AR061583A1 - Acidos 6-(bencilo sustituido con heterociclil)-4-oxiquinolin carboxilicos, inhibidores de vih-integrasas, composiciones farmaceuticas que los contienen y usos como agentes anti-vih. - Google Patents
Acidos 6-(bencilo sustituido con heterociclil)-4-oxiquinolin carboxilicos, inhibidores de vih-integrasas, composiciones farmaceuticas que los contienen y usos como agentes anti-vih.Info
- Publication number
- AR061583A1 AR061583A1 ARP070102755A ARP070102755A AR061583A1 AR 061583 A1 AR061583 A1 AR 061583A1 AR P070102755 A ARP070102755 A AR P070102755A AR P070102755 A ARP070102755 A AR P070102755A AR 061583 A1 AR061583 A1 AR 061583A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- atom
- optionally substituted
- substituents selected
- alkyl
- Prior art date
Links
- 239000002259 anti human immunodeficiency virus agent Substances 0.000 title abstract 2
- 229940124411 anti-hiv antiviral agent Drugs 0.000 title abstract 2
- 239000002253 acid Substances 0.000 title 1
- 150000007513 acids Chemical class 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 9
- 125000001424 substituent group Chemical group 0.000 abstract 9
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 150000001721 carbon Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 229910052717 sulfur Chemical group 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 1
- 208000030507 AIDS Diseases 0.000 abstract 1
- 108010002459 HIV Integrase Proteins 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
- C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/10—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 two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Los compuestos de la presente tienen una actividad inhibidora de la integrasa VIH y son de utilidad como agentes anti-VIH o como agentes para la prevencion o el tratamiento de SIDA. Reivindicacion 1: Un compuesto caracterizado por la formula (1) o una de sus sales farmacéuticamente aceptables o uno de sus solvatos, en donde el anillo A es un grupo heterocíclico monocíclico opcionalmente sustituido con 1 a 5 sustituyentes seleccionados del siguiente grupo A, en donde el grupo heterocíclico monocíclico contiene, además de átomo de carbono, al menos un heteroátomo seleccionado de átomo de nitrogeno, átomo de oxígeno y átomo de azufre; el grupo A es un grupo que consiste en átomo de halogeno, alquilo C1-4, -(CH2)n-ORa1, -NRa3Ra4, -CORa2 y -CONRa3Ra4, en donde Ra1, Ra2, Ra3 y Ra4 son iguales o diferentes y cada uno es un átomo de hidrogeno o un grupo alquilo C1-4 y n es 0 o un numero entero de 1 a 4; R1 es un átomo de hidrogeno, alquilo C1-6 opcionalmente sustituido con 1 a 3 sustituyentes seleccionados del siguiente grupo B, un grupo del anillo de carbono C3-10 opcionalmente sustituido con 1 a 5 sustituyentes seleccionados del grupo A antes mencionado o un grupo heterocíclico opcionalmente sustituido con 1 a 5 sustituyentes seleccionados del grupo A antes mencionado, en donde el grupo heterocíclico contiene, además de átomo de carbono, al menos un heteroátomo seleccionado de átomo de nitrogeno, átomo de oxígeno y átomo de azufre; el grupo B es un grupo que consiste en un grupo del anillo de carbono C3-10 opcionalmente sustituido con 1 a 5 sustituyentes seleccionados del grupo A antes mencionado, un grupo heterocíclico opcionalmente sustituido con 1 a 5 sustituyentes seleccionados del grupo A antes mencionado, en donde el grupo heterocíclico es como se definio con anterioridad, átomo de halogeno, grupo ciano, -ORb1, -SRb1, -NRb2Rb3, -CONRb2Rb3, -SO2NRb2Rb3, -CORb1, -NRb2CORb1, -SO2Rb1, -NRb2SO2Rb1, -COORb1, -NRb2COORb1 y -NRb4CO-NRb2Rb3 en donde Rb1, Rb2, Rb3 y Rb4 son iguales o diferentes y cada uno es un átomo de hidrogeno, un grupo alquilo C1-4, un grupo del anillo de carbono C3-10 opcionalmente sustituido con 1 a 5 sustituyentes seleccionados del grupo A antes mencionado o un grupo heterocíclico opcionalmente sustituido con 1 a 5 sustituyentes seleccionados del grupo A antes mencionado, en donde el grupo heterocíclico es como se definio con anterioridad; R2 es un átomo de hidrogeno, alquilo C1-4 u -OR11, en donde R11 es un átomo de hidrogeno o un grupo alquilo C1-4, R3 y R4 son iguales o diferentes y cada uno es un átomo de hidrogeno, un átomo de halogeno, alquilo C1-4 u -OR12, en donde R12 es un átomo de hidrogeno o alquilo C1-4; R5 es cada uno, de modo independiente, un átomo de halogeno, alquilo C1-4 u -OR13, en donde R13 es un átomo de hidrogeno o alquilo C1-4; m es 0, 1 o 2; y R6 es un átomo de hidrogeno o R1 y R6 forman, junto con los átomos de carbono a los que se unen, un grupo cicloalquilo C3-10 opcionalmente sustituido con 1 a 5 sustituyentes seleccionados del grupo A antes mencionado.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2006174331 | 2006-06-23 | ||
| JP2006220082 | 2006-08-11 | ||
| JP2006274143 | 2006-10-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR061583A1 true AR061583A1 (es) | 2008-09-03 |
Family
ID=38833517
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070102755A AR061583A1 (es) | 2006-06-23 | 2007-06-22 | Acidos 6-(bencilo sustituido con heterociclil)-4-oxiquinolin carboxilicos, inhibidores de vih-integrasas, composiciones farmaceuticas que los contienen y usos como agentes anti-vih. |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US7872004B2 (es) |
| EP (2) | EP2033954A4 (es) |
| JP (1) | JP4038231B1 (es) |
| KR (1) | KR101053811B1 (es) |
| AR (1) | AR061583A1 (es) |
| AU (1) | AU2007262010B2 (es) |
| BR (1) | BRPI0713336A2 (es) |
| CA (1) | CA2653830C (es) |
| CL (1) | CL2007001838A1 (es) |
| CO (1) | CO6150181A2 (es) |
| IL (1) | IL195862A0 (es) |
| MX (1) | MX2009000159A (es) |
| MY (1) | MY144773A (es) |
| NO (1) | NO20090322L (es) |
| NZ (1) | NZ573709A (es) |
| PE (1) | PE20080211A1 (es) |
| SA (1) | SA07280343B1 (es) |
| TW (1) | TW200811153A (es) |
| WO (1) | WO2007148780A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60329318D1 (de) * | 2002-11-20 | 2009-10-29 | Japan Tobacco Inc | 4-oxochinolinverbindungen und deren verwendung als hiv-integrase-inhibitoren |
| TWI411602B (zh) * | 2006-09-12 | 2013-10-11 | Gilead Sciences Inc | 製造整合酶抑制劑的方法及彼所用的中間物 |
| AR068403A1 (es) | 2007-09-11 | 2009-11-18 | Gilead Sciences Inc | Proceso e intermediarios para la preparacion de inhibidores de integrasa |
| KR20120087916A (ko) | 2009-10-13 | 2012-08-07 | 엘랑코 애니멀 헬쓰 아일랜드 리미티드 | 마크로시클릭 인테그라제 억제제 |
| JP5739517B2 (ja) | 2010-04-02 | 2015-06-24 | ヤンセン・アールアンドデイ・アイルランド | 大環状インテグラーゼ阻害剤 |
| WO2013082476A1 (en) | 2011-11-30 | 2013-06-06 | Emory University | Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections |
| AU2013296289B2 (en) | 2012-08-03 | 2017-10-05 | Gilead Sciences, Inc. | Process and intermediates for preparing integrase inhibitors |
| TW202544011A (zh) | 2019-03-22 | 2025-11-16 | 美商基利科學股份有限公司 | 橋鍵聯三環胺甲醯吡啶酮化合物及其醫藥用途 |
| JP7453399B2 (ja) | 2020-02-24 | 2024-03-19 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖ感染症を治療するための四環式化合物及びその使用 |
| KR20230079137A (ko) | 2020-09-30 | 2023-06-05 | 길리애드 사이언시즈, 인코포레이티드 | 가교된 트리사이클릭 카르바모일피리돈 화합물 및 이의 용도 |
| PL4196479T3 (pl) | 2021-01-19 | 2024-03-18 | Gilead Sciences, Inc. | Podstawione związki pirydotriazynowe i ich zastosowania |
| TWI856796B (zh) | 2022-04-06 | 2024-09-21 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
| CN115448866B (zh) * | 2022-10-13 | 2023-11-21 | 中北大学 | 一种1-甲基-2,3,4,5-四硝基吡咯的制备方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU735186B2 (en) | 1997-09-15 | 2001-07-05 | Warner Chilcott Company, Llc | Antimicrobial quinolones, their compositions and uses |
| WO2004004611A1 (en) | 2002-07-08 | 2004-01-15 | Coloplast A/S | Conduit device |
| DE60329318D1 (de) | 2002-11-20 | 2009-10-29 | Japan Tobacco Inc | 4-oxochinolinverbindungen und deren verwendung als hiv-integrase-inhibitoren |
| EP1730135B1 (en) | 2004-03-10 | 2010-09-22 | The United States of America, represented by the Secretary, Department of Health and Human Services | Qiunolin-4-ones as inhibitors of retroviral integrase for the treatment of hiv, aids and aids related complex (arc) |
| WO2005113509A1 (en) | 2004-05-20 | 2005-12-01 | Japan Tobacco Inc. | Novel 4-oxoquinoline compound and use thereof as hiv integrase inhibitor |
| US7745459B2 (en) * | 2004-09-21 | 2010-06-29 | Japan Tobacco Inc. | Quinolizinone compound and use thereof as HIV integrase inhibitor |
| WO2006033422A1 (ja) | 2004-09-21 | 2006-03-30 | Japan Tobacco Inc. | キノリジノン化合物、およびそのｈｉｖインテグラーゼ阻害剤としての利用 |
| JP2006174331A (ja) | 2004-12-20 | 2006-06-29 | Fuji Xerox Co Ltd | 画像圧縮装置、画像圧縮方法及びそのプログラム |
| JP2006220082A (ja) | 2005-02-10 | 2006-08-24 | Denso Corp | 燃料噴射装置 |
| JP4572720B2 (ja) | 2005-03-30 | 2010-11-04 | Ｄｉｃ株式会社 | 水分散型アクリル系樹脂の製造方法、並びにそれにより製造される水分散型アクリル粘着剤組成物及び粘着シート |
| DE102006005861A1 (de) | 2006-02-09 | 2007-08-23 | Aicuris Gmbh & Co. Kg | Substituierte Chinolone III |
-
2007
- 2007-06-21 TW TW096122234A patent/TW200811153A/zh unknown
- 2007-06-22 EP EP07845259A patent/EP2033954A4/en not_active Withdrawn
- 2007-06-22 AR ARP070102755A patent/AR061583A1/es not_active Application Discontinuation
- 2007-06-22 US US11/767,021 patent/US7872004B2/en not_active Expired - Fee Related
- 2007-06-22 CA CA2653830A patent/CA2653830C/en not_active Expired - Fee Related
- 2007-06-22 CL CL200701838A patent/CL2007001838A1/es unknown
- 2007-06-22 PE PE2007000805A patent/PE20080211A1/es not_active Application Discontinuation
- 2007-06-22 NZ NZ573709A patent/NZ573709A/en not_active IP Right Cessation
- 2007-06-22 KR KR1020097001497A patent/KR101053811B1/ko not_active Expired - Fee Related
- 2007-06-22 BR BRPI0713336-7A patent/BRPI0713336A2/pt not_active IP Right Cessation
- 2007-06-22 AU AU2007262010A patent/AU2007262010B2/en not_active Ceased
- 2007-06-22 MX MX2009000159A patent/MX2009000159A/es active IP Right Grant
- 2007-06-22 EP EP11168760A patent/EP2368880A1/en not_active Withdrawn
- 2007-06-22 JP JP2007164676A patent/JP4038231B1/ja not_active Expired - Fee Related
- 2007-06-22 WO PCT/JP2007/062579 patent/WO2007148780A1/ja not_active Ceased
- 2007-06-23 SA SA7280343A patent/SA07280343B1/ar unknown
-
2008
- 2008-12-10 MY MYPI20085006A patent/MY144773A/en unknown
- 2008-12-11 IL IL195862A patent/IL195862A0/en unknown
-
2009
- 2009-01-16 CO CO09003378A patent/CO6150181A2/es unknown
- 2009-01-21 NO NO20090322A patent/NO20090322L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AU2007262010B2 (en) | 2011-05-12 |
| EP2033954A1 (en) | 2009-03-11 |
| BRPI0713336A2 (pt) | 2012-11-06 |
| AU2007262010A1 (en) | 2007-12-27 |
| IL195862A0 (en) | 2009-09-01 |
| CL2007001838A1 (es) | 2008-02-08 |
| US7872004B2 (en) | 2011-01-18 |
| MY144773A (en) | 2011-10-31 |
| NZ573709A (en) | 2011-04-29 |
| KR20090023731A (ko) | 2009-03-05 |
| WO2007148780A1 (ja) | 2007-12-27 |
| NO20090322L (no) | 2009-03-20 |
| PE20080211A1 (es) | 2008-04-23 |
| CA2653830A1 (en) | 2007-12-27 |
| MX2009000159A (es) | 2009-01-23 |
| US20080207618A1 (en) | 2008-08-28 |
| SA07280343B1 (ar) | 2011-01-15 |
| JP2008110960A (ja) | 2008-05-15 |
| JP4038231B1 (ja) | 2008-01-23 |
| KR101053811B1 (ko) | 2011-08-03 |
| EP2033954A4 (en) | 2009-08-12 |
| CO6150181A2 (es) | 2010-04-20 |
| TW200811153A (en) | 2008-03-01 |
| EP2368880A1 (en) | 2011-09-28 |
| CA2653830C (en) | 2011-11-22 |
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