RU2004129767A - Хинолиновые производные - Google Patents
Хинолиновые производные Download PDFInfo
- Publication number
- RU2004129767A RU2004129767A RU2004129767/04A RU2004129767A RU2004129767A RU 2004129767 A RU2004129767 A RU 2004129767A RU 2004129767/04 A RU2004129767/04 A RU 2004129767/04A RU 2004129767 A RU2004129767 A RU 2004129767A RU 2004129767 A RU2004129767 A RU 2004129767A
- Authority
- RU
- Russia
- Prior art keywords
- formula
- acid addition
- free base
- addition salt
- compound
- Prior art date
Links
- 229940027991 antiseptic and disinfectant quinoline derivative Drugs 0.000 title 1
- 125000002943 quinolinyl group Chemical class N1=C(C=CC2=CC=CC=C12)* 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 7
- 239000002253 acid Substances 0.000 claims 5
- 239000012458 free base Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 208000010412 Glaucoma Diseases 0.000 claims 3
- 208000001491 myopia Diseases 0.000 claims 3
- 230000004379 myopia Effects 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 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
- C07D401/02—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
- C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Ophthalmology & Optometry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (5)
1. Соединение формулы Ia
где А и Q каждый представляет собой Н или вместе образуют дополнительную связь и где асимметричный центр в положении 3 может быть рацемическим или в виде оптически активной формы, и где R представляет собой формулу Ib или Ic
и где R1 представляет собой алкил в форме свободного основания или в форме кислотной аддитивной соли.
2. Соединение по п.1, где указанное соединение выбрано из группы, состоящей из соединения формулы I и соединения формулы II
где СН2-S-имидазольный заместитель в формуле I находится в 3R конфигурации, как указано выше в формуле I в форме свободного основания или в форме кислотной аддитивной соли.
3. Соединение по п.1 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли для применения для лечения глаукомы и миопии.
4. Применение соединения по п.1 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли для изготовления лекарственного средства для лечения глаукомы и миопии.
5. Способ лечения глаукомы и миопии у субъекта, нуждающегося в таком лечении, который включает введение такому субъекту терапевтически эффективного количества соединения по п.1 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02005115 | 2002-03-07 | ||
| EP02005117 | 2002-03-07 | ||
| EP02005115.7 | 2002-03-07 | ||
| EP02005117.3 | 2002-03-07 | ||
| EP02005117,3 | 2002-03-07 | ||
| EP02005115,7 | 2002-03-07 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2004129767A true RU2004129767A (ru) | 2005-06-27 |
| RU2345991C2 RU2345991C2 (ru) | 2009-02-10 |
Family
ID=27790094
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2004129767/04A RU2345991C2 (ru) | 2002-03-07 | 2003-03-06 | Хинолиновые производные |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US7399768B2 (ru) |
| EP (1) | EP1480970B1 (ru) |
| JP (2) | JP2005519117A (ru) |
| KR (1) | KR101027977B1 (ru) |
| CN (2) | CN1293070C (ru) |
| AR (1) | AR038730A1 (ru) |
| AU (1) | AU2003219023B2 (ru) |
| BR (1) | BR0308201A (ru) |
| CA (2) | CA2706618A1 (ru) |
| CO (1) | CO5611196A2 (ru) |
| CY (1) | CY1106409T1 (ru) |
| DE (1) | DE60311233T2 (ru) |
| DK (1) | DK1480970T3 (ru) |
| EC (1) | ECSP045271A (ru) |
| EG (1) | EG24415A (ru) |
| ES (1) | ES2279100T3 (ru) |
| IL (1) | IL163769A0 (ru) |
| MX (1) | MXPA04008666A (ru) |
| MY (1) | MY134325A (ru) |
| NO (1) | NO20044117L (ru) |
| NZ (1) | NZ534732A (ru) |
| PE (1) | PE20030927A1 (ru) |
| PL (2) | PL215012B1 (ru) |
| PT (1) | PT1480970E (ru) |
| RU (1) | RU2345991C2 (ru) |
| SI (1) | SI1480970T1 (ru) |
| TW (1) | TW200406401A (ru) |
| WO (1) | WO2003074511A1 (ru) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1757601E (pt) * | 2002-03-07 | 2009-10-23 | Novartis Ag | Derivados de quinolina e sua utilização em glaucoma e miopia |
| CN111386267B (zh) | 2017-11-24 | 2023-12-12 | H.隆德贝克有限公司 | 用于治疗帕金森病的新儿茶酚胺前药 |
| US11111263B2 (en) | 2019-05-20 | 2021-09-07 | H. Lundbeck A/S | Process for the manufacture of (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid |
| US11168056B2 (en) | 2019-05-20 | 2021-11-09 | H. Lundbeck A/S | Process for the manufacturing of (6aR,10aR)-7-propyl-6,6a,7,8,9,10,10a,11-octahydro-[1,3]dioxolo[4′,5′:5,6]benzo[1,2-G]quinoline and (4aR,10aR)-1-propyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[G]quinoline-6,7-diol |
| US11130775B2 (en) | 2019-05-20 | 2021-09-28 | H. Lundbeck A/S | Solid forms of (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4A,5,10,10A-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid |
| US11104697B2 (en) | 2019-05-20 | 2021-08-31 | H. Lundbeck A/S | Process for the manufacture of (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4AR,10AR)-7-hydroxy-1- propyl-1,2,3,4,4A,5,10,10A-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid |
| JP7514859B2 (ja) | 2019-05-21 | 2024-07-11 | ハー・ルンドベック・アクチエゼルスカベット | パーキンソン病の治療に使用するための新規なカテコールアミンプロドラッグ |
| EP3972600B1 (en) | 2019-05-21 | 2026-02-18 | H. Lundbeck A/S | Catecholamine carbamate prodrugs for use in the treatment of parkinson s disease |
| JP7641234B2 (ja) | 2019-05-21 | 2025-03-06 | ハー・ルンドベック・アクチエゼルスカベット | パーキンソン病の治療に使用するための新規なカテコールアミンプロドラッグ |
| CN113727974B (zh) | 2019-05-21 | 2025-01-07 | H.隆德贝克有限公司 | 用于治疗帕金森病的新儿茶酚胺前药 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL100555A (en) * | 1991-02-07 | 2000-08-31 | Hoechst Marion Roussel Inc | N-substituted quinoline derivatives their preparation their use for the preparation of medicaments and the pharmaceutical compositions containing them |
| GB9326010D0 (en) * | 1993-12-21 | 1994-02-23 | Sandoz Ltd | Improvements in or relating to organic compounds |
| TW378209B (en) * | 1996-07-08 | 2000-01-01 | Novartis Ag | Benzo[g]quinoline derivatives, their preparation and the pharmaceutical composition containing them |
| PE20030240A1 (es) * | 2001-07-09 | 2003-04-16 | Novartis Ag | DERIVADOS DE BENZO [g] QUINOLINA |
-
2003
- 2003-03-03 EG EG2003030215A patent/EG24415A/xx active
- 2003-03-05 TW TW092104671A patent/TW200406401A/zh unknown
- 2003-03-05 AR ARP030100740A patent/AR038730A1/es unknown
- 2003-03-05 PE PE2003000212A patent/PE20030927A1/es not_active Application Discontinuation
- 2003-03-06 BR BR0308201-6A patent/BR0308201A/pt not_active Application Discontinuation
- 2003-03-06 CA CA2706618A patent/CA2706618A1/en not_active Abandoned
- 2003-03-06 US US10/506,232 patent/US7399768B2/en not_active Expired - Fee Related
- 2003-03-06 ES ES03714784T patent/ES2279100T3/es not_active Expired - Lifetime
- 2003-03-06 CA CA2477720A patent/CA2477720C/en not_active Expired - Fee Related
- 2003-03-06 PL PL394208A patent/PL215012B1/pl unknown
- 2003-03-06 WO PCT/EP2003/002321 patent/WO2003074511A1/en not_active Ceased
- 2003-03-06 SI SI200330755T patent/SI1480970T1/sl unknown
- 2003-03-06 EP EP03714784A patent/EP1480970B1/en not_active Expired - Lifetime
- 2003-03-06 IL IL16376903A patent/IL163769A0/xx unknown
- 2003-03-06 PL PL370915A patent/PL210336B1/pl unknown
- 2003-03-06 CN CNB038053608A patent/CN1293070C/zh not_active Expired - Fee Related
- 2003-03-06 KR KR1020047012409A patent/KR101027977B1/ko not_active Expired - Fee Related
- 2003-03-06 PT PT03714784T patent/PT1480970E/pt unknown
- 2003-03-06 MX MXPA04008666A patent/MXPA04008666A/es active IP Right Grant
- 2003-03-06 CN CNA2006101357990A patent/CN1939915A/zh active Pending
- 2003-03-06 NZ NZ534732A patent/NZ534732A/en unknown
- 2003-03-06 JP JP2003572979A patent/JP2005519117A/ja active Pending
- 2003-03-06 RU RU2004129767/04A patent/RU2345991C2/ru not_active IP Right Cessation
- 2003-03-06 AU AU2003219023A patent/AU2003219023B2/en not_active Ceased
- 2003-03-06 DK DK03714784T patent/DK1480970T3/da active
- 2003-03-06 DE DE60311233T patent/DE60311233T2/de not_active Expired - Lifetime
- 2003-03-07 MY MYPI20030808A patent/MY134325A/en unknown
-
2004
- 2004-09-02 EC EC2004005271A patent/ECSP045271A/es unknown
- 2004-09-15 CO CO04091781A patent/CO5611196A2/es not_active Application Discontinuation
- 2004-09-28 NO NO20044117A patent/NO20044117L/no not_active Application Discontinuation
-
2007
- 2007-03-22 CY CY20071100405T patent/CY1106409T1/el unknown
-
2008
- 2008-06-12 US US12/137,819 patent/US20080255176A1/en not_active Abandoned
-
2010
- 2010-02-04 JP JP2010022863A patent/JP2010095550A/ja active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20150307 |