TWI589579B - Ｉｒａｋ抑制劑及其用途 - Google Patents

Ｉｒａｋ抑制劑及其用途 Download PDF

Info

Publication number
TWI589579B
TWI589579B TW102101029A TW102101029A TWI589579B TW I589579 B TWI589579 B TW I589579B TW 102101029 A TW102101029 A TW 102101029A TW 102101029 A TW102101029 A TW 102101029A TW I589579 B TWI589579 B TW I589579B
Authority
TW
Taiwan
Prior art keywords
compound
disease
formula
pharmaceutically acceptable
ring
Prior art date
Application number
TW102101029A
Other languages
English (en)
Chinese (zh)
Other versions
TW201333014A (zh
Inventor
吉拉丹Ｃ 何瑞曼
羅納德Ｔ 威斯特
多納Ｌ 羅曼羅
梭尼斯 羅賓森
蜜 莎麗
馬修 大衛 瓦思勒
傑諾米 羅伯特 葛林梧
奎格Ｅ 瑪斯
林柏曼 羅撒納 坎培爾
Original Assignee
林伯士艾瑞斯公司
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 林伯士艾瑞斯公司 filed Critical 林伯士艾瑞斯公司
Publication of TW201333014A publication Critical patent/TW201333014A/zh
Application granted granted Critical
Publication of TWI589579B publication Critical patent/TWI589579B/zh

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—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
    • A61K31/435—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
    • A61K31/4365—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 having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P27/12—Ophthalmic agents for cataracts
    • 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
    • A61P27/14—Decongestants or antiallergics
    • 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
    • A61P27/16—Otologicals
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • 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
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
TW102101029A 2012-01-10 2013-01-10 Ｉｒａｋ抑制劑及其用途 TWI589579B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261585194P 2012-01-10 2012-01-10
US201261663227P 2012-06-22 2012-06-22
US201261682637P 2012-08-13 2012-08-13
US201261724695P 2012-11-09 2012-11-09
US201261734133P 2012-12-06 2012-12-06

Publications (2)

Publication Number Publication Date
TW201333014A TW201333014A (zh) 2013-08-16
TWI589579B true TWI589579B (zh) 2017-07-01

Family

ID=48781892

Family Applications (2)

Application Number Title Priority Date Filing Date
TW102101029A TWI589579B (zh) 2012-01-10 2013-01-10 Ｉｒａｋ抑制劑及其用途
TW106101765A TW201728592A (zh) 2012-01-10 2013-01-10 Ｉｒａｋ抑制劑及其用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW106101765A TW201728592A (zh) 2012-01-10 2013-01-10 Ｉｒａｋ抑制劑及其用途

Country Status (10)

Country Link
US (2) US9212190B2 (cg-RX-API-DMAC7.html)
EP (1) EP2802330A4 (cg-RX-API-DMAC7.html)
JP (2) JP6126131B2 (cg-RX-API-DMAC7.html)
CN (1) CN104582705A (cg-RX-API-DMAC7.html)
AU (2) AU2013207972B2 (cg-RX-API-DMAC7.html)
BR (1) BR112014017021A8 (cg-RX-API-DMAC7.html)
CA (1) CA2863259A1 (cg-RX-API-DMAC7.html)
HK (1) HK1209632A1 (cg-RX-API-DMAC7.html)
TW (2) TWI589579B (cg-RX-API-DMAC7.html)
WO (1) WO2013106535A1 (cg-RX-API-DMAC7.html)

Families Citing this family (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX342405B (es) 2010-06-03 2016-09-28 Pharmacyclics Inc El uso de inhibidores de la tirosina quinasa de bruton (btk).
EP2595993B1 (en) 2010-07-23 2018-04-18 President and Fellows of Harvard College Tricyclic proteasome activity enhancing compounds
EP2663312B1 (en) 2011-01-10 2017-10-11 Nimbus Iris, Inc. Irak inhibitors and uses thereof
HK1209632A1 (en) 2012-01-10 2016-04-08 林伯士艾瑞斯公司 Irak inhibitors and uses thereof
JP2015513317A (ja) * 2012-01-25 2015-05-07 プロテオステイシス セラピューティクス，インコーポレイテッド プロテアソーム活性を増強する化合物
AU2013202368B2 (en) * 2012-01-25 2016-06-16 Proteostasis Therapeutics, Inc. Proteasome activity modulating compounds
EP2872144A4 (en) 2012-07-11 2015-12-02 Nimbus Iris Inc IRAQ INHIBITOR AND USES THEREOF
CN104902959A (zh) 2012-07-11 2015-09-09 林伯士艾瑞斯公司 Irak抑制剂和其用途
BR112015001690A2 (pt) 2012-07-24 2017-11-07 Pharmacyclics Inc mutações associadas com a resistência a inibidores da tirosina quinase de bruton (btk)
BR112015014034A2 (pt) * 2013-01-10 2017-07-11 Nimbus Iris Inc inibidores de irak e usos dos mesmos
US8778365B1 (en) 2013-01-31 2014-07-15 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
EP2951187A1 (en) 2013-02-01 2015-12-09 Bayer Pharma Aktiengesellschaft Substituted thienopyrimidines and pharmaceutical use thereof
KR102280614B1 (ko) 2013-03-15 2021-07-21 글로벌 블러드 테라퓨틱스, 인크. 헤모글로빈 조정을 위한 화합물 및 이의 용도
WO2014194201A2 (en) * 2013-05-31 2014-12-04 Nimbus Iris, Inc. Cdk8 inhibitors and uses thereof
WO2014194242A2 (en) * 2013-05-31 2014-12-04 Nimbus Iris, Inc. Flt3 inhibitors and uses thereof
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
EP3049086A4 (en) * 2013-09-27 2017-02-22 Nimbus Iris, Inc. Irak inhibitors and uses thereof
EA201992707A1 (ru) 2013-11-18 2020-06-30 Глобал Блад Терапьютикс, Инк. Соединения и их применения для модуляции гемоглобина
TW201605867A (zh) * 2013-11-20 2016-02-16 拜耳製藥公司 噻吩并嘧啶
TWI667233B (zh) 2013-12-19 2019-08-01 德商拜耳製藥公司 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途
JP2017509336A (ja) 2014-03-20 2017-04-06 ファーマサイクリックス エルエルシー ホスホリパーゼｃガンマ２及び耐性に関連した変異
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US20160008366A1 (en) * 2014-07-14 2016-01-14 Pharmacyclics Llc Btk inhibitors for the treatment of cns malignancies
PE20171239A1 (es) 2014-10-24 2017-08-24 Bristol Myers Squibb Co Derivados de carbazol
JP2016124791A (ja) * 2014-12-26 2016-07-11 国立大学法人 千葉大学 新規化合物及びこれを有効成分とする抗ウイルス剤
CN104592248A (zh) * 2014-12-31 2015-05-06 芜湖杨燕制药有限公司 一种4-氯-6-取代噻吩并[2,3-d]嘧啶化合物的制备方法
CN113750094A (zh) 2015-04-22 2021-12-07 里格尔药品股份有限公司 吡唑化合物以及制备和使用该化合物的方法
EP3719016A1 (en) * 2015-08-04 2020-10-07 Rigel Pharmaceuticals, Inc. Benzazole compounds and methods for making and using the compounds
SG10201508795XA (en) * 2015-10-23 2017-05-30 Agency Science Tech & Res Method for treating cancer
US11542261B2 (en) 2016-08-17 2023-01-03 Children's Hospital Medical Center Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors
US11254667B2 (en) 2016-08-17 2022-02-22 Children's Hospital Medical Center Substituted imidazo[1,2-A]pyridines as IRAK 1/4 and flt3 inhibitors
WO2018081738A1 (en) * 2016-10-28 2018-05-03 Children's Hospital Medical Center Treatment of diseases associated with activated irak
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
WO2019001461A1 (zh) * 2017-06-27 2019-01-03 南京明德新药研发股份有限公司 Irak4抑制剂
JP7366031B2 (ja) 2017-09-22 2023-10-20 カイメラ セラピューティクス， インコーポレイテッド タンパク質分解剤およびそれらの使用
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
WO2019099926A1 (en) 2017-11-17 2019-05-23 Arvinas, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
CN108033931B (zh) * 2017-12-28 2020-03-10 山东铂源药业有限公司 一种N-Boc哌嗪的合成方法
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
WO2019140387A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
EP3817822A4 (en) 2018-07-06 2022-07-27 Kymera Therapeutics, Inc. PROTEIN DEGRADANTS AND USES THEREOF
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
TWI721483B (zh) 2018-07-13 2021-03-11 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
WO2020016850A1 (en) * 2018-07-20 2020-01-23 Merck Patent Gmbh A substituted amino-pyrimidine compound for use in a method for treatment and prevention of multiple sclerosis
EP3841100A1 (en) 2018-08-20 2021-06-30 Arvinas Operations, Inc. Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases
KR20250167680A (ko) 2018-11-30 2025-12-01 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
US20230030720A1 (en) 2018-12-06 2023-02-02 Daiichi Sankyo Company, Limited Cycloalkane-1,3-diamine derivative
JP7458406B2 (ja) 2018-12-21 2024-03-29 セルジーン コーポレーション Ｒｉｐｋ２のチエノピリジン阻害剤
WO2020264499A1 (en) * 2019-06-28 2020-12-30 Kymera Therapeutics, Inc. Irak degraders and uses thereof
AU2020335903A1 (en) 2019-08-30 2022-03-24 Rigel Pharmaceuticals, Inc. Pyrazole compounds, formulations thereof, and a method for using the compounds and/or formulations
WO2021127190A1 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
US11591332B2 (en) 2019-12-17 2023-02-28 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
AU2021396308A1 (en) * 2020-12-09 2023-06-22 Kymera Therapeutics, Inc. Irak degraders 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
CN116867494A (zh) 2021-02-15 2023-10-10 凯麦拉医疗公司 Irak4降解剂和其用途
TW202245788A (zh) 2021-02-15 2022-12-01 美商凱麥拉醫療公司 Irak4降解劑及其用途
US12357623B2 (en) 2021-03-03 2025-07-15 Rigel Pharmaceuticals, Inc. Method for treating a disease or condition using a pyrazole compound or formulation thereof
WO2022236058A1 (en) 2021-05-07 2022-11-10 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
AU2022378630A1 (en) 2021-10-29 2024-05-09 Kymera Therapeutics, Inc. Irak4 degraders and synthesis thereof
JP2025504059A (ja) 2022-01-31 2025-02-06 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋデグレーダー及びその使用
WO2023183377A1 (en) 2022-03-23 2023-09-28 Rigel Pharmaceuticals, Inc. Pyrimid-2-yl-pyrazole compounds as irak inhibitors
CN118978528A (zh) * 2024-08-02 2024-11-19 上海信诺维生物医药有限公司 一种irak4激酶抑制剂

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1937459A1 (de) * 1968-08-02 1970-02-05 Ciba Geigy Neue Pyrimidinderivate und Verfahren zu ihrer Herstellung
EP1323719A1 (en) 1999-03-30 2003-07-02 Nippon Soda Co., Ltd. Thienopyrimidine compounds and salts thereof and process for the preparation of the same
US6297238B1 (en) 1999-04-06 2001-10-02 Basf Aktiengesellschaft Therapeutic agents
WO2002088138A1 (en) * 2001-04-30 2002-11-07 Bayer Corporation Novel 4-amino-5,6-substituted thiopheno[2,3-d]pyrimidines
AU2002360774A1 (en) 2001-12-28 2003-07-24 Bayer Corporation 4-substituted fused heteropyrimidines and fused hetero-4-pyrimidones
US20030225098A1 (en) * 2002-03-21 2003-12-04 Hirst Gavin C. Kinase inhibitors
JP2006512313A (ja) 2002-10-31 2006-04-13 アムジェン インコーポレイテッド 抗炎症剤
CA2522595A1 (en) * 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
EP1773840B1 (de) 2004-07-23 2010-01-20 The Medicines Company (Leipzig) GmbH Substituierte pyrido[3',2':4,5]thieno[3,2-d]pyrimidine und pyrido[3',2':4,5]furo[3,2-d]-pyrimidine zur verwendung als inhibitoren der pda-4 und/oder tnf-alpha freisetzung
JP5301986B2 (ja) * 2005-06-22 2013-09-25 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 医薬組成物用のチエノピリミジン類
CA2668997C (en) 2006-11-09 2012-10-09 Ardea Biosciences, Inc. 4-cyanophenylamino-substituted bicyclic heterocyclic compounds as hiv inhibitors
US20100227853A1 (en) * 2008-04-18 2010-09-09 Trustees Of Boston College Inhibitors of cyclic amp phosphodiesterases
EP2285217A4 (en) * 2008-05-12 2011-06-08 Amnestix Inc CONNECTIONS TO IMPROVE LEARNING AND MEMORY
US20100063047A1 (en) 2008-09-10 2010-03-11 Kalypsys, Inc. Aminopyrimidine inhibitors of histamine receptors for the treatment of disease
EP2473054B1 (en) * 2009-09-04 2017-06-14 The Regents of the University of Michigan Compositions and methods for treatment of leukemia
JP2012254939A (ja) * 2009-10-07 2012-12-27 Astellas Pharma Inc オキサゾール化合物
WO2011072127A1 (en) * 2009-12-10 2011-06-16 The University Of North Carolina At Chapel Hill Selective beta-glucuronidase inhibitors as a treatment for side effects of camptothecin antineoplastic agents
MX358682B (es) 2010-07-13 2018-08-31 Hoffmann La Roche Derivados de pirazolo [1,5a]pirimidina y de tieno[3,2b] pirimidina como moduladores de la cinasa asociada al receptor de la interleucina 4 (irak4).
EP2595993B1 (en) 2010-07-23 2018-04-18 President and Fellows of Harvard College Tricyclic proteasome activity enhancing compounds
EP2663312B1 (en) * 2011-01-10 2017-10-11 Nimbus Iris, Inc. Irak inhibitors and uses thereof
IN2014CN04558A (cg-RX-API-DMAC7.html) * 2011-11-23 2015-09-18 Cancer Rec Tech Ltd
HK1209632A1 (en) 2012-01-10 2016-04-08 林伯士艾瑞斯公司 Irak inhibitors and uses thereof
CN104902959A (zh) 2012-07-11 2015-09-09 林伯士艾瑞斯公司 Irak抑制剂和其用途
EP2872144A4 (en) 2012-07-11 2015-12-02 Nimbus Iris Inc IRAQ INHIBITOR AND USES THEREOF
WO2014011911A2 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof

Also Published As

Publication number Publication date
US20130231328A1 (en) 2013-09-05
JP2017008110A (ja) 2017-01-12
US9212190B2 (en) 2015-12-15
CA2863259A1 (en) 2013-07-18
AU2013207972B2 (en) 2017-06-15
BR112014017021A2 (pt) 2017-06-13
EP2802330A4 (en) 2015-10-21
JP6126131B2 (ja) 2017-05-10
WO2013106535A9 (en) 2014-09-04
TW201333014A (zh) 2013-08-16
JP2015503618A (ja) 2015-02-02
HK1209632A1 (en) 2016-04-08
TW201728592A (zh) 2017-08-16
CN104582705A (zh) 2015-04-29
BR112014017021A8 (pt) 2017-07-04
AU2013207972A1 (en) 2014-07-31
EP2802330A1 (en) 2014-11-19
AU2017228639A1 (en) 2017-10-26
US20160193216A1 (en) 2016-07-07
WO2013106535A1 (en) 2013-07-18

Similar Documents

Publication Publication Date Title
TWI589579B (zh) Ｉｒａｋ抑制劑及其用途
EP2663312B1 (en) Irak inhibitors and uses thereof
TWI701245B (zh) 酪胺酸蛋白質激酶２（ｔｙｋ２）抑制劑及其用途
US9067948B2 (en) IRAK inhibitors and uses thereof
TWI825663B (zh) Tyk2抑制劑及其用途
TWI707852B (zh) Tyk2 抑制劑及其用途
TW201522349A (zh) Ｉｒａｋ抑制劑及彼等之用途
TW201639849A (zh) 酪胺酸蛋白質激酶２（ｔｙｋ２）抑制劑及其用途
US20250270200A1 (en) Ctps1 inhibitors and uses thereof
US20250162989A1 (en) Usp30 inhibitors and uses thereof
HK40075858A (en) Tyk2 inhibitors and uses thereof
HK1232534A1 (en) Tyk2 inhibitors and uses thereof
HK1232534B (en) Tyk2 inhibitors and uses thereof
BR112016019881B1 (pt) Compostos inibidores de tyk2, composição farmacêutica compreendendo os referidos compostos, usos dos mesmos e método de inibir tyk2 em uma amostra biológica

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees