CN107108561B - 用作irak抑制剂的杂芳基化合物及其用途 - Google Patents

用作irak抑制剂的杂芳基化合物及其用途 Download PDF

Info

Publication number
CN107108561B
CN107108561B CN201580073060.9A CN201580073060A CN107108561B CN 107108561 B CN107108561 B CN 107108561B CN 201580073060 A CN201580073060 A CN 201580073060A CN 107108561 B CN107108561 B CN 107108561B
Authority
CN
China
Prior art keywords
methyl
pyrazol
mmol
phenyl
pyrimidin
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
CN201580073060.9A
Other languages
English (en)
Chinese (zh)
Other versions
CN107108561A (zh
Inventor
C·乔兰德-勒布伦
R·琼斯
A·C·温
N·恩古耶
T·L·约翰逊
L·C·德赛尔姆
K·潘达
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CN107108561A publication Critical patent/CN107108561A/zh
Application granted granted Critical
Publication of CN107108561B publication Critical patent/CN107108561B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
CN201580073060.9A 2014-11-20 2015-11-19 用作irak抑制剂的杂芳基化合物及其用途 Expired - Fee Related CN107108561B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462082231P 2014-11-20 2014-11-20
US62/082,231 2014-11-20
PCT/US2015/061463 WO2016081679A1 (en) 2014-11-20 2015-11-19 Heteroaryl compounds as irak inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
CN107108561A CN107108561A (zh) 2017-08-29
CN107108561B true CN107108561B (zh) 2020-08-28

Family

ID=54705914

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580073060.9A Expired - Fee Related CN107108561B (zh) 2014-11-20 2015-11-19 用作irak抑制剂的杂芳基化合物及其用途

Country Status (24)

Country Link
US (2) US9790221B2 (enExample)
EP (1) EP3221306B1 (enExample)
JP (1) JP6787892B2 (enExample)
KR (2) KR102683518B1 (enExample)
CN (1) CN107108561B (enExample)
AR (1) AR103138A1 (enExample)
AU (1) AU2015349899B9 (enExample)
CA (1) CA2964982C (enExample)
DK (1) DK3221306T3 (enExample)
ES (1) ES2772133T3 (enExample)
HR (1) HRP20200179T1 (enExample)
HU (1) HUE047586T2 (enExample)
IL (1) IL252346B (enExample)
LT (1) LT3221306T (enExample)
MX (1) MX375625B (enExample)
NZ (1) NZ730728A (enExample)
PL (1) PL3221306T3 (enExample)
PT (1) PT3221306T (enExample)
RS (1) RS59974B1 (enExample)
RU (1) RU2743718C2 (enExample)
SG (1) SG11201702741SA (enExample)
SI (1) SI3221306T1 (enExample)
WO (1) WO2016081679A1 (enExample)
ZA (1) ZA201702402B (enExample)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3286181T3 (pl) 2015-04-22 2021-08-02 Rigel Pharmaceuticals, Inc. Związki pirazolowe oraz sposób wytwarzania i zastosowania tych związków
MX2018010192A (es) * 2016-02-25 2019-01-31 Asceneuron S A Inhibidores de glucosidasa.
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
US10414753B2 (en) 2016-10-26 2019-09-17 Rigel Pharmaceuticals, Inc. Amide compounds and method for making and using
US10370367B2 (en) 2016-10-26 2019-08-06 Rigel Pharmaceuticals, Inc. IRAK inhibitors and method for making and using
JP7308146B2 (ja) * 2016-11-22 2023-07-13 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 インターロイキン1受容体関連キナーゼの阻害剤およびその使用
US11072599B2 (en) * 2017-02-01 2021-07-27 Biotheryx, Inc. Pyrazole compounds and uses thereof
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
JP6920467B2 (ja) * 2017-05-02 2021-08-18 コリア リサーチ インスティチュート オブ ケミカル テクノロジーKorea Research Institute Of Chemical Technology ピリミジン誘導体化合物、その光学異性体、またはその薬学的に許容される塩、及びそれを有効成分として含むtyro3関連疾患の予防または治療用組成物
US20210145771A1 (en) * 2017-07-03 2021-05-20 Glaxosmithkline Intellectual Property Development Limited N-(3-(2-(4-chlorophenoxy)acetamido)bicyclo[1.1.1] pentan-1-yl)-2-cyclobutane-1- carboxamide derivatives and related compounds as atf4 inhibitors for treating cancer and other diseases
CN111094233B (zh) 2017-08-09 2024-03-15 戴纳立制药公司 化合物、组合物及方法
PT3676297T (pt) 2017-09-01 2023-08-29 Denali Therapeutics Inc Compostos, composições e métodos
WO2019060742A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc AGENTS FOR DEGRADING PROTEINS AND USES THEREOF
EP3684366A4 (en) 2017-09-22 2021-09-08 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES OF THE LATEST
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
TWI842978B (zh) 2018-07-13 2024-05-21 美商基利科學股份有限公司 衍生物
TWI727392B (zh) * 2018-08-13 2021-05-11 美商基利科學股份有限公司 噻二唑irak4抑制劑
US11352350B2 (en) 2018-11-30 2022-06-07 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
CA3129609A1 (en) 2019-02-13 2020-08-20 Denali Therapeutics Inc. Eukaryotic initiation factor 2b modulators
MA54959A (fr) 2019-02-13 2021-12-22 Denali Therapeutics Inc Composés, compositions et procédés
MX2022002292A (es) 2019-08-30 2022-06-02 Rigel Pharmaceuticals Inc Compuestos de pirazol, formulaciones de los mismos y un metodo para usar los compuestos y/o formulaciones.
EP4076520A4 (en) 2019-12-17 2024-03-27 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021127283A2 (en) 2019-12-17 2021-06-24 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
TW202241891A (zh) 2020-12-30 2022-11-01 美商凱麥拉醫療公司 Irak降解劑及其用途
JP2024506656A (ja) 2021-02-15 2024-02-14 カイメラ セラピューティクス, インコーポレイテッド Irak4分解剤およびその使用
WO2022187303A1 (en) 2021-03-03 2022-09-09 Rigel Pharmaceuticals, Inc. A method for treating a disease or condition using a pyrazole compound or formulation thereof
EP4320103A1 (en) * 2021-04-09 2024-02-14 Quanta Therapeutics, Inc. Pyrimidine based ras modulators and uses thereof
US12097261B2 (en) 2021-05-07 2024-09-24 Kymera Therapeutics, Inc. CDK2 degraders and uses thereof
WO2023076556A1 (en) 2021-10-29 2023-05-04 Kymera Therapeutics, Inc. Irak4 degraders and synthesis thereof
CN116514769B (zh) * 2022-01-21 2024-02-27 中国药科大学 4-羟基嘧啶-5-甲酰腙衍生物、制备方法、药物组合物和应用
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
JP7713603B2 (ja) 2022-02-09 2025-07-25 クアンタ セラピューティクス, インコーポレイテッド Krasモジュレーターおよびその使用
JP2025513716A (ja) 2022-03-23 2025-04-30 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 Irak阻害剤としてのピリミド-2-イル-ピラゾール化合物
CA3257281A1 (en) 2022-05-25 2023-11-30 Quanta Therapeutics Inc PYRIMIDINE-BASED MODULATORS AND THEIR USES
WO2024192424A1 (en) 2023-03-15 2024-09-19 Quanta Therapeutics, Inc. Kras modulators and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009054253A1 (ja) * 2007-10-26 2009-04-30 Konica Minolta Holdings, Inc. 有機エレクトロルミネッセンス素子、表示装置及び照明装置
WO2013134415A1 (en) * 2012-03-07 2013-09-12 Vertex Pharmaceuticals Incorporated Mannose derivatives for treating bacterial infections
WO2014008992A1 (en) * 2012-07-10 2014-01-16 Ares Trading S.A. Pyrimidine pyrazolyl derivatives

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090058276A1 (en) 2007-08-20 2009-03-05 Holliday Bradley J METAL-CONTAINING POLYMERS and uses thereof
DK2307376T3 (en) 2008-08-04 2016-01-11 Merck Patent Gmbh NOVEL phenylamino ISONIKOTINAMIDFORBINDELSER
US20120270237A9 (en) * 2009-04-03 2012-10-25 Cellzone AG Methods for the identification of kinase interacting molecules and for the purification of kinase proteins
JP2011098948A (ja) 2009-06-25 2011-05-19 Yamagata Promotional Organization For Industrial Technology ビピリジン誘導体及びそれを含む有機エレクトロルミネッセンス素子
EP2515657A4 (en) * 2009-12-21 2013-07-03 Merck Sharp & Dohme Tyrosine kinase inhibitor
KR101995013B1 (ko) * 2010-07-13 2019-07-02 에프. 호프만-라 로슈 아게 Irak4 조절제로서 피라졸로[1,5a]피리미딘 및 티에노[3,2b]피리미딘 유도체
JP6036804B2 (ja) * 2012-03-22 2016-11-30 コニカミノルタ株式会社 透明電極、電子デバイス及び有機エレクトロルミネッセンス素子
CA2933107C (en) * 2014-01-09 2022-06-21 Merck Patent Gmbh Pyrimidine pyrazolyl derivatives and their use as irak inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009054253A1 (ja) * 2007-10-26 2009-04-30 Konica Minolta Holdings, Inc. 有機エレクトロルミネッセンス素子、表示装置及び照明装置
WO2013134415A1 (en) * 2012-03-07 2013-09-12 Vertex Pharmaceuticals Incorporated Mannose derivatives for treating bacterial infections
WO2014008992A1 (en) * 2012-07-10 2014-01-16 Ares Trading S.A. Pyrimidine pyrazolyl derivatives

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
RN 1185364-46-8;CAS;《STN REGISTRY》;20090917 *
RN 1185533-85-0;CAS;《STN REGISTRY》;20090917 *

Also Published As

Publication number Publication date
AR103138A1 (es) 2017-04-19
HUE047586T2 (hu) 2020-04-28
KR102683518B1 (ko) 2024-07-10
RU2017120274A3 (enExample) 2019-03-18
LT3221306T (lt) 2020-03-10
WO2016081679A1 (en) 2016-05-26
US9790221B2 (en) 2017-10-17
JP6787892B2 (ja) 2020-11-18
JP2017536369A (ja) 2017-12-07
SI3221306T1 (sl) 2020-03-31
MX375625B (es) 2025-03-06
MX2017006266A (es) 2017-08-14
AU2015349899B9 (en) 2020-06-25
KR20230158647A (ko) 2023-11-20
ES2772133T3 (es) 2020-07-07
HRP20200179T1 (hr) 2020-05-01
EP3221306A1 (en) 2017-09-27
PT3221306T (pt) 2020-02-19
US10030013B2 (en) 2018-07-24
CN107108561A (zh) 2017-08-29
EP3221306B1 (en) 2019-11-13
BR112017009800A2 (pt) 2017-12-26
US20160145252A1 (en) 2016-05-26
US20180002327A1 (en) 2018-01-04
RS59974B1 (sr) 2020-03-31
KR20170086057A (ko) 2017-07-25
PL3221306T3 (pl) 2020-09-07
SG11201702741SA (en) 2017-04-27
ZA201702402B (en) 2020-07-29
CA2964982A1 (en) 2016-05-26
IL252346A0 (en) 2017-07-31
NZ730728A (en) 2022-04-29
AU2015349899B2 (en) 2020-02-06
AU2015349899A1 (en) 2017-04-20
CA2964982C (en) 2022-07-05
IL252346B (en) 2019-09-26
RU2743718C2 (ru) 2021-02-24
DK3221306T3 (da) 2020-01-02
RU2017120274A (ru) 2018-12-20

Similar Documents

Publication Publication Date Title
CN107108561B (zh) 用作irak抑制剂的杂芳基化合物及其用途
US9969710B2 (en) Heteroaryl compounds as IRAK inhibitors and uses thereof
CN112236429B (zh) 用作ii型irak抑制剂的杂芳基化合物及其用途
CN107849055B (zh) 用作irak1/4抑制剂的大环化合物及其用途
US10517872B2 (en) Pyridazinone macrocycles as IRAK inhibitors and uses thereof
US20230019491A1 (en) PYRIMIDINE TBK/IKKe INHIBITOR COMPOUNDS AND USES THEREOF
CN111971278A (zh) 用作irak抑制剂的喹啉化合物及其用途
US11440899B2 (en) Pyrimidine TBK/IKKe inhibitor compounds and uses thereof
HK1242303B (zh) 用作irak抑制剂的杂芳基化合物及其用途
HK1242303A1 (en) Heteroaryl compounds as irak inhibitors and uses thereof
HK40043591A (en) Heteroaryl compounds as type ii irak inhibitors and uses thereof

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1242303

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20200828