baber/WOPTO huggingface dataset:
Patent JP-H08510197-A (JP)
Title: 飲料タンクまたは飲料樽に用いられるタップ栓ヘッド
Inventor: DEGENKOLBE HORST
IPC: B67D1/08
Filed: 1994-05-06
Abstract: (57)【要約】
飲料タンクまたは飲料樽に用いられるタップ栓ヘッドが、ハンドレバーによって操作可能なラム（６）と、飲料接続部（３）と、ガス状の圧力媒体のための接続部（２）と、タンク接続部（８）とを有している。本発明の構成では、タップ栓ヘッド内室内の圧力を危険なく除去するために、タップ栓ヘッド内室（１６）にリリーフ弁（９）が接続されている。
Patent JP-H11501272-A (JP)
Title: フィルムロール用の再使用可能な梱包箱
IPC: B65D85/67
Filed: 1995-03-02
Abstract: (57)【要約】
シート材料の重いロールを取り扱うための再使用可能な梱包箱である。梱包箱は、フレームとさらに発泡層を有する内部の固体支持フレームによってロールを支持する手段を備えている。全ての壁は装填された材料へのアクセスを容易とすべく調整可能である。梱包箱は多数積み重ねられ、空のときの容易な保管と輸送のために折り畳み可能である。
Patent JP-2000504129-A (JP)
Title: アルゴリズム無しで実行される人工神経回路網とその要素
IPC: G06N3/10
Filed: 1997-01-17
Abstract: (57)【要約】
人工神経回路網とその要素とをスプレッドシート環境内で構成し、模擬することは、訓練または操作のためにソフトウェアにベースを置くアルゴリズムを必要とすることがなく、ユーザーフレンドリーな神経回路網とすることができる。このような神経回路網は、スプレッドシート内で同時に訓練する神経回路網を、スプレッドシート内で自己訓練するために自己組織化できる神経回路網と、スプレッドシート内でデータを自主的に動かし、監視し、解析し、そして変更することのできる神経回路網とを有する、複合神経回路網と神経回路網システムとを形成するために、容易に縦続接続することができる。神経回路網は、デバイスプロトタイピングシステムを達成するために自己訓練神経回路網の形でお互いに縦続接続することもできる。
Patent JP-H11502241-A (JP)
Title: 耐加水分解性アラミド類
IPC: C08J5/18
Filed: 1996-02-28
Abstract: (57)【要約】
芳香族ジアミンおよび／または芳香族二酸モノマー単位上にアルキルおよび／またはアルコキシ置換基を少量有するアラミドポリマー類を開示する。上記アラミドポリマー類は、上記置換基を持たない同様なアラミド類に比較して向上した特性を示す。本明細書に記述するアラミド類は、例えば包装、ロープ、フィルターバッグまたは複合体などの製造で用いられる如きフィルムまたは繊維として用いるに有用である。本発明はまた上記ポリマー類の製造方法も包含し、この方法は、上記アラミドポリマー類から成形した繊維またはフィルムに熱処理を張力下で受けさせることを伴う。
Patent JP-2000506702-A (JP)
Title: 単一センサカラーカメラ
IPC: H04N1/48
Filed: 1997-03-14
Abstract: (57)【要約】
画像センサ、電子スチールカメラ、およびそれらに関連する方法が、画像処理に関して開示される。この方法は、色彩をサブサンプリングする方法で画像をサンプリングし、次いで、色彩をサブサンプリングした画素の値を処理することによって、シーンのフルカラー画像を構成するステップを包含する。本発明は、画素のジオメトリを、ストライプ状のカラーフィルタアレイおよび二重解像度再現の状況において、シャープネスを２つの直交するサンプリング方向で平衡させることを可能にする最適化をさらに包含する。
Patent JP-H11509988-A (JP)
Title: 半導体装置
IPC: H01L21/52
Filed: 1997-03-20
Abstract: (57)【要約】
半導体テバイス（１）、例えばパワーレーザダイオードロッドが支持部材上に固定されている。半導体デバイス（１）と支持部材（２）との間にはその膨張率α th が半導体デバイスのそれに適合され高い弾性率を有する応力補償層（３）が備えられてる。機械的応力は弾性ひずみ範囲で応力補償層（３）だけでほぼ完全に補償される。それにより高温耐性及び温度サイクル耐性の接合部を形成することができる。
Patent JP-2000508377-A (JP)
IPC: C23C16/34
Filed: 1997-01-15
Abstract: A cutting tool includes a substrate and a coating on the substrate. The coating includes a base adhesion layer that is on at least a portion of the substrate. A first intermediate adhesion layer, which includes boron and a first element, that is on the base adhesion layer. A second intermediate adhesion layer, which includes boron, the first element, and nitrogen, that is on the first intermediate adhesion layer. An outer adhesion layer, which includes boron and nitrogen preferably in the form of cubic boron nitride, that is on the second intermediate adhesion layer. A wear coating scheme wherein the innermost layer of the wear coating scheme is on the outer adhesion layer.
Patent JP-2000512739-A (JP)
Title: 車両用のナビゲーション装置
IPC: G08G1/0969
Filed: 1997-02-12
Abstract: (57)【要約】
選択可能な種々の群から成る、メモリにファイルされた目標データ（ａ，ｏ）と、選択された目的地（ｚ）と選択された群に対する目標データ（ａ，ｏ）との間の距離を求めるための装置とを備え、選択された群に属する目標データ（ａ，ｏ）は目的地（ｚ）からの求められた距離に依存して呼び出し可能でありかつ再生装置によって再生可能である、車両用のナビゲーション装置において、距離が前以て決められた距離限界値（ｒ）内にある目標データ（ａ）の再生を制御するための装置によって、再生される目標データの効果的な選別が実現される。
Patent JP-2000510274-A (JP)
IPC: G06F3/041
Filed: 1998-02-26
Abstract: A transmitter device is disclosed for use with a conventional pen in which the ultrasound transmitter is a cylindrical element lying coaxial with the pen and adjacent to its tip, and a jointed eraser structure. Conventional triangulation techniques are used to track the position and motion of a writer or eraser. An encoding facility associated with the pen provides the ability to distinguish whether the pen is used for marking or an as erasing implement, as well as determining the nature or character of written line width or eraser swath. A data stream thus generated can be used in a variety of ways, such as for example, to feed information into the memory of a digital computer, and/or to feed information for transmission to remote stations.
Patent JP-2000510900-A (JP)
Title: コポリエステルの製法
IPC: C08K3/24
Filed: 1997-05-13
Abstract: (57)【要約】
５５ないし９５モル％のアルキレンテレフタレート単位と、５ないし４５モル％のアルキレンイソフタレート単位とを含有するコポリエステルを製造する方法は、最終のコポリエステルの重量に対して１０ないし１５０ｐｐｍのチタン原子を触媒として、同じく１０ないし１００ｐｐｍのリン原子を安定剤として含む反応混合物を使用する。このコポリエステルは色特性が良好で、包装用途、特に食品および飲料の包装用に使用するフィルムを成型するのに最適である。
Patent JP-2001519860-A (JP)
Title: 抄紙機またはその同等物の織物の洗浄方法
IPC: D21F1/32
Filed: 1998-04-07
Abstract: (57)【要約】
抄紙機またはその同等物における織物の洗浄方法であって、該方法においては洗浄流体を使用して織物を洗浄する。この方法においては、織物から除去された液体量は少なくとも１点において測定され、この液体量測定に基づいて、織物に使用される洗浄用薬剤の投与量が調節される。
Patent JP-2000511370-A (JP)
Title: セルラ無線通信システムにおける干渉除去組合せおよびダウンリンク・ビームフォーミング
IPC: H04B7/26
Filed: 1997-05-27
Abstract: (57)【要約】
最近、干渉除去組合せ技術が提案されており、これは、Ｃ／Ｉ制限された環境においてアップリンクの性能を相当上昇させることができる。このＩＲＣ技術のもう１つの関心のある特性は、Ｃ／Ｉ性能が受信信号間の相関が増大するときに劣化しないことである。ＩＲＣ技術のこの特徴を本発明で利用することにより、アンテナ間の間隔の低減を可能にする。本発明の別の側面によれば、ダウンリンクの性能は、ビームフォーミング技術を使用して基地局送信を所望の移動局の方にステアリングすることにより改善する。このようにして、ダウンリンクの性能は、ビームフォーミング技術を使用して、ＩＲＣ技術を使用してアップリンクを改善したのと同じ程度にまで改善する。これにより、システム設計者は、アップリンク性能を改善することに関連したシステム設計において、もっと十分に変形例を利用することができる。
Patent JP-2002511848-A (JP)
Title: エラスターゼのオリゴペプチド阻害剤およびその製造方法
IPC: A61P1/02
Filed: 1998-04-27
Abstract: (57)【要約】
本発明は、白血球エラスターゼを有効に阻害する、エラスターゼのオリゴペプチド阻害剤に関する。本阻害剤は、分子のＮ−末端部分に置換リジンが組み込まれたテトラないしペンタペプチドのイソブチルアミドである。この２塩基性アミノ酸はα−およびε−アミノ基の双方において高級飽和酸またはω−カルボキシアルカノール残基で選択的に置換される。これら化合物の１種においては、ε−アミノ基はアシル−アラニンでアシル化される（ここで、アシルは高級飽和酸を意味する）。本発明の化合物は主に歯科診療で使用される医薬製剤の有効化合物である。
Patent JP-2001527457-A (JP)
Title: 中心位置決め装置
IPC: A61F2/36
Filed: 1999-03-19
Abstract: (57)【要約】
股関節置換手術のために患者の大腿骨に埋植されるプロテーゼ大腿骨ステム２用の中心位置決め装置１が提供される。この中心位置決め装置１は凸状湾曲をもった内面２２を備えた細長い環状体１４を有する。この凸状湾曲は、中心位置決め装置１の材料の厚さがフープ荷重の効果を減少させている領域において大腿骨ステム２の表面と点接触または環状接触が行われるのを確実にする。この中心位置決め装置１は概ね矩形状の断面を有し、骨内腔の前面、後面、内側面及び外側面での配置のために当該矩形状断面の側面３０から４つのフィン２０が延出している。
Patent MX-160762-A (MX)
Inventor: GUEUSSIER ANDRE
IPC: C22C38/60
Filed: 1984-03-14
Abstract: The invention relates to the methods for the preparation of steels with high machinability, comprising globular inclusions which allow for high cutting speeds by means of carbide tools. The method according to the invention consists of introducing into a liquid steel which has been deoxidized carefully with aluminum, and desulfurized, additions of calcium and sulfur, carried out by a cored wire, the contents obtained being from 20 to 100 ppm calcium and 150 to 500 ppm sulfur. The steels prepared under this method offer a particular aptitude for high speed machining with the aid of carbide cutting tools.
Patent NZ-199536-A (NZ)
Title: Combustion gas powered fastener driving tool
Inventor: NIKOLICH M
IPC: B25C1/08
Filed: 1982-01-20
Abstract: A fastener applying tool is disclosed, powered by the gases produced from internal combustion of a fuel and air mixture. A piston connected to a fastener driver is slidably mounted within a cylinder to move reciprocally downwardly and upwardly through a driving and a return stroke. A combustion chamber is formed at the upper end of the cylinder. A compression chamber is formed at the lower end of the cylinder. A spark plug powered by a piezo-electric firing device, is located within the combustion chamber. The combustion chamber features a set of fan blades driven by an electric motor which is continuously in operation when the tool is in use. A main valve mechanism actuated by a set of lifting rods which are moved upwardly and downwardly when the tool is moved toward and away from the workpiece, is used to control the flow of fresh air through the combustion chamber. When the combustion chamber is isolated from the atmosphere and the fuel and air are thoroughly mixed, the spark plug is fired to explode the fuel and air mixture and force the piston through its driving stroke. The rapid discharge of combustion gases at the end of the driving stroke produces a thermal vacuum within the combustion chamber. Additional air supplied to the lower face of the piston from the atmosphere forces the piston through its return stroke.
Patent NZ-221422-A (NZ)
Title: Train control system - double handshake communications
Inventor: CORRIE J D
IPC: B61L27/00
Filed: 1987-08-12
Abstract: A railway vehicle control system comprises a railway track (1) and a plurality of transponders (N, N+1, N+2) at predetermined positions along the track. A railway track (2) moves along the track, the vehicle having means (20, 21) for detecting each of the transponders. A control location has means (4, 5, 6, 7, 7a) for periodically transmitting vital safety signalling information to the vehicle via a radio link. In response to detection of one of the transponders, the vehicle sends a first message via the link to the control location and in response to reception of the first message by the control location, the vital safety signalling information is sent a first time from the control location to the vehicle via the link, then from the vehicle to the control location via the link and then a second time from the control location to the vehicle via the link.
Patent NZ-222922-A (NZ)
Title: Morpholinoethylester of mycophenolic acid and derivatives and pharmaceutical compositions
Inventor: NELSON PETER HAROLD
IPC: C07D307/88
Filed: 1987-12-15
Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or -C(O)R, where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents. <CHEM>
Patent NZ-224736-A (NZ)
Title: Leuconostoc polysaccharide compositions for use as quality improvers for food
Inventor: PUCCI MICHAEL J
IPC: A23L29/269
Filed: 1988-05-20
Abstract: Novel dried compositions containing polysaccharides (dextrans and levans) derived using a Leuconostoc to ferment sucrose to produce the polysaccharides are described. In particular, dried compositions incorporating milk solids or other drying aids to facilitate drying and rehydration of the polysaccharides are described. The compositions are useful as quality (e.g. texture, stability or thickness) improvers for foods.
Patent NZ-229081-A (NZ)
Title: (t-pa) tissue plasminogen activator, streptokinase and urokinase analogues with altered glycosylation
Inventor: ANDERSON STEPHEN
IPC: C12N1/19
Filed: 1989-05-11
Abstract: A fibrinolytically active amino acid sequence variant of a plasminogen activator is prepared that has one or more sites that are not glycosylated in the native molecule but are glycosylated in the variant. DNA sequences can be prepared that encode the variants, as well as expression vectors incorporating the DNA sequences, and host cells transformed with the expression vectors. The variants may be used in a pharmaceutical preparation to treat a vascular disease or condition in patients.
Patent NZ-232044-A (NZ)
Title: Production of ceramic composites containing a boride and a metal
Inventor: CLAAR TERRY DENNIS
IPC: C04B35/65
Filed: 1990-01-08
Abstract: This invention relates generally to a novel method of manufacturing a composite body and to novel products made thereby. More particularly, the invention relates to a method of producing a self-supporting body comprising one or more boron-containing compounds, e.g., a boride or a boride and carbide, by reactive infiltration of molten parent metal into a bed or mass containing boron carbide, and, optionally, one or more inert fillers and permitting residual or excess parent metal, to remain bonded to the formed self-supporting body. Excess metal is used to form a bond between the reactively infiltrated body and another body (e.g., a metal or a ceramic body).
Patent NZ-234879-A (NZ)
Title: Production of iminodiacetonitrile,
Inventor: KOENIG KARL ERIC
IPC: C07C227/26
Filed: 1990-08-13
Abstract: An improved process is provided for producing iminodiacetonitrile by contacting ammonia, formaldehyde and hydrogen cyanide, or hexamethylenetetramine, formaldehyde and hydrogen cyanide in a reaction medium, the improvement which comprises the further steps of thereafter adjusting the pH of the reaction medium to a pH between about 5.5 and about pH 10 and heating the reaction medium to an elevated temperature for a sufficient time to convert by-products in the reaction medium to iminodiacetonitrile.
Patent NZ-238901-A (NZ)
Title: Suspension-producing pharmaceuticals
Inventor: ZEMA MARCO
IPC: A61K9/10
Filed: 1991-07-10
Abstract: PCT No. PCT/EP91/01268 Sec. 371 Date Mar. 3, 1992 Sec. 102(e) Date Mar. 3, 1992 PCT Filed Jul. 4, 1991 PCT Pub. No. WO92/00731 PCT Pub. Date Jan. 23, 1992.The invention provides a solid pharmaceutical composition for addition to water to produce a suspension of a drug comprising (a) a drug which is substantially water-insoluble or microencapsulated; (b) a thickening or suspending agent; (c) a pharmaceutically acceptable acid; (d) a pharmaceutically acceptable carbonate or bicarbonate; characterised in that the weight ratio of c+d:b is from 1:1.5 to 1:15 and the amount of c+d is sufficient to obtain rapid hydration of the thickening or suspending agent (b) when the composition is mixed with water such that a homogeneous suspension of the drug is obtained within 30 seconds. A method for preparing the composition is also described.
Patent NZ-239587-A (NZ)
Title: Process for polymerising alpha-olefins
Inventor: HAVAS LASZLO
IPC: C08F2/34
Filed: 1991-08-29
Abstract: Polymerisation in a gas phase polymerisation reactor comprises contacting gaseous reaction mixt., contg. alpha-olefin, with a catalyst of chromium oxide associated with a granular support and activated by heat treatment, the reactor fed with alpha-olefin and catalyst at constant rates. Pref. alpha-olefin feed rate is constant using a flow regulating system, partial pressure pref. 20% min. - 40% max mixt. pressure. The total reaction mixt. pressure is predetermined min. - max. by introducing inert gas of good heat exchange capacity, (1.5-2.5 MPa), max. variations below 0.3 MPa. A chain limiter is introduced for constant partial pressure
Patent NZ-245174-A (NZ)
Title: Pyridine or piperazine substituted cycloalkene and cycloalkane derivatives and pharmaceutical compositions
Inventor: CAPRATHE BRADLEY WILLIAM
IPC: A61K31/435
Filed: 1992-11-18
Abstract: 1,3-Substituted cycloalkenes and cycloalkanes of Formula I Z-CH2-Y I wherein Z is <CHEM>  Y is <CHEM> wherein the meaning of R and m are provided in the description, are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
Patent NZ-249074-A (NZ)
Title: An apparatus and method for recycling an upper surface of an asphalt road or pavement or the like has or uses rupturing devices and heating and mixing devices free thereof and pressing devices to provide a recycled pavement surface
Inventor: WILEY PATRICK C
IPC: E01C7/06
Filed: 1993-02-19
Abstract: PCT No. PCT/CA93/00069 Sec. 371 Date Aug. 22, 1994 Sec. 102(e) Date Aug. 22, 1994 PCT Filed Feb. 19, 1993 PCT Pub. No. WO93/17185 PCT Pub. Date Sep. 2, 1993.A process for recycling an asphaltic surface. The process comprises: (a) providing an asphaltic surface having an upper surface for recycling; (b) rupturing the upper surface to a depth of at least about 1.5 inches to provide a ruptured upper surface; (c) heating and mixing the ruptured upper surface on the asphalt surface to a temperature in the range of from about 100 DEG  to about 350 DEG  F. to produce a heated, ruptured upper surface which is substantially free of moisture; and (d) pressing the heated, ruptured upper surface to provide a recycled pavement surface. An apparatus adapted for carrying out the process is also described.
Patent NZ-263030-A (NZ)
Title: Peptides inducing cytotoxic t-lymphocyte responses to hepatitus b virus (hbv)
Inventor: CHISARI FRANCIS V
IPC: C07K7/06
Filed: 1994-02-25
Abstract: Peptides are used to define epitopes that stimulate HLA-restricted cytotoxic T lymphocyte activity against hepatitis B virus antigens. The peptides are derived from regions of HBV envelope, and are particularly useful in treating or preventing HBV infection, including methods for stimulating the immune response of chronically infected individuals to respond to HBV antigens. <IMAGE>
Patent NZ-263991-A (NZ)
Title: Ear microphone with background noise attenuation
Inventor: NORRIS ELWOOD G
IPC: H04R5/027
Filed: 1994-04-01
Abstract: An ear piece device (10) configured for being supported in the ear and providing a microphone (25) which is within a housing (11). A microphone element (28) is coupled within a casing (25). A support gasket (51) formed of acoustical absorbing materials is interposed around the microphone casing (25) and forms a bridge between the housing (11) and the microphone casing (25). A speaker element (13) may be included within the ear device (10) and can be decoupled acoustically so as to avoid feedback. This device (10) can operate with full duplex and enable hands free communication and direct voice command by user through computer modems, telephone networks and other communication systems.
Patent NZ-280577-A (NZ)
Title: Ophthalmic lens treatment; contact lens disinfecting device, gas liberated during disinfection process; details of lens container and cap
Inventor: ALVORD LARRY ALLEN
IPC: G02C13/00
Filed: 1995-12-01
Abstract: An ophthalmic lens disinfection apparatus, including a container and a mating cap, the apparatus having an improved seal and vent means for venting gas generated within the apparatus. The vent means is an integral part of the disinfection apparatus which allows venting of gas when internal pressure increases, while maintaining a seal which is substantially gas and liquid- impermeable at other times. The seal is defined by the interference mating of a flexible periphery on a container with a rigid mating rim on a cap. The apparatus is particularly useful in the disinfection of contact lenses with hydrogen peroxide in which the excess peroxide is decomposed into water and oxygen. <IMAGE>
Patent NZ-502148-A (NZ)
Title: Interconnecting of tubular members with connector having mouth portion, seal and first and second securing members to prevent longitudinal movement of tubular members relative to connector
Inventor: DAVIDSON PAUL
IPC: F16L37/084
Filed: 1998-06-01
Abstract: A connector (1) is disclosed for connecting together at least two tubular members (3) includes a body (7) having tubular mouth portions, each receiving one of said tubular members. (Only one half of the connector is shown). At least one of the mouth portions is provided with means for connecting the body to a tubular member, the connection means comprising sealing means (17) for sealing the body against the tubular member and securing means for preventing relative longitudinal movement between said body and said tubular member. The securing means comprise a first securing member (25) for engagement with the tubular member and being deformable between a tubular member engaging position and a position allowing said first member to be readily moved along the tubular member, and a second securing member (31) being for holding the first securing member in its tubular member engaging position. The body and first and second securing members are adapted to co-act to prevent, in use, relative longitudinal movement between said first securing member and said body. A connection assembly, which includes a plurality of connectors of the invention, is also described.
Patent NZ-502862-A (NZ)
Title: Optically pure camptothecin analogues, optically pure synthesis intermediate and method for preparing same
Inventor: CAZAUX JEAN-BERNARD
IPC: A61K31/435
Filed: 1998-08-07
Abstract: An analogue of camptothecin characterized in that it possesses one of the general formulae (I) or (II).  These analogues of camptothecin can be used for producing antitumoral, antiviral or antiparasitic medicines.
Patent NZ-503062-A (NZ)
Title: Preparing dihydrate form of L-tartaric acid without isolating (3aR)-2,3a,4,5,6,7-hexahydro-2-methyl-3a-(phenylmethyl)-3H-pyrazolo[4,3-c]pyridin-3-one whereupon the appropriate form is crystallised upon cooling
Inventor: POST RONALD JAMES
IPC: C07D/
Filed: 2000-02-25
Abstract: A process for preparing a L-tartrate salt of formula XX comprising the following steps: (a) reacting 4-oxo-piperidinecarboxylic acid methyl ester hydrochloride with di-t-butyl-dicarbonate and triethylamine in isopropyl ether to form 4-oxo-1,3-piperidinedicarboxylic acid 1-(1-dimethylethyl) 3-methy1 ester; (b) reacting 4-oxo-1,3-piperidinedicarboxylic acid 1-(1-dimethylethyl) 3-methyl ester with benzyl bromide and potassium carbonate in tetrahydrofuran to form 4-oxo (phenylmethyl)-1,3-piperidinedicarboxylic acid 1-(1-dimethylethyl) 3-methyl ester; (c) reacting 4-oxo-(phenylmethyl)-1,3-piperidinedicarboxylic acid 1-(1-dimethylethyl) 3-methyl ester with methylhydrazine in acetic acid and methyl-t-butyl ether to form 2,3a,4,5,6,7-hexahydro-2-methyl-3-oxo-3a-(phenylmethyl)-5H-pyrazolo[4,3-c]pyridin-5-carboxylic acid 1,1-dimethylethyl ester; and (d)  reacting 2,3a,4,5,6,7-hexahydro-2-methyl-3-oxo-3a-(phenylmethyl)-5H-pyrazolo[4,3-c]pyridin-5-carboxylic acid 1.1-dimethylethyl ester with trifluoroacetic acid to form (3aR)-2,3a,4,5,6,7-hexahydro-2-methyl-3a-(phenylmethyl)3H-pyrazolo[4,3-c]pyridin-3-one; (e) reacting (3aR)-2,3a,4,5,6,7-hexahydro-2-methyl-3a-(phenylmethyl)-3H-pyrazolo[4,3-c]pyridin-3-one with L-tartaric acid in acetone and water to form L-tartrate salt of the formula XX.
Patent NZ-504024-A (NZ)
Title: Quinoline- or quinazoline-containing alpha-ketoamide cysteine and serine protease inhibitors
Inventor: SHAM KELVIN C
IPC: C07D401/12
Filed: 1998-10-07
Abstract: A compound having the Formula I, wherein: X is CH, N, or CQ1, with the proviso that when X is CQ1, at least one of Q or Q1 is H; R is H, alkyl, arylalkyl, heteroalkyl, heteroarylalkyl, alkoxyalkyl, a side chain of a naturally occurring amino acid, or (CH2)n NH-L, the alkyl, arylalkyl, heteroalkyl, or heteroarylalkyl groups being optionally substituted; R1 is H, halogen, cyano, nitro, -S(.=O)2 OH, hydroxyl, alkyl, alkoxy, hydroxymethyl, alkoxymethyl, arylalkyl, carboxyl, alkoxycarbonyl, alkylcarbonyloxy, haloalkyl, N(RR3), or acyl; Q is H, lower alkyl, cycloalkyl, hydroxyl, alkoxy, halogen, arylalkyl, arylalkeny, arylalkynyl, aryl, heteroaryl, heteroalkyl, cycloalkyl, S-R, S(.=O)R, S(.=O)2 R, N(RR3), or NHS(.=O)2 R, the arylalkyl, arylalkenyl, arylalkynyl, aryl, heteroaryl, and heteroalkyl groups being optionally substituted; Q1 is the same as Q; Z is COCONH-R7 ; R7 is K, -A-N(R8)-G, -O-A-N(R8)-G, -A-SO2 N(R8) (R9), or -O-A-SO2 N(R8) (R9); K is alkyl, alkenyl, alkynyl, cycloalkyl, heteroalkyl, heteroaryl, aryl, arylalkyl, heterocycloalkyl, alkoxy, alkoxyalkyl, arylalkyloxy, or N(RR3), the K groups being optionally substituted; With the proviso that when R7 is K, then Q is selected from the group consisting of optionally substituted arylalkenyl and optionally substituted arylalkynyl; and with the further proviso that when K is alkyl, then X is not CH when Q is optionally substituted arylalkynyl; Also described as a composition for inhibiting a serine protease or a cysteine protease comprising the compound described above and a pharmaceutically acceptable carrier. The compound of formula I is useful for inhibiting a serine protease or cysteine protease.