HRP20100633T1 - Derivati piridazinona kao agonisti receptora tiroidnih hormona - Google Patents
Derivati piridazinona kao agonisti receptora tiroidnih hormona Download PDFInfo
- Publication number
- HRP20100633T1 HRP20100633T1 HR20100633T HRP20100633T HRP20100633T1 HR P20100633 T1 HRP20100633 T1 HR P20100633T1 HR 20100633 T HR20100633 T HR 20100633T HR P20100633 T HRP20100633 T HR P20100633T HR P20100633 T1 HRP20100633 T1 HR P20100633T1
- Authority
- HR
- Croatia
- Prior art keywords
- dihydro
- oxo
- isopropyl
- phenyl
- pyridazin
- Prior art date
Links
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical class OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 title 1
- 229940127535 Thyroid Hormone Receptor Agonists Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 27
- 125000000217 alkyl group Chemical group 0.000 claims abstract 12
- 150000002148 esters Chemical class 0.000 claims abstract 10
- 150000003839 salts Chemical class 0.000 claims abstract 9
- 125000004122 cyclic group Chemical group 0.000 claims abstract 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims abstract 4
- 125000001183 hydrocarbyl group Chemical group 0.000 claims abstract 2
- 229920006395 saturated elastomer Polymers 0.000 claims abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- -1 Ester compound Chemical class 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000004185 ester group Chemical group 0.000 claims 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 238000011321 prophylaxis Methods 0.000 claims 2
- GPQLQJCVSFKHSX-UHFFFAOYSA-N 2-[3,5-dibromo-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)methyl]phenyl]acetic acid Chemical compound N1C(=O)C(C(C)C)=CC(CC=2C(=CC(CC(O)=O)=CC=2Br)Br)=N1 GPQLQJCVSFKHSX-UHFFFAOYSA-N 0.000 claims 1
- AOXRZYHUTQBXCN-UHFFFAOYSA-N 2-[3,5-dibromo-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)oxy]phenyl]acetic acid Chemical compound N1C(=O)C(C(C)C)=CC(OC=2C(=CC(CC(O)=O)=CC=2Br)Br)=N1 AOXRZYHUTQBXCN-UHFFFAOYSA-N 0.000 claims 1
- JFIWDBBXUIEFQL-UHFFFAOYSA-N 2-[3,5-dichloro-4-(1-methyl-6-oxo-5-propan-2-ylpyridazin-3-yl)oxyphenyl]-3,5-dioxo-1,2,4-triazine-6-carbonitrile Chemical compound CN1C(=O)C(C(C)C)=CC(OC=2C(=CC(=CC=2Cl)N2C(NC(=O)C(C#N)=N2)=O)Cl)=N1 JFIWDBBXUIEFQL-UHFFFAOYSA-N 0.000 claims 1
- OORLQBMJWSBLOY-UHFFFAOYSA-N 2-[3,5-dichloro-4-(1-methyl-6-oxo-5-propan-2-ylpyridazin-3-yl)oxyphenyl]acetic acid Chemical compound CN1C(=O)C(C(C)C)=CC(OC=2C(=CC(CC(O)=O)=CC=2Cl)Cl)=N1 OORLQBMJWSBLOY-UHFFFAOYSA-N 0.000 claims 1
- LWMPMTQXFCDBBA-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(1-methyl-6-oxo-5-propan-2-ylpyridazin-3-yl)methyl]phenyl]-3,5-dioxo-1,2,4-triazine-6-carbonitrile Chemical compound CN1C(=O)C(C(C)C)=CC(CC=2C(=CC(=CC=2Cl)N2C(NC(=O)C(C#N)=N2)=O)Cl)=N1 LWMPMTQXFCDBBA-UHFFFAOYSA-N 0.000 claims 1
- VNNFGQVGJFFVJX-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)methyl]phenyl]-1,2,4-triazine-3,5-dione Chemical compound N1C(=O)C(C(C)C)=CC(CC=2C(=CC(=CC=2Cl)N2C(NC(=O)C=N2)=O)Cl)=N1 VNNFGQVGJFFVJX-UHFFFAOYSA-N 0.000 claims 1
- ZKWUUZVSYHNCBF-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)methyl]phenyl]-3,5-dioxo-1,2,4-triazine-6-carbonitrile Chemical compound N1C(=O)C(C(C)C)=CC(CC=2C(=CC(=CC=2Cl)N2C(NC(=O)C(C#N)=N2)=O)Cl)=N1 ZKWUUZVSYHNCBF-UHFFFAOYSA-N 0.000 claims 1
- HNQWGSLKZWUEDQ-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)methyl]phenyl]acetic acid Chemical compound N1C(=O)C(C(C)C)=CC(CC=2C(=CC(CC(O)=O)=CC=2Cl)Cl)=N1 HNQWGSLKZWUEDQ-UHFFFAOYSA-N 0.000 claims 1
- BDVULFJNTQUGRM-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)oxy]anilino]acetic acid Chemical compound N1C(=O)C(C(C)C)=CC(OC=2C(=CC(NCC(O)=O)=CC=2Cl)Cl)=N1 BDVULFJNTQUGRM-UHFFFAOYSA-N 0.000 claims 1
- GBAQQDSIAACDRK-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)oxy]phenyl]-1,2,4-triazine-3,5-dione Chemical compound N1C(=O)C(C(C)C)=CC(OC=2C(=CC(=CC=2Cl)N2C(NC(=O)C=N2)=O)Cl)=N1 GBAQQDSIAACDRK-UHFFFAOYSA-N 0.000 claims 1
- UCWVDJLQXJXVEB-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)oxy]phenyl]acetic acid Chemical compound N1C(=O)C(C(C)C)=CC(OC=2C(=CC(CC(O)=O)=CC=2Cl)Cl)=N1 UCWVDJLQXJXVEB-UHFFFAOYSA-N 0.000 claims 1
- URNDNHCCRPRCLG-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)sulfanyl]phenyl]acetic acid Chemical compound N1C(=O)C(C(C)C)=CC(SC=2C(=CC(CC(O)=O)=CC=2Cl)Cl)=N1 URNDNHCCRPRCLG-UHFFFAOYSA-N 0.000 claims 1
- YNXHQQAZZSIQKZ-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)sulfinyl]phenyl]acetic acid Chemical compound N1C(=O)C(C(C)C)=CC(S(=O)C=2C(=CC(CC(O)=O)=CC=2Cl)Cl)=N1 YNXHQQAZZSIQKZ-UHFFFAOYSA-N 0.000 claims 1
- FLCRQFBWKJIFKP-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)sulfonyl]phenyl]-1,2,4-triazine-3,5-dione Chemical compound N1C(=O)C(C(C)C)=CC(S(=O)(=O)C=2C(=CC(=CC=2Cl)N2C(NC(=O)C=N2)=O)Cl)=N1 FLCRQFBWKJIFKP-UHFFFAOYSA-N 0.000 claims 1
- ABJHNUXWNJQNQT-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)sulfonyl]phenyl]-3,5-dioxo-1,2,4-triazine-6-carbonitrile Chemical compound N1C(=O)C(C(C)C)=CC(S(=O)(=O)C=2C(=CC(=CC=2Cl)N2C(NC(=O)C(C#N)=N2)=O)Cl)=N1 ABJHNUXWNJQNQT-UHFFFAOYSA-N 0.000 claims 1
- LLSSPNCWDDLGHB-UHFFFAOYSA-N 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)sulfonyl]phenyl]acetic acid Chemical compound N1C(=O)C(C(C)C)=CC(S(=O)(=O)C=2C(=CC(CC(O)=O)=CC=2Cl)Cl)=N1 LLSSPNCWDDLGHB-UHFFFAOYSA-N 0.000 claims 1
- WGHVGSIKRBXLGK-UHFFFAOYSA-N 2-[3,5-dimethyl-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)oxy]phenyl]acetic acid Chemical compound N1C(=O)C(C(C)C)=CC(OC=2C(=CC(CC(O)=O)=CC=2C)C)=N1 WGHVGSIKRBXLGK-UHFFFAOYSA-N 0.000 claims 1
- CHELBMWLOMFCBW-UHFFFAOYSA-N 2-[3-chloro-5-methyl-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)oxy]phenyl]acetic acid Chemical compound N1C(=O)C(C(C)C)=CC(OC=2C(=CC(CC(O)=O)=CC=2C)Cl)=N1 CHELBMWLOMFCBW-UHFFFAOYSA-N 0.000 claims 1
- HKODZJFSSDWZGY-UHFFFAOYSA-N 3-[3,5-dibromo-4-[(6-oxo-5-propan-2-yl-1h-pyridazin-3-yl)oxy]phenyl]propanoic acid Chemical compound N1C(=O)C(C(C)C)=CC(OC=2C(=CC(CCC(O)=O)=CC=2Br)Br)=N1 HKODZJFSSDWZGY-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- AUYYCJSJGJYCDS-LBPRGKRZSA-N Thyrolar Chemical class IC1=CC(C[C@H](N)C(O)=O)=CC(I)=C1OC1=CC=C(O)C(I)=C1 AUYYCJSJGJYCDS-LBPRGKRZSA-N 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000003532 hypothyroidism Diseases 0.000 claims 1
- 230000002989 hypothyroidism Effects 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- MUBZPKHOEPUJKR-UHFFFAOYSA-N oxalic acid Substances OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- FDBYIYFVSAHJLY-UHFFFAOYSA-N resmetirom Chemical compound N1C(=O)C(C(C)C)=CC(OC=2C(=CC(=CC=2Cl)N2C(NC(=O)C(C#N)=N2)=O)Cl)=N1 FDBYIYFVSAHJLY-UHFFFAOYSA-N 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/14—Oxygen atoms
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
- A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
-
- 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
- A61P9/10—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
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/14—Oxygen atoms
- C07D237/16—Two oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/18—Sulfur atoms
-
- 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
- C07D403/10—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 linked by a carbon chain containing aromatic rings
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US70121505P | 2005-07-21 | 2005-07-21 | |
PCT/EP2006/064093 WO2007009913A1 (en) | 2005-07-21 | 2006-07-11 | Pyridazinone derivatives as thyroid hormone receptor agonists |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20100633T1 true HRP20100633T1 (hr) | 2011-01-31 |
Family
ID=37114368
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20100633T HRP20100633T1 (hr) | 2005-07-21 | 2010-11-23 | Derivati piridazinona kao agonisti receptora tiroidnih hormona |
Country Status (32)
Country | Link |
---|---|
US (3) | US7452882B2 (ja) |
EP (1) | EP1919878B1 (ja) |
JP (1) | JP5000649B2 (ja) |
KR (1) | KR100965006B1 (ja) |
CN (1) | CN101228135B (ja) |
AR (1) | AR054848A1 (ja) |
AT (1) | ATE480524T1 (ja) |
AU (1) | AU2006271721C1 (ja) |
BR (1) | BRPI0613754B8 (ja) |
CA (1) | CA2614529C (ja) |
CR (1) | CR9644A (ja) |
CY (1) | CY1110929T1 (ja) |
DE (1) | DE602006016821D1 (ja) |
DK (1) | DK1919878T3 (ja) |
EC (1) | ECSP088120A (ja) |
ES (1) | ES2349131T3 (ja) |
HK (1) | HK1115129A1 (ja) |
HR (1) | HRP20100633T1 (ja) |
IL (1) | IL188476A (ja) |
MA (1) | MA29731B1 (ja) |
MX (1) | MX2008000818A (ja) |
MY (1) | MY142861A (ja) |
NO (1) | NO340679B1 (ja) |
NZ (1) | NZ565190A (ja) |
PL (1) | PL1919878T3 (ja) |
PT (1) | PT1919878E (ja) |
RS (1) | RS51639B (ja) |
RU (1) | RU2379295C2 (ja) |
TW (1) | TWI330636B (ja) |
UA (1) | UA88104C2 (ja) |
WO (1) | WO2007009913A1 (ja) |
ZA (1) | ZA200800405B (ja) |
Families Citing this family (71)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2422450C2 (ru) | 2003-11-19 | 2011-06-27 | Метабазис Терапеутикс, Инк. | Новые фосфорсодержащие тиромиметики |
EP1604988A1 (en) * | 2004-05-18 | 2005-12-14 | Sanofi-Aventis Deutschland GmbH | Pyridazinone derivatives, methods for producing them and their use as pharmaceuticals |
EP1898926A2 (en) | 2005-05-26 | 2008-03-19 | Metabasis Therapeutics, Inc. | Thyromimetics for the treatment of fatty liver diseases |
WO2007009913A1 (en) | 2005-07-21 | 2007-01-25 | F. Hoffmann-La Roche Ag | Pyridazinone derivatives as thyroid hormone receptor agonists |
GB0610680D0 (en) * | 2006-05-31 | 2006-07-12 | Istituto Di Ricerche D Biolog | Therapeutic compounds |
KR20090047458A (ko) | 2006-08-08 | 2009-05-12 | 사노피-아벤티스 | 아릴아미노아릴-알킬-치환된 이미다졸리딘-2,4-디온, 이의 제조방법, 이들 화합물을 포함하는 약제 및 이의 용도 |
WO2008133141A1 (ja) * | 2007-04-24 | 2008-11-06 | Toyo Boseki Kabushiki Kaisha | オスモチン組換えタンパク質およびその製造方法、並びにその利用 |
NZ582273A (en) * | 2007-06-06 | 2011-06-30 | Torrent Pharmaceuticals Ltd | Thyroid like compounds |
US8076334B2 (en) * | 2007-09-20 | 2011-12-13 | Hoffmann-La Roche Inc. | Prodrugs of thyroid hormone analogs |
NZ585395A (en) | 2007-11-15 | 2012-03-30 | Angeletti P Ist Richerche Bio | Pyridazinone derivatives as parp inhibitors |
KR100981781B1 (ko) | 2008-02-29 | 2010-09-10 | 재단법인 한국원자력의학원 | 방사선 치료용 콜리메이터 장치 및 그 장치를 이용한방사선 치료장치 |
AR072707A1 (es) | 2008-07-09 | 2010-09-15 | Sanofi Aventis | Compuestos heterociclicos, procesos para su preparacion, medicamentos que comprenden estos compuestos y el uso de los mismos |
WO2010068601A1 (en) | 2008-12-08 | 2010-06-17 | Sanofi-Aventis | A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof |
WO2010122980A1 (ja) | 2009-04-20 | 2010-10-28 | 田辺三菱製薬株式会社 | 新規甲状腺ホルモンβ受容体作動薬 |
WO2011023754A1 (en) | 2009-08-26 | 2011-03-03 | Sanofi-Aventis | Novel crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use |
JP5847533B2 (ja) * | 2010-10-19 | 2016-01-27 | 田辺三菱製薬株式会社 | 新規甲状腺ホルモンβ受容体作動薬 |
US8901114B2 (en) | 2011-03-08 | 2014-12-02 | Sanofi | Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof |
US8828994B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
EP2683700B1 (de) | 2011-03-08 | 2015-02-18 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
WO2012120055A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
US8828995B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
CA3111317C (en) * | 2012-09-17 | 2023-08-29 | F. Hoffmann-La Roche Ltd. | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
CN105272927A (zh) * | 2015-11-17 | 2016-01-27 | 华中药业股份有限公司 | 一种制备氯氮卓的新方法 |
EP4112056A1 (en) | 2016-10-18 | 2023-01-04 | Madrigal Pharmaceuticals, Inc. | Methods of treating liver disorders or lipid disorders with a thr-beta agonist |
AU2017363206A1 (en) | 2016-11-21 | 2019-06-13 | Viking Therapeutics, Inc. | Method of treating glycogen storage disease |
CA3064940A1 (en) | 2017-06-05 | 2018-12-13 | Viking Therapeutics, Inc. | Compositions for the treatment of fibrosis |
CN111094554A (zh) | 2017-09-14 | 2020-05-01 | 国立研究开发法人理化学研究所 | 视网膜组织的制备方法 |
US11485729B2 (en) | 2018-01-23 | 2022-11-01 | Shenzhen Targetrx, Inc. | Substituted pyridazinone compound |
EP3781126B1 (en) | 2018-04-16 | 2022-05-04 | Ioulia Tseti | A pharmaceutical dry powder composition for inhalation comprising a thyroid hormone |
AU2019287679B2 (en) * | 2018-06-12 | 2022-04-21 | Xizang Haisco Pharmaceutical Co., Ltd. | Thyroid hormone receptor agonists and uses thereof |
WO2019242766A1 (zh) * | 2018-06-22 | 2019-12-26 | 成都海创药业有限公司 | 氘代mgl-3196化合物及其用途 |
AR115666A1 (es) * | 2018-07-02 | 2021-02-10 | Madrigal Pharmaceuticals Inc | Formas sólidas de 2-(3,5-dicloro-4-((5-isopropil-6-oxo-1,6-dihidropiridazin-3-il)oxi)fenil)-3,5-dioxo-2,3,4,5-tetrahidro-1,2,4-triazin-6-carbonitrilo |
US10800767B2 (en) | 2018-08-24 | 2020-10-13 | Terns, Inc. | Thyroid hormone receptor beta agonist compounds |
MA53562A (fr) * | 2018-09-06 | 2021-07-14 | Galmed Res And Development Ltd | Polythérapie destinée au traitement d'une maladie hépatique |
US20210355110A1 (en) * | 2018-10-12 | 2021-11-18 | InventisBio Co., Ltd. | Thyroid hormone receptor agonists |
US11203587B2 (en) | 2018-10-12 | 2021-12-21 | Terns, Inc. | Thyroid hormone receptor beta agonist compounds |
CN111320609A (zh) | 2018-12-13 | 2020-06-23 | 拓臻股份有限公司 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
CN111592528A (zh) * | 2019-02-20 | 2020-08-28 | 苏州泽璟生物制药股份有限公司 | 氘代的哒嗪酮及其衍生物和药物组合物 |
CN113474335A (zh) * | 2019-02-21 | 2021-10-01 | 南京瑞捷医药科技有限公司 | 新型化合物及其作为甲状腺激素受体激动剂的用途 |
US20220170098A1 (en) | 2019-03-13 | 2022-06-02 | Sumitomo Dainippon Pharma Co., Ltd. | Method for Evaluating Quality of Transplant Neural Retina, and Transplant Neural Retina Sheet |
SG11202111552YA (en) * | 2019-05-08 | 2021-11-29 | Aligos Therapeutics Inc | MODULATORS OF THR-ß AND METHODS OF USE THEREOF |
WO2020228577A1 (zh) * | 2019-05-10 | 2020-11-19 | 深圳微芯生物科技股份有限公司 | 一种哒嗪酮衍生物及其应用 |
WO2020239076A1 (zh) * | 2019-05-29 | 2020-12-03 | 南京明德新药研发有限公司 | 作为甲状腺素受体-β激动剂的哒嗪酮类衍生物及其应用 |
WO2021032218A1 (zh) | 2019-08-19 | 2021-02-25 | 苏州闻天医药科技有限公司 | 一种并环THRβ受体激动剂化合物及其制备方法和用途 |
CN112409340B (zh) * | 2019-08-21 | 2022-03-18 | 海创药业股份有限公司 | 卤素取代的苯醚类化合物及其用途 |
WO2021041237A1 (en) | 2019-08-23 | 2021-03-04 | Terns, Inc. | Thyroid hormone receptor beta agonist compounds |
WO2021043185A1 (en) * | 2019-09-04 | 2021-03-11 | Sunshine Lake Pharma Co., Ltd. | A compound as a thyroid hormone beta receptor agonist and use thereof |
JP2022548250A (ja) * | 2019-09-12 | 2022-11-17 | ターンズ・ファーマシューティカルズ・インコーポレイテッド | 甲状腺ホルモン受容体ベータアゴニスト化合物 |
JP2022549009A (ja) * | 2019-09-24 | 2022-11-22 | ▲広▼▲東▼▲東▼▲陽▼光▲薬▼▲業▼有限公司 | 甲状腺ホルモンベータ受容体アゴニストとしての化合物及びその使用 |
CN112707892A (zh) * | 2019-10-24 | 2021-04-27 | 苏州泽璟生物制药股份有限公司 | 哒嗪酮或哒嗪类化合物及其衍生物和药物组合物 |
US20230089582A1 (en) * | 2019-11-26 | 2023-03-23 | Kpc Pharmaceuticals, Inc | 1,2,4-triazine-3,5-dione compound, preparation method therefor, and application thereof |
WO2021129465A1 (zh) * | 2019-12-26 | 2021-07-01 | 苏州科睿思制药有限公司 | 一种Resmetirom晶型及其制备方法和用途 |
MX2022008626A (es) | 2020-01-13 | 2022-08-22 | Eccogene Shanghai Co Ltd | Triazinonas sustituidas como agonistas del receptor de la hormona tiroidea. |
CN113278013B (zh) * | 2020-02-20 | 2022-09-23 | 昆药集团股份有限公司 | 2,6-二取代的1,2,4-三嗪-3,5-二酮化合物及其制备方法和应用 |
CN113698388B (zh) * | 2020-05-20 | 2022-11-22 | 江苏恒瑞医药股份有限公司 | 6-氧代-1,6-二氢吡啶类衍生物、其制备方法及其在医药上的应用 |
CN115768751A (zh) | 2020-06-02 | 2023-03-07 | 成都康弘药业集团股份有限公司 | 新型甲状腺激素β受体激动剂 |
CN116056709A (zh) * | 2020-08-27 | 2023-05-02 | 益方生物科技(上海)股份有限公司 | 哒嗪酮化合物 |
WO2022053028A1 (zh) * | 2020-09-10 | 2022-03-17 | 南京明德新药研发有限公司 | 1,2,4-三嗪-3,5(2h,4h)-二酮类化合物及其应用 |
KR20230066408A (ko) * | 2020-09-10 | 2023-05-15 | 크리스탈 파마슈티컬 (쑤저우) 씨오., 엘티디. | 레스메티롬의 결정형, 이의 제조 방법 및 이의 용도 |
CA3194226A1 (en) | 2020-09-11 | 2022-03-17 | Riken | Complex containing neural retina-containing cell aggregates and matrix, and method for manufacturing same |
US20230310614A1 (en) | 2020-09-11 | 2023-10-05 | Sumitomo Pharma Co., Ltd. | Medium for Tissue for Transplantation |
WO2022068915A1 (zh) * | 2020-09-30 | 2022-04-07 | 江苏恒瑞医药股份有限公司 | 6-氧代-1,6-二氢哒嗪类衍生物、其制备方法及其在医药上的应用 |
EP4204419A1 (en) | 2020-10-19 | 2023-07-05 | Teva Pharmaceuticals International GmbH | Solid state forms of resmetirom |
CN116723844A (zh) * | 2020-11-06 | 2023-09-08 | 阿利戈斯治疗公司 | 作为甲状腺激素受体β (TR-β)激动剂的双环哒嗪酮 |
CN112645936B (zh) | 2020-12-17 | 2022-03-01 | 山东第一医科大学(山东省医学科学院) | 取代的哒嗪酮类化合物及其用途 |
CN114685450A (zh) | 2020-12-30 | 2022-07-01 | 昆药集团股份有限公司 | 2-吡啶酮类衍生物及其制备方法和在医药上的应用 |
CN114907327A (zh) * | 2021-02-10 | 2022-08-16 | 杭州领业医药科技有限公司 | Resmetirom的晶型及其制备方法和用途 |
CN115073429A (zh) * | 2021-03-15 | 2022-09-20 | 昆药集团股份有限公司 | 一种1,2,4-三嗪-3,5-二酮类化合物的盐型、晶型及其制备方法 |
CA3238664A1 (en) | 2021-11-19 | 2023-05-25 | Riken | Production method for sheet-like retinal tissue |
WO2024084491A1 (en) * | 2022-10-21 | 2024-04-25 | Mehta Nilesh Vipinchandra | Process for synthesis of res metirom and its intermediates thereof |
CN115650928B (zh) * | 2022-12-28 | 2023-03-31 | 凯思凯旭(上海)医药科技有限公司 | 一种多环类甲状腺激素β受体激动剂及其用途 |
Family Cites Families (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4582842A (en) | 1981-02-25 | 1986-04-15 | Merck & Co., Inc. | Anti-asthmatic 6H-dibenz-[b,e] [1,4]oxathiepin derivatives, compositions, and method of use therefor |
GB8501372D0 (en) | 1985-01-18 | 1985-02-20 | Smith Kline French Lab | Chemical compounds |
US5284971A (en) * | 1992-07-16 | 1994-02-08 | Syntex (U.S.A.) Inc. | 4-(3-cyclohexyl-4-hydroxy or-methoxy phenylsulfonyl) 3,5 dibromo phenyl acetic thyromimetic cholesterol-lowering agents |
EP0728482A3 (en) | 1995-02-10 | 1999-10-20 | Smithkline Beecham Corporation | Use of hcp specific compounds to enhance erythropoiesis |
CA2222204C (en) | 1995-06-06 | 2002-02-19 | Pfizer Inc. | Process for converting 2,4-dichloropyridines into 2-aryloxy-4-chloropyridines |
AU6480796A (en) | 1995-06-30 | 1997-02-05 | Smithkline Beecham Corporation | Use of stat 6 sh2 domain specific compounds to treat allergic reactions |
US5883294A (en) | 1997-06-18 | 1999-03-16 | The Regeants Of The University Of California | Selective thyroid hormone analogs |
GB9713739D0 (en) * | 1997-06-27 | 1997-09-03 | Karobio Ab | Thyroid receptor ligands |
AR023659A1 (es) | 1998-09-18 | 2002-09-04 | Vertex Pharma | Un compuesto inhibidor de p38, una composicion farmaceutica que lo comprende y el uso de dicha composicion en el tratamiento y prevencion de estados patologicos |
WO2000051971A1 (en) * | 1999-03-01 | 2000-09-08 | Pfizer Products Inc. | Oxamic acids and derivatives as thyroid receptor ligands |
CA2433100A1 (en) * | 2000-12-27 | 2002-07-04 | Helmut Haning | Indole derivatives as ligands of thyroid receptors |
EP1358175A2 (en) * | 2001-02-08 | 2003-11-05 | Karo Bio Ab | Phenoxy substituted benzocondensed heteroaryl derivatives as thyroid receptor ligands |
ATE297902T1 (de) * | 2001-02-28 | 2005-07-15 | Pfizer Prod Inc | Sulfonyl-pyridazinon-derivate zur verwendung als aldose-reduktase-inhibitoren |
RU2422450C2 (ru) | 2003-11-19 | 2011-06-27 | Метабазис Терапеутикс, Инк. | Новые фосфорсодержащие тиромиметики |
WO2005090317A1 (en) * | 2004-03-23 | 2005-09-29 | F.Hoffmann-La Roche Ag | Non-nucleoside reverse transcriptase inhibitors |
WO2007009913A1 (en) | 2005-07-21 | 2007-01-25 | F. Hoffmann-La Roche Ag | Pyridazinone derivatives as thyroid hormone receptor agonists |
-
2006
- 2006-07-11 WO PCT/EP2006/064093 patent/WO2007009913A1/en active Application Filing
- 2006-07-11 ES ES06792493T patent/ES2349131T3/es active Active
- 2006-07-11 DE DE602006016821T patent/DE602006016821D1/de active Active
- 2006-07-11 JP JP2008521935A patent/JP5000649B2/ja active Active
- 2006-07-11 MX MX2008000818A patent/MX2008000818A/es active IP Right Grant
- 2006-07-11 PL PL06792493T patent/PL1919878T3/pl unknown
- 2006-07-11 DK DK06792493.6T patent/DK1919878T3/da active
- 2006-07-11 CN CN2006800267317A patent/CN101228135B/zh active Active
- 2006-07-11 EP EP06792493A patent/EP1919878B1/en active Active
- 2006-07-11 AU AU2006271721A patent/AU2006271721C1/en active Active
- 2006-07-11 CA CA2614529A patent/CA2614529C/en active Active
- 2006-07-11 RS RS20100527A patent/RS51639B/en unknown
- 2006-07-11 PT PT06792493T patent/PT1919878E/pt unknown
- 2006-07-11 BR BRPI0613754A patent/BRPI0613754B8/pt active IP Right Grant
- 2006-07-11 KR KR1020087001480A patent/KR100965006B1/ko active IP Right Grant
- 2006-07-11 NZ NZ565190A patent/NZ565190A/en unknown
- 2006-07-11 AT AT06792493T patent/ATE480524T1/de active
- 2006-07-11 RU RU2008106058/04A patent/RU2379295C2/ru active
- 2006-07-18 TW TW095126242A patent/TWI330636B/zh active
- 2006-07-18 US US11/488,870 patent/US7452882B2/en active Active
- 2006-07-19 AR ARP060103084A patent/AR054848A1/es active IP Right Grant
- 2006-07-19 MY MYPI20063456A patent/MY142861A/en unknown
- 2006-11-07 UA UAA200801933A patent/UA88104C2/ru unknown
-
2007
- 2007-12-27 IL IL188476A patent/IL188476A/en active IP Right Grant
-
2008
- 2008-01-04 NO NO20080058A patent/NO340679B1/no unknown
- 2008-01-08 CR CR9644A patent/CR9644A/es unknown
- 2008-01-14 ZA ZA2008/00405A patent/ZA200800405B/en unknown
- 2008-01-18 EC EC2008008120A patent/ECSP088120A/es unknown
- 2008-02-01 MA MA30618A patent/MA29731B1/fr unknown
- 2008-08-20 US US12/194,643 patent/US7807674B2/en active Active
- 2008-09-17 HK HK08110278.4A patent/HK1115129A1/xx unknown
-
2010
- 2010-11-22 CY CY20101101049T patent/CY1110929T1/el unknown
- 2010-11-23 HR HR20100633T patent/HRP20100633T1/hr unknown
-
2015
- 2015-07-01 US US14/788,921 patent/USRE46024E1/en active Active
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20100633T1 (hr) | Derivati piridazinona kao agonisti receptora tiroidnih hormona | |
AU2014294997B2 (en) | Glyoxamide substituted pyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis B | |
RU2306309C2 (ru) | Производное 8-азапростагландина, фармацевтическая композиция, агент для профилактики заболеваний | |
US7858650B2 (en) | Medicinal composition for inhalation | |
RU2008127312A (ru) | Мезилатное пролекарство леводопы, его композиции и применение | |
NO20111765L (no) | Legemidler for sykdommer med benmassetap som har EP4 agonist som den aktive bestanddel | |
KR20130138811A (ko) | 조영제-유발 신병증의 치료 방법 | |
CA2401502A1 (en) | Carboxylic acid derivatives as ip antagonists | |
WO2013025733A1 (en) | Lysophosphatidic acid receptor antagonists | |
CN101284773A (zh) | 羧酸衍生物及以它为活性成分的药剂 | |
JP2009528333A (ja) | 選択的アンドロゲン受容体モジュレーター | |
MX2010002675A (es) | Profarmacos para analogos de hormonas tiroideas. | |
EP2682387A3 (en) | C7-fluoro substituted tetracycline compounds | |
BRPI0518242A2 (pt) | mÉtodos terapÊuticos e de liberaÇço de agonistas de prostaglandina ep4 | |
MXPA06002310A (es) | Compuesto capaz de enlazarse al receptor s1p y uso farmaceutico del mismo. | |
JPWO2020123827A5 (ja) | ||
WO2006103274A8 (fr) | Inhibiteurs d'age | |
CA3144201A1 (en) | Ep2 antagonist | |
ATE455761T1 (de) | Neue atorvastatinsalze und pharmazeutische zusammensetzungen, die diese enthalten | |
JP7265817B2 (ja) | 甲状腺ホルモン受容体アゴニスト特性を有する肝臓標的化合物及びその医薬組成物 | |
RU2007126973A (ru) | Способ получения n-замещенных салициламидов | |
BRPI0713806A2 (pt) | lactámicos gama substituìdos como agentes terapêuticos | |
US9388129B2 (en) | Mixed inhibitors of aminopeptidase N and neprilysin | |
JP3490114B2 (ja) | 軟骨保護剤 | |
BRPI0416665A (pt) | indóis substituìdos com piperidina ou heteroderivados dos mesmos |