CA2917277A1 - Losmapimod for use in treating glomerular disease - Google Patents
Losmapimod for use in treating glomerular disease Download PDFInfo
- Publication number
- CA2917277A1 CA2917277A1 CA2917277A CA2917277A CA2917277A1 CA 2917277 A1 CA2917277 A1 CA 2917277A1 CA 2917277 A CA2917277 A CA 2917277A CA 2917277 A CA2917277 A CA 2917277A CA 2917277 A1 CA2917277 A1 CA 2917277A1
- Authority
- CA
- Canada
- Prior art keywords
- glomerular disease
- methyl
- nicotinamide
- fluoro
- pharmaceutically acceptable
- 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.)
- Abandoned
Links
- 208000022461 Glomerular disease Diseases 0.000 title claims abstract description 32
- 231100000852 glomerular disease Toxicity 0.000 title claims abstract description 32
- KKYABQBFGDZVNQ-UHFFFAOYSA-N 6-[5-[(cyclopropylamino)-oxomethyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-3-pyridinecarboxamide Chemical compound CC1=C(F)C=C(C(=O)NC2CC2)C=C1C1=CC=C(C(=O)NCC(C)(C)C)C=N1 KKYABQBFGDZVNQ-UHFFFAOYSA-N 0.000 title claims description 9
- 229950003265 losmapimod Drugs 0.000 title description 5
- 150000001875 compounds Chemical class 0.000 claims abstract description 26
- 238000011282 treatment Methods 0.000 claims abstract description 26
- 150000003839 salts Chemical class 0.000 claims description 34
- 239000003814 drug Substances 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 239000013066 combination product Substances 0.000 claims description 6
- 229940127555 combination product Drugs 0.000 claims description 6
- 208000017169 kidney disease Diseases 0.000 claims description 5
- 229940124597 therapeutic agent Drugs 0.000 claims description 5
- 206010020772 Hypertension Diseases 0.000 claims description 4
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 claims description 4
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 claims description 4
- 230000001434 glomerular Effects 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- -1 6-(-cyclopropylcarbamoyl-3-fluoro-2-methyl-phenyl)-N-(2,2-dimethylpropyl)-nicotinamide Chemical compound 0.000 claims description 3
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 3
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 3
- 239000003053 toxin Substances 0.000 claims description 3
- 231100000765 toxin Toxicity 0.000 claims description 3
- 108700012359 toxins Proteins 0.000 claims description 3
- 208000024869 Goodpasture syndrome Diseases 0.000 claims description 2
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims description 2
- 206010021263 IgA nephropathy Diseases 0.000 claims description 2
- 206010037601 Pyelonephritis chronic Diseases 0.000 claims description 2
- 201000006368 chronic pyelonephritis Diseases 0.000 claims description 2
- 239000012458 free base Substances 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 201000008383 nephritis Diseases 0.000 claims description 2
- 201000006292 polyarteritis nodosa Diseases 0.000 claims description 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 208000024985 Alport syndrome Diseases 0.000 claims 1
- 206010002022 amyloidosis Diseases 0.000 claims 1
- 208000003215 hereditary nephritis Diseases 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 abstract description 2
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 abstract description 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract description 2
- 229960003966 nicotinamide Drugs 0.000 description 25
- 239000011570 nicotinamide Substances 0.000 description 25
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 17
- 201000010099 disease Diseases 0.000 description 15
- 210000003734 kidney Anatomy 0.000 description 8
- 201000001474 proteinuria Diseases 0.000 description 5
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 4
- 230000009885 systemic effect Effects 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 239000005541 ACE inhibitor Substances 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 208000020832 chronic kidney disease Diseases 0.000 description 3
- 230000006378 damage Effects 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 230000037390 scarring Effects 0.000 description 3
- 206010018364 Glomerulonephritis Diseases 0.000 description 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 description 2
- 210000004204 blood vessel Anatomy 0.000 description 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 2
- 229940109239 creatinine Drugs 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 229940079832 sodium starch glycolate Drugs 0.000 description 2
- 229920003109 sodium starch glycolate Polymers 0.000 description 2
- 239000008109 sodium starch glycolate Substances 0.000 description 2
- 150000003431 steroids Chemical class 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 210000002700 urine Anatomy 0.000 description 2
- 208000009304 Acute Kidney Injury Diseases 0.000 description 1
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 1
- 206010055171 Hypertensive nephropathy Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
- 206010065673 Nephritic syndrome Diseases 0.000 description 1
- 206010029164 Nephrotic syndrome Diseases 0.000 description 1
- 239000012826 P38 inhibitor Substances 0.000 description 1
- 208000001647 Renal Insufficiency Diseases 0.000 description 1
- 208000033626 Renal failure acute Diseases 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 201000011040 acute kidney failure Diseases 0.000 description 1
- 208000012998 acute renal failure Diseases 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 150000001340 alkali metals Chemical class 0.000 description 1
- 125000005907 alkyl ester group Chemical group 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 238000000502 dialysis Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000002565 electrocardiography Methods 0.000 description 1
- 208000028208 end stage renal disease Diseases 0.000 description 1
- 201000000523 end stage renal failure Diseases 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000035876 healing Effects 0.000 description 1
- 208000006750 hematuria Diseases 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 201000006370 kidney failure Diseases 0.000 description 1
- 230000003907 kidney function Effects 0.000 description 1
- 229960001021 lactose monohydrate Drugs 0.000 description 1
- 238000007449 liver function test Methods 0.000 description 1
- 206010025135 lupus erythematosus Diseases 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000002483 medication Methods 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 150000005480 nicotinamides Chemical class 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 230000002784 sclerotic effect Effects 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 230000002485 urinary effect Effects 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361844491P | 2013-07-10 | 2013-07-10 | |
| US61/844,491 | 2013-07-10 | ||
| PCT/EP2014/064508 WO2015004089A1 (en) | 2013-07-10 | 2014-07-08 | Losmapimod for use in treating glomerular disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2917277A1 true CA2917277A1 (en) | 2015-01-15 |
Family
ID=51134104
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2917277A Abandoned CA2917277A1 (en) | 2013-07-10 | 2014-07-08 | Losmapimod for use in treating glomerular disease |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9707219B2 (enExample) |
| EP (1) | EP3019168A1 (enExample) |
| JP (1) | JP2016523943A (enExample) |
| KR (1) | KR20160030206A (enExample) |
| CN (1) | CN105358148A (enExample) |
| AU (1) | AU2014289296A1 (enExample) |
| CA (1) | CA2917277A1 (enExample) |
| RU (1) | RU2015156417A (enExample) |
| WO (1) | WO2015004089A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3691620T (pt) | 2017-10-05 | 2022-10-06 | Fulcrum Therapeutics Inc | Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| US20200085810A1 (en) * | 2018-07-26 | 2020-03-19 | Hoffmann-La Roche Inc. | Compounds for use in treating kidney disorders |
| GB201821138D0 (en) * | 2018-12-21 | 2019-02-06 | Benevolentai Bio Ltd | Compositions and uses thereof |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101058292B1 (ko) | 2002-02-12 | 2011-08-22 | 글락소스미스클라인 엘엘씨 | Ｐ38 억제제로 유용한 니코틴아미드 유도체 |
| KR20070074576A (ko) * | 2004-10-29 | 2007-07-12 | 코와 가부시키가이샤 | 사구체 질환 치료제 |
| GB0612026D0 (en) * | 2006-06-16 | 2006-07-26 | Smithkline Beecham Corp | New use |
| EP2874627A1 (en) * | 2012-07-17 | 2015-05-27 | Glaxosmithkline LLC | Nicotinamide derivate in the treatment of acute coronary syndrome |
-
2014
- 2014-07-08 KR KR1020167002417A patent/KR20160030206A/ko not_active Withdrawn
- 2014-07-08 WO PCT/EP2014/064508 patent/WO2015004089A1/en not_active Ceased
- 2014-07-08 EP EP14735983.0A patent/EP3019168A1/en not_active Withdrawn
- 2014-07-08 AU AU2014289296A patent/AU2014289296A1/en not_active Abandoned
- 2014-07-08 CN CN201480038296.4A patent/CN105358148A/zh active Pending
- 2014-07-08 RU RU2015156417A patent/RU2015156417A/ru not_active Application Discontinuation
- 2014-07-08 JP JP2016524786A patent/JP2016523943A/ja active Pending
- 2014-07-08 US US14/903,694 patent/US9707219B2/en not_active Expired - Fee Related
- 2014-07-08 CA CA2917277A patent/CA2917277A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2014289296A1 (en) | 2016-02-04 |
| KR20160030206A (ko) | 2016-03-16 |
| US9707219B2 (en) | 2017-07-18 |
| CN105358148A (zh) | 2016-02-24 |
| WO2015004089A1 (en) | 2015-01-15 |
| RU2015156417A (ru) | 2017-08-15 |
| JP2016523943A (ja) | 2016-08-12 |
| US20160220550A1 (en) | 2016-08-04 |
| EP3019168A1 (en) | 2016-05-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Dead |
Effective date: 20180710 |