CL2019003235A1 - Un solvato cristalino de (s)-afoxolaner con tolueno. (divisional solicitud 201802838) - Google Patents
Un solvato cristalino de (s)-afoxolaner con tolueno. (divisional solicitud 201802838)Info
- Publication number
- CL2019003235A1 CL2019003235A1 CL2019003235A CL2019003235A CL2019003235A1 CL 2019003235 A1 CL2019003235 A1 CL 2019003235A1 CL 2019003235 A CL2019003235 A CL 2019003235A CL 2019003235 A CL2019003235 A CL 2019003235A CL 2019003235 A1 CL2019003235 A1 CL 2019003235A1
- Authority
- CL
- Chile
- Prior art keywords
- toluene
- afoxolaner
- crystalline solvate
- divisional request
- quinine
- Prior art date
Links
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 title abstract 6
- 239000012453 solvate Substances 0.000 title abstract 2
- OXDDDHGGRFRLEE-QHCPKHFHSA-N esafoxolaner Chemical compound C1([C@]2(ON=C(C2)C2=CC=C(C3=CC=CC=C32)C(=O)NCC(=O)NCC(F)(F)F)C(F)(F)F)=CC(Cl)=CC(C(F)(F)F)=C1 OXDDDHGGRFRLEE-QHCPKHFHSA-N 0.000 title 1
- LOUPRKONTZGTKE-WZBLMQSHSA-N Quinine Chemical group C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@@H]2[C@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-WZBLMQSHSA-N 0.000 abstract 2
- 239000003444 phase transfer catalyst Substances 0.000 abstract 2
- WEQPBCSPRXFQQS-UHFFFAOYSA-N 4,5-dihydro-1,2-oxazole Chemical compound C1CC=NO1 WEQPBCSPRXFQQS-UHFFFAOYSA-N 0.000 abstract 1
- 235000001258 Cinchona calisaya Nutrition 0.000 abstract 1
- -1 ISOXAZOLINE COMPOUND Chemical class 0.000 abstract 1
- 230000002141 anti-parasite Effects 0.000 abstract 1
- 239000003096 antiparasitic agent Substances 0.000 abstract 1
- LOUPRKONTZGTKE-UHFFFAOYSA-N cinchonine Natural products C1C(C(C2)C=C)CCN2C1C(O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229960000948 quinine Drugs 0.000 abstract 1
Classifications
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- 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
- 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
- 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
- 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
-
- 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)
- Plant Pathology (AREA)
- Pest Control & Pesticides (AREA)
- Engineering & Computer Science (AREA)
- Dentistry (AREA)
- Agronomy & Crop Science (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Environmental Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (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
PROCESOS PARA LA PREPARACIÓN DE COMPUESTOS ANTIPARASITARIOS DE ISOXAZOLINA ENRIQUECIDOS EN UN ENANTIÓMERO USANDO UN CATALIZADOR DE TRANSFERENCIA DE FASE QUIRAL A BASE DE QUININA. TAMBIÉN, NOVEDOSOS CATALIZADORES DE TRANSFERENCIA DE FASE A BASE DE QUININA Y UNA FORMA DE SOLVATO CON TOLUENO DEL COMPUESTO DE ISOXAZOLINA DE LA INVENCIÓN.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662319207P | 2016-04-06 | 2016-04-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2019003235A1 true CL2019003235A1 (es) | 2020-02-14 |
Family
ID=58549312
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2018002838A CL2018002838A1 (es) | 2016-04-06 | 2018-10-05 | Proceso para preparar compuestos de isoxazolina |
| CL2019003235A CL2019003235A1 (es) | 2016-04-06 | 2019-11-12 | Un solvato cristalino de (s)-afoxolaner con tolueno. (divisional solicitud 201802838) |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2018002838A CL2018002838A1 (es) | 2016-04-06 | 2018-10-05 | Proceso para preparar compuestos de isoxazolina |
Country Status (32)
| Country | Link |
|---|---|
| US (3) | US10433552B2 (es) |
| EP (2) | EP3978483B1 (es) |
| KR (2) | KR102403531B1 (es) |
| CN (2) | CN109195955B (es) |
| AR (1) | AR108184A1 (es) |
| AU (2) | AU2017246305B2 (es) |
| CA (2) | CA3214922A1 (es) |
| CL (2) | CL2018002838A1 (es) |
| CO (3) | CO2019013500A2 (es) |
| CY (1) | CY1124797T1 (es) |
| DK (2) | DK3978483T3 (es) |
| EA (1) | EA201892245A1 (es) |
| ES (2) | ES2903286T3 (es) |
| FI (1) | FI3978483T3 (es) |
| HR (2) | HRP20211979T1 (es) |
| HU (2) | HUE056909T2 (es) |
| IL (2) | IL262093B (es) |
| LT (2) | LT3978483T (es) |
| MD (2) | MD4846C1 (es) |
| MX (2) | MX394199B (es) |
| MY (1) | MY189534A (es) |
| NZ (1) | NZ747676A (es) |
| PL (2) | PL3440062T3 (es) |
| PT (2) | PT3978483T (es) |
| RS (2) | RS62755B1 (es) |
| SG (1) | SG11201808756XA (es) |
| SI (2) | SI3978483T1 (es) |
| TW (1) | TWI753897B (es) |
| UA (1) | UA127309C2 (es) |
| UY (2) | UY40619A (es) |
| WO (1) | WO2017176948A1 (es) |
| ZA (1) | ZA201806675B (es) |
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| US20170232024A1 (en) | 2014-08-04 | 2017-08-17 | Jerry Tan Eye Surgery Pte Ltd | Pharmaceutical compositions for demodex related blepharitis and eyelid crusting |
| UY37137A (es) | 2016-02-24 | 2017-09-29 | Merial Inc | Compuestos antiparasitarios de isoxazolina, formulaciones inyectables de acción prolongada que los comprenden, métodos y usos de los mismos |
| US10662163B2 (en) | 2017-04-05 | 2020-05-26 | Boehringer Ingelheim Animal Health USA Inc. | Crystalline forms of (S)-afoxolaner |
| WO2019099669A1 (en) | 2017-11-16 | 2019-05-23 | Avista Pharma Solutions, Inc. | Single enantiomer antiparasitic compounds |
| CN119157876A (zh) | 2017-12-15 | 2024-12-20 | 塔苏斯制药有限公司 | 用于治疗睑炎的异恶唑啉驱虫剂制剂和方法 |
| 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 |
| US20210340113A1 (en) | 2018-10-29 | 2021-11-04 | 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 |
| MX2022007455A (es) | 2019-12-18 | 2022-08-15 | Elanco Tiergesundheit Ag | Derivados de isoxazolina como plaguicidas. |
| 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 |
| JP7724845B2 (ja) | 2020-07-24 | 2025-08-18 | エランコ・ユーエス・インコーポレイテッド | イソオキサゾリン化合物及びその中間体を作製するための方法 |
| KR20230061465A (ko) | 2020-09-04 | 2023-05-08 | 엘랑코 유에스 인코포레이티드 | 기호성 제형 |
| 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 |
| MX2023014962A (es) | 2021-08-11 | 2024-02-13 | Elanco Us Inc | Proceso para elaborar derivado de diaril isoxazolina. |
| 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 |
| WO2026087677A1 (en) | 2024-10-25 | 2026-04-30 | Krka, D.D., Novo Mesto | Enantioselective synthesis of (s)-afoxolaner and solid forms of (s)-afoxolaner |
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| TWI600639B (zh) | 2007-08-17 | 2017-10-01 | 杜邦股份有限公司 | 製備5-鹵烷基-4,5-二氫異唑衍生物之化合物 |
| MX2010003557A (es) | 2007-10-03 | 2010-04-12 | Du Pont | Compuestos de isoxazolina de naftaleno para el control de plagas de invertebrados. |
| JP5365807B2 (ja) | 2007-11-12 | 2013-12-11 | 日産化学工業株式会社 | 光学活性イソキサゾリン化合物の触媒的不斉合成方法 |
| WO2010003923A1 (en) | 2008-07-09 | 2010-01-14 | Basf Se | Pestcidal active mixtures comprising isoxazoline compounds i |
| PL2379537T3 (pl) | 2008-12-19 | 2013-03-29 | Elanco Tiergesundheit Ag | Pochodne izooksazoliny i ich zastosowanie jako pestycydów |
| TWI487486B (zh) | 2009-12-01 | 2015-06-11 | Syngenta Participations Ag | 以異唑啉衍生物為主之殺蟲化合物 |
| KR20120133401A (ko) * | 2010-02-25 | 2012-12-10 | 신젠타 리미티드 | 이속사졸린 유도체의 제조 방법 |
| AR081843A1 (es) | 2010-06-09 | 2012-10-24 | Syngenta Participations Ag | Mezclas pesticidas incluyendo derivados isoxazolina |
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| BR112014019212A8 (pt) | 2012-02-03 | 2017-07-11 | Zoetis Llc | Processo para a preparação de derivados quirais azetidina isoxazolina como agentes antiparasitários |
| JP6234471B2 (ja) | 2012-11-21 | 2017-11-22 | ゾエティス・サービシーズ・エルエルシー | スピロ環状イソキサゾリン誘導体の合成 |
| WO2014090918A1 (en) * | 2012-12-13 | 2014-06-19 | Novartis Ag | Process for the enantiomeric enrichment of diaryloxazoline derivatives |
| LT2950795T (lt) * | 2013-01-31 | 2018-06-25 | Merial, Inc. | Leišmaniozės gydymo ir naikinimo būdas naudojant feksinidazolą |
| AR096022A1 (es) * | 2013-04-11 | 2015-12-02 | Basf Se | Compuestos de pirimidinio sustituido, útiles para combatir plagas de animales |
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