PH12015502141B1 - Substituted xanthines and methods of use thereof - Google Patents
Substituted xanthines and methods of use thereof Download PDFInfo
- Publication number
- PH12015502141B1 PH12015502141B1 PH12015502141A PH12015502141A PH12015502141B1 PH 12015502141 B1 PH12015502141 B1 PH 12015502141B1 PH 12015502141 A PH12015502141 A PH 12015502141A PH 12015502141 A PH12015502141 A PH 12015502141A PH 12015502141 B1 PH12015502141 B1 PH 12015502141B1
- Authority
- PH
- Philippines
- Prior art keywords
- alkyl
- ntn
- compound
- haloalkyl
- alkoxy
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract description 9
- 229940065721 systemic for obstructive airway disease xanthines Drugs 0.000 title description 2
- LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical class O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 48
- 125000000217 alkyl group Chemical group 0.000 claims description 75
- 125000003545 alkoxy group Chemical group 0.000 claims description 24
- 125000001188 haloalkyl group Chemical group 0.000 claims description 24
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 23
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 21
- 125000004104 aryloxy group Chemical group 0.000 claims description 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 17
- 150000003839 salts Chemical class 0.000 claims description 13
- 208000035475 disorder Diseases 0.000 claims description 11
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 8
- 206010015037 epilepsy Diseases 0.000 claims description 4
- 208000017169 kidney disease Diseases 0.000 claims description 4
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 4
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 102000003621 TRPC5 Human genes 0.000 abstract description 13
- 101150042815 TRPC5 gene Proteins 0.000 abstract description 13
- 102000004310 Ion Channels Human genes 0.000 abstract description 9
- 239000000203 mixture Substances 0.000 abstract description 5
- 230000002401 inhibitory effect Effects 0.000 abstract description 3
- 125000003118 aryl group Chemical group 0.000 description 32
- 125000001072 heteroaryl group Chemical group 0.000 description 20
- 230000001404 mediated effect Effects 0.000 description 18
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 17
- 125000003368 amide group Chemical group 0.000 description 15
- 125000004663 dialkyl amino group Chemical group 0.000 description 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 15
- 125000003342 alkenyl group Chemical group 0.000 description 13
- 125000000304 alkynyl group Chemical group 0.000 description 13
- -1 e.g. Chemical group 0.000 description 13
- 125000005843 halogen group Chemical group 0.000 description 13
- 239000011575 calcium Substances 0.000 description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 11
- 229940100389 Sulfonylurea Drugs 0.000 description 9
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 9
- 125000002252 acyl group Chemical group 0.000 description 9
- 125000002102 aryl alkyloxo group Chemical group 0.000 description 9
- 239000004202 carbamide Substances 0.000 description 9
- 125000004093 cyano group Chemical group *C#N 0.000 description 9
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 9
- 125000005864 sulfonamidyl group Chemical group 0.000 description 9
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 description 9
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 8
- 108090000862 Ion Channels Proteins 0.000 description 8
- 125000000753 cycloalkyl group Chemical group 0.000 description 8
- 229910052791 calcium Inorganic materials 0.000 description 7
- 230000004907 flux Effects 0.000 description 7
- 125000005553 heteroaryloxy group Chemical group 0.000 description 7
- 150000002500 ions Chemical class 0.000 description 7
- 125000004076 pyridyl group Chemical group 0.000 description 7
- 239000011734 sodium Substances 0.000 description 7
- 125000003282 alkyl amino group Chemical group 0.000 description 6
- 125000000000 cycloalkoxy group Chemical group 0.000 description 6
- 125000000335 thiazolyl group Chemical group 0.000 description 6
- 241000700159 Rattus Species 0.000 description 5
- 230000004913 activation Effects 0.000 description 5
- 239000005557 antagonist Substances 0.000 description 5
- 210000004027 cell Anatomy 0.000 description 5
- 239000003795 chemical substances by application Substances 0.000 description 5
- 201000010099 disease Diseases 0.000 description 5
- 230000006870 function Effects 0.000 description 5
- 230000014509 gene expression Effects 0.000 description 5
- 229920000609 methyl cellulose Polymers 0.000 description 5
- 229960002900 methylcellulose Drugs 0.000 description 5
- 239000001923 methylcellulose Substances 0.000 description 5
- 238000012360 testing method Methods 0.000 description 5
- 108091005462 Cation channels Proteins 0.000 description 4
- 239000000470 constituent Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 230000003834 intracellular effect Effects 0.000 description 4
- 239000012528 membrane Substances 0.000 description 4
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 description 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 3
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 3
- 238000011785 NMRI mouse Methods 0.000 description 3
- 125000005257 alkyl acyl group Chemical group 0.000 description 3
- 230000001413 cellular effect Effects 0.000 description 3
- 125000001309 chloro group Chemical group Cl* 0.000 description 3
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- 125000002971 oxazolyl group Chemical group 0.000 description 3
- 125000000714 pyrimidinyl group Chemical group 0.000 description 3
- 229910052708 sodium Inorganic materials 0.000 description 3
- 206010001497 Agitation Diseases 0.000 description 2
- 101150107341 RERE gene Proteins 0.000 description 2
- 241000282887 Suidae Species 0.000 description 2
- 125000003710 aryl alkyl group Chemical group 0.000 description 2
- 230000004094 calcium homeostasis Effects 0.000 description 2
- 230000009460 calcium influx Effects 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 230000013632 homeostatic process Effects 0.000 description 2
- 238000005462 in vivo assay Methods 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 239000007928 intraperitoneal injection Substances 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 230000010291 membrane polarization Effects 0.000 description 2
- DDLIGBOFAVUZHB-UHFFFAOYSA-N midazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NC=C2CN=C1C1=CC=CC=C1F DDLIGBOFAVUZHB-UHFFFAOYSA-N 0.000 description 2
- 229960003793 midazolam Drugs 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- JTJMJGYZQZDUJJ-UHFFFAOYSA-N phencyclidine Chemical compound C1CCCCN1C1(C=2C=CC=CC=2)CCCCC1 JTJMJGYZQZDUJJ-UHFFFAOYSA-N 0.000 description 2
- 230000019491 signal transduction Effects 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 241000234282 Allium Species 0.000 description 1
- 235000002732 Allium cepa var. cepa Nutrition 0.000 description 1
- 239000001741 Ammonium adipate Substances 0.000 description 1
- 101100492584 Caenorhabditis elegans ast-1 gene Proteins 0.000 description 1
- 108010001857 Cell Surface Receptors Proteins 0.000 description 1
- 108091006146 Channels Proteins 0.000 description 1
- HCYAFALTSJYZDH-UHFFFAOYSA-N Desimpramine Chemical compound C1CC2=CC=CC=C2N(CCCNC)C2=CC=CC=C21 HCYAFALTSJYZDH-UHFFFAOYSA-N 0.000 description 1
- 108010030204 H-asparaginyl-arginyl-valyl-tyrosyl-isoleucyl-histyl-prolyl-phenylalanyl-histyl-leucyl-valyl-isoleucyl-serine Proteins 0.000 description 1
- 241000575946 Ione Species 0.000 description 1
- LTXREWYXXSTFRX-QGZVFWFLSA-N Linagliptin Chemical compound N=1C=2N(C)C(=O)N(CC=3N=C4C=CC=CC4=C(C)N=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 LTXREWYXXSTFRX-QGZVFWFLSA-N 0.000 description 1
- 101100426589 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) trp-3 gene Proteins 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 102000002628 TRPC Cation Channels Human genes 0.000 description 1
- 108010082847 TRPC Cation Channels Proteins 0.000 description 1
- 102000003627 TRPC1 Human genes 0.000 description 1
- 101150017559 TRPC1 gene Proteins 0.000 description 1
- 102000003629 TRPC3 Human genes 0.000 description 1
- 101150037542 Trpc3 gene Proteins 0.000 description 1
- 241000271897 Viperidae Species 0.000 description 1
- 230000001594 aberrant effect Effects 0.000 description 1
- 230000036982 action potential Effects 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 239000000058 anti acne agent Substances 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 230000001028 anti-proliverative effect Effects 0.000 description 1
- 230000002682 anti-psoriatic effect Effects 0.000 description 1
- 230000001153 anti-wrinkle effect Effects 0.000 description 1
- 229940124340 antiacne agent Drugs 0.000 description 1
- 239000003429 antifungal agent Substances 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 239000004599 antimicrobial Substances 0.000 description 1
- 239000002282 antimigraine agent Substances 0.000 description 1
- 229940125684 antimigraine agent Drugs 0.000 description 1
- 239000003443 antiviral agent Substances 0.000 description 1
- 230000000949 anxiolytic effect Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 229910001424 calcium ion Inorganic materials 0.000 description 1
- 230000000747 cardiac effect Effects 0.000 description 1
- 230000022900 cardiac muscle contraction Effects 0.000 description 1
- 230000003915 cell function Effects 0.000 description 1
- 229960003914 desipramine Drugs 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 239000003966 growth inhibitor Substances 0.000 description 1
- 230000003779 hair growth Effects 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000010262 intracellular communication Effects 0.000 description 1
- 239000003410 keratolytic agent Substances 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 230000028161 membrane depolarization Effects 0.000 description 1
- 102000006240 membrane receptors Human genes 0.000 description 1
- 108020004999 messenger RNA Proteins 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- YLGXILFCIXHCMC-JHGZEJCSSA-N methyl cellulose Chemical compound COC1C(OC)C(OC)C(COC)O[C@H]1O[C@H]1C(OC)C(OC)C(OC)OC1COC YLGXILFCIXHCMC-JHGZEJCSSA-N 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 229960003730 methylcellulose (4000 cps) Drugs 0.000 description 1
- 239000013642 negative control Substances 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 230000001590 oxidative effect Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229950010883 phencyclidine Drugs 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000012232 skeletal muscle contraction Effects 0.000 description 1
- 230000016160 smooth muscle contraction Effects 0.000 description 1
- 229910001415 sodium ion Inorganic materials 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 238000011706 wistar kyoto rat Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
- C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
-
- 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
-
- 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
- C07D487/12—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 three hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Medicinal Preparation (AREA)
- Silver Salt Photography Or Processing Solution Therefor (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Enzymes And Modification Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361789724P | 2013-03-15 | 2013-03-15 | |
| PCT/US2014/027920 WO2014143799A2 (en) | 2013-03-15 | 2014-03-14 | Substituted xanthines and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| PH12015502141A1 PH12015502141A1 (en) | 2016-01-25 |
| PH12015502141B1 true PH12015502141B1 (en) | 2018-10-12 |
Family
ID=50680155
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH12015502141A PH12015502141B1 (en) | 2013-03-15 | 2015-09-15 | Substituted xanthines and methods of use thereof |
Country Status (31)
| Country | Link |
|---|---|
| US (7) | US9359359B2 (enExample) |
| EP (1) | EP2970303B3 (enExample) |
| JP (1) | JP6360149B2 (enExample) |
| KR (1) | KR102227629B1 (enExample) |
| CN (2) | CN105143229B (enExample) |
| AU (1) | AU2014228206C1 (enExample) |
| CA (1) | CA2899646C (enExample) |
| CL (1) | CL2015002738A1 (enExample) |
| CY (1) | CY1119042T1 (enExample) |
| DK (1) | DK2970303T6 (enExample) |
| EA (1) | EA028815B1 (enExample) |
| ES (1) | ES2636835T7 (enExample) |
| HR (1) | HRP20170840T4 (enExample) |
| HU (1) | HUE033528T4 (enExample) |
| IL (1) | IL240216B (enExample) |
| LT (1) | LT2970303T (enExample) |
| MX (1) | MX370372B (enExample) |
| MY (1) | MY189912A (enExample) |
| NZ (1) | NZ711718A (enExample) |
| PE (1) | PE20151779A1 (enExample) |
| PH (1) | PH12015502141B1 (enExample) |
| PL (1) | PL2970303T6 (enExample) |
| PT (1) | PT2970303T (enExample) |
| RS (1) | RS56066B2 (enExample) |
| SG (1) | SG11201506479TA (enExample) |
| SI (1) | SI2970303T1 (enExample) |
| TW (1) | TWI609867B (enExample) |
| UA (1) | UA117470C2 (enExample) |
| UY (1) | UY35488A (enExample) |
| WO (1) | WO2014143799A2 (enExample) |
| ZA (1) | ZA201505414B (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8173750B2 (en) | 2009-04-23 | 2012-05-08 | ATRP Solutions, Inc. | Star macromolecules for personal and home care |
| KR102227629B1 (ko) | 2013-03-15 | 2021-03-16 | 하이드라 바이오사이언시스, 엘엘씨 | 치환된 잔틴 및 그것의 사용 방법 |
| WO2016023831A1 (en) * | 2014-08-11 | 2016-02-18 | Hydra Biosciences, Inc. | Pyrrolo[3,2-d]pyrimidine-2,4(3h,5h)-dione derivatives |
| GB2553686B (en) | 2015-03-27 | 2020-06-03 | Latvian Inst Organic Synthesis | Ethynylxanthines, preparation and use as calcium ion channel modulators |
| GB2553684B (en) | 2015-03-27 | 2020-06-03 | Latvian Inst Organic Synthesis | Ethynylxanthines, preparation and use for cancer treatment |
| GB2553685B (en) | 2015-03-27 | 2020-06-10 | Latvian Inst Organic Synthesis | Novel ethynylxanthines for use as inhibitors of matrix metalloproteinases and angiogenesis |
| US9593118B2 (en) * | 2015-04-08 | 2017-03-14 | Lewis And Clark Pharmaceuticals, Inc. | Xanthine-substituted alkynyl carbamates/reverse carbamates as A2B antagonists |
| CN107118586A (zh) * | 2016-02-24 | 2017-09-01 | 中国科学技术大学 | 含氮杂环基取代的烯类化合物的用途 |
| GB201702160D0 (en) | 2017-02-09 | 2017-03-29 | Univ Leeds Innovations Ltd | Inhibitors for use in therapy |
| US11666577B2 (en) * | 2017-02-28 | 2023-06-06 | National Institute Of Biological Sciences, Beijing | MLKL inhibitors |
| WO2018157800A1 (en) * | 2017-02-28 | 2018-09-07 | National Institute Of Biological Sciences, Beijing | Mlkl inhibitors |
| DK3652176T3 (da) * | 2017-07-11 | 2022-01-17 | Boehringer Ingelheim Int | Substituerede xanthinderivater |
| US11623930B2 (en) | 2018-03-05 | 2023-04-11 | Goldfinch Bio, Inc. | Imidazodiazepinediones and methods of use thereof |
| PL3894410T3 (pl) * | 2018-12-12 | 2024-03-18 | Boehringer Ingelheim International Gmbh | Podstawione pochodne ksantyny |
| EP3894409B1 (en) * | 2018-12-12 | 2023-08-23 | Boehringer Ingelheim International GmbH | Substituted xanthine derivatives |
| CN112979651B (zh) * | 2021-04-09 | 2022-02-01 | 南京纽邦生物科技有限公司 | 一种副黄嘌呤的制备方法 |
| CN113354646B (zh) * | 2021-07-06 | 2022-11-15 | 南开大学 | 8-芳氧基烷氧基取代黄嘌呤衍生物及其制备方法和应用 |
| CN115636831B (zh) * | 2022-10-27 | 2024-11-08 | 中国药科大学 | 稠合嘧啶二酮类化合物、其用途以及药物组合物 |
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| CN118459461A (zh) * | 2023-02-08 | 2024-08-09 | 中国科学院上海药物研究所 | 黄嘌呤类化合物及其用途 |
| WO2025250920A1 (en) | 2024-05-31 | 2025-12-04 | Gfb (Abc), Llc | Pyridazinone phosphate compounds, pharmaceutical compositions, and medical uses thereof |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4304650A1 (de) * | 1993-02-16 | 1994-08-18 | Thomae Gmbh Dr K | Kondensierte 5-gliedrige Heterocyclen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| US6878715B1 (en) * | 1994-02-18 | 2005-04-12 | Cell Therapeutics, Inc. | Therapeutic compounds for inhibiting interleukin-12 signals and method for using same |
| JP4191269B2 (ja) | 1996-05-17 | 2008-12-03 | 興和株式会社 | 新規なアニリド化合物及びこれを含有する医薬 |
| JPH10318487A (ja) | 1997-05-16 | 1998-12-04 | Mitsubishi Gas Chem Co Inc | 真空断熱材用ゲッタ |
| US6075029A (en) | 1998-01-02 | 2000-06-13 | Cell Therapeutics, Inc. | Xanthine modulators of metabolism of cellular P-450 |
| US6187780B1 (en) * | 1998-04-16 | 2001-02-13 | Boehringer Ingelheim Pharma Kg | Assymetrically substituted xanthine derivatives having adenosine A1 antagonistic activity |
| MXPA01010143A (es) * | 1999-04-09 | 2003-07-14 | Cell Therapeutics Inc | Derivados de xantina y analogos como inhibidores de transmision de senales celulares. |
| RU2003103103A (ru) * | 2000-07-04 | 2004-08-20 | Ново Нордиск А/С (DK) | Гетероциклические соединения, которые являются ингибиторами фермента dpp-iv |
| CN1486302A (zh) | 2000-12-07 | 2004-03-31 | CV���ƹ�˾ | 作为抗冠状动脉疾病或动脉硬化的abca-1加强化合物的取代1,3,5-三嗪和嘧啶 |
| CZ305402B6 (cs) * | 2001-02-24 | 2015-09-02 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthinové deriváty, jejich výroba a použití v kombinační terapii |
| RU2318824C2 (ru) * | 2001-11-09 | 2008-03-10 | Си Ви Терапьютикс, Инк. | Антагонисты рецептора аденозина a2b, фармацевтическая композиция на их основе и способ их получения |
| DE60322748D1 (de) * | 2003-05-06 | 2008-09-18 | Cv Therapeutics Inc | Xanthinderivate als a2b-adenosinrezeptorantagonisten |
| US20050182011A1 (en) | 2003-11-13 | 2005-08-18 | Eric Olson | Inhibition of TRP channels as a treatment for cardiac hypertrophy and heart failure |
| US7393827B2 (en) | 2004-12-30 | 2008-07-01 | Diakine Therapeutics, Inc. | Pharmaceutical compositions and methods for restoring β-cell mass and function |
| US8143254B2 (en) | 2005-02-18 | 2012-03-27 | Cornell Research Foundation, Inc. | Methods for modulating ion channels |
| WO2007017262A1 (en) * | 2005-08-10 | 2007-02-15 | Smithkline Beecham Corporation | Xanthine derivatives as selective hm74a agonists |
| JP2009507020A (ja) | 2005-09-06 | 2009-02-19 | スミスクライン ビーチャム コーポレーション | Ｐｌｋ調節物質としてのルベンゾイミダゾールチオフェン化合物 |
| US20090018148A1 (en) * | 2005-12-07 | 2009-01-15 | Ucb Pharma, S.A. | Xanthine Derivatives, Processes For Preparing Them And Their Uses |
| TW201900217A (zh) * | 2005-12-22 | 2019-01-01 | 美商海卓勒生物科學公司 | 用於調節ｔｒｐａ１功能之化合物 |
| WO2007084728A2 (en) | 2006-01-19 | 2007-07-26 | Abbott Laboratories | 2-imino-benzimidazoles |
| WO2007101213A2 (en) | 2006-02-28 | 2007-09-07 | Kalypsys, Inc. | Novel 2-oxo-1,2,3,4-tetrahydropyrimidines, bicyclic pyrimidine diones and imidazolidine-2,4-diones useful as inducible nitric oxide synthase inhibitors |
| US20090269313A1 (en) * | 2006-07-19 | 2009-10-29 | Diakine Therapeutics, Inc. | Encapsulation system |
| WO2009157938A1 (en) * | 2008-06-26 | 2009-12-30 | Cv Therapeutics, Inc. | A2b adenosine receptor antagonists for treating cancer |
| EP2467398B1 (en) | 2009-08-20 | 2019-10-09 | Poseida Therapeutics, Inc. | Trpc4 inhibitors and uses thereof |
| WO2011114184A1 (en) * | 2010-03-15 | 2011-09-22 | Glenmark Pharmaceuticals S.A. | Amides of heterocyclic compounds as trpa1 inhibitors |
| US9260430B2 (en) | 2010-06-08 | 2016-02-16 | Hydra Biosciences, Inc. | Use of TRPA1 antagonists to prevent or treat infections caused by biological-warfare agents |
| JP2013023102A (ja) | 2011-07-22 | 2013-02-04 | Panasonic Corp | 列車情報提供システム |
| BR112014002960A2 (pt) | 2011-08-09 | 2017-02-21 | Cubist Pharm Inc | inibição de canal de íons potencial receptor transiente trpa1 |
| CN103121970B (zh) | 2012-12-04 | 2015-04-29 | 中国科学院昆明植物研究所 | 苯并咪唑及其衍生物，其药物组合物及其在制备抗抑郁药物中的应用 |
| KR102227629B1 (ko) | 2013-03-15 | 2021-03-16 | 하이드라 바이오사이언시스, 엘엘씨 | 치환된 잔틴 및 그것의 사용 방법 |
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