SG11201806700RA - Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof - Google Patents
Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereofInfo
- Publication number
- SG11201806700RA SG11201806700RA SG11201806700RA SG11201806700RA SG11201806700RA SG 11201806700R A SG11201806700R A SG 11201806700RA SG 11201806700R A SG11201806700R A SG 11201806700RA SG 11201806700R A SG11201806700R A SG 11201806700RA SG 11201806700R A SG11201806700R A SG 11201806700RA
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- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 title abstract 4
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 title abstract 2
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102000004669 Protein-Lysine 6-Oxidase Human genes 0.000 title 1
- 108010003894 Protein-Lysine 6-Oxidase Proteins 0.000 title 1
- 125000005334 azaindolyl group Chemical class N1N=C(C2=CC=CC=C12)* 0.000 title 1
- 102220240796 rs553605556 Human genes 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000004316 Oxidoreductases Human genes 0.000 abstract 2
- 108090000854 Oxidoreductases Proteins 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical class C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 abstract 1
- 241000167854 Bourreria succulenta Species 0.000 abstract 1
- 206010016654 Fibrosis Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 230000033115 angiogenesis Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000036952 cancer formation Effects 0.000 abstract 1
- 235000019693 cherries Nutrition 0.000 abstract 1
- 230000004761 fibrosis Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 244000144972 livestock Species 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
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- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- 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
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
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- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—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
- C07D209/20—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 substituted additionally by nitrogen atoms, e.g. tryptophane
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- C07D209/04—Indoles; Hydrogenated indoles
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) CORRECTED VERSION (19) World Intellectual Property Organization International Bureau (43) International Publication Date 17 August 2017 (17.08.2017) WiP0 I PCT 111111111111011010101111101011111 0 01110011011104011011101110# (10) International Publication Number WO 2017/136870 A9 (51) International Patent Classification: CO7D 471/04 (2006.01) A61K 31/404 (2006.01) CO7D 413/04 (2006.01) A61P 1/16 (2006.01) CO7D 405/04 (2006.01) A61P 9/00 (2006.01) CO7D 403/04 (2006.01) A61P 13/12 (2006.01) CO7D 401/04 (2006.01) A61P 29/00 (2006.01) CO7D 209/10 (2006.01) A61P 35/00 (2006.01) A61K 31/33 (2006.01) (21) International Application Number: PCT/AU2017/000039 (22) International Filing Date: 10 February 2017 (10.02.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 2016900478 12 February 2016 (12.02.2016) AU 2016902593 01 July 2016 (01.07.2016) AU (71) Applicant: PHARMAXIS LTD. [AU/AU]; 20 Rodbor- ough Road, Frenchs Forest, NSW 2086 (AU). (72) Inventors: FINDLAY, Alison Dorothy; 20 Rodbor- ough Road, Frenchs Forest, NSW 2086 (AU). TURN- ER, Craig Ivan; 20 Rodborough Road, Frenchs For- est, NSW 2086 (AU). DEODHAR, Mandar; 20 Rod- borough Road, Frenchs Forest, NSW 2086 (AU). FOOT, Jonathan Stuart; 20 Rodborough Road, Frenchs Forest, NSW 2086 (AU). JAROLIMEK, Wolfgang; 20 Rodbor- ough Road, Frenchs Forest, NSW 2086 (AU). ZHOU, Wenbin; 20 Rodborough Road, Frenchs Forest, NSW 2086 (AU). ROBERTSON, Alan Duncan; 12 Cherry Street, Warrawee, NSW 2074 (AU). (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, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) (48) Date of publication of this corrected version: 15 February 2018 (15.02.2018) (15) Information about Correction: see Notice of 15 February 2018 (15.02.2018) W O 20 17 / 13687 0 A9 (74) Agent: SPRUSON & FERGUSON; GPO Box 3898, Syd- ney, New South Wales 2001 (AU). (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. (54) Title: HALOALLYLAMINE INDOLE AND AZAINDOLE DERIVATIVE INHIBITORS OF LYSYL OXIDASES AND USES THEREOF (57) : The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2016900478A AU2016900478A0 (en) | 2016-02-12 | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof | |
| AU2016902593A AU2016902593A0 (en) | 2016-07-01 | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof | |
| PCT/AU2017/000039 WO2017136870A1 (en) | 2016-02-12 | 2017-02-10 | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof |
Publications (1)
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| SG11201806700RA true SG11201806700RA (en) | 2018-09-27 |
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| SG11201806727TA SG11201806727TA (en) | 2016-02-12 | 2017-02-10 | Indole and azaindole haloallylamine derivative inhibitors of lysyl oxidases and uses thereof |
| SG11201806700RA SG11201806700RA (en) | 2016-02-12 | 2017-02-10 | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof |
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| Application Number | Title | Priority Date | Filing Date |
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| SG11201806727TA SG11201806727TA (en) | 2016-02-12 | 2017-02-10 | Indole and azaindole haloallylamine derivative inhibitors of lysyl oxidases and uses thereof |
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| JP (2) | JP6843888B2 (en) |
| KR (2) | KR102742235B1 (en) |
| CN (2) | CN109071533B (en) |
| AU (2) | AU2017217239A1 (en) |
| BR (2) | BR112018016484B1 (en) |
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| WO (2) | WO2017136870A1 (en) |
| ZA (2) | ZA201805675B (en) |
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| EP3414244A4 (en) * | 2016-02-12 | 2019-11-27 | Pharmaxis Ltd. | INHIBITORS OF LYSYL OXIDASES DERIVED FROM HALOGENOALLYLAMINE INDOLE AND AZAINDOLE AND USES THEREOF |
| WO2018157190A1 (en) * | 2017-03-02 | 2018-09-07 | Pharmaxis Ltd. | Haloallylamine pyrazole derivative inhibitors of lysyl oxidases and uses thereof |
| GB201716871D0 (en) | 2017-10-13 | 2017-11-29 | Inst Of Cancer Research: Royal Cancer Hospital | Compounds |
| CN107903281B (en) * | 2017-10-27 | 2019-10-29 | 苏州大学 | A kind of method of synthesizing alkyl boron ester compound |
| AR117398A1 (en) | 2018-03-12 | 2021-08-04 | Abbvie Inc | INHIBITORS OF SIGNALING MEDIATED BY TYROSINE KINASE 2 |
| KR20190110736A (en) | 2018-03-21 | 2019-10-01 | 주식회사유한양행 | Novel triazolone derivatives or its salt and pharmaceutical compositions comprising the same |
| KR20190110740A (en) | 2018-03-21 | 2019-10-01 | 주식회사유한양행 | Novel aryl or heteroaryl triazolone derivatives or its salt and pharmaceutical compositions comprising the same |
| WO2020024017A1 (en) | 2018-08-03 | 2020-02-06 | Pharmaxis Ltd. | Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereof |
| TWI835945B (en) | 2018-12-14 | 2024-03-21 | 南韓商柳韓洋行股份有限公司 | 3,3-difluoroallylamines or salts thereof and pharmaceutical compositions comprising the same |
| TW202039486A (en) | 2018-12-14 | 2020-11-01 | 南韓商柳韓洋行股份有限公司 | Triazolopyridin-3-ones or their salts and pharmaceutical compositions comprising the same |
| US20200225249A1 (en) * | 2019-01-11 | 2020-07-16 | Viscient Biosciences, Inc. | Compositions and methods for the diagnosis and treatment of diseases of the liver |
| WO2020161209A1 (en) | 2019-02-06 | 2020-08-13 | Syngenta Crop Protection Ag | Herbicidal fused pyridazine compounds |
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| KR20220040480A (en) * | 2019-07-25 | 2022-03-30 | 파맥시스 엘티디 | Difluorohaloallylamine sulfone derivative inhibitor of lysyl oxidase, preparation method and use thereof |
| JP7629442B2 (en) | 2019-07-29 | 2025-02-13 | ヘパリジェニックス ゲーエムベーハー | Heteroaryl-substituted pyrazolo-pyridine protein kinase inhibitors for promoting liver regeneration or reducing or preventing liver cell death - Patents.com |
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| WO2021155439A1 (en) * | 2020-02-05 | 2021-08-12 | Pharmaxis Ltd. | Bioprobes for lysyl oxidases and uses thereof |
| US11618751B1 (en) | 2022-03-25 | 2023-04-04 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives |
| US20230301950A1 (en) | 2020-06-26 | 2023-09-28 | Raqualia Pharma Inc. | Method for selecting cancer patients for whom combination therapy with retinoid and cancer therapeutic agent is effective, and combination medicament with retinoid and cancer therapeutic agent |
| JP7384138B2 (en) * | 2020-09-30 | 2023-11-21 | 株式会社島津製作所 | electrophoresis device |
| US11319319B1 (en) | 2021-04-07 | 2022-05-03 | Ventus Therapeutics U.S., Inc. | Compounds for inhibiting NLRP3 and uses thereof |
| EP4397655A4 (en) * | 2021-10-01 | 2025-08-06 | Yuhan Corp | BICYCLIC FUSED RING DERIVATIVE OR SALT THEREOF AND PHARMACEUTICAL COMPOSITION THEREOF |
| US12233056B2 (en) | 2022-04-06 | 2025-02-25 | Syntara Limited | Lysyl oxidase inhibitors for treating myeloid malignancies |
| US12331048B2 (en) | 2022-10-31 | 2025-06-17 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 inhibitors |
| AU2024207083A1 (en) * | 2023-01-09 | 2025-07-17 | University Of Florida Research Foundation, Incorporated | Pparg modulators |
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2020
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