ME02685B - Kristalni oblik pemirolasta - Google Patents
Kristalni oblik pemirolastaInfo
- Publication number
- ME02685B ME02685B MEP-2017-8A MEP817A ME02685B ME 02685 B ME02685 B ME 02685B ME P817 A MEP817 A ME P817A ME 02685 B ME02685 B ME 02685B
- Authority
- ME
- Montenegro
- Prior art keywords
- alkyl
- nrc
- haloalkyl
- halogen
- optionally substituted
- Prior art date
Links
- HIANJWSAHKJQTH-UHFFFAOYSA-N pemirolast Chemical compound CC1=CC=CN(C2=O)C1=NC=C2C=1N=NNN=1 HIANJWSAHKJQTH-UHFFFAOYSA-N 0.000 title 1
- 229960004439 pemirolast Drugs 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 59
- 125000001188 haloalkyl group Chemical group 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 21
- 125000004093 cyano group Chemical group *C#N 0.000 claims 20
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 150000002367 halogens Chemical class 0.000 claims 20
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 20
- 229910003827 NRaRb Inorganic materials 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000002950 monocyclic group Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000004438 haloalkoxy group Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 4
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 201000004624 Dermatitis Diseases 0.000 claims 3
- 150000001356 alkyl thiols Chemical class 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 201000005991 hyperphosphatemia Diseases 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 150000003573 thiols Chemical class 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 102000004311 liver X receptors Human genes 0.000 claims 2
- 108090000865 liver X receptors Proteins 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- 208000000044 Amnesia Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 1
- 208000022461 Glomerular disease Diseases 0.000 claims 1
- 108010081348 HRT1 protein Hairy Proteins 0.000 claims 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 claims 1
- 206010019708 Hepatic steatosis Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 206010055171 Hypertensive nephropathy Diseases 0.000 claims 1
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 1
- 206010021263 IgA nephropathy Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 206010049287 Lipodystrophy acquired Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000010577 Niemann-Pick disease type C Diseases 0.000 claims 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010072170 Skin wound Diseases 0.000 claims 1
- 208000007930 Type C Niemann-Pick Disease Diseases 0.000 claims 1
- 206010048214 Xanthoma Diseases 0.000 claims 1
- 206010048215 Xanthomatosis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 201000001883 cholelithiasis Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 125000004990 dihydroxyalkyl group Chemical group 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000002708 enhancing effect Effects 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 claims 1
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 claims 1
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 208000020346 hyperlipoproteinemia Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 208000006132 lipodystrophy Diseases 0.000 claims 1
- 230000006984 memory degeneration Effects 0.000 claims 1
- 208000023060 memory loss Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 239000008024 pharmaceutical diluent Substances 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 201000001474 proteinuria Diseases 0.000 claims 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 230000009759 skin aging Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 230000037373 wrinkle formation Effects 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—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
- 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
- A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- 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
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—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
- A61P37/00—Drugs for immunological or allergic disorders
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Reproductive Health (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Secondary Cells (AREA)
- Dental Preparations (AREA)
Claims (18)
1. Jedinjenje predstavljeno slijedećom strukturnom formulom: ili njegova farmaceutski prihvatljiva so, gdje X je N ili CRc, R1 je alkil ili -NRaRb; R2 je H; halogen; -CN; -NRC(O)R; -C(O)OR; -C(O)NRaRb; monociklik heteroaromatik opciono supstituisan sa jednom ili više grupa izabranih iz alkila, - CN, -NRC(O)R, -C(O)OR, -C(O)NRaRb i halogena; monocikličnog nearomatičnog heterocikla opciono supstituisanog sa jednom ili više grupa izabranih iz alkil, halogen, -CN i =O; ili alkil opciono supstituisan jednom ili više grupa izabranih iz halogena, hidroksija, alkoksija, -NRaRb, -NRC(O)R,-NRC(O)O(alkil), -NRC(O)N(R)2, -C(O)OR, tiol, alkiltiol, nitro, -CN, =O, -OC(O)H, -OC(O)(alkil), -OC(O)O(alkil), -OC(O)N(R)2 i -C(O)NRaRb; R3 je alkil, haloalkil, hidroksialkil, alkoksialkil, cikloalkil, monociklični nearomatični heterocikl, monociklični heteroaromatik ili fenil, pri čemu je fenil, monociklični nearomatični heterocikl i monociklična heteroaromatična grupa predstavljena pomoću R3 su opciono supstituisane jednom ili više grupa izabranih iz alkila, halogena, haloalkila, alkoksi, haloalkoksi, nitro i -CN; R4 i R5 nezavisno su halogen, -CN, -OR, -SR, -N(R)2, -C(O)R, -C(O)OR, -OC(O)O(alkil), -C(O)O(haloalkil), -OC(O)R, -C(O)N(R)2, -OC(O)N(R)2, -NRC( O)R, -NRC(O)O(alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS(O)R, -NRSO2R, -NRC(O)N(R)2, -NRSO2N(R)2, haloalkil, haloalkoksi, cikloalkoksi, cikloalkil, monociklični nearomatični heterocikl, monociklični heteroaromatik ili alkil, pri čemu alkil, monociklični nearomatični heterocikl i monociklični heteroaromatik grupa predstavljeni pomoću R4 ili R5 se opciono supstituišu sa jednom ili više grupa izabranih iz -CN, -OR, -SR, -N(R)2, =O, -C(O)R, -C(O)OR, -C(O)O(haloalkil), -OC(O)R, -OC(O)O(alkil), -C(O)N(R )2, -OC(O)N(R)2, -NRC(O)R, -NRC(O)O(alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS (O)R, -NRSO2R, -NRC(O)N(R)2 i -NRSO2N(R)2; R6 je H, halogen, -CN, -OR, -SR, -N(R)2, -C(O)R, -C(O)OR, -OC(O)O(alkil), -C(O)O(haloalkil), -OC(O)R, -C(O)N(R)2, -OC(O)N(R)2, -NRC(O)R, -NRC(O)O( alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS(O)R, -NRSO2R, -NRC(O)N(R)2, -NRSO2 N(R)2, haloalkil, haloalkoksi, cikloalkoksi, cikloalkil ili alkil, pri čemu alkil grupa predstavljena pomoću R6 je opciono supstituisana sa jednom ili više grupa izabranih iz -CN, -OR, -SR, -N(R)2, =O, -C(O)R, -C(O)OR, -C(O)O(haloalkil), -OC(O)R, -OC(O)O(alkil), -C(O)N(R) 2, -OC(O)N(R)2, -NRC(O)R, -NRC(O)O(alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS( O)R, -NRSO2R, -NRC(O)N(R)2 i -NRSO2N(R)2; ili R5 i R6, uzeti zajedno sa atomima ugljenika na koje se oni vjezuju, formiraju monociklični nearomatični heterocikl opciono supstituisan sa jednom ili više grupa izabranih iz alkila, halogena, hidroksialkil, alkoksi alkil, haloalkil i =O; i svaki R nezavisno je H ili alkil; Ra i Rb se nezavisno H, alkil ili Ra i Rb moguće je uzeti zajedno sa azotom na koji se oni spoje da formiraju monociklični nearomatični heterocikl; i Rc je H, alkil, ili halogen.
2. Jedinjenje prema patentnom zahtijevu 1, gdje je: R3 je alkil, haloalkil, hidroksialkil, alkoksialkil, cikloalkil ili fenil, pri čemu fenil grupa predstavljena pomoću R3 je opciono supstituisana sa jednom ili više grupa izabranih iz alkila, halogena, haloalkila, alkoksi, haloalkoksi, azot i -CN; R4 i R5 nezavisno su halogen, -CN, -OR, -SR, -N(R)2, -C(O)R, -C(O)OR, -OC(O)O(alkil), -C(O)O(haloalkil), -OC(O)R, -C(O)N(R)2, -OC(O)N(R)2, -NRC( O)R, -NRC(O)O(alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS(O)R, -NRSO2R, -NRC( O)N(R)2, -NRSO2N(R)2, haloalkil, haloalkoksi, cikloalkoksi, cikloalkil ili alkil, pri čemu je alkil predstavljen pomoću R4 ili R5 opciono supstituisan sa jednom ili više grupa izabranih iz -CN, -OR, -SR, -N(R)2, =O, -C(O)R, -C(O)OR, -C(O)O(haloalkil), -OC(O)R, -OC(O)O(alkil), -C(O)N(R )2, -OC(O)N(R)2, -NRC(O)R, -NRC(O)O(alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS (O)R, -NRSO2R, -NRC(O)N(R)2 i -NRSO2N(R)2; R6 je H, halogen, -CN, -OR, -SR, -N(R)2, -C(O)R, -C(O)OR, -OC(O)O(alkil), -C(O)O(haloalkil), -OC(O)R, -C(O)N(R)2, -OC(O)N(R)2, -NRC(O)R, -NRC(O)O (alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS(O)R, -NRSO2R, -NRC(O)N(R)2, -NRSO 2N(R)2, haloalkil, haloalkoksi, cikloalkoksi, cikloalkil ili alkil, pri čemu alkil grupa predstavljena pomoću R6 se opciono supstituiše sa jednom ili više grupa izabranih iz -CN, -OR, -SR, -N(R)2, =O, -C(O)R, -C(O)OR, -C(O)O(haloalkil), -OC(O)R, -OC(O)O(alkil), -C(O)N(R) 2, -OC(O)N(R)2, -NRC(O)R, -NRC(O)O(alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS( O)R, -NRSO2R, -NRC(O)N(R)2 i -NRSO2N(R)2.
3. Jedinjenje prema patentnom zahtijevu 1 ili 2, gdje je jedinjenje predstavljeno slijedećom strukturnom formulom: ili njegova farmaceutski prihvatljiva so.
4. Jedinjenje prema patentnom zahtijevu 1 ili 2, gdje je jedinjenje predstavljeno slijedećom strukturnom formulom: ili njegova farmaceutski prihvatljiva so.
5. Jedinjenje iz bilo kog od prijethodnih patentnih zahtijeva, pri čemu: R1 je metil ili -NH2 ; R2 je H ili metil, pri čemu metil grupa predstavljena pomoću R2 se opciono supstituiše sa jednom ili više grupa izabranih iz halogena, hidroksi, alkoksi, -NRaRb,-NRC(O)R, -NRC(O)O(alkil), -NRC(O)N(R)2, -C(O)OR, tiol, alkiltiol, nitro, -CN, =O,-OC(O)H, -OC(O)(alkil), -OC(O)O(alkil), -C(O)NRaRb i -OC(O)N(R)2; R3 je metil, etil, propil, izopropil, tert-butil, sek-butil, izo-butil, -CH2CF3, -CH(CH2F)2, -CH(CHF2)2, -CH(CF3)2, -CF(CH3)2, -CF3, ciklopropil, ciklobutil, ciklopentil, cikloheksil, -C(OH)(CH3)2, -CH(OH)(CH3), ili fenil, pri čemu fenil grupa, predstavljena pomoću R3 , se opciono supstituiše sa jednom ili više grupa izabranih iz alkil, halogen, haloalkil, alkoksi, haloalkoksi, nitro i -CN; i Rc, gdje je prisutan, je H.
6.Jedinjenje iz bilo kod od prijethodnih patentnih zahtijeva, gdje: R1 je metil; R2 je -CH2OH; R3 je izopropil; i R4 i R5 nezavisno su halogen, hidroksi, alkil, cikloalkil, cikloalkoksi, alkoksi, haloalkoksi, haloalkil, -N(R)2, -C(O)OH, -C(O)O(alkil), -C(O)O(haloalkil), -C(O)(alkil), -C(O) N(R)2, -NRC(O)R, -SO2N(R)2, -OC(O)N(R)2, -CN, hidroksialkil ili dihidroksialkil.
7.Jedinjenje prema bilo kom od prijethodnih patentnih zahtijeva, pri čemu R4 i R5 nezavisno su metil, etil, hidroksi, CF3, izopropil, ciklopropil, -CH2OH, -CH(OH)(CH2)(OH), -C(OH)(CH3)2, -CH(OH)(CH3), -CH(OH)(CH2)(CH3), -CH(OH)(CH2)2(CH3), -C(O)NH2, -C(O)N(CH3)2, -C(O)OH, -C(O)NH(CH3), -C(O)CH3, -C (O)CH2CH3, -C(O)O(CH2)(CH3), -C(O)O(tert-butil), -C(O)O(C)(CH3)2(CF3), -NHC(O)CH3,-OCHF2, -OCF3, -OCH2CH3, -OCH(CH3)2 ili -OCH3.
8.Jedinjenje prema bilo kom od prijethodnih patentnih zahtijeva, pri čemu R4 jeste alkil, haloalkil, cikloalkil, alkoksi, ili haloalkoksi
9.Jedinjenje prema bilo kom od prijethodnih patentnih zahtijeva, pri čemu R4 jeste metil, halogenisani metil, ciklopropil, -OCHF2 ili -OCH3.
10.Jedinjenje iz bilo kog od prijethodnih patentnih zahtijeva, gde R4 jesta CF3.
11.Jedinjenje iz bilo kog od prijethodnih patentnih zahtijeva, pri čemu R5 jeste -C(OH)(CH3)2.
12. Jedinjenje iz patentnog zahtijeva 1, pri čemu je jedinjenje predstavljeno strukturnom formulom izabranom iz i ili njegove farmaceutski prihvatljive soli.
13. Jedinjenje prema patentnom zahtijevu 1, pri čemu je jedinjenje predstavljeno slijedećom strukturnom formulom: ili njegova farmaceutski prihvatljiva so.
14. Farmaceutska supstanca koja obuhvata farmaceutski nosač ili razblaživač i jedinjenje prema bilo kojem od patentnih zahtijeva 1-13.
15. Jedinjenje prema bilo kojem od patentnih zahtijeva 1 -13 za upotrebu u liječenju ispitanika sa bolešću ili poremećajem koji se liječi pojačavanjem aktivnosti jetrenog X receptora (LXR).
16. Upotreba iz patentnog zahtijeva 15, pri čemu je bolest ili poremećaj hiperlipidemija, hiperholesterolemija, hiperlipoproteinemija, hipertrigliceridemija, lipodistrofija, steatoza jetre (bolest masne jetre), nealkoholni steatohepatitis (NASH), nealkoholna bolest masne jetre (NAFLD), hiperglicemija, otpornost na insulin, dijabetes melitus, dislipidemija, ateroskleroza, bolest kamena u žuči, akne vulgaris, dermatitis, psorijaza, kontaktni dermatitis, atopični dermatitis, ekcem, rane na koži, starijenje kože, starijenje usled izloženosti zracima, stvaranje bora, dijabetes, Nieman-Pikova bolest tipa C, Parkinsonova bolest, Alchajmerova bolest, upala, ksantom, gojaznost, metabolički sindrom, X sindrom, moždani udar, periferna bolest začepljenja, gubitak memorije, dijabetesne neuropatije, proteinurije, glomerulopatije, dijabetesna nefropatija, hipertenzivna nefropatija IGA nefropatija, fokalna segmentalna glomeruloskleroza, hiperfosfatemija, kardiovaskularne komplikacije hiperfosfatemije, kancer ili multipla skelroza.
17.Jedinjenje za upotrebu prema patentnom zahtijevu 16 pri čemu je bolest ili poremećaj ateroskleroza, Alchajmerova bolest, kardiovaskularna bolest, kardiovaskularne komplikacije hiperfosfatemije, ili dermatitisa.
18. Jedinjenje predstavljeno slijedećom strukturnom formulom: ili njegova so, pri čemu: X je N ili CRc. R10 je alkil ili -NRaRb; R20 je H; halogen; -CN; -NRC(O)R; -C(O)OR; -C(O)NRaRb; monociklični heteroaromatik opciono supstituisan sa jednom ili više grupa izabranih iz alkila, -CN, -NRC(O)R, -C(O)OR, -C(O)NRaRb i halogena; monocikličnog nearomatičnog heterocikla opciono supstituisanog jednom ili više grupa izabranih iz alkila, halogena, -CN i =O; ili alkil opciono supstituisan jednom ili više grupa izabranih iz halogena, hidroksija, alkoksija, -NRaRb, -NRC(O)R,-NRC(O)O(alki), -NRC(O)N(R)2, -C(O)OR, tiol, alkitiol, nitro, -CN, =O, -OC(O)H, -OC(O)(alkil), -OC(O)O(alkil), -OC(O)N(R)2, -C(O)NRaRb, i-O(zaštitna grupa); R30 je alkil, haloalkil, hidroksialkil, alkoksialkil, cikloalkil ili fenil, pri čemu fenil grupa predstavljena pomoću R30 je opciono supstituisana sa jednom ili više grupa izabranih iz alkil, haloalkil, alkoksi, haloalkoksi, nitro i -CN; svaki R nezavisno je H ili alkil; Ra i Rb su nezavisno H, alkil ili Ra i Rb može da se uzme zajedno sa azotom na koji se oni spoje da formiraju monociklični nearomatični heterocikl; i Rc je H, alkil, ili halogen.
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| US18734809P | 2009-06-16 | 2009-06-16 | |
| US18735509P | 2009-06-16 | 2009-06-16 | |
| EP10732402.2A EP2443120B1 (en) | 2009-06-16 | 2010-06-15 | Crystalline form of pemirolast |
| PCT/GB2010/001168 WO2010146348A2 (en) | 2009-06-16 | 2010-06-15 | New crystalline form of pemirolast |
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| US20120329813A1 (en) * | 2009-11-13 | 2012-12-27 | Cardoz Ab | Pemirolast for the Treatment of Systemic Low Grade Inflammation |
| EA034550B1 (ru) * | 2013-03-09 | 2020-02-19 | КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. | Способы лечения, снижения частоты и/или профилактики ишемических событий |
| US20160243122A1 (en) | 2014-10-23 | 2016-08-25 | Rspr Pharma Ab | Use of pemirolast in the treatment of acute asthma |
| WO2016102941A1 (en) | 2014-12-22 | 2016-06-30 | Rspr Pharma Ab | New combination of pemirolast and montelukast |
| GB201518831D0 (en) | 2015-10-23 | 2015-12-09 | Rspr Pharma Ab | New use |
| US10828303B2 (en) * | 2016-10-03 | 2020-11-10 | Brivention Pharmaceutical (Shanghai) Inc. | Composition comprising combination of TRH analog with arundic acid, and pharmaceutically acceptable salt of arundic acid |
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| US4122274A (en) * | 1977-05-25 | 1978-10-24 | Bristol-Myers Company | 3-Tetrazolo-5,6,7,8-substituted-pyrido[1,2-a]pyrimidin-4-ones |
| JP2504788B2 (ja) | 1987-11-10 | 1996-06-05 | 東京田辺製薬株式会社 | ９−メチル−３−（１Ｈ−テトラゾ―ル−５−イル）−４Ｈ−ピリド［１，２−ａ］ピリミジン−４−オンカリウム塩の水性製剤 |
| JP2837449B2 (ja) * | 1989-08-11 | 1998-12-16 | 東京田辺製薬株式会社 | ピリド［１，２―ａ］ピリミジン誘導体の製造法 |
| ITMI20011764A1 (it) | 2001-08-10 | 2003-02-10 | Dinamite Dipharma Spa | Metodo per l'ottenimento del pemirolast ad elevata purezza |
| KR101361441B1 (ko) | 2005-09-16 | 2014-02-10 | 다이이찌 산쿄 가부시키가이샤 | 광학활성인 디아민 유도체 및 그의 제조방법 |
| WO2008074975A1 (en) | 2006-12-18 | 2008-06-26 | Cardoz Ab | New combination for use in the treatment of inflammatory disorders |
| EP2107907B1 (en) | 2006-12-20 | 2012-02-01 | Cardoz AB | Combination of pemirolast and ramatroban for use in the treatment of inflammatory disorders |
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