Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions

The present invention relates to substituted xanthines of general formula wherein R 1 to R 4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Peptides derived from human bplp protein, polynucleotides coding for said peptides and antibodies directed against said peptides

The invention relates to an in vitro method for prognosis, diagnosis or determination of the evolution of a condition involving an altered production of Basic Proline-rich Lacrimal Protein (BPLP) or of any of its maturation products, by detecting, or quantifying in a biological sample of a test subject, a BPLP protein or a maturation product thereof, and comparing the production of BPLP protein or maturation product with the production of the same in a biological sample of a control subject

Xanthine derivative, production and use thereof as a medicament

The invention relates to substituted xanthines of general formula (I) wherein R1 - R4 are defined as cited in claim 1, the tautomers, stereoisomers, mixtures, prodrugs and salts thereof which exhibit valuable pharmacological properties, particularly an inhibitory effect on the activity of the dipeptidylpeptidase-IV enzyme.

Hydrochlorides and hydrates of 1-[(3-cyanopyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-aminopiperidin-1-yl)xanthine, their preparation and their use as medicaments

The invention relates to salts of 1-[(3-cyanopyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-aminopiperidin-1-yl]xanthine with hydrochloric acid, and also to their enantiomers, mixtures thereof and hydrates thereof.

Extended recombinant polypeptides and compositions comprising same

The present invention relates to compositions comprising biologically active proteins linked to extended recombinant polypeptide (XTEN), isolated nucleic acids encoding the compositions and vectors and host cells containing the same, and methods of using such compositions in treatment of glucose- related diseases, metabolic diseases, coagulation disorders, and growth hormone-related disorders and conditions.

Growth hormone polypeptides and methods of making and using same

The present invention relates to compositions comprising growth hormone linked to extended recombinant polypeptide (XTEN), isolated nucleic acids encoding the compositions and vectors and host cells containing the same, and methods of making and using such compositions in treatment of growth hormone-related diseases, disorders, and conditions.

크산틴 유도체 및 이의 제조방법

본 발명은 약리학적 특성, 특히 디펩티딜펩티다제-IV 효소의 활성에 대해 억제 효과를 나타내는 화학식 I의 치환된 크산틴, 이의 호변이성체, 입체이성체, 혼합물, 프로드럭 및 염(여기서, R 1 내지 R 4 는 청구의 범위 제1항에서 정의한 바와 같다)에 관한 것이다. 크산틴 유도체, 호변이성체, 입체이성체, DPP-IV, I형 당뇨병, II형 당뇨병

Extended recombinant polypeptides and compositions comprising same

본 발명은 연장된 재조합 폴리펩티드 (XTEN)에 링크된 생물학적 활성 단백질을 포함하는 조성물, 이러한 조성물을 인코드하는 단리된 핵산 그리고 이를 포함하는 벡터 및 숙주 세포, 그리고 포도당-관련된 질병, 대사 질병, 응고 장애, 그리고 성장 호르몬-관련된 장애 및 건강 이상의 치료에 이러한 조성물을 이용하는 방법에 관한 것이다. The present invention relates to a composition comprising a biologically active protein linked to an extended recombinant polypeptide (XTEN), to an isolated nucleic acid encoding said composition, to a vector and host cell comprising the same, to a glucose-related disease, metabolic disease, , And methods of using such compositions for the treatment of growth hormone-related disorders and health disorders.

ANXIETY TREATMENT METHODS

Piperidine derivatives or salts thereof

【課題】カルシウム感知受容体（ＣａＳＲ）が関与する疾患、殊に副甲状腺機能亢進症の治療に用いることができる化合物の提供。【解決手段】3位及び4位の一方がアリールアルキル基等で置換されたアミノメチル基で他方がアリール又はヘテロアリール等で置換されていることを特徴とする新規なピペリジン誘導体またはその塩が優れたＣａＳＲ作動的調節作用を有すること、また、薬物相互作用を起こす懸念のあるＣＹＰ２Ｄ６の阻害作用との選択性に優れていることを見出した。以上のことから、これらの新規なピペリジン誘導体はＣａＳＲが関与する疾患（副甲状腺機能亢進症、腎性骨異栄養症、高カルシウム血症等）の治療剤として有用である。【選択図】なし Disclosed is a compound that can be used for the treatment of diseases involving calcium sensing receptor (CaSR), particularly hyperparathyroidism. A novel piperidine derivative or a salt thereof, wherein one of the 3-position and the 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other is substituted with aryl or heteroaryl, etc. It has been found that it has a CaSR-acting regulatory action and is excellent in selectivity with respect to the inhibitory action of CYP2D6, which may cause drug interaction. Based on the above, these novel piperidine derivatives are useful as therapeutic agents for diseases involving CaSR (hyperparathyroidism, renal osteodystrophy, hypercalcemia, etc.). [Selection figure] None

ALARM TREATMENT METHODS

1. Применение соединения для производства лекарственного препарата для лечения тревоги, где соединение имеет следующую формулу: ! ! где Х представляет собой CH2 или CH2-CH2, ! А представляет собой арил или гетероарил, имеющий 0, 1, 2 или 3 атома, выбранных из группы, состоящей из N, S и О, ! где А имеет 0, 1, 2 или 3 заместителя, независимо выбранных из группы, состоящей из от 0 до 8 атомов углерода, от 0 до 3 атомов кислорода, от 0 до 3 атомов галогена, от 0 до 2 атомов азота, от 0 до 2 атомов серы, а также от 0 до 24 атомов водорода. ! 2. Применение по п.1, где А выбрано из группы, состоящей из пиридинила, тиенила, фурила, хинолинила, метилфенила и бифенила. ! 3. Применение по п.2, где А является незамещенным. !4. Применение по п.2, где тревога ассоциирована с общим тревожным расстройством, обсессивно-компульсивным расстройством, паническим расстройством, фобическим расстройством, острым стрессовым расстройством, посттравматическим стрессовым расстройством или смешанной депрессией, связанной с чувством неполноценности. ! 5. Применение по п.1, где А представляет собой ! ! 6. Применение по п.1, где А представляет собой ! ! 7. Применение по п.1, где А представляет собой ! ! 8. Применение по п.1, где А представляет собой ! ! 9. Применение по п.1, где А представляет собой ! ! 10. Применение по п.1, где А представляет собой ! ! 11. Применение по п.1, где А представляет собой ! ! 12. Применение по п.1, где А представляет собой ! ! 13. Применение по п.1, где А представляет собой РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2010 105 135 (13) A (51) МПК A61K 31/40 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2010105135/15, 08.07.2008 (71) Заявитель(и): Аллерган, Инк. (US) Приоритет(ы): (30) Конвенционный приоритет: 17.07.2007 US 60/950,144 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 17.02.2010 2 0 1 0 1 0 5 1 3 5 (86) Заявка PCT: US 2008/069428 (08.07.2008) (87) Публикация ...

PEPTIDE ANTAGONISTS OF PEPTIDE HORMONES FROM THE CALCITONIN FAMILY (CGRP) AND THEIR APPLICATION

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2017 119 773 A (51) МПК A61K 39/395 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2017119773, 06.06.2017 (71) Заявитель(и): СОАРЕС Кристофер Дж. (US) Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы): СОАРЕС Кристофер Дж. (US) 26.01.2012 US 61/591,236 34 Адрес для переписки: 190000, Санкт-Петербург, BOX-1125, "ПАТЕНТИКА" A 2 0 1 7 1 1 9 7 7 3 Y1 выбран из группы, состоящей из Val-Leu-Gly-Arg-Leu-Ser-Gln-Glu-Leu-His-Arg-LeuGln-Thr-Tyr-Pro-Thr-Asn (SEQ ID NO: 59), Val-Leu-Gly-Arg-Leu-Ser-Gln-Glu-Leu-His-ArgLeu-Gln-Thr-Tyr-Pro-Val-Asp (SEQ ID NO: 60) и Val-Thr-His-Arg-Leu-Ala-Gly-Leu-Leu-SerArg-Ser-Gly-Gly-Val-Val-Lys-Asn-Asn-Phe-Val-Pro-Thr-Asn (SEQ ID NO: 61); и где: Z1 выбран из группы, состоящей из Thr-Gly-Ser-Gly-Thr-Pro-NH2 (SEQ ID NO: 62), ProSer-Ser-Pro-His-Ser-Tyr-NH2 (SEQ ID NO: 63) и Val-Gly-Ser-Lys-Ala-Phe-NH2 (SEQ ID NO: 46). Стр.: 1 A X1 является модифицированным N-концевым фрагментом связанного с геном кальцитонина пептида, содержащим от пяти до семи остатков аминокислот, где две аминокислоты указанного N-концевого фрагмента представляют собой остатки цистеина (Cys), при этом C-концевой остаток аминокислоты N-концевого фрагмента является цистеином (Cys), при этом остаток, расположенный непосредственно перед C-концевым остатком Cys указанного N-концевого фрагмента, является заменой остатка треонина (Thr) на не треонин, причем два остатка цистеина разделены четырьмя, пятью или шестью аминокислотами и при этом указанные два остатка цистеина могут образовывать дисульфидную связь; R U (57) Формула изобретения 1. Антагонист на основе связанного с геном кальцитонина пептида или его фармацевтически приемлемая соль, причем указанный антагонист имеет структуру согласно формуле I: 2 0 1 7 1 1 9 7 7 3 (54) ПЕПТИДНЫЕ АНТАГОНИСТЫ ПЕПТИДНЫХ ГОРМОНОВ ИЗ СЕМЕЙСТВА КАЛЬЦИТОНИНА (CGRP) И ИХ ПРИМЕНЕНИЕ R U (43) Дата публикации заявки: 06.12.2018 Бюл. № 2 0 1 7 1 1 9 ...

Peptides derived from human BPLP protein, polynucleotides coding for said peptides and antibodies directed against said peptides

Calcium receptor modulating agents

The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Naphthalene-containing cyclic hydrocarbon compounds for the treatment of disturbances of calcium sensor receptor activity

Calcium receptor active molecules

Method and composition useful for treating a patient having a disease characterized by an abnormal level of one or more components, the activity of which is regulated or affected by activity of one or more Ca 2+ receptors. Novel compounds useful in these methods and compositions are also provided. The method includes administering to the patient a therapeutically effective amount of a molecule active at one or more Ca 2+ receptors as an agonist or antagonist. Preferably, the molecule is able to act as either a selective agonist or antagonist at a Ca 2+ receptor of one or more but not all cells chosen from the group consisting of parathyroid cells, bone osteoclasts, juxtaglomerular kidney cells, proximal tubule kidney cells, keratinocytes, parafollicular thyroid cells and placental throphoblasts and a pharmaceutically acceptable carrier.

Calcium receptor activating molecule

NOVEL ARALKYL-1,2-DIAMINES HAVING CALCIMIMETIC ACTIVITY AND THEIR METHOD OF PREPARATION

Arylalkylamines, compositions, methods of treatment and diagnosis, method of identification of compound

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to a compound, methods and composition used for treatment of patients suffering with diseases that are characterized by anomal level of one or more components regulating or depending on one or more Ca 2+ -receptors. New compounds for these methods and compositions are developed also. Method involves administration to patient molecules at effective amount acting on one or more Ca 2+ -receptors and showing affinity to these receptors or exhibiting antagonistic properties. Preferably, molecule is able to act as a substance showing affinity or as antagonist to Ca 2+ -receptors of one or more but not all cell types taken among the group consisting of parathyroid cells, osseous osteoclasts, juxtaglomerular renal cells, cells of proximal transverse tubule, keratinocytes, thyroid parafollicular cells and placenta trophoblasts. Compositions have also a pharmaceutically acceptable carrier. EFFECT: specificity of effect of compounds, compositions and methods based on thereof. 65 cl, 6 tbl, 98 dwg, 23 ex УУСС ПЧ Го (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (51) МПК? 13) ВИ” 2 147 574 Сл А 61 К 31/135, С 01 М 33/84 С 07 С 211/46, 211/17, 241/19, 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 94020394/14, 21.08.1992 (24) Дата начала действия патента: 21.08.1992 (30) Приоритет: 23.08.1991 Ш$ 07/749.451 11.02.1992 1$ 07/834.044 (46) Дата публикации: 20.04.2000 (56) Ссылки: Гагззоп, ВюсИит. её Вюрпу$. Ас, 1985, 847, р.263-269 ВКОМИМ её а|, Епадосгто]оду, 1991, р.3047. $Ц 455944 А, 05.01.75. 4$ 4988730 А, 29.01.91. 4$ 4980354 А, 25.12.90. (85) Дата перевода заявки РСТ на национальную фазу: 22.02.1994 (86) Заявка РСТ: 1$ 9207175 (21.08.1992) (87) Публикация РСТ: М/О 9304373 (04.03.1993) (98) Адрес для переписки: 103735, Москва, ул.Ильинка, 5/2, Союзпатент (71) Заявитель: Эн-Пи-Эс Фармасьютикалз, Инк. (ЦЗ) (72) Изобретатель: Эдвард Ф.Немет (ЦЭ), Брэдфорд К.Ван Вейгенен ( ...

The purposes of the peptide antagonists and they of the calcitonin C GRP families of peptide hormone

实施方式提供修饰的降钙素基因‑相关的肽拮抗剂，其包括修饰的降钙素基因‑相关的肽或相关的蛋白家族成员的N‑端片段，其中N‑端片段的至少2个残基是半胱氨酸(Cys)，至少一个氨基酸包含苏氨酸(Thr)残基的非‑苏氨酸取代；中央核心，其中中央核心包含α‑螺旋；及修饰的降钙素基因‑相关的肽或包含C‑端酰胺的相关的蛋白家族成员的C‑端片段，且其中C‑端片段的至少一个氨基酸是苯丙氨酸(Phe)，脯氨酸(Pro)，酪氨酸(Tyr)或羟脯氨酸(Hyp)或其药学可接受的盐，以及组合物，包括药物组合物，其包含受试肽。实施方式还提供治疗方法，包括治疗偏头痛的方法，所述方法通常涉及给有需求的个体施用有效量的受试肽或组合物。

ANTAGONIST ANTIBODIES DIRECTED AGAINST THE CALCITONIN GENE-RELATED PEPTIDE AND METHODS USING THE SAME

La invencion presenta una composicion farmaceutica que comprende un anticuerpo monoclonal que inhibe la via del peptido relacionado con el gen de la calcitonina (CGRP) y un excipiente farmaceuticamente aceptable, en la que el anticuerpo monoclonal comprende una cadena pesada con la secuencia de aminoacidos segun la SEQ ID NO: 11 y una cadena ligera con la secuencia de aminoacidos segun la SEQ ID NO: 12, en la que la composicion es una composicion subcutanea. La composicion esta contenida en una jeringa precargada y el anticuerpo monoclonal esta formulado a una concentracion de al menos 150 mg/mL. Dicha composicion es util para prevenir o tratar trastornos asociados con CGRP tal como sintomas vasomotores y/o dolores de cabeza (por ejemplo, migrana, dolor de cabeza en racimos, y el dolor de cabeza por tension). The invention presents a pharmaceutical composition comprising a monoclonal antibody that inhibits the calcitonin gene-related peptide pathway (CGRP) and a pharmaceutically acceptable excipient, in which the monoclonal antibody comprises a heavy chain with the sequence of amino acids according to the SEQ ID NO: 11 and a light chain with the amino acid sequence according to SEQ ID NO: 12, in which the composition is a subcutaneous composition. The composition is contained in a prefilled syringe and the monoclonal antibody is formulated at a concentration of at least 150 mg/mL. Said composition is useful for preventing or treating disorders associated with CGRP such as vasomotor symptoms and/or headaches (eg, migraine, cluster headache, and tension headache).

Novel cyclic hydrocarbon compounds for treatment of diseases

FIELD: medicine, pharmaceutics. SUBSTANCE: invention relates to novel cyclic compounds of general formula which possess properties of CaSR modulator. In general formula I group represents cycloalkyl, which contains 4-7 carbon atoms, optionally substituted with one or several similar or different substituents, selected from R 2 , R 3 , R 4 or R 5 ; A represents 1-naphthyl; R 1 represents methyl, ethyl or n-propyl, each of which is optionally substituted with one or several, similar or different substituents, selected from halogen and hydroxy; R 2 and R 3 represent hydrogen; R 4 represents hydrogen, halogen, hydroxy or C 1-6 alkyl; each R 5 represents independently one or several similar or different substituents, represented by hydrogen or C 1-6 alkyl; G represents -C(O)NH 2 , C 3-8 cycloalkyl, C 1-6 heterocycloalkyl, C 1-6 heterocycloalkenyl, C 3-8 cycloalkenyl, C 6-14 aryl, C 1-10 heteroaryl, C 6-10 arylamino, hydroxyaminocarbonyl, C 6-10 arylaminocarbonyl, C 1-4 aminocarbonyl, C 1-6 heterocycloalkylcarbonyl, C 1-10 heteroarylaminocarbonyl, C 6-10 arylsulfonylaminocarbonyl, C 6-14 aryloxy, or C 1-4 alkoxycarbonyl, where said substituents are optionally additionally substituted with one or several, similar or different substituents. Other values of radicals are given in the formula of invention. EFFECT: compounds can be applied in treatment, relief or prevention of physiological disorders or diseases, associated with impairment of activity of CaSR, such as hyperparathyreosis, and other diseases. 23 cl, 9 dwg, 3 tbl, 315 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 211/35 C07C 211/36 C07C 211/48 C07C 215/28 C07C 217/52 C07C 217/74 ФЕДЕРАЛЬНАЯ СЛУЖБА C07C 233/05 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07C 233/41 C07C 237/24 C07C 237/30 (12) ОПИСАНИЕ (21)(22) Заявка: (13) 2 524 949 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) C07C C07C C07C C07C C07C C07D C07D A61K A61K A61K C2 237/32 (2006.01) 237/34 (2006.01) ...

Antagonist antibodies directed against calcitonin gene-related peptide and methods using same

본 발명은 항-CGRP 길항제 항체 투여에 의해 CGRP 관련된 장애 예컨대 혈관운동 증상 및/또는 두통 (예를 들면, 편두통, 군발성 두통, 및 긴장성 두통)의 예방 또는 치료 방법을 특징으로 한다. 개시된 방법에서 사용하기 위한 조성물이 또한 제공된다. 길항제 항체 G1 및 CGRP에 관련된 G1로부터 유도된 항체가 또한 기재된다.

Peptide antagonists of the calcitonin cgrp family of peptide hormones and their use

본 구현예는 변형된 칼시토닌 유전자-관련된 펩타이드 또는 관련된 단백질 패밀리 멤버의 N-말단 단편으로서, 여기서 상기 N-말단 단편의 적어도 2 개의 잔기는 시스테인 (Cys)이고 적어도 하나의 아미노산은 트레오닌 (Thr) 잔기의 비-트레오닌 치환을 포함하는N-말단 단편; α-나선을 포함하는 중앙 코어; 및 변형된 칼시토닌 유전자-관련된 펩타이드 또는 C-말단 아마이드를 포함하는 관련된 단백질 패밀리 멤버의 C-말단 단편으로서, 여기서 상기 C-말단 단편의 적어도 하나의 아미노산은 페닐알라닌 (Phe), 프롤린 (Pro), 티로신 (Tyr) 또는 하이드록시프롤린 (Hyp)인C-말단 단편을 포함하는 변형된 칼시토닌 유전자-관련된 펩타이드 길항제 또는 그의 약제학적으로 허용가능한 염, 뿐만 아니라 대상 펩타이드를 포함하는 약제학적 조성물을 제공한다. 본 구현예는 추가로, 편두통을 치료하는 방법을 포함하는 치료 방법을 제공하고, 상기 방법은 일반적으로 치료가 필요한 개체에게 효과적인 양의 대상 펩타이드 또는 조성물을 투여하는 것을 수반한다. This embodiment is an N-terminal fragment of a modified calcitonin gene-related peptide or related protein family member, wherein at least two residues of the N-terminal fragment are cysteine (Cys) and at least one amino acid is a threonine (Thr) residue An N-terminal fragment comprising a non-threonine substitution of; a central core comprising a-helix; And a C-terminal fragment of a related protein family member comprising a modified calcitonin gene-related peptide or C-terminal amide, wherein at least one amino acid of the C-terminal fragment is phenylalanine (Phe), proline (Pro), tyrosine A modified calcitonin gene-related peptide antagonist or a pharmaceutically acceptable salt thereof comprising a C-terminal fragment that is (Tyr) or hydroxyproline (Hyp), as well as a pharmaceutical composition comprising a peptide of interest. This embodiment further provides a method of treatment comprising a method of treating migraine headaches, which generally involves administering an effective amount of a subject peptide or composition to a subject in need thereof.

Oral Peptide Pharmaceutical Compositions

경구로 투여되는 펩티드 활성제의 생체이용률은 본 발명의 성분들을 위를 통해서 이송하는 내산성 보호 부형제의 덕택으로 장에 펩티드의 목표 방출을 제공하는 약학적 조성물에 의해서 강화된다. 조성물은 흡수 증강제 및 국소적 장의 pH를 낮추기에 충분한 양의 pH 강하제를 포함한다. 모든 성분들은 펩티드와 함께 장애 같이 방출된다. Bioavailability of orally administered peptide actives is enhanced by pharmaceutical compositions that provide the desired release of peptides into the intestines thanks to acid resistant protective excipients that deliver the components of the present invention through the stomach. The composition includes an absorption enhancer and a pH lowering agent in an amount sufficient to lower the pH of the local intestine. All components are released as disorders with the peptide.

Pharmaceutical composition for oral delivery of physiologically active peptide agent and method of enhancement of its availability

FIELD: medicine, pharmacy. SUBSTANCE: composition comprises therapeutically effective amount of peptide, pharmaceutically acceptable pH- reducing agent, absorption enhancer showing effectiveness for enhancement of bioavailability of indicated peptide and acid-stable protective vehicle. Indicated vehicle promotes to transport of pharmaceutical composition through patient stomach and prevents contact of peptide with gastric proteases. The use of the novel pharmaceutical composition provides oral administration of peptide to patient and selective directed release of indicated peptide in intestine. Proteolytic cleavage of peptide by gastric, intestine and pancreatic proteases is reduced. The improved bioavailability of peptide allows to maintain its concentration in pharmaceutical preparation at relatively low level. EFFECT: improved method of bioavailability of peptide. 20 cl, 9 tbl па (19) 13) ВО” 2 198 677” С2 ОМК А бл К 38/00, 9/52, 9/62, 9/28, 9/30, 9/36, 9/50, А 61 Р 19/08, 19/10 РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 98118692/14, 14.03.1997 (71) Заявитель: ЮНИДЖЕН ЛЭБОРЕТЕРИЗ, ИНК. (45) (24) Дата начала действия патента: 14.03.1997 (72) Изобретатель: СТЕРН Уильям (13), (30) Приоритет: 15.03.1996 Ш$ 08/616,250 ДЖИЛЛИГАН Джеймс П. (4$) (43) Дата публикации заявки: 20.08.2000 (73) Патентообладатель: ЮНИДЖЕН ЛЭБОРЕТЕРИЗ, ИНК. (45$) сч (46) Дата публикации: 20.02.2003 о (74) Патентный поверенный: (56) Ссылки: 4$ 5206219 А, 27.04.1993. 4$ 5350741 Егорова Галина Борисовна А, 27.09.1994. 4$ 5472710 А, 05.12.1995. МАШКОВСКИЙ М.Д. Лекарственные средства. - К М.: Медицина, 1986, ч.1, с.549-550. — (85) Дата перевода заявки РСТ на национальную фазу: 15.10.1998 < (86) Заявка РСТ: со 1$ 97/04024 (14.03.1997) © (87) Публикация РСТ: = М/О 97/33531 (18.09.1997) Сс' (98) Адрес для переписки: 129010, Москва, ул. Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и — Партнеры", пат.пов. Н.Г. ...

Patent RU2017119773A3

7 ВУ’? 2017119773” АЗ Дата публикации: 18.11.2020 Форма № 18 ИЗПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2017119773/10(034357) 06.06.2017 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 61/591,236 26.01.2012 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) ПЕПТИДНЫЕ АНТАГОНИСТЫ ПЕПТИДНЫХ ГОРМОНОВ ИЗ СЕМЕЙСТВА КАЛЬЦИТОНИНА (СОВР) И ИХ ПРИМЕНЕНИЕ Заявитель: СОАРЕС Кристофер Дж., 05 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) С07К 14/585 (2006.01) Аб1К 365/22 (2006.01) Аб1Р 25/06 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) СО7К 14/585, Аб1К 38/22, Аб1Р 25/06 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): Е-Габгагу, Езрасепев, Раеагсв, РАТЕМТСОРЕ, КУРТО, МСВТ, ЕМВГ-ЕВ1, Соозе, Сооз]е эсБо][аг, РиИБМеа, ОЗРТО, Заепсе ес 6. ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ПРЕДМЕТУ ПОИСКА Кате- Наименование ...

Peptides derived from human BPLP protein, polynucleotides coding for said peptides and antibodies directed against said peptides

本发明涉及一种肽，所述肽是碱性富脯氨酸泪液蛋白(BPLP)的成熟产物或所述成熟产物的肽衍生物或模拟物，其中所述肽或其肽衍生物或模拟物表现出对金属外肽酶(特别是NEP和/或APN)的抑制性能。本发明也涉及编码所述肽的多核苷酸以及涉及针对所述肽的抗体。此外，本发明涉及人BPLP蛋白及其所衍生的抑制肽、编码人BPLP蛋白或其所衍生的肽的多核苷酸以及针对BPLP蛋白或其所衍生的肽的抗体的诊断性及治疗性的用途。

8-(3-amino-piperidin-1-yl)-xanthines, their preparation, and their use as pharmaceuticals

The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.

8-(3-amino-piperidin-1-yl)-xanthines, their preparation, and their use as pharmaceuticals

The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.

PEPTIDE ANTAGONISTS OF PEPTIDE HORMONES FROM THE CALCITONIN FAMILY (CGRP) AND THEIR APPLICATION

1. Антагонист на основе модифицированного связанного с геном кальцитонина пептида, причем указанный антагонист имеет структуру согласно формуле I:где Xявляется модифицированным N-концевым фрагментом связанного с геном кальцитонина пептида или другого члена семейства пептидов CT/CGRP, содержащим от пяти до семи остатков аминокислот, где два остатка аминокислот указанного N-концевого фрагмента являются цистеином (Cys), С-концевой остаток является Cys, а остаток, расположенный непосредственно перед С-концевым остатком Cys указанного фрагмента, является заменой остатка треонина (Thr) на не треонин;Yявляется центральной структурой, причем по меньшей мере одна аминокислота указанной центральной структуры является аргинином (Arg) или лизином (Lys), и указанная центральная структура содержит α-спираль; иZявляется модифицированным С-концевым фрагментом связанного с геном кальцитонина пептида или другого члена семейства пептидов CT/CGRP, содержащим от пяти до семи остатков аминокислот с С-концевым амидом, причем по меньшей мере один остаток аминокислот указанного С-концевого фрагмента является фенилаланином (Phe), тирозином (Tyr), пролином (Pro) или гидроксипролином (Hyp);или его фармацевтически приемлемая соль.2. Антагонист по п. 1, отличающийся тем, что Yявляется центральной структурой из 15-22 остатков.3. Антагонист по п. 1, отличающийся тем, что N-концевой фрагмент содержит:Х-Х-Х-Х-Х-Х-Х(SEQ ID №: 16),где Xвыбран из группы, состоящей из аланина (Ala), цистеина (Cys), глицина (Gly), изолейцина (Ile), лейцина (Leu), метионина (Met), фенилаланина (Phe), пролина (Pro), триптофана (Trp) и валина (Val);Xвыбран из группы, состоящей из цистеина (Cys), серина (Ser) и тирозина (Tyr);Xвыбран из группы, состоящей из аргинина (Arg), аспарагина (Asn), аспарагиновой кислоты (Asp), цистеина (Cys), глутаминовой ки РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07K 14/585 (13) 2014 131 605 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) ...

Extended recombinant polypeptides and compositions comprising same

Xanthine derivative, production and use thereof as a medicament

8- (3-amino-piperidin-1-yl) -xanthines, their preparation and their use as pharmaceuticals

Die Erfindung betrifft neue 8-[3-Amino-piperidin-1-yl]-xanthine und deren physiologisch verträgliche Salze, insbesondere deren Hydrochloride. The invention relates to novel 8- [3-amino-piperidin-1-yl] xanthines and their physiologically tolerated salts, in particular their hydrochlorides.

Novel cyclic hydrocarbon compounds for the treatment of diseases

本发明涉及新的环烃化合物及其衍生物、其制备方法，涉及所述化合物作为药物的用途，涉及所述化合物在治疗中的用途，涉及含有所述化合物的药用组合物，涉及采用所述化合物治疗疾病的方法，涉及所述化合物在生产药物中的用途。

Medicinal forms on basis of biphosphonates

FIELD: medicine, pharmaceutics. ^ SUBSTANCE: invention concerns medicine area, namely to peroral medicinal forms on a basis of biphosphonates, containing safe and effective quantity of the pharmaceutical composition containing biphosphonate, chelated agent and an agent for effective delivery of a pharmaceutical composition in the bottom gastroenteric tract of a mammal, and also pharmaceutically active biphosphonate absorption together with nutrition or drinks or without them. The present invention essentially reduces interaction between biphosphonates and nutrition or a drink, which (interaction) leads to that active biphosphonate component is not accessible to absorption. The final peroral medicinal form can be accepted both with food, and without it. Further, the present invention influences delivery biphosphonate and chelated agent in a bottom of GI tract, essentially reducing irritation of top of the GI tract, bound with biphosphonate therapy. ^ EFFECT: maintenance of fuller observance with the patient of a regimen biphosphonate therapy. ^ 23 cl, 20 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 359 678 (13) C2 (51) МПК A61K 31/66 (2006.01) A61K 9/22 (2006.01) A61K 9/52 (2006.01) A61K 47/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21), (22) Заявка: 2006140888/15, 14.04.2005 (24) Дата начала отсчета срока действия патента: 14.04.2005 (72) Автор(ы): ДАНСЕРО Ричард Джон (US), БЕРДЖИО Дэвид Эрнест мл. (US) (43) Дата публикации заявки: 27.06.2008 2 3 5 9 6 7 8 (45) Опубликовано: 27.06.2009 Бюл. № 18 (56) Список документов, цитированных в отчете о поиске: WO 97/44017 А1, 27.11.1997. WO 00/61111 А, 19.10.2000. US 5462932 А, 31.10.1995. WO 93/09785 А, 27.05.1993. US 5431920 А, 11.07.1995. US 6676965 В1, 13.01.2004. WO 01/32185 А, 10.05.2001. 2 3 5 9 6 7 8 R U (86) Заявка PCT: US 2005/012537 (14.04.2005) C 2 C 2 (85) Дата перевода заявки PCT на национальную фазу: 25.12.2006 (87) Публикация PCT ...

Growth hormone polypeptides and its preparation and application

本发明涉及包含与延伸的重组多肽(XTEN)连接的生长激素的组合物、编码所述组合物的分离的核酸和含有所述分离的核酸的载体和宿主细胞，以及制备所述组合物的方法和使用所述组合物治疗生长激素相关疾病、疾患和病症的方法。

Enteric solid oral dosage form of bisphosphonate containing a chelating agent

비스포스포네이트와, 킬레이팅제와, 하부 위장관에서 비스포스포네이트 및 킬레이팅제의 방출을 지연시키기 위한 수단을 포함하는 안전하고 유효한 양의 약학 조성물로 이루어진 비스포스포네이트의 경구 투여 형태는 약학 조성물을 포유류 대상의 하부 위장관에 전달하고 음식 또는 음료와 함께 또는 이들 없이 비스포스포네이트가 약학적으로 효과적으로 흡수되게 한다. 본 발명은 비스포스포네이트와 음식 또는 음료 사이의 상호 작용을 실질적으로 경감시키는데, 이 상호 작용은 비스포스포네이트 활성 성분이 흡수되지 않게 한다. 따라서 생성된 경구 투여 형태는 음식과 함께 또는 음식 없이 복용될 수 있다. 또한, 본 발명은 비스포스포네이트 및 킬레이팅제가 하부 GI 관으로 전달되게 하여, 비스포스포네이트 치료법과 관련된 상부 GI 자극을 실질적으로 경감시킨다. 이들 효과는 이전의 복잡한 치료 섭생법을 단순화하며, 비스포스포네이트 치료법에 대한 환자의 순응도를 증가시킬 수 있다.

Calcilytic compounds

Novel calcilytic compounds and methods of using them are provided.

Methods of treating anxiety

Предложен способ лечения тревоги с помощью введения пациенту, нуждающемуся в таком лечении, соединения, имеющего формулу, выбранную из нижеприведенных (варианты) или его фармацевтически приемлемой соли. Показано значительное (по сравнению с диазепамом и буспироном) снижение тревожности у животных через 60 мин после введения заявленных соединений. 2 н. и 1 з.п. ф-лы, 1 табл. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 491 931 (13) C2 (51) МПК A61K A61K A61K A61K A61K A61P 31/402 (2006.01) 31/4025 (2006.01) 31/4436 (2006.01) 31/4439 (2006.01) 31/444 (2006.01) 5/22 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2010105135/15, 08.07.2008 (24) Дата начала отсчета срока действия патента: 08.07.2008 (72) Автор(ы): ДОНЕЛЛО Джон Е. (US), ЛУРС Лорен М.Б. (US) (73) Патентообладатель(и): Аллерган, Инк. (US) R U Приоритет(ы): (30) Конвенционный приоритет: 17.07.2007 US 60/950,144 (43) Дата публикации заявки: 27.08.2011 Бюл. № 24 C 2 2 4 9 1 9 3 1 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 17.02.2010 (86) Заявка PCT: US 2008/069428 (08.07.2008) R U C 2 (56) Список документов, цитированных в отчете о поиске: RU 2246300 С2, 20.02.2005. US 20070072857 A1, 29.03.2007. WO 2006/081252 A2, 30.08.2006. WO 2006/081273 A1, 03.08.2006. WO 03/045928 A1, 05.06.2003. WALF A.A. et al. The use of the elevated plus maze as an assay of anxiety-related behavior in rodents. Nat. protoc. 2007; 2(2):322-8 [онлайн] [найдено 2012-05-18] (Найдено из базы данных PubMed PMID: 17406592). (54) СПОСОБЫ ЛЕЧЕНИЯ ТРЕВОГИ (87) Публикация заявки РСТ: WO 2009/012082 (22.01.2009) Адрес для переписки: 191002, Санкт-Петербург, а/я 5, ООО "Ляпунов и партнеры", пат.пов. Е.Г.Ильмеру, рег.№ 1144 (57) Реферат: Предложен способ лечения тревоги с помощью введения пациенту, нуждающемуся в таком лечении, соединения, имеющего формулу, выбранную из нижеприведенных (варианты) или его фармацевтически приемлемой соли. Показано значительное (по ...

Extended recombinant polypeptides and compositions comprising the same

【課題】生物活性タンパク質の生物学的、薬学的、安全性および／または治療特性を増強するのに有用であり得る組成物および方法を提供すること。【解決手段】本発明は、延長組換えポリペプチド（ＸＴＥＮ）に連結された生物活性タンパク質を含む組成物、組成物をコードする単離核酸ならびにそれを含有するベクターおよび宿主細胞、ならびにグルコース関連疾患、代謝性疾患、凝固障害、ならびに成長ホルモン関連障害および症状の処置におけるこのような組成物の使用方法に関するものである。一態様において、本発明は延長組換えポリペプチド（ＸＴＥＮ）の組成物を提供し、該組成物は生物活性タンパク質に連結されたときに、得られた融合タンパク質の薬物動態特性を増強し、ならびに／または得られた融合タンパク質の溶解性および安定性を増加させて、一方では生物活性タンパク質の全体的な生物学的活性および／または治療活性を増強する。【選択図】なし

Peptide antagonists of calcitonin cgrp family of peptide hormones and their use

FIELD: biotechnology. SUBSTANCE: invention relates to peptide antagonists of calcitonin gene-associated peptide (CGRP), and can be used in medicine for treating a condition associated with high CGRP, including migraine. Disclosed is a peptide having the structure X 1 -Y 1 -Z 1 , where X 1 is a modified N-terminal CGRP fragment containing from 5 to 7 amino acid residues, where 2 amino acids of said N-terminal fragment are cysteine residues (Cys), wherein the C-terminal amino acid residue of the N-terminal fragment is Cys, residue immediately before C-terminal Cys residue of said N-terminal fragment is a substitution of a residue of threonine (Thr) by nethreonine, wherein two cysteine residues are separated by 4, 5 or 6 amino acids and wherein said 2 Cys residues can form a disulphide bond; Y 1 is selected from Val-Leu-Gly-Arg-Leu-Ser-Gln-Glu-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Thr-Asn, Val-Leu-Gly-Arg-Leu-Ser-Gln-Glu-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Val-Asp; and Z 1 is selected from Thr-Gly-Ser-Gly-Thr-Pro-NH 2 , Pro-Ser-Ser-Pro-His-Ser-Tyr-NH 2 or Val-Gly-Ser-Lys-Ala-Phe-NH 2 . EFFECT: invention provides preparing an effective CGRP antagonist. 13 cl, 7 tbl, 1 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 742 826 C2 (51) МПК C07K 14/585 (2006.01) A61K 38/22 (2006.01) A61P 25/06 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК A61K 38/225 (2020.08); A61K 38/23 (2020.08); A61P 25/06 (2020.08); A61P 5/22 (2020.08); C07K 14/57527 (2020.08); C07K 14/585 (2020.08) (21)(22) Заявка: 2017119773, 06.06.2017 25.01.2013 (73) Патентообладатель(и): СОАРЕС Кристофер Дж. (US) Дата регистрации: 11.02.2021 26.01.2012 US 61/591,236 Номер и дата приоритета первоначальной заявки, из которой данная заявка выделена: 2014131605 25.01.2013 (43) Дата публикации заявки: 06.12.2018 Бюл. № 34 2 7 4 2 8 2 6 R U Адрес для переписки: 190000, Санкт-Петербург, BOX-1125, "ПАТЕНТИКА" C 2 C 2 (45) Опубликовано: 11.02.2021 Бюл. № 5 2 7 4 2 8 2 6 ...

MICROPARTICLES FOR PULMONARY ADMINISTRATION

NOVEL ARALKYL-1,2-DIAMINES HAVING CALCIMIMETIC ACTIVITY AND THEIR METHOD OF PREPARATION

The invention concerns compounds of general formula (I) wherein: X represents a SO2 or CH2 group; R1 represents a hydrogen or halogen atom or an alkoxy, aryl aralkyl group or an alkyl group substituted or not with one or several halogen atoms, n is equal to 0, 1 or 2, and R2 represents a hydrogen or halogen atom or an alkyl or alkoxy group, and their salt with a pharmaceutically acceptable acid. The invention also concerns the method for preparing said compounds, pharmaceutical compositions containing them and their use as modulator of CaSR activity and as medicine particularly designed for treating diseases or physiological disorders involving modulation of CaSR activity.

Medicinal compositions for application to mucosa

Pharmaceutical composition applicable to mucous membrane

The present invention prelates to a pharmaceutical composition for application to the mucosa to be used in medicament therapy comprising one or several water-insoluble and/or water-low soluble substances and one or several medicaments, and an aqueous medium, and having an osmotic pressure equal to or less than 150 mOsm. This composition is superior over conventional pharmaceutical compositions for application to the mucosa, due to efficient and high permeability to the blood at the mucosa. The present invention further provides another pharmaceutical composition suitable for application to the mucosa comprising one or several haemostatic agents and one or several water-insoluble and/or water-low soluble substances, and one or several medicaments. This composition is superior over conventional pharmaceutical compositions for application to the mucosa, due to permeability and retentivity at the mucosa wherein osmotic pressure thereof equals to or is less than 150 mOsm.

Microcapsules for sustained release of drug

(57)【要約】 薬剤のゆっくりした放出のためのマイクロカプセルであって、可塑剤が添加された乳酸−グリコール酸コポリマーから成り、薬剤的に重要な薬剤を内部に含むマイクロカプセル。

Calcilytic compounds

Hydrochlorides and hydrates of 1 - [(3-cyano-pyridin-2-yl) methyl] -3methyl-7- (2-butyn-1-yl) -8- (3-amino-piperidin-1-yl) -xanthine , its manufacture and its use as pharmaceuticals

Medicinal compositions for application to mucosa

Xantine derivatives, preparation and use thereof as a medicament

Oxadiazole compounds and compositions for delivering active agents

Oxadiazole compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Amylin family peptides and methods for making and using them

Provided is a specified amylin family peptide and its variants as well as their use in the manufacture of medicaments for treating eating disorders, diabetes, cardiovascular diseases and other diseases. (62) Divided Out of 549332

Peptide antagonists of peptide hormones from the calcitonin group (calcitonin gene-related peptides (cgrp)) and their application

FIELD: biotechnology. SUBSTANCE: invention relates to peptide antagonists of calcitonin gene-related peptide (CGRP), and can be used in medicine for treatment of a condition associated with elevated levels of CGRP, including migraine. A peptide with a structure X 1 - Y 1 - Z 1 structure is proposed, where X 1 has the X 11 -X 12 -X 13 -X 14 -X 15 -X 16 -X 17 structure (SEQ ID #16), where X 17 is Cys, where X 11 is selected from the group consisting of Ala, Cys and Gly, and where X 12 is selected from the group consisting of Cys and Ser, provided that one of X 11 or X 12 is Cys, where X 13 is selected from the group consisting of Arg, Asn, Asp and Val, where X 14 is selected from the group consisting of Leu, Phe and Thr, where X 15 is selected from the group consisting of Ala, Gly and Ser, where X 16 is selected from the group consisting of Ala, Ile, Leu, Ser, and Val. At that, Y 1 is Val-Leu-Gly-Arg-Leu-Ser-Gln-Glu-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn- (SEQ ID #34); and Z 1 is Val-Gly-Ser-Lys-Ala-Phe-NH 2 (SEQ ID #46). EFFECT: obtaining of an effective antagonist for CGRP. 23 cl, 7 tbl, 1 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 624 016 C2 (51) МПК C07K 14/585 (2006.01) A61K 38/22 (2006.01) A61P 25/06 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ФОРМУЛА (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ 2014131605, 25.01.2013 (24) Дата начала отсчета срока действия патента: 25.01.2013 (72) Автор(ы): СОАРЕС Кристофер Дж. (US) (73) Патентообладатель(и): СОАРЕС Кристофер Дж. (US) Дата регистрации: (56) Список документов, цитированных в отчете о поиске: WO 2006105527 A2, 05.10.2006. RU Приоритет(ы): (30) Конвенционный приоритет: 26.01.2012 US 61/591,236 (45) Опубликовано: 30.06.2017 Бюл. № 19 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 26.08.2014 (86) Заявка PCT: US 2013/023260 (25.01.2013) (87) Публикация заявки PCT: 2 6 2 4 0 1 6 (43) Дата публикации заявки: 20.03.2016 Бюл. № 8 2385878 C2, 10.04.2010. TAYLOR ...

Medicinal preparations for use on mucous membranes

Oral peptide drugs

Xanthine derivatives, their preparation and their use as pharmaceuticals

8-(3-amino-piperidin-1-yl)-xanthines, their preparation and their use as pharmacon

Xanthin derivatives, their production and utilisation as medicine

The invention relates to substituted xanthines of general formula (I), wherein R1-R4 are defined as cited in claim 1, the tautomers, stereoisomers, mixtures, prodrugs and salts thereof which exhibit valuable pharmacological properties, particularly an inhibitory effect on the activity of the dipeptidylpeptidase-IV (DPP-IV) enzyme.

Hydrochlorides and hydrates of 1-[(3-cyanopyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-aminopiperidin-1-yl)xanthine, their preparation and their use as medicaments

본 발명은 1-[(3-시아노-피리딘-2-일)메틸]-3-메틸-7-(2-부틴-1-일)-8-(3-아미노-피페리딘-1-일)-크산틴의 염산과의 염 및 이의 에난티오머, 혼합물 및 수화물에 관한 것이다. The present invention relates to a process for the preparation of 1- [(3-cyano-pyridin-2-yl) methyl] -3-methyl- Yl) -xanthine with hydrochloric acid and its enantiomers, mixtures and hydrates thereof. 1-[(3-시아노-피리딘-2-일)메틸]-3-메틸-7-(2-부틴-1-일)-8-(3-아미노-피페리딘-1-일)-크산틴, 하이드로클로라이드, 수화물, 안정성, 흡습성, 디펩티딜펩티다제-IV 억제 활성 (3-amino-piperidin-l-yl) - (3-cyano-pyridin- Xanthine, hydrochloride, hydrate, stability, hygroscopicity, dipeptidyl peptidase-IV inhibitory activity

Cyclic hydrocarbon compounds for the treatment of diseases

The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Sustained release formulation of a peptide and a copolymer

This invention pertains to a sustained release complex, Compound (I), which comprises Compound (A), having formula (A) or a pharmaceutically acceptable salt thereof, and a copolymer comprising poly-(I)-lactic-glycolic-tartaric acid (P(I)LGT), wherein the amino group of said Compound (A) is ionically bound to a carboxyl group of the P(I)LGT. The present invention further pertains to a process for making said sustained release complex. Further still, the present invention is directed to a pharmaceutical composition comprising said sustained release complex and a pharmaceutically acceptable carrier(s).

Peptide antagonists of the calcitonin cgrp family of peptide hormones and their use

Oral pharmaceutical peptide products

Antagonist antibodies directed against calcitonin gene-related peptide and methods using same

The invention features methods for preventing or treating CGRP associated disorders such as vasomotor symptoms and/or headaches (e.g., migraine, cluster headache, and tension headache) by administering an anti-CGRP antagonist antibody. Compositions for use in the disclosed methods are also provided. Antagonist antibody G1 and antibodies derived from G1 directed to CGRP are also described.

Aralkyl-1,2-diamines having calcimimetic activity and preparation mode

The invention concerns compounds of general formula (I) wherein: X represents a SO2 or CH2 group; R1 represents a hydrogen or halogen atom or an alkoxy, aryl aralkyl group or an alkyl group substituted or not with one or several halogen atoms, n is equal to 0, 1 or 2, and R2 represents a hydrogen or halogen atom or an alkyl or alkoxy group, and their salt with a pharmaceutically acceptable acid. The invention also concerns the method for preparing said compounds, pharmaceutical compositions containing them and their use as modulator of CaSR activity and as medicine particularly designed for treating diseases or physiological disorders involving modulation of CaSR activity.

Patent NO2440241T3

Human procalcitonin and the preparation and use thereof

The invention relates to human procalcitonin and the preparation and use thereof. In particular, a process for preparing human procalcitonin is described wherein a gene coding for a polypeptide comprising the amino acid sequence of human procalcitonin is inserted into a vector; a host organism is transformed with this gene-containing vector; and the polypeptide expressed by the host organism is isolated. Furthermore the use of the polypeptides according to the invention, in particular as medicaments and diagnostic agents is described.

Extended recombinant polypeptides and compositions comprising same

Inhibitors for continuous activation for calcineurin

The object of the present invention is to provide a suppressant for neuronal cell death effective for various diseases which inhibits a constitutive active forming of calcineurin and has less side effect. An inhibitor of constitutive active forming of calcineurin, more specifically a drug which inhibits cleavage of calcineurin subunit A (CaNA) by calpain. Examples thereof include peptides having the amino acid sequence of FDGATAAARKEVIRNK (SEQ No. 1) and REESESVLTLKGLTPTG (SEQ No. 2).

Peptide antagonists of the calcitonin cgrp family of peptide hormones and their use

The embodiments provide a modified calcitonin gene-related peptide antagonist including an N-terminal fragment of modified calcitonin gene-related peptide or related protein family member where at least two residues of the N-terminal fragment are cysteine (Cys) and at least one amino acid comprises a non-threonine substitution of a threonine (Thr) residue; a central core where the central core comprises an oc-helix; and a C-terminal fragment of modified calcitonin gene -related peptide or related protein family member comprising a C-terminal amide and where at least one amino acid of the C-terminal fragment is phenylalanine (Phe), proline (Pro), tyrosine (Tyr) or hydroxyproline (Hyp) or pharmaceutically acceptable salt thereof, as well as compositions, including pharmaceutical compositions, comprising a subject peptide. The embodiments further provide treatment methods, including methods of treating a migraine, the methods generally involving administering to an individual in need thereof an effective amount of a subject peptide or composition.

Calcitonin products and therapies for treating inflammatory or degenerative diseases

Calcitonin products and therapies for treating inflammatory or degenerative diseases are disclosed herein. The pharmaceutical compositions disclosed herein include a first therapeutic agent that is calcitonin, in free or salt form; a second therapeutic agent selected from the group consisting of a protease inhibitor, an antibiotic, a non-steroidal anti-inflammatory agent, a COX-2 inhibitor and a steroidal anti-inflammatory agent other than glucocorticoid; and a pharmaceutically acceptable excipient, carrier or diluent. The methods disclosed herein for treating inflammatory or degenerative diseases in a subject include administering a therapeutically effective amount of calcitonin, in free or salt form, to the subject; and co-administering, as part of a combination therapy, a therapeutically effective amount of a second therapeutic agent selected from the group consisting of a protease inhibitor, an antibiotic, a non-steroidal anti-inflammatory agent, a COX-2 inhibitor and a steroidal anti-inflammatory agent other than glucocorticoid to the subject.

MICROPARTICLES FOR PULMONARY ADMINISTRATION

The invention concerns a biocompatible microparticle designed to be inhaled comprising at least an active principle and at least a layer coating said active particle which is the outer layer of said microparticle, said outer layer comprising at least a coating agent. The invention is characterised in that said microparticle has a mean diameter ranging between 1 mu m and 30 mu m, an apparent density ranging between 0.02 g/cm<3> and 0.8 g/cm<3> and it is obtainable by a method comprising essential steps which consist in bringing together a coating agent and an active principle and introducing a supercritical fluid, under agitation in a closed reactor.

Sustained-release peptide composition

Изобретение относится к пептидной композиции с замедленным высвобождением, представляющей собой соединение (I), содержащее соединение (А) формулы и полимер, содержащий лактидные звенья, гликолидные звенья и звенья винной кислоты – которые находятся в полимере при следующем соотнашении: лактидные звенья составляют от примерно 71% до примерно 73%, гликолидные звенья от примерно 26% до примерно 28%; и звенья винной кислоты от примерно 1% до 3%, а аминогруппы соединения (А) связаны ионной связью с карбоксильными группами кислотных звеньев полимера; макрочастицам соединения I, средний размер которых составляет от примерно 10 микрон до примерно 100 микрон; фармацевтической композиции с замедленным высвобождением и двум способам лечения различных болезней, включающим введение пациенту эффективного количества соединения А, или микрочастиц. 5 н. и 5 з.п. ф-лы, 1 ил. 494$ сс ПЧ сэ (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ "” 2 237 675. (51) МПК? 13) С2 С 07 К 7/06, С 070 241/04, А 61 К 9/16, 47/48 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 2002106820/04, 16.08.2000 (24) Дата начала действия патента: 16.08.2000 (30) Приоритет: 18.08.1999 Ш$ 60/149,649 (43) Дата публикации заявки: 20.09.2003 (45) Дата публикации: 10.10.2004 (56) Ссылки: КУ 2011377 СЛ, 30.09.1994. КИ 94016158 АЛ, 27.09.1995. КУ 2133252 С2, 20.07.1999. КУ 94046097/04, 10.07.2000. КИ 9511839504, 10.01.1998. М/О 94/015587 А, 21.07.1994. \О 95/04752 А, 16.02.1995. \/О 97/39738 А, 17.02.1997. ($ 5552520 А, 03.09.1996. (85) Дата перевода заявки РСТ на национальную фазу: 18.03.2002 (86) Заявка РСТ: 1$ 00/22464 (16.08.2000) (87) Публикация РСТ: М/О 01/12233 (22.02.2001) (98) Адрес для переписки: 129010, Москва, ул. Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е Е .Назиной (72) Изобретатель: МОРО Жак-Пьер (Ц$) (73) Патентообладатель: СОСЬЕТЕ ДЕ КОНСЕЙ ДЕ РЕШЕРШ Э Д'АППЛИКАСЬОН СЬЕНТИФИК С.А.С. (ЕК) (74) Патентный поверенный: Назина Елена ...

Oral Administration of Calcitonin

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2005 105 691 (13) A (51) ÌÏÊ A61K 47/18 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2005105691/15, 31.07.2003 (71) Çà âèòåëü(è): ÍÎÂÀÐÒÈÑ Àà (CH) (30) Ïðèîðèòåò: 01.08.2002 US 60/400,139 (43) Äàòà ïóáëèêàöèè çà âêè: 20.01.2006 Áþë. ¹ 02 (74) Ïàòåíòíûé ïîâåðåííûé: Âåñåëèöêà Èðèíà Àëåêñàíäðîâíà (86) Çà âêà PCT: EP 03/08498 (31.07.2003) Àäðåñ äë ïåðåïèñêè: 101000, Ìîñêâà, Ì.Çëàòîóñòèíñêèé ïåð., ä.10, êâ.15, "ÅÂÐÎÌÀÐÊÏÀÒ", È.À.Âåñåëèöêîé R U Ôîðìóëà èçîáðåòåíè 1. Ñïîñîá ââåäåíè , êîòîðûé çàêëþ÷àåòñ â ïåðîðàëüíîì ââåäåíèè ïàöèåíòó äî ïðèåìà ïèùè ôàðìàöåâòè÷åñêîé êîìïîçèöèè, ñîäåðæàùåé êàëüöèòîíèí â êîìáèíàöèè ñ îäíèì èëè íåñêîëüêèìè ïåðîðàëüíûìè àãåíòàìè äîñòàâêè. 2. Ñïîñîá ïî ï.1, â êîòîðîì ïåðîðàëüíîå ââåäåíèå ïðîâîäèòñ ïðèáëèçèòåëüíî çà 5-30 ìèí äî åäû. 3. Ñïîñîá ïî ï.1 èëè 2, â êîòîðîì óêàçàííà ôàðìàöåâòè÷åñêà êîìïîçèöè ñîäåðæèò à) àãåíò äë ïåðîðàëüíîé äîñòàâêè, êîòîðûì âë åòñ äèíàòðèåâà ñîëü N-(5õëîðñàëèöèëîèë)-8-àìèíîêàïðèëîâîé êèñëîòû, N-(10-[2-ãèäðîêñèáåíçîèë]àìèíî)äåêàíîâîé êèñëîòû, èëè N-(8-[2-ãèäðîêñèáåíçîèë]àìèíî)êàïðèëîâîé êèñëîòû, èëè ãèäðàò, èëè ñîëüâàò óêàçàííîé äèíàòðèåâîé ñîëè; è á) ïðèáëèçèòåëüíî 0,1-2,5 ìã êàëüöèòîíèíà; â êîòîðîé ñîîòíîøåíèå êîëè÷åñòâà àãåíòà äë ïåðîðàëüíîé äîñòàâêè, âûðàæåííîãî êàê ñîîòâåòñòâóþùåå êîëè÷åñòâî ñâîáîäíîé êèñëîòû, ê êîëè÷åñòâó êàëüöèòîíèíà íàõîäèòñ â ïðåäåëàõ ïðèáëèçèòåëüíî îò 10 äî ïðèáëèçèòåëüíî 250:1 ïî ìàññå. 4. Ïðèìåíåíèå ôàðìàöåâòè÷åñêîé êîìïîçèöèè äë ïîëó÷åíè ëåêàðñòâåííîãî ñðåäñòâà äë ëå÷åíè íàðóøåíè , ñâ çàííîãî ñ äåéñòâèåì êàëüöèòîíèíà; óêàçàííà êîìïîçèöè ñîäåðæèò êàëüöèòîíèí â êîìáèíàöèè ñ îäíèì èëè íåñêîëüêèìè àãåíòàìè ïåðîðàëüíîé äîñòàâêè, ïðè÷åì óêàçàííà êîìïîçèöè ââîäèòñ ïàöèåíòó ïåðîðàëüíî äî åäû. 5. Ïðèìåíåíèå ôàðìàöåâòè÷åñêîé êîìïîçèöèè ïî ï.4, â êîòîðîì ïåðîðàëüíîå ââåäåíèå ïðîâîäèòñ ïðèáëèçèòåëüíî çà 5-30 ìèí äî åäû. 6. Ïðèìåíåíèå ôàðìàöåâòè÷åñêîé êîìïîçèöèè ïî ï.4 èëè 5, â ...

GROWTH HORMON POLYPEPTIDES AND PROCEDURES FOR PREPARING AND USING THEREOF

Xanthine derivative, production and use thereof as a medicament

本发明是关于通式(I)的取代的黄嘌呤，其中R 1 至R 4 如权利要求1中定义，其互变异构体及立体异构物，其混合物，其前药及盐，所述化合物显示出有价值的药理学性质，特别是对于二肽基肽酶IV活性有抑制作用。

Adjunctive therapy with 25-hydroxyvitamin d

本發明揭示使用25-羥維生素D之輔助療法之方法、組合物及套組。該25-羥維生素D可與會增加低血鈣症風險之藥物及/或抗癌藥一起投與。該輔助療法可有效地治療及預防醫源性低血鈣症及/或繼發性副甲狀腺功能亢進，及延遲癌症發展及出現治療後骨相關事件之時間。

Antagonist antibodies directed against calcitonin gene-related peptide and methods using same

ORAL PHARMACEUTICAL PRODUCTS WITH PEPTIDES

Calcilytic compounds

Novel phosphate esters compounds and methods of using them as calcilytic compounds are provided.

Enteric solid oral dosage form of a bisphosphonate containing a chelating agent

Oral dosage forms of a bisphosphonate comprised of a safe and effective amount of a pharmaceutical composition comprising a bisphosphonate, a chelating agent, and, means for effecting delayed release of the bisphosphonate and the chelating agent in the lower gastrointestinal tract provide delivery of the pharmaceutical composition to the lower gastrointestinal tract of the mammal subject and pharmaceutically effective absorption of the bisphosphonate with or without food or beverages. The present invention substantially alleviates the interaction between bisphosphonates and food or beverages, which interaction results in the bisphosphonate active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, the present invention effects delivery of the bisphosphonate and the chelating agent to the lower GI tract, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies.

Peptides derived from human bplp protein, polynucleotides encoding peptides, and antibodies directed against peptides

【課題】ヒトＢＰＬＰタンパク質由来のペプチド、該ペプチドをコードするポリヌクレオチド及び該ペプチドに対する抗体の提供。 【解決手段】本発明は、塩基性のプロリンに富んだ涙液タンパク質（ＢＰＬＰ）の成熟生成物であるペプチド、又は該成熟生成物のペプチド誘導体若しくは模倣体に関し、前記ペプチド又はペプチド誘導若しくは模倣体は、金属−エクトペプチダーゼ、特にＮＥＰ及び／又はＡＰＮに対する阻害特性を提示する。本発明はまた、前記ペプチドをコードするポリヌクレオチド、及び前記ペプチドに対する抗体に関する。さらに、本発明は、ヒトＢＰＬＰタンパク質及びそれから誘導された阻害性ペプチド、ヒトＢＰＬＰタンパク質又はそれから誘導されたペプチドをコードするポリペプチド、並びにＢＰＬＰタンパク質又はそれから誘導されたペプチドに対する抗体の診断的及び治療的使用に関する。 【選択図】なし

Antagonist antibodies directed against calcitonin gene-related peptide and methods using same

Calcilytic compounds

本发明是以钙代谢化合物为特征。“钙代谢化合物”指能抑制钙受体活性的化合物。本发明同时叙述了钙代谢化合物抑制钙受体活性和/或在病人中获得有益治疗效果的用途;和可以用于获得其它钙代谢化合物的技术。

Hydrochlorides and hydrates of 1-[(3-cyanopyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-aminopiperidin-1-yl)xanthine, their preparation and their use as medicaments

本发明涉及1－[(3－氰基－吡啶－2－基)甲基]－3－甲基－7－(2－丁炔－1－基)－8－[3－氨基－哌啶－1－基]－黄嘌呤、与盐酸形成的盐，以及其对映体、其混合物及其水合物。

PHARMACEUTICAL PRODUCTS OF ORAL ADMINISTRATION PEPTIDES.

LA BIODISPONIBILIDAD DE AGENTES ACTIVOS PEPTIDOS QUE DEBEN ADMINISTRARSE POR VIA ORAL SE REALZA GRACIAS A UNA COMPOSICION FARMACEUTICA QUE PROPORCIONA UN OBJETIVO DE LIBERACION DEL PEPTIDO AL INTESTINO EN VIRTUD DE UN VEHICULO PROTECTOR RESISTENTE AL ACIDO QUE TRANSPORTA COMPONENTES DE LA INVENCION A TRAVES DEL ESTOMAGO. ESTA COMPOSICION INCLUYE UN ELEMENTO INCREMENTADOR DE ABSORCION DE UN AGENTE DE REDUCCION DE PH AL PH INTESTINAL LOCAL INFERIOR. SE LIBERAN TODOS LOS COMPONENTES JUNTOS DENTRO DEL INTESTINO CON EL PEPTIDO. THE BIODISPONIBILITY OF PEPTIDE ACTIVE AGENTS THAT MUST BE ADMINISTERED BY ORAL ROAD IS ENHANCED THANKS TO A PHARMACEUTICAL COMPOSITION THAT PROVIDES AN OBJECTIVE OF RELEASE OF THE PEPTIDE TO THE INTESTINE UNDER A PROTECTIVE VEHICLE RESISTANT TO THE CONVENTION OF THE INVENT. THIS COMPOSITION INCLUDES AN INCREASING ABSORPTION ELEMENT FROM A PH REDUCTION AGENT TO THE LOWER LOCAL INTESTINAL PH. ALL COMPONENTS ARE RELATED TOGETHER WITHIN THE INTESTINE WITH THE PEPTIDE.

Microparticles for pulmonary administration

The invention concerns a biocompatible microparticle designed to be inhaled comprising at least an active principle and at least a layer coating said active particle which is the outer layer of said microparticle, said outer layer comprising at least a coating agent. The invention is characterised in that said microparticle has a mean diameter ranging between 1 νm and 30 νm, an apparent density ranging between 0.02 g/cm3 and 0.8 g/cm3 and it is obtainable by a method comprising essential steps which consist in bringing together a coating agent and an active principle and introducing a supercritical fluid, under agitation in a closed reactor.

1 - [(3-Cyano-pyridin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8- (3-amino-piperidin-1-yl) hydrochlorides and hydrates -xanthine, its preparation and its use as medicines

Una sal hidrocloruro de 1-[(3-ciano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-amino-piperidin-1-il)-xantina,así como sus hidratos.

Oral Administration of calcitonin

Peptide antagonists of the calcitonin cgrp family of peptide hormones and their use cgrp

Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions

The present invention relates to substituted xanthines of general formula wherein R 1 to R 4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Peptides derived from human bplp protein, polynucleotides coding for said peptides and antibodies directed against said peptides

The invention relates to a peptide that is a maturation product of the Basic Prolin-rich Lacrinal Protein (BPLP) or a peptide derivative or a mimetic of said maturation product, wherein the peptide or peptide derivative or mimetic exhibits an inhibitory property against a metallo-ectopeptidase, especially NEP and/or APN. The present invention also relates to polynucleotides coding for said peptides and to antibodies directed against said peptides. Furthermore, the present invention relates to diagnostic and therapeutic uses of human BPLP protein and inhibitory peptides derived therefrom, polypeptides coding for human BPLP protein or peptides derived therefrom as well as antibodies directed against BPLP protein or peptides derived therefrom.

Medicinal mixtures for application to mucosa

7h-pyrido[3,4-d]pyrimidin-8-ones, their manufacture and use as protein kinase inhibitors

Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.

Enteric solid oral dosage form of bisphosphonate containing a chelating agent

双膦酸酯的口服剂型由安全有效量的药物组合物构成，所述药物组合物包含双膦酸酯、螯合剂和用于影响双膦酸酯和螯合剂在下肠胃道中延时释放的方法，所述双膦酸酯口服剂型向哺乳动物受试者的下肠胃道提供了药物组合物的递送，以及在有或没有食物或饮料的情况下对双膦酸酯的药物有效吸收。本发明充分减轻了双膦酸酯和食物或饮料间的交互作用，这种交互作用导致双膦酸酯活性成分不可用于吸收。因此，所得口服剂型可以在有或没有食物的情况下被服用。本发明还影响双膦酸酯和螯合剂向下肠胃道的递送，充分减轻了与双膦酸酯治疗相关的上肠胃道刺激。这些有益效果简化了以前复杂的治疗方法，并能导致患者对双膦酸酯治疗的顺从性增加。

Calcium receptor modulating agents

7h-pyrido[3,4-d]pyrimidin-8-ones, their manufacture and use as protein kinase inhibitors

本发明的目的是式(I)的化合物，它们的药用盐，对映异构体形式，非对映异构体和外消旋物，上述化合物的制备，包含它们的药物和它们的制备，以及上述化合物在控制或预防诸如癌症的疾病中的应用。

Compounds and methods

This invention relates to quinine and quinidine compounds which are ligands, in particular, antagonists, of the Calcitonin Gene-Related Peptide ('CGRP') receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CGRP, including, but not limited to, headaches, especially migraines; non-insulin dependent diabetes mellitus; cardiovascular disorders; chronic inflammation; endotoxic shock; arthritis; allergic rhinits; and asthma, all in mammals, by the use of quinine and quinidine CGRP receptor antagonists.

Xanthine derivatives, their preparation and their use as a drug.