WO2018127699A1 (en) 2017-01-06 2018-07-12 Bicyclerd Limited Compounds for treating cancer
AU2018230737B2 (en) 2017-03-08 2022-09-22 Takeda Pharmaceutical Company Limited Tyk2 inhibitors, uses, and methods for production thereof
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
WO2018191146A1 (en) 2017-04-10 2018-10-18 Navitor Pharmaceuticals, Inc. Heteroaryl rheb inhibitors and uses thereof
TWI776886B (zh) 2017-04-26 2022-09-11 美商奈維特製藥公司 Sestrin-gator2交互作用之調節劑及其用途
WO2018197893A1 (en) 2017-04-27 2018-11-01 Bicycletx Limited Bicyclic peptide ligands and uses thereof
WO2019002842A1 (en) 2017-06-26 2019-01-03 Bicyclerd Limited BICYCLIC PEPTIDE LIGANDS WITH DETECTABLE FRACTIONS AND USES THEREOF
DK3658557T3 (da) 2017-07-28 2024-07-29 Takeda Pharmaceuticals Co Tyk2-inhibitorer og anvendelser deraf
WO2019025811A1 (en) 2017-08-04 2019-02-07 Bicycletx Limited SPECIFIC BICYCLIC PEPTIDE LIGANDS OF CD137
EP3668887A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand sting conjugates and uses thereof
WO2019034868A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited CONJUGATES PEPTIDE BICYCLIC-LIGAND PPR-A AND USES THEREOF
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
EP3675838A4 (en) 2017-08-29 2021-04-21 PureTech LYT, Inc. Lymphatic system-directing lipid prodrugs
US11358948B2 (en) 2017-09-22 2022-06-14 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
IL307995A (en) 2017-09-22 2023-12-01 Kymera Therapeutics Inc Protein compounds and their uses
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
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
WO2019126378A1 (en) 2017-12-19 2019-06-27 Ariya Therapeutics, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
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
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
EP4616913A2 (en) 2018-01-29 2025-09-17 Merck Patent GmbH Gcn2 inhibitors and uses thereof
SG11202006832YA (en) 2018-01-29 2020-08-28 Merck Patent Gmbh Gcn2 inhibitors and uses thereof
CA3091775A1 (en) 2018-02-23 2019-08-29 Bicycletx Limited Multimeric bicyclic peptide ligands
AU2019229258B2 (en) 2018-02-27 2023-09-14 Artax Biopharma Inc. Chromene derivatives as inhibitors of TCR-Nck interaction
CA3097774A1 (en) 2018-04-24 2019-10-31 Vertex Pharmaceuticals Incorporated Pteridinone compounds and uses thereof
ES2987356T3 (es) 2018-04-24 2024-11-14 Merck Patent Gmbh Compuestos antiproliferación y usos de los mismos
FI3813946T3 (fi) 2018-06-15 2024-06-25 Janssen Pharmaceutica Nv Rapamysiinianalogeja ja niiden käyttötapoja
IL279489B1 (en) 2018-06-22 2025-06-01 Bicycletx Ltd Bicyclic peptide ligands specific for nectin-4, a drug conjugate comprising the peptide ligand and a pharmaceutical composition comprising the drug conjugate
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
EP3817748A4 (en) 2018-07-06 2022-08-24 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
WO2020081508A1 (en) 2018-10-15 2020-04-23 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
US10919937B2 (en) 2018-10-23 2021-02-16 Bicycletx Limited Bicyclic peptide ligands and uses thereof
CA3117336A1 (en) 2018-10-24 2020-04-30 Navitor Pharmaceuticals, Inc. Polymorphs of (s)-2-amino-5,5-difluoro-4,4-dimethylpentanoic acid for use in modulating mtorc1
WO2020092845A1 (en) 2018-11-01 2020-05-07 Rigel Pharmaceuticals, Inc. Method and composition embodiments for treating acute myeloid leukemia
BR112021010484A2 (pt) 2018-11-30 2021-08-24 Kymera Therapeutics, Inc. Degradadores de irak e usos dos mesmos
US11053241B2 (en) 2018-11-30 2021-07-06 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
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
WO2020154474A1 (en) 2019-01-23 2020-07-30 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
AU2020223515B2 (en) 2019-02-14 2024-11-21 Debiopharm International S.A. Afabicin formulation, method for making the same
AU2020253990A1 (en) 2019-04-02 2021-10-28 Bicycletx Limited Bicycle toxin conjugates and uses thereof
MX2021012216A (es) 2019-04-05 2022-01-24 Kymera Therapeutics Inc Degradadores de transductores de señal y activadores de transcripción (stat) y usos de los mismos.
WO2020243423A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors 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
MX2022001890A (es) 2019-08-14 2022-04-26 Rigel Pharmaceuticals Inc Metodo para bloquear o mejorar el sindrome de liberacion de citocinas.
CN115038688A (zh) 2019-09-11 2022-09-09 文森雷生物科学股份有限公司 Usp30抑制剂及其用途
JP2022547719A (ja) 2019-09-13 2022-11-15 ニンバス サターン， インコーポレイテッド Ｈｐｋ１アンタゴニストおよびその使用
MX2022005215A (es) 2019-11-01 2022-06-08 Navitor Pharm Inc Metodos de tratamiento que usan un modulador de la diana mecanicista del complejo 1 de rapamicina (mtorc1).
US11819476B2 (en) 2019-12-05 2023-11-21 Janssen Pharmaceutica Nv Rapamycin analogs and uses thereof
US11779578B2 (en) 2019-12-17 2023-10-10 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CA3162502A1 (en) 2019-12-23 2021-07-01 Yi Zhang Smarca degraders and uses thereof
CN115348864A (zh) 2020-02-05 2022-11-15 纯技术Lyt股份有限公司 神经甾体的脂质前药
AR121506A1 (es) 2020-03-03 2022-06-08 Pic Therapeutics Inc Inhibidores del eif4e y sus usos
PH12022552458A1 (en) 2020-03-19 2024-01-22 Kymera Therapeutics Inc Mdm2 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
US20230250110A1 (en) 2020-06-03 2023-08-10 Kymera Therapeutics, Inc. Deuterated irak degraders and uses thereof
CA3186504A1 (en) 2020-08-17 2022-02-24 Stephen J. Blakemore Bicycle conjugates specific for nectin-4 and uses thereof
CN116601131A (zh) 2020-10-23 2023-08-15 林伯士克洛索有限公司 Ctps1抑制剂及其用途
WO2022120354A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
JP2024503300A (ja) 2020-12-30 2024-01-25 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ分解剤およびそれらの使用
CA3206499A1 (en) 2021-02-02 2022-08-11 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
CN117098757A (zh) 2021-02-02 2023-11-21 里米诺生物科学有限公司 Gpr84拮抗剂和其用途
JP2024506909A (ja) 2021-02-12 2024-02-15 ニンバス サターン， インコーポレイテッド Ｈｐｋ１アンタゴニスト及びその使用
JP2024506657A (ja) 2021-02-15 2024-02-14 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ４分解剤およびその使用
AU2022220043A1 (en) 2021-02-15 2023-08-31 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
WO2022187856A1 (en) 2021-03-05 2022-09-09 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
WO2022213062A1 (en) 2021-03-29 2022-10-06 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
EP4319756A4 (en) 2021-04-09 2025-02-26 Nimbus Clio, Inc. CBL-B MODULATORS AND USES THEREOF
IL307673A (en) 2021-04-16 2023-12-01 Ikena Oncology Inc MEK inhibitors and their use
CA3217792A1 (en) 2021-05-07 2022-11-10 Kymera Therapeutics, Inc Cdk2 degraders and uses thereof
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
WO2023028238A1 (en) 2021-08-25 2023-03-02 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
EP4392422A1 (en) 2021-08-25 2024-07-03 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
CN118302168A (zh) 2021-10-29 2024-07-05 凯麦拉医疗公司 Irak4降解剂和其制备
WO2023081923A1 (en) 2021-11-08 2023-05-11 Frequency 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
AU2023214044A1 (en) 2022-01-31 2024-08-08 Kymera Therapeutics, Inc. Irak degraders and uses thereof
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
EP4532470A1 (en) 2022-05-25 2025-04-09 Ikena Oncology, Inc. Mek inhibitors and uses thereof
TW202416950A (zh) 2022-08-02 2024-05-01 英商利米那生物科技有限公司 雜芳基甲醯胺及相關gpr84拮抗劑及其用途
JP2025527248A (ja) 2022-08-02 2025-08-20 リミナル・バイオサイエンシーズ・リミテッド 置換ピリドンｇｐｒ８４アンタゴニスト及びその使用
IL318577A (en) 2022-08-02 2025-03-01 Liminal Biosciences Ltd ARYL-TRIAZOLYL AND RELATED GPR84 ANTAGONISTS AND THEIR USES
TW202430148A (zh) 2022-11-22 2024-08-01 美商皮克醫療公司 ｅＩＦ４Ｅ抑制劑及其用途
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
WO2025062372A1 (en) 2023-09-21 2025-03-27 Takeda Pharmaceutical Company Limited Tyk2 inhibitors for use in the treatment of inflammatory bowel disease
CN118702735A (zh) * 2024-07-15 2024-09-27 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

Family Cites Families (151)

* 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 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 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
US5430148A (en) * 1992-03-31 1995-07-04 Agouron Pharmaceuticals, Inc. Antiproliferative quinazolines
PL313973A1 (en) 1993-10-12 1996-08-05 Du Pont Merck Pharma 1 n-alkyl-n-arylopyrimidin amines and their derivatives
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
JP4135318B2 (ja) 1997-12-15 2008-08-20 アステラス製薬株式会社 新規なピリミジン−５−カルボキサミド誘導体
US6436989B1 (en) * 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
NZ505515A (en) 1997-12-31 2003-03-28 Univ Kansas Water soluble prodrugs of secondary and tertiary amine containing drugs and methods of making thereof
AU748087B2 (en) 1998-02-17 2002-05-30 Tularik Inc. Anti-viral pyrimidine derivatives
EP1245567B1 (en) 1998-03-27 2011-03-02 Janssen Pharmaceutica NV HIV inhibiting pyrimidine derivatives
KR100643419B1 (ko) 1998-03-27 2006-11-10 얀센 파마슈티카 엔.브이. Ｈｉｖ를 억제하는 피리미딘 유도체
EP1107957B1 (en) 1998-08-29 2006-10-18 AstraZeneca AB Pyrimidine compounds
DE19851421A1 (de) 1998-11-07 2000-05-11 Boehringer Ingelheim Pharma Neue Pyrimidine, deren Herstellung und Verwendung
AU762523C (en) 1998-11-10 2004-02-12 Janssen Pharmaceutica N.V. HIV replication inhibiting pyrimidines
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
CN1234347C (zh) 1999-09-24 2006-01-04 詹森药业有限公司 抗病毒组合物
DE19945982A1 (de) 1999-09-24 2001-03-29 Knoll Ag Geschwindigkeitsbestimmte Partikel
KR20020043223A (ko) 1999-09-30 2002-06-08 해피 페너 ; 해리 에이치. 페너 2세 알킬렌 디아민 치환 헤테로사이클 화합물
AU1026901A (en) 1999-10-29 2001-05-08 Syngenta Participations Ag Novel herbicides
AU2457201A (en) 1999-12-28 2001-07-09 Bristol-Myers Squibb Company Cytokine, especially tnf-alpha, 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
KR20030024659A (ko) 2000-02-17 2003-03-26 암겐 인코포레이티드 키나제 억제제
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
GB0004886D0 (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
CN1249057C (zh) * 2000-04-27 2006-04-05 巴斯利尔药物股份公司 用作抗菌剂的色烯基甲基嘧啶二胺
CA2406562C (en) 2000-05-08 2009-09-15 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines and triazines
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
KR20030032035A (ko) 2000-09-15 2003-04-23 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피라졸 화합물
US6448401B1 (en) * 2000-11-20 2002-09-10 Bristol-Myers Squibb Company Process for water soluble azole compounds
HUP0400908A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors, their use and pharmaceutical compositions containing them
EP2311825B1 (en) 2000-12-21 2015-10-07 Novartis AG Pyrimidineamines as angiogenesis modulators
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
KR20030076688A (ko) 2001-02-20 2003-09-26 아스트라제네카 아베 Ｇｓｋ3-관련 장애의 치료를 위한 2-아릴아미노-피리미딘
EP1392662B1 (de) 2001-05-29 2009-01-07 Bayer Schering Pharma Aktiengesellschaft Cdk inhibitorische pyrimidine, deren herstellung und verwendung als arzneimittel
ATE432929T1 (de) 2001-06-15 2009-06-15 Vertex Pharma 5-(2-aminopyrimidin-4-yl)benzisoxazole als proteinkinasehemmer
JP2005500294A (ja) 2001-06-19 2005-01-06 ブリストル−マイヤーズ　スクイブ　カンパニー ホスホジエステラーゼ７に対するピリミジン阻害剤
AU2002315388A1 (en) 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel phenylamino-pyrimidines and uses thereof
CA2451128A1 (en) 2001-06-26 2003-01-09 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
WO2003026665A1 (en) 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine 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
UY27487A1 (es) 2001-10-17 2003-05-30 Boehringer Ingelheim Pharma Derivados de pirimidina, medicamentos que contienen estos compuestos, su empleo y procedimiento para su preparación
JP2003127790A (ja) 2001-10-25 2003-05-08 Nippon Soken Inc メータ装置
DK1473289T3 (da) 2001-11-28 2009-11-30 Btg Int Ltd Forebyggende eller afhjælpende midler til Alzheimers sygdom eller amyloid-proteinfibroseinhibitorer indeholdende nitrogenholdige heteroarylforbindelser
SE0104140D0 (sv) 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
AU2002367172A1 (en) 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation 2,4-diamino-pyrimidine derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
JP4469179B2 (ja) 2002-01-23 2010-05-26 バイエル ファーマセチカル コーポレーション Ｒｈｏキナーゼ阻害剤としてのピリミジン誘導体
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
JP2005522438A (ja) 2002-02-08 2005-07-28 スミスクライン ビーチャム コーポレーション ピリミジン化合物
MXPA04008458A (es) 2002-03-01 2004-12-06 Smithkline Beecham Corp Diamino pirimidinas y su uso como inhibidores de angiogenesis.
US7288547B2 (en) 2002-03-11 2007-10-30 Schering Ag CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
WO2003076437A1 (de) 2002-03-11 2003-09-18 Schering Aktiengesellschaft Cdk inhibitorische 2-heteroaryl-pyrimidine, deren herstellung und verwendung als arzneimittel
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
JP4359150B2 (ja) 2002-03-20 2009-11-04 ブリストル−マイヤーズ スクイブ カンパニー フルオロオキシインドールのホスフェートプロドラッグ
WO2004039359A2 (en) 2002-05-06 2004-05-13 Bayer Pharmaceuticals Corporation Use of pyrimidine derivates for the manifacture of a medicament for the treatment of hyper-proliferative disorders
AU2003231231A1 (en) 2002-05-06 2003-11-11 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
US7122552B2 (en) 2002-05-30 2006-10-17 Vertex Pharmaceuticals Incorporated Inhibitors of JAK and CDK2 protein kinases
IL165286A0 (en) 2002-06-17 2005-12-18 Smithkline Beecham Corp Chemical process
CN1665789A (zh) 2002-06-28 2005-09-07 山之内制药株式会社 二氨基嘧啶酰胺衍生物
NZ537752A (en) 2002-07-29 2006-12-22 Rigel Pharmaceuticals Inc Use of 2,4-pyrimidinediamine compounds in the preparation of medicaments for treating autoimmune diseases
AU2003249539A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Cyclic compounds containing zinc binding groups as matrix metalloproteinase inhibitors
WO2004016597A2 (en) 2002-08-14 2004-02-26 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
DE60330895D1 (de) 2002-11-01 2010-02-25 Vertex Pharma Verbindungen, die sich als inhibitoren vonjak und anderen proteinkinasen eignen
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
AU2002350719A1 (en) 2002-11-29 2004-06-23 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
JP5602333B2 (ja) 2003-02-07 2014-10-08 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｈｉｖ感染の予防のためのピリミジン誘導体
CL2004000303A1 (es) 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidinas y triazinas; proceso de preparacion; composicion farmaceutica; y su uso para inhibir la replicacion del vih.
ES2325440T3 (es) 2003-02-20 2009-09-04 Smithkline Beecham Corporation Compuestos de pirimidina.
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
WO2004099159A1 (en) 2003-04-30 2004-11-18 The Institutes For Pharmaceutical Discovery, Llc Substituted heteroaryls as inhibitors of protein tyrosine phosphatases
GB0311276D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
WO2005007621A2 (en) 2003-05-30 2005-01-27 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
EP1648877A1 (en) 2003-07-22 2006-04-26 Neurogen Corporation Substituted pyridin-2-ylamine analogues
US7442698B2 (en) 2003-07-24 2008-10-28 Amgen Inc. Substituted heterocyclic compounds and methods of use
ES2421139T3 (es) 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
JP2007500179A (ja) 2003-07-30 2007-01-11 サイクラセル・リミテッド キナーゼ阻害剤としての２−アミノフェニル−４−フェニルピリミジン
JP4741491B2 (ja) 2003-08-07 2011-08-03 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 抗増殖剤としての２，４−ピリミジンジアミン化合物および使用
BR122019017579B8 (pt) 2003-08-15 2021-07-27 Novartis Ag 2,4-pirimidinadiaminas, seus usos, combinação e composição farmacêutica
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
WO2005026130A1 (en) 2003-09-18 2005-03-24 Novartis Ag 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
JP2007515400A (ja) 2003-11-28 2007-06-14 ノバルティス アクチエンゲゼルシャフト タンパク質キナーゼ依存性疾患の処置におけるジアリール尿素誘導体
MY141255A (en) 2003-12-11 2010-03-31 Memory Pharm Corp Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs
JP2007514775A (ja) 2003-12-19 2007-06-07 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 １−（２，４−ピリミジンジアミノ）−２−シクロペンタンカルボキサイミド合成中間体の立体異性体および立体異性体混合物
US7745625B2 (en) * 2004-03-15 2010-06-29 Bristol-Myers Squibb Company Prodrugs of piperazine and substituted piperidine antiviral agents
WO2005118544A2 (en) 2004-05-18 2005-12-15 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
EP1786783A1 (en) 2004-09-01 2007-05-23 Rigel Pharmaceuticals, Inc. Synthesis of 2,4-pyrimidinediamine compounds
WO2006034872A1 (de) 2004-09-29 2006-04-06 Bayer Schering Pharma Aktiengesellschaft Substituierte 2-anilinopyrimidine als zellzyklus -kinase oder rezeptortyrosin-kinase inhibitoren, deren herstellung und verwendung als arzneimittel
US7585883B2 (en) 2004-10-29 2009-09-08 Rigel Pharmaceuticals, Inc. Substituted pyridines and their uses
JP5095409B2 (ja) 2004-11-24 2012-12-12 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 スピロ２，４−ピリミジンジアミン化合物およびその使用
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
WO2006074057A2 (en) 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
MX2007007189A (es) * 2005-01-19 2010-09-28 Rigel Pharmaceuticals Inc Prodrogas de compuestos de 2,4-pirimidindiamina y sus usos.
CA2604551A1 (en) 2005-05-03 2007-03-08 Rigel Pharmaceuticals, Inc. Jak kinase inhibitors and their uses
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
MX286273B (es) 2005-06-08 2011-05-04 Rigel Pharmaceuticals Inc Composiciones y metodos para inhibicion de la via jak.
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
EA200800285A1 (ru) 2005-07-11 2008-08-29 Санофи-Авентис Новые производные 2,4-дианилинопиримидинов, их получение, лекарственные средства, фармацевтические композиции, содержащие указанные производные, и их применение, в частности, в качестве ингибиторов ikk
EP1913009B1 (en) 2005-07-28 2010-05-12 Intervet International BV Novel benzimidazole (thio) carbamates with antiparasitic activity and the synthesis thereof
WO2007032263A1 (ja) 2005-09-13 2007-03-22 Eisai R & D Management Co., Ltd. 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
US20070117775A1 (en) 2005-10-31 2007-05-24 Rigel Pharmaceuticals, Inc. Compositions and Methods For Treating Inflammatory Disorders
WO2007053542A2 (en) 2005-11-01 2007-05-10 Boston Life Sciences, Inc. Methods and compositions for the prevention and regression of neovascularization
RU2589878C2 (ru) 2005-11-01 2016-07-10 Таргеджен, Инк. Би-арил-мета-пиримидиновые ингибиторы киназ
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
SI1984357T1 (sl) 2006-02-17 2014-02-28 Rigel Pharmaceuticals, Inc. Spojine 2,4-pirimidindiamina za zdravljenje ali preventivo avtoimunih bolezni
WO2007098507A2 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
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
CA2673125C (en) 2006-10-19 2015-04-21 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7947698B2 (en) 2007-03-23 2011-05-24 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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010510322A (ja) * 2006-11-21 2010-04-02 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プロドラッグ塩およびそれらの使用

Also Published As

Publication number Publication date
CA2591948A1 (en) 2006-07-27
CA2591948C (en) 2013-11-12
US20120232036A1 (en) 2012-09-13
HUS2000011I1 (hu) 2020-06-29
PT1856135E (pt) 2010-02-26
HK1108896A1 (en) 2008-05-23
US20160136191A1 (en) 2016-05-19
EP1856135B1 (en) 2009-12-09
LUC00153I2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2021-02-15
NO2020010I1 (no) 2020-05-13
IL183890A0 (en) 2007-10-31
US20140357598A1 (en) 2014-12-04
BRPI0606318A2 (pt) 2009-06-16
US20090124580A1 (en) 2009-05-14
BRPI0606318B8 (pt) 2021-05-25
NL301039I2 (nl) 2020-05-12
RU2007131430A (ru) 2009-02-27
US7563892B1 (en) 2009-07-21
US20190292197A1 (en) 2019-09-26
ES2337496T3 (es) 2010-04-26
US9266912B2 (en) 2016-02-23
US7449458B2 (en) 2008-11-11
CY2020012I1 (el) 2020-11-25
US20120108810A1 (en) 2012-05-03
US9532998B2 (en) 2017-01-03
NZ555947A (en) 2010-11-26
CY2020012I2 (el) 2020-11-25
US20200270271A1 (en) 2020-08-27
NO20074179L (no) 2007-10-18
US7538108B2 (en) 2009-05-26
LTC1856135I2 (lt) 2021-07-12
LTPA2020507I1 (lt) 2020-06-25
US7989448B2 (en) 2011-08-02
EP2161275A1 (en) 2010-03-10
US20110319613A1 (en) 2011-12-29
JP2008527048A (ja) 2008-07-24
AU2006206458A1 (en) 2006-07-27
KR101278397B1 (ko) 2013-06-25
BRPI0606318B1 (pt) 2021-02-02
NL301039I1 (nl) 2020-04-29
US8476263B2 (en) 2013-07-02
US10577381B2 (en) 2020-03-03
US20130338357A1 (en) 2013-12-19
US8211889B2 (en) 2012-07-03
US20060234983A1 (en) 2006-10-19
EP1856135A1 (en) 2007-11-21
MX346822B (es) 2017-03-28
SI1856135T1 (sl) 2010-04-30
US8785437B2 (en) 2014-07-22
PL1856135T3 (pl) 2010-05-31
WO2006078846A1 (en) 2006-07-27
US20170291909A1 (en) 2017-10-12
LUC00153I1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2020-05-08
NO339146B1 (no) 2016-11-14
US20060211657A1 (en) 2006-09-21
CN101115761B (zh) 2012-07-18
KR20070098926A (ko) 2007-10-05
JP2011236234A (ja) 2011-11-24
ATE451381T1 (de) 2009-12-15
IL183890A (en) 2012-04-30
AU2006206458B2 (en) 2012-10-25
DE602006010979D1 (de) 2010-01-21
FIC20200014I1 (fi) 2020-05-19
DK1856135T3 (da) 2010-04-12
MX2007007189A (es) 2010-09-28
CY1109888T1 (el) 2014-09-10
RU2416616C2 (ru) 2011-04-20
US8211888B2 (en) 2012-07-03
CN101115761A (zh) 2008-01-30

Similar Documents

Publication Publication Date Title
JP4801096B2 (ja) ２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用
JP5264759B2 (ja) ２，４−ピリミジンジアミン化合物のプロドラッグ塩およびそれらの使用
HK1142079A (en) Prodrugs of 2,4-pyrimidinediamine compounds and their uses
HK1108896B (en) Prodrugs of 2,4-pyrimidinediamine compounds and their uses

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20070919

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20071127

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7422

Effective date: 20080711

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20080828

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20090619

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20090619

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20110406

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20110705

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110708

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20110712

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20110707

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

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20110801

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20110804

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20140812

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Ref document number: 4801096

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20140812

Year of fee payment: 3

S201 Request for registration of exclusive licence

Free format text: JAPANESE INTERMEDIATE CODE: R314201

R360 Written notification for declining of transfer of rights

Free format text: JAPANESE INTERMEDIATE CODE: R360

R370 Written measure of declining of transfer procedure

Free format text: JAPANESE INTERMEDIATE CODE: R370

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R153 Grant of patent term extension

Free format text: JAPANESE INTERMEDIATE CODE: R153

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250