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1. 发明申请

WO2008012290A2 QUINUCLIDINE DERIVATIVES AS M3 ANTAGONISTS 审中-公开
标题翻译：喹啉衍生物作为M3拮抗剂
公开(公告)号：WO2008012290A2
公开(公告)日：2008-01-31
申请号：PCT/EP2007057585
申请日：2007-07-23
申请人： CHIESI FARMA SPA , AMARI GABRIELE , RIZZI ANDREA , PATACCHINI RICCARDO , CENACCHI VALENTINA , VILLETTI GINO , CATENA RUIZ JUAN LORENZO , MASIP MASIP ISABEL
发明人： AMARI GABRIELE , RIZZI ANDREA , PATACCHINI RICCARDO , CENACCHI VALENTINA , VILLETTI GINO , CATENA RUIZ JUAN LORENZO , MASIP MASIP ISABEL
IPC分类号： C07D453/02 , A61K45/06 , A61P11/00
CPC分类号： C07D453/02
摘要： Quinuclidine derivative of the general formula (I) in the form of single enantiomers or mixtures thereof are useful in the manufacture of a medicament for the prevention and therapy of respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), chronic bronchitis, cough and emphysema wherein: R 1 is selected from H, F, C1, Br, I and (C 1 -C 4 )- alkyl; R 2 is optionally substituted 2- or 3-thienyl, or substituted phenyl; R 3 is (CH 2 ) 1-4 -COR 4 or (CH 2 ) 1-4 -S(O) n R 4 , wherein R 4 is optionally substituted phenyl or optionally substituted 2- or 3-thienyl; n is 0, 1 or 2; X - is a pharmaceutically acceptable anion.
摘要翻译：单一对映异构体或其混合物形式的通式（I）的奎宁环衍生物可用于制备用于预防和治疗呼吸系统疾病如哮喘，慢性阻塞性肺疾病（COPD），慢性支气管炎，咳嗽和肺气肿，其中：R 1选自H，F，C 1，Br，I和（C 1 -C 4 - ） - 烷基; R 2是任选取代的2-或3-噻吩基或取代的苯基; R 3是（CH 2）2 - （CH 2）2或 - （CH 2）其中R 4是任选取代的苯基，其中R 4是任选取代的苯基或任选取代的2-或3-噻吩基; n为0,1或2; X 是药学上可接受的阴离子。

2. 发明专利

IT1258939B Linear or cyclic hexapeptide analogues of tachyquinine and their pharmaceutically acceptable salts, their preparation and pharmaceutical compositions containing them 未知
公开(公告)号：IT1258939B
公开(公告)日：1996-03-08
申请号：ITFI920128
申请日：1992-06-19
申请人： QUARTARA LAURA , MAGGI CARLO ALBERTO , PATACCHINI RICCARDO , PESTELLINI VITTORIO , GIACHETTI ANTONIO
发明人： QUARTARA LAURA , MAGGI CARLO ALBERTO , PATACCHINI RICCARDO , PESTELLINI VITTORIO , GIACHETTI ANTONIO
IPC分类号： A61K20060101 , C07G20060101 , A61K , C07G
摘要： Hexapeptide analogues of tachyquinine and their pharmaceutically acceptable salts of general formula: X-NH-CHR1-W-CHR3-CO-A1-A2-A3-βA1a-Y which are useful for the treatment of diseases and in which the tachyquinines have a pathogenetic role in particular against arthritis, asthma, inflammations, tumoural growths, gastrointestinal hypermotility, Huntington's disease, neuritis, neuralgia, migraine, hypertension, urinary incontinence, urticaria, carcinoid syndrome symptoms, influenza and chills are described.

3. 发明专利

IT1251164B New cyclic hexa:peptide derivs., are tachy:kinin antagonists - useful for treating arthritis, asthma, inflammation, tumours, gastrointestinal hyper motility, migraine, hypertension, etc. 未知
公开(公告)号：IT1251164B
公开(公告)日：1995-05-04
申请号：ITMI912231
申请日：1991-08-08
申请人： QUARTARA LAURA , MAGGI CARLO ALBERTO , PATACCHINI RICCARDO , PESTELLINI VITTORIO , GIACHETTI ANTONIO
发明人： QUARTARA LAURA , MAGGI CARLO ALBERTO , PATACCHINI RICCARDO , PESTELLINI VITTORIO , GIACHETTI ANTONIO
IPC分类号： A61K20060101 , A61K
摘要： Cyclic hexapeptides of the formula (I) and their salts are new. In (I), R1 is H or 1-4C alkyl; R3 is a natural or unnatural aminoacid radical with free or protected side chains or R3 is -(CH2)n-R" (where n is 1-5 and R" is cycloctyl, adamantyl, cyclohexyl or naphthyl, or additionally may be phenyl when n is other than 1, or additionally may be a substd. carboxamide gp. when n is 1 or 2); A1 is Gln or DGln; A2 is TrP or DTrp; A3 is Phe or DPhe; W is CONR1 or CH2NR1 (where R1 is H or CH3). The natural aminoacid is glycine, alanine, valine, leucine, isoleucine, proline, phenylalanine, tryptophan, methionine, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, or histidine, in L- or D-form. The unnatural aminoacid is beta-alanine, D or L 2-aminobutyric acid, D or L 2,3-diaminopropionic acid, D or L norleucine, D or L allosoleucine, D or L pyroglutamic acid, L or D 3-hydroxyproline, L or D 4-hydroxyproline, L or D phenylalanine substd. in the ortho, meta or para position, L or D thienylalanine, L or D pyridylalanine, beta (2- or 3-benzothienylalanine), or 1,2,3,4-tetrahydroisoquinolin -3-carboxylic acid. An aminoacid side chain protector is Mbs, Mtr, NO2, Z, Tos, Pmc, For, Me, Ac, 2-Br-Z, 2-Cl-Z, Bzl, 2,6-dichloro-Bzl, SO3H, Fmoc, OMe, OBzl, OFm, ONp or OSu.

4. 发明专利

CA2658649A1 QUINUCLIDINE DERIVATIVES AS M3 ANTAGONISTS 未知
公开(公告)号：CA2658649A1
公开(公告)日：2008-01-31
申请号：CA2658649
申请日：2007-07-23
申请人： CHIESI FARMA SPA
发明人： AMARI GABRIELE , RIZZI ANDREA , VILLETTI GINO , CATENA RUIZ JUAN LORENZO , MASIP MASIP ISABEL , CENACCHI VALENTINA , PATACCHINI RICCARDO
IPC分类号： C07D453/02 , A61K45/06 , A61P11/00
摘要： Quinuclidine derivative of the general formula (I) in the form of single enantiomers or mixtures thereof are useful in the manufacture of a medicamen t for the prevention and therapy of respiratory diseases such as asthma, chr onic obstructive pulmonary disease (COPD), chronic bronchitis, cough and emp hysema wherein: R1 is selected from H, F, C1, Br, I and (C1-C4)- alkyl; R2 i s optionally substituted 2- or 3-thienyl, or substituted phenyl; R3 is (CH2) 1-4-COR4 or (CH2)1-4-S(O)nR4, wherein R4 is optionally substituted phenyl or optionally substituted 2- or 3-thienyl; n is 0, 1 or 2; X- is a pharmaceuti cally acceptable anion.

5. 发明专利

AU2007278231A1 Quinuclidine derivatives as M3 antagonists 未知
公开(公告)号：AU2007278231A1
公开(公告)日：2008-01-31
申请号：AU2007278231
申请日：2007-07-23
申请人： CHIESI FARMA SPA
发明人： AMARI GABRIELE , CENACCHI VALENTINA , MASIP ISABEL MASIP , RUIZ JUAN LORENZO CATENA , PATACCHINI RICCARDO , RIZZI ANDREA , VILLETTI GINO
IPC分类号： A61K45/06 , A61P11/00 , C07D453/02
摘要： Qinuclidine derivative of the general formula (I) in the form of single enantiomers or mixtures thereof are useful in the manufacture of a medicament for the prevention and therapy of respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), chronic bronchitis, cough and emphysema: wherein: R 1 is selected from H, F, Cl, Br, I and (C 1 -C 4 ) - alkyl; R 2 is 2- or 3- optionally substituted thienyl, or substituted phenyl; R 3 is (CH 2 ) 1-4 -COR 4 or (CH 2 ) 1 - 4 -S (O) n R 4 , wherein R 4 is optionally substituted phenyl or 2- or 3- optionally substituted thienyl; n is 0, 1 or 2; X - is a pharmaceutically acceptable anion.

6. 发明专利

BR112013009138A2 composto, usos de um composto, composição farmacêutica, kit de componentes e dispositivos para inalação 未知
公开(公告)号：BR112013009138A2
公开(公告)日：2016-07-26
申请号：BR112013009138
申请日：2011-10-06
申请人： CHIESI FARMA SPA
发明人： GEPPETTI PIERANGELO , PATACCHINI RICCARDO
IPC分类号： C07D453/02 , A61K31/439 , A61P11/14

7. 发明专利

BRPI0713826A2 Derivados dq quinuclidina como antagonistas dos receptores muscarinicos m3 未知
公开(公告)号：BRPI0713826A2
公开(公告)日：2015-05-12
申请号：BRPI0713826
申请日：2007-07-23
申请人： CHIESI FARMA SPA
发明人： AMARI GABRIELE , RIZZI ANDREA , PATACCHINI RICCARDO , CENACCHI VALENTINA , VILLETTI GINO , RUIZ JUAN LORENZO CATENA , MASIP ISABEL MASIP
IPC分类号： C07D453/02 , A61K45/06 , A61P11/00

8. 发明专利

AR083487A1 DERIVADOS DE CARBONATO DE QUINUCLIDINA PARA EL TRATAMIENTO DE TOS 未知
公开(公告)号：AR083487A1
公开(公告)日：2013-02-27
申请号：ARP110103875
申请日：2011-10-19
申请人： CHIESI FARMA SPA
发明人： PATACCHINI RICCARDO , GEPPETTI PIERANGELO
IPC分类号： C07D453/02 , A61K31/439 , A61P11/06 , A61P11/14
摘要： Uso de determinados derivados carbonato de quinuclidina como supresores de la tos, en particular para el tratamiento de pacientes con infecciones del tracto respiratorio superior o asma. Composiciones farmacéuticas.Reivindicación 1: Un compuesto, caracterizado porque es de la fórmula general (1) para su uso en el tratamiento de la tos, en donde R1 y R2 son iguales o diferentes y se seleccionan de manera independiente del grupo que consiste de H, cicloalquilo C3-8, arilo y heteroarilo, en donde dicho arilo o heteroarilo puede estar opcionalmente sustituido con un átomo de halógeno o con uno o más sustituyentes seleccionados de manera independiente del grupo que consiste de OH, O-alquilo C1-10, oxo (=O), SH, S-alquilo C1-10, NO2, CN, CONH2, COOH, alcoxicarbonilo C1-10, alquilsulfanilo C1-10, alquilsulfinilo C1-10, alquilsulfonilo C1-10, alquilo C1-10 y alcoxilo C1-10 o cuando ambos R1 y R2 son de manera independiente arilo o heteroarilo pueden estar unidos a través de un grupo Y que puede ser un grupo (CH2)n (donde n = 0, 1 ó 2), en donde cuando n = 0, Y es un enlace simple, que forma un sistema de anillos tricíclico en donde cualquiera de los átomos de carbono de (CH2)n se puede sustituir con un heteroátomo seleccionado entre O, S, N y con la salvedad que R1 y R2 nunca sean ambos H; y X- es un anión farmacéuticamente aceptable.

9. 发明专利

CA2815035A1 CARBONATE DERIVATIVES FOR THE TREATMENT OF COUGH 未知
公开(公告)号：CA2815035A1
公开(公告)日：2012-04-26
申请号：CA2815035
申请日：2011-10-06
申请人： CHIESI FARMA SPA
发明人： PATACCHINI RICCARDO , GEPPETTI PIERANGELO
IPC分类号： C07D453/02 , A61K31/439 , A61P11/14
摘要： The invention relates to use of certain quinuclidine carbonate derivatives as cough suppressants, particularly for treating patients with upper respiratory tract infections or asthma.

10. 发明专利

EA017698B1 ПРОИЗВОДНЫЕ ХИНУКЛИДИНА В КАЧЕСТВЕ АНТАГОНИСТОВ М3 未知
公开(公告)号：EA017698B1
公开(公告)日：2013-02-28
申请号：EA200970158
申请日：2007-07-23
申请人： CHIESI FARMA SPA
发明人： AMARI GABRIELE , RIZZI ANDREA , PATACCHINI RICCARDO , CENACCHI VALENTINA , VILLETTI GINO , CATENA RUIZ JUAN LORENZO , MASIP MASIP ISABEL
IPC分类号： C07D453/02 , A61K45/06 , A61P11/00
摘要： Представленопроизводноехинуклидинаобщейформулы (Ic), где Rпредставляетсобой 3-фтор; Rявляется 3,4,5-трифторфенилом; X представляетсобой Brили Cl, аименнонастоящееизобретениеотноситсяк новымсоединениям - бромиду (3R)-3-[(3-фторфенил)-(3,4,5-трифторбензил)карбамоилокси]-1-(2-оксо-2-тиофен-2-илэтил)-1-азониабицикло[2.2.2]октанаи хлориду (3R)-3-[(3-фторфенил)-(3,4,5-трифторбензил)карбамоилокси]-1-(2-оксо-2-тиофен-2-илэтил)-1-азониабицикло[2.2.2]октана, применяемымв производствелекарственногосредствадляпредотвращенияилилеченияреспираторныхзаболеваний, такихкакастма, хроническоеобструктивноезаболеваниелегких, хроническийбронхит, кашельи эмфизема. Изобретениетакжеотноситсяк фармацевтическойкомпозициидляпульмональноговведения, содержащейтерапевтическиэффективноеколичествоуказанныхсоединенийи одинилиболеефармацевтическиприемлемыхнаполнителейилиносителей.

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