HRP20110465T1 - Modulatori aktivnosti receptora kemokina, kristalni oblici i postupak - Google Patents
Modulatori aktivnosti receptora kemokina, kristalni oblici i postupak Download PDFInfo
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- HRP20110465T1 HRP20110465T1 HR20110465T HRP20110465T HRP20110465T1 HR P20110465 T1 HRP20110465 T1 HR P20110465T1 HR 20110465 T HR20110465 T HR 20110465T HR P20110465 T HRP20110465 T HR P20110465T HR P20110465 T1 HRP20110465 T1 HR P20110465T1
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- 102000009410 Chemokine receptor Human genes 0.000 title 1
- 108050000299 Chemokine receptor Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 7
- QAPTWHXHEYAIKG-RCOXNQKVSA-N n-[(1r,2s,5r)-5-(tert-butylamino)-2-[(3s)-2-oxo-3-[[6-(trifluoromethyl)quinazolin-4-yl]amino]pyrrolidin-1-yl]cyclohexyl]acetamide Chemical compound CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1C(=O)[C@@H](NC=2C3=CC(=CC=C3N=CN=2)C(F)(F)F)CC1 QAPTWHXHEYAIKG-RCOXNQKVSA-N 0.000 claims abstract 3
- 150000003839 salts Chemical class 0.000 claims abstract 3
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- 208000011231 Crohn disease Diseases 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 206010020718 hyperplasia Diseases 0.000 claims 3
- 201000006417 multiple sclerosis Diseases 0.000 claims 3
- 206010018364 Glomerulonephritis Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 238000002441 X-ray diffraction Methods 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 239000000843 powder Substances 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 238000002054 transplantation Methods 0.000 claims 2
- 206010065040 AIDS dementia complex Diseases 0.000 claims 1
- 206010001889 Alveolitis Diseases 0.000 claims 1
- 206010002329 Aneurysm Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010063209 Chronic allograft nephropathy Diseases 0.000 claims 1
- 201000001200 Crouzon syndrome-acanthosis nigricans syndrome Diseases 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 208000037357 HIV infectious disease Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010048858 Ischaemic cardiomyopathy Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000001155 extrinsic allergic alveolitis Diseases 0.000 claims 1
- 239000000945 filler Substances 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 208000022098 hypersensitivity pneumonitis Diseases 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000003589 nefrotoxic effect Effects 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 231100000381 nephrotoxic Toxicity 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 210000002966 serum Anatomy 0.000 claims 1
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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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Abstract
Spoj N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-2-okso-3-(6-(trifluorometil)kinazolin-4-ilamino)pirolidin-1-il)cikloheksil)acetamid, ili njegova farmaceutski prihvatljiva sol. Patent sadrži još 11 patentnih zahtjeva.
Claims (12)
1. Spoj N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-2-okso-3-(6-(trifluorometil)kinazolin-4-ilamino)pirolidin-1-il)cikloheksil)acetamid, ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1 koji je kristalni oblik N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-2-okso-3-(6-(trifluorometil)kinazolin-4-ilamino)pirolidin-1-il)cikloheksil)acetamida, ili njegove farmaceutski prihvatljive soli.
3. Kristalni oblik prema zahtjevima 1-2, naznačen time što su parametri jedinične ćelije u biti jednaki sljedećima:
Dimenzije ćelije:
a = 18.7240(4)
b= 8.0171(2)
c = 19.6568(5)
α = 90
β = 114.935(2)
γ = 90
V(Å3) = 2675.7(1)
Prostorna grupa P212121
Molekula/jedinična ćelija 2
pri čemu je taj kristal pri temperaturi od oko +22 ̊C (RT).
4. Kristalni oblik prema zahtjevima 1-3, naznačen time što obrazac difrakcije rendgenskog zračenja na prašku obuhvaća tri ili više 2θ vrijednosti (CuKα λ=1.5418 Å) izabrane između 5.5, 9.1, 12.1, 14.0 i 19.2, pri temperaturi od oko 22 ̊C.
5. Kristalni oblik prema zahtjevima 1-4, dalje naznačen time što obrazac difrakcije rendgenskog zračenja na prašku obuhvaća četiri ili više 2θ values (CuKα λ=1.5418 Å) izabrane između 5.5, 9.1, 12.1, 14.0 i 19.2 pri temperaturi od oko 22 ̊C.
6. Kristalni oblik prema zahtjevima 1-5, naznačen time što su frakcijske atomske koordinate u biti onakve kako su navedene u Tablici 3.
7. Kristalni oblik prema zahtjevima 1-6 čiji je obrazac difrakcije rendgenskog zračenja na prašku u biti onakav kao što je prikazano na Slici 2.
8. Farmaceutska smjesa koja sadrži spoj prema zahtjevima 1-7, i farmaceutski prihvatljiv nosač ili punilo.
9. Spoj prema zahtjevima 1-8 za uporabu u liječenju bolesti kod sisavaca, pri čemu se ta bolest izabire između dijabetesa, pretilosti, metaboličkog sindroma, moždanog udara, neuropatske boli, ishemijske kardiomiopatije, psorijaze, hipertenzije, skleroderme, osteoartritisa, aneurizme, povišene temperature, kardiovaskularne bolesti, Crohnove bolesti, kongestivnog zatajenja srca, autoimunih bolesti, HIV-zaraze, demencije povezane s HIV-om, psorijaze, idiopatske plućne fibroze, arterioskleroze transplantata, fizički ili kemijski inducirane traume mozga, inflamatorne bolesti crijeva, alveolitisa, kolitisa, sistemskog lupusa eritematosusa, nefrotoksičnog serumskog nefritisa, glomerulonefritisa, astme, multiple skleroze, ateroskleroze, vaskulitisa, vulnerabilnog plaka, reumatoidnog artritisa, restenoze, venske neointimalne hiperplazije, dijaliza-graft neointimalne hiperplazije, arterio-venske shunt intimalne hiperplazije, transplantacije organa, kronične nefropatije alografta i raka.
10. Spoj prema zahtjevu 9 pri čemu se bolest izabire između dijabetesa, pretilosti, Crohnove bolesti, sistemskog lupusa eritematosusa, glomerulonefritisa, multiple skleroze, ateroskleroze, restenoze i transplantacije organa.
11. Spoj prema zahtjevima 9-10 pri čemu se bolest izabire između multiple skleroze, ateroskleroze, Crohnove bolesti i dijabetesa.
12. Farmaceutska smjesa prema zahtjevu 8 koja dalje sadrži jednu ili više drugih djelatnih tvari.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US83423506P | 2006-07-28 | 2006-07-28 | |
| US89602607P | 2007-03-21 | 2007-03-21 | |
| US11/782,742 US7629351B2 (en) | 2006-07-28 | 2007-07-25 | N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide and other modulators of chemokine receptor activity, crystalline forms and process |
| PCT/US2007/074377 WO2008014360A2 (en) | 2006-07-28 | 2007-07-26 | Modulators of chemokine receptor activity, crystalline forms and process |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20110465T1 true HRP20110465T1 (hr) | 2011-07-31 |
Family
ID=38829183
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20110465T HRP20110465T1 (hr) | 2006-07-28 | 2011-06-20 | Modulatori aktivnosti receptora kemokina, kristalni oblici i postupak |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US7629351B2 (hr) |
| EP (2) | EP2046779B1 (hr) |
| JP (1) | JP5236643B2 (hr) |
| KR (1) | KR20090033915A (hr) |
| CN (1) | CN101535301B (hr) |
| AR (1) | AR062124A1 (hr) |
| AT (2) | ATE522522T1 (hr) |
| AU (1) | AU2007279333B2 (hr) |
| BR (1) | BRPI0715415A2 (hr) |
| CA (2) | CA2831219A1 (hr) |
| CY (1) | CY1111744T1 (hr) |
| DK (1) | DK2046779T3 (hr) |
| EA (1) | EA016563B1 (hr) |
| ES (1) | ES2365264T3 (hr) |
| HK (1) | HK1130476A1 (hr) |
| HR (1) | HRP20110465T1 (hr) |
| IL (2) | IL196427A (hr) |
| MX (1) | MX2009000808A (hr) |
| NO (1) | NO20090190L (hr) |
| NZ (1) | NZ574425A (hr) |
| PE (1) | PE20080732A1 (hr) |
| PL (1) | PL2046779T3 (hr) |
| PT (1) | PT2046779E (hr) |
| SG (1) | SG158924A1 (hr) |
| SI (1) | SI2046779T1 (hr) |
| TW (2) | TW201414729A (hr) |
| WO (1) | WO2008014360A2 (hr) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7687508B2 (en) * | 2006-07-28 | 2010-03-30 | Bristol-Myers Squibb Company | Cyclic derivatives as modulators of chemokine receptor activity |
| US8383812B2 (en) * | 2009-10-13 | 2013-02-26 | Bristol-Myers Squibb Company | N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-A][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes |
| KR20120135716A (ko) * | 2011-06-07 | 2012-12-17 | 한미사이언스 주식회사 | 이중대칭 구조의 퀴나졸린 유도체 화합물 및 이의 용도 |
| EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US8669281B1 (en) | 2013-03-14 | 2014-03-11 | Alkermes Pharma Ireland Limited | Prodrugs of fumarates and their use in treating various diseases |
| TW201625255A (zh) * | 2014-07-17 | 2016-07-16 | 參天製藥股份有限公司 | 後眼部疾病之預防或治療劑 |
| CA3070423A1 (en) * | 2017-07-20 | 2019-01-24 | Bristol-Myers Squibb Company | Process for the preparation of n-((1r,2s,5r)-5-(tert-butylamino)-2-((s)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide |
| CN115677728A (zh) * | 2022-11-02 | 2023-02-03 | 成都科岭源医药技术有限公司 | 一种海鞘素类化合物中间体的制备方法 |
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| JPS6383082A (ja) | 1986-09-26 | 1988-04-13 | Takeda Chem Ind Ltd | テトラヒドロフランカルボン酸誘導体の製造法 |
| CA2084800A1 (en) | 1991-12-16 | 1993-06-17 | Joseph P. Vacca | Hiv protease inhibitors with an internal lactam ring |
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