JP2015528468A5 - - Google Patents
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- Publication number
- JP2015528468A5 JP2015528468A5 JP2015530126A JP2015530126A JP2015528468A5 JP 2015528468 A5 JP2015528468 A5 JP 2015528468A5 JP 2015530126 A JP2015530126 A JP 2015530126A JP 2015530126 A JP2015530126 A JP 2015530126A JP 2015528468 A5 JP2015528468 A5 JP 2015528468A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- alkyl
- heterocyclyl
- carbocyclyl
- hydrogen
- 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.)
- Granted
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims 34
- 239000001257 hydrogen Substances 0.000 claims 34
- 239000008194 pharmaceutical composition Substances 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 29
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 22
- 125000000623 heterocyclic group Chemical group 0.000 claims 17
- 229910052799 carbon Inorganic materials 0.000 claims 16
- 125000004432 carbon atom Chemical group C* 0.000 claims 13
- 125000005843 halogen group Chemical group 0.000 claims 13
- 208000015181 infectious disease Diseases 0.000 claims 13
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 125000004452 carbocyclyl group Chemical group 0.000 claims 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 10
- 125000001153 fluoro group Chemical group F* 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000004429 atom Chemical group 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 125000001309 chloro group Chemical group Cl* 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 208000035473 Communicable disease Diseases 0.000 claims 3
- 241000202934 Mycoplasma pneumoniae Species 0.000 claims 3
- 206010057190 Respiratory tract infections Diseases 0.000 claims 3
- 241000193996 Streptococcus pyogenes Species 0.000 claims 3
- -1 fluoro compound Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 206010040872 skin infection Diseases 0.000 claims 3
- 241000894007 species Species 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 241001156739 Actinobacteria <phylum> Species 0.000 claims 2
- 241000193830 Bacillus <bacterium> Species 0.000 claims 2
- 241000894006 Bacteria Species 0.000 claims 2
- 241001112696 Clostridia Species 0.000 claims 2
- 108010065152 Coagulase Proteins 0.000 claims 2
- 241000194032 Enterococcus faecalis Species 0.000 claims 2
- 241000194031 Enterococcus faecium Species 0.000 claims 2
- 241000606768 Haemophilus influenzae Species 0.000 claims 2
- 241000589242 Legionella pneumophila Species 0.000 claims 2
- 241000588655 Moraxella catarrhalis Species 0.000 claims 2
- 241000186359 Mycobacterium Species 0.000 claims 2
- 241000295644 Staphylococcaceae Species 0.000 claims 2
- 241000193985 Streptococcus agalactiae Species 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 229940115932 legionella pneumophila Drugs 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 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 claims 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- ITHCSGCUQDMYAI-ZMIZWQJLSA-N 2-carboxy-D-arabinitol 1,5-bisphosphate Chemical compound OP(=O)(O)OC[C@@H](O)[C@@H](O)[C@](O)(COP(O)(O)=O)C(O)=O ITHCSGCUQDMYAI-ZMIZWQJLSA-N 0.000 claims 1
- 241000589291 Acinetobacter Species 0.000 claims 1
- 108700042778 Antimicrobial Peptides Proteins 0.000 claims 1
- 102000044503 Antimicrobial Peptides Human genes 0.000 claims 1
- 241000304886 Bacilli Species 0.000 claims 1
- 241000606125 Bacteroides Species 0.000 claims 1
- 241000589968 Borrelia Species 0.000 claims 1
- 241000589876 Campylobacter Species 0.000 claims 1
- 241001185363 Chlamydiae Species 0.000 claims 1
- 241000498849 Chlamydiales Species 0.000 claims 1
- 241000193403 Clostridium Species 0.000 claims 1
- 241000186216 Corynebacterium Species 0.000 claims 1
- 241000588921 Enterobacteriaceae Species 0.000 claims 1
- 241000194033 Enterococcus Species 0.000 claims 1
- 241000589989 Helicobacter Species 0.000 claims 1
- 241000589248 Legionella Species 0.000 claims 1
- 208000007764 Legionnaires' Disease Diseases 0.000 claims 1
- 241000186781 Listeria Species 0.000 claims 1
- 208000016604 Lyme disease Diseases 0.000 claims 1
- RJQXTJLFIWVMTO-TYNCELHUSA-N Methicillin Chemical compound COC1=CC=CC(OC)=C1C(=O)N[C@@H]1C(=O)N2[C@@H](C(O)=O)C(C)(C)S[C@@H]21 RJQXTJLFIWVMTO-TYNCELHUSA-N 0.000 claims 1
- 241001430197 Mollicutes Species 0.000 claims 1
- 241000589289 Moraxellaceae Species 0.000 claims 1
- 241000187479 Mycobacterium tuberculosis Species 0.000 claims 1
- 241000204031 Mycoplasma Species 0.000 claims 1
- 241000204003 Mycoplasmatales Species 0.000 claims 1
- 241000187654 Nocardia Species 0.000 claims 1
- 241000606752 Pasteurellaceae Species 0.000 claims 1
- 206010035664 Pneumonia Diseases 0.000 claims 1
- 241000186429 Propionibacterium Species 0.000 claims 1
- 102100021486 Protein S100-G Human genes 0.000 claims 1
- 101710122252 Protein S100-G Proteins 0.000 claims 1
- 241000606651 Rickettsiales Species 0.000 claims 1
- 241000589973 Spirochaeta Species 0.000 claims 1
- 241000589970 Spirochaetales Species 0.000 claims 1
- 241000191940 Staphylococcus Species 0.000 claims 1
- 241000194017 Streptococcus Species 0.000 claims 1
- 239000004098 Tetracycline Substances 0.000 claims 1
- 241000589886 Treponema Species 0.000 claims 1
- 108010059993 Vancomycin Proteins 0.000 claims 1
- 241000607493 Vibrionaceae Species 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- 230000001580 bacterial effect Effects 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940124307 fluoroquinolone Drugs 0.000 claims 1
- 229940041010 fourth-generation cephalosporins Drugs 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229960003085 meticillin Drugs 0.000 claims 1
- 239000000178 monomer Substances 0.000 claims 1
- 239000003910 polypeptide antibiotic agent Substances 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 claims 1
- 229940041008 second-generation cephalosporins Drugs 0.000 claims 1
- 229960002180 tetracycline Drugs 0.000 claims 1
- 229930101283 tetracycline Natural products 0.000 claims 1
- 235000019364 tetracycline Nutrition 0.000 claims 1
- 229940072172 tetracycline antibiotic Drugs 0.000 claims 1
- 150000003522 tetracyclines Chemical class 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 229940041007 third-generation cephalosporins Drugs 0.000 claims 1
- 229960004089 tigecycline Drugs 0.000 claims 1
- 229960003165 vancomycin Drugs 0.000 claims 1
- MYPYJXKWCTUITO-UHFFFAOYSA-N vancomycin Natural products O1C(C(=C2)Cl)=CC=C2C(O)C(C(NC(C2=CC(O)=CC(O)=C2C=2C(O)=CC=C3C=2)C(O)=O)=O)NC(=O)C3NC(=O)C2NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(CC(C)C)NC)C(O)C(C=C3Cl)=CC=C3OC3=CC2=CC1=C3OC1OC(CO)C(O)C(O)C1OC1CC(C)(N)C(O)C(C)O1 MYPYJXKWCTUITO-UHFFFAOYSA-N 0.000 claims 1
- MYPYJXKWCTUITO-LYRMYLQWSA-O vancomycin(1+) Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C([O-])=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)[NH2+]C)[C@H]1C[C@](C)([NH3+])[C@H](O)[C@H](C)O1 MYPYJXKWCTUITO-LYRMYLQWSA-O 0.000 claims 1
- 150000003952 β-lactams Chemical class 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261695947P | 2012-08-31 | 2012-08-31 | |
| US61/695,947 | 2012-08-31 | ||
| PCT/US2013/057690 WO2014036502A2 (en) | 2012-08-31 | 2013-08-30 | Tetracycline compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018034611A Division JP6691157B2 (ja) | 2012-08-31 | 2018-02-28 | テトラサイクリン化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015528468A JP2015528468A (ja) | 2015-09-28 |
| JP2015528468A5 true JP2015528468A5 (https=) | 2016-10-13 |
| JP6301335B2 JP6301335B2 (ja) | 2018-03-28 |
Family
ID=49170898
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015530126A Active JP6301335B2 (ja) | 2012-08-31 | 2013-08-30 | テトラサイクリン化合物 |
| JP2018034611A Active JP6691157B2 (ja) | 2012-08-31 | 2018-02-28 | テトラサイクリン化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018034611A Active JP6691157B2 (ja) | 2012-08-31 | 2018-02-28 | テトラサイクリン化合物 |
Country Status (27)
| Country | Link |
|---|---|
| US (3) | US9573895B2 (https=) |
| EP (2) | EP2890673B1 (https=) |
| JP (2) | JP6301335B2 (https=) |
| KR (2) | KR102375238B1 (https=) |
| CN (3) | CN108276404A (https=) |
| AU (3) | AU2013308504B2 (https=) |
| BR (1) | BR112015004523B1 (https=) |
| CA (1) | CA2883238C (https=) |
| CY (1) | CY1122744T1 (https=) |
| DK (1) | DK2890673T3 (https=) |
| EA (2) | EA031523B1 (https=) |
| ES (1) | ES2712476T3 (https=) |
| HR (1) | HRP20190268T1 (https=) |
| HU (1) | HUE042600T2 (https=) |
| IL (2) | IL237437B (https=) |
| LT (1) | LT2890673T (https=) |
| ME (1) | ME03329B (https=) |
| MX (2) | MX390763B (https=) |
| NZ (3) | NZ745596A (https=) |
| PL (1) | PL2890673T3 (https=) |
| PT (1) | PT2890673T (https=) |
| RS (1) | RS58572B1 (https=) |
| SG (2) | SG10201801703RA (https=) |
| SI (1) | SI2890673T1 (https=) |
| SM (1) | SMT201900096T1 (https=) |
| TR (1) | TR201902057T4 (https=) |
| WO (1) | WO2014036502A2 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2323972E (pt) | 2008-08-08 | 2013-10-09 | Tetraphase Pharmaceuticals Inc | Compostos de tetraciclina substituídos com c7-flúor |
| EP2427425B1 (en) | 2009-05-08 | 2017-03-08 | Tetraphase Pharmaceuticals, Inc. | Tetracycline compounds |
| IN2012DN02502A (https=) | 2009-08-28 | 2015-08-28 | Tetraphase Pharmaceuticals Inc | |
| BR112015004523B1 (pt) | 2012-08-31 | 2020-08-04 | Tetraphase Pharmaceuticals, Inc | Compostos de tetraciclina, composições farmacêuticas e seus usos |
| CA3034891A1 (en) * | 2016-08-30 | 2018-03-08 | Tetraphase Pharmaceuticals, Inc. | Tetracycline compounds and methods of treatment |
| CN110582486B (zh) | 2016-10-19 | 2024-01-12 | 四相制药公司 | 艾若威四环素的结晶形式 |
| WO2020020999A1 (en) | 2018-07-27 | 2020-01-30 | Sandoz Ag | Process for preparing rapidly or very rapidly dissolving tablets comprising freely soluble api |
| CN113444070A (zh) * | 2021-07-28 | 2021-09-28 | 深圳市真味生物科技有限公司 | 一种由手性叔丁基亚磺酰胺合成手性尼古丁的制备方法 |
| CN115448849B (zh) * | 2022-11-10 | 2023-02-03 | 苏州富士莱医药股份有限公司 | 一种2-苄氧基-3-二苄基氨基-5-氟-6-甲基苯甲酸苯酯的制备方法 |
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|---|---|---|---|---|
| BE639292A (https=) | ||||
| GB935384A (en) * | 1959-03-30 | 1963-08-28 | Pfizer & Co C | Tetracycline derivatives and preparation thereof |
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| GB1065715A (en) * | 1964-04-16 | 1967-04-19 | Pfizer & Co C | Tetracycline derivatives |
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| DE2442829A1 (de) * | 1974-09-06 | 1976-03-18 | Merck Patent Gmbh | Tetracyclische verbindungen und verfahren zu ihrer herstellung |
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| US5770588A (en) | 1991-02-11 | 1998-06-23 | The Research Foundation Of State University Of New York | Non-antibacterial tetracycline compositions of the prevention and treatment of root caries |
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