HUP0202593A2 - Reverz transzkriptáz inhibitor hatású benzofenonok és ilyen vegyületeket tartalmazó gyógyászati készítmények - Google Patents

Reverz transzkriptáz inhibitor hatású benzofenonok és ilyen vegyületeket tartalmazó gyógyászati készítmények

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Publication number
HUP0202593A2
HUP0202593A2 HU0202593A HUP0202593A HUP0202593A2 HU P0202593 A2 HUP0202593 A2 HU P0202593A2 HU 0202593 A HU0202593 A HU 0202593A HU P0202593 A HUP0202593 A HU P0202593A HU P0202593 A2 HUP0202593 A2 HU P0202593A2
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HU
Hungary
Prior art keywords
group
optionally substituted
alkyl
compounds
benzophenones
Prior art date
Application number
HU0202593A
Other languages
English (en)
Inventor
Clarence Webster Andrews III.
Joseph Howing Chan
George Andrew Freeman
Pascal Maurice Charles Pianetti
Karen Rene Romines
Jeffrey H. Tidwell
Original Assignee
Glaxo Group Ltd.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Glaxo Group Ltd. filed Critical Glaxo Group Ltd.
Publication of HUP0202593A2 publication Critical patent/HUP0202593A2/hu
Publication of HUP0202593A3 publication Critical patent/HUP0202593A3/hu

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    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
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    • C07C255/42Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
    • C07C255/44Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms at least one of the singly-bound nitrogen atoms being acylated
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Abstract

A találmány (I) általános képletű vegyületekre és gyógyászatilagelfogadható származékaikra vonatkozik - ahol a képletben X jelentéseC, O vagy N; R1 jelentése 1-8 szénatomos alkilcsoport, 3-6 szénatomoscikloalkilcsoport; esetben szubsztituált 6-14 szénatomos arilcsoport;vagy adott esetben szubsztituált heterociklusos csoport; R2 jelentésehidrogénatom, halogénatom vagy 1-8 szénatomos alkilcsoport; R3 és R4jelentése egymástól függetlenül hidrogénatom; hidroxilcsoport; adottesetben szubsztituált heterociklusos csoport; R5 jelentésehidrogénatom, halogénatom, 1-8 szénatomos alkil-, -NO2, -NH2, 1-8szénatomos alkilamino-, -CF3 vagy alkoxicsoport. A találmány szerintivegyületek vírusos fertőzések, különösen HIV-fertőzés kezelésérealkalmasak. A találmány tárgyát képezik továbbá a fenti vegyületekettartalmazó gyógyászati készítmények. Ó
HU0202593A 1999-09-04 2000-08-31 Benzophenones as inhibitors of reverse transcriptase HUP0202593A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9920872.0A GB9920872D0 (en) 1999-09-04 1999-09-04 Benzophenones as inhibitors of reverse transcriptase
PCT/EP2000/008487 WO2001017982A1 (en) 1999-09-04 2000-08-31 Benzophenones as inhibitors of reverse transcriptase

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HUP0202593A2 true HUP0202593A2 (hu) 2002-12-28
HUP0202593A3 HUP0202593A3 (en) 2004-10-28

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HU0202593A HUP0202593A3 (en) 1999-09-04 2000-08-31 Benzophenones as inhibitors of reverse transcriptase

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Families Citing this family (42)

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Publication number Priority date Publication date Assignee Title
AU6589801A (en) * 2000-04-28 2001-11-12 F. Hoffmann-La Roche Ag P-(sulfonyl)aryl and heteroaryls
EA200401437A1 (ru) 2002-04-26 2005-04-28 Джилид Сайэнс, Инк. Ненуклеозидные ингибиторы обратной транскриптазы для лечения вич инфекции, способ их получения (варианты), способ увеличения периода полупревращения ненуклеозидного соединения, обладающего активностью против ретровирусов, и способ получения фармацевтической композиции, обладающей специфичностью к лейкоцитам
US7378550B2 (en) 2003-03-27 2008-05-27 Smithkline Beecham Corporation Process for preparing reverse transcriptase inhibitors
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
JP2006524710A (ja) 2003-04-25 2006-11-02 ギリアード サイエンシーズ, インコーポレイテッド キナーゼインヒビターホスホネート抱合体
US7432261B2 (en) 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
WO2004096287A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
DK1628685T3 (da) 2003-04-25 2011-03-21 Gilead Sciences Inc Antivirale phosphonatanaloge
US7470724B2 (en) 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US7407965B2 (en) 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
WO2005002626A2 (en) 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
WO2004096285A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
AU2004290298A1 (en) 2003-10-24 2005-05-26 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds
WO2005044279A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Purine nucleoside phosphonate conjugates
WO2005044308A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
CA2545821C (en) * 2003-12-22 2010-09-21 Basilea Pharmaceutica Ag Aroylfuranes and aroylthiophenes
US20080287471A1 (en) 2003-12-22 2008-11-20 Maria Fardis 4'-Substituted Carbovir And Abacavir-Derivatives As Well As Related Compounds With Hiv And Hcv Antiviral Activity
FR2866880A1 (fr) * 2004-02-27 2005-09-02 Oreal Para-phenylenediamine secondaire n-alkylaminee ortho-et/ou meta-substituee, composition de teinture des fibres keratiniques contenant une telle para-phenylenediamine, procedes mettant en oeuvre cette composition et utilisations
US7625949B2 (en) 2004-04-23 2009-12-01 Roche Palo Alto Llc Methods for treating retroviral infections
US7166738B2 (en) 2004-04-23 2007-01-23 Roche Palo Alto Llc Non-nucleoside reverse transcriptase inhibitors
CN1946680B (zh) * 2004-04-23 2011-04-06 弗·哈夫曼-拉罗切有限公司 非核苷逆转录酶抑制剂
WO2005121094A1 (en) * 2004-06-09 2005-12-22 Pfizer Limited Piperazine and piperidine derivatives as anti-hiv-agents
HUE043207T2 (hu) 2004-07-27 2019-08-28 Gilead Sciences Inc HIV-gátló vegyületek foszfonát analógjai
US20060025480A1 (en) * 2004-08-02 2006-02-02 Boehringer Ingelheim International Gmbh Benzoic acid derivatives as non nucleoside reverse transcriptase inhibitors
CA2577144C (en) * 2004-09-30 2011-06-21 Boehringer Ingelheim International Gmbh Alkynyl compounds as non-nucleoside reverse transcriptase inhibitors
EP1819348A1 (en) * 2004-12-01 2007-08-22 Boehringer Ingelheim International Gmbh Method for treating hiv infection through co-administration of tipranavir and gw695634
AR057455A1 (es) 2005-07-22 2007-12-05 Merck & Co Inc Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica
KR20080056220A (ko) 2005-10-19 2008-06-20 에프. 호프만-라 로슈 아게 페닐-아세트아마이드 nnrt 저해제
CN101108178B (zh) * 2006-07-20 2010-09-15 复旦大学 一种亲环素a抑制剂在制备抗艾滋病药物中的应用
US20100311965A1 (en) 2007-12-28 2010-12-09 Carna Biosciences Inc. 2-aminoquinazoline derivative
US20100093667A1 (en) 2008-07-08 2010-04-15 Gilead Sciences, Inc. Salts of hiv inhibitor compounds
WO2011060394A1 (en) * 2009-11-16 2011-05-19 Schering Corporation Compounds useful as chemokine receptor antagonists
CN102229547A (zh) * 2011-04-20 2011-11-02 复旦大学 一种萘苯醚类苯磺酰胺衍生物及其制备方法和用途
CN102206177A (zh) * 2011-04-20 2011-10-05 复旦大学 1-萘基苯甲酮衍生物及其制备方法和用途
CN102219717A (zh) * 2011-04-20 2011-10-19 复旦大学 N-苯基芳基甲酰胺衍生物及其制备方法和用途
CN102212022A (zh) * 2011-04-20 2011-10-12 复旦大学 二苯甲醇衍生物及其制备方法和用途
US10138255B2 (en) 2014-03-10 2018-11-27 Merck Sharp & Dohme Corp. Piperazine derivatives as HIV protease inhibitors
US10851125B2 (en) 2017-08-01 2020-12-01 Gilead Sciences, Inc. Crystalline forms of ethyl ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl(-L-alaninate
RU2729792C1 (ru) * 2019-07-29 2020-08-12 Акционерное общество "Научно-производственное объединение "ДОМ ФАРМАЦИИ" Способы повышения растворимости лекарственного средства на основе пиримидинового производного бензофенона
CN113444010B (zh) * 2020-03-28 2023-09-05 南京正大天晴制药有限公司 一种沙芬酰胺有关物质的制备方法
CN113461502B (zh) * 2021-07-15 2023-07-28 台州臻挚生物科技有限公司 2-羟基二苯甲酮类化合物及其卤化衍生物的制备方法
CN114163361B (zh) * 2021-12-14 2023-08-01 无锡捷化医药科技有限公司 一种3-溴-5-羟基苯磺酰胺的制备方法

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1552793A (hu) * 1966-12-07 1969-01-10
US4207234A (en) * 1975-07-07 1980-06-10 Fujisawa Pharmaceutical Co., Ltd. 4-Unsubstituted azetidinone derivatives and process for preparation thereof
JPS5973579A (ja) * 1982-10-19 1984-04-25 Kotobuki Seiyaku Kk ベンゾフラン又はベンゾチオフェン誘導体,この化合物を有効成分とする尿酸排泄剤及びその製造方法
JPS59181246A (ja) 1983-03-31 1984-10-15 Chugai Pharmaceut Co Ltd ベンゾフエノン誘導体
IN167395B (hu) * 1987-07-21 1990-10-20 Hoffmann La Roche
WO1993015043A1 (en) 1992-01-24 1993-08-05 Yoshitomi Pharmaceutical Industries, Ltd. Arylalkananilide compound and pharmaceutical use thereof
FR2716195B1 (fr) 1994-02-14 1996-06-21 Sanofi Sa Dérivés de 3-acylamino-5-phényl-1,4-benzodiazépin-2-one polysubstitués, leur procédé de préparation et les compositions pharmaceutiques les contenant.
AU687202B2 (en) 1994-05-31 1998-02-19 Teijin Limited Naphthalene derivative
EP1082310A4 (en) * 1998-04-29 2001-09-12 Univ Georgetown METHODS RELATING TO THE IDENTIFICATION AND USE OF COMPOUNDS THAT BIND TO HLA MOLECULES AS AGONISTS OR ANTAGONISTS TO HLA

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