MD4846B1 - Procedeu de preparare a compuşilor izoxazolinici enantiomeric îmbogăţiţi şi a solvatului de toluen cristalin al (S)-afoxolanerului - Google Patents
Procedeu de preparare a compuşilor izoxazolinici enantiomeric îmbogăţiţi şi a solvatului de toluen cristalin al (S)-afoxolanerului Download PDFInfo
- Publication number
- MD4846B1 MD4846B1 MDA20180090A MD20180090A MD4846B1 MD 4846 B1 MD4846 B1 MD 4846B1 MD A20180090 A MDA20180090 A MD A20180090A MD 20180090 A MD20180090 A MD 20180090A MD 4846 B1 MD4846 B1 MD 4846B1
- Authority
- MD
- Moldova
- Prior art keywords
- afoxolaner
- preparation
- isoxazoline compounds
- toluene solvate
- enantiomerically enriched
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
- A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
- A01N43/42—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/64—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
- A01N43/647—Triazoles; Hydrogenated triazoles
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
- A01N43/80—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N55/00—Biocides, pest repellants or attractants, or plant growth regulators, containing organic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen and sulfur
- A01N55/08—Biocides, pest repellants or attractants, or plant growth regulators, containing organic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen and sulfur containing boron
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
- C07D453/04—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems having a quinolyl-4, a substituted quinolyl-4 or a alkylenedioxy-quinolyl-4 radical linked through only one carbon atom, attached in position 2, e.g. quinine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- 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
- C07B2200/07—Optical isomers
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Dentistry (AREA)
- Wood Science & Technology (AREA)
- Environmental Sciences (AREA)
- Zoology (AREA)
- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
- Plant Pathology (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Tropical Medicine & Parasitology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
Invenţia se referă la un procedeu de preparare a compuşilor izoxazolinici antiparazitari îmbogăţiţi enantiomeric, folosind un catalizator de transfer de fază chiral bazat pe chinină. Invenţia, de asemenea, se referă la o formă cristalină a solvatului de toluen al (S)-afoxolanerului.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662319207P | 2016-04-06 | 2016-04-06 | |
| PCT/US2017/026245 WO2017176948A1 (en) | 2016-04-06 | 2017-04-05 | Process for the preparation of enantiomerically enriched isoxazoline compounds - crystalline toluene solvate of (s)-afoxolaner |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| MD20180090A2 MD20180090A2 (ro) | 2019-02-28 |
| MD4846B1 true MD4846B1 (ro) | 2023-02-28 |
| MD4846C1 MD4846C1 (ro) | 2023-10-31 |
Family
ID=58549312
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDA20220052A MD20220052A2 (ro) | 2016-04-06 | 2017-04-05 | Procedeu de preparare a compuşilor izoxazolinici enantiomeric îmbogăţiţi şi a solvatului de toluen cristalin al (S)-afoxolanerului |
| MDA20180090A MD4846C1 (ro) | 2016-04-06 | 2017-04-05 | Procedeu de preparare a compuşilor izoxazolinici enantiomeric îmbogăţiţi şi a solvatului de toluen cristalin al (S)-afoxolanerului |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDA20220052A MD20220052A2 (ro) | 2016-04-06 | 2017-04-05 | Procedeu de preparare a compuşilor izoxazolinici enantiomeric îmbogăţiţi şi a solvatului de toluen cristalin al (S)-afoxolanerului |
Country Status (32)
| Country | Link |
|---|---|
| US (3) | US10433552B2 (ro) |
| EP (2) | EP3440062B1 (ro) |
| KR (2) | KR102438541B1 (ro) |
| CN (2) | CN114805234A (ro) |
| AR (1) | AR108184A1 (ro) |
| AU (2) | AU2017246305B2 (ro) |
| CA (2) | CA3019947A1 (ro) |
| CL (2) | CL2018002838A1 (ro) |
| CO (3) | CO2019013841A2 (ro) |
| CY (1) | CY1124797T1 (ro) |
| DK (2) | DK3978483T3 (ro) |
| EA (1) | EA201892245A1 (ro) |
| ES (2) | ES2903286T3 (ro) |
| FI (1) | FI3978483T3 (ro) |
| HR (2) | HRP20211979T1 (ro) |
| HU (2) | HUE056909T2 (ro) |
| IL (2) | IL262093B (ro) |
| LT (2) | LT3440062T (ro) |
| MD (2) | MD20220052A2 (ro) |
| MX (2) | MX378893B (ro) |
| MY (1) | MY189534A (ro) |
| NZ (1) | NZ747676A (ro) |
| PL (2) | PL3978483T3 (ro) |
| PT (2) | PT3440062T (ro) |
| RS (2) | RS62755B1 (ro) |
| SG (1) | SG11201808756XA (ro) |
| SI (2) | SI3978483T1 (ro) |
| TW (1) | TWI753897B (ro) |
| UA (1) | UA127309C2 (ro) |
| UY (2) | UY37196A (ro) |
| WO (1) | WO2017176948A1 (ro) |
| ZA (1) | ZA201806675B (ro) |
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| WO2016022066A1 (en) | 2014-08-04 | 2016-02-11 | Jerry Tan Eye Surgery Pte Ltd | Pharmaceutical compositions for demodex related blepharitis and eyelid crusting |
| UY40429A (es) | 2016-02-24 | 2023-10-13 | Boehringer Ingelheim Animal Health Usa Inc | Compuestos antiparasitarios de isoxazolina, formulaciones inyectables de acción prolongada que los comprenden, métodos y usos de los mismos |
| CA3059114A1 (en) * | 2017-04-05 | 2018-10-11 | Boehringer Ingelheim Animal Health USA Inc. | Crystalline forms of (s)-afoxolaner |
| US10807992B2 (en) | 2017-11-16 | 2020-10-20 | Avista Pharma Solutions, Inc. | Single enantiomer antiparasitic compounds |
| KR20250057155A (ko) | 2017-12-15 | 2025-04-28 | 타르서스 파마수티칼스, 아이엔씨. | 안검염을 치료하기 위한 이속사졸린 구충제 제제 및 방법 |
| TWI812673B (zh) | 2018-02-12 | 2023-08-21 | 美商富曼西公司 | 用於防治無脊椎害蟲之萘異噁唑啉化合物 |
| CA3113874A1 (en) | 2018-10-29 | 2020-05-07 | Basf Se | Process for preparation of optically enriched aldol compounds |
| US12502377B2 (en) | 2019-04-04 | 2025-12-23 | Tarsus Pharmaceuticals, Inc. | Method of eradicating ticks that attach to humans using lotilaner formulations |
| CA3164924A1 (en) | 2019-12-18 | 2021-06-24 | Elanco Tiergesundheit Ag | Isoxazoline derivatives as pesticides |
| WO2021254445A1 (zh) * | 2020-06-19 | 2021-12-23 | 东莞市东阳光仿制药研发有限公司 | 一种gaba抑制剂的晶型及其制备方法 |
| KR20230043904A (ko) * | 2020-07-24 | 2023-03-31 | 엘랑코 유에스 인코포레이티드 | 이속사졸린 화합물 및 이의 중간체의 제조 공정 |
| EP4208157A1 (en) | 2020-09-04 | 2023-07-12 | Elanco Us Inc. | Palatable formulations |
| CN112724095A (zh) * | 2020-09-25 | 2021-04-30 | 安徽省公众检验研究院有限公司 | 氟雷拉钠晶型及其制备方法 |
| CA3224225A1 (en) * | 2021-06-25 | 2022-12-29 | In The Bowl Animal Health, Inc. | Oral feline feed and methods for controlling flea infestations in a feline |
| CA3224701A1 (en) | 2021-08-11 | 2023-02-16 | Jingdan Hu | Process for making diaryl isoxazoline derivative |
| CN115710185B (zh) * | 2021-08-23 | 2024-05-03 | 中国石油化工股份有限公司 | 利用金属碳化物催化剂生产甲胺的方法 |
| CN114113388B (zh) * | 2021-11-24 | 2023-05-23 | 丽珠集团新北江制药股份有限公司 | 一种4-肟甲基-1-萘甲酸中有关物质的检测方法 |
| CN116253658B (zh) * | 2022-11-25 | 2023-08-11 | 济南久隆医药科技有限公司 | 一种阿福拉纳中间体合成方法 |
| CN115959979A (zh) * | 2022-12-29 | 2023-04-14 | 南京正荣医药化学有限公司 | 一种3-氯-4-氟-5-三氟甲基三氟苯乙酮的制备方法 |
| CN116143652B (zh) * | 2023-01-13 | 2024-06-28 | 四川青木制药有限公司 | 一种阿福拉纳中间体及其制备方法和应用 |
| CN117486869A (zh) * | 2023-11-06 | 2024-02-02 | 北京康立生医药技术开发有限公司 | 一种眼科治疗药物新的制备方法 |
| WO2025257633A1 (en) | 2024-06-12 | 2025-12-18 | Boehringer Ingelheim Vetmedica Gmbh | Long-acting castor oil-containing injectable formulations and methods of use thereof |
| WO2026043852A1 (en) | 2024-08-20 | 2026-02-26 | Zoetis Services Llc | Process for preparing optically enriched isoxazolines |
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| AR096022A1 (es) * | 2013-04-11 | 2015-12-02 | Basf Se | Compuestos de pirimidinio sustituido, útiles para combatir plagas de animales |
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Owner name: BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC, US 3239 SATELLITE BLVD., DULUTH, GA 30096, STATELE UNITE ALE AMERICII Free format text: PREVIOUS APPLICANT: MERIAL, INC., US STR. 3239 SATELLITE BOULEVARD, DULUTH, GEORGIA 30096, STATELE UNITE ALE AMERICII, STATELE UNITE ALE AMERICII |
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| FG4A | Patent for invention issued |