AR074608A1 - Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianas - Google Patents
Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianasInfo
- Publication number
- AR074608A1 AR074608A1 ARP090104826A ARP090104826A AR074608A1 AR 074608 A1 AR074608 A1 AR 074608A1 AR P090104826 A ARP090104826 A AR P090104826A AR P090104826 A ARP090104826 A AR P090104826A AR 074608 A1 AR074608 A1 AR 074608A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocycle
- amino
- independently selected
- optionally substituted
- Prior art date
Links
- 208000035143 Bacterial infection Diseases 0.000 title abstract 2
- 208000022362 bacterial infectious disease Diseases 0.000 title abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 11
- 125000000623 heterocyclic group Chemical group 0.000 abstract 7
- 229910052757 nitrogen Inorganic materials 0.000 abstract 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 239000000460 chlorine Substances 0.000 abstract 2
- 229910052801 chlorine Inorganic materials 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- -1 -OH Chemical group 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000005336 allyloxy group Chemical group 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Otolaryngology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
También se describen procesos para su preparación, composiciones farmacéuticas que los contienen, su uso como medicamentos y uso en el tratamiento de infecciones bacterianas. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1): una sal farmacéuticamente aceptable del mismo, en donde: R1 es cloro o ciano; R2 es hidrógeno, cloro o ciano; R3 es halo, alquiloC1-4, alcoxiC1-4 o aliloxi; R4 es hidrógeno o alquiloC1-4; el Anillo A se selecciona de la fórmula (2), (3) o (4); en donde: "*" es el punto de unión al anillo de tiazolilo; X es CH, CR o N; R5 es H, un alquiloC1-4 o alcoxiC1-4alquiloC1-4; R6, en cada oportunidad, se selecciona independientemente de halo, -NR7R8, -OR8 y heterociclo en donde dicho heterociclo comprende al menos un miembro nitrógeno del anillo y está opcionalmente sustituido en uno o más átomos de carbono por uno o más R9 y está opcionalmente sustituido en uno o más nitrógenos del anillo por R10; R6 es hidrógeno o R6; R7 y R8 cada uno, independientemente, se selecciona del grupo que consiste en hidrógeno y un aIquiIoC1-6, en donde dicho alquilo está opcionalmerte sustituido por uno o más independientemente seleccionados de -OH, N,N-di(alquilC1-4)amino, un alcoxiC1-6 un alcoxiC1-6aIcoxiC1-6 y heterociclo, en donde dicho heterociclo está opcionalmente sustituido en uno o más átomos de carbono por uno o más independientemente seleccionados de halo, alquiloC1-6 y alcoxiC1-6 y en donde si dicho heterociclilo contiene un resto -NH- dicho nitrógeno puede sustituirse opcionalmente por un alquiloC1-4; R9, en cada oportunidad, se selecciona independientemente de un alquiloC1-4, halo, hidroxi, alcoxiC1-4, amino, N-(alquilC1-4)amino y N,N-di(alquilC1-4)amino; R10, en cada oportunidad, se selecciona independientemente de un alquiloC1-4 opcionalmente sustituido por N,N-di(alquilC1-4)amino, -OH, heterociclo y cicloalquiloC3-6, en donde el heterociclo puede sustituirse opcionalmente por alquilo C1-4; y n es 0, 1, 2 ó 3.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12195308P | 2008-12-12 | 2008-12-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074608A1 true AR074608A1 (es) | 2011-01-26 |
Family
ID=41818426
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104826A AR074608A1 (es) | 2008-12-12 | 2009-12-11 | Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianas |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US8071605B2 (es) |
| EP (1) | EP2376488A1 (es) |
| JP (1) | JP2012511561A (es) |
| KR (1) | KR20110097825A (es) |
| CN (1) | CN102317286A (es) |
| AR (1) | AR074608A1 (es) |
| AU (1) | AU2009326141A1 (es) |
| BR (1) | BRPI0923326A2 (es) |
| CA (1) | CA2745063A1 (es) |
| MX (1) | MX2011005909A (es) |
| TW (1) | TW201026695A (es) |
| UY (1) | UY32315A (es) |
| WO (1) | WO2010067123A1 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2598423C (en) * | 2005-02-18 | 2014-05-27 | Astrazeneca Ab | Antibacterial piperidine derivatives |
| TW201026694A (en) * | 2008-12-12 | 2010-07-16 | Astrazeneca Ab | Compound 468 |
| AU2011210765A1 (en) | 2010-01-28 | 2012-09-13 | President And Fellows Of Harvard College | Compositions and methods for enhancing proteasome activity |
| US9556166B2 (en) | 2011-05-12 | 2017-01-31 | Proteostasis Therapeutics, Inc. | Proteostasis regulators |
| US9849135B2 (en) | 2013-01-25 | 2017-12-26 | President And Fellows Of Harvard College | USP14 inhibitors for treating or preventing viral infections |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| MX2016009135A (es) | 2014-01-14 | 2016-10-05 | Millennium Pharm Inc | Heteroarilos y usos de estos. |
| EP3094326A4 (en) | 2014-01-14 | 2017-07-26 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2016183515A1 (en) * | 2015-05-13 | 2016-11-17 | Alivecor, Inc. | Discordance monitoring |
| CN105067814A (zh) * | 2015-07-24 | 2015-11-18 | 中国科学院成都生物研究所 | 解旋酶水解atp活性测定方法 |
| ES2817749T3 (es) | 2015-09-30 | 2021-04-08 | Daiichi Sankyo Co Ltd | Derivados de hidroxialquil tiadiazol |
| WO2018048882A1 (en) | 2016-09-06 | 2018-03-15 | The Research Foundation For The State University Of New York | Positron imaging tomography imaging agent composition and method for bacterial infection |
| EP3596071A1 (en) | 2017-03-14 | 2020-01-22 | Daiichi Sankyo Company, Limited | N-phosphonoxymethyl prodrugs of hydroxyalkyl thiadiazole derivatives |
| WO2018174288A1 (ja) | 2017-03-24 | 2018-09-27 | 大正製薬株式会社 | ２（１ｈ）－キノリノン誘導体 |
| WO2020048949A1 (en) | 2018-09-03 | 2020-03-12 | Univerza V Ljubljani | New class of dna gyrase and/or topoisomerase iv inhibitors with activity against gram-positive and gram-negative bacteria |
| US20250002455A1 (en) | 2020-12-17 | 2025-01-02 | Univerza V Ljubljani | New n-phenylpyrrolamide inhibitors of dna gyrase and topoisomerase iv with antibacterial activity |
| CN115466246B (zh) * | 2021-06-11 | 2024-02-06 | 中国医学科学院药物研究所 | 吡咯酰哌啶胺类化合物及其用途 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2735475B1 (fr) | 1995-06-13 | 1997-07-11 | Synthelabo | Derives de n-((1,4-diazabicyclo(2.2.2)oct-2-yl)methyl) benzamide, leur preparation et leur application en therapeutique |
| TW538046B (en) | 1998-01-08 | 2003-06-21 | Hoechst Marion Roussel Inc | Aromatic amides having antiobiotic activities and the preparation processes, intermediates and pharmaceutical composition thereof |
| CN1230166C (zh) | 2000-01-18 | 2005-12-07 | 沃泰克斯药物股份有限公司 | 回旋酶抑制剂及其用途 |
| EP1341769B1 (en) | 2000-12-15 | 2007-10-17 | Vertex Pharmaceuticals Incorporated | Bacterial gyrase inhibitors and uses thereof |
| US20030220341A1 (en) | 2001-12-21 | 2003-11-27 | Gary Bridger | Chemokine receptor binding heterocyclic compounds with enhanced efficacy |
| TW200526626A (en) | 2003-09-13 | 2005-08-16 | Astrazeneca Ab | Chemical compounds |
| CA2598423C (en) * | 2005-02-18 | 2014-05-27 | Astrazeneca Ab | Antibacterial piperidine derivatives |
| EP1856044A2 (en) | 2005-02-18 | 2007-11-21 | AstraZeneca AB | Pyrrole derivatives as dna gyrase and topoisomerase inhibitors |
| WO2006087544A2 (en) | 2005-02-18 | 2006-08-24 | Astrazeneca Ab | Pyrrole derivatives as dna gyrase and topoisomerase inhibitors |
| EP1861396A1 (en) | 2005-03-04 | 2007-12-05 | AstraZeneca AB | Tricyclic derivatives of azetidine and pyrrole with antibacterial activity |
| US20080269214A1 (en) | 2005-03-04 | 2008-10-30 | Astrazeneca Ab | Pyrrole Derivatives as Dna Gyrase and Topoisomerase Inhibitors |
| TW200819437A (en) | 2006-08-17 | 2008-05-01 | Astrazeneca Ab | Chemical compounds |
| TW200906412A (en) | 2007-06-12 | 2009-02-16 | Astrazeneca Ab | Piperidine compounds and uses thereof |
-
2009
- 2009-12-10 TW TW098142349A patent/TW201026695A/zh unknown
- 2009-12-10 US US12/634,809 patent/US8071605B2/en not_active Expired - Fee Related
- 2009-12-11 WO PCT/GB2009/051691 patent/WO2010067123A1/en not_active Ceased
- 2009-12-11 KR KR1020117013309A patent/KR20110097825A/ko not_active Withdrawn
- 2009-12-11 JP JP2011540213A patent/JP2012511561A/ja active Pending
- 2009-12-11 CN CN2009801567543A patent/CN102317286A/zh active Pending
- 2009-12-11 AU AU2009326141A patent/AU2009326141A1/en not_active Abandoned
- 2009-12-11 UY UY0001032315A patent/UY32315A/es not_active Application Discontinuation
- 2009-12-11 BR BRPI0923326A patent/BRPI0923326A2/pt not_active IP Right Cessation
- 2009-12-11 EP EP09771588A patent/EP2376488A1/en not_active Withdrawn
- 2009-12-11 CA CA2745063A patent/CA2745063A1/en not_active Abandoned
- 2009-12-11 MX MX2011005909A patent/MX2011005909A/es not_active Application Discontinuation
- 2009-12-11 AR ARP090104826A patent/AR074608A1/es unknown
-
2011
- 2011-10-06 US US13/267,271 patent/US20120028979A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2009326141A1 (en) | 2011-06-30 |
| CA2745063A1 (en) | 2010-06-17 |
| JP2012511561A (ja) | 2012-05-24 |
| TW201026695A (en) | 2010-07-16 |
| US20120028979A1 (en) | 2012-02-02 |
| UY32315A (es) | 2010-07-30 |
| KR20110097825A (ko) | 2011-08-31 |
| CN102317286A (zh) | 2012-01-11 |
| EP2376488A1 (en) | 2011-10-19 |
| MX2011005909A (es) | 2011-06-20 |
| US20100173909A1 (en) | 2010-07-08 |
| WO2010067123A1 (en) | 2010-06-17 |
| US8071605B2 (en) | 2011-12-06 |
| BRPI0923326A2 (pt) | 2017-07-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |