SG11201805387RA - Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists - Google Patents
Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonistsInfo
- Publication number
- SG11201805387RA SG11201805387RA SG11201805387RA SG11201805387RA SG11201805387RA SG 11201805387R A SG11201805387R A SG 11201805387RA SG 11201805387R A SG11201805387R A SG 11201805387RA SG 11201805387R A SG11201805387R A SG 11201805387RA SG 11201805387R A SG11201805387R A SG 11201805387RA
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- SG
- Singapore
- Prior art keywords
- international
- pharmaceutical agents
- meta
- benzoic acid
- acid derivatives
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
- C07D239/12—Nitrogen atoms not forming part of a nitro radical
- C07D239/14—Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to said nitrogen atoms
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
- C07D239/12—Nitrogen atoms not forming part of a nitro radical
- C07D239/16—Nitrogen atoms not forming part of a nitro radical acylated on said nitrogen atoms
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- C07—ORGANIC CHEMISTRY
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- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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- C07—ORGANIC CHEMISTRY
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Dermatology (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
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- Emergency Medicine (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
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- Neurology (AREA)
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Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 6 July 2017 (06.07.2017) WIPOIPCT (10) International Publication Number WO 2017/117538 A1 (51) International Patent Classification: C07D 239/16 (2006.01) C07D 401/12 (2006.01) C07D 239/14 (2006.01) C07D 233/28 (2006.01) C07D 239/02 (2006.01) A61K31/44 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2016/069511 30 December 2016 (30.12.2016) English English (30) Priority Data: 62/273,246 30 December 2015 (30.12.2015) US (71) Applicant: SAINT LOUIS UNIVERSITY [US/US]; 221 N. Grand Blvd., St. Louis, MO 63103 (US). (72) Inventors: RUMINSKI, Peter, G.; 33 Blackwolf Run Court, Wildwood, MO 63040 (US). GRIGGS, David, W.; 1237 Oak Borough Drive, Ballwin, MO 63021 (US). (74) Agent: LONG, S., Reid; Parker Highlander PLLC, 1120 S. Capital Of Texas Highway, Building One, Suite 200, Austin, TX 78746 (US). (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, 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)) (54) Title: META-AZACYCLIC AMINO BENZOIC ACID DERIVATIVES AS PAN INTEGRIN ANTAGONISTS OH 00 m i> CO,R' (I) i-H (57) : The present disclosure provides pharmaceutical agents of the formula: wherein the variables are defined herein. Also © provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of us -CJ ing the pharmaceutical agents for the treatment of a variety of diseases and disorders are also provided.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562273246P | 2015-12-30 | 2015-12-30 | |
| PCT/US2016/069511 WO2017117538A1 (en) | 2015-12-30 | 2016-12-30 | Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201805387RA true SG11201805387RA (en) | 2018-07-30 |
Family
ID=57868367
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201805387RA SG11201805387RA (en) | 2015-12-30 | 2016-12-30 | Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists |
Country Status (16)
| Country | Link |
|---|---|
| US (3) | US10035778B2 (en) |
| EP (2) | EP3294716B1 (en) |
| JP (1) | JP2019500355A (en) |
| KR (1) | KR20180107121A (en) |
| CN (1) | CN108779077A (en) |
| AU (1) | AU2016381336A1 (en) |
| BR (1) | BR112018012981A2 (en) |
| CA (1) | CA3008023A1 (en) |
| CO (1) | CO2018007278A2 (en) |
| ES (1) | ES2806276T3 (en) |
| HK (1) | HK1244806A1 (en) |
| IL (1) | IL259951A (en) |
| PH (1) | PH12018501362A1 (en) |
| RU (1) | RU2729518C2 (en) |
| SG (1) | SG11201805387RA (en) |
| WO (1) | WO2017117538A1 (en) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HK1244806A1 (en) * | 2015-12-30 | 2018-08-17 | Saint Louis University | Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists |
| BR112019017929A2 (en) | 2017-02-28 | 2020-05-19 | Morphic Therapeutic Inc | integrin (alpha-v) (beta-6) inhibitors |
| EP4147698A1 (en) | 2017-02-28 | 2023-03-15 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| EP3710008A4 (en) * | 2017-11-14 | 2021-08-25 | The Schepens Eye Research Institute, Inc. | INHIBITION OF RUNX1 FOR THE TREATMENT OF PROLIFERATIVE VITREORETINOPATHY AND CONDITIONS ASSOCIATED WITH EPITHELIAL TO MESENCHYMATIC TRANSITION |
| ES3019404T3 (en) | 2018-08-29 | 2025-05-20 | Morphic Therapeutic Inc | Integrin inhibitors |
| WO2021059023A1 (en) | 2019-09-26 | 2021-04-01 | Abionyx Pharma Sa | Compounds useful for treating liver diseases |
| KR20220119424A (en) * | 2019-12-20 | 2022-08-29 | 노파르티스 아게 | Combination treatment of liver disease with integrin inhibitors |
| EP4151632A4 (en) * | 2020-05-14 | 2024-04-24 | UBE Corporation | 1,4,5,6-TETRAHYDROPYRIMIDINE-2-AMINE DERIVATIVE |
| WO2022189856A1 (en) | 2021-03-08 | 2022-09-15 | Abionyx Pharma Sa | Compounds useful for treating liver diseases |
| EP4431098A4 (en) * | 2021-11-12 | 2025-10-08 | Ube Corp | Pharmaceutical composition for the treatment of Alport syndrome |
| WO2024262620A1 (en) * | 2023-06-22 | 2024-12-26 | 株式会社抗体医学研究所 | Integrin-inhibiting small molecule compound |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5639765A (en) | 1995-01-17 | 1997-06-17 | G. D. Searle & Co. | Guanidinoalkyl glycine β-amino acids useful for inhibiting bone loss |
| US5602155A (en) | 1995-01-17 | 1997-02-11 | G. D. Searle & Co. | Platelet aggregation inhibitors |
| US5681820A (en) | 1995-05-16 | 1997-10-28 | G. D. Searle & Co. | Guanidinoalkyl glycine β-amino acids useful for inhibiting tumor metastasis |
| US6013651A (en) * | 1995-08-30 | 2000-01-11 | G. D. Searle & Co. | Meta-azacyclic amino benzoic acid compounds and derivatives thereof |
| US6100423A (en) | 1995-08-30 | 2000-08-08 | G. D. Searle & Co. | Amino benzenepropanoic acid compounds and derivatives thereof |
| AU702487B2 (en) * | 1995-08-30 | 1999-02-25 | G.D. Searle & Co. | Meta-guanidine, urea, thiourea or azacyclic amino benzoic acid derivatives as integrin antagonists |
| ES2162676T3 (en) | 1996-03-29 | 2002-01-01 | Searle & Co | PHENYLENE DERIVATIVES REPLACED IN META AND ITS USE AS ANTAGONISTS OR INHIBITORS OF INTEGRINA ALFAV, BETA3. |
| JP2000510098A (en) | 1996-03-29 | 2000-08-08 | ジー.ディー.サール アンド カンパニー | Cinnamic acid derivative |
| ES2172780T3 (en) | 1996-03-29 | 2002-10-01 | Searle & Co | DERIVATIVES OF PHENYLPROPANOIC ACID SUBSTITUTED IN FOR AS INTEGRINE ANTAGONISTS. |
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-
2016
- 2016-12-30 HK HK18104335.6A patent/HK1244806A1/en unknown
- 2016-12-30 KR KR1020187021837A patent/KR20180107121A/en not_active Withdrawn
- 2016-12-30 CA CA3008023A patent/CA3008023A1/en not_active Abandoned
- 2016-12-30 BR BR112018012981-0A patent/BR112018012981A2/en not_active Application Discontinuation
- 2016-12-30 CN CN201680081360.6A patent/CN108779077A/en active Pending
- 2016-12-30 ES ES16829387T patent/ES2806276T3/en active Active
- 2016-12-30 SG SG11201805387RA patent/SG11201805387RA/en unknown
- 2016-12-30 EP EP16829387.6A patent/EP3294716B1/en active Active
- 2016-12-30 EP EP20169477.5A patent/EP3738953A1/en not_active Withdrawn
- 2016-12-30 AU AU2016381336A patent/AU2016381336A1/en not_active Abandoned
- 2016-12-30 RU RU2018120935A patent/RU2729518C2/en active
- 2016-12-30 WO PCT/US2016/069511 patent/WO2017117538A1/en not_active Ceased
- 2016-12-30 JP JP2018530561A patent/JP2019500355A/en active Pending
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2017
- 2017-11-14 US US15/812,986 patent/US10035778B2/en active Active
-
2018
- 2018-06-11 IL IL259951A patent/IL259951A/en unknown
- 2018-06-25 PH PH12018501362A patent/PH12018501362A1/en unknown
- 2018-07-12 CO CONC2018/0007278A patent/CO2018007278A2/en unknown
- 2018-07-30 US US16/049,679 patent/US10577330B2/en active Active
-
2020
- 2020-03-02 US US16/806,963 patent/US20200199079A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| NZ743308A (en) | 2019-10-25 |
| WO2017117538A1 (en) | 2017-07-06 |
| CO2018007278A2 (en) | 2018-10-10 |
| RU2018120935A3 (en) | 2020-03-20 |
| ES2806276T3 (en) | 2021-02-17 |
| EP3294716A1 (en) | 2018-03-21 |
| AU2016381336A1 (en) | 2018-06-28 |
| RU2729518C2 (en) | 2020-08-07 |
| CA3008023A1 (en) | 2017-07-06 |
| HK1244806A1 (en) | 2018-08-17 |
| US20190023663A1 (en) | 2019-01-24 |
| US10035778B2 (en) | 2018-07-31 |
| PH12018501362A1 (en) | 2019-02-27 |
| JP2019500355A (en) | 2019-01-10 |
| US20200199079A1 (en) | 2020-06-25 |
| CN108779077A (en) | 2018-11-09 |
| KR20180107121A (en) | 2018-10-01 |
| IL259951A (en) | 2018-07-31 |
| BR112018012981A2 (en) | 2018-12-04 |
| EP3738953A1 (en) | 2020-11-18 |
| US20180072684A1 (en) | 2018-03-15 |
| EP3294716B1 (en) | 2020-04-15 |
| RU2018120935A (en) | 2020-01-30 |
| US10577330B2 (en) | 2020-03-03 |
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