BR112021004057A2 - métodos de tratar ou prevenir uma infecção micobacteriana, de tratar ou prevenir, de controlar ou reduzir o avanço, severidade ou efeitos de uma doença micobacteriana, tuberculose, lepra, bronquiectasia, doença pulmonar cavitária, linfadenite, uma doença de tecido mole, granuloma de aquário, úlcera de buruli, uma doença ocular e doença óssea em um indivíduo em necessidade dos mesmos, e, métodos de tratar um indivíduo com uma doença pulmonar e de tratar um indivíduo com uma condição imunossuprimida. - Google Patents
métodos de tratar ou prevenir uma infecção micobacteriana, de tratar ou prevenir, de controlar ou reduzir o avanço, severidade ou efeitos de uma doença micobacteriana, tuberculose, lepra, bronquiectasia, doença pulmonar cavitária, linfadenite, uma doença de tecido mole, granuloma de aquário, úlcera de buruli, uma doença ocular e doença óssea em um indivíduo em necessidade dos mesmos, e, métodos de tratar um indivíduo com uma doença pulmonar e de tratar um indivíduo com uma condição imunossuprimida. Download PDFInfo
- Publication number
- BR112021004057A2 BR112021004057A2 BR112021004057-9A BR112021004057A BR112021004057A2 BR 112021004057 A2 BR112021004057 A2 BR 112021004057A2 BR 112021004057 A BR112021004057 A BR 112021004057A BR 112021004057 A2 BR112021004057 A2 BR 112021004057A2
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- alkynyl
- alkenyl
- individual
- alkylsulfinyl
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims abstract description 294
- 208000027531 mycobacterial infectious disease Diseases 0.000 title claims abstract description 82
- 206010062207 Mycobacterial infection Diseases 0.000 title claims abstract description 45
- 230000000694 effects Effects 0.000 title claims description 98
- 208000019693 Lung disease Diseases 0.000 title claims description 57
- 201000008827 tuberculosis Diseases 0.000 title claims description 41
- 201000009267 bronchiectasis Diseases 0.000 title claims description 31
- 208000016247 Soft tissue disease Diseases 0.000 title claims description 26
- 206010024229 Leprosy Diseases 0.000 title claims description 25
- 208000006448 Buruli Ulcer Diseases 0.000 title claims description 24
- 208000023081 Buruli ulcer disease Diseases 0.000 title claims description 24
- 206010066289 Mycobacterium ulcerans infection Diseases 0.000 title claims description 24
- 201000003265 lymphadenitis Diseases 0.000 title claims description 23
- 208000037946 swimming pool granuloma Diseases 0.000 title claims description 23
- 208000031116 aquarium granuloma Diseases 0.000 title claims description 22
- 208000020084 Bone disease Diseases 0.000 title claims description 19
- 208000030533 eye disease Diseases 0.000 title claims description 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims description 13
- 201000010099 disease Diseases 0.000 title claims description 12
- 230000002685 pulmonary effect Effects 0.000 title claims description 6
- -1 tetracycline compound Chemical class 0.000 claims abstract description 293
- 239000004098 Tetracycline Substances 0.000 claims abstract description 155
- 229960002180 tetracycline Drugs 0.000 claims abstract description 155
- 235000019364 tetracycline Nutrition 0.000 claims abstract description 155
- 229930101283 tetracycline Natural products 0.000 claims abstract description 155
- 150000003839 salts Chemical class 0.000 claims abstract description 122
- 229950004150 omadacycline Drugs 0.000 claims abstract description 120
- 238000011282 treatment Methods 0.000 claims abstract description 10
- JEECQCWWSTZDCK-IQZGDKDPSA-N omadacycline Chemical compound C([C@H]1C2)C3=C(N(C)C)C=C(CNCC(C)(C)C)C(O)=C3C(=O)C1=C(O)[C@@]1(O)[C@@H]2[C@H](N(C)C)C(O)=C(C(N)=O)C1=O JEECQCWWSTZDCK-IQZGDKDPSA-N 0.000 claims abstract 60
- 239000001257 hydrogen Substances 0.000 claims description 430
- 229910052739 hydrogen Inorganic materials 0.000 claims description 430
- 125000000217 alkyl group Chemical group 0.000 claims description 380
- 125000003342 alkenyl group Chemical group 0.000 claims description 362
- 125000000304 alkynyl group Chemical group 0.000 claims description 362
- 150000002431 hydrogen Chemical group 0.000 claims description 312
- 125000003545 alkoxy group Chemical group 0.000 claims description 300
- 125000003282 alkyl amino group Chemical group 0.000 claims description 300
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims description 300
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 300
- 125000004414 alkyl thio group Chemical group 0.000 claims description 300
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 300
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 300
- 125000003118 aryl group Chemical group 0.000 claims description 262
- 229940002612 prodrug Drugs 0.000 claims description 212
- 239000000651 prodrug Substances 0.000 claims description 212
- 229910052736 halogen Inorganic materials 0.000 claims description 206
- 150000002367 halogens Chemical class 0.000 claims description 206
- 150000002148 esters Chemical class 0.000 claims description 119
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 118
- 125000001072 heteroaryl group Chemical group 0.000 claims description 106
- 125000001589 carboacyl group Chemical group 0.000 claims description 55
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims description 50
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 50
- 125000003435 aroyl group Chemical group 0.000 claims description 50
- 125000005199 aryl carbonyloxy group Chemical group 0.000 claims description 50
- 125000000623 heterocyclic group Chemical group 0.000 claims description 50
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 50
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 50
- 241000186359 Mycobacterium Species 0.000 claims description 49
- 241000894007 species Species 0.000 claims description 44
- 230000002829 reductive effect Effects 0.000 claims description 41
- 239000007943 implant Substances 0.000 claims description 36
- 239000003814 drug Substances 0.000 claims description 17
- 229940079593 drug Drugs 0.000 claims description 17
- 208000015181 infectious disease Diseases 0.000 claims description 16
- 241001508003 Mycobacterium abscessus Species 0.000 claims description 13
- 241000187478 Mycobacterium chelonae Species 0.000 claims description 13
- 125000002252 acyl group Chemical group 0.000 claims description 12
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 12
- 241000186365 Mycobacterium fortuitum Species 0.000 claims description 10
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 9
- 230000001506 immunosuppresive effect Effects 0.000 claims description 9
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 8
- 241000186367 Mycobacterium avium Species 0.000 claims description 8
- 241001302239 Mycobacterium tuberculosis complex Species 0.000 claims description 8
- 239000002537 cosmetic Substances 0.000 claims description 8
- 230000002526 effect on cardiovascular system Effects 0.000 claims description 8
- AEUTYOVWOVBAKS-UWVGGRQHSA-N ethambutol Chemical compound CC[C@@H](CO)NCCN[C@@H](CC)CO AEUTYOVWOVBAKS-UWVGGRQHSA-N 0.000 claims description 8
- 210000004072 lung Anatomy 0.000 claims description 8
- 230000000399 orthopedic effect Effects 0.000 claims description 8
- 208000017520 skin disease Diseases 0.000 claims description 8
- 241000186366 Mycobacterium bovis Species 0.000 claims description 7
- 241000186363 Mycobacterium kansasii Species 0.000 claims description 7
- 241000187489 Mycobacterium simiae Species 0.000 claims description 7
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 claims description 7
- 241000211133 Mycobacterium caprae Species 0.000 claims description 6
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 6
- 125000004685 alkoxythiocarbonyl group Chemical group 0.000 claims description 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 230000007547 defect Effects 0.000 claims description 6
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 6
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 6
- 150000003522 tetracyclines Chemical class 0.000 claims description 6
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims description 6
- 208000026350 Inborn Genetic disease Diseases 0.000 claims description 5
- 241000187494 Mycobacterium xenopi Species 0.000 claims description 5
- 210000000988 bone and bone Anatomy 0.000 claims description 5
- 229960002626 clarithromycin Drugs 0.000 claims description 5
- AGOYDEPGAOXOCK-KCBOHYOISA-N clarithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@](C)([C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)OC)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 AGOYDEPGAOXOCK-KCBOHYOISA-N 0.000 claims description 5
- 208000016361 genetic disease Diseases 0.000 claims description 5
- 230000001900 immune effect Effects 0.000 claims description 5
- 210000001165 lymph node Anatomy 0.000 claims description 5
- 208000014055 occupational lung disease Diseases 0.000 claims description 5
- 241001467553 Mycobacterium africanum Species 0.000 claims description 4
- 241000187482 Mycobacterium avium subsp. paratuberculosis Species 0.000 claims description 4
- 241000178954 Mycobacterium avium subsp. silvaticum Species 0.000 claims description 4
- 241001312372 Mycobacterium canettii Species 0.000 claims description 4
- 241000254210 Mycobacterium chimaera Species 0.000 claims description 4
- 241000419175 Mycobacterium colombiense Species 0.000 claims description 4
- 241001494992 Mycobacterium indicus pranii Species 0.000 claims description 4
- 241000186364 Mycobacterium intracellulare Species 0.000 claims description 4
- 241000186362 Mycobacterium leprae Species 0.000 claims description 4
- 241000187493 Mycobacterium malmoense Species 0.000 claims description 4
- 241000187492 Mycobacterium marinum Species 0.000 claims description 4
- 241000187919 Mycobacterium microti Species 0.000 claims description 4
- 241000699502 Mycobacterium mungi Species 0.000 claims description 4
- 241000656726 Mycobacterium orygis Species 0.000 claims description 4
- 241001457456 Mycobacterium pinnipedii Species 0.000 claims description 4
- 241000187490 Mycobacterium scrofulaceum Species 0.000 claims description 4
- 241000187644 Mycobacterium vaccae Species 0.000 claims description 4
- 206010062255 Soft tissue infection Diseases 0.000 claims description 4
- 229960004821 amikacin Drugs 0.000 claims description 4
- LKCWBDHBTVXHDL-RMDFUYIESA-N amikacin Chemical compound O([C@@H]1[C@@H](N)C[C@H]([C@@H]([C@H]1O)O[C@@H]1[C@@H]([C@@H](N)[C@H](O)[C@@H](CO)O1)O)NC(=O)[C@@H](O)CCN)[C@H]1O[C@H](CN)[C@@H](O)[C@H](O)[C@H]1O LKCWBDHBTVXHDL-RMDFUYIESA-N 0.000 claims description 4
- 210000000481 breast Anatomy 0.000 claims description 4
- 230000000747 cardiac effect Effects 0.000 claims description 4
- 230000001684 chronic effect Effects 0.000 claims description 4
- 229960000285 ethambutol Drugs 0.000 claims description 4
- 210000003709 heart valve Anatomy 0.000 claims description 4
- 238000001990 intravenous administration Methods 0.000 claims description 4
- UCSJYZPVAKXKNQ-HZYVHMACSA-N streptomycin Chemical compound CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@@H]1[C@](C=O)(O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](NC(N)=N)[C@H](O)[C@@H](NC(N)=N)[C@H](O)[C@H]1O UCSJYZPVAKXKNQ-HZYVHMACSA-N 0.000 claims description 4
- 238000002054 transplantation Methods 0.000 claims description 4
- 208000030507 AIDS Diseases 0.000 claims description 3
- 206010001881 Alveolar proteinosis Diseases 0.000 claims description 3
- 206010003504 Aspiration Diseases 0.000 claims description 3
- 206010006474 Bronchopulmonary aspergillosis allergic Diseases 0.000 claims description 3
- 208000025678 Ciliary Motility disease Diseases 0.000 claims description 3
- 208000031886 HIV Infections Diseases 0.000 claims description 3
- 208000037357 HIV infectious disease Diseases 0.000 claims description 3
- 102000013462 Interleukin-12 Human genes 0.000 claims description 3
- 108010065805 Interleukin-12 Proteins 0.000 claims description 3
- 208000029523 Interstitial Lung disease Diseases 0.000 claims description 3
- 241000513886 Mycobacterium avium complex (MAC) Species 0.000 claims description 3
- 241001175601 Mycobacterium sarraceniae Species 0.000 claims description 3
- 208000006778 allergic bronchopulmonary aspergillosis Diseases 0.000 claims description 3
- 238000011319 anticancer therapy Methods 0.000 claims description 3
- 229960004099 azithromycin Drugs 0.000 claims description 3
- MQTOSJVFKKJCRP-BICOPXKESA-N azithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)N(C)C[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 MQTOSJVFKKJCRP-BICOPXKESA-N 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 claims description 3
- 230000009395 genetic defect Effects 0.000 claims description 3
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims description 3
- 238000002650 immunosuppressive therapy Methods 0.000 claims description 3
- 108010085650 interferon gamma receptor Proteins 0.000 claims description 3
- 229940117681 interleukin-12 Drugs 0.000 claims description 3
- 230000002045 lasting effect Effects 0.000 claims description 3
- 210000000056 organ Anatomy 0.000 claims description 3
- 206010035653 pneumoconiosis Diseases 0.000 claims description 3
- 201000003489 pulmonary alveolar proteinosis Diseases 0.000 claims description 3
- 210000004872 soft tissue Anatomy 0.000 claims description 3
- 208000011580 syndromic disease Diseases 0.000 claims description 3
- MQJKPEGWNLWLTK-UHFFFAOYSA-N Dapsone Chemical compound C1=CC(N)=CC=C1S(=O)(=O)C1=CC=C(N)C=C1 MQJKPEGWNLWLTK-UHFFFAOYSA-N 0.000 claims description 2
- 241000836445 Mycobacterium abscessus subsp. abscessus Species 0.000 claims description 2
- 241001332087 Mycobacterium abscessus subsp. bolletii Species 0.000 claims description 2
- 241001105445 Mycobacterium abscessus subsp. massiliense Species 0.000 claims description 2
- 241001509442 Mycobacterium agri Species 0.000 claims description 2
- 241000187475 Mycobacterium aichiense Species 0.000 claims description 2
- 241000622918 Mycobacterium algericum Species 0.000 claims description 2
- 241001650273 Mycobacterium alsense Species 0.000 claims description 2
- 241000957223 Mycobacterium alvei Species 0.000 claims description 2
- 241001469010 Mycobacterium angelicum Species 0.000 claims description 2
- 241001453037 Mycobacterium anyangense Species 0.000 claims description 2
- 241000594851 Mycobacterium arabiense Species 0.000 claims description 2
- 241001318887 Mycobacterium aromaticivorans Species 0.000 claims description 2
- 241001368179 Mycobacterium arosiense Species 0.000 claims description 2
- 241000687894 Mycobacterium arupense Species 0.000 claims description 2
- 241000187474 Mycobacterium asiaticum Species 0.000 claims description 2
- 241001332085 Mycobacterium aubagnense Species 0.000 claims description 2
- 241000187473 Mycobacterium aurum Species 0.000 claims description 2
- 241000180044 Mycobacterium avium subsp. avium Species 0.000 claims description 2
- 241000114135 Mycobacterium avium subsp. hominissuis Species 0.000 claims description 2
- 241000871709 Mycobacterium bacteremicum Species 0.000 claims description 2
- 241001316387 Mycobacterium boenickei Species 0.000 claims description 2
- 241000567118 Mycobacterium bohemicum Species 0.000 claims description 2
- 241001662551 Mycobacterium botniense Species 0.000 claims description 2
- 241001378818 Mycobacterium bouchedurhonense Species 0.000 claims description 2
- 241000158042 Mycobacterium bourgelatii Species 0.000 claims description 2
- 241001467552 Mycobacterium bovis BCG Species 0.000 claims description 2
- 241000157299 Mycobacterium branderi Species 0.000 claims description 2
- 241001674312 Mycobacterium brumae Species 0.000 claims description 2
- 241000318680 Mycobacterium canariasense Species 0.000 claims description 2
- 241001134667 Mycobacterium celatum Species 0.000 claims description 2
- 241000826000 Mycobacterium celeriflavum Species 0.000 claims description 2
- 241000187472 Mycobacterium chitae Species 0.000 claims description 2
- 241000187913 Mycobacterium chubuense Species 0.000 claims description 2
- 241001134628 Mycobacterium confluentis Species 0.000 claims description 2
- 241000178318 Mycobacterium conspicuum Species 0.000 claims description 2
- 241000187487 Mycobacterium cookii Species 0.000 claims description 2
- 241001420379 Mycobacterium cosmeticum Species 0.000 claims description 2
- 241000559497 Mycobacterium crocinum Species 0.000 claims description 2
- 241000187912 Mycobacterium diernhoferi Species 0.000 claims description 2
- 241000587727 Mycobacterium doricum Species 0.000 claims description 2
- 241001532524 Mycobacterium duvalii Species 0.000 claims description 2
- 241001609973 Mycobacterium elephantis Species 0.000 claims description 2
- 241001139336 Mycobacterium engbaekii Species 0.000 claims description 2
- 241000252261 Mycobacterium europaeum Species 0.000 claims description 2
- 241000187471 Mycobacterium fallax Species 0.000 claims description 2
- 241000187486 Mycobacterium flavescens Species 0.000 claims description 2
- 241001136226 Mycobacterium florentinum Species 0.000 claims description 2
- 241001420342 Mycobacterium fluoranthenivorans Species 0.000 claims description 2
- 241001295721 Mycobacterium fortuitum subsp. acetamidolyticum Species 0.000 claims description 2
- 241001295730 Mycobacterium fortuitum subsp. fortuitum Species 0.000 claims description 2
- 241001447133 Mycobacterium fragae Species 0.000 claims description 2
- 241000690955 Mycobacterium franklinii Species 0.000 claims description 2
- 241000187470 Mycobacterium gadium Species 0.000 claims description 2
- 241000187485 Mycobacterium gastri Species 0.000 claims description 2
- 241000187910 Mycobacterium gilvum Species 0.000 claims description 2
- 241000936963 Mycobacterium goodii Species 0.000 claims description 2
- 241000187484 Mycobacterium gordonae Species 0.000 claims description 2
- 241001147828 Mycobacterium haemophilum Species 0.000 claims description 2
- 241000202700 Mycobacterium hassiacum Species 0.000 claims description 2
- 241000142650 Mycobacterium heckeshornense Species 0.000 claims description 2
- 241000520088 Mycobacterium heidelbergense Species 0.000 claims description 2
- 241001175599 Mycobacterium helvum Species 0.000 claims description 2
- 241000673373 Mycobacterium heraklionense Species 0.000 claims description 2
- 241001147834 Mycobacterium hiberniae Species 0.000 claims description 2
- 241000275248 Mycobacterium hippocampi Species 0.000 claims description 2
- 241001644172 Mycobacterium holsaticum Species 0.000 claims description 2
- 241001316369 Mycobacterium houstonense Species 0.000 claims description 2
- 241001086787 Mycobacterium icosiumassiliensis Species 0.000 claims description 2
- 241001646019 Mycobacterium immunogenum Species 0.000 claims description 2
- 241000437390 Mycobacterium insubricum Species 0.000 claims description 2
- 241001467535 Mycobacterium interjectum Species 0.000 claims description 2
- 241001136174 Mycobacterium intermedium Species 0.000 claims description 2
- 241001166087 Mycobacterium iranicum Species 0.000 claims description 2
- 241000640723 Mycobacterium komanii Species 0.000 claims description 2
- 241000187483 Mycobacterium komossense Species 0.000 claims description 2
- 241000459710 Mycobacterium koreense Species 0.000 claims description 2
- 241000516643 Mycobacterium kubicae Species 0.000 claims description 2
- 241001078572 Mycobacterium kumamotonense Species 0.000 claims description 2
- 241000272747 Mycobacterium kyorinense Species 0.000 claims description 2
- 241000439014 Mycobacterium lacus Species 0.000 claims description 2
- 241001248583 Mycobacterium lentiflavum Species 0.000 claims description 2
- 241000908167 Mycobacterium lepraemurium Species 0.000 claims description 2
- 241000178382 Mycobacterium lepromatosis Species 0.000 claims description 2
- 241000035554 Mycobacterium liflandii Species 0.000 claims description 2
- 241000755466 Mycobacterium llatzerense Species 0.000 claims description 2
- 241001234301 Mycobacterium lutetiense Species 0.000 claims description 2
- 241001553029 Mycobacterium madagascariense Species 0.000 claims description 2
- 241000520670 Mycobacterium mageritense Species 0.000 claims description 2
- 241000640725 Mycobacterium malmesburyense Species 0.000 claims description 2
- 241000821413 Mycobacterium mantenii Species 0.000 claims description 2
- 241001378821 Mycobacterium marseillense Species 0.000 claims description 2
- 241001662309 Mycobacterium minnesotense Species 0.000 claims description 2
- 241001673077 Mycobacterium monacense Species 0.000 claims description 2
- 241001532511 Mycobacterium moriokaense Species 0.000 claims description 2
- 241000557009 Mycobacterium mucogenicum Species 0.000 claims description 2
- 241001062465 Mycobacterium murale Species 0.000 claims description 2
- 241001013798 Mycobacterium nebraskense Species 0.000 claims description 2
- 241000187469 Mycobacterium neoaurum Species 0.000 claims description 2
- 241001316374 Mycobacterium neworleansense Species 0.000 claims description 2
- 241000187491 Mycobacterium nonchromogenicum Species 0.000 claims description 2
- 241000611872 Mycobacterium novocastrense Species 0.000 claims description 2
- 241000187918 Mycobacterium obuense Species 0.000 claims description 2
- 241001321752 Mycobacterium oryzae Species 0.000 claims description 2
- 241000103226 Mycobacterium pallens Species 0.000 claims description 2
- 241001659709 Mycobacterium palustre Species 0.000 claims description 2
- 241000327798 Mycobacterium paraense Species 0.000 claims description 2
- 241001532512 Mycobacterium parafortuitum Species 0.000 claims description 2
- 241000339390 Mycobacterium paragordonae Species 0.000 claims description 2
- 241000704107 Mycobacterium paraintracellulare Species 0.000 claims description 2
- 241000459708 Mycobacterium parakoreense Species 0.000 claims description 2
- 241000961132 Mycobacterium parascrofulaceum Species 0.000 claims description 2
- 241001269530 Mycobacterium paraterrae Species 0.000 claims description 2
- 241001101480 Mycobacterium parmense Species 0.000 claims description 2
- 241000187481 Mycobacterium phlei Species 0.000 claims description 2
- 241001332086 Mycobacterium phocaicum Species 0.000 claims description 2
- 241001532509 Mycobacterium porcinum Species 0.000 claims description 2
- 241001606460 Mycobacterium psychrotolerans Species 0.000 claims description 2
- 241001115881 Mycobacterium pyrenivorans Species 0.000 claims description 2
- 241001509458 Mycobacterium rhodesiae Species 0.000 claims description 2
- 241000256084 Mycobacterium riyadhense Species 0.000 claims description 2
- 241001318886 Mycobacterium rufum Species 0.000 claims description 2
- 241000103231 Mycobacterium rutilum Species 0.000 claims description 2
- 241000633217 Mycobacterium salmoniphilum Species 0.000 claims description 2
- 241001027257 Mycobacterium saopaulense Species 0.000 claims description 2
- 241000224454 Mycobacterium saskatchewanense Species 0.000 claims description 2
- 241000594848 Mycobacterium sediminis Species 0.000 claims description 2
- 241000187468 Mycobacterium senegalense Species 0.000 claims description 2
- 241000542761 Mycobacterium senuense Species 0.000 claims description 2
- 241000409180 Mycobacterium septicum Species 0.000 claims description 2
- 241000024083 Mycobacterium setense Species 0.000 claims description 2
- 241001002112 Mycobacterium sherrisii Species 0.000 claims description 2
- 241001147832 Mycobacterium shimoidei Species 0.000 claims description 2
- 241000944068 Mycobacterium shinjukuense Species 0.000 claims description 2
- 241000919916 Mycobacterium shottsii Species 0.000 claims description 2
- 241000383305 Mycobacterium sinense Species 0.000 claims description 2
- 241000187480 Mycobacterium smegmatis Species 0.000 claims description 2
- 241000187497 Mycobacterium sphagni Species 0.000 claims description 2
- 241001093674 Mycobacterium suricattae Species 0.000 claims description 2
- 241000187496 Mycobacterium szulgai Species 0.000 claims description 2
- 241000187495 Mycobacterium terrae Species 0.000 claims description 2
- 241000187477 Mycobacterium thermoresistibile Species 0.000 claims description 2
- 241001378820 Mycobacterium timonense Species 0.000 claims description 2
- 241001532502 Mycobacterium tokaiense Species 0.000 claims description 2
- 241000218972 Mycobacterium triplex Species 0.000 claims description 2
- 241000187476 Mycobacterium triviale Species 0.000 claims description 2
- 241001072371 Mycobacterium tuberculosis subsp. tuberculosis Species 0.000 claims description 2
- 241001293520 Mycobacterium tusciae Species 0.000 claims description 2
- 241000187917 Mycobacterium ulcerans Species 0.000 claims description 2
- 241000142559 Mycobacterium vanbaalenii Species 0.000 claims description 2
- 241001154668 Mycobacterium virginiense Species 0.000 claims description 2
- 241000163206 Mycobacterium vulneris Species 0.000 claims description 2
- 241000611277 Mycobacterium wolinskyi Species 0.000 claims description 2
- 241000969523 Mycobacterium yongonense Species 0.000 claims description 2
- 229960004287 clofazimine Drugs 0.000 claims description 2
- WDQPAMHFFCXSNU-BGABXYSRSA-N clofazimine Chemical compound C12=CC=CC=C2N=C2C=C(NC=3C=CC(Cl)=CC=3)C(=N/C(C)C)/C=C2N1C1=CC=C(Cl)C=C1 WDQPAMHFFCXSNU-BGABXYSRSA-N 0.000 claims description 2
- 229960000860 dapsone Drugs 0.000 claims description 2
- TYZROVQLWOKYKF-ZDUSSCGKSA-N linezolid Chemical compound O=C1O[C@@H](CNC(=O)C)CN1C(C=C1F)=CC=C1N1CCOCC1 TYZROVQLWOKYKF-ZDUSSCGKSA-N 0.000 claims description 2
- 229960003907 linezolid Drugs 0.000 claims description 2
- 206010040872 skin infection Diseases 0.000 claims description 2
- 229960005322 streptomycin Drugs 0.000 claims description 2
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 75
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 239000000443 aerosol Substances 0.000 claims 3
- HBUJYEUPIIJJOS-PBHICJAKSA-N (5r)-3-[4-[1-[(2s)-2,3-dihydroxypropanoyl]-3,6-dihydro-2h-pyridin-4-yl]-3,5-difluorophenyl]-5-(1,2-oxazol-3-yloxymethyl)-1,3-oxazolidin-2-one Chemical compound C1N(C(=O)[C@@H](O)CO)CCC(C=2C(=CC(=CC=2F)N2C(O[C@@H](COC3=NOC=C3)C2)=O)F)=C1 HBUJYEUPIIJJOS-PBHICJAKSA-N 0.000 claims 2
- 208000035484 Cellulite Diseases 0.000 claims 2
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 206010049752 Peau d'orange Diseases 0.000 claims 2
- 239000004479 aerosol dispenser Substances 0.000 claims 2
- 229940034014 antimycobacterial agent Drugs 0.000 claims 2
- 239000003926 antimycobacterial agent Substances 0.000 claims 2
- 230000036232 cellulite Effects 0.000 claims 2
- 238000012423 maintenance Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims 2
- BISOEENGZHMDEO-RLXIHFJVSA-N (2s,3s,4s)-2-[(1r)-2-amino-1-[(2s,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-4-hydroxy-3-methoxyoxolan-2-yl]-2-oxoethoxy]-3,4-dihydroxy-n-[(3s)-2-oxoazepan-3-yl]-3,4-dihydro-2h-pyran-6-carboxamide Chemical compound O([C@@H]([C@H]([C@@H](O)C=1)O)O[C@H]([C@H]2O[C@H]([C@H](O)[C@@H]2OC)N2C(NC(=O)C=C2)=O)C(N)=O)C=1C(=O)N[C@H]1CCCCNC1=O BISOEENGZHMDEO-RLXIHFJVSA-N 0.000 claims 1
- VCOPTHOUUNAYKQ-WBTCAYNUSA-N (3s)-3,6-diamino-n-[[(2s,5s,8e,11s,15s)-15-amino-11-[(6r)-2-amino-1,4,5,6-tetrahydropyrimidin-6-yl]-8-[(carbamoylamino)methylidene]-2-(hydroxymethyl)-3,6,9,12,16-pentaoxo-1,4,7,10,13-pentazacyclohexadec-5-yl]methyl]hexanamide;(3s)-3,6-diamino-n-[[(2s,5s,8 Chemical compound N1C(=O)\C(=C/NC(N)=O)NC(=O)[C@H](CNC(=O)C[C@@H](N)CCCN)NC(=O)[C@H](C)NC(=O)[C@@H](N)CNC(=O)[C@@H]1[C@@H]1NC(N)=NCC1.N1C(=O)\C(=C/NC(N)=O)NC(=O)[C@H](CNC(=O)C[C@@H](N)CCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CNC(=O)[C@@H]1[C@@H]1NC(N)=NCC1 VCOPTHOUUNAYKQ-WBTCAYNUSA-N 0.000 claims 1
- RXZBMPWDPOLZGW-XMRMVWPWSA-N (E)-roxithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=N/OCOCCOC)/[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 RXZBMPWDPOLZGW-XMRMVWPWSA-N 0.000 claims 1
- XUBOMFCQGDBHNK-JTQLQIEISA-N (S)-gatifloxacin Chemical compound FC1=CC(C(C(C(O)=O)=CN2C3CC3)=O)=C2C(OC)=C1N1CCN[C@@H](C)C1 XUBOMFCQGDBHNK-JTQLQIEISA-N 0.000 claims 1
- NSYKYZBOQLCIHR-UHFFFAOYSA-N 2-nitro-1,3-benzothiazole Chemical compound C1=CC=C2SC([N+](=O)[O-])=NC2=C1 NSYKYZBOQLCIHR-UHFFFAOYSA-N 0.000 claims 1
- YZEUHQHUFTYLPH-UHFFFAOYSA-N 2-nitroimidazole Chemical compound [O-][N+](=O)C1=NC=CN1 YZEUHQHUFTYLPH-UHFFFAOYSA-N 0.000 claims 1
- MJNPHLBKHKJDEF-UHFFFAOYSA-N 2h-1$l^{4},2-benzothiazine 1-oxide Chemical compound C1=CC=C2S(=O)NC=CC2=C1 MJNPHLBKHKJDEF-UHFFFAOYSA-N 0.000 claims 1
- WUBBRNOQWQTFEX-UHFFFAOYSA-N 4-aminosalicylic acid Chemical compound NC1=CC=C(C(O)=O)C(O)=C1 WUBBRNOQWQTFEX-UHFFFAOYSA-N 0.000 claims 1
- 101710081722 Antitrypsin Proteins 0.000 claims 1
- 241000283707 Capra Species 0.000 claims 1
- 108010065839 Capreomycin Proteins 0.000 claims 1
- 241000700199 Cavia porcellus Species 0.000 claims 1
- DYDCUQKUCUHJBH-UWTATZPHSA-N D-Cycloserine Chemical compound N[C@@H]1CONC1=O DYDCUQKUCUHJBH-UWTATZPHSA-N 0.000 claims 1
- DYDCUQKUCUHJBH-UHFFFAOYSA-N D-Cycloserine Natural products NC1CONC1=O DYDCUQKUCUHJBH-UHFFFAOYSA-N 0.000 claims 1
- 241000282326 Felis catus Species 0.000 claims 1
- 206010061598 Immunodeficiency Diseases 0.000 claims 1
- GSDSWSVVBLHKDQ-JTQLQIEISA-N Levofloxacin Chemical compound C([C@@H](N1C2=C(C(C(C(O)=O)=C1)=O)C=C1F)C)OC2=C1N1CCN(C)CC1 GSDSWSVVBLHKDQ-JTQLQIEISA-N 0.000 claims 1
- 241000699666 Mus <mouse, genus> Species 0.000 claims 1
- 241001524108 Mycobacterium chlorophenolicum Species 0.000 claims 1
- 241001280523 Mycobacterium longobardum Species 0.000 claims 1
- 241001494479 Pecora Species 0.000 claims 1
- KLBQZWRITKRQQV-UHFFFAOYSA-N Thioridazine Chemical compound C12=CC(SC)=CC=C2SC2=CC=CC=C2N1CCC1CCCCN1C KLBQZWRITKRQQV-UHFFFAOYSA-N 0.000 claims 1
- QXHKKCITURTUFC-UHFFFAOYSA-N [1,2]thiazolo[3,4-h]quinoline 8-oxide Chemical compound C1=CN=C2C3=CS(=O)N=C3C=CC2=C1 QXHKKCITURTUFC-UHFFFAOYSA-N 0.000 claims 1
- 229960004909 aminosalicylic acid Drugs 0.000 claims 1
- 230000001475 anti-trypsic effect Effects 0.000 claims 1
- 229960004602 capreomycin Drugs 0.000 claims 1
- 229960003077 cycloserine Drugs 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 229960003276 erythromycin Drugs 0.000 claims 1
- 229960003923 gatifloxacin Drugs 0.000 claims 1
- 229960000318 kanamycin Drugs 0.000 claims 1
- 229930027917 kanamycin Natural products 0.000 claims 1
- SBUJHOSQTJFQJX-NOAMYHISSA-N kanamycin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CN)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](N)[C@H](O)[C@@H](CO)O2)O)[C@H](N)C[C@@H]1N SBUJHOSQTJFQJX-NOAMYHISSA-N 0.000 claims 1
- 229930182823 kanamycin A Natural products 0.000 claims 1
- 229960003376 levofloxacin Drugs 0.000 claims 1
- 229960003702 moxifloxacin Drugs 0.000 claims 1
- FABPRXSRWADJSP-MEDUHNTESA-N moxifloxacin Chemical compound COC1=C(N2C[C@H]3NCCC[C@H]3C2)C(F)=CC(C(C(C(O)=O)=C2)=O)=C1N2C1CC1 FABPRXSRWADJSP-MEDUHNTESA-N 0.000 claims 1
- 239000002777 nucleoside Substances 0.000 claims 1
- 229950004447 posizolid Drugs 0.000 claims 1
- SGHWBDUXKUSFOP-KYALZUAASA-N rifalazil Chemical compound O([C@](C1=O)(C)O/C=C/[C@@H]([C@H]([C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(C)/C(=O)N=C2C(=O)C=3C(O)=C4C)C)OC)C4=C1C=3C(NC1=C(O)C=3)=C2OC1=CC=3N1CCN(CC(C)C)CC1 SGHWBDUXKUSFOP-KYALZUAASA-N 0.000 claims 1
- 229950005007 rifalazil Drugs 0.000 claims 1
- WDZCUPBHRAEYDL-GZAUEHORSA-N rifapentine Chemical compound O([C@](C1=O)(C)O/C=C/[C@@H]([C@H]([C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(C)/C(=O)NC=2C(O)=C3C(O)=C4C)C)OC)C4=C1C3=C(O)C=2\C=N\N(CC1)CCN1C1CCCC1 WDZCUPBHRAEYDL-GZAUEHORSA-N 0.000 claims 1
- 229960005224 roxithromycin Drugs 0.000 claims 1
- 238000009097 single-agent therapy Methods 0.000 claims 1
- FNDDDNOJWPQCBZ-ZDUSSCGKSA-N sutezolid Chemical compound O=C1O[C@@H](CNC(=O)C)CN1C(C=C1F)=CC=C1N1CCSCC1 FNDDDNOJWPQCBZ-ZDUSSCGKSA-N 0.000 claims 1
- 229960003250 telithromycin Drugs 0.000 claims 1
- LJVAJPDWBABPEJ-PNUFFHFMSA-N telithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)[C@@H](C)C(=O)O[C@@H]([C@]2(OC(=O)N(CCCCN3C=C(N=C3)C=3C=NC=CC=3)[C@@H]2[C@@H](C)C(=O)[C@H](C)C[C@@]1(C)OC)C)CC)[C@@H]1O[C@H](C)C[C@H](N(C)C)[C@H]1O LJVAJPDWBABPEJ-PNUFFHFMSA-N 0.000 claims 1
- SRVJKTDHMYAMHA-WUXMJOGZSA-N thioacetazone Chemical compound CC(=O)NC1=CC=C(\C=N\NC(N)=S)C=C1 SRVJKTDHMYAMHA-WUXMJOGZSA-N 0.000 claims 1
- 229960003231 thioacetazone Drugs 0.000 claims 1
- 229960002784 thioridazine Drugs 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 239000002753 trypsin inhibitor Substances 0.000 claims 1
- 150000003573 thiols Chemical group 0.000 description 75
- VJYKVCURWJGLPG-IQZGDKDPSA-N Omadacycline Chemical compound C1C2=C(N(C)C)C=C(CNCC(C)(C)C)C(O)=C2C(O)=C2[C@@H]1C[C@H]1[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]1(O)C2=O VJYKVCURWJGLPG-IQZGDKDPSA-N 0.000 description 63
- SOVUOXKZCCAWOJ-HJYUBDRYSA-N (4s,4as,5ar,12ar)-9-[[2-(tert-butylamino)acetyl]amino]-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1C2=C(N(C)C)C=C(NC(=O)CNC(C)(C)C)C(O)=C2C(O)=C2[C@@H]1C[C@H]1[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]1(O)C2=O SOVUOXKZCCAWOJ-HJYUBDRYSA-N 0.000 description 15
- 229960004089 tigecycline Drugs 0.000 description 15
- 239000003242 anti bacterial agent Substances 0.000 description 8
- 229940088710 antibiotic agent Drugs 0.000 description 8
- 206010047700 Vomiting Diseases 0.000 description 5
- 206010018691 Granuloma Diseases 0.000 description 4
- 239000003120 macrolide antibiotic agent Substances 0.000 description 4
- 229960004023 minocycline Drugs 0.000 description 4
- JQXXHWHPUNPDRT-WLSIYKJHSA-N rifampicin Chemical compound O([C@](C1=O)(C)O/C=C/[C@@H]([C@H]([C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(C)/C(=O)NC=2C(O)=C3C([O-])=C4C)C)OC)C4=C1C3=C(O)C=2\C=N\N1CC[NH+](C)CC1 JQXXHWHPUNPDRT-WLSIYKJHSA-N 0.000 description 4
- 229960001225 rifampicin Drugs 0.000 description 4
- FFTVPQUHLQBXQZ-KVUCHLLUSA-N (4s,4as,5ar,12ar)-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1C2=C(N(C)C)C=CC(O)=C2C(O)=C2[C@@H]1C[C@H]1[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]1(O)C2=O FFTVPQUHLQBXQZ-KVUCHLLUSA-N 0.000 description 3
- 125000000174 L-prolyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(*)=O 0.000 description 3
- 210000004027 cell Anatomy 0.000 description 3
- 210000002540 macrophage Anatomy 0.000 description 3
- FELGMEQIXOGIFQ-CYBMUJFWSA-N (3r)-9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1h-carbazol-4-one Chemical compound CC1=NC=CN1C[C@@H]1C(=O)C(C=2C(=CC=CC=2)N2C)=C2CC1 FELGMEQIXOGIFQ-CYBMUJFWSA-N 0.000 description 2
- SGKRLCUYIXIAHR-AKNGSSGZSA-N (4s,4ar,5s,5ar,6r,12ar)-4-(dimethylamino)-1,5,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1=CC=C2[C@H](C)[C@@H]([C@H](O)[C@@H]3[C@](C(O)=C(C(N)=O)C(=O)[C@H]3N(C)C)(O)C3=O)C3=C(O)C2=C1O SGKRLCUYIXIAHR-AKNGSSGZSA-N 0.000 description 2
- 206010007882 Cellulitis Diseases 0.000 description 2
- 241000187479 Mycobacterium tuberculosis Species 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- 210000001132 alveolar macrophage Anatomy 0.000 description 2
- 230000003115 biocidal effect Effects 0.000 description 2
- 231100000676 disease causative agent Toxicity 0.000 description 2
- 229960003722 doxycycline Drugs 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 229960005343 ondansetron Drugs 0.000 description 2
- 210000003491 skin Anatomy 0.000 description 2
- 125000004898 2,2-dimethylpropylamino group Chemical group CC(CN*)(C)C 0.000 description 1
- 241000251468 Actinopterygii Species 0.000 description 1
- 241000304886 Bacilli Species 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 241000236488 Lepra Species 0.000 description 1
- 208000032376 Lung infection Diseases 0.000 description 1
- 241000168058 Mycobacterium peregrinum Species 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- 102100035107 Neurotrimin Human genes 0.000 description 1
- 208000011623 Obstructive Lung disease Diseases 0.000 description 1
- 208000005141 Otitis Diseases 0.000 description 1
- 206010052428 Wound Diseases 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- JEECQCWWSTZDCK-XRPYGRFESA-N [H][C@@]12CC3=C(C=C(CNCC(C)(C)C)C(O)=C3C(=O)C1=C(O)[C@]1(O)C(=O)C(C(N)=O)=C(O)C(N(C)C)[C@]1([H])C2)N(C)C Chemical group [H][C@@]12CC3=C(C=C(CNCC(C)(C)C)C(O)=C3C(=O)C1=C(O)[C@]1(O)C(=O)C(C(N)=O)=C(O)C(N(C)C)[C@]1([H])C2)N(C)C JEECQCWWSTZDCK-XRPYGRFESA-N 0.000 description 1
- 206010000269 abscess Diseases 0.000 description 1
- 208000022531 anorexia Diseases 0.000 description 1
- 230000003474 anti-emetic effect Effects 0.000 description 1
- 229940125683 antiemetic agent Drugs 0.000 description 1
- 239000002111 antiemetic agent Substances 0.000 description 1
- 230000002238 attenuated effect Effects 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- WZOZEZRFJCJXNZ-ZBFHGGJFSA-N cefoxitin Chemical compound N([C@]1(OC)C(N2C(=C(COC(N)=O)CS[C@@H]21)C(O)=O)=O)C(=O)CC1=CC=CS1 WZOZEZRFJCJXNZ-ZBFHGGJFSA-N 0.000 description 1
- 229960002682 cefoxitin Drugs 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 210000000038 chest Anatomy 0.000 description 1
- 229940125904 compound 1 Drugs 0.000 description 1
- 206010061428 decreased appetite Diseases 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 208000019258 ear infection Diseases 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 208000010758 granulomatous inflammation Diseases 0.000 description 1
- 244000052637 human pathogen Species 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 229960003350 isoniazid Drugs 0.000 description 1
- QRXWMOHMRWLFEY-UHFFFAOYSA-N isoniazide Chemical compound NNC(=O)C1=CC=NC=C1 QRXWMOHMRWLFEY-UHFFFAOYSA-N 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000013508 migration Methods 0.000 description 1
- 230000005012 migration Effects 0.000 description 1
- 230000001459 mortal effect Effects 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 230000000149 penetrating effect Effects 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 201000009266 primary ciliary dyskinesia Diseases 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 229960005206 pyrazinamide Drugs 0.000 description 1
- IPEHBUMCGVEMRF-UHFFFAOYSA-N pyrazinecarboxamide Chemical compound NC(=O)C1=CN=CC=N1 IPEHBUMCGVEMRF-UHFFFAOYSA-N 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 238000011272 standard treatment Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000008673 vomiting 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
- A61K31/65—Tetracyclines
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/08—Antibacterial agents for leprosy
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862726738P | 2018-09-04 | 2018-09-04 | |
| US62/726,738 | 2018-09-04 | ||
| US201862731410P | 2018-09-14 | 2018-09-14 | |
| US62/731,410 | 2018-09-14 | ||
| US201862746039P | 2018-10-16 | 2018-10-16 | |
| US62/746,039 | 2018-10-16 | ||
| US201862760131P | 2018-11-13 | 2018-11-13 | |
| US62/760,131 | 2018-11-13 | ||
| PCT/US2019/049368 WO2020051151A1 (en) | 2018-09-04 | 2019-09-03 | Methods of treating mycobacterial infections using tetracycline compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112021004057A2 true BR112021004057A2 (pt) | 2021-05-25 |
Family
ID=69722600
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112021004057-9A BR112021004057A2 (pt) | 2018-09-04 | 2019-09-03 | métodos de tratar ou prevenir uma infecção micobacteriana, de tratar ou prevenir, de controlar ou reduzir o avanço, severidade ou efeitos de uma doença micobacteriana, tuberculose, lepra, bronquiectasia, doença pulmonar cavitária, linfadenite, uma doença de tecido mole, granuloma de aquário, úlcera de buruli, uma doença ocular e doença óssea em um indivíduo em necessidade dos mesmos, e, métodos de tratar um indivíduo com uma doença pulmonar e de tratar um indivíduo com uma condição imunossuprimida. |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US12161655B2 (https=) |
| EP (1) | EP3846805A4 (https=) |
| JP (2) | JP7466544B2 (https=) |
| KR (2) | KR20260036400A (https=) |
| CN (1) | CN113164456A (https=) |
| AU (2) | AU2019335203B2 (https=) |
| BR (1) | BR112021004057A2 (https=) |
| CA (1) | CA3111447A1 (https=) |
| MA (1) | MA53564A (https=) |
| MX (2) | MX2021002503A (https=) |
| PH (1) | PH12021550452A1 (https=) |
| SG (1) | SG11202102149SA (https=) |
| WO (1) | WO2020051151A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7840880B2 (ja) * | 2020-06-11 | 2026-04-06 | 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 | オマダサイクリンの結晶形態、その合成方法及びその使用方法 |
| TW202237116A (zh) * | 2020-12-02 | 2022-10-01 | 日商塩野義製藥股份有限公司 | 以組合細胞色素bc1抑制劑與克拉黴素或阿奇黴素為特徵之用於治療分枝桿菌感染之藥物 |
| JP2024511419A (ja) * | 2021-03-24 | 2024-03-13 | インスメッド インコーポレイテッド | 非結核性抗酸菌肺疾患を治療するための併用療法 |
| WO2025221846A1 (en) * | 2024-04-18 | 2025-10-23 | St. Jude Children's Research Hospital, Inc. | Compositions and methods for treating non-tuberculosis mycobacteria infections |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA009175B1 (ru) | 2000-07-07 | 2007-12-28 | Трастис Оф Тафтс Коллидж | Замещенные соединения миноциклина, фармацевтическая композиция и способ лечения чувствительного к тетрациклину состояния млекопитающего |
| US7553828B2 (en) | 2001-03-13 | 2009-06-30 | Paratek Pharmaceuticals, Inc. | 9-aminomethyl substituted minocycline compounds |
| US20060194773A1 (en) | 2001-07-13 | 2006-08-31 | Paratek Pharmaceuticals, Inc. | Tetracyline compounds having target therapeutic activities |
| EP2311451A1 (en) | 2002-03-08 | 2011-04-20 | Paratek Pharmaceuticals, Inc. | Amino-methyl substituted tetracycline compounds |
| PT2271348T (pt) * | 2008-03-28 | 2018-04-16 | Paratek Pharm Innc | Formulação de comprimido oral de composto de tetraciclina |
| TWI680117B (zh) | 2008-05-19 | 2019-12-21 | 派洛泰克藥物股份有限公司 | 四環素化合物之甲苯磺酸鹽及同素異形體 |
| KR101732084B1 (ko) | 2011-07-26 | 2017-05-02 | 케이비피 바이오사이언시즈 씨오., 엘티디. | 9-아미노메틸 치환된 테트라사이클린 화합물 |
| JP2015527403A (ja) | 2012-09-11 | 2015-09-17 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | Hivプロテアーゼ阻害剤 |
| CA3018872A1 (en) * | 2016-03-24 | 2017-09-28 | Paratek Pharmaceuticals, Inc. | Methods of treating a bacterial infection in a subject at risk of developing c. difficile infection |
| JP2019514952A (ja) * | 2016-05-02 | 2019-06-06 | 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 | 9−アミノメチルミノサイクリン化合物及び尿路感染症(uti)の処置におけるその使用方法 |
| TW202206081A (zh) * | 2016-08-03 | 2022-02-16 | 美商派瑞泰Spv2有限公司 | 9—胺甲基米諾四環素化合物及其用途 |
| GB201615693D0 (en) * | 2016-09-15 | 2016-11-02 | Combinatorx Infection Ltd | Combinations |
-
2019
- 2019-09-03 EP EP19858573.9A patent/EP3846805A4/en active Pending
- 2019-09-03 US US17/273,034 patent/US12161655B2/en active Active
- 2019-09-03 AU AU2019335203A patent/AU2019335203B2/en active Active
- 2019-09-03 BR BR112021004057-9A patent/BR112021004057A2/pt unknown
- 2019-09-03 MA MA053564A patent/MA53564A/fr unknown
- 2019-09-03 KR KR1020267005925A patent/KR20260036400A/ko active Pending
- 2019-09-03 CN CN201980072989.8A patent/CN113164456A/zh active Pending
- 2019-09-03 CA CA3111447A patent/CA3111447A1/en active Pending
- 2019-09-03 KR KR1020217009806A patent/KR102933150B1/ko active Active
- 2019-09-03 SG SG11202102149SA patent/SG11202102149SA/en unknown
- 2019-09-03 WO PCT/US2019/049368 patent/WO2020051151A1/en not_active Ceased
- 2019-09-03 MX MX2021002503A patent/MX2021002503A/es unknown
- 2019-09-03 JP JP2021536672A patent/JP7466544B2/ja active Active
-
2021
- 2021-03-02 MX MX2024008671A patent/MX2024008671A/es unknown
- 2021-03-03 PH PH12021550452A patent/PH12021550452A1/en unknown
-
2024
- 2024-04-02 JP JP2024059527A patent/JP2024084794A/ja active Pending
- 2024-10-30 US US18/932,596 patent/US20250332178A1/en active Pending
-
2025
- 2025-09-18 AU AU2025234215A patent/AU2025234215A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP2021536504A (ja) | 2021-12-27 |
| US20210346408A1 (en) | 2021-11-11 |
| EP3846805A1 (en) | 2021-07-14 |
| CN113164456A (zh) | 2021-07-23 |
| US20250332178A1 (en) | 2025-10-30 |
| US12161655B2 (en) | 2024-12-10 |
| MX2021002503A (es) | 2021-06-15 |
| AU2025234215A1 (en) | 2025-10-16 |
| KR20260036400A (ko) | 2026-03-16 |
| AU2019335203B2 (en) | 2025-06-19 |
| KR102933150B1 (ko) | 2026-03-03 |
| EP3846805A4 (en) | 2022-08-24 |
| MA53564A (fr) | 2021-07-14 |
| WO2020051151A1 (en) | 2020-03-12 |
| SG11202102149SA (en) | 2021-04-29 |
| PH12021550452A1 (en) | 2021-12-06 |
| MX2024008671A (es) | 2024-07-23 |
| JP2024084794A (ja) | 2024-06-25 |
| CA3111447A1 (en) | 2020-03-12 |
| KR20210090160A (ko) | 2021-07-19 |
| AU2019335203A1 (en) | 2021-05-06 |
| JP7466544B2 (ja) | 2024-04-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US20250332178A1 (en) | Methods of treating mycobacterial infections using tetracycline compounds | |
| Metcalf et al. | Use of ethanol locks to prevent recurrent central line sepsis | |
| US11116765B2 (en) | Liposomal ciprofloxacin formulations with activity against non-tuberculous mycobacteria | |
| JP5469511B2 (ja) | 微生物の院内感染症の治療用医薬の製造におけるタウロリジンまたはタウラルタムのような抗微生物薬剤の使用 | |
| JP5619352B2 (ja) | 細菌を処置するための組成物および方法 | |
| EP1077718B1 (en) | Enhancement of oxazolidinone antibacterial agents activity by arginine derivatives | |
| CN106456551A (zh) | 冻融后形成药物纳米晶体的脂质体 | |
| TWI419690B (zh) | 使用化合物i來預防或治療生物膜的形成 | |
| US20190274978A1 (en) | Antibacterial compositions | |
| JP2012501349A (ja) | オリタバンシンの単回用量を用いる治療の方法 | |
| US20200046653A1 (en) | Iron chelator therapy method | |
| US20190307744A1 (en) | Pharmaceutical compositions comprising clofazimine analog compound b746 or clofazimine analog compound b826 | |
| JP2002500189A5 (https=) | ||
| ES2690725T3 (es) | Composiciones que comprenden cefepima y tazobactam | |
| US20130338233A1 (en) | Methods for microbial biofilm destruction | |
| JP5276653B2 (ja) | カルバペネム類を含む殺菌性抗mrsa活性医薬組成物 | |
| PT1663233E (pt) | Utilização de tigeciclina isolada ou em combinação com rifampina para o tratamento de osteomielite e/ou artrite séptica | |
| RU2831120C2 (ru) | Способы лечения микобактериальных инфекций с применением тетрациклиновых соединений | |
| Amangeldykyzy et al. | The effect of a combined choline salicylate and cetalkonium chloride gel on particular strains of Pseudomonas aeruginosa, Staphylococcus spp. and Streptococcus spp. | |
| CN114617886A (zh) | 化合物及其药学上可接受的盐的抗菌用途 | |
| WO2024175768A1 (en) | Combination of fabi inhibitor and antibiotic agent | |
| Muggleton | Why Cefuroxime? | |
| JP2003525298A (ja) | 抗−感染性ectatm | |
| Session | I92-MAY 1978 o |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06W | Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette] |