HRP20210748T1 - Postupak priprave spojeva s aktivnošću inhibitora hiv integraze - Google Patents
Postupak priprave spojeva s aktivnošću inhibitora hiv integraze Download PDFInfo
- Publication number
- HRP20210748T1 HRP20210748T1 HRP20210748TT HRP20210748T HRP20210748T1 HR P20210748 T1 HRP20210748 T1 HR P20210748T1 HR P20210748T T HRP20210748T T HR P20210748TT HR P20210748 T HRP20210748 T HR P20210748T HR P20210748 T1 HRP20210748 T1 HR P20210748T1
- Authority
- HR
- Croatia
- Prior art keywords
- inhivitory
- activity
- hiv integrase
- producing compounds
- maxima
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 3
- 108010002459 HIV Integrase Proteins 0.000 title 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 239000013078 crystal Substances 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 238000001228 spectrum Methods 0.000 claims 2
Classifications
-
- 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
- C07D498/12—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 three hetero rings
- C07D498/14—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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
- C07D211/94—Oxygen atom, e.g. piperidine N-oxide
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
- C07D213/80—Acids; Esters in position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Heat Sensitive Colour Forming Recording (AREA)
Claims (2)
1. Kristal spoja kojeg prikazuje formula (U2) ili njegovog solvata:
[image]
,
(gdje je Me metil, a Bn je benzil)
naznačen time što ima maksimume u difrakcijskom spektaru rendgenskih zraka na prahu pod difrakcijskim kutom (2θ): 7,3° ± 0,2°, 14,4° ± 0,2°, 16,1° ± 0,2°, 18,4° ± 0,2°, 22,3° ± 0,2° i 23,1° ± 0,2°.
2. Kristal spoja kojeg prikazuje formula (U3) ili njegovog solvata:
[image]
,
(gdje je Me metil, a Bn je benzil)
naznačen time što ima maksimume u difrakcijskom spektaru rendgenskih zraka na prahu pod difrakcijskim kutom (2θ): 7,2° ± 0,2°, 16,1° ± 0,2°, 18,3° ± 0,2°, 20,6° ± 0,2°, 22,6° ± 0,2°, 23,1° ± 0,2° i 23,7° ± 0,2°.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2010175899 | 2010-08-05 | ||
JP2010277713 | 2010-12-14 | ||
EP18203589.9A EP3456721B1 (en) | 2010-08-05 | 2011-08-04 | Method of producing compounds having hiv integrase inhivitory activity |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20210748T1 true HRP20210748T1 (hr) | 2021-06-25 |
Family
ID=45559561
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20210748TT HRP20210748T1 (hr) | 2010-08-05 | 2021-05-12 | Postupak priprave spojeva s aktivnošću inhibitora hiv integraze |
Country Status (18)
Country | Link |
---|---|
US (8) | US20140011995A1 (hr) |
EP (3) | EP3456721B1 (hr) |
JP (1) | JP5636054B2 (hr) |
CN (3) | CN106083891B (hr) |
BR (1) | BR112013002461A2 (hr) |
CY (1) | CY1124582T1 (hr) |
DK (1) | DK3456721T3 (hr) |
ES (3) | ES2710609T3 (hr) |
HR (1) | HRP20210748T1 (hr) |
HU (1) | HUE054473T2 (hr) |
LT (1) | LT3456721T (hr) |
PL (1) | PL3456721T3 (hr) |
PT (3) | PT3456721T (hr) |
RS (1) | RS61796B1 (hr) |
SG (1) | SG187683A1 (hr) |
SI (1) | SI3456721T1 (hr) |
TW (1) | TWI510451B (hr) |
WO (1) | WO2012018065A1 (hr) |
Families Citing this family (42)
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EP2320909B8 (en) | 2008-07-25 | 2016-03-30 | VIIV Healthcare Company | Chemical compounds |
KR101678563B1 (ko) | 2008-12-11 | 2016-11-22 | 비이브 헬쓰케어 컴퍼니 | 카르바모일피리돈 hiv 인테그라제 억제제를 위한 제조방법 및 중간체 |
MX351942B (es) | 2008-12-11 | 2017-11-03 | Shionogi & Co | Sintesis de inhibidores de integrasa de vih de carbamoil-piridona e intermediarios. |
TWI518084B (zh) | 2009-03-26 | 2016-01-21 | 鹽野義製藥股份有限公司 | 哌喃酮與吡啶酮衍生物之製造方法 |
TWI582097B (zh) | 2010-03-23 | 2017-05-11 | Viiv醫療保健公司 | 製備胺甲醯吡啶酮衍生物及中間體之方法 |
ES2710609T3 (es) * | 2010-08-05 | 2019-04-26 | Shionogi & Co | Procedimiento de preparación de un compuesto que tiene actividad inhibidora de la integrasa del HIV |
UA114351C2 (uk) | 2012-12-21 | 2017-05-25 | Гіліад Сайєнсіз, Інк. | Поліциклічні карбамоїлпіридонові сполуки та їх фармацевтичне застосування |
NO2865735T3 (hr) | 2013-07-12 | 2018-07-21 | ||
PL3019503T3 (pl) | 2013-07-12 | 2018-01-31 | Gilead Sciences Inc | Policykliczne związki karbamoilopirydonowe i ich zastosowanie do leczenia infekcji hiv |
US9856271B2 (en) | 2014-01-21 | 2018-01-02 | Laurus Labs Limited | Process for the preparation of dolutegravir and pharmaceutically acceptable salts thereof |
CN106831819B (zh) * | 2014-03-19 | 2019-01-04 | 杭州普晒医药科技有限公司 | 德罗格韦钠盐的晶型及其制备方法 |
NO2717902T3 (hr) | 2014-06-20 | 2018-06-23 | ||
TWI677489B (zh) * | 2014-06-20 | 2019-11-21 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
TW201613936A (en) | 2014-06-20 | 2016-04-16 | Gilead Sciences Inc | Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide |
EP3229804B1 (en) * | 2014-12-09 | 2020-05-06 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as hiv integrase inhibitors |
WO2016092527A1 (en) * | 2014-12-12 | 2016-06-16 | Sun Pharmaceutical Industries Limited | A process for the preparation of dolutegravir |
TWI695003B (zh) | 2014-12-23 | 2020-06-01 | 美商基利科學股份有限公司 | 多環胺甲醯基吡啶酮化合物及其醫藥用途 |
CN104557686A (zh) * | 2014-12-29 | 2015-04-29 | 徐俊烨 | 一种吡啶酮类化合物的合成方法 |
EP3045461A1 (en) | 2015-01-16 | 2016-07-20 | LEK Pharmaceuticals d.d. | Processes for preparing dolutegravir and analogues thereof |
SI3466490T1 (sl) | 2015-04-02 | 2020-12-31 | Gilead Sciences, Inc. | Policiklične spojine karbamoilpiridona in njihova farmacevtska uporaba |
EP3394069B1 (en) | 2015-12-21 | 2019-05-22 | Lupin Limited | Process for the preparation of hiv integrase inhibitors |
EP4299133A3 (en) * | 2016-06-23 | 2024-03-13 | VIIV Healthcare Company | Compositions and methods for the delivery of therapeutics |
JOP20190130A1 (ar) | 2016-12-02 | 2019-06-02 | Merck Sharp & Dohme | مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv) |
ZA201803942B (en) * | 2017-06-13 | 2021-05-26 | Cipla Ltd | Novel processes for preparation of integrase inhibitor |
US11286262B2 (en) | 2017-10-06 | 2022-03-29 | Shionogi & Co., Ltd. | Stereoselective process for preparing substituted polycyclic pyridone derivatives |
CN108101838B (zh) * | 2017-12-18 | 2020-10-20 | 安徽唯诗杨信息科技有限公司 | 一种度鲁特韦中间体的合成方法及其有关物质检测方法 |
US11634431B2 (en) | 2018-07-12 | 2023-04-25 | Laurus Labs Limited | Process for purification of protected polycyclic carbamoylpyridone derivatives |
KR20210081394A (ko) | 2018-10-22 | 2021-07-01 | 보드 오브 리젠츠 오브 디 유니버시티 오브 네브라스카 | 항바이러스성 프로드러그 및 이의 나노제제 |
UA127822C2 (uk) | 2019-03-22 | 2024-01-10 | Гіліад Сайєнсіз, Інк. | Місткові трициклічні карбамоїлпіридонові сполуки та їх фармацевтичне застосування |
CN110396099A (zh) * | 2019-05-22 | 2019-11-01 | 博诺康源(北京)药业科技有限公司 | 一种度鲁特韦原料中非对映异构体杂质的合成方法 |
CN110128448A (zh) * | 2019-05-22 | 2019-08-16 | 博诺康源(北京)药业科技有限公司 | 一种度鲁特韦原料及中间体中非对映异构体杂质的合成方法 |
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CN110698473B (zh) * | 2019-10-08 | 2020-12-18 | 浙江大学 | 哌嗪酮并羟基吡啶酮-5-羧基类化合物及制备和应用 |
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CN111620891B (zh) * | 2020-05-27 | 2023-07-14 | 上海启讯医药科技有限公司 | 一种多替拉韦关键中间体溶剂化物多晶型物及其制备方法和用途 |
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CN112480007B (zh) * | 2020-12-08 | 2022-11-18 | 宿迁市科莱博生物化学有限公司 | 一种1,3-二甲基-1h-吡唑-4-羧酸的合成方法 |
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KR101678563B1 (ko) | 2008-12-11 | 2016-11-22 | 비이브 헬쓰케어 컴퍼니 | 카르바모일피리돈 hiv 인테그라제 억제제를 위한 제조방법 및 중간체 |
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2011
- 2011-08-04 ES ES16190894T patent/ES2710609T3/es active Active
- 2011-08-04 LT LTEP18203589.9T patent/LT3456721T/lt unknown
- 2011-08-04 PL PL18203589T patent/PL3456721T3/pl unknown
- 2011-08-04 DK DK18203589.9T patent/DK3456721T3/da active
- 2011-08-04 EP EP18203589.9A patent/EP3456721B1/en active Active
- 2011-08-04 JP JP2012527760A patent/JP5636054B2/ja active Active
- 2011-08-04 SI SI201131966T patent/SI3456721T1/sl unknown
- 2011-08-04 PT PT182035899T patent/PT3456721T/pt unknown
- 2011-08-04 ES ES11814690.1T patent/ES2608377T3/es active Active
- 2011-08-04 PT PT16190894T patent/PT3127908T/pt unknown
- 2011-08-04 ES ES18203589T patent/ES2870006T3/es active Active
- 2011-08-04 RS RS20210566A patent/RS61796B1/sr unknown
- 2011-08-04 PT PT118146901T patent/PT2602260T/pt unknown
- 2011-08-04 CN CN201610447148.9A patent/CN106083891B/zh active Active
- 2011-08-04 EP EP11814690.1A patent/EP2602260B1/en active Active
- 2011-08-04 CN CN201610447110.1A patent/CN106046022B/zh active Active
- 2011-08-04 SG SG2013008057A patent/SG187683A1/en unknown
- 2011-08-04 HU HUE18203589A patent/HUE054473T2/hu unknown
- 2011-08-04 EP EP16190894.2A patent/EP3127908B1/en active Active
- 2011-08-04 CN CN201180048343.XA patent/CN103154004B/zh active Active
- 2011-08-04 US US13/814,333 patent/US20140011995A1/en not_active Abandoned
- 2011-08-04 BR BR112013002461A patent/BR112013002461A2/pt not_active Application Discontinuation
- 2011-08-04 WO PCT/JP2011/067832 patent/WO2012018065A1/ja active Application Filing
- 2011-08-05 TW TW100127858A patent/TWI510451B/zh active
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2014
- 2014-10-20 US US14/518,209 patent/US9321789B2/en active Active
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2016
- 2016-03-17 US US15/072,388 patent/US9650394B2/en active Active
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2017
- 2017-03-28 US US15/471,133 patent/US9802959B2/en active Active
- 2017-09-20 US US15/709,716 patent/US10125146B2/en active Active
- 2017-09-20 US US15/709,742 patent/US9969750B2/en active Active
- 2017-09-20 US US15/709,701 patent/US10000508B2/en active Active
- 2017-09-20 US US15/709,728 patent/US10125147B2/en active Active
-
2021
- 2021-05-12 HR HRP20210748TT patent/HRP20210748T1/hr unknown
- 2021-05-17 CY CY20211100423T patent/CY1124582T1/el unknown
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