Claims for Patent: 9,994,550
✉ Email this page to a colleague
Summary for Patent: 9,994,550
Title: | Heterocyclic modulators of lipid synthesis for use against cancer and viral infections |
Abstract: | Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds. |
Inventor(s): | Wagman; Allan S. (Belmont, CA), Johnson; Russell J. (Sunnyvale, CA), Zaharia; Cristiana A. (Redwood City, CA), Cai; Haiying (Cupertino, CA), Hu; Lily W. (Palo Alto, CA), Duke; Greg (Menlo Park, CA), Ohol-Gupta; Yamini (Menlo Park, CA), Heuer; Timothy (Menlo Park, CA), O\'Farrell; Marie (Menlo Park, CA) |
Assignee: | 3-V Biosciences, Inc. (Menlo Park, CA) |
Application Number: | 15/110,154 |
Patent Claims: | 1. A compound of Formula I: ##STR00040## or a pharmaceutically acceptable salt thereof, wherein: L-Ar is ##STR00041## Ar is ##STR00042## R.sup.1 is H, --CN, halogen,
C.sub.1-C.sub.4 alkyl, --O--(C.sub.3-C.sub.5 cycloalkyl), --O-(4- to 6-membered heterocycle) or --O--(C.sub.1-C.sub.4 alkyl), wherein when R.sup.1 is not H, --CN or halogen, R.sup.1 is optionally substituted with one or more halogen; each R.sup.2 is
independently hydrogen, halogen or C.sub.1-C.sub.4 alkyl; R.sup.3 is H or F; R.sup.21 is H, halogen, C.sub.1-C.sub.4 alkyl, C.sub.3-C.sub.5 cycloalkyl or 4- to 6-membered heterocycle; R.sup.22 is H, halogen or C.sub.1-C.sub.2 alkyl; R.sup.24 is
--O--(C.sub.1-C.sub.4 alkyl), --O--(C.sub.1-C.sub.4 alkyl)-O--(C.sub.1-C.sub.4 alkyl), --O--(C.sub.3-C.sub.5 cycloalkyl), or --O-(4- to 6-membered heterocycle), wherein R.sup.24 is optionally substituted with one or more hydroxyl or halogen; and
R.sup.25 is H, halogen, C.sub.1-C.sub.4 alkyl or C.sub.3-C.sub.5 cycloalkyl, wherein R.sup.25 is optionally substituted with one or more halogen; wherein the compound is not: ##STR00043##
2. The compound of claim 1, wherein L-Ar is ##STR00044## 3. The compound of claim 1, wherein L-Ar is ##STR00045## 4. The compound of claim 1, wherein L-Ar is ##STR00046## 5. The compound of claim 1, wherein R.sup.3 is H. 6. The compound of claim 1, wherein R.sup.1 is --CN or --O--(C.sub.1-C.sub.4 alkyl), wherein when R.sup.1 is not --CN, R.sup.1 is optionally substituted with one or more halogen; or R.sup.1 is --CN; or R.sup.1 is --O--(C.sub.1-C.sub.4 alkyl) optionally substituted with one or more halogen. 7. The compound of claim 1, wherein each R.sup.2 is hydrogen. 8. The compound of claim 1, wherein R.sup.21 is C.sub.1-C.sub.4 alkyl. 9. The compound claim 1, wherein R.sup.22 is H or C.sub.1-C.sub.2 alkyl. 10. The compound of claim 1, wherein R.sup.24 is --O--(C.sub.1-C.sub.4 alkyl) optionally substituted with one or more hydroxyl or halogen; or R.sup.24 is --O--(C.sub.1-C.sub.4 alkyl) optionally substituted with one or more hydroxyl. 11. The compound of claim 1, wherein R.sup.25 is --CH.sub.3. 12. The compound of claim 1, having one of the following structures: ##STR00047## ##STR00048## ##STR00049## ##STR00050## 13. The compound of claim 1, wherein the compound is: ##STR00051## 14. The compound of claim 1, wherein the compound is: ##STR00052## 15. A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, excipient, or diluent. 16. A method of treating a condition characterized by disregulation of a fatty acid synthase pathway in a subject by administering to the subject a therapeutically effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein the condition characterized by disregulation of a fatty acid synthase pathway is a cancer. 17. The method of claim 16, wherein the cancer is selected from the group consisting of breast cancer; mantle cell lymphoma; renal cell carcinoma; acute myelogenous leukemia (AML); chronic myelogenous leukemia (CML); diffuse large B cell lymphoma (DLBCL); sarcoma; rhabdomyosarcoma; ovarian cancer; endometrial tumors; non small cell lung carcinoma (NSCLC); small cell, squamous, large cell and adenocarcinoma; lung cancer; colon cancer; colorectal tumors; KRAS-mutated colorectal tumors; gastric carcinomas; hepatocellular tumors; liver tumors; primary melanomas; pancreatic cancer; prostate carcinoma; thyroid carcinoma; follicular thyroid carcinoma; anaplastic large cell lymphoma (ALCL); hamaratomas, angiomyelolipomas, TSC-associated and sporadic lymphangioleiomyomatosis: Cowden's disease (multiple hamaratoma syndrome); sclerosing hemangioma; Peutz-Jeghers syndrome (PJS); head and neck cancer; neurofibromatosis; macular degeneration; macular edema; myeloid leukemia; systemic lupus; and autoimmune lymphoproliferative syndrome (ALPS). 18. The method of claim 17, further comprising administering a second therapeutic agent, wherein the second therapeutic agent is a cancer therapeutic agent selected from paclitaxel, doxorubicin, vincristine, actinomycin D, altretamine, asparaginase, bleomycin, busulphan, cabazitaxel, capecitabine, carboplatin, carmustine, chlorambucil, cisplatin, cyclophosphamide, cytarabine, dacarbazine, daunorubicin, docetaxel, epirubicin, etoposide, fludarabine, fluorouracil, gemcitabine, hydroxyurea, idarubicin, ifosfamide, irinotecan, lomustine, melphalan, mercaptopurine, methotrexate, mitomycin, mitozantrone, oxaliplatin, procarbazine, steroids, streptozocin, taxotere, tamozolomide, thioguanine, thiotepa, tomudex, topotecan, treosulfan, uracil-tegufur, vinblastine, vindesine, nivolumab, pembrolizumab, MPDL3280A, MEDI4736, olaparib, erlotinib, necitumumab, traztuzamab, pertuzamab, lapatinib, crizotinib, cabozantinib, onartuamab, ramucirumab, bevacizumab, enzalutamide, abiraterone, tamoxifen, cobimetinib, vemurafenib, everolimus, lapatinib, trastuzumab, Kadyzla, sirolimus, avastin, nexavar, sutent, exemtesane, femora, enzalutamide, bicalutamide, Tafinlar, and Zelboraf. |
Details for Patent 9,994,550
Applicant | Tradename | Biologic Ingredient | Dosage Form | BLA | Approval Date | Patent No. | Expiredate |
---|---|---|---|---|---|---|---|
Recordati Rare Diseases, Inc. | ELSPAR | asparaginase | For Injection | 101063 | 01/10/1978 | ⤷ Try a Trial | 2034-01-07 |
Genentech, Inc. | HERCEPTIN | trastuzumab | For Injection | 103792 | 09/25/1998 | ⤷ Try a Trial | 2034-01-07 |
Genentech, Inc. | HERCEPTIN | trastuzumab | For Injection | 103792 | 02/10/2017 | ⤷ Try a Trial | 2034-01-07 |
Genentech, Inc. | AVASTIN | bevacizumab | Injection | 125085 | 02/26/2004 | ⤷ Try a Trial | 2034-01-07 |
Eli Lilly And Company | CYRAMZA | ramucirumab | Injection | 125477 | 04/21/2014 | ⤷ Try a Trial | 2034-01-07 |
Merck Sharp & Dohme Corp. | KEYTRUDA | pembrolizumab | For Injection | 125514 | 09/04/2014 | ⤷ Try a Trial | 2034-01-07 |
>Applicant | >Tradename | >Biologic Ingredient | >Dosage Form | >BLA | >Approval Date | >Patent No. | >Expiredate |
Make Better Decisions: Try a trial or see plans & pricing
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.