JP2014508175A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014508175A5 JP2014508175A5 JP2013558200A JP2013558200A JP2014508175A5 JP 2014508175 A5 JP2014508175 A5 JP 2014508175A5 JP 2013558200 A JP2013558200 A JP 2013558200A JP 2013558200 A JP2013558200 A JP 2013558200A JP 2014508175 A5 JP2014508175 A5 JP 2014508175A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- compound according
- alkyl
- compound
- disease
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 37
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 208000028017 Psychotic disease Diseases 0.000 claims description 10
- 208000035475 disorder Diseases 0.000 claims description 10
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 6
- 208000010877 cognitive disease Diseases 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 208000011580 syndromic disease Diseases 0.000 claims description 6
- 102000003676 Glucocorticoid Receptors Human genes 0.000 claims description 5
- 108090000079 Glucocorticoid Receptors Proteins 0.000 claims description 5
- 208000030507 AIDS Diseases 0.000 claims description 4
- 241000725303 Human immunodeficiency virus Species 0.000 claims description 4
- 208000002193 Pain Diseases 0.000 claims description 4
- 208000013200 Stress disease Diseases 0.000 claims description 4
- 230000000561 anti-psychotic effect Effects 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 4
- 208000024714 major depressive disease Diseases 0.000 claims description 4
- 230000004584 weight gain Effects 0.000 claims description 4
- 235000019786 weight gain Nutrition 0.000 claims description 4
- 230000003042 antagnostic effect Effects 0.000 claims description 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 2
- 208000026872 Addison Disease Diseases 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000019901 Anxiety disease Diseases 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 208000010392 Bone Fractures Diseases 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- 206010006895 Cachexia Diseases 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 208000000094 Chronic Pain Diseases 0.000 claims description 2
- 208000028698 Cognitive impairment Diseases 0.000 claims description 2
- 208000014311 Cushing syndrome Diseases 0.000 claims description 2
- 206010012218 Delirium Diseases 0.000 claims description 2
- 206010012289 Dementia Diseases 0.000 claims description 2
- 206010012335 Dependence Diseases 0.000 claims description 2
- 201000010374 Down Syndrome Diseases 0.000 claims description 2
- 206010017076 Fracture Diseases 0.000 claims description 2
- 208000010412 Glaucoma Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 206010061598 Immunodeficiency Diseases 0.000 claims description 2
- 208000029462 Immunodeficiency disease Diseases 0.000 claims description 2
- 102000006992 Interferon-alpha Human genes 0.000 claims description 2
- 108010047761 Interferon-alpha Proteins 0.000 claims description 2
- 208000019695 Migraine disease Diseases 0.000 claims description 2
- 208000010428 Muscle Weakness Diseases 0.000 claims description 2
- 206010028372 Muscular weakness Diseases 0.000 claims description 2
- 208000012902 Nervous system disease Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 208000001132 Osteoporosis Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 201000009916 Postpartum depression Diseases 0.000 claims description 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 2
- 208000036142 Viral infection Diseases 0.000 claims description 2
- 208000021017 Weight Gain Diseases 0.000 claims description 2
- 230000001919 adrenal effect Effects 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 230000007815 allergy Effects 0.000 claims description 2
- 208000022531 anorexia Diseases 0.000 claims description 2
- 230000036506 anxiety Effects 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 230000015556 catabolic process Effects 0.000 claims description 2
- 208000025302 chronic primary adrenal insufficiency Diseases 0.000 claims description 2
- 231100000876 cognitive deterioration Toxicity 0.000 claims description 2
- 230000037410 cognitive enhancement Effects 0.000 claims description 2
- 206010061428 decreased appetite Diseases 0.000 claims description 2
- 230000000994 depressogenic effect Effects 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 230000006870 function Effects 0.000 claims description 2
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims description 2
- 201000001421 hyperglycemia Diseases 0.000 claims description 2
- 230000007813 immunodeficiency Effects 0.000 claims description 2
- 230000007365 immunoregulation Effects 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 206010027599 migraine Diseases 0.000 claims description 2
- 208000027061 mild cognitive impairment Diseases 0.000 claims description 2
- 230000036457 multidrug resistance Effects 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 230000002980 postoperative effect Effects 0.000 claims description 2
- 208000021011 postpartum psychosis Diseases 0.000 claims description 2
- 201000009395 primary hyperaldosteronism Diseases 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 206010039083 rhinitis Diseases 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 230000009385 viral infection Effects 0.000 claims description 2
- 230000029663 wound healing Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 6
- 238000000034 method Methods 0.000 description 9
- 0 *N(C(C(Cc1ccccc1)=C(C(CC1)CCC1c1ccccc1)N1)=O)C1=O Chemical compound *N(C(C(Cc1ccccc1)=C(C(CC1)CCC1c1ccccc1)N1)=O)C1=O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161454289P | 2011-03-18 | 2011-03-18 | |
| US61/454,289 | 2011-03-18 | ||
| PCT/US2012/029376 WO2012129074A1 (en) | 2011-03-18 | 2012-03-16 | Pyrimidine cyclohexyl glucocorticoid receptor modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014508175A JP2014508175A (ja) | 2014-04-03 |
| JP2014508175A5 true JP2014508175A5 (enExample) | 2015-03-19 |
| JP6039587B2 JP6039587B2 (ja) | 2016-12-07 |
Family
ID=46879684
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013558200A Active JP6039587B2 (ja) | 2011-03-18 | 2012-03-16 | ピリミジンシクロヘキシルグルココルチコイドレセプター調節因子 |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US8685973B2 (enExample) |
| EP (1) | EP2685827B1 (enExample) |
| JP (1) | JP6039587B2 (enExample) |
| KR (2) | KR101889742B1 (enExample) |
| CN (1) | CN103596431B (enExample) |
| AU (1) | AU2012231265B2 (enExample) |
| BR (1) | BR112013023689B1 (enExample) |
| CA (1) | CA2830411C (enExample) |
| CL (1) | CL2013002667A1 (enExample) |
| CO (1) | CO6821943A2 (enExample) |
| DK (1) | DK2685827T3 (enExample) |
| ES (1) | ES2563444T3 (enExample) |
| IL (1) | IL228466A (enExample) |
| MX (1) | MX347862B (enExample) |
| MY (1) | MY161170A (enExample) |
| PE (1) | PE20141378A1 (enExample) |
| PH (1) | PH12013501906A1 (enExample) |
| PL (1) | PL2685827T3 (enExample) |
| RU (1) | RU2599253C2 (enExample) |
| SG (1) | SG193509A1 (enExample) |
| UA (1) | UA109931C2 (enExample) |
| WO (1) | WO2012129074A1 (enExample) |
| ZA (1) | ZA201307245B (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2685827B1 (en) * | 2011-03-18 | 2016-02-03 | Corcept Therapeutics, Inc. | Pyrimidine cyclohexyl glucocorticoid receptor modulators |
| US12226412B2 (en) | 2012-05-25 | 2025-02-18 | Corcept Therapeutics, Inc. | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
| US8859774B2 (en) | 2012-05-25 | 2014-10-14 | Corcept Therapeutics, Inc. | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
| US10183949B2 (en) | 2014-08-29 | 2019-01-22 | The University Of Tokyo | Pyrimidinone derivative having autotaxin-inhibitory activity |
| PH12017500710B1 (en) * | 2014-10-15 | 2024-01-17 | Corcept Therapeutics Inc | Fatty liver disease treatment using glucocorticoid and mineralocorticoid receptor antagonists |
| AU2016226451B2 (en) * | 2015-03-02 | 2019-12-19 | Corcept Therapeutics, Inc. | Use of glucocorticoid receptor antagonist and somatostatin analogues to treat ACTH-secreting tumors |
| AU2016243625B2 (en) * | 2015-03-30 | 2020-09-10 | Corcept Therapeutics, Inc. | Use of glucocorticoid receptor antagonists in combination with glucocorticoids to treat adrenal insufficiency |
| CA2994422A1 (en) | 2015-08-13 | 2017-02-16 | Corcept Therapeutics, Inc. | Method for differentially diagnosing acth-dependent cushing's syndrome |
| PL3350175T3 (pl) * | 2015-09-15 | 2020-07-27 | Leo Pharma A/S | Niesteroidowe modulatory receptora glukokortykoidowego do miejscowego dostarczania leku |
| AU2017210156B2 (en) | 2016-01-19 | 2021-10-28 | Corcept Therapeutics, Inc. | Differential diagnosis of Ectopic Cushing's Syndrome |
| EP3592358A4 (en) | 2017-03-09 | 2020-12-16 | Corcept Therapeutics, Inc. | USE OF GLUCOCORTICOID RECEPTOR MODULATORS IN TREATMENT OF CATECHOLAMINE SECRETTING TUMORS |
| MX2019011543A (es) | 2017-03-31 | 2019-12-16 | Corcept Therapeutics Inc | Moduladores del receptor de glucocorticoides para el tratamiento de cancer cervical. |
| ES3043682T3 (en) * | 2017-06-20 | 2025-11-25 | Corcept Therapeutics Inc | Treatment of neuroepithelial tumors using selective glucocorticoid receptor modulators |
| KR102589213B1 (ko) * | 2018-06-04 | 2023-10-12 | 코어셉트 쎄라퓨틱스 인코포레이티드 | 피리미딘 사이클로헥세닐 글루코코르티코이드 수용체 조절제 |
| IL263184A (en) | 2018-11-21 | 2020-05-31 | Yarden Yosef | Method of treating cancer and compositions for same |
| US11234971B2 (en) | 2018-12-19 | 2022-02-01 | Corcept Therapeutics Incorporated | Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent |
| WO2020132046A1 (en) | 2018-12-19 | 2020-06-25 | Corcept Therapeutics Incorporated | Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent |
| KR102657097B1 (ko) | 2018-12-19 | 2024-04-15 | 코어셉트 쎄라퓨틱스 인코포레이티드 | 헤테로아릴-케톤 융합 아자데칼린 화합물인 렐라코릴란트를 함유하는 약학적 제제 |
| AU2020400061B2 (en) | 2019-12-11 | 2025-02-13 | Corcept Therapeutics Incorporated | Methods of treating antipsychotic-induced weight gain with miricorilant |
| AU2020408057A1 (en) | 2019-12-21 | 2022-06-16 | Corcept Therapeutics Incorporated | Treatment of, and differential diagnosis between, ACTH-Dependent Cushing's syndrome and ACTH-Independent Cushing's syndrome |
| US11548856B2 (en) | 2020-05-06 | 2023-01-10 | Corcept Therapeutics Incorporated | Polymorphs of pyrimidine cyclohexyl glucocorticoid receptor modulators |
| BR112022022473A2 (pt) * | 2020-05-06 | 2022-12-13 | Corcept Therapeutics Inc | Formulações de moduladores de receptor de glucocorticoide ciclo-hexil pirimidina |
| IL303881A (en) * | 2020-12-21 | 2023-08-01 | Corcept Therapeutics Inc | Method of preparing pyrimidine cyclohexyl glucocorticoid receptor modulators |
| WO2022134033A1 (en) | 2020-12-25 | 2022-06-30 | Corcept Therapeutics Incorporated | Methods of preparing heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
| EP4333848A4 (en) * | 2021-05-05 | 2025-03-19 | Corcept Therapeutics Incorporated | Methods for reducing liver fat and treating fatty liver disease |
| CA3243549A1 (en) * | 2021-12-21 | 2023-06-29 | Corcept Therapeutics Inc | INDAZOLE PIPERAZINE-BASED GLUCOCORTICOID RECEPTOR ANTAGONISTS |
| CN119997939A (zh) | 2022-10-06 | 2025-05-13 | 科赛普特治疗公司 | 糖皮质激素受体调节剂的制剂 |
| KR20250102046A (ko) | 2022-10-28 | 2025-07-04 | 코어셉트 쎄라퓨틱스 인코포레이티드 | 다주코릴란트를 이용한 근위축성 측삭경화증의 치료 |
| US20250011290A1 (en) * | 2023-05-30 | 2025-01-09 | Corcept Therapeutics Incorporated | Pyrylium method of preparing pyrimidine cyclohexyl glucocorticoid receptor modulators |
| US20250002462A1 (en) * | 2023-05-30 | 2025-01-02 | Corcept Therapeutics Incorporated | Sulfone method of preparing pyrimidine cyclohexyl glucocorticoid receptor modulators |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4391904A (en) | 1979-12-26 | 1983-07-05 | Syva Company | Test strip kits in immunoassays and compositions therein |
| DE3011809A1 (de) | 1980-03-27 | 1981-10-01 | Cassella Ag, 6000 Frankfurt | Pyrimidyl-chinazoline, verfahren zu ihrer herstellung, sie enthaltende pharmazeutische praeparate und ihre verwendung |
| US5008267A (en) | 1988-10-29 | 1991-04-16 | Mitsui Toatsu Chemicals, Incorporated | Pyrimidinedione compounds, method of producing the same and antiarrythmic agents containing the same |
| JPH06128238A (ja) | 1992-10-20 | 1994-05-10 | Mitsui Toatsu Chem Inc | 新規ピリミジンジオン誘導体 |
| EP0722732A1 (en) | 1995-01-24 | 1996-07-24 | Mitsui Toatsu Chemicals, Inc. | Long-acting drug formulation containing pyrimidinedione derivatives |
| ES2157366T3 (es) * | 1995-06-09 | 2001-08-16 | Hoffmann La Roche | Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos. |
| JPH1017555A (ja) | 1996-07-02 | 1998-01-20 | Mitsui Petrochem Ind Ltd | 6−アミノ−5−メチルウラシル誘導体 |
| EP1201660B1 (en) | 2000-10-30 | 2005-08-31 | Pfizer Products Inc. | Glucocorticoid receptor modulators |
| GB0029100D0 (en) | 2000-11-29 | 2001-01-10 | Karobio Ab | Compounds active at the glucocorticoid receptor |
| WO2003084937A2 (en) | 2002-04-10 | 2003-10-16 | Orchid Chemicals & Pharmaceuticals Limited | Pyrimidinedione derivatives useful for the treatment of inflammation and immunological diseases |
| US7135575B2 (en) * | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| NZ548374A (en) * | 2004-01-09 | 2010-05-28 | Corcept Therapeutics Inc | Azadecalin glucocorticoid receptor modulators |
| EP1778236B1 (en) | 2004-07-02 | 2010-07-14 | Corcept Therapeutics, Inc. | Modified pyrimidine glucocorticoid receptor modulators |
| KR101237312B1 (ko) * | 2006-02-10 | 2013-03-04 | 삼진제약주식회사 | 피리미딘다이온 유도체를 포함하는 c형 간염의 예방 및치료용 약학 조성물 |
| DE102006033109A1 (de) * | 2006-07-18 | 2008-01-31 | Grünenthal GmbH | Substituierte Heteroaryl-Derivate |
| SA08280783B1 (ar) * | 2007-01-11 | 2011-04-24 | استرازينيكا ايه بي | مشتقات بيريدوبيريميدين كمثبطات pde4 |
| EP2685827B1 (en) | 2011-03-18 | 2016-02-03 | Corcept Therapeutics, Inc. | Pyrimidine cyclohexyl glucocorticoid receptor modulators |
-
2012
- 2012-03-16 EP EP12760812.3A patent/EP2685827B1/en active Active
- 2012-03-16 CA CA2830411A patent/CA2830411C/en active Active
- 2012-03-16 PE PE2013002053A patent/PE20141378A1/es active IP Right Grant
- 2012-03-16 MY MYPI2013003340A patent/MY161170A/en unknown
- 2012-03-16 RU RU2013146518/04A patent/RU2599253C2/ru not_active IP Right Cessation
- 2012-03-16 UA UAA201312083A patent/UA109931C2/ru unknown
- 2012-03-16 JP JP2013558200A patent/JP6039587B2/ja active Active
- 2012-03-16 DK DK12760812.3T patent/DK2685827T3/en active
- 2012-03-16 PL PL12760812T patent/PL2685827T3/pl unknown
- 2012-03-16 KR KR1020137027459A patent/KR101889742B1/ko active Active
- 2012-03-16 US US13/422,399 patent/US8685973B2/en active Active
- 2012-03-16 PH PH1/2013/501906A patent/PH12013501906A1/en unknown
- 2012-03-16 ES ES12760812.3T patent/ES2563444T3/es active Active
- 2012-03-16 BR BR112013023689-2A patent/BR112013023689B1/pt active IP Right Grant
- 2012-03-16 CN CN201280023901.1A patent/CN103596431B/zh active Active
- 2012-03-16 KR KR1020187011496A patent/KR101925955B1/ko active Active
- 2012-03-16 MX MX2013010490A patent/MX347862B/es active IP Right Grant
- 2012-03-16 AU AU2012231265A patent/AU2012231265B2/en active Active
- 2012-03-16 SG SG2013069992A patent/SG193509A1/en unknown
- 2012-03-16 WO PCT/US2012/029376 patent/WO2012129074A1/en not_active Ceased
-
2013
- 2013-09-16 CL CL2013002667A patent/CL2013002667A1/es unknown
- 2013-09-16 IL IL228466A patent/IL228466A/en active IP Right Grant
- 2013-09-27 ZA ZA2013/07245A patent/ZA201307245B/en unknown
- 2013-10-16 CO CO13245606A patent/CO6821943A2/es not_active Application Discontinuation
-
2014
- 2014-02-13 US US14/179,960 patent/US8906917B2/en active Active
- 2014-11-07 US US14/535,719 patent/US9321736B2/en active Active