HRP20210036T1 - Soli inhibitora pi3k i postupci za njihovo dobivanje - Google Patents
Soli inhibitora pi3k i postupci za njihovo dobivanje Download PDFInfo
- Publication number
- HRP20210036T1 HRP20210036T1 HRP20210036TT HRP20210036T HRP20210036T1 HR P20210036 T1 HRP20210036 T1 HR P20210036T1 HR P20210036T T HRP20210036T T HR P20210036TT HR P20210036 T HRP20210036 T HR P20210036T HR P20210036 T1 HRP20210036 T1 HR P20210036T1
- Authority
- HR
- Croatia
- Prior art keywords
- disease
- lymphoma
- cancer
- cell lymphoma
- salt according
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title claims 14
- 238000000034 method Methods 0.000 title claims 7
- 239000012828 PI3K inhibitor Substances 0.000 title 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title 1
- 201000010099 disease Diseases 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical class Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 11
- 208000003950 B-cell lymphoma Diseases 0.000 claims 8
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 7
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 6
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 6
- 206010047115 Vasculitis Diseases 0.000 claims 6
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 4
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 3
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 3
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 3
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 3
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 2
- 201000004331 Henoch-Schoenlein purpura Diseases 0.000 claims 2
- 206010019617 Henoch-Schonlein purpura Diseases 0.000 claims 2
- 241000711549 Hepacivirus C Species 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 208000031814 IgA Vasculitis Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 208000007048 Polymyalgia Rheumatica Diseases 0.000 claims 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 2
- 206010043540 Thromboangiitis obliterans Diseases 0.000 claims 2
- 206010069351 acute lung injury Diseases 0.000 claims 2
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 2
- 230000002489 hematologic effect Effects 0.000 claims 2
- 208000015446 immunoglobulin a vasculitis Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000032671 Allergic granulomatous angiitis Diseases 0.000 claims 1
- 206010002412 Angiocentric lymphomas Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000027496 Behcet disease Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000033386 Buerger disease Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 208000006344 Churg-Strauss Syndrome Diseases 0.000 claims 1
- 208000010007 Cogan syndrome Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000019707 Cryoglobulinemic vasculitis Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000018428 Eosinophilic granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010018372 Glomerulonephritis membranous Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000011200 Kawasaki disease Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 241000721454 Pemphigus Species 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010065857 Primary Effusion Lymphoma Diseases 0.000 claims 1
- 206010036711 Primary mediastinal large B-cell lymphomas Diseases 0.000 claims 1
- 208000033766 Prolymphocytic Leukemia Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000004732 Systemic Vasculitis Diseases 0.000 claims 1
- 208000001106 Takayasu Arteritis Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 210000003719 b-lymphocyte Anatomy 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 201000003278 cryoglobulinemia Diseases 0.000 claims 1
- 230000001086 cytosolic effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 201000006569 extramedullary plasmacytoma Diseases 0.000 claims 1
- 230000003325 follicular Effects 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 210000001102 germinal center b cell Anatomy 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000003445 large cell neuroendocrine carcinoma Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 210000003563 lymphoid tissue Anatomy 0.000 claims 1
- 208000006116 lymphomatoid granulomatosis Diseases 0.000 claims 1
- 201000007919 lymphoplasmacytic lymphoma Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000007924 marginal zone B-cell lymphoma Diseases 0.000 claims 1
- 208000021937 marginal zone lymphoma Diseases 0.000 claims 1
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims 1
- 231100000855 membranous nephropathy Toxicity 0.000 claims 1
- 201000005328 monoclonal gammopathy of uncertain significance Diseases 0.000 claims 1
- 208000001725 mucocutaneous lymph node syndrome Diseases 0.000 claims 1
- 210000004877 mucosa Anatomy 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 210000004180 plasmocyte Anatomy 0.000 claims 1
- 201000006292 polyarteritis nodosa Diseases 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000010721 smoldering plasma cell myeloma Diseases 0.000 claims 1
- 206010062113 splenic marginal zone lymphoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 206010043207 temporal arteritis Diseases 0.000 claims 1
- 238000001757 thermogravimetry curve Methods 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic 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
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—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
- A61P1/18—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
- A61P11/06—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
- A61P13/08—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
- A61P13/12—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
- 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
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- A61P21/04—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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- 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
- A61P37/06—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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- 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
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Neurology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyrrole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (14)
1. Sol koja je sol klorovodične kiseline (R)-4-(3-((S)-1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil)-5-kloro-2-etoksi-6-fluorofenil)pirolidin-2-ona, koja je kristalna.
2. Sol prema zahtjevu 1 koja je u stehiometrijskom odnosu 1:1 (R)-4-(3-((S)-1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil)-5-kloro-2-etoksi-6-fluorofenil)pirolidin-2-ona prema klorovodičnoj kiselini.
3. Sol prema zahtjevu 1 ili 2, naznačena sa DSC termogramom koji ima endotermni signal na 207 ± 3 °C.
4. Sol prema bilo kojem od patentnih zahtjeva 1-3 koja ima DSC termogram kao što je dolje prikazano:
[image]
5. Sol prema bilo kojem od patentnih zahtjeva 1-4 koja ima TGA termogram kao što je dolje prikazano:
[image]
6. Sol prema bilo kojem od zahtjeva 1-5 koja ima:
(a) najmanje jedan XRPD signal, u smislu 2-teta, odabran od 11.3° ± 0.2°, 16.4° ± 0.2°, 21.0° ± 0.2°, 23.0° ± 0.2°, 28.1° ± 0.2°, 31.2° 6 0.2°, i 32.8° 6 0.2°;
(b) najmanje dva XRPD signala, u smislu 2-teta, odabrana od 11.3° ± 0.2°, 16.4° ± 0.2°, 21.0° ± 0.2°, 23.0° ± 0.2°, 28.1° ± 0.2°, 31.2° ± 0.2°, i 32.8° ± 0.2°;
(c) najmanje tri XRPD signala, u smislu 2-teta, odabrana od 11.3° ± 0.2°, 16.4° ± 0.2°, 21.0° ± 0.2°, 23.0° ± 0.2°, 28.1° ± 0.2°, 31.2° ± 0.2°, i 32.8° ± 0.2°;
(d) najmanje četiri XRPD signala, u smislu 2-teta, odabrana od 11.3° ± 0.2°, 16.4° ± 0.2°, 21.0° ± 0.2°, 23.0° ± 0.2°, 28.1° ± 0.2°, 31.2° ± 0.2°, i 32.8° ± 0.2°;
(e) najmanje pet XRPD signala, u smislu 2-teta, odabrana od 11.3° ± 0.2°, 16.4° ± 0.2°, 21.0° ± 0.2°, 23.0° ± 0.2°, 28.1° ± 0.2°, 31.2° ± 0.2°, i 32.8° ± 0.2°.
7. Sol prema bilo kojem od zahtjeva 1-5 koja ima profil XRPD kao što je dolje prikazano:
[image]
8. Farmaceutski sastav koji sadrži sol prema bilo kojem od zahtjeva 1-7 i farmaceutski prihvatljivi nosač.
9. Postupak za inhibiranje aktivnosti PI3Kδ kinaze, in vitro, koji obuhvaća dovođenje u kontakt kinaze sa soli prema bilo kojem od zahtjeva 1-7.
10. Sol prema bilo kojem od zahtjeva 1 do 7, za upotrebu u liječenju bolesti kod pacijenta, pri čemu je spomenuta bolest izabrana od idiopatske trombocitopenijske purpure (ITP), autoimune hemolitične anemije, vaskulitisa, sistemskog lupusa eritematozusa, lupusa nefritisa, pemfigusa, autoimune hemolitične anemije (AIHA), membranozne nefropatije, kronične limfocitne leukemije (CLL), Ne-hodgkinovog limfoma (NHL), leukemije dlakastih stanica, limfoma Mantle stanica, Burkitovog limfoma, malog limfocinog limfoma, folikularnog limfoma, limfoplazmacitnog limfoma, limfoma ekstranodalne marginalne zone, Hodgkinovog limfoma, Waldenstromove makrogloblinemije, prolimfocitne leukemije, akutne limfoblastne leukemije, mijelofibroze, limfoma limfatičnog tkiva povezanog sa mukozom (MALT), limfoma B-stanica, mediastinalnog (timičnog) limfoma velikih B-stanica, limfomatoidne granulomatoze, limfoma marginalne zone slezene, primarnog efuzionog limfoma, intravaskularnog limfoma velikih B-stanica, leukemije plazma stanica, ekstramedularnog plazmacitoma, pritajenog mijeloma (tj. asimptomatskog mijeloma), monoklonalne gamapatije neodređenog značaja (MGUS) I limfoma B stanica;
ili je bolest idiopatska trombocitopenijska purpura (ITP) izabrana od relapsnog ITP i refraktornog ITP;
ili je bolest vaskulitis izabran od Behçetove bolesti, Coganovog sindroma, temporalni arteritis, reumatske polimijalgije (PMR), Takayasujevog arteritisa, Buergerove bolesti (thromboangiitis obliterans), vaskulitisa centralnog nervnog sistema, Kawasakijeve bolesti, poliarteritis nodoza, Churg-straussovog sindroma, vaskulitisa mješovite krioglobulinemije (esencijalnog ili induciranog virusom hepatitisa C (HCV)), Henoch-Schonleinove purpure (HSP), vaskulitisa induciranog hiperpreosetljivošću, mikroskopskog angilitisa, Wegenerove granulomatoze, i sistemskog vaskulitisa (AASV) induciranog sa anti-neutrofilnim citoplazmatskim antitijelom (ANCA);
ili je bolest ne-Hodgkinov limfom (NHL) odabran od relapsnog NHL, refraktornog NHL, i rekurentnog folikularnog NHL;
ili je bolest limfom B stanica, pri čemu spomenuti limfom B stanice je difuzni krupnostanični limfom B-stanica (DLBCL);
ili je bolest limfom B stanica, pri čemu spomenuti limfom B stanica je aktiviranim B-stanicama sličan (ABC) difuzni krupnostanični B limfom, ili difuzni krupnostanični B limfom (GCB) B stanica germinalnog centra;
ili je bolest osteoartritis, restenoza, ateroskleroza, poremećaji kostiju, artritis, dijabetska retnopatija, psorijaza, benigna hipertrofija prostate, upala, angiogeneza, pankreatitis, bolest bubrega, upalna bolest crijeva, mijastenija gravis, multipla skleroza, ili Sjögrenov sindrom;
ili je bolest reumatoidni artritis, alergija, astma, glomerulonefritis, lupus, ili upala povezana sa bilo kojim od prethodno spomenutih;
ili je bolest lupus koji je sistemski lupus eritematozus ili lupus nefritis;
ili je bolest rak grudi, rak prostate, rak debelog crijeva, rak endometrijuma, rak mozga, rak mokraćnog mjehura, rak kože, rak maternice, rak jajnika, rak pluća, rak gušterače, rak bubrega, rak želudca, ili hematološki rak;
ili je bolest hematološki rak koji je akutna mijeloblastna leukemija ili kronična mijeloidna leukemija;
ili je bolest akutna povreda pluća (ALI) ili adultni respiratorni distres sindrom (ARDS).
11. Postupak za dobivanje soli prema bilo kojem od patentnih zahtjeva 1-7, koji obuhvaća reakciju spoja Formule I:
[image]
sa klorovodičnom kiselinom da bi se oblikovala spomenuta sol.
12. Postupak prema zahtjevu 11, pri čemu spomenuta klorovodična kiselina je 1 M klorovodična kiselina u vodi.
13. Postupak prema zahtjevu 11 ili 12, pri čemu se spomenuta reakcija izvodi na temperaturi od oko 45 °C do 55 °C.
14. Postupak prema bilo kojem od zahtjeva 11-13, što postupak dalje obuhvaća:
dodavanje klorovodične kiseline spoju Formule I na sobnoj temperaturi da bi se oblikovala suspenzija; zagrijavanje spomenute suspenzije do temperature od oko 45 °C do 55 °C da bi se oblikovao rastvor; i hlađenje rastvora do temperature od oko 0 °C do 5 °C da bi spomenuta sol kristalizala.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562121697P | 2015-02-27 | 2015-02-27 | |
PCT/US2016/019741 WO2016138363A1 (en) | 2015-02-27 | 2016-02-26 | Salts of pi3k inhibitor and processes for their preparation |
EP16718921.6A EP3262046B1 (en) | 2015-02-27 | 2016-02-26 | Salts of pi3k inhibitor and processes for their preparation |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20210036T1 true HRP20210036T1 (hr) | 2021-03-05 |
Family
ID=55854770
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20221444TT HRP20221444T1 (hr) | 2015-02-27 | 2016-02-26 | Postupci za pripravu pi3k inhibitora |
HRP20210036TT HRP20210036T1 (hr) | 2015-02-27 | 2021-01-08 | Soli inhibitora pi3k i postupci za njihovo dobivanje |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20221444TT HRP20221444T1 (hr) | 2015-02-27 | 2016-02-26 | Postupci za pripravu pi3k inhibitora |
Country Status (37)
Country | Link |
---|---|
US (2) | US10336759B2 (hr) |
EP (3) | EP3831833B1 (hr) |
JP (2) | JP6816005B2 (hr) |
KR (1) | KR20170132185A (hr) |
CN (4) | CN117777139A (hr) |
AR (1) | AR103804A1 (hr) |
AU (3) | AU2016222556B2 (hr) |
BR (1) | BR122021004509B1 (hr) |
CA (1) | CA2977659A1 (hr) |
CL (2) | CL2017002179A1 (hr) |
CO (1) | CO2017008924A2 (hr) |
CR (2) | CR20210055A (hr) |
CY (1) | CY1123729T1 (hr) |
DK (2) | DK3262046T3 (hr) |
EA (1) | EA201791923A1 (hr) |
EC (2) | ECSP17064131A (hr) |
ES (2) | ES2843522T3 (hr) |
HK (1) | HK1248229A1 (hr) |
HR (2) | HRP20221444T1 (hr) |
HU (2) | HUE053025T2 (hr) |
IL (1) | IL254093B (hr) |
LT (2) | LT3262046T (hr) |
MA (2) | MA41607B1 (hr) |
MD (2) | MD3262046T2 (hr) |
MX (2) | MX2017010918A (hr) |
MY (1) | MY187502A (hr) |
NZ (2) | NZ734993A (hr) |
PE (2) | PE20230156A1 (hr) |
PH (2) | PH12017501538A1 (hr) |
PL (2) | PL3262046T3 (hr) |
PT (2) | PT3831833T (hr) |
RS (2) | RS61233B1 (hr) |
SG (3) | SG10201907576SA (hr) |
SI (2) | SI3831833T1 (hr) |
TW (2) | TWI764392B (hr) |
UA (1) | UA122332C2 (hr) |
WO (1) | WO2016138363A1 (hr) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101763656B1 (ko) | 2009-06-29 | 2017-08-01 | 인사이트 홀딩스 코포레이션 | Pi3k 저해물질로서의 피리미디논 |
JP5961187B2 (ja) | 2010-12-20 | 2016-08-02 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Pi3k阻害剤としてのn−(1−(置換フェニル)エチル)−9h−プリン−6−アミン |
WO2013033569A1 (en) | 2011-09-02 | 2013-03-07 | Incyte Corporation | Heterocyclylamines as pi3k inhibitors |
AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
TWI687220B (zh) * | 2013-03-01 | 2020-03-11 | 美商英塞特控股公司 | 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途 |
CN106413716B (zh) | 2014-04-08 | 2020-03-27 | 因赛特公司 | 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤 |
WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
NZ734993A (en) | 2015-02-27 | 2024-03-22 | Incyte Holdings Corp | Salts of pi3k inhibitor and processes for their preparation |
US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
EP3360878B9 (en) | 2015-12-11 | 2021-05-05 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Azetidine derivative, preparation method therefor, and use thereof |
HUE057970T2 (hu) | 2018-03-08 | 2022-06-28 | Incyte Corp | Aminopirazindiol-vegyületek mint PI3K-Y inhibitorok |
MA52761A (fr) * | 2018-06-01 | 2021-04-14 | Incyte Corp | Schéma posologique destiné au traitement de troubles liés à la pi3k |
WO2022115120A1 (en) | 2020-11-30 | 2022-06-02 | Incyte Corporation | Combination therapy with an anti-cd19 antibody and parsaclisib |
JP2023551519A (ja) | 2020-11-30 | 2023-12-08 | インサイト・コーポレイション | 抗cd19抗体とパルサクリシブの組み合わせ療法 |
US20230190755A1 (en) | 2021-12-16 | 2023-06-22 | Incyte Corporation | Topical formulations of PI3K-delta inhibitors |
CN114409654A (zh) * | 2021-12-30 | 2022-04-29 | 安徽普利药业有限公司 | 一种btk抑制剂的中间体合成方法 |
Family Cites Families (281)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3169967A (en) | 1957-11-14 | 1965-02-16 | Ciba Geigy Corp | Methyl o-lower alkanoyl-reserpates |
US3037980A (en) | 1955-08-18 | 1962-06-05 | Burroughs Wellcome Co | Pyrrolopyrimidine vasodilators and method of making them |
US3506643A (en) | 1966-12-09 | 1970-04-14 | Max Thiel | N**6-aralkyl-adenosine derivatives |
DE2139107A1 (de) | 1971-08-04 | 1973-02-15 | Merck Patent Gmbh | Heterocyclisch substituierte adenosinverbindungen |
US3962443A (en) | 1972-08-14 | 1976-06-08 | Dainippon Pharmaceutical Co., Ltd. | Antibacterial pharmaceutical compositions and processes for preparation thereof |
DE2248232A1 (de) | 1972-10-02 | 1974-04-11 | Basf Ag | 4-thiopyrimido eckige klammer auf 4,5-d eckige klammer zu pyrimidine |
AR204003A1 (es) | 1973-04-03 | 1975-11-12 | Dainippon Pharmaceutical Co | Procedimiento para preparar compuestos derivados del acido 2-(1-piperazinil)-5-oxopirido-(2,3-d)pirimidino-6-carboxilico y sus sales farmaceuticamente aceptables |
US3936454A (en) | 1973-08-14 | 1976-02-03 | Warner-Lambert Company | 5-Amino-4-chloro-6-(substituted amino)-pyrimidines |
US3862189A (en) | 1973-08-14 | 1975-01-21 | Warner Lambert Co | Aralkyl-substituted purines and pyrimidines as antianginal bronchodilator agents |
DK3375A (hr) | 1974-01-25 | 1975-09-15 | Ciba Geigy Ag | |
JPS587626B2 (ja) | 1974-02-13 | 1983-02-10 | 大日本製薬株式会社 | ナフチリジン オヨビ キノリンユウドウタイノセイホウ |
JPS5359663A (en) | 1976-11-09 | 1978-05-29 | Sumitomo Chem Co Ltd | 2-halogeno methyl indole derivatives and process for praparation of the same |
JPS52106897A (en) | 1977-01-10 | 1977-09-07 | Dainippon Pharmaceut Co Ltd | Synthesis of piperazine derivatives |
JPS5392767A (en) | 1977-01-27 | 1978-08-15 | Sumitomo Chem Co Ltd | Preparation of 2-phthalimidomethylindole derivatives |
JPS5625234A (en) | 1979-08-02 | 1981-03-11 | Hitachi Denshi Ltd | Dropout display system |
JPS56123981A (en) | 1981-02-23 | 1981-09-29 | Dainippon Pharmaceut Co Ltd | Preparation of 1,4-disubstituted piperazine |
JPS5883698A (ja) | 1981-11-13 | 1983-05-19 | Takeda Chem Ind Ltd | キノン化合物およびその製造法 |
JPS58162949A (ja) | 1982-03-20 | 1983-09-27 | Konishiroku Photo Ind Co Ltd | ハロゲン化銀カラ−写真感光材料 |
JPS60140373U (ja) | 1984-02-28 | 1985-09-17 | 東洋ハ−ネス株式会社 | ワイヤハ−ネスのア−ス構造 |
JPS6190153A (ja) | 1984-10-09 | 1986-05-08 | Fuji Photo Film Co Ltd | ハロゲン化銀写真感光材料の処理方法 |
JPS62103640A (ja) | 1985-07-18 | 1987-05-14 | Fuji Photo Film Co Ltd | ハロゲン化銀カラ−写真感光材料 |
JPH07119970B2 (ja) | 1986-04-18 | 1995-12-20 | 富士写真フイルム株式会社 | 画像形成方法 |
JPS6310746A (ja) | 1986-07-01 | 1988-01-18 | Tanabe Seiyaku Co Ltd | ナフタレン誘導体 |
CA1324609C (en) | 1986-07-30 | 1993-11-23 | Eastman Kodak Company | Photographic element and process |
US4861701A (en) | 1987-10-05 | 1989-08-29 | Eastman Kodak Company | Photographic element and process comprising a compound which comprises two timing groups in sequence |
AT388372B (de) | 1987-10-08 | 1989-06-12 | Tanabe Seiyaku Co | Neue naphthalinderivate und sie enthaltende pharmazeutika |
JPH01250316A (ja) | 1987-12-28 | 1989-10-05 | Tanabe Seiyaku Co Ltd | 抗脂血剤 |
EP0364598A4 (en) | 1988-03-02 | 1992-01-15 | Yoshitomi Pharmaceutical Industries, Ltd. | 3,4-dihydrothieno 2,3-d¨pyrimidine compounds and pharmaceutical application thereof |
US5208250A (en) | 1988-05-25 | 1993-05-04 | Warner-Lambert Company | Known and selected novel arylmethylenyl derivatives of thiazolidinones, imidazolidinones and oxazolidinones useful as antiallergy agents and anti-inflammatory agents |
UA27031A1 (uk) | 1990-04-25 | 2000-02-28 | Ніссан Кемікал Індастріз Лтд | Похідhі 3(2h)піридазиhоhу або їх фармацевтичhо прийhятhі солі, що мають протитромботичhу, позитивhу іhотропhу, судиhорозширювальhу дію й аhтиалергічhу активhість та фармацевтичhа композиція hа їх осhові |
SU1712359A1 (ru) | 1990-05-07 | 1992-02-15 | Уфимский Нефтяной Институт | Гидрохлорид 8 @ -гидроксихинолинового эфира 8-гидроксихинолин-7-карбоновой кислоты, в качестве бактерицида дл подавлени сульфатвосстанавливающих бактерий и культур РSеUDомоNаS и АRтнRовастеR |
EP0464612B1 (en) | 1990-06-28 | 1998-05-13 | Fuji Photo Film Co., Ltd. | Silver halide photographic materials |
EP0481614A1 (en) | 1990-10-01 | 1992-04-22 | Merck & Co. Inc. | Substituted pyridopyrimidinones and related heterocycles as angiotensin II antagonists |
JPH04190232A (ja) | 1990-11-26 | 1992-07-08 | Fuji Photo Film Co Ltd | ハロゲン化銀カラー写真感光材料 |
US5480883A (en) | 1991-05-10 | 1996-01-02 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
IL101860A0 (en) | 1991-05-31 | 1992-12-30 | Ici Plc | Heterocyclic derivatives |
JP3108483B2 (ja) | 1991-09-30 | 2000-11-13 | 日清製粉株式会社 | インドール誘導体およびこれを有効成分とする抗潰瘍薬 |
HUT64064A (en) | 1992-02-13 | 1993-11-29 | Chinoin Gyogyszer Es Vegyeszet | Process for producing puyrido/1,2-a/pyrimidine derivatives and pharmaceutical compositions comprising same as active ingredient |
US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
WO1993022291A1 (en) | 1992-04-24 | 1993-11-11 | E.I. Du Pont De Nemours And Company | Arthropodicidal and fungicidal aminopyrimidines |
TW229140B (hr) | 1992-06-05 | 1994-09-01 | Shell Internat Res Schappej B V | |
FR2714907B1 (fr) | 1994-01-07 | 1996-03-29 | Union Pharma Scient Appl | Nouveaux dérivés de l'Adénosine, leurs procédés de préparation, compositions pharmaceutiques les contenant. |
US6342501B1 (en) | 1994-02-25 | 2002-01-29 | The Regents Of The University Of Michigan | Pyrrolo[2,3-d] pyrimidines as antiviral agents |
JPH0987282A (ja) | 1995-09-21 | 1997-03-31 | Kyowa Hakko Kogyo Co Ltd | チアゾール誘導体 |
JPH09176162A (ja) | 1995-12-22 | 1997-07-08 | Toubishi Yakuhin Kogyo Kk | チアゾリジンジオン誘導体及びその製造法並びにそれを含む医薬組成物 |
JPH09176116A (ja) | 1995-12-27 | 1997-07-08 | Toray Ind Inc | 複素環誘導体およびその医薬用途 |
JPH1025294A (ja) | 1996-03-26 | 1998-01-27 | Akira Matsuda | 縮合ヘテロ環誘導体、その製造法及びそれを含有する悪性腫瘍治療剤 |
WO1997048697A1 (en) | 1996-06-19 | 1997-12-24 | Rhone-Poulenc Rorer Limited | Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase |
NZ329798A (en) | 1996-07-03 | 1999-04-29 | Japan Energy Corp | Purine derivatives their tautomers and salts thereof and interferon secretion inducers, antiviral agents and anticancer drugs containing the same |
US5866702A (en) | 1996-08-02 | 1999-02-02 | Cv Therapeutics, Incorporation | Purine inhibitors of cyclin dependent kinase 2 |
US6630496B1 (en) | 1996-08-26 | 2003-10-07 | Genetics Institute Llc | Inhibitors of phospholipase enzymes |
JPH10231297A (ja) | 1997-02-20 | 1998-09-02 | Japan Energy Corp | 新規なアデニン−1−n−オキシド誘導体およびその医薬用途 |
EP1043324B1 (en) | 1997-11-12 | 2004-06-16 | Mitsubishi Chemical Corporation | Purine derivatives and medicine containing the same as the active ingredient |
TW572758B (en) | 1997-12-22 | 2004-01-21 | Sumitomo Pharma | Type 2 helper T cell-selective immune response inhibitors comprising purine derivatives |
CA2322161A1 (en) | 1998-02-25 | 1999-09-02 | Yibin Xiang | Inhibitors of phospholipase enzymes |
US6828344B1 (en) | 1998-02-25 | 2004-12-07 | Genetics Institute, Llc | Inhibitors of phospholipase enzymes |
ID26123A (id) | 1998-02-25 | 2000-11-23 | Genetics Inst | Penghambat-penghambat phospholipase a2 |
US6479487B1 (en) | 1998-02-26 | 2002-11-12 | Aventis Pharmaceuticals Inc. | 6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines |
BR9911017A (pt) | 1998-05-04 | 2001-02-06 | Asta Medica Ag | Derivados de indol e seu emprego para o tratamento de doenças malignas e outras, que se baseiam na proliferação de células patológicas |
WO1999061436A1 (fr) | 1998-05-26 | 1999-12-02 | Chugai Seiyaku Kabushiki Kaisha | Derives d'indole heterocycliques et derives de mono ou de di-azaindole |
JP3997651B2 (ja) | 1998-06-24 | 2007-10-24 | コニカミノルタホールディングス株式会社 | 新規色素及び画像記録材料及び感熱転写材料及びインクジェット記録液 |
ATE459616T1 (de) | 1998-08-11 | 2010-03-15 | Novartis Ag | Isochinoline derivate mit angiogenesis-hemmender wirkung |
DE69913712T2 (de) | 1998-08-25 | 2004-10-07 | Uab Res Foundation Birmingham | Inhibitoren der bakteriellen nad synthetase |
US6133031A (en) | 1999-08-19 | 2000-10-17 | Isis Pharmaceuticals Inc. | Antisense inhibition of focal adhesion kinase expression |
IL144675A0 (en) | 1999-02-01 | 2002-05-23 | Cv Therapeutics Inc | PURINE INHIBITORS OF CYCLIN DEPENDENT KINASE 2 AND IkB-α |
GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
JP2000281654A (ja) | 1999-03-26 | 2000-10-10 | Tanabe Seiyaku Co Ltd | イソキノリン誘導体 |
DE19932571A1 (de) | 1999-07-13 | 2001-01-18 | Clariant Gmbh | Verfahren zur Herstellung von Biarylen unter Palladophosphacyclobutan-Katalyse |
JP2001151771A (ja) | 1999-09-10 | 2001-06-05 | Kyowa Hakko Kogyo Co Ltd | 含窒素芳香族複素環誘導体 |
GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
US6436965B1 (en) | 2000-03-02 | 2002-08-20 | Merck Frosst Canada & Co. | PDE IV inhibiting amides, compositions and methods of treatment |
EP1138328A1 (en) | 2000-03-29 | 2001-10-04 | Eli Lilly And Company Limited | Naphthalene derivatives as CNS drugs |
US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
IL153231A0 (en) | 2000-06-28 | 2003-07-06 | Smithkline Beecham Plc | Wet milling process |
CN1331340A (zh) | 2000-06-30 | 2002-01-16 | 上海博德基因开发有限公司 | 一种新的多肽——人拓扑异构酶12.1和编码这种多肽的多核苷酸 |
AU2001271022B2 (en) | 2000-07-05 | 2006-08-17 | Astellas Pharma Inc. | Propane-1,3-dione derivatives |
FR2814073B1 (fr) | 2000-09-21 | 2005-06-24 | Yang Ji Chemical Company Ltd | Composition pharmaceutique antifongique et/ou antiparasitaire et nouveaux derives de l'indole a titre de principes actifs d'une telle composition |
DOP2002000334A (es) | 2001-02-14 | 2002-08-30 | Warner Lambert Co | Pirimidinas biciclicas como inhibidores de metaloproteinasas de matriz |
SE0100568D0 (sv) | 2001-02-20 | 2001-02-20 | Astrazeneca Ab | Compounds |
CN1659143A (zh) | 2001-03-01 | 2005-08-24 | 盐野义制药株式会社 | 具有hiv整合酶抑制活性的含氮杂芳基化合物 |
UA76977C2 (en) | 2001-03-02 | 2006-10-16 | Icos Corp | Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers |
WO2002078700A1 (en) | 2001-03-30 | 2002-10-10 | Smithkline Beecham Corporation | Pyralopyridines, process for their preparation and use as therapteutic compounds |
US20050107400A1 (en) | 2001-03-30 | 2005-05-19 | Boyd Leslie F. | Use of pyrazolopyridines as therapeutic compounds |
ES2242028T3 (es) | 2001-04-27 | 2005-11-01 | Smithkline Beecham Corporation | Derivados de pirazolo(1,5-a)piridina. |
CZ294535B6 (cs) | 2001-08-02 | 2005-01-12 | Ústav Experimentální Botaniky Avčr | Heterocyklické sloučeniny na bázi N6-substituovaného adeninu, způsoby jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující |
GB0121033D0 (en) | 2001-08-30 | 2001-10-24 | Novartis Ag | Organic compounds |
US8124625B2 (en) | 2001-09-14 | 2012-02-28 | Shionogi & Co., Ltd. | Method of enhancing the expression of apolipoprotein AI using olefin derivatives |
IL160915A0 (en) | 2001-09-19 | 2004-08-31 | Aventis Pharma Sa | Indolizines inhibiting kinase proteins |
RU2004112771A (ru) | 2001-09-26 | 2005-10-10 | Байер Фармасьютикалс Корпорейшн (US) | Производные 1, 8-нафтиридина как противодиабетические средства |
WO2003029209A2 (en) | 2001-10-02 | 2003-04-10 | Smithkline Beecham Corporation | Chemical compounds |
RU2337692C3 (ru) | 2001-10-30 | 2020-11-09 | Новартис Аг | Производные стауроспорина в качестве ингибиторов активности рецепторной тирозинкиназы flt3 |
JP4663233B2 (ja) | 2001-11-09 | 2011-04-06 | エンゾン,インコーポレーテッド | ベンジル脱離系を利用する高分子チオール結合プロドラッグ |
EP1314733A1 (en) | 2001-11-22 | 2003-05-28 | Aventis Pharma Deutschland GmbH | Indole-2-carboxamides as factor Xa inhibitors |
ATE424388T1 (de) | 2001-12-06 | 2009-03-15 | Merck & Co Inc | Mitotische kinesinhemmer |
DE60222302T2 (de) | 2001-12-06 | 2008-05-29 | Merck & Co., Inc. | Inhibitoren von mitotischem kinesin |
TW200301135A (en) | 2001-12-27 | 2003-07-01 | Otsuka Maryland Res Inst Inc | Pharmaceutical compositions comprising a multifunctional phosphodiesterase inhibitor and an adenosine uptake inhibitor |
AU2003211931A1 (en) | 2002-02-13 | 2003-09-04 | Takeda Chemical Industries, Ltd. | Jnk inhibitor |
AU2003225668A1 (en) | 2002-03-01 | 2003-09-16 | Pintex Pharmaceutical, Inc. | Pin1-modulating compounds and methods of use thereof |
AU2003222106A1 (en) | 2002-04-03 | 2003-10-20 | Bristol-Myers Squibb Company | Thiopene-based tricyclic compounds and pharmaceutical compositions comprising same |
EP1501850A2 (en) | 2002-05-06 | 2005-02-02 | Genelabs Technologies, Inc. | Nucleoside derivatives for treating hepatitis c virus infection |
TW200406374A (en) | 2002-05-29 | 2004-05-01 | Novartis Ag | Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases |
GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
EP2045242A1 (en) | 2002-08-13 | 2009-04-08 | Shionogi&Co., Ltd. | Heterocyclic compounds having inhibitory activity against HIV integrase |
JP4190232B2 (ja) | 2002-08-26 | 2008-12-03 | 富士通株式会社 | 機械研磨を行う方法 |
BR0314761A (pt) | 2002-09-27 | 2005-07-26 | Sumitomo Pharma | Composto de adenina e seu uso |
AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
KR101052482B1 (ko) | 2002-11-21 | 2011-07-28 | 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 | 포스포티딜이노시톨(pi) 3-키나제 억제제인 2,4,6-삼치환피리미딘 및 암의 치료에서 이들의 사용 |
US7494987B2 (en) | 2002-11-25 | 2009-02-24 | Mochida Pharmaceutical Co., Ltd. | Agent for treating respiratory diseases containing 4-hydroxypiperidine derivative as active ingredient |
UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
CA2512000C (en) | 2002-12-26 | 2011-08-09 | Eisai Co., Ltd. | Selective estrogen receptor modulator |
CZ294538B6 (cs) | 2002-12-30 | 2005-01-12 | Ústav Experimentální Botaniky Akademie Vědčeské Re | Substituční deriváty N6-benzyladenosinu, způsob jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující |
RU2233842C1 (ru) | 2003-01-13 | 2004-08-10 | Петров Владимир Иванович | Производные пурина, обладающие противовирусной активностью |
AR043692A1 (es) | 2003-02-06 | 2005-08-10 | Novartis Ag | 2-cianopirrolopirimidinas y sus usos farmaceuticos |
GB0304640D0 (en) | 2003-02-28 | 2003-04-02 | Novartis Ag | Organic compounds |
GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
SE0300908D0 (sv) | 2003-03-31 | 2003-03-31 | Astrazeneca Ab | Azaindole derivatives, preparations thereof, uses thereof and compositions containing them |
US7129264B2 (en) | 2003-04-16 | 2006-10-31 | Bristol-Myers Squibb Company | Biarylmethyl indolines and indoles as antithromboembolic agents |
EP1619948A4 (en) | 2003-05-05 | 2007-02-14 | Neurogen Corp | SUBSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS |
PT1636225E (pt) | 2003-06-20 | 2010-05-03 | Novartis Vaccines & Diagnostic | Compostos piridino[1,2-a]pirimidin-4-ona como agentes anti-cancerígenos |
WO2005000309A2 (en) | 2003-06-27 | 2005-01-06 | Ionix Pharmaceuticals Limited | Chemical compounds |
JP4570015B2 (ja) | 2003-07-14 | 2010-10-27 | クミアイ化学工業株式会社 | 2−イソオキサゾリン誘導体及びそれを有効成分として含有する除草剤 |
SG145748A1 (en) | 2003-08-15 | 2008-09-29 | Irm Llc | 6-substituted anilino purines as rtk inhibitors |
BRPI0414533A (pt) | 2003-09-18 | 2006-11-07 | Conforma Therapeutics Corp | composto, composição farmacêutica, e, métodos para inibir um hsp90 e para tratar um indivìduo tendo um distúrbio mediado por hsp90 |
WO2005046578A2 (en) | 2003-09-23 | 2005-05-26 | Merck & Co., Inc. | Isoquinolinone potassium channel inhibitors |
AR045944A1 (es) | 2003-09-24 | 2005-11-16 | Novartis Ag | Derivados de isoquinolina 1.4-disustituidas |
JP2007520559A (ja) | 2004-02-03 | 2007-07-26 | アボット・ラボラトリーズ | 治療薬としてのアミノベンゾオキサゾール類 |
WO2005077948A1 (ja) | 2004-02-16 | 2005-08-25 | Daiichi Pharmaceutical Co., Ltd. | 抗真菌作用複素環化合物 |
CN1560035A (zh) | 2004-03-12 | 2005-01-05 | 沈阳药科大学 | 5-羟基吲哚-3-羧酸脂类衍生物 |
WO2005091857A2 (en) | 2004-03-12 | 2005-10-06 | Bayer Pharmaceuticals Corporation | 1,6-naphthyridine and 1,8-naphthyridine derivatives and their use to treat diabetes and related disorders |
WO2005092892A1 (ja) | 2004-03-26 | 2005-10-06 | Dainippon Sumitomo Pharma Co., Ltd. | 8−オキソアデニン化合物 |
US7217702B2 (en) | 2004-04-02 | 2007-05-15 | Adenosine Therapeutics, Llc | Selective antagonists of A2A adenosine receptors |
ES2605792T3 (es) | 2004-05-13 | 2017-03-16 | Icos Corporation | Quinazolinona usada como inhibidor de la fosfatidilinositol 3-quinasa delta humana |
US20060074102A1 (en) | 2004-05-14 | 2006-04-06 | Kevin Cusack | Kinase inhibitors as therapeutic agents |
US20070287703A1 (en) | 2004-07-22 | 2007-12-13 | Astrazeneca Ab | Fused Pyrimidones Useful in the Treatment and the Prevention of Cancer |
DE102004044221A1 (de) | 2004-09-14 | 2006-03-16 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue 3-Methyl-7-butinyl-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
GB0420719D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
US7608723B2 (en) | 2004-10-19 | 2009-10-27 | Novartis Vaccines And Diagnostics, Inc. | Indole and benzimidazole derivatives |
US20080004269A1 (en) | 2004-11-04 | 2008-01-03 | Yuelian Xu | Pyrazolylmethy Heteroaryl Derivatives |
EP1831225A2 (en) | 2004-11-19 | 2007-09-12 | The Regents of the University of California | Anti-inflammatory pyrazolopyrimidines |
EP1885352A2 (en) | 2004-11-24 | 2008-02-13 | Novartis AG | Combinations comprising jak inhibitors and at least one of bcr-abl, flt-3, fak or raf kinase inhibitors |
CA2598409A1 (en) | 2005-02-17 | 2006-08-24 | Icos Corporation | Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation |
CA2612585A1 (en) | 2005-06-27 | 2007-01-04 | Amgen Inc. | Anti-inflammatory aryl nitrile compounds |
FR2889192A1 (fr) | 2005-07-27 | 2007-02-02 | Cytomics Systems Sa | Composes antifongiques, compositions contenant ces composes et leurs utilisations |
US20070066624A1 (en) | 2005-08-16 | 2007-03-22 | Anormed, Inc. | Chemokine receptor binding compounds |
US7642270B2 (en) | 2005-09-14 | 2010-01-05 | Janssen Pharmaceutica N.V. | 5-oxo-5,8-dihydro-pyrido-pyrimidine as inhibitors of c-fms kinase |
US20090118263A1 (en) | 2005-09-22 | 2009-05-07 | Dainippon Sumitomo Pharma Co., Ltd. | Novel Adenine Compound |
GB0520657D0 (en) | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
PT1951684T (pt) | 2005-11-01 | 2016-10-13 | Targegen Inc | Inibidores de cinases de tipo biaril-meta-pirimidina |
EP1783114A1 (en) | 2005-11-03 | 2007-05-09 | Novartis AG | N-(hetero)aryl indole derivatives as pesticides |
DK1954274T3 (da) | 2005-11-10 | 2011-01-31 | Chemocentryx Inc | Substituerede quinoloner og fremgangsmåder til anvendelse |
PT3184526T (pt) | 2005-12-13 | 2018-12-19 | Incyte Holdings Corp | Derivados de pirrolo[2,3-d]pirimidina como inibidores da cinase janus |
US7989461B2 (en) | 2005-12-23 | 2011-08-02 | Amgen Inc. | Substituted quinazolinamine compounds for the treatment of cancer |
US20100227880A1 (en) | 2006-01-25 | 2010-09-09 | Kristjan Gudmundsson | Chemical compounds |
UY30118A1 (es) | 2006-01-31 | 2007-06-29 | Tanabe Seiyaku Co | Compueto amina trisustituido |
PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
WO2007102392A1 (ja) | 2006-03-03 | 2007-09-13 | Shionogi & Co., Ltd. | Mmp-13選択的阻害剤 |
BRPI0709699A2 (pt) | 2006-03-29 | 2011-07-26 | Foldrx Pharmaceuticals Inc | inibiÇço da toxidez da alfa-sinucleina |
EA200870409A1 (ru) | 2006-04-04 | 2009-04-28 | Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния | Антагонисты киназы pi3 |
US8933130B2 (en) | 2006-06-23 | 2015-01-13 | Radius Health, Inc. | Treatment of vasomotor symptoms with selective estrogen receptor modulators |
US20080004253A1 (en) | 2006-06-30 | 2008-01-03 | Bryan James Branstetter | Thiazolopyrimidine modulators of TRPV1 |
US20080009508A1 (en) | 2006-07-10 | 2008-01-10 | Lucie Szucova | 6,9-Disubstituted Purine Derivatives And Their Use For Treating Skin |
AU2007272009A1 (en) | 2006-07-12 | 2008-01-17 | Syngenta Limited | Triazolopyridine derivatives as herbicides |
PT2050749T (pt) | 2006-08-08 | 2018-01-02 | Chugai Pharmaceutical Co Ltd | Derivado de pirimidina como inibidador de pi3k e sua utilização |
BRPI0716239A2 (pt) | 2006-08-30 | 2013-08-13 | Cellzome Ltd | derivados de triazol como inibidores de cinase |
WO2008032033A1 (en) | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
EP1972631A1 (en) | 2007-03-23 | 2008-09-24 | Novartis AG | Imidazopyridazines as PI3K lipid kinase inhibitors |
US20080114007A1 (en) | 2006-10-31 | 2008-05-15 | Player Mark R | 5-oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of c-fms kinase |
JP5313909B2 (ja) | 2006-11-13 | 2013-10-09 | アイコス コーポレイション | 炎症性疾患および癌の処置のためのチエノピリミジノン |
ME02372B (me) | 2006-11-22 | 2016-06-20 | Incyte Holdings Corp | Imidazotriazini i imidazopiramidini kao inhibitori kinaze |
US20100298314A1 (en) | 2006-12-20 | 2010-11-25 | Schering Corporation | Novel jnk inhibitors |
WO2008080844A1 (en) | 2006-12-29 | 2008-07-10 | F. Hoffmann-La Roche Ag | Azaspiro derivatives |
CA2677493A1 (en) | 2007-02-05 | 2008-08-14 | Xenon Pharmaceuticals Inc. | Pyridopyrimidinone compounds useful in treating sodium channel-mediated diseases or conditions |
WO2008100867A2 (en) | 2007-02-12 | 2008-08-21 | Intermune, Inc. | Novel inhibitors hepatitis c virus replication |
AR065784A1 (es) | 2007-03-20 | 2009-07-01 | Dainippon Sumitomo Pharma Co | Derivados de 8-oxo adenina,medicamentos que los contienen y usos como agentes terapeuticos para enfermedades alergicas, antivirales o antibacterianas. |
US20080233127A1 (en) | 2007-03-21 | 2008-09-25 | Wyeth | Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors |
JP2010522177A (ja) | 2007-03-23 | 2010-07-01 | アムジエン・インコーポレーテツド | 複素環化合物およびその使用 |
MX2009009968A (es) | 2007-03-23 | 2009-10-08 | Amgen Inc | Compuestos heterociclicos y sus usos. |
US8039505B2 (en) | 2007-04-11 | 2011-10-18 | University Of Utah Research Foundation | Compounds for modulating T-cells |
US8633186B2 (en) | 2007-06-08 | 2014-01-21 | Senomyx Inc. | Modulation of chemosensory receptors and ligands associated therewith |
US9603848B2 (en) | 2007-06-08 | 2017-03-28 | Senomyx, Inc. | Modulation of chemosensory receptors and ligands associated therewith |
WO2008156783A2 (en) | 2007-06-18 | 2008-12-24 | University Of Louisville Research Foundation, Inc. | Family of pfkfb3 inhibitors with anti-neoplastic activities |
EA024359B1 (ru) | 2007-06-29 | 2016-09-30 | Джилид Сайэнс, Инк. | Пуриновые производные и их применение в качестве модуляторов толл-подобного рецептора 7 |
WO2009042294A2 (en) | 2007-08-10 | 2009-04-02 | Burnham Institute For Medical Research | Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof |
JP2009076865A (ja) | 2007-08-29 | 2009-04-09 | Fujifilm Corp | 有機電界発光素子 |
WO2009026701A1 (en) | 2007-08-29 | 2009-03-05 | Methylgene Inc. | Sirtuin inhibitors |
WO2009034386A1 (en) | 2007-09-13 | 2009-03-19 | Astrazeneca Ab | Derivatives of adenine and 8-aza-adenine and uses thereof-796 |
JP2009080233A (ja) | 2007-09-26 | 2009-04-16 | Kyocera Mita Corp | 電子写真感光体 |
CZ300774B6 (cs) | 2007-10-05 | 2009-08-05 | Univerzita Palackého | Substituované 6-(alkylbenzylamino)purinové deriváty pro použití jako antagonisté cytokininových receptoru a prípravky obsahující tyto slouceniny |
AU2008323694A1 (en) | 2007-11-07 | 2009-05-14 | Foldrx Pharmaceuticals, Inc. | Modulation of protein trafficking |
WO2009063235A1 (en) | 2007-11-13 | 2009-05-22 | Astrazeneca Ab | Derivatives of 1,9-dihydro-6h-purin-6-one and uses thereof-018 |
JP2009120686A (ja) | 2007-11-14 | 2009-06-04 | Toyo Ink Mfg Co Ltd | 光重合開始剤、重合性組成物、および重合物の製造方法。 |
PE20091268A1 (es) | 2007-12-19 | 2009-09-19 | Amgen Inc | Derivados heterociclicos como inhibidores de pi3 quinasa |
ES2587738T3 (es) | 2007-12-21 | 2016-10-26 | Ucb Biopharma Sprl | Derivados de quinoxalina y quinolina como inhibidores de quinasa |
CA2710452A1 (en) | 2007-12-21 | 2009-07-09 | Wyeth Llc | Imidazo [1,2-a] pyridine compounds |
JP2011507910A (ja) | 2007-12-21 | 2011-03-10 | ユニバーシティー オブ ロチェスター | 真核生物の寿命を変更するための方法 |
US7960397B2 (en) | 2007-12-28 | 2011-06-14 | Institute Of Experimental Botany, Academy Of Sciences Of The Czech Republic | 6,9-disubstituted purine derivatives and their use as cosmetics and cosmetic compositions |
BRPI0722222A2 (pt) | 2007-12-28 | 2015-06-16 | Topharman Shangai Co Ltd | N-{1-[3-(2-etóxi-5-(4-etilpiperazinil)sulfonilfenil)-4,5-di hidro-5-oxo-1,2,4-triazina-6-il]etil}butiramida, seu método de preparo e seu uso |
US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
WO2009098715A2 (en) | 2008-01-11 | 2009-08-13 | Natco Pharma Limited | Novel pyrazolo [3, 4 -d] pyrimidine derivatives as anti -cancer agents |
US9089572B2 (en) | 2008-01-17 | 2015-07-28 | California Institute Of Technology | Inhibitors of p97 |
CA2711759A1 (en) | 2008-01-30 | 2009-08-06 | Genentech, Inc. | Pyrazolopyrimidine pi3k inhibitor compounds and methods of use |
JPWO2009128520A1 (ja) | 2008-04-18 | 2011-08-04 | 塩野義製薬株式会社 | Pi3k阻害活性を有する複素環化合物 |
US8119647B2 (en) | 2008-04-23 | 2012-02-21 | Glenmark Pharmaceuticals S.A. | Fused pyrimidineone compounds as TRPV3 modulators |
WO2009140215A2 (en) | 2008-05-11 | 2009-11-19 | Geraghty, Erin | Method for treating drug-resistant bacterial and other infections with clioquinol, phanquinone, and related compounds |
US10301265B2 (en) | 2008-05-28 | 2019-05-28 | Virginia I. Roxas-Duncan | Small molecule inhibitors of botulinum neurotoxins |
CA2727174A1 (en) | 2008-06-20 | 2010-01-21 | Jiangao Song | Aryl gpr119 agonists and uses thereof |
US8026271B2 (en) | 2008-07-11 | 2011-09-27 | National Health Research Institutes | Formulations of indol-3-yl-2-oxoacetamide compounds |
WO2010018458A2 (en) | 2008-08-12 | 2010-02-18 | Crystalgenomics, Inc. | Phenol derivatives and methods of use thereof |
WO2010036380A1 (en) | 2008-09-26 | 2010-04-01 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
WO2010057048A1 (en) | 2008-11-13 | 2010-05-20 | Calistoga Pharmaceuticals Inc. | Therapies for hematologic malignancies |
EP2379547A1 (en) | 2008-12-16 | 2011-10-26 | Schering Corporation | Pyridopyrimidine derivatives and methods of use thereof |
WO2010074588A2 (en) | 2008-12-24 | 2010-07-01 | BIAL - PORTELA & Cª, S.A. | Pharmaceutical compounds |
US8563579B2 (en) | 2009-01-15 | 2013-10-22 | Anvyl Llc | α-7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof |
WO2010092340A1 (en) | 2009-02-13 | 2010-08-19 | Ucb Pharma S.A. | Fused pyridine and pyrazine derivatives as kinase inhibitors |
AU2010232642A1 (en) | 2009-03-31 | 2011-10-20 | Arqule, Inc. | Substituted indolo-piperidine compounds |
WO2010118367A2 (en) | 2009-04-10 | 2010-10-14 | Progenics Pharmaceuticals, Inc. | Antiviral pyrimidines |
KR20120005523A (ko) | 2009-04-20 | 2012-01-16 | 길리아드 칼리스토가 엘엘씨 | 고형 종양의 치료 방법 |
WO2010127208A1 (en) | 2009-04-30 | 2010-11-04 | Forest Laboratories Holdings Limited | Inhibitors of acetyl-coa carboxylase |
CA2760791C (en) | 2009-05-07 | 2017-06-20 | Intellikine, Inc. | Heterocyclic compounds and uses thereof |
ES2487542T3 (es) | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
JP2012531435A (ja) | 2009-06-25 | 2012-12-10 | アムジエン・インコーポレーテツド | PI3K阻害剤としての4H−ピリド[1,2−a]ピリミジン−4−オン誘導体 |
AR077267A1 (es) | 2009-06-25 | 2011-08-17 | Amgen Inc | Derivados nitrogenados heterociclicos inhibidores selectivos de pi3k, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades inflamatorias y/o autoinmunes. |
KR101763656B1 (ko) | 2009-06-29 | 2017-08-01 | 인사이트 홀딩스 코포레이션 | Pi3k 저해물질로서의 피리미디논 |
FR2947269B1 (fr) | 2009-06-29 | 2013-01-18 | Sanofi Aventis | Nouveaux composes anticancereux |
AR077252A1 (es) | 2009-06-29 | 2011-08-10 | Xenon Pharmaceuticals Inc | Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos |
KR101850813B1 (ko) | 2009-06-29 | 2018-04-20 | 아지오스 파마슈티컬스 아이엔씨. | 치료용 화합물 및 조성물 |
AU2010276160A1 (en) | 2009-07-21 | 2012-02-09 | Gilead Calistoga Llc | Treatment of liver disorders with PI3K inhibitors |
DK2470546T3 (da) | 2009-08-28 | 2013-10-14 | Takeda Pharmaceutical | HEXAHYDROOXAZINOPTERIDIN- forbindelser til anvendelse som mTOR INHIBITORER |
AR078012A1 (es) | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
CN102666545B (zh) | 2009-10-20 | 2016-04-06 | 塞尔卓姆有限公司 | 作为jak抑制剂的杂环吡唑并嘧啶类似物 |
EP2491035B1 (en) | 2009-10-22 | 2017-08-30 | Gilead Sciences, Inc. | Derivatives of purine or deazapurine useful for the treatment of (inter alia) viral infections |
KR102012398B1 (ko) | 2009-11-05 | 2019-08-20 | 리젠 파마슈티컬스 소시에떼 아노님 | 신규한 벤조피란 키나제 조절제 |
MX2012005429A (es) | 2009-11-10 | 2012-06-19 | Pfizer | Inhibidores de n1-pirazoloespirocetona acetil-coa carboxilasa. |
WO2011058111A1 (en) | 2009-11-12 | 2011-05-19 | Ucb Pharma S.A. | Aminopurine derivatives as kinase inhibitors |
ES2534096T3 (es) | 2009-11-12 | 2015-04-17 | Ucb Pharma, S.A. | Derivados de piridina y pirazina bicíclicos condensados como inhibidores de quinasa |
JP2013513551A (ja) | 2009-12-10 | 2013-04-22 | 中国医学科学院葯物研究所 | N6−置換アデノシン誘導体とn6−置換アデニン誘導体の鎮静、催眠,抗うつ,抗痙攣,抗てんかん,抗パーキンソン病と認知証予防・治療の用途 |
EP2513109A1 (en) | 2009-12-18 | 2012-10-24 | Amgen Inc. | Heterocyclic compounds and their uses |
WO2011075643A1 (en) | 2009-12-18 | 2011-06-23 | Incyte Corporation | Substituted heteroaryl fused derivatives as pi3k inhibitors |
TW201130842A (en) | 2009-12-18 | 2011-09-16 | Incyte Corp | Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors |
JP2011136925A (ja) | 2009-12-28 | 2011-07-14 | Dainippon Sumitomo Pharma Co Ltd | 含窒素二環性化合物 |
MX2012007954A (es) | 2010-01-07 | 2012-08-03 | Dow Agrosciences Llc | Tiazolo [5, 4-d] pirimidinas y su uso como agroquimicos. |
US8633183B2 (en) | 2010-01-26 | 2014-01-21 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
TWI766281B (zh) | 2010-03-10 | 2022-06-01 | 美商英塞特控股公司 | 作為jak1抑制劑之哌啶-4-基三亞甲亞胺衍生物 |
US20130203778A1 (en) | 2010-03-22 | 2013-08-08 | Glenmark Pharmaceuticals S.A. | Pharmaceutical composition comprising a pyrimidineone derivative |
UY33304A (es) | 2010-04-02 | 2011-10-31 | Amgen Inc | Compuestos heterocíclicos y sus usos |
JP5816678B2 (ja) | 2010-04-14 | 2015-11-18 | インサイト・コーポレイションIncyte Corporation | PI3Kδ阻害剤としての縮合誘導体 |
EP2571357B1 (en) | 2010-05-21 | 2016-07-06 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulation |
US20110306622A1 (en) | 2010-06-11 | 2011-12-15 | Calitoga Pharmaceuticals, Inc. | Methods of treating hematological disorders with quinazolinone compounds in selected subjects |
WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
ES2472720T3 (es) | 2010-07-01 | 2014-07-02 | Amgen Inc. | Compuestos heteroc�clicos y su uso como inhibidores de actividad PI3K |
EP2588467A1 (en) | 2010-07-01 | 2013-05-08 | Amgen Inc. | Heterocyclic compounds and their use as inhibitors of pi3k activity |
AU2011272850A1 (en) | 2010-07-02 | 2013-01-10 | Amgen Inc. | Heterocyclic compounds and their use as inhibitors of PI3K activity |
WO2012040634A1 (en) | 2010-09-24 | 2012-03-29 | Gilead Calistoga Llc | Atropisomers of pi3k-inhibiting compounds |
MX2013005005A (es) | 2010-11-04 | 2013-10-25 | Amgen Inc | Derivados de ciano-4,6-diaminopirimidina o 6-aminopurina como inhibidores de pi3k-delta. |
WO2012064973A2 (en) | 2010-11-10 | 2012-05-18 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
EP2640715A1 (en) | 2010-11-17 | 2013-09-25 | Amgen Inc. | Quinoline derivatives as pik3 inhibitors |
AR083933A1 (es) | 2010-11-19 | 2013-04-10 | Incyte Corp | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
JP5917544B2 (ja) | 2010-11-19 | 2016-05-18 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン |
EP2651405A2 (en) | 2010-12-14 | 2013-10-23 | Electrophoretics Limited | Casein kinase 1 (ck1 ) inhibitors |
JP5961187B2 (ja) | 2010-12-20 | 2016-08-02 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Pi3k阻害剤としてのn−(1−(置換フェニル)エチル)−9h−プリン−6−アミン |
CA2822590A1 (en) | 2010-12-23 | 2012-06-28 | Amgen Inc. | Heterocyclic compounds and their uses |
AR084824A1 (es) | 2011-01-10 | 2013-06-26 | Intellikine Inc | Procesos para preparar isoquinolinonas y formas solidas de isoquinolinonas |
AU2012212323A1 (en) | 2011-02-01 | 2013-09-12 | The Board Of Trustees Of The University Of Illinois | HDAC inhibitors and therapeutic methods using the same |
WO2012125629A1 (en) | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
EA201490042A1 (ru) | 2011-06-20 | 2014-10-30 | Инсайт Корпорейшн | Азетидинил-фенил-, пиридил- или пиразинилкарбоксамидные производные как ингибиторы jak |
AU2012284088B2 (en) | 2011-07-19 | 2015-10-08 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
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 |
WO2013033569A1 (en) | 2011-09-02 | 2013-03-07 | Incyte Corporation | Heterocyclylamines as pi3k inhibitors |
WO2013052699A2 (en) | 2011-10-04 | 2013-04-11 | Gilead Calistoga Llc | Novel quinoxaline inhibitors of pi3k |
AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
AR091079A1 (es) | 2012-05-18 | 2014-12-30 | Incyte Corp | Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak |
CN107936039A (zh) | 2012-11-01 | 2018-04-20 | 因赛特公司 | 作为jak抑制剂的三环稠合噻吩衍生物 |
TWI687220B (zh) * | 2013-03-01 | 2020-03-11 | 美商英塞特控股公司 | 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途 |
KR102311329B1 (ko) | 2013-03-15 | 2021-10-14 | 얀센 파마슈티카 엔.브이. | 약제를 제조하기 위한 방법 및 중간체 |
PL3786162T3 (pl) | 2013-05-17 | 2024-04-08 | Incyte Holdings Corporation | Pochodne bipirazolu jako inhibitory jak |
WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
NZ734993A (en) | 2015-02-27 | 2024-03-22 | Incyte Holdings Corp | Salts of pi3k inhibitor and processes for their preparation |
US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
WO2016183062A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Salts of (s)-7-(1-(9h-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5h-thiazolo[3,2-a]pyrimidin-5-one |
-
2016
- 2016-02-26 NZ NZ734993A patent/NZ734993A/en unknown
- 2016-02-26 HU HUE16718921A patent/HUE053025T2/hu unknown
- 2016-02-26 DK DK16718921.6T patent/DK3262046T3/da active
- 2016-02-26 PE PE2022000834A patent/PE20230156A1/es unknown
- 2016-02-26 LT LTEP16718921.6T patent/LT3262046T/lt unknown
- 2016-02-26 UA UAA201709412A patent/UA122332C2/uk unknown
- 2016-02-26 CN CN202311519531.7A patent/CN117777139A/zh active Pending
- 2016-02-26 BR BR122021004509-7A patent/BR122021004509B1/pt active IP Right Grant
- 2016-02-26 ES ES16718921T patent/ES2843522T3/es active Active
- 2016-02-26 RS RS20201563A patent/RS61233B1/sr unknown
- 2016-02-26 SI SI201631644T patent/SI3831833T1/sl unknown
- 2016-02-26 LT LTEP20201979.0T patent/LT3831833T/lt unknown
- 2016-02-26 JP JP2017544953A patent/JP6816005B2/ja active Active
- 2016-02-26 HU HUE20201979A patent/HUE060953T2/hu unknown
- 2016-02-26 MD MDE20180031T patent/MD3262046T2/ro unknown
- 2016-02-26 TW TW109141640A patent/TWI764392B/zh active
- 2016-02-26 KR KR1020177027583A patent/KR20170132185A/ko active IP Right Grant
- 2016-02-26 AR ARP160100515A patent/AR103804A1/es unknown
- 2016-02-26 AU AU2016222556A patent/AU2016222556B2/en active Active
- 2016-02-26 SG SG10201907576SA patent/SG10201907576SA/en unknown
- 2016-02-26 MY MYPI2017001264A patent/MY187502A/en unknown
- 2016-02-26 PL PL16718921T patent/PL3262046T3/pl unknown
- 2016-02-26 PT PT202019790T patent/PT3831833T/pt unknown
- 2016-02-26 SI SI201630994T patent/SI3262046T1/sl unknown
- 2016-02-26 CN CN202311539089.4A patent/CN117800973A/zh active Pending
- 2016-02-26 NZ NZ773226A patent/NZ773226A/en unknown
- 2016-02-26 RS RS20221159A patent/RS63963B1/sr unknown
- 2016-02-26 PE PE2017001461A patent/PE20180129A1/es unknown
- 2016-02-26 PT PT167189216T patent/PT3262046T/pt unknown
- 2016-02-26 WO PCT/US2016/019741 patent/WO2016138363A1/en active Application Filing
- 2016-02-26 CR CR20210055A patent/CR20210055A/es unknown
- 2016-02-26 DK DK20201979.0T patent/DK3831833T3/da active
- 2016-02-26 CR CR20170389A patent/CR20170389A/es unknown
- 2016-02-26 MX MX2017010918A patent/MX2017010918A/es active IP Right Grant
- 2016-02-26 EP EP20201979.0A patent/EP3831833B1/en active Active
- 2016-02-26 CN CN201680011760.XA patent/CN107580597A/zh not_active Withdrawn
- 2016-02-26 CA CA2977659A patent/CA2977659A1/en active Pending
- 2016-02-26 PL PL20201979.0T patent/PL3831833T3/pl unknown
- 2016-02-26 EA EA201791923A patent/EA201791923A1/ru unknown
- 2016-02-26 MA MA41607A patent/MA41607B1/fr unknown
- 2016-02-26 EP EP22202130.5A patent/EP4183789A1/en active Pending
- 2016-02-26 HR HRP20221444TT patent/HRP20221444T1/hr unknown
- 2016-02-26 US US15/054,474 patent/US10336759B2/en active Active
- 2016-02-26 MD MDE20220030T patent/MD3831833T2/ro unknown
- 2016-02-26 TW TW105106000A patent/TWI748941B/zh active
- 2016-02-26 MA MA55193A patent/MA55193B1/fr unknown
- 2016-02-26 SG SG10201912302VA patent/SG10201912302VA/en unknown
- 2016-02-26 EP EP16718921.6A patent/EP3262046B1/en active Active
- 2016-02-26 CN CN202311505572.0A patent/CN117736209A/zh active Pending
- 2016-02-26 SG SG11201706917WA patent/SG11201706917WA/en unknown
- 2016-02-26 ES ES20201979T patent/ES2933694T3/es active Active
-
2017
- 2017-08-22 IL IL254093A patent/IL254093B/en unknown
- 2017-08-24 MX MX2019012927A patent/MX2019012927A/es unknown
- 2017-08-25 CL CL2017002179A patent/CL2017002179A1/es unknown
- 2017-08-25 PH PH12017501538A patent/PH12017501538A1/en unknown
- 2017-08-30 CO CONC2017/0008924A patent/CO2017008924A2/es unknown
- 2017-09-26 EC ECIEPI201764131A patent/ECSP17064131A/es unknown
-
2018
- 2018-06-14 HK HK18107731.9A patent/HK1248229A1/zh unknown
-
2019
- 2019-06-21 US US16/448,815 patent/US11084822B2/en active Active
- 2019-11-07 CL CL2019003188A patent/CL2019003188A1/es unknown
-
2020
- 2020-05-07 PH PH12020550575A patent/PH12020550575A1/en unknown
- 2020-08-11 AU AU2020217339A patent/AU2020217339B2/en active Active
- 2020-09-09 JP JP2020151255A patent/JP7080941B2/ja active Active
-
2021
- 2021-01-08 HR HRP20210036TT patent/HRP20210036T1/hr unknown
- 2021-01-22 CY CY20211100051T patent/CY1123729T1/el unknown
- 2021-03-02 EC ECSENADI202114448A patent/ECSP21014448A/es unknown
- 2021-12-10 AU AU2021282550A patent/AU2021282550A1/en not_active Abandoned
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20210036T1 (hr) | Soli inhibitora pi3k i postupci za njihovo dobivanje | |
CA3025806C (en) | Degradation of bromodomain-containing protein 9 (brd9) by conjugation of brd9 inhibitors with e3 ligase ligand and methods of use | |
HRP20201582T1 (hr) | Polimorf sik inhibitora | |
ES2873001T3 (es) | Heterociclaminas como inhibidores de PI3K | |
IL283943B2 (en) | Use of pyrazolopyrimidine derivatives for the treatment of p13k associated disorders | |
CN102869359A (zh) | 咪唑并吡啶和嘌呤化合物、组合物和使用方法 | |
WO2015191677A1 (en) | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors | |
HRP20221221T1 (hr) | Pirimidinski spoj kao inhibitor jak kinaze | |
AU2012204982A1 (en) | 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as FAK/Pyk2 inhibitors | |
CN102858754A (zh) | Raf抑制剂化合物及其使用方法 | |
Farag et al. | Reprofiling of pyrimidine-based DAPK1/CSF1R dual inhibitors: identification of 2, 5-diamino-4-pyrimidinol derivatives as novel potential anticancer lead compounds | |
EP3947373A1 (en) | Bicyclic hpk1 inhibitors | |
TW202126643A (zh) | 雜環化合物 | |
WO2020010003A1 (en) | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS | |
Siddesh et al. | Synthesis of thiophene-linked pyrimidopyrimidines as pharmaceutical leads | |
CN104557871B (zh) | 具有螺环取代基的芳基吗啉类化合物,其制备方法和用途 | |
KR102124449B1 (ko) | 7H-피롤로[2,3-d]피리미딘 화합물을 제조하기 위한 방법 | |
CN103827115A (zh) | 咪唑并吡啶化合物、组合物和使用方法 | |
AU2020386189B2 (en) | Adenosine receptor antagonist compounds | |
CA3159211A1 (en) | Fluorinated quinoline, quinoxaline and benzo[b][1,4]oxazine derivatives as dihydroorotate dehydrogenase (dhodh) inhibitors for the treatment of cancer, autoimmune and inflammatory diseases | |
CN113453764A (zh) | 7H-吡咯并[2,3-d]嘧啶-4-胺衍生物 | |
HRP20240252T1 (hr) | Kristalni oblici inhibitora fosfoinozitid 3 kinaze (pi3k) | |
Tănase et al. | New carbocyclic nucleoside analogues with a bicyclo [2.2. 1] heptane fragment as sugar moiety; synthesis, X-ray crystallography and anticancer activity | |
Torres-Gómez et al. | Synthesis of 3-aza [4.4. 3] propellanes with high σ1 receptor affinity | |
Masagalli et al. | Synthesis and molecular docking studies of 1-trityl-5-azaindazole derivatives |