AR073769A1 - Inhibidores de la integrasa del vih derivados de azepina y oxazepinas condensadas, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de infecciones por vih. - Google Patents
Inhibidores de la integrasa del vih derivados de azepina y oxazepinas condensadas, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de infecciones por vih.Info
- Publication number
- AR073769A1 AR073769A1 ARP090103831A ARP090103831A AR073769A1 AR 073769 A1 AR073769 A1 AR 073769A1 AR P090103831 A ARP090103831 A AR P090103831A AR P090103831 A ARP090103831 A AR P090103831A AR 073769 A1 AR073769 A1 AR 073769A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- compound
- hiv
- oxazepins
- integress
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/10—Anthelmintics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/14—Ectoparasiticides, e.g. scabicides
-
- 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
- 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
- C07D487/04—Ortho-condensed systems
-
- H—ELECTRICITY
- H01—ELECTRIC ELEMENTS
- H01L—SEMICONDUCTOR DEVICES NOT COVERED BY CLASS H10
- H01L2924/00—Indexing scheme for arrangements or methods for connecting or disconnecting semiconductor or solid-state bodies as covered by H01L24/00
- H01L2924/0001—Technical content checked by a classifier
- H01L2924/0002—Not covered by any one of groups H01L24/00, H01L24/00 and H01L2224/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable del mismo, donde: cada X1 y X2 es independientemente H, halogeno, o alquilo C1-3, con la condicion de que al menos uno de X1 y X2 sea distinto de H; Y es CH2 u O; R1A es H o alquilo C1-3; R1B es H, alquilo C1-3 u O-alquilo C1-4; R2 es H o alquilo C1-3, y R3 es alquilo C1-3; y con la condicion de que: (C) cuando Y es O, entonces R1A y R1B sean los dos H, R2 sea alquilo C1-3 y (D) cuando Y es CH2, entonces (i) R2 sea H, R1A sea alquilo C1-3 y R1B sea alquilo C1-3 u O-alquilo C1-4, (ii) R2 sea alquilo C1-3, R1A sea H y R1B sea H; o (iii) R2 sea H, R1A sea H y R1B sea O-alquilo C1-4. Reivindicacion 10: Un compuesto de acuerdo con la reivindicacion 9 que es una forma cristalina del compuesto 2A, donde el compuesto cristalino 2A se caracteriza por un patron de difraccion de polvos por rayos X obtenido usando radiacion de cobre Kalfa que comprende valores 2theta en grados de aproximadamente 8,5; 9,3; 13,3; 17,0; 18,8 y 20,8. Reivindicacion 13: Un compuesto de acuerdo con la reivindicacion 12 que es una forma cristalina del compuesto 4A, donde el compuesto 4A cristalino se caracteriza por un patron de difraccion de polvos por rayos X obtenido usando radiacion de cobre Kalfa que comprende valores 2theta en grados de aproximadamente 6,1; 10,4; 12,9; 13,7; 19,4; y 22,9. Reivindicacion 18: Un compuesto de acuerdo con la reivindicacion 16 que es una forma cristalina del compuesto 5A, donde el compuesto 5A cristalino se caracteriza por un patron de difraccion de polvos por rayos X obtenido usando radiacion de cobre Kalfa que comprende valores 2theta en grados de aproximadamente 8,4; 8,6; 18,0; 20,4; 20.8; 25,9; 26,2; y 27,1. Reivindicacion 21: Un compuesto de acuerdo con la reivindicacion 20 que es una forma cristalina del compuesto 6A, donde el compuesto 6A cristalino se caracteriza por un patron de difraccion de polvos por rayos X obtenido usando radiacion de cobre Kalfa que comprende valores 2theta en grados de aproximadamente 10,6; 14,2; 17,4; 18,8 y 20,4.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19527108P | 2008-10-06 | 2008-10-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR073769A1 true AR073769A1 (es) | 2010-12-01 |
Family
ID=41682332
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090103831A AR073769A1 (es) | 2008-10-06 | 2009-10-05 | Inhibidores de la integrasa del vih derivados de azepina y oxazepinas condensadas, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de infecciones por vih. |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US8513234B2 (es) |
| EP (1) | EP2349276B1 (es) |
| JP (2) | JP4880097B1 (es) |
| KR (1) | KR20110066224A (es) |
| CN (1) | CN102239172A (es) |
| AR (1) | AR073769A1 (es) |
| AU (1) | AU2009302663B2 (es) |
| BR (1) | BRPI0920605A8 (es) |
| CA (1) | CA2738814C (es) |
| CO (1) | CO6382127A2 (es) |
| CR (1) | CR20110184A (es) |
| DO (1) | DOP2011000093A (es) |
| EA (1) | EA201170537A1 (es) |
| EC (1) | ECSP11010959A (es) |
| IL (1) | IL212019A0 (es) |
| MA (1) | MA32764B1 (es) |
| MX (1) | MX2011003637A (es) |
| NI (1) | NI201100069A (es) |
| PE (1) | PE20110344A1 (es) |
| TW (1) | TW201020251A (es) |
| WO (2) | WO2010042392A2 (es) |
| ZA (1) | ZA201102620B (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8283366B2 (en) | 2010-01-22 | 2012-10-09 | Ambrilia Biopharma, Inc. | Derivatives of pyridoxine for inhibiting HIV integrase |
| WO2014008636A1 (en) * | 2012-07-11 | 2014-01-16 | Merck Sharp & Dohme Corp. | Macrocyclic compounds as hiv integrase inhibitors |
| CN102936188B (zh) * | 2012-11-19 | 2015-07-15 | 湖北吉和昌化工科技有限公司 | 一种丙炔醇缩水甘油醚的合成方法 |
| EP2986291B1 (en) | 2013-04-16 | 2020-05-27 | Merck Sharp & Dohme Corp. | 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors |
| CN107722106A (zh) * | 2016-08-11 | 2018-02-23 | 重庆大学 | Hiv抑制剂 |
| WO2019155582A1 (ja) | 2018-02-08 | 2019-08-15 | 株式会社ソシオネクスト | 増幅回路、加算回路、受信回路及び集積回路 |
| EP4122537A1 (en) | 2019-03-22 | 2023-01-25 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use |
| AU2021225809B2 (en) | 2020-02-24 | 2023-08-24 | Gilead Sciences, Inc. | Tetracyclic compounds for treating HIV infection |
| CN111454214B (zh) * | 2020-05-27 | 2023-04-07 | 龙曦宁（上海）医药科技有限公司 | 一种2-甲氧基1-嘧啶乙胺盐酸盐的合成方法 |
| CR20230315A (es) | 2021-01-19 | 2023-09-01 | Gilead Sciences Inc | Compuestos de piridotriazina sustituidos y usos de estos |
| TWI843506B (zh) | 2022-04-06 | 2024-05-21 | 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 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3042894T1 (da) | 2001-08-10 | 2016-11-07 | Shionogi & Co | Antiviralt middel |
| CN102219750B (zh) | 2001-10-26 | 2013-05-29 | P.安杰莱蒂分子生物学研究所 | 关于hiv整合酶的n-取代的羟基嘧啶酮甲酰胺抑制剂 |
| AU2002334205B2 (en) | 2001-10-26 | 2007-07-05 | Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa | Dihydroxypyrimidine carboxamide inhibitors of HIV integrase |
| DE60315796T2 (de) | 2002-01-17 | 2008-06-05 | Merck & Co., Inc. | Hydroxynaphthyridinoncarbonsäureamide, die sich als inhibitoren der hiv-integrase eignen |
| JP4733986B2 (ja) | 2002-12-27 | 2011-07-27 | イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー | ＨＩＶインテグラーゼ阻害薬として有用なテトラヒドロ−４Ｈ−ピリド［１，２−ａ］ピリミジン類および関連する化合物 |
| US7135467B2 (en) | 2003-01-13 | 2006-11-14 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7037908B2 (en) | 2003-04-24 | 2006-05-02 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| AR046938A1 (es) | 2003-12-12 | 2006-01-04 | Merck & Co Inc | Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares |
| TW200526635A (en) | 2003-12-22 | 2005-08-16 | Shionogi & Co | Hydroxypyrimidinone derivative having HIV integrase inhibitory activity |
| JP4895220B2 (ja) | 2004-04-06 | 2012-03-14 | ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド | キネシン有糸分裂インヒビター |
| US7273859B2 (en) | 2004-05-12 | 2007-09-25 | Bristol-Myers Squibb Company | HIV integrase inhibitors: cyclic pyrimidinone compounds |
| US7115601B2 (en) | 2004-05-18 | 2006-10-03 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7173022B2 (en) | 2004-05-28 | 2007-02-06 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7192948B2 (en) | 2004-05-28 | 2007-03-20 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7157447B2 (en) | 2004-05-28 | 2007-01-02 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7176196B2 (en) | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| WO2006060225A2 (en) | 2004-11-23 | 2006-06-08 | Merck & Co., Inc. | Process for asymmetric synthesis of hexahydropyrimido[1,2-a] azepine-2-carboxamides and related compounds |
| EP1866313A1 (en) * | 2005-03-31 | 2007-12-19 | Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. | Hiv integrase inhibitors |
| US7494984B2 (en) | 2005-08-31 | 2009-02-24 | Bristol-Myers Squibb Company | Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors |
| WO2007058646A1 (en) | 2005-11-15 | 2007-05-24 | Bristol-Myers Squibb Company | Hiv integrase inhibitors: cyclic pyrimidinone compounds |
| WO2007059125A2 (en) | 2005-11-15 | 2007-05-24 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| US7902182B2 (en) | 2005-11-16 | 2011-03-08 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US8039458B2 (en) | 2005-11-17 | 2011-10-18 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| WO2007064316A1 (en) | 2005-11-30 | 2007-06-07 | Bristol-Myers Squibb Company | Bicyclic heterocycles as hiv integrase inhibitors |
| WO2007143446A1 (en) | 2006-05-30 | 2007-12-13 | Bristol-Myers Squibb Company | Spiro-condensed heterotricyclic compounds as hiv integrase inhibitors |
| US7893055B2 (en) | 2006-06-28 | 2011-02-22 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
-
2009
- 2009-10-02 WO PCT/US2009/059308 patent/WO2010042392A2/en active Application Filing
- 2009-10-02 EP EP09740569.0A patent/EP2349276B1/en active Active
- 2009-10-02 WO PCT/US2009/059306 patent/WO2010042391A2/en active Application Filing
- 2009-10-02 KR KR1020117010300A patent/KR20110066224A/ko not_active Application Discontinuation
- 2009-10-02 CA CA2738814A patent/CA2738814C/en not_active Expired - Fee Related
- 2009-10-02 AU AU2009302663A patent/AU2009302663B2/en not_active Ceased
- 2009-10-02 PE PE2011000840A patent/PE20110344A1/es not_active Application Discontinuation
- 2009-10-02 EA EA201170537A patent/EA201170537A1/ru unknown
- 2009-10-02 MX MX2011003637A patent/MX2011003637A/es not_active Application Discontinuation
- 2009-10-02 CN CN2009801489012A patent/CN102239172A/zh active Pending
- 2009-10-02 US US12/572,341 patent/US8513234B2/en active Active
- 2009-10-02 BR BRPI0920605A patent/BRPI0920605A8/pt not_active IP Right Cessation
- 2009-10-02 JP JP2011530255A patent/JP4880097B1/ja not_active Expired - Fee Related
- 2009-10-05 AR ARP090103831A patent/AR073769A1/es unknown
- 2009-10-06 TW TW098133878A patent/TW201020251A/zh unknown
-
2011
- 2011-03-29 IL IL212019A patent/IL212019A0/en unknown
- 2011-04-04 DO DO2011000093A patent/DOP2011000093A/es unknown
- 2011-04-05 NI NI201100069A patent/NI201100069A/es unknown
- 2011-04-06 CR CR20110184A patent/CR20110184A/es unknown
- 2011-04-06 EC EC2011010959A patent/ECSP11010959A/es unknown
- 2011-04-08 ZA ZA2011/02620A patent/ZA201102620B/en unknown
- 2011-04-11 CO CO11044772A patent/CO6382127A2/es not_active Application Discontinuation
- 2011-05-02 MA MA33804A patent/MA32764B1/fr unknown
- 2011-09-30 JP JP2011215915A patent/JP5600311B2/ja not_active Expired - Fee Related
-
2013
- 2013-08-19 US US13/970,130 patent/US20130338141A1/en not_active Abandoned
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