TWI445709B - Ｈｉｖ複製之抑制劑 - Google Patents
Ｈｉｖ複製之抑制劑 Download PDFInfo
- Publication number
- TWI445709B TWI445709B TW100141049A TW100141049A TWI445709B TW I445709 B TWI445709 B TW I445709B TW 100141049 A TW100141049 A TW 100141049A TW 100141049 A TW100141049 A TW 100141049A TW I445709 B TWI445709 B TW I445709B
- Authority
- TW
- Taiwan
- Prior art keywords
- methyl
- mmol
- tetrahydro
- compound
- pyridin
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41361810P | 2010-11-15 | 2010-11-15 | |
| US201161485355P | 2011-05-12 | 2011-05-12 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201300395A TW201300395A (zh) | 2013-01-01 |
| TWI445709B true TWI445709B (zh) | 2014-07-21 |
Family
ID=44999830
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW100141049A TWI445709B (zh) | 2010-11-15 | 2011-11-10 | Ｈｉｖ複製之抑制劑 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US8809363B2 (https=) |
| EP (1) | EP2640729B1 (https=) |
| JP (2) | JP5902704B2 (https=) |
| CN (2) | CN103429595B (https=) |
| AR (1) | AR083870A1 (https=) |
| AU (2) | AU2011330850B2 (https=) |
| BR (1) | BR112013011991A2 (https=) |
| CA (1) | CA2817896A1 (https=) |
| CL (1) | CL2013001338A1 (https=) |
| MX (1) | MX343274B (https=) |
| RU (1) | RU2564445C2 (https=) |
| TW (1) | TWI445709B (https=) |
| UY (1) | UY33729A (https=) |
| WO (1) | WO2012066442A1 (https=) |
| ZA (1) | ZA201303433B (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0908394D0 (en) | 2009-05-15 | 2009-06-24 | Univ Leuven Kath | Novel viral replication inhibitors |
| MX2012015097A (es) | 2010-07-02 | 2013-05-28 | Gilead Sciences Inc | Derivados de acido naft-2-ilacetico para tratar sida. |
| EP2588455B1 (en) | 2010-07-02 | 2018-04-04 | Gilead Sciences, Inc. | 2-quinolinyl-acetic acid derivatives as hiv antiviral compounds |
| EP2640729B1 (en) * | 2010-11-15 | 2016-12-21 | VIIV Healthcare UK Limited | Inhibitors of hiv replication |
| KR20140003438A (ko) | 2010-11-15 | 2014-01-09 | 카톨리에케 유니버시테이트 루벤 | 항바이러스성 축합 헤테로사이클릭 화합물 |
| UA111841C2 (uk) | 2011-04-21 | 2016-06-24 | Гіліад Сайєнсіз, Інк. | Сполуки бензотіазолу та їх фармацевтичне застосування |
| WO2013062028A1 (ja) | 2011-10-25 | 2013-05-02 | 塩野義製薬株式会社 | Ｈｉｖ複製阻害剤 |
| US9284323B2 (en) | 2012-01-04 | 2016-03-15 | Gilead Sciences, Inc. | Naphthalene acetic acid derivatives against HIV infection |
| US9376392B2 (en) | 2012-01-04 | 2016-06-28 | Gilead Sciences, Inc. | 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS |
| UY34750A (es) | 2012-04-20 | 2013-11-29 | Gilead Sciences Inc | ?compuestos para el tratamiento del hiv, composiciones,métodos de preparación, intermediarios y métodos terapéuticos?. |
| US8906929B2 (en) | 2012-08-16 | 2014-12-09 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| TW201441197A (zh) | 2013-01-31 | 2014-11-01 | Shionogi & Co | Ｈｉｖ複製抑制劑 |
| WO2014164409A1 (en) | 2013-03-13 | 2014-10-09 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| ES2619708T3 (es) | 2013-03-13 | 2017-06-26 | VIIV Healthcare UK (No.5) Limited | Inhibidores de la replicación del virus de inmunodeficiencia humana |
| WO2014164467A1 (en) | 2013-03-13 | 2014-10-09 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| CN105008369B (zh) | 2013-03-14 | 2017-07-11 | 百时美施贵宝公司 | 人类免疫缺陷病毒复制抑制剂 |
| JP2016512558A (ja) | 2013-03-14 | 2016-04-28 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | ヒト免疫不全ウイルス複製の阻害剤 |
| TWI648272B (zh) | 2013-06-25 | 2019-01-21 | 美商必治妥美雅史谷比公司 | 經取代之四氫咔唑及咔唑甲醯胺化合物 |
| AU2014302550A1 (en) | 2013-06-25 | 2016-02-11 | Bristol-Myers Squibb Company | Carbazole carboxamide compounds useful as kinase inhibitors |
| EP2821082A1 (en) | 2013-07-05 | 2015-01-07 | Laboratoire Biodim | Method of producing an inactivated lentivirus, especially HIV, vaccine, kit and method of use |
| EP3105236B1 (en) | 2014-02-12 | 2017-10-18 | ViiV Healthcare UK (No.5) Limited | Benzothiazole macrocycles as inhibitors of human immunodeficiency virus replication |
| WO2015126758A1 (en) | 2014-02-18 | 2015-08-27 | Bristol-Myers Squibb Company | Imidazopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication |
| US9834566B2 (en) | 2014-02-18 | 2017-12-05 | VIIV Healthcare UK (No.5) Limited | Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication |
| US9409922B2 (en) | 2014-02-18 | 2016-08-09 | Bristol-Myers Squibb Company | Imidazopyridine macrocycles as inhibitors of human immunodeficiency virus replication |
| PT3107913T (pt) | 2014-02-19 | 2018-09-28 | Viiv Healthcare Uk No 5 Ltd | Inibidores da replicação do vírus da imunodeficiência humana |
| US9273067B2 (en) | 2014-02-19 | 2016-03-01 | Bristol-Myers Squibb Company | Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication |
| US9975906B2 (en) | 2014-05-16 | 2018-05-22 | Shionogi & Co., Ltd. | Tricyclic heterocycle derivatives having HIV replication inhibitory effect |
| MX2017005060A (es) | 2014-10-24 | 2017-07-05 | Bristol Myers Squibb Co | Compuestos atropisomeros triciclicos. |
| RS59707B1 (sr) | 2014-10-24 | 2020-01-31 | Bristol Myers Squibb Co | Derivati karbazola |
| PE20190710A1 (es) | 2014-10-24 | 2019-05-17 | Bristol Myers Squibb Co | Compuestos de indol carboxamida utiles como inhibidores de cinasas |
| EP3294277B1 (en) | 2015-05-08 | 2021-01-20 | Katholieke Universiteit Leuven | Functional cure of retroviral infection |
| TWI700284B (zh) | 2015-05-29 | 2020-08-01 | 日商塩野義製藥股份有限公司 | 具有ｈｉｖ複製抑制作用之含氮３環性衍生物 |
| CN111018912A (zh) * | 2019-11-22 | 2020-04-17 | 苏州二叶制药有限公司 | 一种抗病毒药物关键中间体的合成和纯化方法 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| US5489586A (en) * | 1994-03-07 | 1996-02-06 | Warner-Lambert Company | Method for treating inflammatory disease in humans |
| GB9518953D0 (en) | 1995-09-15 | 1995-11-15 | Pfizer Ltd | Pharmaceutical formulations |
| WO2000035296A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Improved release of medicament active agents from a chewing gum coating |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| EP1310488A4 (en) * | 2000-08-09 | 2005-08-10 | Mitsubishi Pharma Corp | CONCENTRATED BICYCLIC AMID COMPOUNDS AND THEIR MEDICAL USE |
| JP2003171381A (ja) | 2001-09-25 | 2003-06-20 | Takeda Chem Ind Ltd | エントリー阻害剤 |
| JP2003119137A (ja) | 2001-10-10 | 2003-04-23 | Japan Tobacco Inc | Ｈｉｖ阻害剤 |
| ATE355064T1 (de) | 2001-10-26 | 2006-03-15 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase |
| AU2002349675A1 (en) | 2001-12-05 | 2003-06-17 | Shionogi And Co., Ltd. | Derivative having hiv integrase inhibitory activity |
| CA2469592C (en) | 2001-12-12 | 2005-08-23 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| MY138657A (en) | 2001-12-21 | 2009-07-31 | Tibotec Pharm Ltd | broadspectrum heterocyclic substituted phenyl containing sulfonamide hiv protease inhibitors |
| EP1467970B1 (en) | 2002-01-17 | 2007-08-22 | Merck & Co., Inc. | Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors |
| TW200306192A (en) | 2002-01-18 | 2003-11-16 | Bristol Myers Squibb Co | Tricyclic 2-pyrimidone compounds useful as HIV reverse transcriptase inhibitors |
| US7875604B2 (en) * | 2004-02-04 | 2011-01-25 | University Of Virginia Patent Foundation | Compounds that inhibit HIV particle formation |
| JP2008524134A (ja) * | 2004-12-17 | 2008-07-10 | エフ．ホフマン−ラ ロシュ アーゲー | Ｇａｂａ−ｂアロステリックエンハンサーとしてのチエノ−ピリジン誘導体 |
| ES2402322T3 (es) * | 2007-11-15 | 2013-04-30 | Gilead Sciences, Inc. | Inhibidores de la replicación del virus de la inmunodeficiencia humana |
| RU2402531C2 (ru) * | 2008-09-24 | 2010-10-27 | Александр Леонидович Гинцбург | Биологически активные вещества, подавляющие патогенные бактерии |
| GB0908394D0 (en) * | 2009-05-15 | 2009-06-24 | Univ Leuven Kath | Novel viral replication inhibitors |
| GB0913636D0 (en) | 2009-08-05 | 2009-09-16 | Univ Leuven Kath | Novel viral replication inhibitors |
| SG181423A1 (en) | 2009-12-23 | 2012-07-30 | Univ Leuven Kath | Novel antiviral compounds |
| KR20140003438A (ko) | 2010-11-15 | 2014-01-09 | 카톨리에케 유니버시테이트 루벤 | 항바이러스성 축합 헤테로사이클릭 화합물 |
| EP2640729B1 (en) * | 2010-11-15 | 2016-12-21 | VIIV Healthcare UK Limited | Inhibitors of hiv replication |
| WO2012102985A1 (en) | 2011-01-24 | 2012-08-02 | Glaxosmithkline Llc | Isoquinoline compounds and methods for treating hiv |
| WO2013012649A1 (en) | 2011-07-15 | 2013-01-24 | Glaxosmithkline Llc | Azaindole compounds and methods for treating hiv |
-
2011
- 2011-11-01 EP EP11785122.0A patent/EP2640729B1/en active Active
- 2011-11-01 RU RU2013121788/04A patent/RU2564445C2/ru not_active IP Right Cessation
- 2011-11-01 AU AU2011330850A patent/AU2011330850B2/en not_active Ceased
- 2011-11-01 CN CN201180065030.5A patent/CN103429595B/zh not_active Expired - Fee Related
- 2011-11-01 BR BR112013011991A patent/BR112013011991A2/pt not_active IP Right Cessation
- 2011-11-01 JP JP2013538301A patent/JP5902704B2/ja not_active Expired - Fee Related
- 2011-11-01 MX MX2013005486A patent/MX343274B/es active IP Right Grant
- 2011-11-01 WO PCT/IB2011/054852 patent/WO2012066442A1/en not_active Ceased
- 2011-11-01 CN CN201510602538.4A patent/CN105330675A/zh active Pending
- 2011-11-01 CA CA2817896A patent/CA2817896A1/en not_active Abandoned
- 2011-11-10 TW TW100141049A patent/TWI445709B/zh not_active IP Right Cessation
- 2011-11-14 AR ARP110104246A patent/AR083870A1/es unknown
- 2011-11-14 US US13/295,167 patent/US8809363B2/en not_active Expired - Fee Related
- 2011-11-14 UY UY0001033729A patent/UY33729A/es not_active Application Discontinuation
-
2013
- 2013-05-10 ZA ZA2013/03433A patent/ZA201303433B/en unknown
- 2013-05-14 CL CL2013001338A patent/CL2013001338A1/es unknown
-
2014
- 2014-07-02 US US14/322,134 patent/US9447116B2/en not_active Expired - Fee Related
-
2016
- 2016-03-10 JP JP2016046384A patent/JP2016164163A/ja active Pending
- 2016-04-22 AU AU2016202565A patent/AU2016202565A1/en not_active Abandoned
- 2016-08-19 US US15/241,520 patent/US20160355528A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP2013542247A (ja) | 2013-11-21 |
| JP5902704B2 (ja) | 2016-04-13 |
| MX2013005486A (es) | 2013-12-12 |
| UY33729A (es) | 2012-06-29 |
| CL2013001338A1 (es) | 2014-03-28 |
| CN103429595A (zh) | 2013-12-04 |
| BR112013011991A2 (pt) | 2016-08-30 |
| US9447116B2 (en) | 2016-09-20 |
| US20140315927A1 (en) | 2014-10-23 |
| CN105330675A (zh) | 2016-02-17 |
| RU2564445C2 (ru) | 2015-10-10 |
| AU2011330850B2 (en) | 2016-01-28 |
| ZA201303433B (en) | 2014-12-23 |
| AU2011330850A1 (en) | 2013-06-27 |
| TW201300395A (zh) | 2013-01-01 |
| WO2012066442A1 (en) | 2012-05-24 |
| US20120136023A1 (en) | 2012-05-31 |
| EP2640729B1 (en) | 2016-12-21 |
| AR083870A1 (es) | 2013-03-27 |
| CN103429595B (zh) | 2015-10-21 |
| RU2013121788A (ru) | 2014-12-27 |
| JP2016164163A (ja) | 2016-09-08 |
| CA2817896A1 (en) | 2012-05-24 |
| US8809363B2 (en) | 2014-08-19 |
| EP2640729A1 (en) | 2013-09-25 |
| US20160355528A1 (en) | 2016-12-08 |
| MX343274B (es) | 2016-10-31 |
| AU2016202565A1 (en) | 2016-05-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Annulment or lapse of patent due to non-payment of fees |