SG11201808108XA - Synthesis of indazoles - Google Patents
Synthesis of indazolesInfo
- Publication number
- SG11201808108XA SG11201808108XA SG11201808108XA SG11201808108XA SG11201808108XA SG 11201808108X A SG11201808108X A SG 11201808108XA SG 11201808108X A SG11201808108X A SG 11201808108XA SG 11201808108X A SG11201808108X A SG 11201808108XA SG 11201808108X A SG11201808108X A SG 11201808108XA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- str
- pct
- wuppertal
- berlin
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- 150000002473 indoazoles Chemical class 0.000 title 1
- 102220240796 rs553605556 Human genes 0.000 abstract 4
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 abstract 2
- -1 2-substituted indazole Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/86—Hydrazides; Thio or imino analogues thereof
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- C—CHEMISTRY; METALLURGY
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- 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
- C07D401/12—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 chain containing hetero atoms as chain links
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A—HUMAN NECESSITIES
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Gastroenterology & Hepatology (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Reproductive Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization 0 111111101111 0 DOI 010111110101111 0 111 011111011111111111111111111111111111111 International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2017/186689 Al 02 November 2017 (02.11.2017) W I PO I PCT (51) International Patent Classification: CO7D 401/12 (2006.01) A61P 37/00 (2006.01) TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). A61K 31/4439 (2006.01) A61P 9/00 (2006.01) A61P 35/00 (2006.01) A61P 27/00 (2006.01) Declarations under Rule 4.17: (21) International Application Number: — PCT/EP2017/059744 as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(u)) (22) International Filing Date: Published: 25 April 2017 (25.04.2017) — with international search report (Art. 21(3)) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 16167652.3 29 April 2016 (29.04.2016) EP (71) Applicant: BAYER PHARMA AKTIENGESEL- LSCHAFT [DE/DE]; Milllerstr. 178, 13353 Berlin (DE). (72) Inventors: THALER, Tobias; Adalbert-Stifter-Weg 54, 42109 Wuppertal (DE). PLATZEK, Johannes; Grottkauer _ Str. 55, 12621 Berlin (DE). GUIMOND, Nicolas; Katern- berger Str. 126, 42115 Wuppertal (DE). — = (74) Agent: BIP PATENTS; Alfred-Nobel-Str. 10, 40789 Mon- heim am Rhein (DE). = (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, = = _= CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, = _ MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, = PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, _ SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. = = (84) Designated States (unless otherwise indicated, for every _ _ kind of regional protection available): ARIPO (BW, GH, = GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, = UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, = TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, = EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, — MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, = (54) Title: SYNTHESIS OF INDAZOLES .4 (57) : The present invention relates to a novel method of preparing a 2-substitut- 0\ ed indazole of structure:(I), to intermediate compounds, and to the use of intermediate cam- = 0 pounds for the preparation of said 2-substituted indazole. F 3 C 0 HN ',...0 cc ,—, aim RIP \ IN HO 11 © ei (I) O
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16167652 | 2016-04-29 | ||
| PCT/EP2017/059744 WO2017186689A1 (en) | 2016-04-29 | 2017-04-25 | Synthesis of indazoles |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201808108XA true SG11201808108XA (en) | 2018-10-30 |
Family
ID=55860769
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201808108XA SG11201808108XA (en) | 2016-04-29 | 2017-04-25 | Synthesis of indazoles |
| SG11201808566WA SG11201808566WA (en) | 2016-04-29 | 2017-04-25 | Polymorphic form of n-{6-(2-hydroxypropan-2-yl)-2-[2-(methylsulphonyl)ethyl]-2h-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carboxamide |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201808566WA SG11201808566WA (en) | 2016-04-29 | 2017-04-25 | Polymorphic form of n-{6-(2-hydroxypropan-2-yl)-2-[2-(methylsulphonyl)ethyl]-2h-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carboxamide |
Country Status (43)
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3705B1 (en) | 2014-11-26 | 2021-01-31 | Bayer Pharma AG | Novel substituted indazoles, processes for preparation thereof, pharmaceutical preparations comprising them and use thereof for production of medicaments |
| CA3016364A1 (en) | 2016-03-03 | 2017-09-08 | Bayer Pharma Aktiengesellschaft | New 2-substituted indazoles, methods for producing same, pharmaceutical preparations that contain same, and use of same to produce drugs |
| CN109071491B (en) | 2016-04-29 | 2020-08-21 | 拜耳医药股份有限公司 | Indazole synthesis |
| MX2018013235A (en) * | 2016-04-29 | 2019-02-13 | Bayer Pharma AG | Polymorphic form of n-{6-(2-hydroxypropan-2-yl)-2-[2-(methylsulph onyl)ethyl]-2h-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carbo xamide. |
| KR102547834B1 (en) * | 2016-06-01 | 2023-06-26 | 바이엘 애니멀 헬스 게엠베하 | Substituted indazoles useful for the treatment and prevention of allergic and/or inflammatory diseases in animals |
| BR112018074919A2 (en) | 2016-06-01 | 2020-11-03 | Bayer Pharma Aktiengesellschaft | use of 2-substituted indoles for treatment and prophylaxis of autoimmune diseases. |
| JOP20180011A1 (en) | 2017-02-16 | 2019-01-30 | Gilead Sciences Inc | PYRROLO[1,2-b] PYRIDAZINE DERIVATIVES |
| KR20210024543A (en) | 2018-06-25 | 2021-03-05 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | Isothiazolo[5,4-d]pyrimidine compounds as IRAK4 inhibitors |
| TWI721483B (en) | 2018-07-13 | 2021-03-11 | 美商基利科學股份有限公司 | Pyrrolo[1,2-b]pyridazine derivatives |
| CN110981903A (en) * | 2019-11-28 | 2020-04-10 | 南京正济医药研究有限公司 | Refining method for improving optical purity of eribulin intermediate compound |
| US10894812B1 (en) | 2020-09-30 | 2021-01-19 | Alpine Roads, Inc. | Recombinant milk proteins |
| CA3191387A1 (en) | 2020-09-30 | 2022-04-07 | Nobell Foods, Inc. | Recombinant milk proteins and food compositions comprising the same |
| US10947552B1 (en) | 2020-09-30 | 2021-03-16 | Alpine Roads, Inc. | Recombinant fusion proteins for producing milk proteins in plants |
| CN114469979B (en) * | 2021-12-15 | 2024-04-09 | 安徽贝克生物制药有限公司 | Pharmaceutical composition of ribonucleoside analogue, inhalant and application thereof |
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| US20100048660A1 (en) | 2006-02-10 | 2010-02-25 | Graham Michael Wynne | Treatment of duchenne muscular dystrophy |
| JP5258563B2 (en) | 2006-06-29 | 2013-08-07 | 日産化学工業株式会社 | Alpha amino acid derivatives and pharmaceuticals containing them as active ingredients |
| CA2663100A1 (en) | 2006-09-07 | 2008-03-13 | Biogen Idec Ma Inc. | Indazole derivatives as modulators of interleukin-1 receptor-associated kinase |
| US20120196824A1 (en) | 2009-10-09 | 2012-08-02 | Mitsubishi Tanabe Pharma Corporation | Therapeutic agent for cerebral infarction |
| WO2011153588A1 (en) | 2010-06-10 | 2011-12-15 | Biota Scientific Management Pty Ltd | Viral polymerase inhibitors |
| US9073892B2 (en) | 2010-12-20 | 2015-07-07 | Merck Serono S.A. | Indazolyl triazol derivatives |
| WO2013106254A1 (en) | 2012-01-11 | 2013-07-18 | Dow Agrosciences Llc | Pesticidal compositions and processes related thereto |
| US9126984B2 (en) * | 2013-11-08 | 2015-09-08 | Iteos Therapeutics | 4-(indol-3-yl)-pyrazole derivatives, pharmaceutical compositions and methods for use |
| EP3066090A1 (en) | 2013-11-08 | 2016-09-14 | iTeos Therapeutics | 4-(indol-3-yl)-pyrazole derivatives, pharmaceutical compositions and methods for use |
| TWI667233B (en) * | 2013-12-19 | 2019-08-01 | 德商拜耳製藥公司 | Novel indazolecarboxamides, processes for their preparation, pharmaceutical preparations comprising them and their use for producing medicaments |
| SG11201605408RA (en) * | 2014-01-10 | 2016-07-28 | Aurigene Discovery Tech Ltd | Indazole compounds as irak4 inhibitors |
| JO3705B1 (en) * | 2014-11-26 | 2021-01-31 | Bayer Pharma AG | Novel substituted indazoles, processes for preparation thereof, pharmaceutical preparations comprising them and use thereof for production of medicaments |
| WO2016174183A1 (en) | 2015-04-30 | 2016-11-03 | Bayer Pharma Aktiengesellschaft | Combinations of inhibitors of irak4 with inhibitors of btk |
| BR112018000624A2 (en) | 2015-07-15 | 2018-09-18 | Aurigene Discovery Technologies Limited | indazole and azaindazole compounds as irak-4 inhibitors |
| CA3016364A1 (en) | 2016-03-03 | 2017-09-08 | Bayer Pharma Aktiengesellschaft | New 2-substituted indazoles, methods for producing same, pharmaceutical preparations that contain same, and use of same to produce drugs |
| EP3219329A1 (en) * | 2016-03-17 | 2017-09-20 | Bayer Pharma Aktiengesellschaft | Combinations of copanlisib |
| CN109071491B (en) | 2016-04-29 | 2020-08-21 | 拜耳医药股份有限公司 | Indazole synthesis |
| MX2018013235A (en) | 2016-04-29 | 2019-02-13 | Bayer Pharma AG | Polymorphic form of n-{6-(2-hydroxypropan-2-yl)-2-[2-(methylsulph onyl)ethyl]-2h-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carbo xamide. |
| KR102547834B1 (en) | 2016-06-01 | 2023-06-26 | 바이엘 애니멀 헬스 게엠베하 | Substituted indazoles useful for the treatment and prevention of allergic and/or inflammatory diseases in animals |
| BR112018074919A2 (en) | 2016-06-01 | 2020-11-03 | Bayer Pharma Aktiengesellschaft | use of 2-substituted indoles for treatment and prophylaxis of autoimmune diseases. |
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