AU2008239606A1 - Methods for treating spinal muscular atrophy using tetracycline compounds - Google Patents
Methods for treating spinal muscular atrophy using tetracycline compounds Download PDFInfo
- Publication number
- AU2008239606A1 AU2008239606A1 AU2008239606A AU2008239606A AU2008239606A1 AU 2008239606 A1 AU2008239606 A1 AU 2008239606A1 AU 2008239606 A AU2008239606 A AU 2008239606A AU 2008239606 A AU2008239606 A AU 2008239606A AU 2008239606 A1 AU2008239606 A1 AU 2008239606A1
- Authority
- AU
- Australia
- Prior art keywords
- alkyl
- heterocyclic
- aryl
- hydrogen
- carbonyl
- 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.)
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- -1 tetracycline compounds Chemical class 0.000 title claims description 497
- 238000000034 method Methods 0.000 title claims description 413
- 239000004098 Tetracycline Substances 0.000 title claims description 141
- 235000019364 tetracycline Nutrition 0.000 title claims description 141
- 229930101283 tetracycline Natural products 0.000 title claims description 119
- 229960002180 tetracycline Drugs 0.000 title claims description 118
- 208000002320 spinal muscular atrophy Diseases 0.000 title claims description 50
- 125000000217 alkyl group Chemical group 0.000 claims description 583
- 229910052739 hydrogen Inorganic materials 0.000 claims description 512
- 239000001257 hydrogen Substances 0.000 claims description 512
- 125000003118 aryl group Chemical group 0.000 claims description 495
- 125000000623 heterocyclic group Chemical group 0.000 claims description 446
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 388
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 365
- 125000003545 alkoxy group Chemical group 0.000 claims description 347
- 125000003342 alkenyl group Chemical group 0.000 claims description 338
- 229910052736 halogen Inorganic materials 0.000 claims description 338
- 150000002431 hydrogen Chemical group 0.000 claims description 337
- 125000002252 acyl group Chemical group 0.000 claims description 335
- 150000002367 halogens Chemical group 0.000 claims description 333
- 125000000304 alkynyl group Chemical group 0.000 claims description 330
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 329
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 327
- 150000003568 thioethers Chemical group 0.000 claims description 327
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims description 324
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 123
- 125000001931 aliphatic group Chemical group 0.000 claims description 110
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 89
- 229910052757 nitrogen Inorganic materials 0.000 claims description 89
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 52
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 39
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- 101000617738 Homo sapiens Survival motor neuron protein Proteins 0.000 claims description 30
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- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 8
- 239000000651 prodrug Chemical group 0.000 claims description 8
- 229940002612 prodrug Drugs 0.000 claims description 8
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 7
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- VMJNTFXCTXAXTC-UHFFFAOYSA-N 2,2-difluoro-1,3-benzodioxole-5-carbonitrile Chemical group C1=C(C#N)C=C2OC(F)(F)OC2=C1 VMJNTFXCTXAXTC-UHFFFAOYSA-N 0.000 claims description 5
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 5
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- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims description 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 2
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims description 2
- 125000002541 furyl group Chemical group 0.000 claims description 2
- 125000005928 isopropyloxycarbonyl group Chemical group [H]C([H])([H])C([H])(OC(*)=O)C([H])([H])[H] 0.000 claims description 2
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- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 2
- LURQBQNWDYASPJ-UHFFFAOYSA-N hydrazinyl Chemical compound N[NH] LURQBQNWDYASPJ-UHFFFAOYSA-N 0.000 claims 2
- WZZBNLYBHUDSHF-DHLKQENFSA-N 1-[(3s,4s)-4-[8-(2-chloro-4-pyrimidin-2-yloxyphenyl)-7-fluoro-2-methylimidazo[4,5-c]quinolin-1-yl]-3-fluoropiperidin-1-yl]-2-hydroxyethanone Chemical compound CC1=NC2=CN=C3C=C(F)C(C=4C(=CC(OC=5N=CC=CN=5)=CC=4)Cl)=CC3=C2N1[C@H]1CCN(C(=O)CO)C[C@@H]1F WZZBNLYBHUDSHF-DHLKQENFSA-N 0.000 claims 1
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 claims 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 1
- 125000005036 alkoxyphenyl group Chemical group 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
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- 210000005228 liver tissue Anatomy 0.000 claims 1
- VNWKTOKETHGBQD-UHFFFAOYSA-N methane Natural products C VNWKTOKETHGBQD-UHFFFAOYSA-N 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 210000005084 renal tissue Anatomy 0.000 claims 1
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- 229940040944 tetracyclines Drugs 0.000 description 23
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- 235000018102 proteins Nutrition 0.000 description 14
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- 125000001072 heteroaryl group Chemical group 0.000 description 8
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 description 7
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 5
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- 230000004083 survival effect Effects 0.000 description 5
- 208000033526 Proximal spinal muscular atrophy type 3 Diseases 0.000 description 4
- 208000003954 Spinal Muscular Atrophies of Childhood Diseases 0.000 description 4
- 125000004442 acylamino group Chemical group 0.000 description 4
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- 230000000694 effects Effects 0.000 description 1
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- 210000003292 kidney cell Anatomy 0.000 description 1
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- AHEVKYYGXVEWNO-UEPZRUIBSA-N lymecycline Chemical compound C1=CC=C2[C@](O)(C)[C@H]3C[C@H]4[C@H](N(C)C)C(O)=C(C(=O)NCNCCCC[C@H](N)C(O)=O)C(=O)[C@@]4(O)C(O)=C3C(=O)C2=C1O AHEVKYYGXVEWNO-UEPZRUIBSA-N 0.000 description 1
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- 230000035515 penetration Effects 0.000 description 1
- MEGKRPMNPGTIIG-VNYBMUHKSA-N penimepicycline Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)COC1=CC=CC=C1.O=C([C@@]1(O)C(O)=C2[C@@H]([C@](C3=CC=CC(O)=C3C2=O)(C)O)C[C@H]1[C@@H](C=1O)N(C)C)C=1C(=O)NCN1CCN(CCO)CC1 MEGKRPMNPGTIIG-VNYBMUHKSA-N 0.000 description 1
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- XATZHCXBMKRRDO-REHNUXHNSA-N pipacycline Chemical compound O=C([C@@]1(O)C(O)=C2[C@@H]([C@](C3=CC=CC(O)=C3C2=O)(C)O)C[C@H]1[C@@H](C=1O)N(C)C)C=1C(=O)NCN1CCN(CCO)CC1 XATZHCXBMKRRDO-REHNUXHNSA-N 0.000 description 1
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- 208000023504 respiratory system disease Diseases 0.000 description 1
- 229910052702 rhenium Inorganic materials 0.000 description 1
- HMEYVGGHISAPJR-IAHYZSEUSA-N rolitetracycline Chemical compound O=C([C@@]1(O)C(O)=C2[C@@H]([C@](C3=CC=CC(O)=C3C2=O)(C)O)C[C@H]1[C@@H](C=1O)N(C)C)C=1C(=O)NCN1CCCC1 HMEYVGGHISAPJR-IAHYZSEUSA-N 0.000 description 1
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Classifications
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- 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
- A61K31/65—Tetracyclines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (11)
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| US60/923,031 | 2007-04-12 | ||
| US93088307P | 2007-05-18 | 2007-05-18 | |
| US60/930,883 | 2007-05-18 | ||
| US94611007P | 2007-06-25 | 2007-06-25 | |
| US60/946,110 | 2007-06-25 | ||
| US99416307P | 2007-09-18 | 2007-09-18 | |
| US60/994,163 | 2007-09-18 | ||
| US98619207P | 2007-11-07 | 2007-11-07 | |
| US60/986,192 | 2007-11-07 | ||
| PCT/US2008/004827 WO2008127722A1 (en) | 2007-04-12 | 2008-04-14 | Methods for treating spinal muscular atrophy using tetracycline compounds |
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| AU2008239606A1 true AU2008239606A1 (en) | 2008-10-23 |
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| EP (1) | EP2144614A1 (enExample) |
| JP (1) | JP2010523684A (enExample) |
| AU (1) | AU2008239606A1 (enExample) |
| CA (1) | CA2688725A1 (enExample) |
| WO (1) | WO2008127722A1 (enExample) |
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| US6756365B2 (en) * | 1991-11-06 | 2004-06-29 | Trustees Of Tufts College | Reducing tetracycline resistance in living cells |
| JP2002501026A (ja) * | 1998-01-23 | 2002-01-15 | トルスティーズ オブ トゥフツ カレッジ | 薬学的に活性の化合物及びその利用法 |
| US20040224927A1 (en) | 2000-06-16 | 2004-11-11 | Trustees Of Tufts College | 7-N-substituted phenyl tetracycline compounds |
| US20020132798A1 (en) * | 2000-06-16 | 2002-09-19 | Nelson Mark L. | 7-phenyl-substituted tetracycline compounds |
| US7094806B2 (en) | 2000-07-07 | 2006-08-22 | Trustees Of Tufts College | 7, 8 and 9-substituted tetracycline compounds |
| KR101027625B1 (ko) * | 2000-07-07 | 2011-04-06 | 파라테크 파마슈티컬스, 인크. | 7-치환 테트라사이클린 화합물 |
| US8088820B2 (en) * | 2001-04-24 | 2012-01-03 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds for the treatment of malaria |
| EP1562608A4 (en) | 2002-10-24 | 2010-09-01 | Paratek Pharm Innc | METHOD OF USE OF SUBSTITUTED TETRACYCLINE COMPOUNDS FOR MODULATING THE RNA |
| KR101228706B1 (ko) | 2003-07-09 | 2013-02-01 | 파라테크 파마슈티컬스, 인크. | 치환된 테트라시클린 화합물 |
| US20060287283A1 (en) * | 2003-07-09 | 2006-12-21 | Paratek Pharmaceuticals, Inc. | Prodrugs of 9-aminomethyl tetracycline compounds |
| EP2269978A3 (en) * | 2004-10-25 | 2011-09-21 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds |
| AU2006210406C1 (en) | 2005-02-04 | 2013-03-07 | Paratek Pharmaceuticals, Inc. | 11a, 12-derivatives of tetracycline compounds |
| CA2616224A1 (en) * | 2005-07-21 | 2007-02-01 | Paratek Pharmaceuticals, Inc. | 10-substituted tetracyclines and methods of use thereof |
| EP2537934A3 (en) * | 2006-05-15 | 2013-04-10 | Paratek Pharmaceuticals, Inc. | Methods of regulating expression of genes or of gene products using substituted tetracycline compounds |
| EP3045449A1 (en) * | 2006-12-21 | 2016-07-20 | Paratek Pharmaceuticals, Inc. | Tetracycline derivatives for the treatment of bacterial, viral and parasitic infections |
| CA2673486C (en) | 2006-12-21 | 2015-09-08 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds for treatment of inflammatory skin disorders |
| WO2008127722A1 (en) | 2007-04-12 | 2008-10-23 | Paratek Pharmaceuticals, Inc. | Methods for treating spinal muscular atrophy using tetracycline compounds |
| BRPI0908951A2 (pt) | 2008-03-05 | 2017-01-17 | Paratek Pharm Innc | compostos de minociclina e método de uso dos mesmos |
| EP2276342A4 (en) * | 2008-04-14 | 2012-02-22 | Paratek Pharm Innc | SUBSTITUTED TETRACYCLIN COMPOUNDS |
| PL3000805T3 (pl) | 2008-08-08 | 2018-04-30 | Tetraphase Pharmaceuticals, Inc. | C7-fluoro podstawione związki tetracyklinowe |
| WO2010033939A1 (en) * | 2008-09-19 | 2010-03-25 | Paratek Pharmaceuticals, Inc. | Tetracycline compounds for the treatment of rheumatoid arthritis and related methods of treatment |
| ES2627772T3 (es) | 2009-05-08 | 2017-07-31 | Tetraphase Pharmaceuticals, Inc. | Compuestos de tetraciclina |
| WO2011025982A2 (en) | 2009-08-28 | 2011-03-03 | Tetraphase Pharmaceuticals, Inc. | Tetracycline compounds |
| JP6522498B2 (ja) * | 2012-05-30 | 2019-05-29 | パラテック ファーマシューティカルズ インコーポレイテッド | ７−二置換フェニルテトラサイクリン誘導体 |
| AU2013308504B2 (en) | 2012-08-31 | 2016-11-10 | Tetraphase Pharmaceuticals, Inc. | Tetracycline compounds |
| LT3368069T (lt) | 2016-06-13 | 2020-12-10 | Scholar Rock, Inc. | Miostatino inhibitorių naudojimas, ir kombinuotas gydymas |
| KR102880712B1 (ko) | 2016-10-19 | 2025-11-03 | 테트라페이즈 파마슈티컬스, 인코포레이티드 | 에라바사이클린의 결정질 형태 |
| WO2018085216A1 (en) | 2016-11-01 | 2018-05-11 | Paratek Pharmaceuticals, Inc. | 9-aminomethyl minocycline compounds and use thereof in treating community-acquire bacterial pneumonia (cabp) |
| CA3193909A1 (en) | 2020-10-26 | 2022-05-05 | George NOMIKOS | Use of anti-pro/latent myostatin antibody for treating spinal muscular atrophy |
| WO2023215384A2 (en) | 2022-05-04 | 2023-11-09 | Scholar Rock, Inc. | Use of myostatin inhibitor for treating spinal muscular atrophy |
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| US3062717A (en) * | 1958-12-11 | 1962-11-06 | Pfizer & Co C | Intramuscular calcium tetracycline acetic or lactic acid carboxamide vehicle preparation |
| US3165531A (en) * | 1962-03-08 | 1965-01-12 | Pfizer & Co C | 13-substituted-6-deoxytetracyclines and process utilizing the same |
| US3454697A (en) * | 1965-06-08 | 1969-07-08 | American Cyanamid Co | Tetracycline antibiotic compositions for oral use |
| NL6607516A (enExample) * | 1966-05-31 | 1967-12-01 | ||
| DE1767891C3 (de) * | 1968-06-28 | 1980-10-30 | Pfizer | Verfahren zur Herstellung von wäßrigen arzneilichen Lösungen für die parenterale, perorale und lokale Anwendung mit einem Gehalt an einem Tetracyclinderivat |
| CA999855A (en) | 1972-09-18 | 1976-11-16 | Societa' Farmaceutici Italia S.P.A. | Process for the preparation of tetracyclines derivatives in the 7 position |
| US3957980A (en) * | 1972-10-26 | 1976-05-18 | Pfizer Inc. | Doxycycline parenteral compositions |
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| EP2537934A3 (en) | 2006-05-15 | 2013-04-10 | Paratek Pharmaceuticals, Inc. | Methods of regulating expression of genes or of gene products using substituted tetracycline compounds |
| CA2673486C (en) | 2006-12-21 | 2015-09-08 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds for treatment of inflammatory skin disorders |
| WO2008127722A1 (en) | 2007-04-12 | 2008-10-23 | Paratek Pharmaceuticals, Inc. | Methods for treating spinal muscular atrophy using tetracycline compounds |
| WO2008134048A2 (en) | 2007-04-27 | 2008-11-06 | Paratek Pharmaceuticals, Inc. | Methods for synthesizing and purifying aminoalkyl tetracycline compounds |
| EA201070048A1 (ru) | 2007-07-06 | 2010-10-29 | Паратек Фармасьютикалс, Инк. | Способы синтеза замещённых соединений тетрациклина (варианты) |
-
2008
- 2008-04-14 WO PCT/US2008/004827 patent/WO2008127722A1/en not_active Ceased
- 2008-04-14 AU AU2008239606A patent/AU2008239606A1/en not_active Abandoned
- 2008-04-14 CA CA2688725A patent/CA2688725A1/en not_active Abandoned
- 2008-04-14 EP EP08742883A patent/EP2144614A1/en not_active Withdrawn
- 2008-04-14 JP JP2010503091A patent/JP2010523684A/ja active Pending
- 2008-04-14 US US12/102,623 patent/US7935687B2/en not_active Expired - Fee Related
-
2011
- 2011-05-03 US US13/099,993 patent/US8399437B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US20110207706A1 (en) | 2011-08-25 |
| US7935687B2 (en) | 2011-05-03 |
| US8399437B2 (en) | 2013-03-19 |
| US20090118269A1 (en) | 2009-05-07 |
| CA2688725A1 (en) | 2008-10-23 |
| EP2144614A1 (en) | 2010-01-20 |
| JP2010523684A (ja) | 2010-07-15 |
| WO2008127722A1 (en) | 2008-10-23 |
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