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31. 发明专利

AU746750B2 Therapeutic dinucleotide and derivatives 未知
公开(公告)号：AU746750B2
公开(公告)日：2002-05-02
申请号：AU4083999
申请日：1999-05-19
申请人： INSPIRE PHARMACEUTICALS INC , UNIV NORTH CAROLINA
发明人： YERXA BENJAMIN R , PENDERGAST WILLIAM , RIDEOUT JANET L , PICHER MARYSE , BOUCHER RICHARD C , STUTTS MONROE JACKSON
IPC分类号： C07H19/10 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7084 , A61P11/00 , A61P11/10 , A61P11/12 , A61P27/04 , A61P27/16 , C07H19/207 , C07H21/00 , A61K31/00
摘要： The present invention relates to P1-(cytidine 5'-)-P-(uridine 5'-)tetraphosphates and its salts, esters and amides, and formulations thereof which are highly stable and selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. The compounds of the invention are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, primary ciliary dyskinesia, cystic fibrosis, as well as prevention of pneumonia due to immobility, and the induction of sputum and its expectoration. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis and otitis media.

32. 发明专利

NZ501696A Method for large-scale production of sodium and ammonium salts of di(uridine 5')-tetraphosphate 未知
公开(公告)号：NZ501696A
公开(公告)日：2001-08-31
申请号：NZ50169698
申请日：1998-07-24
申请人： INSPIRE PHARMACEUTICALS INC
发明人： PENDERGAST WILLIAM , YERXA BENJAMIN R
IPC分类号： C07H19/10 , A61K31/7084 , A61P11/00 , A61P11/10 , A61P15/02 , A61P27/02 , A61P27/16 , C07H21/00 , A61K31/706
摘要： The compounds of formula I, wherein X is selected from Na, NH4 and H, (provided that all X groups are not H) may be used in medicaments for treating chronic obstructive pulmonary diseases, sinusitis, otitis media or nasolacrimal duct obstruction, dry eye, retinal detachment, female infertility or vaginal irritation due to vaginal dryness and for facilitating sputum induction and expectoration. The compounds of formula I may be prepared by; a) dissolving uridine, UMP, UDP or UTP in a polar, aprotic organic solvent and a hydrophobic amine; b) phosphorylating with a phosphorylating agent of Formulas IVa-b and/or activating a phosphate group with an activating agent of Formulas IIIa-c; and c) purification by ion exchange chromatography of the compounds of Formula I. In Formula IIIa: Carbodiimide R1 and R2 are independently selected from the group consisting of C1-C8 alkyl, cycloalkyl and aryl, each of which may be optionally substituted with hydroxy or amino groups. In Formula IIIb: Activated Carbonvl X is independently selected from the group consisting of imidazole, tetrazole and halogen. In Formula IIIc: Activated Phosphorus X is halogen and R1 and R2 are each independently selected from the group consisting of C1-C8 alkyl, cycloalkyl, C1-C8 alkoxy, C1-C8 cycloalkoxy, aryl and aryloxy, each of which may be optionally substituted with hydroxy, amino, alkoxy or halogen groups. In Formula IVa: Monophosphorvlating Agents X is halogen. In Formula IVb: Diphosphorylating Agents X is selected from the group consisting of oxygen, hydroxy and halogen.

33. 发明专利

NO20012555D0 未知
公开(公告)号：NO20012555D0
公开(公告)日：2001-05-23
申请号：NO20012555
申请日：2001-05-23
申请人： INSPIRE PHARMACEUTICALS INC
发明人： PENDERGAST WILLIAM , SHAVER SAMMY R , DRUTZ DAVID J , RIDEOUT JANET L
IPC分类号： C07H19/10 , A61K31/00 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7084 , A61P15/02 , C07H19/20 , C07H19/207 , C07H21/00 , A61K
摘要： The present invention provides a method of stimulating cervical and vaginal secretions in a mammal by treatment with P2Y 2 and/or P2Y 4 purinergic receptor agonists. Treatment of vaginal dryness associated with menopause, chemotherapy, and various disease states as well as the treatment of vulvar pain is discussed. Suitable agonists such as UTP, CTP, ATP, dinucleotides and analogs thereof are disclosed.

34. 发明专利

NO20003246L 未知
公开(公告)号：NO20003246L
公开(公告)日：2000-08-23
申请号：NO20003246
申请日：2000-06-21
申请人： INSPIRE PHARMACEUTICALS INC
发明人： LACROIX KAROL K , SHAFFER CHRISTY L , JACOBUS KARLA M , RIDEOUT JANET L , DRUTZ DAVID J , EVANS RICHARD M , PENDERGAST WILLIAM
IPC分类号： A61K9/00 , A61K9/08 , A61K9/72 , A61K31/70 , A61K31/7072 , A61K47/02 , A61P43/00
摘要： Novel pharmaceutical compositions of uridine 5'-triphosphate (UTP) for use in promoting increased mucociliary clearance of retained mucous secretions of the human airways, middle/inner ears or sinuses are disclosed. Novel Formulation I comprises UTP and aqueous solution having a therapeutic concentration between 5 and 45 mg/mL, a controlled tonicity within the range of 250 to 100 mOsM, a pH between 7.0 and 7.5, and is sterile. The pH-adjusted composition is capable of long-term storage in the refrigerated state with a shelf life of up to 30 months. Formulation I may be delivered therapeutically either in a nebulized form or in a liquid form. Novel Formulation II comprises UTP in an aqueous solution or suspension having a therapeutic concentration approaching the limit of UTP's solubility at ambient temperature. This high concentration allows delivery of a therapeutic amount of UTP in very small volumes (50 to 100 mu L) suitable for administration via portable hand-held devices such as metered dose inhalers. Formulation II has extended shelf life without the need for refrigeration after being dispensed to the patient.

35. 发明专利

CA2332540A1 THERAPEUTIC DINUCLEOTIDE AND DERIVATIVES 未知
公开(公告)号：CA2332540A1
公开(公告)日：1999-12-02
申请号：CA2332540
申请日：1999-05-19
申请人： UNIV NORTH CAROLINA , INSPIRE PHARMACEUTICALS INC
发明人： STUTTS MONROE JACKSON , BOUCHER RICHARD C , PICHER MARYSE , RIDEOUT JANET L , YERXA BENJAMIN R , PENDERGAST WILLIAM
IPC分类号： C07H19/10 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7084 , A61P11/00 , A61P11/10 , A61P11/12 , A61P27/04 , A61P27/16 , C07H19/207 , C07H21/00
摘要： The present invention relates to P1-(cytidine 5'-)-P4-(uridine 5'- )tetraphosphates and its salts, esters and amides, and formulations thereof which are highly stable and selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. The compounds of the invention are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, primary ciliary dyskinesia, cystic fibrosis, as well as preventi on of pneumonia due to immobility, and the induction of sputum and its expectoration. Furthermore, because of their general ability to clear retain ed mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis and otitis media. They are also useful in the treatment of dry eye disease and retinal detachment.

37. 发明专利

CA2259552A1 METHOD OF TREATING SINUSITIS WITH URIDINE TRIPHOSPHATES AND RELATED COMPOUNDS 未知
公开(公告)号：CA2259552A1
公开(公告)日：1998-01-29
申请号：CA2259552
申请日：1997-07-03
申请人： INSPIRE PHARMACEUTICALS INC
发明人： PENDERGAST WILLIAM , YERXA BEN , RIDEOUT JANET L , JACOBUS KARLA M , SIDDIQI SUHAIB , DRUTZ DAVID J
IPC分类号： C07H19/067 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61P11/02 , A61P43/00 , C07H19/10 , C07H19/167 , C07H19/20 , A61K31/70
摘要： The invention is the method of treating sinusitis using nucleoside phosphates selected from UTP, ATP, CTP or derivative thereof, or using dinucleoside tetraphosphates of adenosine or uridine.

38. 发明专利

ES2325892T3 METODO PARA TRATAR LA QUERATO CONJUNTIVITIS CON ANTAGONISTAS RECEPTORES PURINERGICOS. 未知
公开(公告)号：ES2325892T3
公开(公告)日：2009-09-23
申请号：ES98907434
申请日：1998-02-06
申请人： INSPIRE PHARMACEUTICALS INC
发明人： YERXA BENJAMIN R , JACOBUS KARLA M , PENDERGAST WILLIAM , RIDEOUT JANET L
IPC分类号： A61K9/00 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/127 , A61K9/14 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/7084 , A61K45/06 , A61K47/02 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/34 , A61K47/36 , A61P27/02 , A61P27/04 , C07H19/10 , C07H19/20 , C07H21/00
摘要： Preparación estéril adaptada para su administración tópica en el ojo, que comprende: - una cantidad efectiva de un compuesto que activa los receptores purinérgicos en tejidos lagrimales, seleccionándose dicho compuesto de un grupo consistente en uridina 5'' trifosfato como se describe en la fórmula I, dinucleótidos como los descritos en las fórmulas II, II(a) y II(b), derivados de adenosina 5''-trifosfato como se describen en la fórmula II y citidina 5''trifosfato como se muestra en la fórmula IV, así como sus análogos y derivados activos, y sus sales farmacológicamente aceptables; y - un vehículo fisiológicamente compatible seleccionado del grupo consistente en soluciones acuosas de electrolito, poliéteres, polivinilos, polímeros de ácido acrílico, lanolina y glucosaminoglicanos; -fomentando dicha preparación la secreción lagrimal de los tejidos lagrimales de un sujeto que precise dicho tratamiento:** ver fórmula** donde: X 1, X 2 y X 3 son independientemente O- o S-, R1 es O, imido, metileno o dihalometileno R2 es H o Br,** ver fórmula** donde X es oxígeno, imido, metileno o difluorometileno; n = 0 o 1; m = 0 o 1; n + m = 0, 1 o 2; y B son B'' independientemente un residuo de purina, como en la fórmula IIa, o un residuo de pirimidina, como en la fórmula IIb, enlazados a través de la posición 9- o 1-, respectivamente: ** ver fórmula** donde: R3 es hidrógeno o NHR, R 1 y R'' de los grupos 8-NHR se seleccionan en el grupo consistente en grupos hidrógeno, arilalquilo (C1-6) en los que el grupo arilo tiene opcionalmente grupos funcionales, alquilo, grupos alquilo con grupos funcionales, omega-A (alquil) CONH(alquil)- y omega-A(alquil) NHCO(alquil)- donde A es amino, mercapto, hidroxi o carboxil; R2 es O o está ausente; o R1 y R2 se toman de un anillo de imidazol en huso de 5 elementos, sustituido opcionalmente en las posiciones 4'' y 5''; donde: R4 es hidroxi, mercapto, amino, ciano, aralcoxi, C1-6 alcoxi, C1-6 alquilamino y dialquilamino, estando opcionalmente los grupos alquilo enlazados para formar un heterociclo; R 5 es hidrógeno, acilo, C 1-6 alquilo, aroilo, C 1-5 alcanoilo, benzoilo, o sulfonato; R6 es hidroxi, amino, mercapto, alcoxi, aralcoxi, C1-6-alquilotio, C1-5 amino disustituido, triazolil, alquilamino o dialquilamino, donde los grupos alquilo están opcionalmente enlazados para formar un heterociclo o están enlazados a N 3 para formar un anillo opcionalmente sustituido; R7 es hidrógeno, hidroxi, ciano, nitro, alquenil, con el grupo alquenil opcionalmente enlazado a través del oxígeno para formar un anillo opcionalmente sustituido en el carbono adyacente al oxígeno con grupos alquilo o arilo, alquinilo sustituido, halógeno, alquilo, alquilo sustituido, perhalometilo, C2-6 alquilo, C2-3 alquenilo o etenilo sustituido; o conjuntamente, R 6-R 7 pueden formar un anillo saturado o insaturado de 5 o 6 elementos enlazado mediante N u O en R 6, pudiendo contener dicho anillo sustitutos que comprenden diversas funciones; siempre que cuando R 8 sea un amino o amino sustituido, R7 es hidrógeno; y R 8 es hidrógeno, alcoxi, arylalcoxi, alquilotio, arilalquilotio, carbozamidometilo, carboximetilo, metoxi, metiltio, fenoxi o feniltío. ** ver fórmula** donde: X1, X2 y X3 se definen como en la fórmula I. R3 y R4 son H mientras que R1 es imido, metileno o diahalometileno, R2 no es nada y hay un doble enlace entre N- 1 y C-6, o R3 y R4 son H mientras que R1 es O, imido, metileno o diahalometileno, R2 es O, y hay un doble enlace entre N-1 y C-6, o R 3, R 4 y R 2 tomados en conjunto son -CH=CH-, formando un anillo desde N-6 a N-1 con un doble enlace entre N- 6 y C-6, y R1 es imido, metileno o diahalometileno; donde: R 1, X 1, X 2 y X 3 se definen como en la fórmula I. R5 y R6 son H mientras que R7 no es nada y existe un doble enlace entre N-3 y C-4, o R5, R6 y R7 tomados en su conjunto son -CH=CH-, formando un anillo desde N-3 a N-4 con un doble enlace entre N-4 y C-4 opcionalmente sustituido en la posición 4- o 5-del anillo eteno.

39. 发明专利

AT428400T 未知
公开(公告)号：AT428400T
公开(公告)日：2009-05-15
申请号：AT98907434
申请日：1998-02-06
申请人： INSPIRE PHARMACEUTICALS INC
发明人： YERXA BENJAMIN , JACOBUS KARLA , PENDERGAST WILLIAM , RIDEOUT JANET
IPC分类号： A61K9/00 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/127 , A61K9/14 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/7084 , A61K45/06 , A61K47/02 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/34 , A61K47/36 , A61P27/02 , A61P27/04 , C07H19/10 , C07H19/20 , C07H21/00
摘要： A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5′-triphosphate (UTP), dinucleotides, cytidine 5′-triphosphate (CTP), adenosine 5′-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.

40. 发明专利

CA2250188C METHOD OF TREATING CILIARY DYSKINESIA WITH URIDINE TRIPHOSPHATES AND RELATED COMPOUNDS 未知
公开(公告)号：CA2250188C
公开(公告)日：2008-12-09
申请号：CA2250188
申请日：1997-03-27
申请人： INSPIRE PHARMACEUTICALS INC , UNIV NORTH CAROLINA
发明人： JACOBUS KARLA M , PENDERGAST WILLIAM , YERXA BENJAMIN R , GEARY CARA A , LAZAROWSKI EDUARDO R , RIDEOUT JANET L , STUTTS MONROE JACKSON III , DRUTZ DAVID J , JAMES MICHAEL K , BOUCHER RICHARD C JR
IPC分类号： A61K31/70 , C07H19/10 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/70 , A61K31/00 , A61K31/505 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/7084 , A61P11/00 , A61P13/00 , A61P15/00 , A61P27/00 , A61P27/02 , A61P27/16 , A61P37/00 , A61P37/04 , C07H19/20 , C07H21/02
摘要： A method of stimulating ciliary beat frequency in a subject in need of such treatment is disclosed. The method comprises administering to the airways, ears, eyes, or genito-urinary tract of the subject a triphosphate nucleotide such as uridine 5'-triphosphate (UTP), an analog of UTP, or any other analog, in an amount effective to stimulate ciliary bea t frequency. This method is useful for treating patients afflicted with ciliary dyskinesia, Kartagener's syndrome, or any other disease involvi ng dysfunction of ciliary movement, such as male infertility caused by impairment of propulsion of the spermatozoa or immune deficiency caused by impairment of ciliary movement in neutrophils or macrophages. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal spray or nasal or eye drops), oral, inhaled by nebulization, topical, injected, suppository, intra-operative by instillation or application, or ex vivo direct applicatio n to spermatozoa.

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