HRP20221430T1 - Inhibitori aldozoreduktaze i njihova uporaba - Google Patents
Inhibitori aldozoreduktaze i njihova uporaba Download PDFInfo
- Publication number
- HRP20221430T1 HRP20221430T1 HRP20221430TT HRP20221430T HRP20221430T1 HR P20221430 T1 HRP20221430 T1 HR P20221430T1 HR P20221430T T HRP20221430T T HR P20221430TT HR P20221430 T HRP20221430 T HR P20221430T HR P20221430 T1 HRP20221430 T1 HR P20221430T1
- Authority
- HR
- Croatia
- Prior art keywords
- hydrogen
- alkyl
- inhibitor
- use according
- image
- Prior art date
Links
- 239000003288 aldose reductase inhibitor Substances 0.000 title claims 3
- 229940090865 aldose reductase inhibitors used in diabetes Drugs 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 26
- 239000001257 hydrogen Substances 0.000 claims 26
- 239000003112 inhibitor Substances 0.000 claims 16
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 11
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 229910052760 oxygen Inorganic materials 0.000 claims 11
- 229910052717 sulfur Inorganic materials 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000001188 haloalkyl group Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 6
- 206010012601 diabetes mellitus Diseases 0.000 claims 5
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 claims 4
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 125000002252 acyl group Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims 4
- 125000004995 haloalkylthio group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 229940118148 Aldose reductase inhibitor Drugs 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- MNQZXJOMYWMBOU-UHFFFAOYSA-N glyceraldehyde Chemical compound OCC(O)C=O MNQZXJOMYWMBOU-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Cosmetics (AREA)
Claims (15)
1. Inhibitor aldoza reduktaze za uporabu u liječenju kardiovaskularnog poremećaja ili komplikacija koje proizlaze od dijabetesa, pri čemu je inhibitor aldoreduktaze spoj formule (I) ili njegova farmaceutski prihvatljiva sol ili solvat,
[image]
gdje je R1 H, (C1-C6)-alkil, (C1-C6)-hidroksialkil ili (C1-C6)-aminoalkil;
X1 je N ili CR3;
X2 je N ili CR4;
X3 je N ili CR5;
X4 je N ili CR6; uz uvjet da su dva ili tri od X1, X2, X3 ili X4 N;
Y je veza, C=O, C=S, C=NH ili C=N(C1-C4)-alkil;
Z je
[image]
A1 je NR11, O, S ili CH2;
A2 je N ili CH;
A3 je NR11, O ili S;
R3 do R10 su neovisno vodik, halogen, cijano, acil, haloalkil, haloalkoksi, haloalkiltio, trifluoroacetil, (C1-C4)-alkil, (C1-C4)-alkoksi, (C1-C4)-alkiltio, (C1-C4)-alkilsulfinil ili(C1-C4)-alkilsulfonil; ili dva od R3 do R6 ili dva od R7 do R10 uzeti zajedno su (C1-C4)-alkilendioksi; i
R11 je vodik, C1-C4 alkil ili C(O)O-(C1-C4))-alkil.
2. Inhibitor za uporabu sukladno zahtjevu 1, naznačen time, da je R1 vodik ili (C1-C6)-alkil;
X1 i X4 su N;
X2 je CR4;
X3 je CR5;
Y je C=O;
Z je
[image]
A1 je NR11, O ili S;
A2 je N;
A3 je O ili S;
R4 i R5 su vodik;
R7 do R10 su neovisno vodik, halogen, cijano, acil, haloalkil, haloalkoksi, haloalkiltio, (C1-C4)-alkil, (C1-C4)-alkoksi, (C1-C4))-alkiltio, (C1-C4)-alkilsulfinil ili (C1-C4)-alkilsulfonil; i
R11 je vodik, C1-C4 alkil ili C(O)O-(C1-C4)-alkil.
3. Inhibitor za uporabu sukladno zahtjevu 2, naznačen time, da je R1 vodik ili tert-butil;
X1 i X4 su N;
X2 je CR4;
X3 je CR5;
Y je C=O;
Z je
[image]
A1 je NR11, O ili S;
A2 je N;
A3 je O ili S;
R4 i R5 su vodik;
R7 do R10 su neovisno vodik, halogen ili haloalkil; i
R11 je vodik, (C1-C4))-alkil ili C(O)O-tert-butil.
4. Inhibitor za uporabu sukladno zahtjevu 1, naznačen time, da je Z
[image]
5. Inhibitor za uporabu sukladno zahtjevu 4, naznačen time, da R1 je vodik ili (C1-C6)-alkil;
X1 i X4 su N;
X2 je CR4;
X3 je CR5;
Y je C=O;
A1 je NR11, O ili S;
A2 je N;
R4 i R5 su vodik;
R7 do R10 su neovisno vodik, halogen, cijano, acil, haloalkil, haloalkoksi, haloalkiltio, (C1-C4)-alkil, (C1-C4)-alkoksi, (C1-C4))-akltio, (C1-C4)-alkilsulfinil ili (C1-C4)-alkilsulfonil; i
R11 je vodik, C1-C4 alkil ili C(O)O-(C1-C4)-alkil.
6. Inhibitor za uporabu sukladno zahtjevu 5, naznačen time što je R1 vodik ili tert-butil;
X1 i X4 su N;
X2 je CR4;
X3 je CR5;
Y je C=O;
A1 je NR11, O ili S;
A2 je N;
R4 i R5 su vodik;
R7 do R10 su neovisno vodik, halogen ili haloalkil; i
R11 je vodik, (C1-C4)-alkil ili C(O)O-tert-butil.
7. Inhibitor za uporabu sukladno zahtjevu 1, naznačen time, da je Z
[image]
8. Inhibitor za uporabu sukladno zahtjevu 7, naznačen time, da je R1 vodik ili (C1-C6)-alkil;
X1 i X4 su N;
X2 je CR4;
X3 je CR5;
Y je C=O;
A3 je NR11, O ili S;
R4 i R5 su vodik;
R7 do R10 su neovisno vodik, halogen, cijano, acil, haloalkil, haloalkoksi, haloalkiltio, (C1-C4)-alkil, (C1-C4)-alkoksi, (C1-C4)-akltio, (C1-C4)-alkilsulfinil ili (C1-C4)-alkilsulfonil; i
R11 je vodik, C1-C4 alkil ili C(O)O-(C1-C4)-alkil.
9. Inhibitor za uporabu sukladno zahtjevu 8, naznačen time, da je R1 vodik ili tert-butil;
X1 i X4 su N;
X2 je CR4;
X3 je CR5;
Y je C=O;
A3 je NR11, O ili S;
R4 i R5 su vodik;
R7 do R10 su neovisno vodik, halogen ili haloalkil; i
R11 je vodik, (C1-C4)-alkil ili C(O)O-tert-butil.
10. Inhibitor za uporabu sukladno zahtjevu 1, naznačen time, da je inhibitor aldoreduktaze
[image]
ili njegova farmaceutski prihvatljiva sol; ili
pri čemu je inhibitor aldoreduktaze
[image]
ili njegova farmaceutski prihvatljiva sol.
11. Inhibitor za uporabu sukladno bilo kojem od zahtjeva 1-10, za uporabu u liječenju kardiovaskularnog poremećaja.
12. Inhibitor za uporabu sukladno bilo kojem od zahtjeva 1-10, za uporabu u liječenju komplikacija koje proizlaze od dijabetesa.
13. Inhibitor za uporabu sukladno zahtjevu 12, naznačen time, da je komplikacija koja proizlazi od dijabetesa dijabetička nefropatija.
14. Inhibitor za uporabu sukladno zahtjevu 12, naznačen time što je komplikacija koja proizlazi iz dijabetesa dijabetička neuropatija.
15. Inhibitor za uporabu sukladno zahtjevu 12, naznačen time, da je komplikacija koja proizlazi od dijabetesa dijabetička retinopatija.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36509810P | 2010-07-16 | 2010-07-16 | |
| EP19194956.9A EP3597650B1 (en) | 2010-07-16 | 2011-07-14 | Aldose reductase inhibitors and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20221430T1 true HRP20221430T1 (hr) | 2023-01-06 |
Family
ID=45469805
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20221430TT HRP20221430T1 (hr) | 2010-07-16 | 2011-07-14 | Inhibitori aldozoreduktaze i njihova uporaba |
Country Status (16)
| Country | Link |
|---|---|
| EP (4) | EP4124620A1 (hr) |
| JP (4) | JP5934206B2 (hr) |
| CN (2) | CN105732640B (hr) |
| AU (1) | AU2011279058B2 (hr) |
| CA (1) | CA2804640C (hr) |
| DK (3) | DK2593456T3 (hr) |
| ES (3) | ES2613700T3 (hr) |
| HK (1) | HK1223925A1 (hr) |
| HR (1) | HRP20221430T1 (hr) |
| HU (3) | HUE031506T2 (hr) |
| LT (1) | LT3597650T (hr) |
| PL (3) | PL2593456T3 (hr) |
| PT (1) | PT3597650T (hr) |
| RS (1) | RS63796B1 (hr) |
| SI (1) | SI3597650T1 (hr) |
| WO (1) | WO2012009553A1 (hr) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8916563B2 (en) | 2010-07-16 | 2014-12-23 | The Trustees Of Columbia University In The City Of New York | Aldose reductase inhibitors and uses thereof |
| EP4124620A1 (en) * | 2010-07-16 | 2023-02-01 | The Trustees of Columbia University in the City of New York | Aldose reductase inhibitors and uses thereof |
| US20140228319A1 (en) * | 2013-02-13 | 2014-08-14 | Banavara L. Mylari | Water soluble salts of aldose reductase inhibitors for treatment of diabetic complications |
| PT3352754T (pt) | 2016-06-21 | 2020-12-07 | Univ Columbia | Inibidores da aldose redutase e métodos de seu uso |
| EP3658142B1 (en) | 2017-07-28 | 2024-04-17 | Applied Therapeutics, Inc. | Compositions and methods for treating galactosemia |
| CN108101883B (zh) * | 2018-01-31 | 2018-11-13 | 佳木斯大学附属第一医院 | 一种用于防治糖尿病视网膜病变的药物及其制备方法 |
| EP3924060A4 (en) * | 2019-02-12 | 2023-03-22 | Applied Therapeutics, Inc. | METHODS FOR TREATMENT OF SKIN AGING |
| AU2020229932B2 (en) * | 2019-02-28 | 2023-09-21 | Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. | Salt of aldose reductase inhibitor, and preparation method and application thereof |
| EP3947391A1 (en) * | 2019-04-01 | 2022-02-09 | Applied Therapeutics Inc. | Inhibitors of aldose reductase |
| EP3966320A4 (en) | 2019-05-07 | 2023-10-25 | University of Miami | TREATMENT AND DETECTION OF HEREDITARY NEUROPATHIES AND ASSOCIATED DISORDERS |
| KR20230005944A (ko) | 2020-05-01 | 2023-01-10 | 어플라이드 테라퓨틱스 인크. | 소르비톨 데히드로게나제 결핍 치료를 위한 알도스 리덕타제 억제제 |
| EP4211136A1 (en) * | 2020-09-08 | 2023-07-19 | Teva Pharmaceuticals International GmbH | Solid state forms of at-001 and process for preparation thereof |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US557A (en) | 1838-01-09 | James macgregor | ||
| US5304A (en) | 1847-09-25 | Improvement in preparing and hardening raw hides | ||
| CA1299178C (en) * | 1985-11-07 | 1992-04-21 | Banavara Lakshmana Mylari | Heterocyclic oxophtalazinyl acetic acids |
| US4939140A (en) | 1985-11-07 | 1990-07-03 | Pfizer Inc. | Heterocyclic oxophthalazinyl acetic acids |
| IL80475A (en) * | 1985-11-07 | 1993-01-31 | Pfizer | Heterocyclic-substituted 4-oxo (or thio)-3h- phthalazinyl-acetic acid derivatives and pharmaceutical compositions containing them |
| WO1989006651A1 (en) * | 1988-01-19 | 1989-07-27 | Pfizer Inc. | 1h-indazole-3-acetic acids as aldose reductase inhibitors |
| US4954629A (en) | 1989-05-11 | 1990-09-04 | Pfizer Inc. | Process and intermediates for the preparation of oxophthalazinyl acetic acids and analogs thereof |
| US4996204A (en) * | 1989-05-11 | 1991-02-26 | Pfizer Inc. | Pyrido[2,3-d]pyridazinones as aldose reductase inhibitors |
| FR2647676A1 (fr) * | 1989-06-05 | 1990-12-07 | Union Pharma Scient Appl | Nouveaux derives de pyridazinone, leurs procedes de preparation, medicaments les contenant, utiles notamment comme inhibiteurs de l'aldose reductase |
| US5304557A (en) | 1989-12-15 | 1994-04-19 | Pfizer Inc. | Substituted oxoophthalazinyl acetic acids and analogs thereof |
| JPH0495025A (ja) | 1990-08-08 | 1992-03-27 | Asahi Chem Ind Co Ltd | アルドースリダクターゼ阻害剤 |
| WO1997008126A1 (en) | 1995-08-28 | 1997-03-06 | American Home Products Corporation | Phenoxy acetic acids as aldose reductase inhibitors and antihyperglycemic agents |
| OA11622A (en) * | 1998-03-31 | 2004-09-16 | Inst For Pharm Discovery Inc | Substituted indolealkanoic acids. |
| EP0982306A3 (en) | 1998-08-21 | 2000-07-05 | Pfizer Products Inc. | Polymorph of zopolrestat monohydrate |
| US6570013B2 (en) | 2000-02-16 | 2003-05-27 | Pfizer Inc | Salts of zopolrestat |
| EP1469851B1 (en) | 2002-01-23 | 2006-10-11 | Eli Lilly And Company | Melanocortin receptor agonists |
| EP4124620A1 (en) * | 2010-07-16 | 2023-02-01 | The Trustees of Columbia University in the City of New York | Aldose reductase inhibitors and uses thereof |
-
2011
- 2011-07-14 EP EP22183971.5A patent/EP4124620A1/en active Pending
- 2011-07-14 HU HUE11807523A patent/HUE031506T2/en unknown
- 2011-07-14 HU HUE19194956A patent/HUE060473T2/hu unknown
- 2011-07-14 PL PL11807523T patent/PL2593456T3/pl unknown
- 2011-07-14 HR HRP20221430TT patent/HRP20221430T1/hr unknown
- 2011-07-14 ES ES11807523T patent/ES2613700T3/es active Active
- 2011-07-14 AU AU2011279058A patent/AU2011279058B2/en active Active
- 2011-07-14 PT PT191949569T patent/PT3597650T/pt unknown
- 2011-07-14 CN CN201610124090.4A patent/CN105732640B/zh active Active
- 2011-07-14 ES ES19194956T patent/ES2931319T3/es active Active
- 2011-07-14 SI SI201132072T patent/SI3597650T1/sl unknown
- 2011-07-14 WO PCT/US2011/044038 patent/WO2012009553A1/en active Application Filing
- 2011-07-14 DK DK11807523.3T patent/DK2593456T3/en active
- 2011-07-14 CN CN201180034944.5A patent/CN103052637B/zh active Active
- 2011-07-14 RS RS20221062A patent/RS63796B1/sr unknown
- 2011-07-14 DK DK16187936T patent/DK3192796T3/da active
- 2011-07-14 LT LTEP19194956.9T patent/LT3597650T/lt unknown
- 2011-07-14 PL PL19194956.9T patent/PL3597650T3/pl unknown
- 2011-07-14 EP EP16187936.6A patent/EP3192796B1/en active Active
- 2011-07-14 CA CA2804640A patent/CA2804640C/en active Active
- 2011-07-14 EP EP19194956.9A patent/EP3597650B1/en active Active
- 2011-07-14 ES ES16187936T patent/ES2769950T3/es active Active
- 2011-07-14 EP EP11807523.3A patent/EP2593456B1/en active Active
- 2011-07-14 DK DK19194956.9T patent/DK3597650T3/da active
- 2011-07-14 HU HUE16187936A patent/HUE047346T2/hu unknown
- 2011-07-14 JP JP2013520752A patent/JP5934206B2/ja active Active
- 2011-07-14 PL PL16187936T patent/PL3192796T3/pl unknown
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2016
- 2016-01-14 JP JP2016005570A patent/JP6165897B2/ja active Active
- 2016-10-20 HK HK16112126.4A patent/HK1223925A1/zh unknown
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2017
- 2017-06-20 JP JP2017120238A patent/JP6306251B2/ja active Active
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2018
- 2018-03-07 JP JP2018040694A patent/JP6430670B2/ja active Active
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