SG11201906922TA - Processes for preparing ag-10, its intermediates, and salts thereof - Google Patents
Processes for preparing ag-10, its intermediates, and salts thereofInfo
- Publication number
- SG11201906922TA SG11201906922TA SG11201906922TA SG11201906922TA SG11201906922TA SG 11201906922T A SG11201906922T A SG 11201906922TA SG 11201906922T A SG11201906922T A SG 11201906922TA SG 11201906922T A SG11201906922T A SG 11201906922TA SG 11201906922T A SG11201906922T A SG 11201906922TA
- Authority
- SG
- Singapore
- Prior art keywords
- floor
- san francisco
- international
- street
- formula
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title abstract 4
- 239000000543 intermediate Substances 0.000 title abstract 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 abstract 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 abstract 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 2
- WMFOQBRAJBCJND-UHFFFAOYSA-M Lithium hydroxide Chemical compound [Li+].[OH-] WMFOQBRAJBCJND-UHFFFAOYSA-M 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 102220240796 rs553605556 Human genes 0.000 abstract 2
- 208000016057 CHAND syndrome Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
- C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
- C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
- A61K31/415—1,2-Diazoles
-
- 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
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 23 August 2018 (23.08.2018) WIP0 I PCT omit Ill °nolo onm ono oimIE (10) International Publication Number WO 2018/151815 Al (51) International Patent Classification: A61K 31/415 (2006.01) A61P 17/06 (2006.01) A61P 13/12 (2006.01) (21) International Application Number: PCT/US2018/000025 (22) International Filing Date: 16 February 2018 (16.02.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/460,576 17 February 2017 (17.02.2017) US (71) Applicant: EIDOS THERAPEUTICS, INC. [US/US]; 101 Montgomery Street, 25th Floor, San Francisco, CA 94104 (US). (72) Inventors: CHAND, Pooran; 101 Montgomery Street, 25th Floor, San Francisco, CA 94104 (US). GUPTA, Yo- gesh, Kumar; 101 Montgomery Street, 25th Floor, San Francisco, CA 94104 (US). KUMAWAT, Rakesh, Ku- mar; 101 Montgomery Street, 25th Floor, San Francisco, CA 94104 (US). ALHAMADSHEH, Mamoun; 101 Mont- gomery Street, 25th Floor, San Francisco, CA 94104 (US). ZAMBONI, Robert; 101 Montgomery Street, 25th Floor, San Francisco, CA 94104 (US). (74) Agent: KEZER, William B. et al.; Mintz Levin Cohn Fer- ris Glovsky Popeo, P.C., One Financial Center, Boston, MA 02111 (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, JO, 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, (54) Title: PROCESSES FOR PREPARING AG-10, ITS INTERMEDIATES, AND SALTS THEREOF 0 0 K 2 CO 3 +Br'' . \"-\"Br Acetone HO N 2 H. I _H 2 0 HN Ethanol IV— PBr 3 HN OH 0 ' I N— Br+ COOMe OH Vila IN/ Vla 1-1 to 1-1 00 1-1 In 1-1 00 1-1 O DMF K 2 CO 3 COOH COOMe 4 Methanol IX Villa FIG. 1 (57) : Provided herein are improved processes for the preparation of a compound of Formula IX (AG- 10). Also provided herein are pharmaceutically acceptable salts of Formula (I) and Formula (lb) as well as crystalline types of Formula IX (AG- 10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification. [Continued on next page] LiOH WO 2018/151815 Al MIDEDIMOMOIDEIREE3110111HOHOMEEN 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)) before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h))
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762460576P | 2017-02-17 | 2017-02-17 | |
| PCT/US2018/000025 WO2018151815A1 (en) | 2017-02-17 | 2018-02-16 | Processes for preparing ag-10, its intermediates, and salts thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201906922TA true SG11201906922TA (en) | 2019-09-27 |
Family
ID=63166944
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201906922TA SG11201906922TA (en) | 2017-02-17 | 2018-02-16 | Processes for preparing ag-10, its intermediates, and salts thereof |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US10513497B2 (en) |
| EP (1) | EP3582773A4 (en) |
| JP (2) | JP7157752B2 (en) |
| KR (2) | KR20240068787A (en) |
| CN (3) | CN110381940B (en) |
| AU (2) | AU2018222739C1 (en) |
| BR (1) | BR112019016935A2 (en) |
| CA (1) | CA3051357A1 (en) |
| CL (1) | CL2019002321A1 (en) |
| EA (1) | EA201991921A1 (en) |
| IL (2) | IL298196A (en) |
| MA (1) | MA47511A (en) |
| MX (3) | MX2021015220A (en) |
| NZ (1) | NZ755597A (en) |
| SG (1) | SG11201906922TA (en) |
| TW (2) | TWI791487B (en) |
| WO (1) | WO2018151815A1 (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ755597A (en) | 2017-02-17 | 2023-06-30 | Eidos Therapeutics Inc | Processes for preparing ag-10, its intermediates, and salts thereof |
| JP2021518381A (en) | 2018-03-23 | 2021-08-02 | エイドス セラピューティクス，インコーポレイティド | Treatment of TTR Amyloidosis Using AG10 |
| US11260047B2 (en) | 2018-08-17 | 2022-03-01 | Eidos Therapeutics, Inc. | Formulations of AG10 |
| US20220071965A1 (en) | 2018-12-20 | 2022-03-10 | Pfizer Inc. | Pharmaceutical Compositions and Methods Comprising A Combination of a Benzoxazole Transthyretin Stabilizer and an Additional Therapeutic Agent |
| WO2022112919A1 (en) | 2020-11-25 | 2022-06-02 | Pfizer Inc. | (aza)benzothiazolyl substituted pyrazole compounds |
| WO2023009612A1 (en) | 2021-07-28 | 2023-02-02 | Protego Biopharma, Inc. | Acoramidis (3-(3-(3,5-dimethyl-1h-pyrazol-4-yl)propoxy)-4-fluorobenzoic acid) derivatives for stabilizing transthyretin (tts) and inhibiting tts misfolding for the treatment of e.g. peripheral ttr amyloidosis |
| WO2023052652A1 (en) | 2021-10-01 | 2023-04-06 | Sandoz Ag | Crystalline form of acoramidis hydrochloride |
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