CA3119909A1 - A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension - Google Patents
A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension Download PDFInfo
- Publication number
- CA3119909A1 CA3119909A1 CA3119909A CA3119909A CA3119909A1 CA 3119909 A1 CA3119909 A1 CA 3119909A1 CA 3119909 A CA3119909 A CA 3119909A CA 3119909 A CA3119909 A CA 3119909A CA 3119909 A1 CA3119909 A1 CA 3119909A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- pharmaceutically acceptable
- diazaspiro
- pyrimidin
- acceptable salt
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 title claims abstract description 55
- 238000000034 method Methods 0.000 title claims abstract description 45
- 150000001875 compounds Chemical class 0.000 claims abstract description 59
- 150000003839 salts Chemical class 0.000 claims abstract description 23
- 239000003112 inhibitor Substances 0.000 claims abstract description 14
- TZSZZENYCISATO-WIOPSUGQSA-N rodatristat Chemical compound CCOC(=O)[C@@H]1CC2(CN1)CCN(CC2)c1cc(O[C@H](c2ccc(Cl)cc2-c2ccccc2)C(F)(F)F)nc(N)n1 TZSZZENYCISATO-WIOPSUGQSA-N 0.000 claims abstract description 14
- 239000000203 mixture Substances 0.000 claims description 20
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 14
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 8
- 101001074035 Homo sapiens Zinc finger protein GLI2 Proteins 0.000 claims description 7
- 102100035558 Zinc finger protein GLI2 Human genes 0.000 claims description 7
- 239000004305 biphenyl Substances 0.000 claims description 5
- 239000000843 powder Substances 0.000 claims description 4
- 239000003826 tablet Substances 0.000 claims description 4
- 239000002775 capsule Substances 0.000 claims description 3
- 239000008187 granular material Substances 0.000 claims description 3
- 239000007788 liquid Substances 0.000 claims description 3
- 239000002552 dosage form Substances 0.000 claims description 2
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 101000830742 Homo sapiens Tryptophan 5-hydroxylase 1 Proteins 0.000 abstract description 12
- 102100024971 Tryptophan 5-hydroxylase 1 Human genes 0.000 abstract description 12
- ZNSPHKJFQDEABI-NZQKXSOJSA-N Nc1nc(O[C@H](c2ccc(Cl)cc2-c2ccccc2)C(F)(F)F)cc(n1)N1CCC2(CN[C@@H](C2)C(O)=O)CC1 Chemical compound Nc1nc(O[C@H](c2ccc(Cl)cc2-c2ccccc2)C(F)(F)F)cc(n1)N1CCC2(CN[C@@H](C2)C(O)=O)CC1 ZNSPHKJFQDEABI-NZQKXSOJSA-N 0.000 abstract description 5
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 44
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 20
- 201000010099 disease Diseases 0.000 description 12
- 229940076279 serotonin Drugs 0.000 description 12
- -1 RVT-1201 compound Chemical class 0.000 description 8
- 208000035475 disorder Diseases 0.000 description 8
- DUUGKQCEGZLZNO-UHFFFAOYSA-N 5-hydroxyindoleacetic acid Chemical compound C1=C(O)C=C2C(CC(=O)O)=CNC2=C1 DUUGKQCEGZLZNO-UHFFFAOYSA-N 0.000 description 6
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical group COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 description 6
- 230000007170 pathology Effects 0.000 description 6
- 241000282412 Homo Species 0.000 description 5
- 241000700159 Rattus Species 0.000 description 5
- 230000015572 biosynthetic process Effects 0.000 description 5
- 208000019693 Lung disease Diseases 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 4
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 description 4
- 238000000605 extraction Methods 0.000 description 4
- 230000002401 inhibitory effect Effects 0.000 description 4
- 210000004072 lung Anatomy 0.000 description 4
- 230000002093 peripheral effect Effects 0.000 description 4
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- 241000282414 Homo sapiens Species 0.000 description 3
- 208000014777 Pulmonary venoocclusive disease Diseases 0.000 description 3
- 108010031944 Tryptophan Hydroxylase Proteins 0.000 description 3
- 102000005506 Tryptophan Hydroxylase Human genes 0.000 description 3
- 210000004027 cell Anatomy 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 210000001035 gastrointestinal tract Anatomy 0.000 description 3
- 239000008297 liquid dosage form Substances 0.000 description 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 3
- 239000006186 oral dosage form Substances 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 230000002265 prevention Effects 0.000 description 3
- 239000007909 solid dosage form Substances 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 239000003981 vehicle Substances 0.000 description 3
- HNXQXTQTPAJEJL-UHFFFAOYSA-N 2-aminopteridin-4-ol Chemical compound C1=CN=C2NC(N)=NC(=O)C2=N1 HNXQXTQTPAJEJL-UHFFFAOYSA-N 0.000 description 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- 102000003823 Aromatic-L-amino-acid decarboxylases Human genes 0.000 description 2
- 108090000121 Aromatic-L-amino-acid decarboxylases Proteins 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 208000031886 HIV Infections Diseases 0.000 description 2
- 208000037357 HIV infectious disease Diseases 0.000 description 2
- 101000892398 Homo sapiens Tryptophan 2,3-dioxygenase Proteins 0.000 description 2
- 101000851865 Homo sapiens Tryptophan 5-hydroxylase 2 Proteins 0.000 description 2
- 206010020772 Hypertension Diseases 0.000 description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- OFBQJSOFQDEBGM-UHFFFAOYSA-N Pentane Chemical compound CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 description 2
- 108010069013 Phenylalanine Hydroxylase Proteins 0.000 description 2
- 102100038223 Phenylalanine-4-hydroxylase Human genes 0.000 description 2
- 206010039710 Scleroderma Diseases 0.000 description 2
- 102100036474 Tryptophan 5-hydroxylase 2 Human genes 0.000 description 2
- 229940127410 Tryptophan Hydroxylase Inhibitors Drugs 0.000 description 2
- 108091000117 Tyrosine 3-Monooxygenase Proteins 0.000 description 2
- 102000048218 Tyrosine 3-monooxygenases Human genes 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 150000001298 alcohols Chemical class 0.000 description 2
- 239000000090 biomarker Substances 0.000 description 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 210000002569 neuron Anatomy 0.000 description 2
- 238000007911 parenteral administration Methods 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 208000002815 pulmonary hypertension Diseases 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- FNKQXYHWGSIFBK-RPDRRWSUSA-N sapropterin Chemical compound N1=C(N)NC(=O)C2=C1NC[C@H]([C@@H](O)[C@@H](O)C)N2 FNKQXYHWGSIFBK-RPDRRWSUSA-N 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 238000007910 systemic administration Methods 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 230000003442 weekly effect Effects 0.000 description 2
- DJHVIWBKTVKTFY-JTQLQIEISA-N (2s)-2-(ethynylamino)-3-phenylpropanoic acid Chemical compound C#CN[C@H](C(=O)O)CC1=CC=CC=C1 DJHVIWBKTVKTFY-JTQLQIEISA-N 0.000 description 1
- LDCYZAJDBXYCGN-VIFPVBQESA-N 5-hydroxy-L-tryptophan Chemical compound C1=C(O)C=C2C(C[C@H](N)C(O)=O)=CNC2=C1 LDCYZAJDBXYCGN-VIFPVBQESA-N 0.000 description 1
- 229940000681 5-hydroxytryptophan Drugs 0.000 description 1
- 102000000632 Aromatic amino acid hydroxylases Human genes 0.000 description 1
- 108050008079 Aromatic amino acid hydroxylases Proteins 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 1
- 208000029147 Collagen-vascular disease Diseases 0.000 description 1
- 208000002330 Congenital Heart Defects Diseases 0.000 description 1
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 description 1
- 241000283086 Equidae Species 0.000 description 1
- 241000282326 Felis catus Species 0.000 description 1
- NIGWMJHCCYYCSF-UHFFFAOYSA-N Fenclonine Chemical compound OC(=O)C(N)CC1=CC=C(Cl)C=C1 NIGWMJHCCYYCSF-UHFFFAOYSA-N 0.000 description 1
- 208000018522 Gastrointestinal disease Diseases 0.000 description 1
- 208000015872 Gaucher disease Diseases 0.000 description 1
- 208000031953 Hereditary hemorrhagic telangiectasia Diseases 0.000 description 1
- 101000631929 Homo sapiens Sodium-dependent serotonin transporter Proteins 0.000 description 1
- 206010021143 Hypoxia Diseases 0.000 description 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 description 1
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 208000014767 Myeloproliferative disease Diseases 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 241001494479 Pecora Species 0.000 description 1
- 241000288906 Primates Species 0.000 description 1
- 102000001708 Protein Isoforms Human genes 0.000 description 1
- 108010029485 Protein Isoforms Proteins 0.000 description 1
- 208000031467 Pulmonary capillary hemangiomatosis Diseases 0.000 description 1
- 241000283984 Rodentia Species 0.000 description 1
- 102100028874 Sodium-dependent serotonin transporter Human genes 0.000 description 1
- 241000282898 Sus scrofa Species 0.000 description 1
- 208000024799 Thyroid disease Diseases 0.000 description 1
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 description 1
- 229940116984 Tryptophan 5 hydroxylase inhibitor Drugs 0.000 description 1
- 108090000885 Tryptophan 5-monooxygenases Proteins 0.000 description 1
- 102000004271 Tryptophan 5-monooxygenases Human genes 0.000 description 1
- 241000251539 Vertebrata <Metazoa> Species 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 239000002830 appetite depressant Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 238000004166 bioassay Methods 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 210000000038 chest Anatomy 0.000 description 1
- 208000019902 chronic diarrheal disease Diseases 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 229960003920 cocaine Drugs 0.000 description 1
- 239000007891 compressed tablet Substances 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 229940124301 concurrent medication Drugs 0.000 description 1
- 208000028831 congenital heart disease Diseases 0.000 description 1
- 210000002808 connective tissue Anatomy 0.000 description 1
- 208000018631 connective tissue disease Diseases 0.000 description 1
- 230000002596 correlated effect Effects 0.000 description 1
- 230000000875 corresponding effect Effects 0.000 description 1
- QPNKYNYIKKVVQB-UHFFFAOYSA-N crotaleschenine Natural products O1C(=O)C(C)C(C)C(C)(O)C(=O)OCC2=CCN3C2C1CC3 QPNKYNYIKKVVQB-UHFFFAOYSA-N 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 229910001882 dioxygen Inorganic materials 0.000 description 1
- 208000037765 diseases and disorders Diseases 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 231100000371 dose-limiting toxicity Toxicity 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000003974 emollient agent Substances 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 239000002702 enteric coating Substances 0.000 description 1
- 238000009505 enteric coating Methods 0.000 description 1
- 150000002170 ethers Chemical class 0.000 description 1
- 238000013265 extended release Methods 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000005176 gastrointestinal motility Effects 0.000 description 1
- 208000007345 glycogen storage disease Diseases 0.000 description 1
- 230000033444 hydroxylation Effects 0.000 description 1
- 238000005805 hydroxylation reaction Methods 0.000 description 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 1
- 239000003701 inert diluent Substances 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 206010025135 lupus erythematosus Diseases 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 239000004530 micro-emulsion Substances 0.000 description 1
- QVCMHGGNRFRMAD-XFGHUUIASA-N monocrotaline Chemical compound C1OC(=O)[C@](C)(O)[C@@](O)(C)[C@@H](C)C(=O)O[C@@H]2CCN3[C@@H]2C1=CC3 QVCMHGGNRFRMAD-XFGHUUIASA-N 0.000 description 1
- QVCMHGGNRFRMAD-UHFFFAOYSA-N monocrotaline Natural products C1OC(=O)C(C)(O)C(O)(C)C(C)C(=O)OC2CCN3C2C1=CC3 QVCMHGGNRFRMAD-UHFFFAOYSA-N 0.000 description 1
- 230000004899 motility Effects 0.000 description 1
- 238000000465 moulding Methods 0.000 description 1
- 210000003249 myenteric plexus Anatomy 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 239000002858 neurotransmitter agent Substances 0.000 description 1
- 239000012457 nonaqueous media Substances 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- LDCYZAJDBXYCGN-UHFFFAOYSA-N oxitriptan Natural products C1=C(O)C=C2C(CC(N)C(O)=O)=CNC2=C1 LDCYZAJDBXYCGN-UHFFFAOYSA-N 0.000 description 1
- 230000008506 pathogenesis Effects 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 239000008177 pharmaceutical agent Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 210000004560 pineal gland Anatomy 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 208000007232 portal hypertension Diseases 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 230000008433 psychological processes and functions Effects 0.000 description 1
- 210000003492 pulmonary vein Anatomy 0.000 description 1
- 238000011552 rat model Methods 0.000 description 1
- 238000009790 rate-determining step (RDS) Methods 0.000 description 1
- JWEQRJSCTFBRSI-PCLIKHOPSA-N rboxylate Chemical compound COC(=O)C1C(N2C3=O)C4=CC=CC=C4OC1(C)N=C2S\C3=C\C(C=1)=CC=C(OC)C=1COC1=CC=CC=C1C JWEQRJSCTFBRSI-PCLIKHOPSA-N 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 239000003352 sequestering agent Substances 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000010911 splenectomy Methods 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000002485 urinary effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862768575P | 2018-11-16 | 2018-11-16 | |
| US62/768,575 | 2018-11-16 | ||
| PCT/IB2019/001224 WO2020099926A1 (en) | 2018-11-16 | 2019-11-15 | A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3119909A1 true CA3119909A1 (en) | 2020-05-22 |
Family
ID=69182543
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3119909A Pending CA3119909A1 (en) | 2018-11-16 | 2019-11-15 | A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US11413287B2 (https=) |
| EP (1) | EP3880203A1 (https=) |
| JP (2) | JP2022507533A (https=) |
| KR (1) | KR20210105343A (https=) |
| CN (1) | CN113242736A (https=) |
| AU (1) | AU2019382168A1 (https=) |
| CA (1) | CA3119909A1 (https=) |
| WO (1) | WO2020099926A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11413287B2 (en) | 2018-11-16 | 2022-08-16 | Altavant Sciences Gmbh | Method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension |
| WO2020128614A1 (en) * | 2018-12-17 | 2020-06-25 | Altavant Sciences Gmbh | Method for treating interstital lung disease |
| MX2021009055A (es) | 2019-01-30 | 2021-10-22 | Altavant Sciences Gmbh | Pauta posológica y método para tratar la hipertensión arterial pulmonar con rodatristat etilo. |
| AU2020244278A1 (en) * | 2019-03-15 | 2021-09-30 | Altavant Sciences Gmbh | A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension and daily dosing |
| WO2023062595A1 (en) * | 2021-10-14 | 2023-04-20 | Altavant Sciences Gmbh | Treatment of subjects having pulmonary arterial hypertension with rodatristat ethyl |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7875622B2 (en) | 2007-07-11 | 2011-01-25 | Lexicon Pharmaceuticals, Inc. | Methods and compositions for treating pulmonary hypertension and related diseases and disorders |
| TW201245183A (en) * | 2010-11-05 | 2012-11-16 | Lexicon Pharmaceuticals Inc | Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid |
| UA119247C2 (uk) * | 2013-09-06 | 2019-05-27 | РОЙВЕНТ САЙЕНСИЗ ҐмбГ | Спіроциклічні сполуки як інгібітори триптофангідроксилази |
| US9399741B2 (en) | 2013-10-09 | 2016-07-26 | Uop Llc | Methods and apparatuses for desulfurizing hydrocarbon streams |
| CA3119912A1 (en) * | 2018-11-14 | 2020-05-22 | Altavant Sciences Gmbh | A crystalline spirocyclic compound inhibitor of tryptophan hydroxylase 1 (tph1) for treating diseases or disorders associated with peripheral serotonin |
| US11413287B2 (en) | 2018-11-16 | 2022-08-16 | Altavant Sciences Gmbh | Method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension |
| WO2020128614A1 (en) * | 2018-12-17 | 2020-06-25 | Altavant Sciences Gmbh | Method for treating interstital lung disease |
| WO2020128608A1 (en) | 2018-12-17 | 2020-06-25 | Altavant Sciences Gmbh | Compound for use in a method for treating sarcoidosis-associated pulmonary hypertension |
| MX2021009055A (es) * | 2019-01-30 | 2021-10-22 | Altavant Sciences Gmbh | Pauta posológica y método para tratar la hipertensión arterial pulmonar con rodatristat etilo. |
| AU2020244278A1 (en) | 2019-03-15 | 2021-09-30 | Altavant Sciences Gmbh | A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension and daily dosing |
| CN115379825A (zh) | 2020-01-31 | 2022-11-22 | 阿尔塔万特科学公司 | 用rodatristat治疗肺动脉高压的剂量和方法 |
| US11937070B2 (en) | 2021-07-01 | 2024-03-19 | Tencent America LLC | Layered description of space of interest |
| WO2023079486A1 (en) | 2021-11-03 | 2023-05-11 | Altavant Sciences Gmbh | Treatment of pulmonary arterial hypertension with rodatristat and ambrisentan |
-
2019
- 2019-11-15 US US16/685,165 patent/US11413287B2/en active Active
- 2019-11-15 CN CN201980083698.9A patent/CN113242736A/zh not_active Withdrawn
- 2019-11-15 AU AU2019382168A patent/AU2019382168A1/en not_active Abandoned
- 2019-11-15 WO PCT/IB2019/001224 patent/WO2020099926A1/en not_active Ceased
- 2019-11-15 KR KR1020217016464A patent/KR20210105343A/ko not_active Ceased
- 2019-11-15 CA CA3119909A patent/CA3119909A1/en active Pending
- 2019-11-15 EP EP19839404.1A patent/EP3880203A1/en not_active Withdrawn
- 2019-11-15 JP JP2021526561A patent/JP2022507533A/ja active Pending
-
2022
- 2022-07-18 US US17/813,173 patent/US11911382B2/en active Active
-
2023
- 2023-12-25 JP JP2023217954A patent/JP2024019691A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US11911382B2 (en) | 2024-02-27 |
| US20230000866A1 (en) | 2023-01-05 |
| AU2019382168A1 (en) | 2021-06-03 |
| CN113242736A (zh) | 2021-08-10 |
| JP2022507533A (ja) | 2022-01-18 |
| US11413287B2 (en) | 2022-08-16 |
| KR20210105343A (ko) | 2021-08-26 |
| WO2020099926A1 (en) | 2020-05-22 |
| JP2024019691A (ja) | 2024-02-09 |
| US20200155552A1 (en) | 2020-05-21 |
| EP3880203A1 (en) | 2021-09-22 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US11911382B2 (en) | Method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension | |
| US20240024316A1 (en) | Method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension and daily dosing | |
| US20220096475A1 (en) | Method for treating sarcoidosis-associated pulmonary hypertension | |
| JPH01294688A (ja) | パーキンソン症候群の治療用医薬、およびその製造方法 | |
| RS65874B1 (sr) | Primena sepiapterina bez hrane za upotrebu u postupku za povećanje izloženosti plazme sepiapterinu | |
| WO2007149283B1 (en) | Use of kw-3902 for achieving diuresis in patients with congestive heart failure and acute fluid overload | |
| EP3917531A1 (en) | A dosage regime and method for treating pulmonary arterial hypertension with rodatristat ethyl | |
| US20210128593A1 (en) | Synergistic nutritional neuroprotective compositions for ameliorating neural dysfunction | |
| US9642860B2 (en) | Combinations of corroles and statins | |
| EP4045058A1 (fr) | Utilisation de nictotinamide mononucléotide (nmn) pour la prevention et/ou le traitement de la polyarthrite rhumatoïde et compositions correspondantes | |
| US20200188399A1 (en) | Method for treating interstitial lung disease | |
| JPS61286326A (ja) | パ−キンソン病治療薬 | |
| KR20150043288A (ko) | 운동 뉴런의 자가 포식 작용 억제를 위한 약학적 조성물 및 이의 용도 | |
| KR100725263B1 (ko) | ＨＭＧ-ＣｏＡ 리덕타제 억제제 및 카르니틴을 포함하는 항지질혈성 복합제 | |
| HK40058221A (en) | A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension | |
| HK40065546A (en) | A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension and daily dosing | |
| CN118871096A (zh) | 包含l-色氨酸、l-5-羟基色氨酸和外周降解抑制剂的药物组合物和药物 | |
| KR20180010475A (ko) | Trpc3의 억제제를 유효성분으로 포함하는 가려움증 치료용 약제학적 조성물 | |
| CN117243947A (zh) | 瑞香素及包含其的组合在制备糖尿病并发症药物中的应用 | |
| CA2554045A1 (en) | Method for treating erectile dysfunction | |
| Hanna | Experimental study of new 3-(2-R1-6-R2-4-oxyquinoline-3 (4H)-yl) alkyl (alkaryl-, aryl) carboxylic acid derivative (PC-66 compound) | |
| JP2000327571A (ja) | 抗かゆみ組成物 | |
| DE102004040630A1 (de) | Kombinationstherapie mit Procain |