BR112020020351A2 - Agentes farmacológicos para o tratamento de doenças oculares - Google Patents
Agentes farmacológicos para o tratamento de doenças oculares Download PDFInfo
- Publication number
- BR112020020351A2 BR112020020351A2 BR112020020351-3A BR112020020351A BR112020020351A2 BR 112020020351 A2 BR112020020351 A2 BR 112020020351A2 BR 112020020351 A BR112020020351 A BR 112020020351A BR 112020020351 A2 BR112020020351 A2 BR 112020020351A2
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- cycloalkyl
- halo
- fact
- hydrogen
- Prior art date
Links
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- 238000000034 method Methods 0.000 claims abstract description 206
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- 239000001257 hydrogen Substances 0.000 claims description 165
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 50
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- 125000000623 heterocyclic group Chemical group 0.000 claims description 32
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- 125000003827 glycol group Chemical group 0.000 claims description 26
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 25
- 125000000217 alkyl group Chemical group 0.000 claims description 24
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims description 24
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- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 229940023490 ophthalmic product Drugs 0.000 description 1
- 125000001715 oxadiazolyl group Chemical group 0.000 description 1
- 125000000160 oxazolidinyl group Chemical group 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- 125000003566 oxetanyl group Chemical group 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 239000012466 permeate Substances 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 229920001983 poloxamer Polymers 0.000 description 1
- 229920001442 polyethylene glycol-block-polycaprolactone Polymers 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 208000022256 primary systemic amyloidosis Diseases 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 description 1
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 125000004929 pyrrolidonyl group Chemical group N1(C(CCC1)=O)* 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 125000005493 quinolyl group Chemical group 0.000 description 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 210000001525 retina Anatomy 0.000 description 1
- 210000003583 retinal pigment epithelium Anatomy 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- 230000002784 sclerotic effect Effects 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 238000002864 sequence alignment Methods 0.000 description 1
- 231100000161 signs of toxicity Toxicity 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 238000002415 sodium dodecyl sulfate polyacrylamide gel electrophoresis Methods 0.000 description 1
- QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 108010074609 steroid hormone 6-beta-hydroxylase Proteins 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000012916 structural analysis Methods 0.000 description 1
- WPLOVIFNBMNBPD-ATHMIXSHSA-N subtilin Chemical compound CC1SCC(NC2=O)C(=O)NC(CC(N)=O)C(=O)NC(C(=O)NC(CCCCN)C(=O)NC(C(C)CC)C(=O)NC(=C)C(=O)NC(CCCCN)C(O)=O)CSC(C)C2NC(=O)C(CC(C)C)NC(=O)C1NC(=O)C(CCC(N)=O)NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C1NC(=O)C(=C/C)/NC(=O)C(CCC(N)=O)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C2NC(=O)CNC(=O)C3CCCN3C(=O)C(NC(=O)C3NC(=O)C(CC(C)C)NC(=O)C(=C)NC(=O)C(CCC(O)=O)NC(=O)C(NC(=O)C(CCCCN)NC(=O)C(N)CC=4C5=CC=CC=C5NC=4)CSC3)C(C)SC2)C(C)C)C(C)SC1)CC1=CC=CC=C1 WPLOVIFNBMNBPD-ATHMIXSHSA-N 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 229940124530 sulfonamide Drugs 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940126703 systemic medication Drugs 0.000 description 1
- 238000009121 systemic therapy Methods 0.000 description 1
- 231100000057 systemic toxicity Toxicity 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 description 1
- 125000005958 tetrahydrothienyl group Chemical group 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- RSPCKAHMRANGJZ-UHFFFAOYSA-N thiohydroxylamine Chemical compound SN RSPCKAHMRANGJZ-UHFFFAOYSA-N 0.000 description 1
- 125000003396 thiol group Chemical group [H]S* 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 230000000472 traumatic effect Effects 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- LUIFZQQTAGEAEO-UHFFFAOYSA-K trisodium propane-1,2-diol phosphate Chemical compound C(C(C)O)O.P(=O)([O-])([O-])[O-].[Na+].[Na+].[Na+] LUIFZQQTAGEAEO-UHFFFAOYSA-K 0.000 description 1
- 238000009281 ultraviolet germicidal irradiation Methods 0.000 description 1
- 210000001745 uvea Anatomy 0.000 description 1
- PXXNTAGJWPJAGM-UHFFFAOYSA-N vertaline Natural products C1C2C=3C=C(OC)C(OC)=CC=3OC(C=C3)=CC=C3CCC(=O)OC1CC1N2CCCC1 PXXNTAGJWPJAGM-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
- A61K31/6615—Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
-
- 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
- A61K31/12—Ketones
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4741—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
-
- 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
- A61P27/12—Ophthalmic agents for cataracts
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862653249P | 2018-04-05 | 2018-04-05 | |
| US62/653,249 | 2018-04-05 | ||
| US201862694729P | 2018-07-06 | 2018-07-06 | |
| US62/694,729 | 2018-07-06 | ||
| PCT/US2019/026112 WO2019195761A2 (en) | 2018-04-05 | 2019-04-05 | Pharmacological agents for treating ocular diseases |
Publications (1)
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| BR112020020351A2 true BR112020020351A2 (pt) | 2021-01-12 |
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| BR112020020351-3A BR112020020351A2 (pt) | 2018-04-05 | 2019-04-05 | Agentes farmacológicos para o tratamento de doenças oculares |
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| US (1) | US11872236B2 (https=) |
| JP (1) | JP7532259B2 (https=) |
| CN (1) | CN112601513B (https=) |
| BR (1) | BR112020020351A2 (https=) |
| MX (1) | MX2020010502A (https=) |
| WO (1) | WO2019195761A2 (https=) |
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| CN120097859A (zh) * | 2019-02-19 | 2025-06-06 | 加利福尼亚大学董事会 | Nurr1受体调节剂 |
| EP3976017A4 (en) * | 2019-05-31 | 2023-06-14 | Plex Pharmaceuticals, Inc. | PHARMACOLOGICAL SUBSTANCES FOR THE TREATMENT OF PROTEIN AGGREGATION DISEASES OF THE EYE |
| WO2021086834A1 (en) * | 2019-10-28 | 2021-05-06 | Kebotix, Inc. | Electronic control of transmittance of visible and near-infrared radiation |
| WO2022098847A1 (en) * | 2020-11-04 | 2022-05-12 | Corino Therapeutics, Inc. | Tolcapone analogs and methods of use |
| CN116963727A (zh) * | 2020-11-13 | 2023-10-27 | 普莱克斯医药公司 | 用于治疗眼部病症的药剂 |
| JP2023549533A (ja) * | 2020-11-13 | 2023-11-27 | プレックス ファーマスーティカルズ，インク | 眼の状態を処置するための薬理剤 |
| US20250019352A1 (en) * | 2021-06-29 | 2025-01-16 | Plex Pharmaceuticals, Inc. | Pharmacological agents for treating ophthalmic diseases |
| GB202204798D0 (en) | 2022-04-01 | 2022-05-18 | Bial Portela & Ca Sa | Prodrugs of opicapone |
| WO2024123100A1 (ko) * | 2022-12-09 | 2024-06-13 | 경희대학교 산학협력단 | 신규 아밀로이드-베타 응집체 분해제와 이를 이용한 뇌 표적화 약물 전달 시스템 |
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| US5236952A (en) * | 1986-03-11 | 1993-08-17 | Hoffmann-La Roche Inc. | Catechol derivatives |
| DK175069B1 (da) | 1986-03-11 | 2004-05-24 | Hoffmann La Roche | Pyrocatecholderivater |
| JPH1036257A (ja) * | 1996-05-22 | 1998-02-10 | Kikkoman Corp | メイラード反応阻害剤 |
| ID19540A (id) | 1997-01-22 | 1998-07-23 | Hoffmann La Roche | Metode pembuatan turunan-turunan benzofenon |
| JP2000256259A (ja) * | 1999-03-11 | 2000-09-19 | Nippon Zoki Pharmaceut Co Ltd | メイラード反応阻害剤 |
| US8299079B2 (en) | 2009-05-22 | 2012-10-30 | Kaufman Herbert E | Preparations and methods for ameliorating or reducing presbyopia |
| WO2011047412A1 (en) * | 2009-10-22 | 2011-04-28 | The Heart Research Institute Ltd | Tyrosine and l-dopa for reducing l-dopa incorporation into proteins |
| WO2011140333A1 (en) * | 2010-05-07 | 2011-11-10 | The Board Of Trustees Of The Leland Stanford Junior University | Identification of stabilizers of multimeric proteins |
| WO2014147464A2 (en) | 2013-03-20 | 2014-09-25 | Ra Chem Pharma Limited | Novel process for the preparation of tolcapone |
| WO2015095257A2 (en) * | 2013-12-18 | 2015-06-25 | Emory University | Managing visual dysfunction or loss of vision for diabetic subjects |
| RU2724190C2 (ru) | 2014-02-08 | 2020-06-23 | Дженентек, Инк. | Способы лечения болезни альцгеймера |
| KR20170048426A (ko) * | 2014-08-22 | 2017-05-08 | 광저우 캉루이 바이오로지컬 파마슈티컬 테크놀로지 씨오., 엘티디. | 시각 장애를 치료하기 위한 조성물 및 방법 |
| WO2017039525A1 (en) | 2015-09-04 | 2017-03-09 | Lobsor Pharmaceuticals Aktiebolag | Method of treating a dopamine related disorder in a subject by administering levodopa, in combination with a dopamine decarboxylase inhibitor and a catechol-o-methyltransferase inhibitor |
| CN116963727A (zh) | 2020-11-13 | 2023-10-27 | 普莱克斯医药公司 | 用于治疗眼部病症的药剂 |
| JP2023549533A (ja) | 2020-11-13 | 2023-11-27 | プレックス ファーマスーティカルズ，インク | 眼の状態を処置するための薬理剤 |
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Also Published As
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| EP3773438A2 (en) | 2021-02-17 |
| WO2019195761A2 (en) | 2019-10-10 |
| WO2019195761A3 (en) | 2020-07-23 |
| CN112601513A (zh) | 2021-04-02 |
| JP7532259B2 (ja) | 2024-08-13 |
| CN112601513B (zh) | 2023-12-22 |
| US20210154213A1 (en) | 2021-05-27 |
| US11872236B2 (en) | 2024-01-16 |
| JP2021532059A (ja) | 2021-11-25 |
| MX2020010502A (es) | 2021-03-25 |
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