JP5225079B2 - Ｊａｋ経路の阻害のための組成物および方法 - Google Patents

Ｊａｋ経路の阻害のための組成物および方法 Download PDF

Info

Publication number
JP5225079B2
JP5225079B2 JP2008515989A JP2008515989A JP5225079B2 JP 5225079 B2 JP5225079 B2 JP 5225079B2 JP 2008515989 A JP2008515989 A JP 2008515989A JP 2008515989 A JP2008515989 A JP 2008515989A JP 5225079 B2 JP5225079 B2 JP 5225079B2
Authority
JP
Japan
Prior art keywords
substituted
group
alkyl
heterocyclic
cycloalkyl
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.)
Expired - Fee Related
Application number
JP2008515989A
Other languages
English (en)
Japanese (ja)
Other versions
JP2008543778A (ja
JP2008543778A5 (enExample
Inventor
ホイ リー，
サンバイア ソータ，
デイビッド キャロル，
アンクシュ アルガーデ，
キン ツォー，
アルビンダー スラン，
ジェフリー クラウ，
ホルガー カイム，
ソマセカー バーミディパティ，
バネッサ テイラー，
ロビン クーパー，
ラジンダー シン，
ブライアン ウォン，
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
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 JP2008543778A publication Critical patent/JP2008543778A/ja
Publication of JP2008543778A5 publication Critical patent/JP2008543778A5/ja
Application granted granted Critical
Publication of JP5225079B2 publication Critical patent/JP5225079B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic 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
    • A61K31/695—Silicon compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A61K38/13—Cyclosporins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • 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
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15—Six-membered rings
    • C07D285/16—Thiadiazines; Hydrogenated thiadiazines
    • C07D285/18—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
    • C07D285/20—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems
    • C07D285/22—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Microbiology (AREA)
  • Endocrinology (AREA)
  • Mycology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2008515989A 2005-06-08 2006-06-08 Ｊａｋ経路の阻害のための組成物および方法 Expired - Fee Related JP5225079B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US68903205P 2005-06-08 2005-06-08
US60/689,032 2005-06-08
US70663805P 2005-08-08 2005-08-08
US60/706,638 2005-08-08
US77663606P 2006-02-24 2006-02-24
US60/776,636 2006-02-24
PCT/US2006/022590 WO2006133426A2 (en) 2005-06-08 2006-06-08 Compositions and methods for inhibition of the jak pathway

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2012129760A Division JP5480936B2 (ja) 2005-06-08 2012-06-07 Ｊａｋ経路の阻害のための組成物および方法

Publications (3)

Publication Number Publication Date
JP2008543778A JP2008543778A (ja) 2008-12-04
JP2008543778A5 JP2008543778A5 (enExample) 2009-07-23
JP5225079B2 true JP5225079B2 (ja) 2013-07-03

Family

ID=37499158

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2008515989A Expired - Fee Related JP5225079B2 (ja) 2005-06-08 2006-06-08 Ｊａｋ経路の阻害のための組成物および方法
JP2012129760A Expired - Fee Related JP5480936B2 (ja) 2005-06-08 2012-06-07 Ｊａｋ経路の阻害のための組成物および方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2012129760A Expired - Fee Related JP5480936B2 (ja) 2005-06-08 2012-06-07 Ｊａｋ経路の阻害のための組成物および方法

Country Status (16)

Country Link
US (9) US7491732B2 (enExample)
EP (1) EP1904457B1 (enExample)
JP (2) JP5225079B2 (enExample)
KR (1) KR101312225B1 (enExample)
CN (1) CN105348203B (enExample)
AU (1) AU2006254840B2 (enExample)
BR (1) BRPI0610876B8 (enExample)
CA (1) CA2608367C (enExample)
ES (1) ES2651349T3 (enExample)
IL (1) IL187257A (enExample)
MX (1) MX286273B (enExample)
NO (1) NO341966B1 (enExample)
NZ (1) NZ563454A (enExample)
RU (1) RU2485106C2 (enExample)
SG (1) SG137989A1 (enExample)
WO (1) WO2006133426A2 (enExample)

Families Citing this family (137)

* 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
BR0313059B8 (pt) 2002-07-29 2021-07-27 Rigel Pharmaceuticals composto, e, composição farmacêutica
CN102358738A (zh) 2003-07-30 2012-02-22 里格尔药品股份有限公司 2,4-嘧啶二胺化合物及其预防和治疗自体免疫疾病的用途
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
JP4801096B2 (ja) * 2005-01-19 2011-10-26 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およびそれらの使用
US20070203161A1 (en) * 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
EP1904457B1 (en) 2005-06-08 2017-09-06 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CA2607901C (en) 2005-06-13 2016-08-16 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders using a syk inhibitory 2,4-pyrimidinediamine
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
US7528143B2 (en) 2005-11-01 2009-05-05 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
CN103214484B (zh) 2005-12-13 2016-07-06 因塞特控股公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶
JP4653842B2 (ja) * 2006-02-17 2011-03-16 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 自己免疫疾患を治療または予防するための２，４−ピリミジンジアミン化合物
JP2009528295A (ja) 2006-02-24 2009-08-06 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
EP2054392A2 (en) 2006-06-15 2009-05-06 Boehringer Ingelheim International GmbH 2-anilino-4-(heterocyclic)amino-pyrimidines as inhibitors of protein kinase c-alpha
ATE497496T1 (de) * 2006-10-19 2011-02-15 Rigel Pharmaceuticals Inc 2,4-pyridimediamon-derivate als hemmer von jak- kinasen zur behandlung von autoimmunerkrankungen
ES2555803T3 (es) 2006-10-23 2016-01-08 Cephalon, Inc. Fusión de derivados bicíclicos 2,4-diaminopirimidina como utilizar inhibidores ALK y c-Met
ES2380551T3 (es) 2006-11-21 2012-05-16 Rigel Pharmaceuticals, Inc. Sales de profármaco de compuestos de 2,4-pirimidindiamina y sus usos
BRPI0722383A2 (pt) 2006-12-08 2012-06-05 Irm Llc compostos inibidores de proteìna quinase, composições contendo os mesmos bem como seus usos
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
US20090036440A1 (en) * 2007-04-27 2009-02-05 Astrazeneca Ab Novel pyrimidine derivatives - 816
HUE029236T2 (en) 2007-06-13 2017-02-28 Incyte Holdings Corp (R) -3- (4- (7H-Pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanenitrile Crystalline salts of Janus kinase inhibitor
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
FR2919869B1 (fr) * 2007-08-09 2009-09-25 Sanofi Aventis Sa Nouveaux derives de n, n'-2,4-dianilinopyrimidines, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
WO2009109991A2 (en) * 2008-01-23 2009-09-11 Sun Pharma Advanced Research Company Ltd., Novel hydrazide containing tyrosine kinase inhibitors
EP2300013B2 (en) 2008-05-21 2024-11-13 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
US20100035875A1 (en) 2008-06-20 2010-02-11 Bing-Yan Zhu Triazolopyridine jak inhibitor compounds and methods
KR20110033223A (ko) 2008-06-20 2011-03-30 제넨테크, 인크. 트리아졸로피리딘 ｊａｋ 억제제 화합물 및 방법
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
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US20110172217A1 (en) * 2008-09-05 2011-07-14 Shionogi & Co., Ltd. Ring-fused morpholine derivative having pi3k-inhibiting activity
CA2735420C (en) * 2008-09-08 2016-06-28 Merck Patent Gmbh Macrocyclic pyrimidines as protein kinase inhibitors
CA2736258C (en) * 2008-09-23 2016-11-29 Rigel Pharmaceuticals, Inc. Tricyclic carbamate jak inhibitors
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
AU2009320683B2 (en) 2008-11-28 2012-07-19 Kowa Company, Ltd. Pyridine-3-carboxyamide derivative
US8809343B2 (en) * 2008-12-26 2014-08-19 Fudan University Pyrimidine derivative, preparation method and use thereof
CA2749195C (en) 2009-01-15 2017-03-07 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
PL2389372T3 (pl) 2009-01-23 2016-02-29 Rigel Pharmaceuticals Inc Kompozycje i sposoby hamowania szlaku JAK
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Ｅｇｆｒ阻害剤及び疾患の治療方法
MY156727A (en) 2009-05-22 2016-03-15 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EP2432472B1 (en) 2009-05-22 2019-10-02 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
CN102498110A (zh) 2009-06-10 2012-06-13 雅培制药有限公司 作为激酶抑制剂的2-(lh-吡唑-4-基氨基)-嘧啶
CA2768543C (en) * 2009-07-28 2017-06-20 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
IN2012DN02577A (enExample) 2009-10-15 2015-08-28 Pfizer
ES2461967T3 (es) 2009-12-18 2014-05-21 Pfizer Inc. Compuestos de pirrolo[2,3-d]pirimidina
WO2011100455A1 (en) 2010-02-12 2011-08-18 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Inhibition of antibody responses to foreign proteins
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
AR084691A1 (es) 2010-05-21 2013-06-05 Incyte Corp Formulacion de uso topico para un inhibidor de jak y metodo para tratar trastorno de la piel
EP2395001A1 (en) 2010-05-21 2011-12-14 Chemilia AB Novel pyrimidine derivatives
AU2011255218B2 (en) 2010-05-21 2015-03-12 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
BR112012029647A2 (pt) 2010-05-21 2016-08-02 Chemilia Ab novos derivados de pirimidinas
US8354420B2 (en) 2010-06-04 2013-01-15 Genentech, Inc. Aminopyrimidine derivatives as LRRK2 inhibitors
JP6035238B2 (ja) * 2010-07-21 2016-11-30 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 プロテインキナーゼｃ阻害剤およびその使用
CN105566229A (zh) 2010-08-10 2016-05-11 西建阿维拉米斯研究公司 Btk抑制剂的苯磺酸盐及其用途和制备方法
US9238629B2 (en) 2010-11-01 2016-01-19 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
SG10201508958WA (en) 2010-11-01 2015-11-27 Celgene Avilomics Res Inc Heterocyclic Compounds And Uses Thereof
US9198911B2 (en) 2010-11-02 2015-12-01 The Trustees Of Columbia University In The City Of New York Methods for treating hair loss disorders
WO2012060847A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
SI2638031T1 (en) 2010-11-10 2018-02-28 Genentech, Inc. Pyrazole aminopyrimidine derivatives as LRRK2 modulators
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
HRP20181286T1 (hr) * 2011-03-10 2018-10-05 Rigel Pharmaceuticals, Inc. 2,4 supstituirani pirimidindiamini za uporabu kod diskoidnog lupusa
EP2502924A1 (en) 2011-03-24 2012-09-26 Chemilia AB Novel pyrimidine derivatives
JP5886411B2 (ja) 2011-03-24 2016-03-16 ノビガ・リサーチ・エービーＮｏｖｉｇａ Ｒｅｓｅａｒｃｈ ＡＢ 新規のピリミジン誘導体
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
CA2834062A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
AU2012253885A1 (en) 2011-05-10 2013-10-31 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
EP2751093A1 (en) 2011-08-29 2014-07-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
EP2763974B1 (en) 2011-10-05 2016-09-14 Merck Sharp & Dohme Corp. Phenyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
WO2013052393A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2763976B1 (en) 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
JP2014532658A (ja) 2011-10-28 2014-12-08 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 ブルトン型チロシンキナーゼ疾患または障害を治療する方法
CA2857189A1 (en) * 2011-12-08 2013-06-13 Rigel Pharmaceuticals, Inc. Topical formulation for administering a compound
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
CA2866857C (en) 2012-03-15 2021-03-09 Celgene Avilomics Research, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
EP2863914B1 (en) 2012-06-20 2018-10-03 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
WO2013192128A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
US9416111B2 (en) 2012-06-22 2016-08-16 Merck Sharp & Dohme Corp. Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors
EP2863916B1 (en) 2012-06-22 2018-07-18 Merck Sharp & Dohme Corp. Substituted pyridine spleen tyrosine kinase (syk) inhibitors
US9353066B2 (en) 2012-08-20 2016-05-31 Merck Sharp & Dohme Corp. Substituted phenyl-Spleen Tyrosine Kinase (Syk) inhibitors
JP2015528501A (ja) 2012-09-12 2015-09-28 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 白斑の治療法
EP2711365A1 (en) 2012-09-21 2014-03-26 Chemilia AB 4-Indazolylamino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer
EP2711364A1 (en) 2012-09-21 2014-03-26 Chemilia AB 4-(Indolyl or benzimidazolyl)amino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer
US9586931B2 (en) 2012-09-28 2017-03-07 Merck Sharp & Dohme Corp. Triazolyl derivatives as Syk inhibitors
TWI761825B (zh) 2012-11-15 2022-04-21 美商英塞特控股公司 盧梭利替尼之緩釋性劑型
US9624210B2 (en) 2012-12-12 2017-04-18 Merck Sharp & Dohme Corp. Amino-pyrimidine-containing spleen tyrosine kinase (Syk) inhibitors
EP2935226A4 (en) 2012-12-21 2016-11-02 Celgene Avilomics Res Inc HETEROARYL COMPOUNDS AND USES THEREOF
US9598405B2 (en) 2012-12-21 2017-03-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
US9561228B2 (en) 2013-02-08 2017-02-07 Celgene Avilomics Research, Inc. ERK inhibitors and uses thereof
MX384910B (es) 2013-03-06 2025-03-14 Incyte Holdings Corp Procesos e intermedios para hacer un inhibidor de jak.
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
WO2014176210A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
EP2988749B1 (en) 2013-04-26 2019-08-14 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
SG11201600815WA (en) 2013-08-07 2016-03-30 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
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
BR112016008080B1 (pt) * 2013-10-16 2021-02-23 Fujifilm Corporation sal de ácido carboxílico ou um sal de ácido mineral, cristal de succinato, cristal de fumarato e composição farmacêutica
EP3083560B1 (en) 2013-12-20 2021-10-27 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
US9783531B2 (en) 2013-12-20 2017-10-10 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
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
EP3099677A4 (en) * 2014-01-31 2017-07-26 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
WO2015138273A1 (en) 2014-03-13 2015-09-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
EP3177626A4 (en) 2014-08-08 2017-12-27 Dana Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
US10005760B2 (en) 2014-08-13 2018-06-26 Celgene Car Llc Forms and compositions of an ERK inhibitor
CN107072995B (zh) 2014-08-22 2020-02-21 富士胶片株式会社 用于处置flt3突变阳性癌的医药组合物、突变型flt3抑制剂以及这些的应用
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND CHINESE INHIBITORS
JP6412471B2 (ja) 2015-07-15 2018-10-24 富士フイルム株式会社 含窒素複素環化合物の製造方法およびその中間体
UA123946C2 (uk) 2015-09-11 2021-06-30 Дана-Фарбер Кенсер Інстітьют, Інк. Ацетамідтієнотриазолодіазепіни й шляхи їх застосування
PE20181287A1 (es) 2015-09-11 2018-08-07 Dana Farber Cancer Inst Inc Ciano tienotriazolpirazinas y usos de las mismas
CA3003288A1 (en) 2015-11-25 2017-06-01 Dana-Farber Cancer Institute, Inc. Bivalent bromodomain inhibitors and uses thereof
JP6999688B2 (ja) * 2016-12-13 2022-02-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｃｌ６阻害剤としての新規の６－アミノキノリノン化合物および誘導体
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
CN107805212B (zh) * 2017-11-03 2021-08-20 宿迁德威化工股份有限公司 一种2-甲基-5-氨基苯磺酰胺的制备方法
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
JP7393348B2 (ja) 2018-01-30 2023-12-06 インサイト・コーポレイション （１－（３－フルオロ－２（トリフルオロメチル）イソニコチニル）ピぺリジン―４－オン）を作製するためのプロセス及び中間体
CN113768934A (zh) 2018-03-30 2021-12-10 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
BR112022001418A2 (pt) 2019-08-08 2022-06-07 Rigel Pharmaceuticals Inc Compostos e método para tratar a síndrome de liberação de citocinas
AU2020385527B2 (en) * 2019-11-21 2023-04-13 Tyk Medicines, Inc. Compound used as EGFR kinase inhibitor and use thereof
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN116444512A (zh) * 2023-04-13 2023-07-18 常州英诺升康生物医药科技有限公司 一种苯磺酰胺化合物的制备方法
US11773084B1 (en) * 2023-04-14 2023-10-03 King Faisal University 4-arylamino-2-(6-indolylamino)pyrimidine compounds as antibacterial agents

Family Cites Families (169)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4166452A (en) 1976-05-03 1979-09-04 Generales Constantine D J Jr Apparatus for testing human responses to stimuli
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4166542A (en) * 1977-12-05 1979-09-04 Bryan John F Jr Telescoping lattice boom crane
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
CN87210811U (zh) 1987-07-25 1988-04-20 徐正斌 方便投药盒
US5728536A (en) 1993-07-29 1998-03-17 St. Jude Children's Research Hospital Jak kinases and regulation of Cytokine signal transduction
CA2174080A1 (en) * 1993-10-12 1995-04-20 Paul Edward Aldrich 1n-alkyl-n-arylpyrimidinamines and derivatives thereof
US5700904A (en) 1995-06-07 1997-12-23 Eli Lilly And Company Preparation of an acylated protein powder
US6316635B1 (en) 1995-06-07 2001-11-13 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US6696448B2 (en) 1996-06-05 2004-02-24 Sugen, Inc. 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors
JPH10271051A (ja) 1997-03-11 1998-10-09 Alcatel Alsthom Co General Electricite 双方向等化を伴う送／受信装置
US6486185B1 (en) 1997-05-07 2002-11-26 Sugen, Inc. 3-heteroarylidene-2-indolinone protein kinase inhibitors
US6316429B1 (en) 1997-05-07 2001-11-13 Sugen, Inc. Bicyclic protein kinase inhibitors
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US6133305A (en) 1997-09-26 2000-10-17 Sugen, Inc. 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity
JP2002503662A (ja) 1998-02-17 2002-02-05 テュラリク インコーポレイテッド 抗ウイルス性ピリミジン誘導体
EP1091739A1 (en) 1998-06-30 2001-04-18 Parker Hughes Institute Method for inhibiting c-jun expression using jak-3 inhibitors
EP1105378B1 (en) 1998-08-21 2005-03-30 Parker Hughes Institute Quinazoline derivatives
DE69933680T2 (de) 1998-08-29 2007-08-23 Astrazeneca Ab Pyrimidine verbindungen
JP3635238B2 (ja) 1998-11-10 2005-04-06 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の複製を阻害するピリミジン類
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6841567B1 (en) 1999-02-12 2005-01-11 Cephalon, Inc. Cyclic substituted fused pyrrolocarbazoles and isoindolones
US6624171B1 (en) 1999-03-04 2003-09-23 Smithkline Beecham Corporation Substituted aza-oxindole derivatives
GB9904995D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Substituted aza-oxindole derivatives
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
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
WO2001045641A2 (en) 1999-11-30 2001-06-28 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
EA006227B1 (ru) 1999-12-10 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА
CA2395520A1 (en) 1999-12-21 2001-06-28 Sugen, Inc. 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
ATE449764T1 (de) 1999-12-28 2009-12-15 Pharmacopeia Inc Cytokine, insbesondere tnf-alpha, hemmer
ATE369844T1 (de) 2000-01-24 2007-09-15 Genzyme Corp Inhibitoren des jak/stat-weges und deren verwendung zur behandlung von allgemeiner primärer osteoarthritis
DE10003668B4 (de) 2000-01-28 2005-09-15 Xion Gmbh Flexibles Endoskop
WO2001056993A2 (en) 2000-02-05 2001-08-09 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of erk
IL145757A (en) 2000-02-05 2007-12-03 Vertex Pharma History of pyrazole and pharmaceutical preparations containing them
HUP0301117A3 (en) 2000-02-17 2004-01-28 Amgen Inc Thousand Oaks Imidazole derivatives kinase inhibitors, their use, process for their preparation and pharmaceutical compositions containing them
GB0004888D0 (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
GB0004886D0 (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
US6608048B2 (en) 2000-03-28 2003-08-19 Wyeth Holdings Tricyclic protein kinase inhibitors
AR028261A1 (es) 2000-03-28 2003-04-30 Wyeth Corp Inhibidores triciclicos de la proteina quinasa
US7276510B2 (en) 2000-05-08 2007-10-02 Janssen Pharmaceutica, Inc. HIV replication inhibitors
US7034019B2 (en) 2000-05-08 2006-04-25 Janssen Pharmaceutica N.V. Prodrugs of HIV replication inhibiting pyrimidines
EA006153B1 (ru) 2000-06-26 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ
GB0016877D0 (en) * 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
WO2002043735A1 (en) 2000-11-29 2002-06-06 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
US20020115173A1 (en) 2000-12-11 2002-08-22 Children's Medical Center Corporation Short peptides from the 'A-region' of protein kinases which selectively modulate protein kinase activity
AR035721A1 (es) 2000-12-20 2004-07-07 Sugen Inc Indolinonas 4-aril sustituidas; sus composiciones farmaceuticas y metodo para modular la actividad catalitica de una proteina quinasa
ES2556946T3 (es) * 2000-12-21 2016-01-21 Novartis Ag Pirimidinaminas como moduladores de la angiogénesis
EP1345925B1 (en) 2000-12-21 2006-05-17 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
EP1363702A4 (en) 2001-01-30 2007-08-22 Cytopia Pty Ltd PROCESS FOR INHIBITING KINASES
AUPR279101A0 (en) 2001-01-30 2001-02-22 Cytopia Pty Ltd Protein kinase signalling
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
BR0207096A (pt) 2001-02-20 2004-01-20 Astrazeneca Ab Uso de um composto, compostos, formulação farmacêutica, e, método de tratamento e/ou profilaxia de condições associadas com a inibição de glicogênio sintase quinase-3
AU2002312933B2 (en) * 2001-05-29 2007-12-06 Schering Ag CDK inhibiting pyrimidines, production thereof and their use as medicaments
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
DE60232510D1 (de) 2001-06-15 2009-07-16 Vertex Pharma 5-(2-aminopyrimidin-4-yl)benzisoxazole als proteinkinasehemmer
WO2002102313A2 (en) 2001-06-19 2002-12-27 Bristol-Myers Squibb Company Pyrimidine inhibitors of phosphodiesterase (pde) 7
US6878697B2 (en) 2001-06-21 2005-04-12 Ariad Pharmaceuticals, Inc. Phenylamino-pyrimidines and uses thereof
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
US6433018B1 (en) 2001-08-31 2002-08-13 The Research Foundation Of State University Of New York Method for reducing hypertrophy and ischemia
AU2002334355A1 (en) 2001-09-06 2003-03-18 Prochon Biotech Ltd. Protein tyrosine kinase inhibitors
EP1436259A1 (en) 2001-09-10 2004-07-14 Congxin Liang 3-(4,5,6,7-tetrahydroindol-2-ylmethylidiene)-2-indolinone derivatives as kinase inhibitors
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
EP1453516A2 (de) * 2001-10-17 2004-09-08 Boehringer Ingelheim Pharma GmbH & Co.KG 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren
DK1438053T3 (da) 2001-10-17 2008-12-08 Boehringer Ingelheim Pharma Pyrimidinderivater, lægemiddel indeholdende disse forbindelser, deres anvendelse og fremgangsmåder til deres fremstilling
PY0228255A (es) 2001-12-06 2004-06-01 Pfizer Prod Inc Compuestos cristalinos novedosos
SE0104140D0 (sv) 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
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
WO2003066601A1 (en) 2002-02-08 2003-08-14 Smithkline Beecham Corporation Pyrimidine compounds
US7338959B2 (en) 2002-03-01 2008-03-04 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
US7271179B2 (en) 2002-05-06 2007-09-18 Vertex Pharmaceuticals Incorporated Inhibitors of JAK protein kinase
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
AU2003231880A1 (en) 2002-05-30 2003-12-19 Vertex Pharmaceuticals Incorporated Inhibitors of jak and cdk2 protein kinases
CN1688553A (zh) 2002-06-17 2005-10-26 史密丝克莱恩比彻姆公司 化学方法
EP1518855B1 (en) 2002-06-28 2011-10-26 Astellas Pharma Inc. Diaminopyrimidinecarboxa mide derivative
AU2003252216A1 (en) 2002-07-17 2004-02-02 Mitsubishi Chemical Corporation Water-soluble complex dye, recording fluid, and method of recording
BR0313059B8 (pt) 2002-07-29 2021-07-27 Rigel Pharmaceuticals composto, e, composição farmacêutica
CA2495386C (en) 2002-08-14 2011-06-21 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
ATE375338T1 (de) * 2002-08-21 2007-10-15 Teva Pharma Verfahren zur aufreinigung von lanzoprazol
BR0314603A (pt) 2002-09-20 2005-07-26 Alcon Inc Uso de inibidores da sìntese de citoquina para o tratamento de distúrbios de olhos secos
EP2172460A1 (en) 2002-11-01 2010-04-07 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
US7259161B2 (en) 2002-11-04 2007-08-21 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
US7348335B2 (en) 2002-11-05 2008-03-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
KR100481130B1 (ko) 2002-11-08 2005-04-07 주식회사 웨어밸리 데이터베이스 시스템에 접속하지 않고 데이터베이스시스템을 모니터링하는 방법
GB0226582D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Anti-viral compounds
GB0226583D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
CN101353321A (zh) 2002-11-21 2009-01-28 辉瑞产品公司 3-氨基-哌啶衍生物及其制备方法
AU2003276591A1 (en) 2002-11-26 2004-06-18 Pfizer Products Inc. Method of treatment of transplant rejection
ATE425160T1 (de) 2002-12-18 2009-03-15 Vertex Pharma Benzisoxazolderivate, die sich als inhibitoren von proteinkinasen eigen
PL227577B1 (pl) 2003-02-07 2017-12-29 Janssen Pharmaceutica Nv Zastosowanie pochodnych pirymidyny do wytwarzania leku do zapobiegania zakażeniu wirusem HIV oraz kompozycja farmaceutyczna
GB2398582A (en) 2003-02-20 2004-08-25 Schlumberger Holdings System and method for maintaining zonal isolation in a wellbore
DE602004021472D1 (en) 2003-02-20 2009-07-23 Smithkline Beecham Corp Pyrimiidinverbindungen
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.
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
WO2004092154A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
DE602004008762T2 (de) 2003-04-30 2008-06-12 The Institutes for Pharmaceutical Discovery, LLC, Branford Substituierte heteroarylverbindungen als inhibitoren von proteintyrosinphosphatasen
GB0311276D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
GB0311274D0 (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
US7979448B2 (en) 2003-06-25 2011-07-12 International Business Machines Corporation Mail and calendar tool and method
AU2004257260A1 (en) 2003-07-10 2005-01-27 Neurogen Corporation Substituted heterocyclic diarylamine analogues
JP2007526894A (ja) 2003-07-16 2007-09-20 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 グリコーゲンシンターゼキナーゼ３インヒビターとしてのトリアゾロピリミジン誘導体
ATE370142T1 (de) * 2003-07-16 2007-09-15 Janssen Pharmaceutica Nv Triazolopyrimidinderivate als inhibitoren von glycogensynthasekinase-3
US20070161637A1 (en) 2003-07-22 2007-07-12 Neurogen Corporation Substituted pyridin-2-ylamine analogues
WO2005009957A1 (en) 2003-07-24 2005-02-03 Merck & Co., Inc. Tyrosine kinase inhibitors
CN102358738A (zh) * 2003-07-30 2012-02-22 里格尔药品股份有限公司 2,4-嘧啶二胺化合物及其预防和治疗自体免疫疾病的用途
EP1648875A1 (en) 2003-07-30 2006-04-26 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
EP1663242B1 (en) * 2003-08-07 2011-04-27 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents
BRPI0413469A (pt) 2003-08-14 2006-10-17 Pfizer derivados de piperazina para o tratamento de infecções por hiv
TWI378923B (en) * 2003-08-15 2012-12-11 Novartis Ag Pyrimidine derivatives
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
WO2005028467A1 (en) 2003-09-15 2005-03-31 Anadys Pharmaceuticals, Inc. Antibacterial 3,5-diaminopiperidine-substitute aromatic and heteroaromatic compounds
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
BRPI0414544A (pt) * 2003-09-18 2006-11-07 Novartis Ag 2,4-di-(fenilamino) pirimidinas úteis no tratamento de transtornos proliferativos
AP2006003517A0 (en) 2003-09-25 2006-02-28 Janssen Pharmaceutica Nv Hiv replication purine derivatives.
MXPA06003749A (es) 2003-10-03 2006-06-14 Pfizer Derivados de tropano.
DE10349423A1 (de) 2003-10-16 2005-06-16 Schering Ag Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
TW200529849A (en) 2003-11-28 2005-09-16 Novartis Ag Diaryl urea derivatives in the treatment of protein kinase dependent diseases
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
US20080207613A1 (en) 2004-01-12 2008-08-28 Cytopia Research Pty Ltd Selective Kinase Inhibitors
GB0402653D0 (en) 2004-02-06 2004-03-10 Cyclacel Ltd Compounds
KR100645040B1 (ko) 2004-02-09 2006-11-10 삼성전자주식회사 소오스 스트래핑을 갖는 플래시 메모리 소자의 셀 어레이
CA2553785C (en) 2004-02-14 2011-02-08 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2005107760A1 (en) 2004-04-30 2005-11-17 Irm Llc Compounds and compositions as inducers of keratinocyte differentiation
US7754714B2 (en) * 2004-05-18 2010-07-13 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
US7268012B2 (en) 2004-08-31 2007-09-11 Micron Technology, Inc. Methods for fabrication of thin semiconductor assemblies including redistribution layers and packages and assemblies formed thereby
WO2006028833A1 (en) * 2004-09-01 2006-03-16 Rigel Pharmaceuticals, Inc. Synthesis of 2,4-pyrimidinediamine compounds
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
US7531548B2 (en) 2004-09-30 2009-05-12 Tibotec Pharmaceuticals Ltd HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
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
CA2590110C (en) * 2004-12-30 2014-06-03 Exelixis, Inc. Kinase modulators and method of use
JP4801096B2 (ja) * 2005-01-19 2011-10-26 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およびそれらの使用
US20060270694A1 (en) 2005-05-03 2006-11-30 Rigel Pharmaceuticals, Inc. JAK kinase inhibitors and their uses
WO2006129100A1 (en) * 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
EP1904457B1 (en) * 2005-06-08 2017-09-06 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CA2607901C (en) * 2005-06-13 2016-08-16 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders using a syk inhibitory 2,4-pyrimidinediamine
NZ564872A (en) 2005-07-11 2010-01-29 Sanofi Aventis Novel 2,4-dianilinopyrimidine derivatives, the preparation thereof, their use as medicaments, pharmaceutical compositions and, in particular, as ikk inhibitors
US8321953B2 (en) 2005-07-14 2012-11-27 Imation Corp. Secure storage device with offline code entry
WO2007053844A2 (en) * 2005-10-31 2007-05-10 Rigel Pharmaceuticals, Inc. Compositions and methods for treating inflammatory disorders
US7528143B2 (en) 2005-11-01 2009-05-05 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US7962290B1 (en) * 2006-01-09 2011-06-14 Rigel Pharmaceuticals, Inc. Identification of pharmacophores from co-crystals of spleen tyrosine kinase (SYK) and SYK ligands
WO2007085540A1 (en) 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
JP4653842B2 (ja) * 2006-02-17 2011-03-16 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 自己免疫疾患を治療または予防するための２，４−ピリミジンジアミン化合物
JP2009528295A (ja) * 2006-02-24 2009-08-06 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
GB0605691D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
ATE497496T1 (de) * 2006-10-19 2011-02-15 Rigel Pharmaceuticals Inc 2,4-pyridimediamon-derivate als hemmer von jak- kinasen zur behandlung von autoimmunerkrankungen
ES2380551T3 (es) 2006-11-21 2012-05-16 Rigel Pharmaceuticals, Inc. Sales de profármaco de compuestos de 2,4-pirimidindiamina y sus usos
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
WO2009003136A1 (en) 2007-06-26 2008-12-31 Rigel Pharmaceuticals, Inc. Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders
CA2691914C (en) 2007-07-11 2012-06-26 Pfizer Inc. Pharmaceutical compositions and methods of treating dry eye 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
PL2389372T3 (pl) * 2009-01-23 2016-02-29 Rigel Pharmaceuticals Inc Kompozycje i sposoby hamowania szlaku JAK

Also Published As

Publication number Publication date
NZ563454A (en) 2011-03-31
IL187257A0 (en) 2008-02-09
ES2651349T3 (es) 2018-01-25
CN105348203B (zh) 2018-09-18
US20090041786A1 (en) 2009-02-12
IL187257A (en) 2014-07-31
WO2006133426A3 (en) 2007-11-08
US20160102084A1 (en) 2016-04-14
US11827628B2 (en) 2023-11-28
US20170298054A1 (en) 2017-10-19
US20060293311A1 (en) 2006-12-28
US20130142807A1 (en) 2013-06-06
EP1904457A2 (en) 2008-04-02
RU2007148812A (ru) 2009-07-20
MX286273B (es) 2011-05-04
SG137989A1 (en) 2008-01-28
US8815848B2 (en) 2014-08-26
AU2006254840B2 (en) 2012-08-02
BRPI0610876B8 (pt) 2021-05-25
JP2008543778A (ja) 2008-12-04
WO2006133426A2 (en) 2006-12-14
US20080306099A1 (en) 2008-12-11
US20220098181A1 (en) 2022-03-31
US8415365B2 (en) 2013-04-09
US10421752B2 (en) 2019-09-24
US9732073B2 (en) 2017-08-15
EP1904457B1 (en) 2017-09-06
CA2608367C (en) 2014-08-19
US20200181130A1 (en) 2020-06-11
CA2608367A1 (en) 2006-12-14
NO20080075L (no) 2008-03-03
RU2485106C2 (ru) 2013-06-20
KR20080017454A (ko) 2008-02-26
NO341966B1 (no) 2018-03-05
JP5480936B2 (ja) 2014-04-23
AU2006254840A1 (en) 2006-12-14
US7491732B2 (en) 2009-02-17
US8399472B2 (en) 2013-03-19
JP2012229217A (ja) 2012-11-22
US9248190B2 (en) 2016-02-02
US11198689B2 (en) 2021-12-14
US20140314785A1 (en) 2014-10-23
BRPI0610876A2 (pt) 2008-12-02
MX2007015464A (es) 2008-03-04
CN105348203A (zh) 2016-02-24
EP1904457A4 (en) 2010-06-02
BRPI0610876B1 (pt) 2020-12-29
KR101312225B1 (ko) 2013-09-26

Similar Documents

Publication Publication Date Title
US11827628B2 (en) Compositions and methods for inhibition of the JAK pathway
US11667611B2 (en) Compositions and methods for inhibition of the JAK pathway
US9481654B2 (en) Compositions and methods for inhibition of the JAK pathway
CN101282945A (zh) 抑制jak途径的组合物和方法
HK1115134A (en) Compositions and methods for inhibition of the jak pathway
HK1115134B (en) Compositions and methods for inhibition of the jak pathway

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20080827

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20081009

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20090603

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20090603

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20120118

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20120130

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20120427

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20120509

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120607

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20120808

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20121207

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130125

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20130204

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: 20130220

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20130312

R150 Certificate of patent or registration of utility model

Ref document number: 5225079

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: 20160322

Year of fee payment: 3

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

LAPS Cancellation because of no payment of annual fees