MX2018001722A - Derivados del acido 5-(n-bencil-tetrahidroisoquinolin-6-il)-piridi n-3-il acetico como inhibidores de la replicacion del virus de la inmunodeficiencia humana. - Google Patents
Derivados del acido 5-(n-bencil-tetrahidroisoquinolin-6-il)-piridi n-3-il acetico como inhibidores de la replicacion del virus de la inmunodeficiencia humana.Info
- Publication number
- MX2018001722A MX2018001722A MX2018001722A MX2018001722A MX2018001722A MX 2018001722 A MX2018001722 A MX 2018001722A MX 2018001722 A MX2018001722 A MX 2018001722A MX 2018001722 A MX2018001722 A MX 2018001722A MX 2018001722 A MX2018001722 A MX 2018001722A
- Authority
- MX
- Mexico
- Prior art keywords
- alkyl
- alkoxy
- compounds
- tetrahydroisoquinolin
- pyridin
- Prior art date
Links
- WGNUNYPERJMVRM-UHFFFAOYSA-N 3-pyridylacetic acid Chemical class OC(=O)CC1=CC=CN=C1 WGNUNYPERJMVRM-UHFFFAOYSA-N 0.000 title 1
- 241000725303 Human immunodeficiency virus Species 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 230000029812 viral genome replication Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- -1 homopiperidinyl Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 208000030507 AIDS Diseases 0.000 abstract 1
- 108010002459 HIV Integrase Proteins 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 abstract 1
- 125000005433 dihydrobenzodioxinyl group Chemical group O1C(COC2=C1C=CC=C2)* 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 abstract 1
Classifications
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- A61K31/435—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
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Virology (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (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)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se divulgan compuestos de Fórmula I, incluyendo sales farmacéuticamente aceptables, composiciones farmacéuticas que comprenden los compuestos, procedimientos de preparación de los compuestos y su uso en la inhibición de la integrasa del VIH y tratamiento de infectados con el VIH o SIDA. En los compuestos de la fórmula (I); R1 está seleccionado de hidrógeno, alquilo o cicloalquilo; R2 está seleccionado de tetrahidroisoquinolinilo y está sustituido con 1 sustituyente R6 y también con 0-3 sustituyentes halo o alquilo; R3 está seleccionado de azetidinilo, pirrolidinilo, piperidinilo, piperazinilo, morfolinilo, homopiperidinilo, homopiperazinilo u homomorfolinilo, y está sustituido con 0-3 sustituyentes seleccionados de ciano, halo, alquilo, haloalquilo, alcoxi y haloalcoxi; R4 está seleccionado de alquilo o haloalquilo; R5 es alquilo; R6 está seleccionado de Ar1, (Ar1)alquilo, (cromanil)alquilo, cianocicloalquilo o (dihidrobenzodioxinil)alqui lo; y Ar1 es fenilo sustituido con 0-5 sustituyentes seleccionados de ciano, halo, alquilo, cicloalquilo, haloalquilo, hidroxi, alcoxi, haloalcoxi, (hidroxi)alcoxi, (alcoxi)alcoxi, fenoxi, benciloxi, carboxi, fenilo y cianocicloalquilo. (ver Fórmula).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562203791P | 2015-08-11 | 2015-08-11 | |
| PCT/IB2016/054832 WO2017025917A1 (en) | 2015-08-11 | 2016-08-10 | 5-(n-benzyl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2018001722A true MX2018001722A (es) | 2018-05-16 |
Family
ID=56851651
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2018001722A MX2018001722A (es) | 2015-08-11 | 2016-08-10 | Derivados del acido 5-(n-bencil-tetrahidroisoquinolin-6-il)-piridi n-3-il acetico como inhibidores de la replicacion del virus de la inmunodeficiencia humana. |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US10189816B2 (es) |
| EP (1) | EP3334716A1 (es) |
| JP (1) | JP6782766B2 (es) |
| KR (1) | KR20180032649A (es) |
| CN (1) | CN108137534A (es) |
| AR (1) | AR105653A1 (es) |
| AU (1) | AU2016306089B2 (es) |
| CA (1) | CA2994791A1 (es) |
| CL (1) | CL2018000363A1 (es) |
| CO (1) | CO2018001359A2 (es) |
| CR (1) | CR20180091A (es) |
| DO (1) | DOP2018000035A (es) |
| EA (1) | EA033057B1 (es) |
| HK (1) | HK1249503A1 (es) |
| IL (1) | IL257240B (es) |
| MA (1) | MA42614A (es) |
| MX (1) | MX2018001722A (es) |
| PE (1) | PE20181002A1 (es) |
| PH (1) | PH12018500294A1 (es) |
| TW (1) | TWI657086B (es) |
| UA (1) | UA120464C2 (es) |
| WO (1) | WO2017025917A1 (es) |
| ZA (1) | ZA201800689B (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3334723B1 (en) * | 2015-08-12 | 2019-09-18 | VIIV Healthcare UK (No.5) Limited | 5-(n-[6,5]-fused bicyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
| TW201718537A (zh) * | 2015-08-12 | 2017-06-01 | Viiv醫療保健英國(No.5)有限公司 | 做為人類免疫缺陷病毒複製抑制劑之吡啶-3-基乙酸衍生物 |
| EP3455217A1 (en) * | 2016-05-11 | 2019-03-20 | ViiV Healthcare UK (No.5) Limited | Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
| US10407410B2 (en) | 2016-05-11 | 2019-09-10 | VIIV Healthcare UK (No.5) Limited | Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
| US20190152957A1 (en) * | 2016-05-11 | 2019-05-23 | VIIV Healthcare UK (No.5) Limited | Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
| US20200016136A1 (en) * | 2017-01-03 | 2020-01-16 | Viiv Healthcare Uk (No. 5) Limited | Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
| WO2018127800A1 (en) * | 2017-01-03 | 2018-07-12 | VIIV Healthcare UK (No.5) Limited | Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7939545B2 (en) * | 2006-05-16 | 2011-05-10 | Boehringer Ingelheim International Gmbh | Inhibitors of human immunodeficiency virus replication |
| JP5269086B2 (ja) * | 2007-11-15 | 2013-08-21 | ギリアード サイエンシス インコーポレーテッド | ヒト免疫不全ウイルスの複製阻害薬 |
| WO2009062288A1 (en) | 2007-11-15 | 2009-05-22 | Boehringer Ingelheim International Gmbh | Inhibitors of human immunodeficiency virus replication |
| WO2009062308A1 (en) | 2007-11-16 | 2009-05-22 | Boehringer Ingelheim International Gmbh | Inhibitors of human immunodeficiency virus replication |
| BRPI0820307A2 (pt) | 2007-11-16 | 2019-09-24 | Boehringer Ingelheim Int | inibidores de replicação do vírus da imunodeficiência humana |
| US8338441B2 (en) * | 2009-05-15 | 2012-12-25 | Gilead Sciences, Inc. | Inhibitors of human immunodeficiency virus replication |
| 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 |
| KR101483834B1 (ko) | 2009-12-23 | 2015-01-16 | 카트호리이케 유니버시타이트 로이펜 | 항바이러스 화합물 |
| US8633200B2 (en) | 2010-09-08 | 2014-01-21 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| US8629276B2 (en) | 2012-02-15 | 2014-01-14 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| US9034882B2 (en) | 2012-03-05 | 2015-05-19 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| CN105189511B (zh) | 2013-03-13 | 2017-05-24 | 百时美施贵宝公司 | 人免疫缺陷病毒复制的抑制剂 |
| ES2623904T3 (es) | 2013-03-14 | 2017-07-12 | VIIV Healthcare UK (No.5) Limited | Inhibidores de la replicación del virus de la inmunodeficiencia humana |
| US9193720B2 (en) * | 2014-02-20 | 2015-11-24 | Bristol-Myers Squibb Company | Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
| PT3116880T (pt) * | 2014-02-20 | 2018-05-10 | Viiv Healthcare Uk No 5 Ltd | Macrociclos de ácido piridin-3-il acético como inibidores da replicação do vírus da imunodeficiência humana |
| EP3334723B1 (en) * | 2015-08-12 | 2019-09-18 | VIIV Healthcare UK (No.5) Limited | 5-(n-[6,5]-fused bicyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
| TW201718537A (zh) * | 2015-08-12 | 2017-06-01 | Viiv醫療保健英國(No.5)有限公司 | 做為人類免疫缺陷病毒複製抑制劑之吡啶-3-基乙酸衍生物 |
| US10214516B2 (en) * | 2015-08-12 | 2019-02-26 | VIIV Healthcare UK (No.5) Limited | 5-(N-fused tricyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
-
2016
- 2016-08-09 TW TW105125345A patent/TWI657086B/zh not_active IP Right Cessation
- 2016-08-09 AR ARP160102438A patent/AR105653A1/es unknown
- 2016-08-10 EP EP16758283.2A patent/EP3334716A1/en not_active Withdrawn
- 2016-08-10 PE PE2018000174A patent/PE20181002A1/es unknown
- 2016-08-10 AU AU2016306089A patent/AU2016306089B2/en not_active Ceased
- 2016-08-10 MA MA042614A patent/MA42614A/fr unknown
- 2016-08-10 CA CA2994791A patent/CA2994791A1/en not_active Abandoned
- 2016-08-10 CR CR20180091A patent/CR20180091A/es unknown
- 2016-08-10 HK HK18108030.5A patent/HK1249503A1/zh unknown
- 2016-08-10 JP JP2018507010A patent/JP6782766B2/ja active Active
- 2016-08-10 KR KR1020187006791A patent/KR20180032649A/ko not_active Withdrawn
- 2016-08-10 WO PCT/IB2016/054832 patent/WO2017025917A1/en not_active Ceased
- 2016-08-10 UA UAA201801137A patent/UA120464C2/uk unknown
- 2016-08-10 US US15/749,176 patent/US10189816B2/en active Active
- 2016-08-10 EA EA201890361A patent/EA033057B1/ru not_active IP Right Cessation
- 2016-08-10 CN CN201680059469.XA patent/CN108137534A/zh active Pending
- 2016-08-10 MX MX2018001722A patent/MX2018001722A/es unknown
-
2018
- 2018-01-30 IL IL257240A patent/IL257240B/en not_active IP Right Cessation
- 2018-02-01 ZA ZA2018/00689A patent/ZA201800689B/en unknown
- 2018-02-06 DO DO2018000035A patent/DOP2018000035A/es unknown
- 2018-02-08 CL CL2018000363A patent/CL2018000363A1/es unknown
- 2018-02-09 PH PH12018500294A patent/PH12018500294A1/en unknown
- 2018-02-09 CO CONC2018/0001359A patent/CO2018001359A2/es unknown
- 2018-11-28 US US16/202,653 patent/US20190092754A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| DOP2018000035A (es) | 2018-03-30 |
| JP2018522927A (ja) | 2018-08-16 |
| IL257240B (en) | 2020-02-27 |
| ZA201800689B (en) | 2021-08-25 |
| UA120464C2 (uk) | 2019-12-10 |
| CR20180091A (es) | 2018-06-13 |
| AU2016306089A1 (en) | 2018-03-01 |
| CN108137534A (zh) | 2018-06-08 |
| EP3334716A1 (en) | 2018-06-20 |
| PE20181002A1 (es) | 2018-06-26 |
| TW201718549A (zh) | 2017-06-01 |
| HK1249503A1 (zh) | 2018-11-02 |
| MA42614A (fr) | 2021-05-26 |
| EA033057B1 (ru) | 2019-08-30 |
| CO2018001359A2 (es) | 2018-05-10 |
| IL257240A (en) | 2018-03-29 |
| US10189816B2 (en) | 2019-01-29 |
| CA2994791A1 (en) | 2017-02-16 |
| EA201890361A1 (ru) | 2018-11-30 |
| AU2016306089B2 (en) | 2018-08-09 |
| US20180230129A1 (en) | 2018-08-16 |
| JP6782766B2 (ja) | 2020-11-11 |
| WO2017025917A1 (en) | 2017-02-16 |
| TWI657086B (zh) | 2019-04-21 |
| KR20180032649A (ko) | 2018-03-30 |
| US20190092754A1 (en) | 2019-03-28 |
| AR105653A1 (es) | 2017-10-25 |
| PH12018500294A1 (en) | 2018-08-13 |
| CL2018000363A1 (es) | 2018-07-06 |
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