CA2447479A1 - Novel arylaminopropane analogues and their use for the treatment of glaucoma - Google Patents
Novel arylaminopropane analogues and their use for the treatment of glaucoma Download PDFInfo
- Publication number
- CA2447479A1 CA2447479A1 CA002447479A CA2447479A CA2447479A1 CA 2447479 A1 CA2447479 A1 CA 2447479A1 CA 002447479 A CA002447479 A CA 002447479A CA 2447479 A CA2447479 A CA 2447479A CA 2447479 A1 CA2447479 A1 CA 2447479A1
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- Canada
- Prior art keywords
- 3alkyl
- compounds
- compound
- hydrogen
- conr1r2
- Prior art date
- Legal status (The legal status 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 status listed.)
- Abandoned
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- 208000010412 Glaucoma Diseases 0.000 title claims abstract description 24
- 150000001875 compounds Chemical class 0.000 claims abstract description 73
- 239000000203 mixture Substances 0.000 claims abstract description 29
- 238000000034 method Methods 0.000 claims abstract description 23
- 230000004406 elevated intraocular pressure Effects 0.000 claims abstract description 6
- 230000004493 normal intraocular pressure Effects 0.000 claims abstract description 5
- 125000003118 aryl group Chemical group 0.000 claims description 15
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- 239000001257 hydrogen Substances 0.000 claims description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 9
- 229910052736 halogen Inorganic materials 0.000 claims description 8
- 150000002367 halogens Chemical class 0.000 claims description 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 5
- 125000004076 pyridyl group Chemical group 0.000 claims description 5
- 125000001544 thienyl group Chemical group 0.000 claims description 5
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- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
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- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 4
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- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 4
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
- C07C225/02—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton
- C07C225/04—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being saturated
- C07C225/06—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being saturated and acyclic
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C211/00—Compounds containing amino groups bound to a carbon skeleton
- C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
- C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
- C07C211/30—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the six-membered aromatic ring being part of a condensed ring system formed by two rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C215/48—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups
- C07C215/52—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C217/56—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms
- C07C217/60—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C217/64—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms
- C07C217/66—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms with singly-bound oxygen atoms and six-membered aromatic rings bound to the same carbon atom of the carbon chain
- C07C217/70—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms with singly-bound oxygen atoms and six-membered aromatic rings bound to the same carbon atom of the carbon chain linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29542601P | 2001-06-01 | 2001-06-01 | |
| US60/295,426 | 2001-06-01 | ||
| PCT/US2002/016842 WO2002098400A1 (en) | 2001-06-01 | 2002-05-30 | Novel arylaminopropane analogues and their use for the treatment of glaucoma |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2447479A1 true CA2447479A1 (en) | 2002-12-12 |
Family
ID=23137665
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002447479A Abandoned CA2447479A1 (en) | 2001-06-01 | 2002-05-30 | Novel arylaminopropane analogues and their use for the treatment of glaucoma |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US7071225B2 (enExample) |
| EP (1) | EP1392269A1 (enExample) |
| JP (1) | JP2004534781A (enExample) |
| CN (1) | CN1512879A (enExample) |
| AR (1) | AR036076A1 (enExample) |
| AU (1) | AU2002259312B2 (enExample) |
| BR (1) | BR0210238A (enExample) |
| CA (1) | CA2447479A1 (enExample) |
| MX (1) | MXPA03010806A (enExample) |
| WO (1) | WO2002098400A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US6960579B1 (en) | 1998-05-19 | 2005-11-01 | Alcon Manufacturing, Ltd. | Serotonergic 5HT7 receptor compounds for treating ocular and CNS disorders |
| TW593302B (en) | 2001-12-20 | 2004-06-21 | Alcon Inc | Novel benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma |
| US20060106106A1 (en) * | 2002-09-24 | 2006-05-18 | Glennon Richard A | Beta-hydroxyphenylalkylamines and their use for treating glaucoma |
| AU2003300915B2 (en) | 2002-12-13 | 2008-08-28 | Alcon, Inc. | Novel benzopyran analogs and their use for the treatment of glaucoma |
| WO2005053688A1 (en) * | 2003-11-26 | 2005-06-16 | Alcon, Inc. | Substituted furo[2,3-g] indazoles for the treatment of glaucoma |
| AR046890A1 (es) | 2003-12-15 | 2005-12-28 | Alcon Inc | [1,4] oxazino [2,3-g] indazoles sustituidos para el tratamiento del glaucoma. |
| US7129257B1 (en) | 2003-12-15 | 2006-10-31 | Alcon, Inc. | Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma |
| US7338972B1 (en) | 2003-12-15 | 2008-03-04 | Alcon, Inc. | Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma |
| EP2400300A1 (en) | 2004-08-25 | 2011-12-28 | Takeda Pharmaceutical Company Limited | Method of screening preventives/remedies for stress urinary incontinence |
| US7674822B2 (en) | 2004-11-24 | 2010-03-09 | Wyeth | PTP1b inhibitors |
| WO2006062839A1 (en) | 2004-12-08 | 2006-06-15 | Alcon, Inc. | Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma |
| TW200744567A (en) * | 2005-09-23 | 2007-12-16 | Alcon Inc | Phenylethylamine analogs and their use for treating glaucoma |
| WO2007132841A1 (ja) | 2006-05-16 | 2007-11-22 | Takeda Pharmaceutical Company Limited | 縮合複素環化合物およびその用途 |
| WO2007149728A2 (en) * | 2006-06-20 | 2007-12-27 | Alcon Research, Ltd. | Aryl and heteroaryl tetrahydrobenzazepine derivatives and their use for treating glaucoma |
| JP5520051B2 (ja) | 2007-11-15 | 2014-06-11 | 武田薬品工業株式会社 | 縮合ピリジン誘導体およびその用途 |
| JPWO2011071136A1 (ja) | 2009-12-11 | 2013-04-22 | アステラス製薬株式会社 | 線維筋痛症治療剤 |
| US20190337889A1 (en) * | 2015-10-18 | 2019-11-07 | Onco Therapies Llc | Compositions and methods of regulating cancer related disorders and diseases |
| US20210052600A1 (en) | 2017-12-27 | 2021-02-25 | Takeda Pharmaceutical Company Limited | Therapeutic agents for stress urinary incontinence and incotinence of feces |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2534580A1 (fr) * | 1982-10-13 | 1984-04-20 | Synthelabo | Derives de phenyl-1 piperidino-2 propanol, leur preparation, et medicaments qui les contiennent |
| US5151444B1 (en) * | 1987-09-18 | 1999-07-06 | R Tech Ueno Ltd | Ocular hypotensive agents |
| US5296504A (en) * | 1988-09-06 | 1994-03-22 | Kabi Pharmacia | Prostaglandin derivatives for the treatment of glaucoma or ocular hypertension |
| EP0569046B1 (en) * | 1988-09-06 | 2002-11-13 | Pharmacia Aktiebolag | Prostaglandin derivatives for the treatment of glaucoma or ocular hypertension |
| US5578612A (en) * | 1990-10-15 | 1996-11-26 | Pfizer Inc. | Indole derivatives |
| WO1992020338A1 (en) | 1991-05-10 | 1992-11-26 | Merrell Dow Pharmaceuticals Inc. | Method for the treatment of glaucoma |
| JPH06508354A (ja) * | 1991-06-21 | 1994-09-22 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | トリプタミン類似体、その合成法およびその5−ht↓1様または5−ht↓2受容体作用物質としての使用 |
| US5352708A (en) * | 1992-09-21 | 1994-10-04 | Allergan, Inc. | Non-acidic cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives as therapeutic agents |
| US5922773A (en) | 1992-12-04 | 1999-07-13 | The Children's Medical Center Corp. | Glaucoma treatment |
| US5510383A (en) * | 1993-08-03 | 1996-04-23 | Alcon Laboratories, Inc. | Use of cloprostenol, fluprostenol and their salts and esters to treat glaucoma and ocular hypertension |
| TW270114B (enExample) * | 1993-10-22 | 1996-02-11 | Hoffmann La Roche | |
| US5874477A (en) * | 1994-08-12 | 1999-02-23 | The University Of Hawaii | Method of treatment for malaria utilizing serotonin receptor ligands |
| US5998467A (en) | 1995-10-25 | 1999-12-07 | Mitsubishi Chemical Corporation | Medicine for oculopathy |
| AU2104097A (en) | 1996-03-13 | 1997-10-01 | Glaxo Group Limited | Medicaments comprising 5ht1-like receptor agonists with an increased absorption |
| US5902815A (en) * | 1996-09-03 | 1999-05-11 | Washington University | Use of 5HT-2A serotonin agonists to prevent adverse effects of NMDA receptor hypofunction |
| WO1998018458A1 (en) | 1996-10-31 | 1998-05-07 | Alcon Laboratories, Inc. | Opthalmological compositions containing serotonin 5-ht1a receptor agonist and their use in the treatment of glaucoma |
| GB9700899D0 (en) | 1997-01-17 | 1997-03-05 | Smithkline Beecham Plc | Novel treatment |
| GB9819035D0 (en) | 1998-09-01 | 1998-10-28 | Cerebrus Res Ltd | Chemical compounds VII |
| GB9819033D0 (en) | 1998-09-01 | 1998-10-28 | Cerebrus Ltd | Chemical compounds VI |
| DE69928542T2 (de) | 1998-09-18 | 2006-03-30 | Alcon Manufacturing Ltd., Fort Worth | 5HT2-Agonisten zur Behandlung des Glaukoms |
| CZ20012193A3 (cs) | 1998-12-17 | 2001-12-12 | American Home Products Corporation | Deriváty 2,3,4,4a-tetrahydro-1H-pyrazino(1,2-a)chinoxalin-5(6H)onu, způsob jejich výroby a jejich pouľití |
| GB9902047D0 (en) | 1999-01-29 | 1999-03-17 | Cerebrus Ltd | Chemical compounds XI |
| CN1370176A (zh) * | 1999-06-15 | 2002-09-18 | 布里斯托尔-迈尔斯斯奎布药品公司 | 取代的杂环稠合γ-咔啉 |
| US6713471B1 (en) * | 1999-06-15 | 2004-03-30 | Bristol-Myers Squibb Pharma Company | Substituted heterocycle fused gamma-carbolines |
-
2002
- 2002-05-30 WO PCT/US2002/016842 patent/WO2002098400A1/en not_active Ceased
- 2002-05-30 JP JP2003501440A patent/JP2004534781A/ja active Pending
- 2002-05-30 AU AU2002259312A patent/AU2002259312B2/en not_active Ceased
- 2002-05-30 EP EP02729314A patent/EP1392269A1/en not_active Withdrawn
- 2002-05-30 BR BR0210238-2A patent/BR0210238A/pt not_active Application Discontinuation
- 2002-05-30 CN CNA028110102A patent/CN1512879A/zh active Pending
- 2002-05-30 CA CA002447479A patent/CA2447479A1/en not_active Abandoned
- 2002-05-30 MX MXPA03010806A patent/MXPA03010806A/es unknown
- 2002-05-31 AR ARP020102053A patent/AR036076A1/es not_active Application Discontinuation
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2003
- 2003-11-26 US US10/723,208 patent/US7071225B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| MXPA03010806A (es) | 2004-11-22 |
| CN1512879A (zh) | 2004-07-14 |
| US7071225B2 (en) | 2006-07-04 |
| BR0210238A (pt) | 2004-07-20 |
| AR036076A1 (es) | 2004-08-11 |
| EP1392269A1 (en) | 2004-03-03 |
| US20040110791A1 (en) | 2004-06-10 |
| JP2004534781A (ja) | 2004-11-18 |
| WO2002098400A1 (en) | 2002-12-12 |
| AU2002259312B2 (en) | 2007-01-04 |
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Legal Events
| Date | Code | Title | Description |
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| EEER | Examination request | ||
| FZDE | Discontinued |