[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-flouro-1-(2-methoxy-ethyl)-4-trifluorom as an inhibitor of mast cell tryptase
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IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07D-401/00
A61K-031/445
출원번호
US-0028745
(2011-02-16)
등록번호
US-8217178
(2012-07-10)
발명자
/ 주소
Choi-Sledeski, Yong Mi
Choy, Nakyen
Poli, Gregory Bernard
Shay, Jr., John J.
Shum, Patrick Wai-Kwok
Sledeski, Adam W.
출원인 / 주소
Sanofi
대리인 / 주소
Ort, Ronald G.
인용정보
피인용 횟수 :
0인용 특허 :
17
초록▼
The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by
The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.
대표청구항▼
1. A compound of formula I: or a pharmaceutically acceptable salt thereof. 2. The compound of claim 1 as a pharmaceutically acceptable salt selected from: hydrochloride, fumarate, besylate, tosylate, sulfate, citrate, methanesulfonate, tartrate, phosphate, glutamate and benzoate. 3. The compound acc
1. A compound of formula I: or a pharmaceutically acceptable salt thereof. 2. The compound of claim 1 as a pharmaceutically acceptable salt selected from: hydrochloride, fumarate, besylate, tosylate, sulfate, citrate, methanesulfonate, tartrate, phosphate, glutamate and benzoate. 3. The compound according to claim 2, wherein the salt is benzoate. 4. A crystalline form A of the compound according to claim 3, wherein the crystalline form has XRPD peaks at at least five of the following 2 theta angles: 7.75; 10.13; 17.03; 17.16; 18.39; 21.33; and 21.88. 5. A crystalline form of the compound according to claim 3, wherein the crystalline form melts at 162 degrees Celsius. 6. A method for treating a patient suffering from a physiological condition selected from the group consisting of inflammatory disease, a disease of joint cartilage destruction, inflammatory bowel disease, asthma, interstitial lung disease, fibrosis, chronic obstructive pulmonary disease, pulmonary fibrosis, myocardial fibrosis, and neurofibroma, comprising administering to the patient a therapeutically effective amount of the compound according to claim 1. 7. The method of claim 6, wherein the physiological condition is COPD. 8. An intermediate compound having a formula selected from the group consisting of: 9. A compound having the formula:
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이 특허에 인용된 특허 (17)
Astles, Peter C.; Eastwood, Paul R.; Houille, Olivier; Levell, Julian; Pauls, Heinz; Czekaj, Mark; Liang, Guyan; Gong, Yong; Pribish, James; Neuenschwander, Kent, Chemical compounds.
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Woodle Martin C. (Menlo Park CA) Martin Francis J. (San Francisco CA) Yau-Young Annie (Los Altos CA) Redemann Carl T. (Walnut Creek CA), Liposomes with enhanced circulation time.
Tucker Mark J. (Round Steps ; High Street Stow-on-the-Wold ; Gloucester GL54 1DL GBX) Tucker Mark R. (P.O. Box 23530 Bahrain BHX), Occlusive body for administering a physiologically active substance.
Platz Robert M. (Half Moon Bay CA) Winters Mark A. (Mountain View CA) Pitt Colin G. (Thousand Oaks CA), Pulmonary administration of granulocyte colony stimulating factor.
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