JP2013508299A5 - - Google Patents
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- JP2013508299A5 JP2013508299A5 JP2012534413A JP2012534413A JP2013508299A5 JP 2013508299 A5 JP2013508299 A5 JP 2013508299A5 JP 2012534413 A JP2012534413 A JP 2012534413A JP 2012534413 A JP2012534413 A JP 2012534413A JP 2013508299 A5 JP2013508299 A5 JP 2013508299A5
- Authority
- JP
- Japan
- Prior art keywords
- unsaturated
- group
- membered saturated
- alkyl
- aromatic
- 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.)
- Pending
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- 229920006395 saturated elastomer Polymers 0.000 claims description 126
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 89
- 229910052757 nitrogen Inorganic materials 0.000 claims description 68
- 229910052760 oxygen Inorganic materials 0.000 claims description 68
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 66
- 125000005842 heteroatom Chemical group 0.000 claims description 66
- 239000001301 oxygen Substances 0.000 claims description 66
- 229910052717 sulfur Chemical group 0.000 claims description 64
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 63
- 239000011593 sulfur Chemical group 0.000 claims description 63
- 125000003118 aryl group Chemical group 0.000 claims description 60
- 125000000217 alkyl group Chemical group 0.000 claims description 58
- 229910052739 hydrogen Inorganic materials 0.000 claims description 54
- 150000002148 esters Chemical class 0.000 claims description 47
- 239000000651 prodrug Substances 0.000 claims description 47
- 229940002612 prodrug Drugs 0.000 claims description 47
- 150000003839 salts Chemical class 0.000 claims description 47
- 150000001875 compounds Chemical class 0.000 claims description 45
- 239000001257 hydrogen Substances 0.000 claims description 44
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 43
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 32
- 208000015181 infectious disease Diseases 0.000 claims description 30
- 125000000304 alkynyl group Chemical group 0.000 claims description 26
- 125000003342 alkenyl group Chemical group 0.000 claims description 24
- 229910052799 carbon Inorganic materials 0.000 claims description 23
- 125000004432 carbon atom Chemical group C* 0.000 claims description 15
- 241001465754 Metazoa Species 0.000 claims description 13
- 230000000813 microbial effect Effects 0.000 claims description 10
- 206010040872 skin infection Diseases 0.000 claims description 9
- 206010035664 Pneumonia Diseases 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- 206010062255 Soft tissue infection Diseases 0.000 claims description 7
- 150000002431 hydrogen Chemical class 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 7
- 208000008745 Healthcare-Associated Pneumonia Diseases 0.000 claims description 4
- 241000282412 Homo Species 0.000 claims description 4
- 125000003725 azepanyl group Chemical group 0.000 claims description 4
- 125000002393 azetidinyl group Chemical group 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 125000003678 cyclohexadienyl group Chemical group C1(=CC=CCC1)* 0.000 claims description 4
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims description 4
- 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 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 125000002541 furyl group Chemical group 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 4
- 239000000126 substance Substances 0.000 claims description 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 4
- 125000005942 tetrahydropyridyl group Chemical group 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 3
- 230000002194 synthesizing effect Effects 0.000 claims description 3
- HCUOEKSZWPGJIM-IYNMRSRQSA-N (e,2z)-2-hydroxyimino-6-methoxy-4-methyl-5-nitrohex-3-enamide Chemical compound COCC([N+]([O-])=O)\C(C)=C\C(=N\O)\C(N)=O HCUOEKSZWPGJIM-IYNMRSRQSA-N 0.000 claims description 2
- 206010060968 Arthritis infective Diseases 0.000 claims description 2
- 208000031729 Bacteremia Diseases 0.000 claims description 2
- 206010018612 Gonorrhoea Diseases 0.000 claims description 2
- 201000009906 Meningitis Diseases 0.000 claims description 2
- 206010031252 Osteomyelitis Diseases 0.000 claims description 2
- 206010058674 Pelvic Infection Diseases 0.000 claims description 2
- 206010035148 Plague Diseases 0.000 claims description 2
- 206010035737 Pneumonia viral Diseases 0.000 claims description 2
- 206010057190 Respiratory tract infections Diseases 0.000 claims description 2
- 206010040047 Sepsis Diseases 0.000 claims description 2
- 206010058028 Shunt infection Diseases 0.000 claims description 2
- 206010041925 Staphylococcal infections Diseases 0.000 claims description 2
- 108010059993 Vancomycin Proteins 0.000 claims description 2
- 208000009470 Ventilator-Associated Pneumonia Diseases 0.000 claims description 2
- 241000607479 Yersinia pestis Species 0.000 claims description 2
- 230000001154 acute effect Effects 0.000 claims description 2
- 208000022338 anthrax infection Diseases 0.000 claims description 2
- 230000001580 bacterial effect Effects 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 206010014665 endocarditis Diseases 0.000 claims description 2
- 208000001786 gonorrhea Diseases 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
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 206010034674 peritonitis Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 238000011321 prophylaxis Methods 0.000 claims description 2
- 210000001519 tissue Anatomy 0.000 claims description 2
- 201000008827 tuberculosis Diseases 0.000 claims description 2
- 229960003165 vancomycin Drugs 0.000 claims description 2
- 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 description 2
- 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 description 2
- 208000009421 viral pneumonia Diseases 0.000 claims description 2
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 4
- 150000001721 carbon Chemical group 0.000 claims 3
- 206010056519 Abdominal infection Diseases 0.000 claims 2
- 208000035473 Communicable 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
- 206010062910 Vascular infections Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 229960003085 meticillin Drugs 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 208000020029 respiratory tract infectious disease Diseases 0.000 claims 1
- 208000015339 staphylococcus aureus infection Diseases 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 description 2
- 239000004599 antimicrobial Substances 0.000 description 2
- 208000036209 Intraabdominal Infections Diseases 0.000 description 1
- 208000037942 Methicillin-resistant Staphylococcus aureus infection Diseases 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 208000019206 urinary tract infection Diseases 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25247809P | 2009-10-16 | 2009-10-16 | |
| US61/252,478 | 2009-10-16 | ||
| US31428710P | 2010-03-16 | 2010-03-16 | |
| US61/314,287 | 2010-03-16 | ||
| US35820110P | 2010-06-24 | 2010-06-24 | |
| US61/358,201 | 2010-06-24 | ||
| PCT/US2010/052928 WO2011047323A2 (en) | 2009-10-16 | 2010-10-15 | Antimicrobial compounds and methods of making and using the same |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016015912A Division JP2016121171A (ja) | 2009-10-16 | 2016-01-29 | 抗微生物性化合物および抗微生物性化合物の製造方法および使用方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013508299A JP2013508299A (ja) | 2013-03-07 |
| JP2013508299A5 true JP2013508299A5 (https=) | 2013-11-07 |
Family
ID=44343890
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012534413A Pending JP2013508299A (ja) | 2009-10-16 | 2010-10-15 | 抗微生物性化合物および抗微生物性化合物の製造方法および使用方法 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US9216979B2 (https=) |
| EP (1) | EP2488502A4 (https=) |
| JP (1) | JP2013508299A (https=) |
| KR (1) | KR20180069098A (https=) |
| CN (1) | CN102725274A (https=) |
| AU (3) | AU2010306650B2 (https=) |
| BR (1) | BR112012008795A2 (https=) |
| CA (1) | CA2777741A1 (https=) |
| EA (1) | EA023350B1 (https=) |
| IL (1) | IL219135A0 (https=) |
| MX (2) | MX339000B (https=) |
| MY (1) | MY176900A (https=) |
| NZ (1) | NZ599290A (https=) |
| WO (1) | WO2011047323A2 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
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| MX2012004341A (es) | 2009-10-16 | 2012-10-05 | Rib X Pharmaceuticals Inc | Compuestos antimicrobianos y metodos para fabricar y utilizar los mismos. |
| NZ599290A (en) * | 2009-10-16 | 2014-10-31 | Melinta Therapeutics Inc | Antimicrobial compounds and methods of making and using the same |
| WO2012097270A1 (en) | 2011-01-14 | 2012-07-19 | Vertex Pharmaceuticals Incorporated | Solid forms of gyrase inhibitor (r)-1-ethyl-3-[5-[2-{1-hydroxy-1-methyl-ethyl}pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl}-1h-benzimidazol-2-yl]urea |
| CN103384665B (zh) | 2011-01-14 | 2018-01-09 | 斯派罗吹耐姆公司 | 制备促旋酶和拓扑异构酶抑制剂的方法 |
| US8476281B2 (en) | 2011-01-14 | 2013-07-02 | Vertex Pharmaceuticals Incorporated | Solid forms of gyrase inhibitor (R)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl)pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1H-benzimidazol-2-yl]urea |
| AU2012205415B2 (en) | 2011-01-14 | 2017-02-02 | Spero Therapeutics, Inc. | Pyrimidine gyrase and topoisomerase IV inhibitors |
| CN103702994B (zh) | 2011-06-20 | 2016-03-23 | 沃泰克斯药物股份有限公司 | 旋转酶和拓扑异构酶抑制剂的磷酸酯 |
| US9572809B2 (en) | 2012-07-18 | 2017-02-21 | Spero Trinem, Inc. | Combination therapy to treat Mycobacterium diseases |
| WO2014015105A1 (en) | 2012-07-18 | 2014-01-23 | Vertex Pharmaceuticals Incorporated | Solid forms of (r)-2-(5-(2-(3-ethylureido)-6-fluoro-7-(tetrahydrofuran-2-yl)-1h-benzo[d]imidazol-5-yl)pyrimidin-2-yl)propan-2-yl dihydrogen phosphate and salts thereof |
| EP3038623A4 (en) | 2013-09-09 | 2017-04-19 | Melinta Therapeutics, Inc. | Antimicrobial compounds and methods of making and using the same |
| CA2923214A1 (en) | 2013-09-09 | 2015-03-12 | Melinta Therapeutics, Inc. | Antimicrobial compounds and methods of making and using the same |
| CA2955569C (en) * | 2014-08-06 | 2023-02-14 | Ascendis Pharma A/S | Prodrugs comprising an aminoalkyl glycine linker |
| HK1249758A1 (zh) | 2015-03-11 | 2018-11-09 | Melinta Therapeutics, Inc. | 抗微生物化合物及其制备和使用方法 |
| EP3957627B1 (en) | 2015-04-24 | 2024-06-19 | Shionogi & Co., Ltd | 6-membered heterocyclic derivative and pharmaceutical composition comprising same |
| US11098047B2 (en) * | 2016-05-06 | 2021-08-24 | BioVersys AG | Antimicrobials and methods of making and using same |
| KR102528627B1 (ko) | 2016-10-17 | 2023-05-03 | 시오노기 앤드 컴파니, 리미티드 | 2환성 함질소 헤테로환 유도체 및 그를 함유하는 의약 조성물 |
| WO2019013789A1 (en) | 2017-07-12 | 2019-01-17 | Curza Global, Llc | ANTIMICROBIAL COMPOUNDS |
| WO2019013790A1 (en) | 2017-07-12 | 2019-01-17 | Curza Global, Llc | ANTIMICROBIAL COMPOUNDS AND USES THEREOF |
| JP2022518229A (ja) * | 2019-01-16 | 2022-03-14 | カーザ グローバル， エルエルシー | 抗菌化合物及び方法 |
| CA3126798A1 (en) * | 2019-01-16 | 2020-07-23 | Curza Global, Llc | Antimicrobial compounds and methods |
| EP4085910A1 (en) * | 2021-05-05 | 2022-11-09 | 4Living Biotech | Use of a compound such as plerixafor for treating a viral pulmonary disease |
| TW202313065A (zh) | 2021-05-28 | 2023-04-01 | 美商季卡尼醫療公司 | 用於治療遺傳疾病之化合物 |
| WO2023250513A1 (en) | 2022-06-24 | 2023-12-28 | Zikani Therapeutics, Inc. | 13-membered macrolide compounds for treating diseases mediated by abnormal protein translation |
| WO2024036254A2 (en) | 2022-08-11 | 2024-02-15 | Zikani Therapeutics, Inc. | Synthetic processes and intermediates for preparing therapeutic azaketolides |
| JP2025530776A (ja) | 2022-09-01 | 2025-09-17 | ジカニ セラピューティクス， インコーポレイテッド | １３員環マクロライドを使用した家族性大腸腺腫症の処置 |
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-
2010
- 2010-10-15 NZ NZ599290A patent/NZ599290A/en not_active IP Right Cessation
- 2010-10-15 EP EP10824207.4A patent/EP2488502A4/en not_active Withdrawn
- 2010-10-15 KR KR1020187016578A patent/KR20180069098A/ko not_active Ceased
- 2010-10-15 MX MX2012004342A patent/MX339000B/es active IP Right Grant
- 2010-10-15 CN CN2010800573060A patent/CN102725274A/zh active Pending
- 2010-10-15 MY MYPI2012001649A patent/MY176900A/en unknown
- 2010-10-15 JP JP2012534413A patent/JP2013508299A/ja active Pending
- 2010-10-15 WO PCT/US2010/052928 patent/WO2011047323A2/en not_active Ceased
- 2010-10-15 EA EA201270567A patent/EA023350B1/ru not_active IP Right Cessation
- 2010-10-15 AU AU2010306650A patent/AU2010306650B2/en not_active Ceased
- 2010-10-15 US US13/501,834 patent/US9216979B2/en not_active Expired - Fee Related
- 2010-10-15 BR BR112012008795-9A patent/BR112012008795A2/pt active Search and Examination
- 2010-10-15 CA CA2777741A patent/CA2777741A1/en not_active Abandoned
- 2010-10-15 MX MX2014010301A patent/MX358697B/es unknown
-
2012
- 2012-04-15 IL IL219135A patent/IL219135A0/en unknown
-
2015
- 2015-10-16 US US14/884,985 patent/US9845297B2/en not_active Expired - Fee Related
-
2016
- 2016-09-22 AU AU2016231568A patent/AU2016231568A1/en not_active Abandoned
-
2017
- 2017-12-18 US US15/844,817 patent/US20180334439A1/en not_active Abandoned
-
2018
- 2018-03-23 AU AU2018202065A patent/AU2018202065A1/en not_active Abandoned
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